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112 Cards in this Set
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Cardiovascular drugs - includes medication affect heart and blood vessels and anticoagulant and antiplatelet agents that prevent clotting - Drugs: Cardiac glycosides, antiarrhythmic agents, antilipemic agents, antihypertensives, vasodilators, vasoconstrictors, anticoagulants, platelet inhibitors, and thrombolytic agents |
Congestive Heart Failure (CHF) Definition: CHF is a condition in which the heart is unable to pump sufficient blood to the tissues of the body - occurs when the heart cannot pump sufficient blood to the tissues of the body. = causes the accumulation of blood in the heart, lungs, and veins of the lower extremities. = This congestion may cause formation of blood clots in the veins, pulmonary edema, and cardiac arrhythmias. |
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Congestive Heart Failure (CHF) - releasing norepinephrine and epinephrine, = leading to vasoconstriction = increased heart rate and force of contractions. In this way the body tries to pump blood throughout the body and relieve the congestion. The kidneys are then affected since sodium and water are retained which causes an increased blood volume and blood pressure. |
Congestive Heart Failure (CHF) Drug classes: cardiac glycosides, diuretics, ACE (angiotensin converting enzyme) inhibitors, ARB (angiotensin receptor blockers), alpha/beta adrenergic blockers, vasodilators. |
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Cardiac Glycosides (Digoxin) - Occur widely in nature or can be prepared synthetically - Act directly on the myocardium to increase the force of myocardial contractions (without increasing oxygen consumption) thereby increasing cardiac output = Digoxin is the only clinical drug currently used in the cardiac glycoside family - Used primarily in treatment of heart failure in patients with symptoms that persist after optimization of treatment with an ACE inhibitor, a beta-adrenergic blocker, and/or a diuretic |
Diuretics - also affect blood vessels, and reduce blood pressure |
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Cardiac Glycosides - sometimes used alone or in conjunction with other meds (such as calcium channel blockers) to SLOW the ventricular response in patients with atrial fibrillation or flutter - Act directly on the myocardium to increase the force of myocardial contractions (without increasing oxygen consumption) thereby increasing cardiac output = heart beasts slower, heart size shrinks and concurrent diuretic therapy decreases edema (as a result of increased efficiency) - also lower norepinephrine levels (which are elevated in heart failure and are toxic to failing heart) |
In patients with heart failure, - heart fails to adequately pump nutrients and oxygen to body tissues = since heart is failing, body attempts to compensate by retaining salt and fluid (may result in both pulmonary and peripheral edema) = heart increases in size (compensate for increased work load) Symptoms of heart failure: - fatigue, weakness, dyspnea, cyanosis, increased heart rate, cough, and pitting edema *small % of patients with heart failure will develop atrial fibrillation = 2 disabling and devastating complications of atrial fibrillation= ischemic stroke and systemic embolism |
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Most commonly used Cardiac Glycosides = digitalis products: digoxin (Lanoxin) the only product still marketed for clinical use because it can be administered orally and parenterally and has immediate duration of action - very narrow margin between effective therapy with digoxin and dangerous toxicity. = careful monitoring of cardiac rate and rhythm with EKG, cardiac function, side effects, and serum digoxin levels is required to determine therapeutic maintenance dose - check apical pulse before administering digoxin, if apical pulse rate less than 60, digoxin may need to be withheld until physician is consulted (action taken should be documented) |
Modification of dosage based on individual requirements and response as determined by general conditions, renal function, and cardiac function, monitored by EKG - ** digoxin dosage adjustment required when changing from tablets or IM therapy to elixir or IV therapy. ** |
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Cardiac glycosides (digoxin) toxic side effects (should be reported to physician immediately) - anorexia, nausea, and vomiting (early signs of toxicity) - abdominal cramp, distention, and diarrhea - headache, fatigue, lethargy and muscle weakness - vertigo, restlessness, irritability tremors and seizures - visual disturbances (blurring, diplopia- double vision) or halos - cardiac arrhythmias of all kinds (esp bradycardia - rate less than 60) - Electrolyte imbalance, esp potassium (either hyperkalemia or hypokalemia can cause arrhythmias) - Insomnia, confusion, and mental disorders, especially with older adults |
Treatment of digoxin toxicity - discontinuing the drug immediately (usually sufficient) - monitoring electrolytes for hyperkalemia, hypokalemia, hypomagnesemia, and hypercalcemia - drugs such as atropine for symptomatic bradycardia - Digoxin-specific Fab fragments (DigiFab) as an antidote in life-threatening toxicity |
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Precautions or Contraindications of digoxin - severe pulmonary disease - hypothyroidism - acute myocardial infarction, acute myocarditis and severe heart failure - impaired renal function; hypokalemia, and hypomagnesemia - arrhythmias not caused by heart failure - pregnancy and lactation - high doses in older adults |
Interactions of digoxin may occur with - antacids, cholestyramine, neomycin, and rifampin (reduce absorption of digoxin; administer far apart) - diuretics, calcium, and corticosteroids (can increase chance of arrhythmias) - macrolides and antiarrhythmics (esp quinidine and verapamil; may potential digoxin toxicity) - Adrenergics (epinephrine, ephedrine and isoproterenol; increase risk of arrhythmias) |
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Patient education on digoxin - recognition and immediate reporting of side effects - holding med, if any side effects occur, until physician can be consulted - avoid taking other meds at same time without physician approval - avoid all OTC meds, esp antacids and cold remedies - avoid abrupt withdrawal after prolonged use; must be reduced gradually under physician supervision - Checking heart rate (pulse) on a regular basis |
Antiarrhythmic Agents - “Arrhythmia" refers to any change from the normal sequence of electrical impulses of the heart - Antiarrhythmic agents act in different ways to suppress various types of cardiac arrhythmias = Atrial or ventricular tachycardias, atrial fibrillation or flutter, and arrhythmias that occur with digoxin toxicity or during surgery and anesthesia |
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Antiarrhythmic agents - electrical impulses may happen too fast, too slowly or erratically - causing heart to beat too fast (tachycardia), - too slowly (bradycardia) or - erratically (fibrillation) choice of particular agent depends on type of arrhythmia, frequency, cardiac, renal, or other pathological condition; and current signs and symptoms |
Role of health care practitioner is critical - accurate and timely reporting of vital signs, pertinent observations regarding effectiveness of meds and adverse side effects, and modifications of precipitating causes = knowledge of drug action and effects with good judgment |
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*keep in mind that most drugs given to counteract arrhythmias have potential for lowering blood pressure and slowing heartbeat = important to alert for signs of HYPOTENSION and BRADYCARDIA = could lead to cardiac arrest - although antiarrhythmics commonly slow heart rate, there are exceptions: (e.g. procainamide and quinidine - may cause tachycardia) - when other drugs administered concomitantly, cardiac effects may be additive or antagonistic - antiarrhythmic agents can worse existing arrhythmias or cause new arrhythmias = careful monitoring essential |
Arrhythmia detection or monitoring - EKG rhythm strips - 24h Holter monitorings - electrolyte surveillance (esp for disorders of potassium and magnesium - importnat for patients on antiarrhythmic agents) - non drug therapy can include insertion of a pacemaker or an automatic implantable cardioverter-defibrillator (AICD) = AICD has been widely accepted as most effective treatment for patients with life-threatening ventricular tachycardia or fibrillation and for patients who have survived a cardiac arrest and prevent sudden death in certain patients with heart failure. |
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Antiarrhythmic Agents Adenosine (Adenocard) - Injectable antiarrhythmic agent - Multiple electrophysiologic activities = Restores normal sinus rhythm in paroxysmal supraventricular tachycardia (PSVT) by slowing conduction time through the atrioventricular (AV) node = also has Vasodilatory, antiadrenergic, and negative chronotropic (decrease in rate) properties that act to decrease cardiac oxygen demand |
Antiarrhythmic Agents Adenosine is equal in effectiveness to diltiazem or verapamil in converting PSVT but is less likely to cause hypotension. Common Side Effects: flushing, lightheadedness, headache, dyspnea, and chest pressure Contraindicated in patients with second-or third-degree heart block or symptomatic bradycardia (unless a functioning artificial pacemaker is present) |
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Antiarrhythmic Agents Amiodarone (Cordarone) - Oral and injectable antiarrhythmic agent approved for treatment of refractory life-threatening ventricular arrhythmias - Widely used for preventing recurrence of atrial fibrillation (despite its problematic organ toxicity profile and black box warning) - considered a broad-spectrum antiarrhythmic with multiple and complex electrophysiological effects - also relaxes both smooth and cardiac muscle = cause decrease in coronary and peripheral vascular resistance and decrease in systolic pressure |
Antiarrhythmic Agents Side effects of Amiodarone (some which are severe and potentially fatal, but may be less of a problem with lower doses (e.g 200-400 mg per day) - pulmonary fibrosis - cardiac arrhythmias (induction or worsening of heart failure and hypotension) - hepatitis (rare) - hyperthyroidism or hypothyroidism - neurotoxicity (remor, peripheral neuropathy, paresthesias [numbness, tingling, esp in extremities]) - visual disturbances; optic neuropathy and or neuritis (may progress to permanent blindness) - dermatological reactions, esp photosensitivity (avoid exposure, wear protective clothing) |
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Antiarrhythmic Agents Precautions or contraindications for amiodarone - patients with a second-or third-degree heart block, marked sinus bradycardia due to severe sinus node dysfunction, and when bradycardia has caused syncope (unless a functioning artificial pacemaker is present); cardiogenic shock - patients with thyroid disease (due to large amount of iodine contained in amiodarone) - iodine hypersensitivity - older adults (more susceptible to thyrotoxic and neurotoxic adverse effects |
Antiarrhythmic Agents Interactions with amiodarone are numerous and significant - certain fluoroquinolones, macrolide antibiotics, systemic azole antifungals (AQ prolongation) - Warfarin (can result in serious or fatal bleeding if warfarin dose is not reduced; effect may persist for months after discontinuation) - certain antiarrhythmics, digoxin, and phytoin (amiodarone increases serum concentrations of these drugs) - protease inhibitors and grapefruit juice (increase amiodarone concentrations); beta-blockers, calcium channel blockers, and lidocaine (additive adverse cardiac effects) - Cholestyramine, phenytoin, and rifampin (serum concentrations of amiodarone are decreased, reducing its pharmacological effect) |
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Beta-Adrenergic Blockers Antiarrhythmic Agents - Antiarrhythmics that combat arrhythmias by inhibiting adrenergic (sympathetic) nerve receptors Ex: propranolol (Inderal) are antiarrhythmics (combat arrhythmias by inhibiting adrenergic (sympathetic) nerve receptors) - the action is complex, results can include a membrane-stabilizing effect on heart. - propranolol is a nonselective beta-blocker, = effective in management of some cardiac arrhythmias and less effective with others = also used to treat hypertension and some forms of chronic angina (can block the beta2receptors in lungs = can lead to bronchospasm) - low doses of metoprolol (Lopressor): selective beta1-antagonist, may be used with caution in patients with lung conditions that cause bronchospasm |
Beta1receptors are found primarily in heart and when stimulated, cause increase in rate and force contraction - found primarily in lungs (when stimulated cause relaxation of bronchodilation of airways), and blood vessels (when stimulated cause vasodilation) *One heart, Two lungs - the class of beta-blockers would decrease rate and force of contraction of heart and if nonselective may also cause bronchospasm and mild vasoconstriction of blood vessels |
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Antiarrhythmic Agents Side effects of beta-blockers (esp patients over 60 years old and more commonly with IV administration of drug) - hypotension with vertigo and syncope - bradycardia (with rarely heart block and cardiac arrest) - CNS symptoms (usually with long-term treatment with high doses), include dizziness, irritability, confusion, nightmares, insomnia, visual disturbances, weakness, sleepiness, lassitude or fatigue - GI symptoms, including nausea, vomiting and diarrhea or constipation - Rash or hematological effects (rare or transient) - bronchospasm, esp with history of asthma - hypoglycemia - impotence (reported rarely) |
Antiarrhythmic Agents: Beta-blockers precautions or contraindications - withdrawal after prolonged use (should always be gradual) - withdrawal before surgery (weigh risk vs. benefits) - diabetes (may cause hypoglycemia and mask tachycardic response to hypoglycemia) - renal and hepatic impairment - asthma and allergic rhinitis (may cause bronchospasm) - bradycardia, heart block and congestive heart failure CHF) - pediatric use - pregnancy and lactation - COPD |
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Antiarrhythmic Agents Interactions of betablockers include antagonism - adrenergics (e.g. epinephrine and isoproterenol) - NSAIDs and salicylates - Tricyclic antidepressants |
Antiarrhythmic Agents Potentiation of Hypotensive effect of propranolol occurs with - diuretics and other antihypertensives (ex: calcium channel blockers) - MAOIs; phenothiazine and other tranquilizers - Cimetidine (Tagamet) slows metabolism of drug - Certain antiarrhythmic drugs (eg adenosine, digoxin and quinidine) which may potentiate toxic effects - alcohol, muscle relaxants, and sedatives, which may precipitate hypotension, dizziness, confusion or sedation |
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Antiarrhythmic Agents Calcium channel blockers - Verapamil (Calan) and diltiazem (Cardizem) - Indicated for treatment of atrial fibrillation/flutter and PSVT - Verapamil and diltiazem counteract arrhythmias by slowing AV nodal conduction * Calcium channel blockers are also used in treatment of angina and hypertension |
Antiarrhythmic Agents Side effects of Calcium Channel Blockers - hypotension, with vertigo and headache - bradycardia with heart block - edema - constipation, nausea and abdominal discomfort |
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Antiarrhythmic Agents Precautions or contraindications for calcium channel blockers - Heart block, heart failure, or angina - hepatic and renal impairment - pregnancy and lactation - children - hypotension and heart block - certain arrhythmias and severe heart failure |
Antiarrhythmic Agents Interactions of Calcium Channel Blockers with other cardiac drugs: ex digoxin (can potentiate both good and adverse effects) |
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Antiarrhythmic Agents Antagonistic Effects of Calcium Channel Blockers - Barbiturates, cimetidine, phenytoin, ranitidine, and rifampin - hypotensive effect potentiated with diuretics, ACE (angiotensin-converting enzyme) inhibitors, beta-blockers and quinidine. |
Ludocaine Antiarrhythmic Agents - Local anesthetic (amide type)) - Administered for antiarrhythmic effects and membrane-stabilizing action - Second choice for treatment of ventricular arrhythmias (behind other alternative agents (e.g. IV amiodarone)) |
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Antiarrhythmic Agents Side effects of lidocaine are usually of short duration are dose related and can include - CNS symptoms, including tremors, seizures, dizziness, confusion and blurred vision - hypotension, bradycardia and heart block - dyspnea, respiratory depression and arrest - EKG monitoring and availability of resuscitative equipment are necessary during the IV administration of lidocaine |
Precautions or contraindications with Lidocaine (antiarrhythmic agents) - patients hypersensitive to local anesthetics of this type (amide type) - heart block and respiratory depression - pregnancy and lactation - children |
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Interactions of lidocaine with other cardiac drugs may be additive or antagonistic and my potentiate adverse effects -other interactions may be of minor clinical significance since lidocaine is usually titrated to response |
Do not take grapefruit juice with certain calcium channel blockers since adverse effects may be potentiated |
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Procainamide Procainamide, quinidine, and disopyramide (Norpace) = Antiarrhythmic agents - Act by decreasing myocardial excitability, inhibiting conduction; may depress myocardial contractility = used orally primarily as prophylactic therapy to maintain normal rhythm after conversion by other methods - Possess anticholinergic properties - IV procainamide is a potential treatment alternative to (amiodarone) for the treatment of ventricular tachycardia during CPR |
Side effects of this class (procainamide, quinidine and disopyramid) of antiarrhythmics are numerous and my necessitate cessation of treatment (Procainamide) - diarrhea, anorexia, nausea, and vomiting, and abdominal pain (which are common) - anticholinergic effects, including dry mouth, blurred vision, confusion, constipation, and urinary retention |
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Precautions or Contraindications with procainamide, quinidine and disopyramide - atrioventricular block and conduction defects - electrolyte imbalance - digoxin toxicity - heart failure and hypotension - myasthenia gravis - older adults - more susceptible to hypertensive and anticholinergic effects - children - pregnancy and lactation - hepatic and renal disorders - hypersensitivity to "ester-type" local anesthetics with procainamide - systemic lupus erythematosus (SLE) with procainamide |
procainamide, quinidine and disopyramide Interactions with increased possibility of toxicity may occur with - muscle relaxants and neuromuscular blockers - anticholinergics, tricyclic antidepressants, and phenothiazines - other cardiac drugs, esp digoxin and antihypertensives |
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Interactions with increased possibility of quinidine toxicity ay occur with - antiretroviral protease inhibitors - antacids or sodium bicarbonate - anticonvulsants (e.g. phenytoin and phenobarbital; cause decreased serum levels) - anticoagulants (action can be potentiated by quinidine) |
Propafenone (Rythmol) - oral antiarrhythmic agents - Treats symptomatic supraventricular arrhythmias or severe, life-threatening ventricular arrhythmias - useful in converting atrial fibrillation to sinus rhythm and maintaining it - has local anesthetic effects, direct stabilizing action on myocardial membranes, and beta-adrenergic blocking properties |
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Side effects of propafenone may include - dizziness and blurred vision - nausea, vomiting, unusual taste and constipation - angina, heart failure, palpitations, arrhythmia and dyspnea - fatigue and weakness and headache - rash |
Precautions or contraindications of propafenone - asthma or acute bronchospasm - second or third-degree heart block (in absence of a pacemaker), cardiogenic shock, heart failure and bradycardia - marked hypotension and electrolyte imbalance |
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Interactions of propafenone may occur with - Quinidine, ritonavir, and certain SSRIs (may cause serum levels of propafenone to be elevated) - Beta-blockers, digoxin and theophylline (may result in increased serum levels of the same) |
Patient Education: patients taking antiarrhythmics - immediate reporting of adverse side effects (esp palpitations, irregular or slow heartbeat, faintness, dizziness, weakness, respiratory distress and visual disturbances) - holding medication, if there are side effects, until physician is contacted - rising slowly from reclining position - modification of lifestyle to reduce stress - mild exercise on regular basis as approved by physician - not discontinuing med even if patient feels well - taking proper dosageon medication on time as prescribed wihtout skipping any dose - if med is forgotten, not doubling dose - taking med with full glass of water on empty stomach (1 h before or 2 hour after meals - so will be absorbed more efficiently unless stomach upset occurs or physician prescribes otherwise) - Avoiding taking any other meds including OTC meds, unless approved by physician - discarding expired meds and renewing prescription - avoiding comparison with other patients on similar drugs - contacting physician immediately with any concerns regarding medicines |
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Table 25-1 page 512 Cardiac Glycoside - Digoxin (Lanoxin) PO tablets, elixir, IM, IV for heart failure Antiarrhythmics IA procainamide - IV = for VTach, afib, PAT, PSVT , has anticholinergic properties IBlidocaine (Xylocaine) - IV diluted - local anesthetic- amide, type for Vfib, Vtach, check IV dilutions IC propafenone (Rythmol) PO q8h For afib, pSVT, Vtach II metoprolol (Lopressor) PO, BID, IV, IV bolus, repeat q5 min for 3 doses total = beta blocker for heart rate control in afib III amiodarone (Cordarone, Pacerone) - IV,PO, for ventricular arrhythmias, also vasodilator; medication guide required IV verapamil (Calan)- IV, PO - calcium channel blocker for afib and PSVT adenosine (Adenocard) IV bolus , then PRN for PSVT; do not confuse with amiodarone |
Antihypertensives What is hypertension? - Systolic blood pressure (SBP) of 140 or greater or - diastolic blood pressure (DBP) of 90 or greater = strong consistent relationship between blood pressure and risk of cardiovascular disease (CVD) = Antihypertensives may control hypertension, but they do not cure it - Drugs given to lower blood pressure act in various ways = Varies according to stage of hypertension, physical factors, and effectiveness in individual cases - after withdrawal of drug, BP will return to levels similar to those before treatment with meds, if all other factors remain constant - if antihypertensive therapy is to be terminated, dosage should be gradually reduced, as abrupt withdrawal can cause rebound hypertension |
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High blood pressure increases risk of - angina, myocardial infarction, heart failure, stroke, retinopathy, peripheral arterial disease, and kidney disease and thus requires aggressive treatment |
Prehypertension SBP range 120-189 and DBP range 80-89 = condition that may identify patients who are at a higher cardiovascular risk based on BP and a higher risk for developing sustained hypertension in later years - purpose of this class is to encourage patients to initiate or continue healthy lifestyle practices (rather than to begin antihypertensive drug therapy) = weight reduction (patients who are overweight and obese), use DASH eating plan, dietary sodium reduction, increased physical activity, modified alcohol use and smoking cessation |
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Drugs given to lower blood pressure act in various ways - drug of choice depends on stage of hypertension (1 or 2) and effectiveness in individual cases - health practitioner must be observant of vital signs and side effects in order to assist physician in most effective treatment of hypertension |
Side effects of antihypertensives are common - most common is hypotension (esp postural hypotension) - bradycardia (exceptions include hydralazine - which can cause tachycardia) |
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Thiazide Diuretics - Most patients meeting the criteria for drug therapy should be started on thiazide-type diuretics = Either alone or in combination with a drug from one of the other drug classes (ACE inhibitors, angiotensin receptor blockers, beta-blockers, or calcium channel blockers) - Appear to be as effective as other antihypertensive agents and are inexpensive - |
Thiazide Diuretics Beta-adrenergic blockers - Suitable for initial therapy in some patients with angina, postmyocardial infarction, ischemic heart disease, heart failure, and certain arrhythmias - like thiazide diuretics, beta-adrenergic blockers (carvedilol (Coreg) and metoprolol (Lopressor, Toprol XL) are well tolerate and are suitable for initial therapy in some patients with angina, postmyocardial infarction, ischemic heart disease, heart failure, and certain arrhythmias - only bisoprolol, carvedilol, and metoprolol extended-release have been proven to reduce mortality when used in patients with heart failure. - Atenolol should not be used to treat hypertension because this drug has no effect in reducing cardiovascular events and mortality |
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Calcium Channel Blockers - diltiazem (Cardizem) and nifedipine (Procardia) are an initial therapy option for hypertensive patients with diabetes or high coronary disease risk. - more effective in treating African-American patients older adults, and patients with higher pretreatment blood pressure readings - may also be preferred in patients with obstructive airways disease) - short-acting calcium channel blockers should never be used to manage hypertensive crisis because of reports of increased risk of myocardial infarction and mortality |
Because of their pharmacology, verapamil and diltiazem may be used to treat various arrhythmias |
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Angiotensin-Converting Enzyme (ACE) Inhibitors (ACEIs) Angiotensin-converting enzyme inhibitors ACEIs - First- or second-line agents in the treatment of hypertension - Excellent alone or in combination with other antihypertensives (e.g., diuretics) - good choice for patients who also have other serious conditions (heart failure, following myocardial infarction, when high coronary disease risk exists, diabetes, renal disease and cerebrovascular disease) Ex: ACEIs can be considered drug of choice for hypertensive patients with nephropathy because they slow the progression of renal disease - they are more effective in younger and white populations and less effective in black patients, unless given higher doses or in combo with diuretic |
Side effects of ACE inhibitors (infrequent and usually mild) - rash or photosensitivity - loss of taste perception; metallic taste - blood dyscrasias - renal impairment - severe hypotension - chronic dry cough or nasal congestion - hyperkalemia (monitor serum potassium levels periodically) |
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Precautions or Contraindications with ACE inhibitors - collagen disease, (lupus or scleroderma) - heart failure - angioedema - pregnancy and lactation - children |
Interactions of ACE inhibitors (ACEIs) apply to - diuretics (potentiate hypotension; watch BP closely) - Vasodilators (watch BP closely) - Potassium - sparing diuretics and potassium supplements (hyperkalemia risk) - NSAIDS, and salicylates (antagonize effects of ACE inhibitors and increase deterioration of renal function in patients with compromised renal function) - antacids (decrease absorption) - Lithium (risk of lithium toxicity) |
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Angiotensin Receptor Blockers (ARBs) similar to ACE inhibitors and are generally used as alternatives - Block angiotensin receptor that causes vasoconstriction when stimulated by angiotensin II - Ex: losartan (Cozaar) and valsartan (Diovan) block the effects of angiotensin II, decreasing blood pressure without a marked change in heart rate - compared to ACEIs, ARBs are associated with lower inciddence of drug-induced cough, rash , and or taste disturbances and used in those patients who cannot tolerate ACEIs. - Like ACEIs, African American patients experience smaller antihypertensive response with ARBs compared to other ethnic groups - addition of a low-dose thiazide diuretic to an ARB significantly improves hypertensive efficacy. - also good choices for patients with other serious conditions (heart failure, diabetes and renal disease) |
Side effects are relatively uncommon with ARBs, and include - dizziness - orthostatic hypotension, - upper respiratory tract infections and - hyperkalemia |
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Precautions or contraindications for ARBs - renal impairment - pregnancy and lactation - children |
Interactions with ARBs are similar to ACEIs diuretics (potentiate hypotension; watch BP closely) - Vasodilators (watch BP closely) - Potassium - sparing diuretics and potassium supplements (hyperkalemia risk) - NSAIDS, and salicylates (antagonize effects of ACE inhibitors and increase deterioration of renal function in patients with compromised renal function) - antacids (decrease absorption) - digoxin (possible digitalis toxicity) - Lithium (risk of lithium toxicity) |
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Other Antihyperintensives - Antiadrenergic Agents - Peripheral Vasodilator |
Other Antihyperintensives Antiadrenergic Agents Clonidine (Catapres) a central-acting alpha-adrenergic agent, used mainly in treatment of hypertension - available in oral preparation, transdermal system, injection for epidural use. - used successfully in variety of other conditions including ADHD, nicotine/opiate withdrawal, vascular headaches, glaucoma, ulcerative colitis, Tourette's syndrome, and treatment of severe pain in cancer patients |
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Other Antihyperintensives Antiadrenergic Agents Prazosin (Minipress) is a peripherally acting alpha-adrenergic blocker used primarily to treat hypertension - Other agents in this class are used to treat benign prostatic hypertrophy (BPH) - treatment with alpha-adrenergic blockers once was considered potentially favorable for management of hypertension in patients with BPH to target both blood pressure and BPH symptoms - study determined that patients treated with alpha-blocker doxazosin, when compared with those treated with diuretic cholarthalidone (had increased risk for stroke and heart failure)** - Therefore, hypertension should not be managed with an alpha-blocker alone, and BPH symptoms should be managed separately. |
Other Antihistamines: Peripheral Vasodilator - Hydralazine: Hydralazine is sometimes used in the treatment of moderate to severe hypertension (esp in patients with CHF, it increases heart rate and cardiac output) - this drug generally used in conjunction with a diuretic and another hypotensive agent (ex: a beta-blocker) - fixed-dose combination of isosorbide dinitrate and hydralazine (BiDil) available for treatment of heart failure. |
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Side Effects of Hydralazine (Peripheral vasodilator) can include - Tachycardia and palpitations - headache and flushing - orthostatic hypotension - GI effects, including nausea, vomiting, diarrhea and constipation - blood abnormalities - edema and weight gain |
Precautions or contraindications for hydralazine (Peripheral vasodilator) - systemic lupus erythematosus (SLE) - Renal disease - coronary artery disease and rheumatic heart disease - pregnancy usually (however, many regard hydralazine as antihypertensive of choice during preeclampsia) |
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Drug use to treat hypertension - alpha adrenergic blocker: blocks alpha effects from nervous system of vasoconstriction therefore causing vasodilation. Ex: drug prazosin (Minipress) - peripheral vasodilator: Cause smooth muscle relaxation of arterioles causing direct vasodilation; Ex: drug hydralazine - beta adrenergic blocker: reduce cardiac output by decreasing heart rate and force of contraction (ex: drugs; cavedilol (Coreg) and metoprolol (Lopressor) - Calcium Channel Blocker: blocks calcium ion channels needed for smooth muscle contraction and therefore causes smooth muscle relaxation and resulting vasodilation; Ex: drugs amiodipine (Norvasc) and verapamil (Calan) - Angiotension Receptor Blockers (ARB's): prevents angiotension II from reaching receptors and therefore causes vasodilation; ex: losartan (Cozaar) and valsartan (Diovan) - ACE inhibitors (ACEI's): block formation of angiotension II from causing vasoconstriction, therefore causing vasodilation; also blocks aldosterone secretion, thereby caused increased urine output: Ex: drugs lisinipril (prinivil) and enalapril (Vasotec) - Thiazide Diuretics: decrease blood volume by increasing urine output; ex: hydrochlorothiazide (Microzide) |
All beta-adrenergic blockers end in "lol" All ACE inhibtiors end in "pril" All angiotension receptor blockers end in "sartan" |
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Patient eduction on taking antihypertensives - routinely monitoring blood pressure at home, keeping a log of blood pressure reading, sharing info with physician - immediate reporting of any adverse side effects, esp slow or irregular heartbeat, dizziness, weakness, breathing difficulty, gastric distress and numbness or swelling of extremities - Taking meds on time as prescribed by physician (not skipping a dose or doubling a dose; not discontinuing the medicine, even if patient is feeling well without consulting physician first - rising slowly from reclining position to reduce light headed feeling - taking care in driving a car or operating machinery if meds cause drowsiness (ask physician, nurse, or pharmacist about specific meds since meds differ and individual reactions differ: older people are more susceptible to this effect) - potentiation of adverse side effects by alcohol, esp dizziness, weakness, sleepiness and confusion - reduction or cessation of smoking to help lower blood pressure - lifestyle modification: exercise, quitting smoking, limiting alcohol usage, eating healthy diet in control of blood pressure; following the physician's instructions, appropriate diet may include, low salt or low sodium or weight-reduction diet - mild exercise on regular basis - always swallowing the extended-release products intact. Quick release meds into system can cause blood pressure to drop suddenly, cause loss of consciousness and possible shock - avoiding grapefruit juice while taking calcium channel blockers (can increase risk of hypotension and other adverse cardiac effects) |
Coronary Vasodilators - Treat angina - Acute pain resulting from insufficient blood supply (ischemia) to a part of the heart - Angina pectoris: most common form of angina = Involves chest pain resulting from decreased blood supply to the heart muscle = Nitrates most commonly used for relief of acute angina pectoris (nitroglycerin and isosorbide)
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- Vasodilators administered to dilate these blood vessels (thus increasing myocardial oxygen supply) and stop attacks of angina or reduce the frequency of angina when administered prophylactically. |
Coronary Vasodilators - used in treatment and prophylactic management of angina includes nitrate, beta-blockers and calcium channel blockers |
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Nitrates - used most commonly for relief of acute angina pectoris and long-term prophylactic management: are nitroglycerin and isosobide (e.g. Isordil, Imdur) - Nitroglycerin is available in several forms and can be administered in sublingual tablets allowed to dissolve under tongue or a sublingual spray for relief of acute angina pectoris - if chest pain not relieved or worsens, 5 min after a dose, EMS should be activated because unrelieved chest pain can indicate an acute myocardial infarction - traditional recommendation take up to 3 SL nitroglycerin doses over 15 min before accessing emergency system, recent - new guidelines recommend instructing patient with prior prescription for nitroglycerin to call 911 immediately if chest discomfort or pain is persistent or worsened 5 min after one dose of nitrogylcerin - self-treatment with nitrates has been identified as factor resulting in delays in emergency evaluation |
Nitroglycerin - available in time-released capsules and tablets and in injectable formulation that must be diluted carefully according to manufacturers instructions for IV administration - tablets and capsules must be stored only in glass containers with tight-fitting metal screw tops away from HEAT |
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For long term prophylactic management of angina pectoris, nitroglycerin is frequently applied topically as a transdermal system - one type absorbed thru skin is Nitro-Bid ointment: applied with applicator-measuring (Appli-ruler) paper. = usual dosage: 0.5-2 inches applied every 8 h - removed old paper first - ointment spread lightly (not massaged or rubbed) over any hairless skin area and applicator paper is taped in place - avoid touching the ointment when applying (accidental absorption thru skin of fingers scan cause HEADACHE) - if nitroglycerin is discontinued, dose and frequency must be decreased gradually to prevent sudden withdrawal reations |
Another topical nitroglycerin product: longer action, in transdermal form (Nitro-Dur) - skin patch applied every 24 h (on in AM off 12 h later in PM) to clean dry hairless area of upper arm of body. - do not apply below elbow or knee - sites should be rotated to avoid skin rotation, and raw, scarred, or callused areas should be avoided (Check prescribed dosage carefully, remove old patch) |
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Another nitrate used for ACUTE RELIEF of ANGINA PECTORIS and for PROPHYLACTIC long-term management = Isosorbide - available in SL tablets, regular release tablets, timed-released capsules and tablets - when using long-acting nitrates, a 12-14h nitrate free interval between the last dose of day and first dose of following day is recommended to lessen risk of nitrate tolerance |
Side Effects of the nitrates can include - headache (usually diminishes over time; analgesics may be give to alleviate pain) - postural hypotension, (dizziness, weakness, and syncope: patients should be sitting during administration of fast-acting nitrates) - rash and skin irritation with transdermal forms - blurred vision and dry mouth (discontinue the drug with these symptoms - hypersensitivity reactions, enhanced by alcohol, including nausea, vomiting, diarrhea, cold sweats, tachycardia and syncope |
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Precautions or contraindications for nitrates (coronary vasodilators) apply - Glaucoma - GI hypermotility or malabsorption (with timed-released forms) - Intracranial pressure - severe anemia - hypotension |
Interactions of nitrates (coronary vasodilators) may occur with alcohol, potentiates hypotensive effects - Phosphodiesterase (PDE) inhibitors such as sildenafil (Viagra) used for erectile dysfunction, are contraindicated in men taking nitrates - two drugs interact to cause a large, sudden, dangerous drop in blood pressure - For long-term prophylactic treatment of angina pectoris, beta-blockers such as metoprolol (Lopressor) and calcium channel blockers such as diltiazem (Cardizem) and verapamil (Calan) frequently sued |
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Patient Eduction for coronary vasodilators (nitrates) - administering fast-acting preparations (sublingual tablets or spray) while sitting down because the patient may become lightheaded - rising slowly from a reclining position - not drinking alcohol or taking PDE inhibitors while take these medicines, which can cause a serious drop in blood pressure - used timed-release capsules or tablets to prevent attacks (they work too slowly to help once an attack has started) - the fact that nitrates taken for chronic angina may require periods of drug-free intervals to avoid development of nitrate tolerance and lessening of antianginal effects - Taking timed-release capsules or tablets on an empty stomach with a full glass of water - allowing sublingual tablets to dissolve under tongue or in the cheek pouch and not chewing or swallowing them - repeating sublingual tablets or spray in 5-10 min for a max of 3 tablets or sprays (if no relief or worsening of chest pain within 5 min after the first tablet, activate EMS, or if EMS is unavailable,, report to emergency department) for patients know to have frequent angina, physicians may provide individualized instructions for the use of SL nitroglycerin, based on the characteristics of patient's angina, time course, and response to treatment - not discontinuing the med suddenly if administered for several weeks (dosage must be reduced gradually under physician's supervision) - sensations expected: facial flushing, headache for a short time and lightheadedness upon rising too suddenly (if symptoms persist or become more severe or other symptoms occur: irregular heartbeat or blurred vision, notify physician at once) - preventing attacks of angina by administering a sublingual tablet or spray before physical exertion or emotional stress (preferable to avoid physical or emotional stress when possible) |
Drugs used to treat ANGINA - beta-blockers: decrease rate and force of contraction of heart thereby reducing workload and oxygen demand Ex: drug metoprolol (Lopressor) - Calcium Channel Blockers: Dilates arterial smooth muscle causing vasodilation thereby decreasing blood pressure and cardiac oxygen demand Ex: drugs diltiazem (Cardizem) and verapamil (Calan) - Coronary Vasodilators: dilate coronary arteries to increase blood supply and oxygen delivery to heart, IN addition reduces venous blood return to heart Ex: drugs Nitroglycerin (various forms including transdermal and isosorbide (Isordil) |
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Nitrates - Nitroglycerin (Nitrostat tabs, Nitrolingual spray, caps E.R., Nitro-Bid oint 2%, Nitro-Dur, Minitran, IV, (premixed or sol for inj) - Isosorbide dinitrate (isordil, Dilatrate SR) - with Hydralazine (BiDil) - Isosorbide Mononitrate (Imdur SR) |
Antilipemic Agents - Elevated total blood cholesterol levels above 200 mg/dL = Key risk factor for coronary heart disease (CHD) - Cardiovascular disease is the leading killer of men and women in the United States - High cholesterol can lead to: = Arterial blockage, hardening of the arteries, blood clots, heart attack, or stroke, and may even play a role in dementia |
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Antilipemic Agents
- lipoproteins are responsible for transporting cholesterol and other fats thru blood stream - Low-density lipoproteins (LDLs: "bad cholesterol") carry largest amount of cholesterol in blood and are responsible for transporting and depositing it in arterial walls - Very low-density lipoproteins (VLDLs; triglycerides) are precursors of the LDL and compose largest proportion of lipids in diet, adipose tissue and blood. - Triglycerides (TGs) are source of energy; excess dietary calories are converted to TGs and stored as fat in adipose tissue for future energy needs. Excess TGs (greater than normal 150 level) can be independent risk factor leading to atherosclerosis and CHD, as well as pancreatitis. |
High-Density Lipoproteins (HDL's "good cholesterol" - help transport LDL cholesterol from the walls of the arteries thru the blood stream to the liver for excretion. - HDL level below 40 mg.dL is LOW - each 1 mg.dL increase in the HDL level associated with a 6% lower risk of cardiovascular disease - LDL cholesterol is primary target of treatment in clinical lipid management - the use of therapeutic lifestyle changes (TLCs) including LDL-lowering dietary management (E.g. restriction of saturated and trans fats or cholesterol intake, (fiber and soy protein in diet) weight control, appropriate exercise, limiting alcohol intake, smoking cessation, will achieve the therapeutic goal (LDL below 100 mg/dL) in many persons. - if measures are inadequate dug therapy may be added. = drug therapy aimed at reducing cholesterol levels either reduces hepatic production or intestinal absorption of cholesterol |
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6 categories of antilipemic agents to lower blood cholesterol levels are available: HMG-CoA reductase inhibitors (the statins) bile acid sequestrants, nicotinic acid (niacin), fibric acid derivatives, cholesterol absorption inhibitor and omega-3 fatty acids |
Antilipemic Agents: Statins - HMG-CoA reductase inhibitors (statins) inhibit the enzyme for cholesterol synthesis - Most potent lipid-lowering medications available for monotherapy - First choice in managing high cholesterol - Statins (atorvastatin- LIpitor; simvastatin-Zocor) have been shown to be effective in lowering LDL levels (up to 60%) and are modestly effective in reducing TG levels and increasing HDL levels, thereby reducing cardiovascular morbidity and mortality. Statins are generally well tolerated. |
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HMG-CoA (Statins) - most active at night when dietary intake is low (most statins generally given at bedtime; provide optimal decreases in LDL levels) - longer half-lives, atorvastatin and rosuvastatin can be given at same time each day any time of day. - Max dose of simvastatin was reduced from 80 to 40 mg (if using for less than 12 months) because of increased risk of myopathy form higher dose |
Side Effects of Statins include (Antilipemic agents) - mild GI disturbances, headache, rash, fatigue - myalgia and muscle weakness (can try switching to a different statin if problematic) - Rhabdomyolysis (destruction of muscle tissue leading to renal failure; reported rarely) - Elevated liver enzymes (FDA recently revised statin labeling by removing recommendation for periodic liver function tests; baseline tests are still suggested, but follow-up monitoring necessary only if clinically indicated) - Increased risk (9% to 13%) of new-onset diabetes mellitus with high-dose statin use (benefits of statin therapy far outweigh risk of statin-induced diabetes; be considerate of risk and monitor the patient) |
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Interactions of certain statins with - amiodarone - dronedarone - immunosuppressive drugs - erythromycin - azole antifungals - diltiazem - verapamil - grapefruit juice - other antilipemic drugs (fibrates and niacin) increase risk for myopathy and renal failure - recently: max recommended dose for most statins, when taking with certain interacting drugs was REDUCED due to safety considerations |
Antilipemic agents: Bile-Acid Sequestrants - Cholestyramine (Questran) and colesevelam (WelChol) - Bind bile acids in the intestine, interrupting the process by which bile acids are returned to the liver for reuse - since bile acids formed from cholesterol, sequestrants reduce total body cholesterol - Bile acid sequestrants can be used as monotherapy when moderate reductions in LDL levels are required or as an add-on therapy to statins - should not be used as a single agents in the presence of elevated TGs |
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Side Effects of bile acids sequestrants include - constipation, gas, cramps, heartburn, nausea, anorexia, abdominal pain, and bloating (occurs frequently and my affect compliance) - Colesevelam administered at lower doses because of its higher bile-binding capacity and associated with fewer GI adverse effects |
Precautions or contraindications for bile acid sequestrants apply to (Antilipemic Agents) - biliary cirrhosis and obstruction - GI obstruction or fecal impaction |
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Interactions with bile acid sequestrants can reduce absorption of many drugs - antibiotics, cardiac glycosides, fat-soluble vitamins, thiazide diuretics, thyroid hormones (administer at least 1h before or 4 h after the bile acid sequestrants) |
Antilipemic agents Nicotinic Acid (Niacin) - Reduces hepatic synthesis of triglycerides; inhibits the mobilization of free fatty acids from the peripheral tissues - Lowers serum total, LDL cholesterol, and triglyceride levels - Raises HDL cholesterol levels - may be useful in combination with a statin in patients with diabetic dyslipidemia (abnormal levels of various blood lipid fractions) |
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Antilipemic agents Side effects of niacin - GI upset, dyspepsia (indigestion) blurred vision, and fatigue - skin flushing, itching and irritation (more common with immediate-release preparations; pretreatment with aspirin or ibuprofen can diminish cutaneous reactions) - glucose intolerance and hyperuricemia (abnormal uric acid levels in blood) (higher doses) - hepatoxicity (esp with sustained-release products; monitoring hepatic function is recommended for all niacin formulations) |
Precautions or Contraindications of niacin include - hepatic, gallbladder or peptic ulcer disease; diabetes; glaucoma; or gout - pregnancy and lactation (high doses) - children (<10 years old) |
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(Antilipemic agents) Interactions of niacin occur with - antihypertensives and vasodilators (potentiate hypotensive effects) - antidiabetic agents with loss of blood glucose control - alcohol (worsens flushing) |
(Antilipemic agents): Fibric Acid Derivatives (Fibrates) - Fibrates fenofibrate (TriCor) and gemfibrozil (Lopid) possess minimal LDL-reducing capacity - BUT Especially effective in patients who have extremely high triglyceride levels, elevated cholesterol levels, and combined forms of hyperlipidemia - good choice for diabetics because they improve glucose tolerance = mechanism: fibrates reduce TGs is poorly understood - fibrates may be used in combo with other anilipemics (these agents appear to be additive in LOWERING LDL and RAISING HDL cholesterol = fibrates are generally well-tolerated |
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Side effects of fibrates (fibric acid derivatives) - GO complaints (Diarrhea, dyspepsia, nausea and vomiting and abdominal pain - Cholethiasis (gallstones in gallbladder) due to increased biliary excretion of cholesterol, jaundice, blood dyscrasias, myopathy (abnormal condition of skeletal muscles - hypersensitivity reactions (rare) - increased risk of pulmonary emboli (PE) |
Precautions or Contraindications fibrates (fibric acid derivatives) - Gallbladder, hepatic, renal disease, or peptic ulcer - pregnancy and lactation - children - Gemfibrozil with statins (increased risk for myopathy and rhabdomyolysis) |
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Interactions fibrates (fibric acid derivatives) - oral anticoagulants and hypoglycemic agents (potentiate effects) - Statins to increase the risk of serious muscle problems and elevated liver enzymes (use together only in lowest effective doses and if benefits outweighs risks) - Ezetimibe is not advised (increased risk of cholethiasis) |
Cholesterol Absorption Inhibitor - Ezetimibe (Zetia) moderately reduces LDL by inhibiting intestinal absorption of both dietary and biliary cholesterol, blocking its transport in the small intestine - can be taken simultaneously with a statin (Vytorin - combination product) allow for lower doses of statin to be used and the LDL-lowering effects of the two drugs are additive. - Ezetimibe is generally well tolerated, with abdominal pain, back pain, and arthralgia being reported - patients with gallbladder disease and moderate to severe hepatic insufficiency should not take it - administer ezetimibe at least 1 to 2h before or 2 to 4 hour after administering antacids and bile acid sequestrants (respectively) *avoid use with cyclosporine (increases serum concentrations of both drugs) and fibrates (increased risk of cholethiasis) |
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Omega-3 Fatty Acids Eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) - Prevent primary and secondary heart disease and reduce triglycerides (TGs) as an adjunct to diet or simvastatin. - Best source of omega-3 is fatty fish (salmon) but fish oil capsules may be more convenient (esp if high doses are needed) - Lovaza: highly concentrated, purified form (used for high doses) by prescription ONLY. Fish oil can cause- nausea, heartburn, or diarrhea - fishy aftertaste can be reduced by refrigeration or freezing (Lozava * should NOT be frozen) Since omega-3 fatty acids inhibit platelet aggregation, caution is advised when used concurrently with anticoagulants, platelet inhibitors, and thrombolytic agents - DHA component of omega-3 acids may be responsible for elevations of LDL levels seen with these products; patients should be monitored to ensure their LDL levels do not increase excessively
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Antilipemic Agents Statins: - atorvatatin (Lipitor) - lovastatin (Mevacor) PO at bedtime with food - pravastatin (Pravachol) PO at bedtime - rosuvastatin (Crestor) PO daily - simvastatin (Zocor) PO bed time (80 mg if already on it with no evidence of myopathy) Bile Acid Sequestrants - cholestyramine (Questran, Questran Light): 1-2 times per day ac; mix powder with water, milk or juice - colesevelam (Welchol) 6 tabs daily or 3 tabs BID with food and a full glass of water; max 7 tabs per day Nicotinic Acid - niacin (Niaspan (RX), (Slo-Niacin OTC): dose varies with response, take after meals or a snack Fibric Acid Derivatives - fenofibrate (Antara, Lofibra, Tricor, Trilipix): PO daily with food depending on formulation/manufacturer - gemfibrozil (Lopid) PO BID ac Cholesterol Absorption Inhibitor - ezetimibe (Zetia) PO daily Omega-3 fatty acids - fish oil (OTC) - (Lovaza- Rx) Combinations - atorvastatin/amlodipine (Caduet) - ezetimibe/simvastatin (Vytorin) - lovastatin/niacin (Advicor (POD daily bedtime with food, dose varies with response) |
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Patient ed on antilipemic therapy - continue diet (low-fat, low-cholesterol) and aerobic exercise - taking meds with meals to reduce GI upset - report side effects to physician immediately (esp muscle pain, tenderness, weakness, dark-stained urine or bleeding - with cholestyramine: importance of high fiber diet and or a stool softener, fat-soluble vitamin and folic acid supplements, and not taking toher meds with in 4 h - expecting facial flushing with niacin (unless extended release formula used) - avoid grapefruit juice while taking statins; adverse effects are potentiated - give healthcare provider list of all meds, herbs, nonprescription drugs or dietary supplements (so potential interactions can be identified) - importance of initial liver function test - if all factors remain same, meds will proba need to be taken throughout patient's lifetime, sometimes diet and exercise will eliminate the need |
Antithrombotic Agents Inappropriate thrombus formation - Can be caused by vessel-wall injury, circulatory stasis, increased blood coagulability, immobilization, obesity, cigarette smoking, medication therapy, and other factors - inappropriate thrombus formation or clot can dislodge and travel thru bloodstream (thromboembolism or TE) where it can fully or partially obstruct blood flow leading to tissue damage Antithrombotic agents interfere with or prevent thrombosis or blood coagulation - Include: Anticoagulants, platelet inhibitors, and thrombolytics |
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Antithrombotic Agents - blood has ability to flow freely thru blood vessels yet cloth when need arises - normal hemostasis or blood coagulation involves formation of a fibrin clot or thrombus (minor cut would not cause us to bleed profusely) |
Anticoagulants Antithrombotic Agents - Prevent formation of fibrin clot by interfering with one of the steps leading to fibrin formation - Oral (coumarin derivatives and the new oral anticoagulants) - injectable (heparins) = action of these two classes different = however purpose os same: to prevent formation of clots or decrease the extension of existing cloths in such conditions (venous thrombosis, stroke, pulmonary embolism, and coronary artery occlusion) - many patients with artifical heart valves, mitral valve disease or chronic atrial fibrillation or postsurgical patients (cardiac bypass, vascular surgery and hip or knee replacement) receive anticoagulants to prevent embolism or thrombosis - patients on anticoagulants (esp older patients) should be constantly observed for bleeding complications (cerebrovascular accidents CVAs) - Coumarin derivatives (Warfarin) and heparin, do not dissolve existing cloths; only interfere with the coagulation process preventing clot formation and or propagation. |
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Antithrombotic Agents: Warfarin (Coumadin) - is administered orally (also available as injectable preparation which is rarely used) - Alters synthesis of blood coagulation factors in the liver by interfering with the action of vitamin K - the antidote for serious bleeding complications during warfarin therapy is prothrombin complex concentrate or fresh frozen plasma and vitamin K - action of warfarin: slower than that of heparin, therefore warfarin is generally used as follow-up for long-term anticoagulant therapy. (warfarin may be started at the same time as heparin) - most commonly used laboratory method of monitoring therapy with warfarin is International Normalized Ration (INR)- Guide in determining dosage |
Interactions of warfarin with many drugs have been reported concurrent administration of any other drug should be investigated and should be avoided following drugs (some drugs may increase response to warfarin include) - anabolic steroids - alcohol (acute intoxication) - proton pump inhibitors - ALL NSAIDs including aspirin; thrombolytics - tricyclic antidepressants; SSRIs - thyroid drugs - amiodarone, propafenone, and quinidine - many anti-infective agents - Acetaminophen (large daily doses or long duration) Some of the drugs that may decrease response to warfarin - alcohol (chronic alcoholism) - barbiturates - estrogen (including oral contraceptives) - antiretroviral protease inhibitors |
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New Oral Anticoagulants - Dabigatran (Pradaza) first oral anticoagulant (direct thrombin inhibitor) to be approved by FDA, (store in original container only up to 4 months) = rivaroxaban (Xarelto), and apixaban (Eliquis) - compared to warfarin, new oral anticoagulants have a Rapid Onset & predictable anticoagulant effects and fewer food and drug interactions (routine lab monitoring is not required) - cannot be monitored with standard lab testing (currently no reversal agent in case of uncontrolled major bleeding or need for emergency surgery) Dabigatran, rivaroxaban, and apixaban are all indicated for reducing the risk of STROKE and SYSTEMIC EMBOLISM in patients with NONVALVULAR ATRIAL FIBRILLATION - Rivaroxaban is also indicated for venous thromboembolism prevention, post-hip or -knee replacement, and DVT/PE treatment or prevention of recurrence |
Heparin and Low-Molecular-Weight Heparins 2 Types of Heparin: unfractioned type (UFH) and the low-molecular-weight heparins (LMWHs) - Heparin is not absorbed from the GI tract and standard type (UFH) must be administered intravenously or subcutaneously - LMWH type is usually only administered subcutaneously but may be given IV Heparin acts on thrombin (inhibiting action of fibrin in clot formation) - antidote for serious bleeding complication during heparin therapy is Protamine Sulfate - when administered IV: action of heparin is immediate - dilute flushing solution of heparin is also used to maintain patency of indwelling venipuncture devices used to obtain blood specimens and of catheters used for arterial access (arterial lines) *be sure to check that it is a dilute flushing solution before injection, and NOT full-strength heparin*!!!!! - however 0.9% sodium chloride (normal saline) injection alone is used to flush peripheral venipuncture devices (for ex (PRN adapters) - Heparin is not normally used to flush these devices because of possible drug incompatibilities and lab test interferences |
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LMWHs include enoxaparin (Lovenox) and dalteparin (Fragmin) - when administered subcutaneously, monitoring of anticoagulant effect is not necessary, but periodic complete blood counts (CBCs), stool occult blood tests and platelet counts are recommended during treatment - unlike UFH, in case of clinically significant bleeding, no agent fully reverses activity of LMWHs (although protamine has some activity and should be given for life-threatening bleeding alone with packed red blood cells and fresh frozen plasma transfusions if indicated - Fondaparinux (Arixtra) closely related (to the LMWHs) and is a closely realted pentasaccharaide is not generally classified as an LMWH (although often discussed with the same) it is an indirect clotting factor Xa inhibitor and lacks a specific antidote in event of excessive anticoagulation |
Enoxaparin was the first LMWH to be approved in U.S. - currently approved for prevention of deep vein thrombosis (DVT) in patients undergoing knee or hip replacement or abdominal surgery for treatment of unstable angina and ST-elevation myocardial infarction (STEMI) and for inpatient treatment of acute DVT and pulmonary embolism (PE). and for outpatients treatment of acute DVT not associated with pulmonary embolism and is combined with warfarin (until INR reaches 2-3) |
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When heparin is administered subcutaneously, esp if patients is discharged and meds will be administered at home, be sure to stress patient EDUCATION. - measurements of activated partial thromboplastin time (aPTT) is most common lab test for monitoring Heparin Therapy. - when long-term anticoagulant therapy has begun with warfarin, there is short-term overlap period in which both heparin and warfarin are administered concurrently. |
Interactions of all anticoagulants with other anticoagulants (ex: aspirin and NSAIDs, platelet inhibitors and fish oil or with thrombolytic agents for ex alteplase (tPA) may increase risk of hemorrhage) |
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Side effects of all anticoagulants (antithrombotic agents) (Warfarin, new oral anticoagulants, heparin and LMWHs) can include - major hemorrhage - thrombocytopenia - minor bleeding (e.g. petechiae, nosebleed and bruising - blood in urine (hematuria) or stools (melena) - osteoporosis with long-term heparin use (less with the LMWHs; none with the other agents) |
Precautions or contraindications with anticoagulants (antithrombotic agents) (Warfarin, new oral anticoagulants, heparin and LMWHs) - GI disorders and ulcerations of GI tract - Hepatic and renal dysfunction - blood dyscrasias - pregnancy (heparin can be used with caution as it does not cross the placenta) - stroke (may increase risk of fetal cerebral hemorrhage after stroke) - patients with prosthetic heart valves (with the new oral anticoagulants) - lumbar puncture and epidural anesthesia (could result in paralysis) |
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Platelet Inhibitor Therapy Anti-platelet agents - Inhibit aggregation (clumping) and release of thromboplastin from the platelets to begin the clotting process Platelet inhibitors utilize a variety of mechanisms to interfere with activation pathways to prevent platelet clumping - Given as prophylactic therapy or as secondary prevention in patients with history of recent stroke, recent MI, or established peripheral vascular disease - also used in pharmacologic management of post-acute coronary syndrome (ACS)- spectrum of clinical conditions ranging from unstable angina to acute myocardial infarction, with or without ST-segment elevation - Platelet inhibitors are also used prior to and following percutaneous coronary intervention (PCDI) with coronary stenting to prevent stent thrombosis |
Patient education on anticoagulant therapy ((Warfarin, new oral anticoagulants, heparin and LMWHs) - reading FDA approved Medication guide dispensed with the oral anticoagulants - compliance with taking meds as prescribed and required lab monitoring (if any) - does not dissolve clots, it decreases clotting ability of blood and helps prevent formation of harmful blood clots in blood vessels and heart - taking meds as prescribed at same time every day - not changing brands of meds without doctor approval - avoiding eating large amounts of grapefruit/ drinking grapefruit juice or cranberry juice - avoid shots: flue shots, shingle vaccine, and pneumonia vaccine - avoid activities and contact sports that my cause injury, cuts, bruises - using a soft toothbrush and electric razor to shave to prevent cuts - always wearing closed-toe shoes - using a night light to prevent falls - immediately report unusal bleeding, bruising, brown spots, or blood-tinged secretions, injury, trauma, dizziness, abdominal pain or swelling, back pain, headaches and joint pain and swelling to physician - if prescribed, carrying vitamin K for emergency - using reliable birth control method - report allergic reactions (skin rash) - avoid smoking, use of alcohol and OTC meds - wearing identifications and name alerts all time - keeping follow-up appointments with physician for lab work and needed dosage change *Vit K large amount can counteract warfarin therapy. - patients should be educated on modifying risk factors for CHD and stroke (abstinence from all tobacco, weight control, low-fat, and low-cholesterol diet and aerobic exercises on regular basis) |
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Platelet Inhibitor Therapy: Dipyridamole (Persantine) - Non-nitrate coronary vasodilator that inhibits platelet aggregation - when used alone, ineffective as antithrombotic for patients with AMi, DVT, or transient ischemic attacks (TIAs_ and therefore must be combined with other anticoagulant drugs - Dipyridamole is used in combo with aspirin in prevention of ischemic stroke |
Side effects of dipyridamole (usually transient) - headaches, dizziness, and weakness - nausea, vomiting, and diarrhea - flushing and rash
- combo of low-dose aspirin with extended-release dypyridamole (Aggrenox) approved for stroke prophylaxis - most adverse effects are mild and similar to those with eight agent alone |
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Aspirin Platelet Inhibitor Therapy Ability to inhibit platelet aggregation clumping - Used after myocardial infarction or recurrent transient ischemic attacks to reduce risk of recurrence - Used to reduce risk of myocardial infarction in patients with unstable angina - aspirin therapy is not recommended for low-risk patients because of increased risk of hemorrhagic stroke associated with long-term aspirin therapy - pateints should be instructed not to start aspirin therapy without consulting physician first - because gastric irritation, aspirin should be administered with food or milk - film-coated tablets, enteric-coated tablets and buffered aspirin preps are available to reduce gastric irritation |
Adenosine Diphosphate ADP Receptor Antagonists - Blocks activation of the platelet’s receptor surface, thereby inhibiting platelet activation - Clopidogrel (Plavix) first agent approved in this class used to reduce atherosclerotic events (myocardial infarction, stroke, and vascular death) in patients with history of recent stroke, recent MI or established peripheral vascular disease - Clopidogrel also used in combo with aspirin to prevent thrombosis of stents that are used to prop open disease coronary arteries - Prasugrel (Effient) is more potent antiplatelet agent with no clinically significant drug interactions identified to date. - newest agent in this class ticargrelor (brilinta) first reversible oral ADP receptor antagonist = quicker onset of antiplatelet activity allows platelet function to return to baseline quicker and may result in fewer coronary artery bypass surgery- related bleeding events in patients requiring emergent intervention = Ticagrelor's shorter half-life necessitates twice-daily dosing compared with once-daily dosing of clopidogrel and prasugrel - Ticagrelor is contraindicated in severe hepatic impairment |
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Adenosine Diphosphate ADP Receptor Antagonists - all ADP receptor antagonist are contraindicated in patients with active pathological bleeding (peptic ulcer) or history of intracranial hemorrhage - Interactions of all platelet inhibitors with other anticoagulants for ex: aspirin and NSAIDs, other platelet inhibitors or thrombolytic acgents may increase risk of bleeding - use of certain PPIs (esomeprazole, omeprazole, including Prilosec OTC) , azole antifungals most macrolide antibiotics (except azithromycin) certain SSRis (fluoxetine, fluvoxamine) and HIV NNRTIs may make clopidogrel less effective by inhibiting enzyme that converts clopidogrel to the active form of drug - the plasma concentrations of tricagrelor may be elevated by azole antifungals, HIV protease inhibitors and some macrolide antibiotics they may be reduced by carbamazepine, phenobarbital, phenytoin, and rifampin - Ticargrelor can increase digoxin concentrations (monitor levels) and increase lovastatin and simvastatin concentrations (avoid doses > 40 mg) |
Thrombolytic Agents The body maintains a process to dissolve clots (fibrinolysis) after they have formed - Tissue plasminogen activator (t-PA) is a natural peptide that initiates fibrinolysis - Thrombolytic agents dissolve and liquefy the fibrin of an existing clot - Thrombolytic drugs (e.g., reteplase and alteplase) potentiate t-PA, resulting in clot dissolution, reperfusion of organs, and restoration of blood flow to tissues |
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Thrombolytic agents - given IV, reduce mortality when used as early as possible but within the first 12 h after the onset of acute STEMI, - Alteplase is also used to treat acute ischemic stroke (within 3-4.5 h of the onset of stroke symptoms) and acute pulmonary embolism. - administered in an ER or ICU setting, dose monitoring of hemodynamics and vital signs is generally considered standard with thrombolytic therapy; particularly during the initial 24-48h - intracranial hemorrhage is most serious complication of thrombolytic therapy - but bleeding occur at any site of body = bleeding cocurs most commonly at access sites such as catheter insertion sites or venipuncture sites - patients with preexisting coagulation problems, uncontrolled hypertension, severe chronic heart failure, and recent stroke are at highest risk for developing bleeding complications during thrombolytic therapy - hemorrhage can result from concomitant therapy with heparin or other platelet-aggregation inhibitors = if severe bleeding occurs during therapy, drug should be discontinued PROMPTLY. - rapid coronary lysis can result in development of arrhythmias; however they are generally transient in nature |
What is hematopoiesis? = The formation, differentiation, and maturation of blood cells into specific cell lines - products of recombinant technology 2 types discussed in this book Erythropoiesis-stimulating agents (ESAs) = Responsible for regulation of the production and development of blood cells, normally in the bone marrow - Example: epoetin alfa (Epogen or Procrit) Colony Stimulating Factors (CSFs) |
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Erythropoiesis-Stimulating Agents (ESAs) - epoetin alfa (Epogen or Procrit) responsible for regulation of production and development of blood cells, normally in bone marrow. - Epoetin alfa stimulates bone marrow to produce more RBCs and approved for treatment of anemia in chronic renal failure, HIV infection and anemia associated with chemotherapy. - also reduces the need for blood transfusions in anemic patients scheduled to undergo certain kinds of surgery - Darbepoetin alfa (Aranesp) is a second-generation agent that is dosed LESS Frequently than Epoetin Alfa - Before initiating ESA therapy. supplemental iron (folic acid and or vitamin B12 if necessary) is usually needed because adequate iron stores are necessary to incorporate iron into hemoglobin - treatment of iron deficiency by regular use of iron improves erythropoiesis and response to ESA therapy. - as of march 2010, prescribers and hospitals must enroll in and comply with ESA APPRISE Oncology Program to prescribe and or dispense epoetin alfa to patients with cancer, recently FDA updated safety info in black box warning regarding use of ESAs: use lowest dose possible to gradually increase hemoglobin (HgB) concentration to avoid need for Transfusion |
Side Effects of epoetin alfa (Epogen) - hypertension (esp in dialysis patients) - flu-like symptoms - GI effects - Rash - Chest Pain - Increased mortality, MI, stroke, thrombosis, of vascular access, venous thromboembolic events, and increased risk of tumor progression or recurrence. |
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Colony Stimulating Factors (CSFs) - A granulocyte colony-stimulating factor (G-CSF), filgrastim (Neupogen), is involved in the regulation and production of neutrophils in response to host defense needs - Lessens severity of myelosuppression in cancer patients; has allowed chemotherapy dose intensification or maintenance of dose intensity * use with cautions in patients with sickle cell disorders |
Side Effects of filgrastim include - bone pain (common) - headache - dermatological reactions |
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Table 25-6 Platelet inhibitors, thrombolytic agents and hematopoetic agents Platelet inhibitors: aspirin, dipyradamole, dipyradamole with aspirin, ADP Receptor Antagonists, clopidrogrel, prasugrel, ticagrelor Thrombolytic agents: alteplase, tPA (Activase, Cathflo Activase) reteplase, r-PA (Retavase) tenecteplase, TNK-tPA (TNKase) Hematopoetic Agents (IV or subcutaneous) ESAs darbepoetin alfa (Aranesp) epoetin alfa (Epogen, Procrit) CSFs filgrastim, G-CSF |
Chapter 26 Respiratory System Drugs and Antihistamine page 543 |
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Respiratory diseases and disorders - According to the American Lung Association, lung disease is the third leading cause of death in the U.S. Respiratory diseases range from mild and self-limiting such as the common cold, to life-threatening such as bacterial pneumonia, pulmonary embolism, and lung cancer |
COPD chronic obstructive pulmonary disease: group of progressive lung disease - chronic bronchitis (inflammation of bronchial tubes, which leads to chronic mucus production and a wet cough) - emphysema (destruction of the tiny air sacs at the base of the lungs, diminishing the capacity and efficiency of the lungs to utilize oxygen, leading to shortness of breath and exercise intolerance) - COPD is a progressive disease that worsens with time and has systemic manifestations (including muscle wasting) (cigarette smoking is a primary cause of COPD, less often it is caused by long-term exposure to lung pollutants |
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Therapeutic measures for respiratory distress include Oxygen therapy Respiratory stimulants Bronchodilators Corticosteroids Mucolytics and expectorants Antitussives Smoking cessation |
Oxygen Therapy - Used therapeutically for hypoxia (insufficient oxygen supply to the tissues) - Decreases the workload of the heart and respiratory system (especially during distress) - Treats heart and lung diseases and some central nervous system (CNS) conditions with respiratory difficulty or failure - oxygen may be administered by endotracheal intubation , nasal cannula, various masks, tents and hoods |
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Oxygen Therapy Side Effects if oxygen delivered at too high a concentration or for prolonged periods of time without proper monitoring - hypoventilation (particularly with COPD; may cause CO2 retention and acidosis) - confusion - changes in the alveoli of the lungs - blindness (in premature infants) |
Precautions or Contraindications of Oxygen therapy - patients with COPD (high oxygen concentrations may cause hypoventilation or apnea (cessation of breathing) - after long-term oxygen therapy, patients should be reassessed periodically for the need of oxygen - danger of fire when oxygen is used. Oxygen is not flammable but does support combustion = smoking, matches, cleaning aerosols, and electrical equipment that may spark (e.g. electric razors, hair dryers, curling irons) are not allowed in rooms where oxygen is in use |
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Respiratory Stimulants - Caffeine citrate Treats neonatal apnea of prematurity - Theophylline Administered IV and orally to stimulate respiration in infants (as an alternative to caffeine) |
Bronchodilators Act by relaxing smooth muscles of the bronchial tree, relieving bronchospasm and decreasing the work of breathing - For symptomatic treatment of acute respiratory conditions such as asthma and some forms of COPD - Can be given orally, parenterally, and by inhalation = Metered dose inhalers (MDIs), dry-powder inhalers (DPIs), and small volume nebulizers (SVNs) - classification of bronchodilators: sympathomimetics (adrenergics), the anticholinergics (parasympatholytics), and xanthine derivatives |
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Bronchodilator Administration - can be given orally, parenterally, and by inhalation = inhalation route is preferred to minimize systemic adverse effects Metered-dose inhalers (MDIs) - popular due to easy use - efficacy - portability In past, all MDIs contained chlorofluorocarbon (CFC) as propellant (because of detrimental effects on ozone layer, use of CFC was phased out. some reformulated their MDI to contain hydrofluoroalkane (HFA) as the propellant, which has not been linked to depletion of the ozone layer and is nonflammable. - MDIs are frequently used and use of a spacer or reservoir device assists in optimizing drug delivery within the lungs |
Dry-powder inhalers (DPIs) - provide meds (esp corticosteroids and long-acting beta2 agonists) only under pressure of inspiration rather than through compression of the valve. Therefore, patient must be able to generate sufficient inspiratory effort on his or her own to deliver the meds, therefore device should not be used in acute respiratory distress. (this option is useful for patients who are unable to coordinate inspiration with actuation of a conventional MDI) |
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Small-Volume Nebulizers (SVNs) - create an aerosol mist of a drug solution that can then be inhaled into the lungs thru a mouth piece or a mask - aerosol is created by either compressed air or oxygen gas and optimal breathing pattern is a slow, deep breath, with a sustained breath hold; the aerosol should be delivered over an 9-12 min period |
Bronchdilators: Sympathomimetics (Adrenergics) - Potent bronchodilators that increase vital capacity and decrease airway resistance - work on smooth muscles in lungs to cause RELAXATION. - Examples: albuterol, epinephrine, salmeterol, and others |
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Sympathomimetics SABAs (short-acting beta-agonists) - albuterol = drug of choice for managing acute exacerbations of asthma AKA Rescue Medications LABAs (Long-acting beta-agonists) - salmeterol = used for prophylactic treatment AKA Maintenance Medications |
Side effects of adrenergics include potentiation of theophylline effects with increased risk of toxicity esp - GI (nausea, vomtiing, and decreased appetite) - Cough, throat irritation, hoarseness, and sinusitis with inhaled preps - CNS stimulation (nervousness, tremor, dizziness and headache) - Cardiac irregularities (tachycardia, palpitations, arrhythmias and angina) (Levalbuterol [Xopenex], an isomer of albuterol, may cause less cardiac stimulation and less incidence of certain systemic adverse reactions such as tremor and nervousness compared to albuterol; the clinical significance of these small differences are unknown) - hypertension - hyperglycemia and hypokalemia (caution with loop or thiazide diuretics) |
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Precautions or contraindications for adrenergics - first administration, which should be observed by medical personnel for hypersensitivity reactions - contacting the physician if decreased effectiveness occurs - close monitoring, if administrating oral inhaled adrenergics with other oral inhaled bronchodilators for cardiovascular effects - patients with cardiovascular or kidney disorders, diabetes, seizure disorders, or hyperthyroidism |
Due to prolonged onset of action, long-acting beta2 agonists (salmeterol) should NOT be used to treat acute asthma attack or bronchospasm. these are indicated only for asthma prophylaxis in combo with an asthma controller med such as inhaled corticosteroids - a short-acting beta2 agonist (albuterol) should alway be available for the RESCUE TREATMENT of an acute attack - when patients increase use of rescue inhalers is a sign of deteriorating asthma control - long-acting beta2 agonists have been associated with an increased of severe asthma exacerbations and asthma-related deaths |
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Anticholinergics (parasympatholytics) - Decrease the chemical that promotes bronchospasm - anticholinergics block the parasympathetic nervous system and can cause drying of pulmonary secretions - adequate hydration should be encrouaged to avoid mucus plugging - First-line therapy: inhaled anticholinergics for COPD once symptoms become persistent - Example: Atrovent |
Side effects of anticholinergics - cardiac effects (changes in heart rate and palpitations) - CNS stimulations (headache, drowsiness, dizziness, confusion and agitation) - Thickened secretions and mucus plugging; dry mouth and metallic taste - constipation and abdominal pain |
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Cautions: anticholinergics are not indicated for patients with unstable cardiac status, history of heart attacks, glaucoma, drug sensitivity, or prostatic hypertrophy - Tiotropium (spiriva) structurally similar to ipratropium (Atrovent) administered daily as maintenance drug in a dry-powder inhaler (DPI) (vs. three to four times daily for ipratropium) - more efficient than ipratropium for maintenance treatment of COPD and may lead to reduction in the use of sympathomimetics for. rescue therapy |
Bronchodilators; Xanthines Relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels - May possess anti-inflammatory actions - No longer a first-line treatment = due to Modest clinical effectiveness, the Need for serum monitoring, and Many adverse effects and drug interactions - Theophylline is generally reserved for patients with COPD who do not respond to or cannot take inhaled long-term bronchodilators = when used, xanthines are usually administered as sustained-release formulations with other respiratory system drugs (adrenergics and anticholinergics for additive effects on symptom relief and breathing functions) |
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Side effects of theophyllines (can be mild or severe with acute toxicity) - GI distress (nausea, vomiting, epigastric pain, abdominal cramps, anorexia, or diarrhea) to reduce gastric irritation take with MEALS - CNS stimulation (nervousness, insomnia, irritability, headache, tremors, and seizures can be fatal) - Cardiac effects (palpitation, tachycardia, arrhythmias, esp with rapid IV administration) - urinary frequency (mild diuresis) - hyperglycemia |
precautions and contraindications with administering theophylline apply - sudden cessation of tobacco smoking (may result in reduced clearance of theophylline and increased serum theophylline concentrations) - cardiovascular, kidney, pulmonary or liver dysfunction - diabetes, peptic ulcer, or glaucoma - children and older adults (more prone to toxicity) - patients undergoing influenza immunization or who have influenza - pregnancy and lactation |
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Interactions occur with - Cimetidine, allopurinol, erythromycins, quinolones, oral contraceptives, calcium channel blockers , and beta-blockers (increase theophylline levels) - smoking, barbiturates, phenytoin, and rifampin (decrease theophylline effective) - roflumilast or PDE-4 inhibitor |
Patient Education taking bronchodilators (e.g. adrenergics, anticholinergics, or the xanthines) should be - follow instructions on package regarding dosage and administration (dangerous side effects) - proper technique for inhaler use; capsules used with DPIs must not be swallowed - use of spacers for patients who have difficulty using MDIs - watching closely for cardiac irregularities or CNS stimulation (e.g. nervousness, tremor, dizziness, confusion, and headache) and reporting these symptoms to physician immediately - other side effects: possible with adrenergics and xanthines (ex: gastric distress insomnia, or hyperglycemia) - drinking adequate fluids to prevent mucus plugging, esp with anticholinergics - importance of quitting smoking and avoiding second-hand smoke, fumes, or pollution - asthma guidelines state that: OTC bronchodilators are NOT RECOMMENDED because the temporary relief provided may delay patient from seeking medical care - Avoiding any new meds including OTC drugs without consulting the physician first, because danger of serious complications, many interactions are possible - avoiding changing brands of meds without consulting physician or pharmacist) |
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Bronchodilators Sympathomimetics: - SABA (rescue meds) - albuterol sulfate (proair HFA, Proventil HFA, Ventolin HFA) - levalbuterol (Xopenex, Xopenex HFA) -LABA (maintenance meds) - arformoterol (brovana), formoterol (Foradil Aerolizer, Performist) - salmeterol (Serevent diskus) - other : epinephrine (adrenalin) racepinephrine (asthmanefrin(OTC)) Anticholinergics Short Acting - ipratropium bromide (Atrovent HFA, Atrovent) - ipratropium/albuterol (combo of anticholinergics and sympathomimetic) Long acting - tiotropium (Spiriva Handihaler) Xanthines - Theophylline (RTU infusion in D5q, Elixophyllin, Theo-24) |
Corticosteroids Synthetic corticosteroids - Relieve inflammation, reduce swelling, decrease bronchial hyper-responsiveness to triggers, and suppress symptoms in acute and chronic reactive airway disease (asthma and some COPDs) - Administered systemically (oral and injectable forms) for short-term “bursts” during exacerbations, and occasionally at the beginning of treatment until symptoms are controlled |
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Inhaled corticosteroids (SVN aerosol, DPI, MDI) - Preferred drug therapy in long-term prophylactic management of persistent asthma of various severities - regular long-term treatment reduces exacerbations, improves control of symptoms and lung function, and reduces hospital admissions and deaths from asthma - inhaled corticosteroids with long-acting beta-agonists are also used on regular long-term scheduled basis in patients with COPD to improve symptoms and quality of life - inhaled corticosteroids have less systemic side effects than oral or injectable administration |
Intranasal - Increasingly considered first-line therapy for most noninfectious types of rhinitis - Reduce congestion, edema, and inflammation - should be started before symptoms occur and taken regularly throughout the period of exposure. - Aerosol corticosteroid preparations seem to be more irritating (burning, sneezing), to the nasal mucosa. - Aqueous prep may drip into throat, result in reduced deposition of drug in nasal mucosa |
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Side effects of inhaled corticosteroids - throat irritation and dry mouth - hoarseness - coughing and dysphonia (hoarsness) - oral fungal infections (patients should be encouraged to rinse mouth with mouthwash or water after administration) - increased susceptibility to pneumonia |
Precautions or Contraindications with corticosteroids - viral, bacterial or fungal infections - hypertension or congestive heart failure - diabetes - hypothyroidism or cirrhosis - renal failure |
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Asthma Prophylaxis - Leukotriene inhibitors - Zafirlukast (Accolate) and montelukast (Singulair) = Oral leukotriene receptor antagonists for asthma prophylaxis, prevention of exercise-induced bronchoconstriction, and treatment of chronic asthma = Help control inflammatory process of asthma caused by leukotriene production, thus helping to prevent asthma symptoms and acute attacks - can be used as monotherapy or as add-on therapy in patients whose persistent mild to moderate asthma is inadequately controlled with inhaled corticosteroids. - Montelukast can be used in CHILDREN as young as 2 years old and has fewer DRUG INTERACTIONS compared to ZAFIRLUKAST |
Side effects of Singulair - headache, dizziness, nausea or dyspepsia, pain, fatigue, respiratory infections and fever , behavior or mood changes, sleep disturbances and suicidal ideation (both drugs) |
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Precautions or contraindications of Leukotriene inhibitors - hepatotoxicity (zafirlukast) - Pregnancy or lactation - treatment of acute episodes of asthma (these are not Rescue Medications) |
Leukotriene Inhibitors Drug interactions occur with - aspirin (increased levels of zafirlukast) - erythromycin and theophylline (decreased levels of zafirlukast) - Warfarin and zafirlukast (increased prothrombin time) - Phenobarbital and rifampin (decreased levels of montelukast) |
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Mast Cell Stabilizers - Rupture or degranulation of mast cells and subsequent spilling of their chemical mediator contents cause an inflammatory response that can lead to asthma - Stabilizing the mast cell membrane has anti-inflammatory actions that modify the release of mediators from mast cells and eosinophils - Example: cromolyn |
Mast Cell Stabilizers - prophylactic for asthma, Cromolyn was one of first classified mast-cell stabilizer -Cromolyn has no value in treatment of acute attacks of asthma - has been sued in prevention of exercise-induced bronchospasm - cromolyn is available as a solution for inhalation or a nasal solution (to treat seasonal allergic rhinitis) for use in adults and children as young as 2 years old - to be effective, follow directions on manufactureres |
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Side effects of cromolyn (mast cell stabilizer) can include - throat irritation, cough and bronchospasm - nose burning, stinging and sneezing (with nasal solution) - nausea or headache |
Cromolyn Caution applies to - those with cardiovascular disorders - proper use on a regular schedule |
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Patient ed for inhaled corticosteroids or asthma prophylaxis agents - these agents are not effective for ACUTE exacerbations of asthma or immediate proper symptoms - side effects to expect: such as throat irritation, dry mouth, and cough (rinse mouth and gargle to minimize) and with products administered nasally; for ex, nose burning, stinging or sneezing - complications of inhaled corticosteroids without proper precautions Ex: oral fungal infections (patient should be encouraged to rinse mouth with mouthwash or water after treatment and to always rinse and air dry equipment after use - reporting side effects to the physician esp respiratory distress - the importance of not smoking |
Mucolytics and Expectorants
Mucolytics - Decrease hypersecretion and increase thinning of pulmonary secretions - Example: acetylcysteine (Mucomyst) Neb Expectorants - Increase secretions, reduce viscosity, and help to expel sputum - Example: guaifenesin |
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Mucolytics - decrease hypersecretion of and liquefy pulmonary secretions - thick secretions can be a problem in patients with obstructive lung disease but little evidence that inhaled acetylcysteine is more effective than adequate hydration for thinning or increasing the clearance of secretions |
Precautions or contraindications for mucolytics apply to - asthma or a history of bronchospasm (IV administration or inhalation may result in acute bronchospasm or anaphylaxis) - respiratory insufficiency, inadequate cough mechanism or gag reflex depression (liquefied pulmonary secretions can occlude the airway if patient is unable to adequately clear secretions |
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Expectorants - Increase secretions, reduce viscosity, and help to expel sputum but like mucolytics offer little clinical benefit for patients - Example: guaifenesin (only agent approved for use as expectorant) (Mucinex, Robitussin) - adequate fluid intake is important to maintain normal fluid volume, but excessive fluid intake is of no value - Guaifenesin commonly combined in cough syrups for symptomatic management of productive "wet" coughs associated with upper respiratory tract infections, bronchitis, pharyngitis, influenza, and measles or coughs provoked by sinusitis, but evidence of benefit is lacking - expectorants should not be used for self-medications or persistent or chronic coughs such as those associated with smoking or COPD. - persistent cough may be indicative of a serious condition - if cough persists for more than a week, recurrent or is accompanied by a fever, a physician should be consulted |
Side effects of expectorants are infrequent (usually not serius at recommended doses ) - nausea, vomiting and diarrhea - drowsiness, dizziness and headache
- persistent or chronic cough - some asthmatics prone to bronchospasm - cardiovascular disease and hypertension, diabetes, glaucoma, hyperthyroidism and prostatic hypertrophy esp with combination products - pregnancy or lactation |
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Antitussives - Prevent coughing in patients not requiring a productive cough - Most produce cough suppression by acting centrally on the cough center located in the brainstem - Narcotic antitussive example: codeine - Nonnarcotic antitussive example: dextromethorphan |
Antitussives - divided into narcotic preparations (codeine and hydrocodone) and non-narcotic preparations (dextromethorphan) - Codeine (narcotic antitussive) widely sued as cough suppressant due to reduced incidence of side effects (respiratory depressant action and bronchial constriction) at antitussive doses as compared to morphine) - codeine is available behind pharmacy counter as an OTC cough medication - hydrocodone (another narcotic cough suppressant) has slightly greater antitussive activity compared to codeine but is more sedating |
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FDA strongest warning added to drug label of codeine-containing products about risk of codeine used to manage pain in children after a tonsillectomy and or adenoidectomy *some children died after given codeine in amounts that were within recommended dose range - codeine converted to morphine in liver by enzyme - some people are ultrarapid metabolizers who likely to have higher-than normal amounts of morphine in blood after taking codeine - high levels of morphine can result in difficulty breathing can be fatal. - also bear consideration when codeine used as antitussive |
Non-narcotic antitussives (e.g. dextromethorphan) - are used more frequently because they do not depress respirations, do not cause dependence and have few side effects at recommended doses - Benzonatate (Tessalon) chemically related to the local anesthetic tetracaine, suppress cough peripherally by anesthetizing receptors in alveoli of lungs, bronchi, and pleura, also acts centrally like other antitussives. - Diphenhydramine (Benadryl) a first generation antihistamine, is also used as a cough suppressant |
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Side effects of antitussives - respiratory depression (large doses or excessive use) - constipation - urinary retention with narcotic antitussives - sedation and dizziness - nausea and vomiting |
Precautions or contraindications for antitussives apply - addiction-prone patients - asthma; COPD - other CNS depressants |
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Caution for antitussives with children - some CNS side effects, behavioral disturbances, and respiratory depression reported, esp with large doses - ester-type anesthetic (e.g. tetracaine) hypersensitivity with benzonatate
- triptans used for migraine head - Monoamine oxidase inhibitors MAOIs resulting in "serotonin syndrome" (applies to benzonatate as well) - THe SSRIs fluoxetine and paroxetine (reduce dextromethrophan dose) - memantine (Namenda) Recommended use of cough suppressants in coughs associated with upper respiratory infection (URI) because of their limited efficacy - recommended that patients experiencing cough associated with common cold or postnasal drip associated with a URI use a first generation antihistamine and a decongestant to treat cough |
table 26-5 Antitussives page 557 Narcotic - codeine with guaifenesin (Cheratussin AC) - codeine wih promethazine (Phenergan) with codeine - hydrocodone with homatropine (Hydroment) - Hydrocodone with chlorpheniramine (Tussionex) **** Antitussive dose is lower than required for analgesia, any cough meds containing a controlled substance is not for extended use, can develop physical dependence and tolerance (watch for side effects) |
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Non-narcotic - benzonatate (Tessalon) - dextromethrophan (Delsym) - with guaifenesin (Rubitussin DM) - Diphenhydramine (Benadryl) (antihistamine with anticholinergic effects esp drying)* |
Antihistamines Competitively antagonize the histamine1 receptor sites - Combat the increased capillary permeability and edema, inflammation, and itch caused by sudden histamine release = To treat allergy symptoms - used to treat symptoms of allergies (eg. rhinitis, conjunctivitis, and rash) - also used to reduce nasal secretions in common cold, the consequent thickening of bronchial secretions may result in further airway obstruction esp with COPD and asthma - H1-blockers are grouped into 2 categories: First generation: diphenhydramine (Benadryl) Second-generation: fexofenadine (Allegra) and loratadine (Claritin) |
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First Generation these antihistaines (diphenhydramine (benadryl) were first group of meds available to treat symptoms of allergies - diphenhydramine approved as an antitussive, nighttime sleep aid and antiemetic. , adjunctive treatment of anaphylactic reactions after acute symptoms (e.g. laryngeal edema and shock) have been controlled with epinephrine and corticosteroids - some antihistamines used in symptomatic treatment of vertigo associated with pathology of middle ear or in prevention and treatment of motion sickness |
Side effects of first-generation antihistamines are primarily anticholinergic in action - drying of secretions, esp of the eyes, ears, nose and throat - sedation, dizziness, tachycardia, hypotension, esp in older adults - muscular weakness and decreased coordination; cognitive impairment - urinary retention and constipation - visual disorders - paradoxical excitement, insomnia, and tremors, esp in children* - GI effects: nausea, vomiting, and anorexia - nasal irritation, epistaxis, and bitter taste with nasal spray |
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Precautions or contraindications for first-generation antihistamines apply to - Persons operating machinery or driving - older adults (extended half-life with sedation) - closed-angle glaucoma - cardiovascular disorders - benign prostatic hyperplasia (BPH) - children under the age of 6 years - pregnancy and lactation - seizure disorders |
Interactions of first-generation antihistamine may occur with - potentiation of CNS depression with tranquilizers, analgesics, hypnotics, alcohol, and muscle relaxants |
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Patient ed taking first-generation antihistamines - avoid frequent or prolonged use of antihistamine (may cause increased bronchial or nasal congestion and dry cough - not using antihistamines to sedate children - no self-medication (check with physician first) in those with COPD or cardiovascular disorders, BPH, older adults and children - taking care in driving or operating machinery because of sedative effect - not mixing with alcohol or any other CNS depressants drugs |
Second generation - fexofenadine (Allegra) and loratadine (Claritin) - selective (have greater specificity for) histamine1 receptor antagonists and have FEWER CNS effects Ex: less sedation, less anticholinergic effects compared to FIRST-Generation antihistamines - agents can cause little or no sedation, important to note the incidence of sedation is not zero. They are used to provide symptomatic relief of seasonal allergic rhinitis for ex hay fever - second-generation antihistamines are not effective in treatment of cough |
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Side effects of second generation antihistamines usually mild - headache, dizziness, fatigue, and drowsiness (esp cetirizine) - dry mouth and pharyngitis |
Precautions or Contraindications for second generation antihistamines apply to - asthma - renal and hepatic impairment - hydroxyzine (Vistaril) allergy with Zyrtec - driving or operating machinery - pregnancy or lactation - children less than 2 years of age |
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Patient ed for second-generation antihistamines - avoid any other drug including OTC, without consulting physician first - report symptoms (fainting, dizziness, or palpitations to physicians immediately) - using caution with driving or operating machinery until you know how these drugs affect you |
Precautions or contraindications for decongestants - cardiovascular disorders - hyperthyroid or diabetes - older adults- esp those with glaucoma or BPH - pregnancy or lactation |
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Interactions of decongestants may occur with - potentiation of adverse side effects with other adrenergics, ergot, tricyclics, MAOIs. |
Patient ed for decongestants - using decongestants for only a few days (3 days for nasal; seven days for oral) to avoid rebound congestion - avoiding when cardiac or thyroid conditions or diabetes are present - discontinuing with side effects such as nervousness, tremor, palpitations, or headache - avoiding combining with any other meds without consulting the physician |
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First generation Antihistamines - azelastine (Rx) (Astelin, Astepro) - chlorpheniramine (Chlor-Trimeton, Aller-Chlor) - clemastine (Rx/OTC) (Tavist Allergy) - diphenydramine (Rx/OTC) (Diphenhist) (Benadryl Allergy, Benadryl) Second Generation Antihistamine - certirizine (Zyrtec) - deslsoratadine (Rx) (Clarinex) - fexofenadine (Allegra) - Levocetirizine (rx) (Xyzal) - Loratadine (Claritin, Alavert) Decongestants - oxymetazoline (Afrin) - phenylephrine (Neo-Synephrine) (sudafed PE) |
Safety of cough-cold allergy products - Many cough and cold formulations combine several drugs (antitussives with expectorants, antihistamines, and decongestants to treat two or more simultaneous symptoms - combination formulations should be used only if corresponding symptoms is present and each individual component is available in proper strength and dosing interval patient need - Use only if the corresponding symptom is present and each individual component is available in the proper strength and dosing interval a patient may need - Caution patients to seek advice from a healthcare professional familiar with each ingredient, and avoid duplicant of therapy and potential for inadvertent overdose |
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FDA's nonprescription drug and pediatric advisory committee foung that there was no proof that theses meds eased cold symptoms in children while there were reports that they caused serious adverse effects, overdose and even deaths |
Patient ed taking respiratory system drugs should be - use of appropriate nondrug measures for patient's particular symptoms - care in taking meds only as prescribed and required; do not give children medicine labeled only for adults - use and safety concerns of combination products - avoid combining respiratory system drugs with other prescription or OTC drugs or alcohol, which could potentiate CNS stimulation or depression, result in serious side effects - choosing OTC couch and cold meds with child-resistant safety caps, using only measuring devices that come with product or made for measuring - avoid self-medication when cardiac, thyroid or CNS conditions present - benefits from desensitization therapy and air-conditioned environmental control for patients with allergic condition - avoiding air POLLUTION (e.g. smoked-filled rooms) - importance of receiving (and safety of ) inactivated influenza vaccination in adults and children with asthma which can reduce serious illness, complications and mortality - proper use of inhalers when prescribed (see admin with inhalers), - not crushing chewing or breaking extended-release preparations, swallow WHOLE |
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Smoking Cessation Aids - Nicotine replacement therapy = Help lessen withdrawal symptoms by slowly lowering the level of nicotine in the body = Examples: Nicorette gum, Commit lozenges, Nicoderm CQ patch, and Nicotrol inhaler and nasal spray - |
Smoking cessation Aid - Nicotine Nicorette, Commit, Nicoderm CQ, Nicotrol NS (Rx), Nicotrol Inhaler (Rx) - Bupropion (Zyban Rx) - varenicline (Chantix Rx) |
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Side effects of nicotine replacement products (could be related to nicotine withdrawal symptoms) - mechanical problems with chewing gum, especially if the patient has dentures - cardiac irritability - chewing too fast (may cause lightheadedness, nausea, heartburn, vomiting, and throat and mouth irritation) skin reaction at the application site |
Precautions or contraindications for nicotine replacement products - dental problems that might be exacerbated by chewing gum - drug abuse and or overdependence - overdosage- studies have shown that combination therapy (nicotine patch plus one other form of nicotine replacement), is more effective if unable to quiet using a single agent but little safety data on this, combination therapy, may increase risk of nicotine overdose - pregnancy and lactation - unstable cardiovascular disease - patients should be warned not to smoke - proper disposal to avoid accidental ingestion by children and pets |
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Bupropion - oral antidepressant drug (Wellbutrin) also prescribed as an aid to smoking cessation (marketed as Zyban) and has associated to decrease cravings for cigarettes and lessening of nicotine withdrawal. - Zyban is indicated for use in combinations with nicotine patches for treating the symptoms of nicotine withdrawal Oral antidepressant drug (Wellbutrin) - Associated with decreases in cravings and lessening of nicotine withdrawal |
Varenicline (Prescription only) Partial nicotine receptor agonist-antagonist - Alleviates symptoms of nicotine craving and withdrawal through agonist activity while inhibiting the effects of repeated nicotine exposure by its antagonist activity - Eliminates the pleasurable feelings associated with smoking - mild to moderate nausea and vomiting, sleep disturbance and abnormal dreams are the most common side effects with nausea and vomiting occurring in nearly one third of patients (take after a meal with fluids) = no clinically significant drug interactions have been identified - have been reports of serious neuropsychiatric symptoms (changes in behavior, agitation, depressed mood, and suicidal ideation and behavior associated with varenicline - safety and efficacy of varenicline in pateients with serious psychiatric disorders such as schizophrenia, bipolar and major depression has not been established. - patients and caregivers should be aware of need to monitor for these symptoms and report immediately to physicians |
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Decongestants - Constrict blood vessels in the respiratory tract = Results in shrinkage of swollen mucous membranes and helps to open nasal airway passages - Frequently combined with antihistamines, analgesics, caffeine, and/or antitussives = Examples: phenylephrine (Neo-Synephrine) or pseudoephedrine (Sudafed) |
the end |
