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159 Cards in this Set
- Front
- Back
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Importance of a lipid...
Importance of cholesterol... precursor to... Triglycerides are composed of...used for... Term for: High lipids & lipoproteins... High cholesterol... High triglycerides... |
-Necessary for human life
-Essential to cell membrane -Sterol, steroid compounds -Fatty acids and glycerol -High energy -Hyperlipidemia/ Hyperproteinemia -Hypercholesterolemia -Hypertriglyceridemia |
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Hypercholesterolemia:
Contributes to... Associated w/... Hypertriglyceridemia: Associated w/... Risk factors for CHD... |
-Arthrosclerosis
-CAD -Pancreatitis, arthrosclerosis & heart disease -Smoking -HTN -Low HDL (<40mg/dL) |
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Normal Cholesterol Levels:
Total... HDL... LDL... Triglycerides... |
- <200 mg/dL
- >60 - <100 - <150 |
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STATINS:
Also called... Have low what... due to... Prodrugs include... Active drugs include... Mechanism of action... |
-HMG-CoA Reductase Inhibitors
-Bioavailability, due to extensive 1st pass metabolism -Lovastatin and Simvastatin -Atorvastatin, Fluvastatin, Pravastatin, Rosuvastatin -Inhibits the enzyme HMG-CoA reductase, which catalyzes a step in cholesterol synthesis |
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STATINS:
In pts w/ hypercholesterolemia, actions by statins are... Other therapeutic effects... |
-Decrease of 20-40% of serum LDL level
-Increase of 10% in HDL level -decrease VLDL and triglycerides -Slow progression of CAD -Decrease in MI and stroke and decrease in need for myocardial revascularization |
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Adverse Effects of Statins:
Most frequent problem is... A less frequent effect... More serious ADE is... |
-GI problems (Cramps, constipation, diarrhea, and heartburn)
-Hepatitis- due to elevated serum levels of hepatic enzymes -Rhabdomyolysis- potentially fatal form of statin-induced skeletal muscle toxicity (myopathy) |
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Drug Interactions w/ Statins:
Fibric acid derivatives can cause... Erythromycin and itraconazole can... Statins can also interact w/...Increase levels of... |
-Myopathies (avoid use of these drugs w/ statins or use w/ great caution)
-Inhibit the metabolism of statins and increase the incidence of adverse effects -Drugs that are metabolized by cytochrome P450 -Increase warfarin levels by inhibiting warfarin metabolism |
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Indications to use Statins:
Used for what... How does it compare to other drugs... Most potent statin currently available is... followed by... Most statins taken when...why? Lovastatin taken when...why? Others taken how... |
-To reduce bld cholesterol levels in pts w/ hypercholesterolemia
-Reduces levels to greater extent than any other drug -Rosuvastatin is most potent, then Atorvastatin -Evening or bedtime to inhibit nocturnal cholesterol biosynthesis -Taken w/ evening meal, facilitates w/ absorption -w/o regard to food |
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Atorvastatin:
Brand name... Dose... Fluvastatin... Lovastitin... Pravastatin... Rosuvastatin... Simvastatin... |
-Lipitor
-10-80 mg/d -Lescol -20-80 mg/d -Mevacor -10-80 mg/d (IR) -10-60 mg/d (ER) -Pravachol -10-80 mg/d -Crestor -5-40 mg/d -Zocor -5-80 mg/d |
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Potentcy of statins...
How to dose statins... Re-check labs how often... |
-Crestor
-Lipitor -Zocor -Start w/ low doses and titrate up -Every 2-3 weeks |
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DRUGS FOR HYPERLIPIDEMIA:
Fibric Acid Derivaties... Other agents... |
-Fenofibrate (Tricor)
-Gemfibrozil (Lopid) -Nicotinic Acid (Niacin) |
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Fibric Acid Derivatives:
Primarily used to treat... Which is largely obsolete...why... Which ones are currently available... Mechanism of action: Reduces levels of... Increases levels of... Which causes greater reduction in LDL... |
-Hypertriglyceridemia or marked HDL deficiency
-Clofibrate -Gemfibrozil and Fenofibrate -Reduces plasma levels of VLDL, triglycerides and LDL -Increases levels of HDL -Fenofibrate more than Gemfibrozil |
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Adverse Effects of Fibric Acid Derivatives...
Interactions: Fibrates can be given w/... Separate doses how... why... |
-Hypersensitivity reactions
-GI effects (nausea, diarrhea, liver irritation, gallstones) -Rhabdomyolysis and other myopathies -Cholestyramine and colestipol -By more than 2 hours b/c they reduce fibrate absorption |
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Indications to use Gemfibrozil:
Primarily indicated for tx of... Use in what type of pts... Brand name... Dose... |
-Hypertriglyceridemia
-Pts w/ hypertriglyceridemia and hypercholesterolemia. -And can be given to increase HDL in pts w/ HDL deficiency -Lopid -600 mg BID |
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Indications to use Fenofibrate:
Used in treatment of... Brand name... Dose... |
-High triglyceride levels and mixed hyperlipidemia w/ elevated triglyceride and cholesterol levels
-Tricor -48-145 mg/d |
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Nicotinic Acid (Niacin):
Drawback is... but still valuable in tx of pts w/... Also known as... Absorbed how... |
-Many adverse effects
-Hyperlipidemia -Vitamin B3 -Well absorbed from gut and extensively metabolized before renal excretion |
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Mechanism of Action of Niacin:
Type of doses required... These doses produce effects similar to... Acts by what... How does it effect HDL and LDL... |
-Large doses for pharmacologic effect
-Fenofibrate -Inhibiting synthesis and secretion of VLDL, the major carrier of plasma triglycerides, and the precursor to LDL -Also inhibits lipolysis -It can decrease serum LDL, but also significantly increase HDL |
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Adverse Effects and Interactions of Niacin:
Large doses can cause what... This can be reduced by... Niacin also produces...may activate... Can also cause what...and aggravate what... |
-Marked vasodilation, flushing of the skin, w/ pruritis and a warm, tingling feeling
-Pretreatment w/ aspirin or sustained release niacin -Gastric distress and may activate a peptic ulcer -Glucose intolerance -Diabetes mellitus |
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Indications to Take Niacin:
Nicotinic acid is an effective drug for tx of... Can also be used in tx of... Brand name of Niacin... Dose... |
-Mixed hyperlipidemia
-Hypertriglyceridemia or hypercholesterolemia -Niaspan -500-2000 mg/d |
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Examples of Bile Acid Binding Resins...
Example of Cholesterol Absorption Inhibitor... |
-Chlestyramine
-Colestipol -Colesevelam (Welchol) -Ezetimibe (Zetia) |
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HTN:
How many ppl in US have it... White adults in US... Black adults in US... Over 50% are over age of... What % have a specific cause... % w/ primary HTN... % who don't know they have it... % of all HTN pts not on therapy... % on inadequate therapy... Higher incidence of HTN in what type of ppl... |
-50 million
-20% -30% -65 yrs old -15% -85% -35% -52% -27% -ppl w/ lower education and income |
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HTN is defined as...
Classifications: Normal: Systolic... Diastolic... High normal... Stage 1 HTN... Stage 2 HTN... Stage 3 HTN... |
-Sustained systolic pressure of 140mmHg or higher OR
-A sustained diastolic pressure of 90mmHg or higher - <130 - <185 -130-139 -85-89 -140-159 -90-99 -160-179 -90-99 - >= 180 - >= 110 |
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Untreated HTN can cause...
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-Damaged bld vessels
-Accelerates arteriosclerosis -LVH -Ischemic HD -Stroke -Heart and renal failure |
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HTN Types:
Essential HTN (Primary): Classified as... Accelerated Malignant HTN: Defined as... Associated w/... Isolated Systolic HTN: Classified as... Occurs when... |
-Stage 1-2 (DBP 90-104) in 80%
-Recent substantial BP increase -Retinal vessel damage -DBP>140 -SBP >160 -DBP <90 -5th decade, 11% > 75yrs old |
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Life Style Changes for Managing HTN...
Diet changes... |
-Loose wt. (may normalize w/ 10lb wt loss)
-Limit alcohol to <1oz/day -Aerobic exercise (3/week for 30mins) -Stop smoking -Reduce stress -Low salt, cholesterol & saturated fat -High fiber, potassium -Increase fruits & vegetables -Reduce SBP 5.5-11.4 and DBP 3-5.5 |
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Sodium Restriction:
Amount of salt allowed in a NO salt diet... Done w/ what conditions... Restricted diet w/ what conditions... |
- <3000-4000mg (135-138 meq/day)
-Hypertension -CHF -Acute or chronic renal failure -Liver cirrhosis or failure -Moderate to severe CHF |
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Monotherapy of HTN...
Agents to avoid as monotherapy... Agents to avoid if non-compliance rebound HTN occurs... |
-Diuretics (HCTZ initial choice)
-Beta blockers -ACE Inhibitors -ARB's -Alpha blockers -Hydralazine -Minoxidil -Beta blockers -Clonidine |
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THIAZIDE DIURETICS:
Indications to use... MOA... Efficacy when used alone... |
-1st line against HTN
-Heart failure (adjunct to loop) -Inhibits Na reabsorption, causing increased excretion of Na & H20 (as well as K & H ions) -Decrease peripheral resistance -10-15 mmHg |
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Indications of Thiazide Diuretics:
Used in pts w/... Most frequently what... Not useful for who... Adverse effects... |
-Mild to moderate HTN
-Antihypertensive in US -Pts w/ renal insufficiency (CrCl <40ml) -Hyperuricemia (occurs w/ doses >25mg)- avoid w/ gout -Hypokalemia-food replacement -Hyponatremia -Hypomagnesemia -Hyperglycemia -Hyperlipidemia |
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THIAZIDES:
Hydrochlorothiazide: Brand name... Dose... HCTZ and Triameterene... Chlorothiazide... Chlorthalidone... Indapamide... Metolazone... |
-Esidrex, Hydrodiuril
-12-25mg PO daily -Dyazide -25-50 PO daily -Maxide -50-75 PO daily -Diuril -125-250mg PO daily or BID -Hygroton -12.5-25mg PO daily -Lozol -1.25-5mg PO daily -Zaroxolyn -0.5-1mg PO daily |
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LOOP DIURETICS:
Mechanism of action... Action compared to thiazides... Effects... |
-Inhibits reabsorption of Na & Cl at ascending loop of Henle
-Shorter duration of action -Direct venodilation (in pulm edema) by reducing venous return (preload) and central venous pressure -Reduces intravascular volume (CO) |
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Indications to use Loop...
Lasix indicated for... |
-HTN pts refractory to thiazides
-Reduce pulmonary & peripheral edema (in renal insufficiency and HF) -Management of pulm congestion (LV dysfunction in CHF) |
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Furosemide:
Brand name... Initial dose PO... Initial dose IV... Infusion dose... Infusion LD... Max dose... Duration... |
-Lasix
-20-40 mg PO daily or BID -20-40 mg IV -0.25-0.75 mg/kg/hr -40mg, then 10-40 mg/hr IV -600 mg/day PO -6-8 hrs -Diuresis = 10 mins |
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Bumetamide:
Brand name... Initial dose PO... Initial dose IV... Infusion LD... Infusion MD... PO Max dose... IV Max dose... Duration... |
-0.5-1mg PO BID
-1mg IV/dose -1mg IV -0.5-2mg/hr IV -10 mg/day PO -4-8 mg IV/dose -4-6 hrs |
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Torsemide:
Brand name... Initial dose... IV dose... Infusion LD... Infusion MD... PO Max dose... IV Max dose... Duration... |
-Demadex
-10-20 mg PO daily -10 mg IV -20 mg -5-20 mg/hr -200 mg/day PO -100-200 mg/day IV -12-16 hrs |
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Adverse Effects of Loop Diuretics...
Thing to remember w/ loop when starting ACE-i... |
-Volume depletion- dehydration
-Hypotension -Hypokaemia -Hyponatremia -Hypomagnesemia -Hypocalcaemia -Renal Dysfunction -Hold or reduce dose |
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Loop Diuretic Resistance can be due to...
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-Renal Insufficiency (EX: NSAIDs)
-Decrease oral absorption -Structural changes in kidney(EX: distal tubal hypertrophy (add thiazide)) -Increase Na intake (in CHF patients –avoid Na retainer) |
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Examples of K sparing diuretics...
Exmaples of K sparing diuretics and ALDO antagonist... |
-Amiloride (midamor)
-Triameterne (Dyrenium) -Spirinolactione (Aldactone) -Eplerenone (Inspra) |
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Spirinolactone:
What is it... MOA... How is it eliminated... Half life... |
-An ALDO competitive inhibitor
-Increases NaCI & H20 excretion of distal renal tubule, while increasing K & H ions -Renal -14-16 hrs |
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Indications to use Spirinolactone...
Contraindications to use it... |
-L sided CHF- 1st line with ACE-i
-Refractory HTN- combo therapy Edematous States: -Cirrhosis of liver -Nephrotic Syndrome -Primary hyperaldosteronism -Anuria -Renal insufficiency (SCr >2.4) -Hyperkalemia |
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Drug Interactions w/ Spirinolactone...
Dose for CHF... Dose for HTN... Dose for edema... |
-Hyperkalema- w/ NSAIDs, ACE-i, and K supplements
-Increases Digoxin t1/2 -25-50mg PO QD -12.5-50mg PO QD -50-200mg/d (1 or 2 doses) |
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Eplerenone (Inspra):
What is it... Different from spirinolactone how... Indications to use it... Contraindications to not use it... |
-An ALDO receptor antagonist
-More selective for ALDO -CHF -HTN -Hyperkalemia -Renal insufficiency -SCr >2 in men, >1.8 in women, or Crcl<50 mls |
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Adverse Effects of Eplerenone (Inspra)...
Drug Interactions... Dose for CHF... Dose for HTN... |
-Hyperkalemia
-Hyponatremia -Hypertriglycerdemia -Dizziness and Fatigue -Diarrhea -Cough -K supplements -ACE-i -Cytochrome P450 inhibitor –ketoconazole -Initial 25mg PO QD, max 50mg -Initial-50mg PO QD, max 50mg BID |
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Triamterene (Dyrenium):
Type of activity... Adverse effects... Drug interactions... |
-Weak antihypertensive activity of its own
-Hyperkalemia, GI disturbances -NSAIDs -ACE-i's |
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ACE INHIBITORS:
Type of drug... Indications to use it... |
-Angiotensin receptor blocker
-HTN- useless pt has low renin (blacks). They respond better to diuretics -MI- start w/in 24hr of Anterior wall MI -Reduction in CHF death and lower mortality in1 yr -CHF- LV systolic dysfunction -Diabetic nephropathy -Renal insufficiency |
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Adverse Effects of ACE-i's...
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-Cough- (5-20%)- common in women, blacks
-Relief w/ inhalers- (Cromolyn 20mg QID, Tilade 2puffs QID) -Hyperkalemia-5% -Teratogenic -2nd or 3rd trimester -Hypotension – reduce dose -Angioedema, rash |
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Captopril:
Brand name... Initial dose... Max dose... Enalapril... Lisinopril... |
-Capoten
-6.25mg PO TID -50mg -Zestril -2.5mg PO BID -10-20mg -Prinivil,Zestril -2.5mg PO QD -20-40mg |
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Fosinopril...
Benazepril ... Moexipril... |
-Monopril
-2.5-5mg PO QD -20-40mg -Lotensin -10mg PO QD -20-40mg -Univasc -7.5mg PO QD -30-40mg |
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Perindopril ...
Quinapril ... Ramipril ... Trandopril ... |
-Aceon
-2mg PO QD -8-16mg -Accupril -5mg PO BID -20mg -Altace -1.25mg-2.5mg PO QD -10mg -Mavik -1mg PO QD -4mg |
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BETA BLOCKERS:
MOA... Cardiac effects... |
-Block b-adrenergic receptors & inhibit effect of circulating catecholamines
-Negative ionotropic and chronotropic - Reduce BP -Decrease myocardial O2 demand -Antiarrhythmic effects |
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Indications to use b-blockers...
Contraindications... Adverse Effects... |
-HTN, MI
-A-fib -CHF (carvediol) -Refractory arrhythmia (V-tach, V-fib) -Migraine prophylaxis -Reactive airway disease (asthma, COPD) -Acute CHF exacerbation -AV nodal blockade -Hypotension, fatigue -Bradycardia (give atropine) -Bronchospasm (aminophylline) |
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Selective b-blocker agents...
Non Selective Agents... |
-Atenolol (Tenormin)
-Dose 50mg PO QD (max 100mg/day) -For AMI: 5mg IV over 5mins (repeat in 10mins) -Metoprolol (Lopressor) -Esmolol (Brevibloc) -Propranol (Inderal) -Carvediol (Coreg) -Timolol (blocadren)- 10mg PO BID (Max 60mg/day) -Nadolol (Corgard)- 40mg PO QD (Max 320mg/day) |
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CA CHANNEL BLOCKERS:
MOA... Adverse Effects... |
-Inhibits Ca influx into vascular smooth muscle
-Relax peripheral arteriole smooth muscle, so reduces total peripheral resistance -Short Acting- MI risk (60%) -Long acting- no increased risk -High Incidence of GI hemorrhage in elderly (platelet aggregation) -Bowel changes -Flushing, nausea, nasal congestion |
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Monotherapy:
Diltiazem: Brand name... Action... Side effects... Verapamil: Brand name... Greatest effect where... Sid effects... |
-Cardizem
-Intermediate effect on heart & bld vessels -Dizziness, headache, edema, bradycardia -Calan -Greatest effect on heart -Dizziness, headache, edema, bradycardia constipation |
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Nifedipine:
Type of therapy.. used for... Brand name... Type of drug... How does it compare to verapamil or diltiazem... Side effects... Drugs used for Bradycardia or LV dysfunction... |
-Combination therapy w/ b-blocker for CAD
-Procardia -A dihydropyridine, relatively selective vasodilator -Less cardiac depression -Tachycardia, headache, peripheral edema, flushing -Amlodopine (Norvasc) -Felodopine -Isradipine |
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HTN Emergencies:
Nitroglycerin: Causes what... Which type is preferred...why? Dose by IV... |
-Relaxation of vascular smooth muscle, which decreases BP
-IV over oral or transdermal b/c it is easily titrated -IV 5-10 mcg/min -Titrate dose to a 10% reduction in MAP or limiting side effects of hypotension (>30% reduction in MAP or systolic BP <90) |
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Nitroprusside:
Dose... Average dose... Adverse Effects... |
-0.3-10mcg/kg/min
-3mcg/kg/min -Cyanide toxicity -Hypotensive episodes -Increased intracranial pressure -Bowel obstruction -Cardiac dysrhythmias |
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Central Acting Agents:
Examples... Drawback of these... Not recommended for what... Adverse Effects... |
-Clonidine (comes in short acting and patch)
-Methyldopa -Guanfacine -More side effects than other antiHTN agents -Inital Rx of most HTN pts -Sedation, dry mouth -Rebound HTN- clonidine -Hemolytic anemia and Hepatitis- Methyldopa |
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ANGINA:
Definition... 3 types of angina... |
-Chest pain due to a reduced perfusion of the heart, which doesn’t meet metabolic demands
-Classic (Effort or stable) -Variant (Prinzmetal's) -Unstable |
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Classic (Stable) Angina:
Pain associated w/ what... Have w/ presence of... Have pain when... |
-Increased work or emotional stress
-Coronary disease (atherosclerosis) -No pain at rest, even if coronary artery may be partially concluded |
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Variant (Prinzmetal's) Angina:
How common... Pain when... No evidence of... Caused by...which reduces what... Mechanism... |
-Less common than stable angina
-Pain experienced at rest or during sleep -CAD -Coronary vasospasm -Bld flow to the heart when large coronary arteries are consticting -Is unknown, may be due to circulating vasoactive substances |
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Unstable Angina:
Most dangerous form b/c... Pain when... An extension of... |
-It indicates that MI is about to happen
-Experienced at rest (comes & goes) and with effort -Classic angina |
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Treatment of Classical Angina:
Objective of therapy is to... B/c why... |
-Reduce the myocardial O2 therapy demand
-There is already max bld flow- not possible to increase it more - |
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Ways to Decrase O2 demand w/ Classical Angina...
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-Decrease preload (use vasodilators)
-Reduce myocardial contractility (use Β-blockers) -Decrease afterload (use Ca channel antagonists) |
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Examples of Organic Nitrites and Nitrates...
Example of Ca channel blockers... |
-Amyl Nitrite
-Isosorbide dinitrate -Isosorbide Mononitrate -Nitroglycerin -Amlodopine (Norvasc) -Nifedipine (Procardia) -Bepridil (Vascor) -Diltiazem (Cardiazem) -Verapamil (Calan) |
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Examples of B-adrenergic Receptor Antagonists...
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-Atenolol (Tenormin)
-Metroprolol (Lopressor) -Nadolol (Corgard) -Propranolol (Inderal) |
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Amyl Nitrite:
Most rapid what... Shortest what... Special how... Administered how... Dose... Effective in the tx of... |
-Onset of action (~30 sec)
-Duration of action (3-5 mins) -Only nitrite compound used to tx angina -Inhalation -2-6 inhalations, nasally, repeat q3-5mins PRN -Acute anginal attack and in initial management of cyanide poisoning |
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MOA of Nitrites...
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-Reduces systemic and pulm arterial pressure (afterload) & decreases CO because of peripheral vasodilatation
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Amyl Nitrite:
MOA w/ cyanide toxicity... |
-Nitrites oxidize hemoglobin to methhemoglobin
-Methhemoglobin has an affinity for cyanide -Traps compound in the form of cyanomethemoglobin -Thiosulfate then administered to convert cyanide to inactive thiocyanate |
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Organic Nitrates:
Type of drugs... Onset and duration of action... |
-Prodrugs which produce nitrous oxide (NO2), a powerful vasodilator
-Vary w/ physical properties and route of admin |
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NITRATES:
Isorsorbide compounds: MOA... Examples of these compounds... Nitrates are soluble where... Administered how... Type of onset and duration... |
-Relaxes vascular smooth muscles, resulting in dilatation of peripheral arteries and veins
-Isosorbide Mononitrate (Imdur, Imdur ER, Ismo) -A metabolite of Isosorbide Dinitrate -Isosorbide Dinitrate (Isordil) -In H20 and lipids -SubL, oral, or transdermal -Slowest onset and longest duration |
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NITRATES:
Nitroglycerin (NTG): Type of onset and duration... Metabolized how... Indication to use nitrates... Administered how... |
-Intermediate
-Extensively metabolized by the liver -Prevention and tx of anginal attacks -Rapid dissolution & absorption after SL or buccal adm. |
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NITRATES:
Mechanism of Action... This leads to... Nitrates reduce what... |
-Releases nitrous oxide in vascular smooth muscle cells and relaxes it
-Nitric oxide also has small effect on arteriolar smooth muscle -Venous pooling of bld, decrease in venous bld return to the heart, decrease in ventricular volume & wall tension -Reduce cardiac work & O2 demand. Reduce preload, reduce CO, thereby reduces BP |
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NITRATES:
Tolerance results from... Occurs w/ what types... Tolerance can be prevented by... |
-Continuous administration
-IV, PO, & transdermal admin, and sustained release formulas -Remove skin patches for at least 10hrs daily -Give long acting oral meds 1-2x/daily |
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Adverse Effects caused by excessive vasodilation...
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-Headache
-Hypotension -Dizziness -Reflex tachycardia |
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Tachycardia as an Adverse Effect:
Tachycardia increases what... So be sure to avoid what... To prevent reflex tachycardia, what can be given... |
-Increases O2 demands, counteracting beneficial effects of nitrates
-Excessive doses of nitrates --Β-blocker (synergistic therapeutic effect) |
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Nitroglycerin is available in what formulations...
Used to prevent what... |
-Sublingual- used for acute attacks
-Oral (SR) capsules- used to prevent angina; undergoes first pass effect; large doses needed -Transdermal (Patches)- slow release- used to prevent angina attacks -Ointment- used primarily in hospitalized pts w/ angina or MI (absorbed thru the skin) -IV- used primarily to reduce preload and also to reduce afterload in pts w/ acute HF associated w/ MI |
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ISOSORBIDE DINITRATE:
Administered how... Used for what... Produces same effect as...but difference is... Converted to what active compound... |
-PO and SL
-Prevent and Rx anginal attacks -Nitroglycerin but slightly slower onset of action and longer duration -Isosorbide mononitrate |
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Isosorbide Mononitrate:
Dose... Brand names... Onset... |
-5-10mg PO BID (7 hrs apart)
-Imdur, Monoket -30-60 mg QD -Imdur ER, Ismo - 120-240 mg QD -30-60 mins |
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Nitroglycerin:
Brand name... Dose... IV dose... Ointment dose... SL dose... Onset SL... Oral... Topical... |
-Nitro-Dur
-2.5-6.5mg 3-4x/day -IV: 5-20mcg/min -Oint: 0.5-2 QID -SL: 0.4mg Q 5mins x 3doses -SL: 5 min -Oral: 40-60 min -Topical: 30-60 min |
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Isosorbide Dinitrate:
Brand name... Dose... SR dose... Onset SL... Chew... Oral... |
-Isordil
-5-40mg PO QID -40mg SR Q8-12hrs -SL: 2-10 min -Chew: 3 min -Oral: 40-60 min |
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CA CHANNEL BLOCKERS:
Examples of CCB's belonging to the Dihydropyridine class... brand name... Which one is NOT used to Tx angina... what is it used for... |
-Amlodopine (Norvasc)
-Felodipine (Plendil) -Isradipine (DynaCirc) -Nicardipine (Cardene) -Nifedipine (Procardia) -Nimodipine (Nimotop) -Nimodipine used to tx subarachnoid hemorrhage |
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Other CCB's...
All CCB's are used to Tx of HTN except... Which are also used to Tx certain arrhythmias... |
-Bepridil (Vascor)- D/C in 2003
-Diltiazem (Cardizem) -Verapamil (Calan, Isoptin) -Bepridil & nimodipine -Diltiazem & verapamil |
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Nimodipine:
Used to Tx what... Effects it has... Can reduce what... Dose... |
-Subarachnoid hemorrhage, which is a cause of stroke
-Dilates small cerebral vessels, increasing collateral circulation -Cerebral damage caused by cerebral ischemia from excessive Ca release -60mg PO Q4hrs x 21 days |
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Pharmacokinetics of CCB's:
Well absorbed thru which route... Those w/ short t1/2 available in IR and SR formulas... Those w/ long t1/2 given 1-2x/day... |
-Oral (most undergo 1st pass effect)
-Diltiazem, Nicardipine, Nifedipine, Verapamil -Amlodopine, Bepridil |
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Mechanism of Action of CCB's:
Ca channels are located where... Influx of Ca causes what... CCB's work how... All CCB's effect what... but some differ w/... |
-Plasma membrane of smooth muscle & cardiac tissue
-Membrane depolarization & muscle contraction -By binding to channels and prevent Ca from entering, causing muscle relaxation & suppression of cardiac activity -Vascular smooth muscle but some differ on effect on cardiac tissue |
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Dihydropyridines:
What is it... What does it do to some pts... Supresses what... Reduces what... |
-Potent vasodilator
-Reduces BP to evoke reflex tachycardia & causes cardiac arrhythmias -Cardiac fxn compared to other CCB's -CO in pts w/ cardiac failure |
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Adverse Effects of CCB's...
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-Fatigue
-Headache, Dizziness -Flushing, Hypotension -Peripheral edema -Increased risk of cardiovascular events & GI bleeding -Gingival Hyperplasia(occasional) |
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Dihydropyridines Approved for Angina:
Drug... Type of t1/2... |
-Amlodipine- long t1/2, Q24h adm (No effect on HR, AV node conduction & cardiac contractility)
-Felodipine –intermediate t1/2 -Nicardipine- short t1/2 -Nifedipine - short t1/2 |
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Beperidil:
Different from other CCB's how... Effects... Reserved for what type of pts... |
-Blocks Ca channels & Na channels in cardiac tissue
-Slows HR slightly -Increases AV nodal conduction -Prolongs QT interval and can cause cardiac arrhythmias (torsade de pointes) -Pts who have not responded to other antianginal agents |
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Diltiazem and Verapamil:
Used for Rx of... Effect... Adverse Effects... |
-Typical or variant angina
-Suppress cardiac contractility (use caution in pts w/ HF) -In typical angina (w/o HF), decreases HR and contractility -Constipation- Verapamil & others due to relaxation of GI smooth muscle & decreased peristalsis -Reduced clearance of Digoxin – can lead to toxicity |
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Amlodipine:
Bioavailability... T1/2... % urine... Felodipine... Nicardipine... |
-75%
-40 hrs -10% -20% -14 hrs -1% -35% -3 hrs -1% |
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Nifedipine...
Bepridil... Diltiazem... Verapamil... |
-60%
-3 hrs -1% -60% -25 hrs -5% -55% -5 hrs -3% -25% -5 hrs -3% |
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BETA ADRENERGIC BLOCKERS:
Indications to use them... |
-Treatment of hypertension or arrhythmia
-Management of Acute MI -Treatment of (typical) Angina -Atenolol -Metoprolol -Naldolol -Propranolol |
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BETA BLOCKERS:
In typical angina, BBs used prophylactically due to their ability to prevent... Type of effect they have that can be hazardous to pts w/ HF... |
-Prevent exercise induced tachycardia
-Prevent increased myocardial O2 demand -Prevent reflex tachycardia induced by organic nitrates or dihydropyridine CCBs -Negative inotropic effect |
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Partial Fatty Acid Oxidation (pFOX) Inhibitors:
Acts how... Examples... Dose... Max dose... MOA: The heart uses what for energy... Glucose metabolized why... pFOX inhibitors do what... |
-By modifying myocardial metabolism
-Trimetazidine (in France) -Ranolazine Ranexa (in US) -500mg PO BID -2000mg/day -Glucose, fatty acids, and lactate -To generate 15% more energy, (although fatty acids are a major source of energy for the heart) -Inhibit fatty acids, which leads to increase in glucose oxidation |
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Ranolazine:
Improves what... Reduces what... Has no effect on... Acts solely by modifying what... |
-Exercise capacity
-Electrographic evidence of ischemia -Frequency of angina attacks & need for NTG -HR, BP or coronary blood flow -Myocardial metabolism |
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Objectives of Therapy in Tx'ing Angina Pectoris...
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-Relieve acute symptoms
-Prevent ischemic attacks -Improve quality of life -Reduce risk of MI & other problems -Rx of concurrent HTN, hyperlipidemia, DM, obesity can decrease CAD progression -Aspirin- decreases risk of coronary thrombosis, MI, and prolongs life in chronic angina |
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Treatment Summary:
Occasional angina episode... Predictable episodes w/ exertion... Severe angina w/ regular use of NTG SL... Angiography may be performed to determine what... |
-NTG SL prn
-Use NTG SL or isosorbide before exercise -Consider long term prophylactic therapy -If angioplasty or coronary artery bypass grafting (CABG) is appropriate |
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Treatment Summary:
Stable angina requiring long term Rx... Chronic stable angina... Exercise induced angina... |
-Use b-blocker, long acting nitrate, or CCB
-Use b-blocker -B-blocker effective by improving exercise capacity, preventing ischemic episodes, & sudden cardiac death in angina. Also reducing incidence of ventricular arrhythmia post MI that cause sudden death |
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Treatment Summary:
B-blockers are the DOC for pts w/.... They prevent what... Many pts w/ chronic angina require what... CCB is less suitable than b-blocker in pts w/... B-blockers ineffective in Rx of... |
-Angina pectoris, especially unstable angina
-Reflex tachycardia caused by nitrates & some CCB's -More than 1 medicine -Unstable angina or recent MI -Variant angina caused by coronary vasospasm |
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Treatment Summary:
Aspirin is given to who... Or use what... HF and angina are treated w/... Low dose b-blocker not used why... |
-Pts w/ unstable angina (they have high risk of MI)
-Antithrombotic agents to prevent platelet aggregation & thrombus formation -Long acting nitrate preferred for prophylaxis -Not used in HF b/c it may not adequately control angina |
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Treatment Summary:
CCB's used to tx... Preferred for angina w/ concomitant what... B-blockers are contraindicated in who... why? |
-Variant angina (Verapamil; Bepridil not approved)
-Asthma b/c it relaxes smooth muscle -Pts w/ asthma b/c they block beta2 receptors in bronchial smooth muscle, causing bronchoconstriction |
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GI Disorders include...
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-Peptic Ulcer Disease
-Inflammatory bowel disease -GI motility disorders -Nausea and vomiting |
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PEPTIC ULCER DISEASE (PUD):
Characterized by... Ulcers occur when what happens... Damage to GI mucosa can be caused by several factors... |
-Inflamed lesions or excavations (ulcers) of mucosa & tissue of upper GI tract
-Damage to mucosa that protects the esophagus, stomach and duodenum from gastric acid & pepsin -Excessive acid and pepsin production -Bile acid reflux -Advancing age -Ischemia -Inhibition of prostaglandin synthesis -Helicobacter pylori |
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H. PYLORI:
Occurs in what % of ppl... Persons at risk include... What is a risk factor for PUD... |
-5-20% of persons by age 45
-Smokers, elderly -Ingesting excessive alcohol or anti-inflammatory agents- NSAIDs -GI Ischemia -Prolonged use of glucocorticoids |
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PUD:
What precedes development of PUD... H. pylori found in GI tract of who... Organism penetrates mucosa and does what... Eradication of it does what... Tx includes what type of drugs... |
-H. pylori induced gastritis
-Almost all pts w/ duodenal ulcers & 80% of pts w/ gastric ulcers -Releases enzymes that damages the mucosal membranes & causes inflammation & tissue destruction -Heals peptic ulcer, reduces reoccurrence rates of gastric & duodenal ulcers -Decrease hyperacidity (H2 antagonists & PPIs) -Eliminate H. Pylori -Exert a cytoprotective effect on GI tract |
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H2 Antagonist drugs include...
Brand name... |
-Cimetidine (Tagamet)
-Ranitidine (Zantac) -Famotidine (Pepcid) -Nizatidine (Axid) |
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Mechanism of Action of H2 Receptor Antagonists or H2 Blockers:
Structure is similar to what... This enables them to do what... They inhibit what... A decrease in gastric acid causes what... Has no effect on what... |
-Histamine
-Compete w/ histamine for binding to H2 receptors on parietal cells -Both meal stimulated secretion & basal secretion of gastric acid -Decrease in production of pepsin b/c gastric acid converts inactive pepsinogen to pepsin -No effect on gastric emptying time |
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Pharmacokinetics:
Excreted how... T1/2 how long.. Duration... Indications: Used to Tx excessive acid conditions including... |
-In urine
-2-3 hrs -Longer (Q12 or 24 hr administration) -Dyspepsia -Peptic Ulcer Disease -GERD -Occasionally used with H1 blocker for allergic rxns |
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RX or Prevention of Dyspepsia...
Take when... Rx of PUD: Take when... Increases what... Rx for how long... |
-Use OTC meds (lower doses)
-Take 30mins prior to dyspepsia provoking meal -Given once daily at hs or twice daily -Raises pH for about 13 hours -Rx for 6-8 weeks |
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H2 Receptor Antagonists or H2 blockers:
MOA/Activity... Healing time... Controlled studies indicate what... 80-90% recurrence w/in 1 yr of D/C if... Less than 5% ulcer recurrence in pts who... |
Supresses acid secretion and relieves pain
-Heal 70% of ulcers in 4 wks & about 85% in 8 weeks -All available H2 blockers produce comparable healing rates -Pt was on monotherapy w/ just a H2 blocker -Undergoes therapy w/ H2 blocker & clarithromycin |
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Clarithromycin is aimed at...
Therefore what is recommended... |
-Eradicating H. Pylori infection
-Combination therapy |
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H2 Antagonists Adverse Effects:
Cimetidine can cause... H2 blockers available how... |
-Gynecomatsia in elderly men (due to weak antiandrogenic activity). This is less common w/ other H2 blockers
-OTC due to nontoxic profile |
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Drug Interactions w/ Cimetidine:
Cimetidine inhibits what... which is important why... Drugs to monitor for signs of toxicity when taking Cimetidine concurrently... Other H2 blockers that can be taken instead of Cimetidine... |
-Cytochrome P450 isoenzymes
-Is involved in the metabolism of numerous drugs -Carbamezapine -Cisapride, -Felodipine -Lovastatin -Phenytoin -Saquinavir -Warfarin -Alprazolam -Ranitidine & famotidine- less interactions |
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H2 Antagonists:
Cimetidine: Relative Potency... Dose for Duodenal or Gastric Ulcer... Dose for GERD...OTC type... Dose for preventing stress related bleed... Ranitidine... Famotidine... |
-1
-800mg hs or 400mg bid -800mg bid (OTC Tagamet HB) -50mg/hr continuous infusion -4-10x -300mg hs or 150mg bid -150mg bid (OTC-Zantac 75) -50mg IV Q6-8h or 6.25mg/hr -20-50x -40mg hs or 20mg bid -20mg bid (OTC-Pepcid AC) -20mg IV Q12h |
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Nizatidine:
Relative Potency... Dose for Duodenal or Gastric Ulcer... Dose for GERD...OTC type... Dose for preventing stress related bleed... |
-4-10x
-300mg hs or 150mg bid -150mg bid (OTC Axid AR) -Not available |
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PROTON PUMP INHIBITORS (PPIs):
MOA... Proton pump is located... PPI's can produce dose dependent inhibition of up to... Single dose lasts how long... PPI's compared to H2 blockers... Should be used when... |
-Inhibits the H-K-ATPase pump, so parietal cells are inhibited from releasing H ions and gastric acid secretion is also inhibited
-In the membrane of gastric parietal cells -95% of gastric acid secretion -1-2 days -More efficacious and longer lasting -When other agents don't work and in recurrence |
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Using PPI's against PUD:
PPI's heal peptic ulcers... H2 blockers heal peptic ulcers... Comparing relapse rate... Recurrence is cause by...so use... |
-75-80% healed in 4 weeks
-70% healed in 4 weeks -It is similar -Persistant H. pylori, so use PPIs w/ drugs that eliminate H. Pylori infection |
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PPI's are the DOC for...
For Rx of dyspepsia... |
-Zollinger–Ellison syndrome (severe ulcers from gastrin- secreting tumors- gastrinomas). Higher doses required than for Rx of PUD
-Also GERD -Omeperazole available OTC |
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PUD- Drugs for H. Pylori Infection:
Type of therapy that must be used... Rx of PUD regimens include... Give gastric acid secretion inhibitors for how long... antimicrobial agents for how long... |
-Multiple drug therapy, single drug is rarely effective in eradication
-A PPI or H2 blocker & 2 or more the following agents: -Amoxicillin, clarithromycin, metronidazole & tetracycline -6-8 weeks -2 weeks |
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90% Eradication rate w/ what type of drug regimen...
Regimens w/ Clarithromycin may have... |
-3 drug regimen- PPI and 2 antimicrobials
-Higher eradication rates in a shorter time |
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Pharmacokinetics & Dosing for PPIs:
Omeprazole: Brand name... Bioavailability... T1/2 (hrs)... Dose for PUD or GERD... Esomeprazole... Lansoprazole... |
-Prilosec
-30-65% -0.5-1.5 -20-40mg QD (OTC-10mg) -Nexium ->80% -1.2-1.5 -20-40mg QD (IV & PO) -Prevacid ->80% -1.5 -30mg QD (IV & PO) |
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Pantoprazole:
Brand name... Bioavailability... T1/2 (hrs)... Dose for PUD or GERD... Rabeprazole... |
-Protonix
-77% -1-1.9 -40mg QD(IV & PO) -Aciphex -52% -1-2 -20mg QD |
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CYTOPROTECTIVE AGENTS:
These are GI drugs that do what... 2 agents in this category... |
-Protect the intestinal mucosa
-Sucralfate (Carafate) -Misoprostol (Cytotec) |
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SUCRALFATE:
MOA... Important why... PK Properties: Given how... Not absorbed significantly where... Primarily excreted how... |
-Stimulates prostaglandin (PG) synthesis in mucosal cells
-PG helps form a protective barrier to acid & pepsin, facilitating ulcer healing -Oral as a tablet or suspension -IN the gut -In the feces |
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Indications to use Sucralfate with PUD:
Can be used to tx... Less effective than what kind of agents... Primarily used in what type of pts... |
-Active duodenal ulcer or suppress recurrence of ulcers
-Agents that inhibit gastric acid secretion -Pts who cannot tolerate H2 blockers or PPIs |
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Adverse Effects of Sucralfate...
Decreases absorption of... This can be avoided by... |
-Constipation
-Laryngospasms- occasionally -Digoxin, Fluoroquinolones, ketoconazole, Phenytoin -Giving sucralfate 2 hrs before or after these agents |
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MISOPROTOL:
Type of drug... Exerts what kind of effects... Indications to use... Reserved for who... Dose given how... |
-A prostaglandin E analogue
-Cytoprotective effect by inhibiting gastric acid secretion & promoting secretion of mucus & bicarbonate -Used to prevent gastric and duodenal ulcers in pts taking NSAIDs on a long term basis -Pts at high risk for NSAID induced ulcers -200 mcg QID w/ food for duration of NSAID therapy |
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Adverse Effects of Misoprotol...
Contraindications of taking Misoprotol... |
-Diarrhea
-Intestinal cramping -Can stimulate uterine contractions & induce labor -Pregnancy! |
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PROKINETIC DRUGS:
Use in what type of disorders... Effects of Prokinetic agents... Effects of Laxatives... |
-Disorders of GI hypo motility
-Increase activity of GI smooth muscle throughout GI tract -Stimulate intestinal peristalsis by increasing the amt. of water & bulk in intestinal lumen |
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Metoclopramide (Reglan):
A prokinetic drug that increases GI motility by... Oral bioavailability... T1/2... Excreted how... Indications: Reglan used in Rx of... Also used for... Exerts anti-emetic effect by... |
-Blocking D2 receptors which prevents relaxation of GI smooth muscle produced by dopamine
-85% (also given by IV) -4 hrs -In the urine -GERD, diabetic gastroparesis, hiccups -Intubation of small bowel during radiological exams -Blocking D2 & serotonin 5HT3 receptors in the chemoreceptor trigger zone |
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Adverse Effects of Reglan...
Contraindications of use... |
-CNS Effects (drowsiness, extra pyramidal effects, and seizures)
-Hyperprolactinemia -Diarrhea -Seizure disorder -Mechanical obstruction of GI tract -GI hemorrhage |
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Tegaserod:
Brand name... Type of drug... Indicated for who... Given how... Adverse Effects... Doses available... Recently was... |
-Zelnorm
-A promotility agent -Women w/ irritable bowel syndrome whose predominant symptom is constipation -Orally BID before meals -Diarrhea (mild & transient) -Ischemic colitis -2 and 6 mg tablets -Withdrawn from market |
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LAXATIVE DRUGS:
Lubiprostone: Brand name... MOA... Indications to use... Dose for indication... Contraindications... |
-Amitiza
-Acts on membrane of GI tract to increase intestinal fluid secretion -Irritable bowel syndrome -8mcg PO BID -Idiopathic constipation(Chronic) -24mcg PO BID with food -GI obstruction |
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Lubiprostone-Amitiza:
Precautions... Adverse Effects... Excreted how... Available how... |
-Severe diarrhea
-Abd. Distension (6%) -Abd. Pain (3-8%) -Diarrhea (12%) -Nausea (8-29%) -HA (3-11%) -Renal (60%) -Fecal (30%) -Oral capsule, liquid filles-8 or 24mcg |
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CONSTIPATION:
Characterized by... 2 types... Non-pharmacological Tx includes... Pharmacological Tx includes... |
-Difficult passage of hard feces
-Acute or chronic -Adequate fluid intake -Increase dietary fiber -Exercise -Bulk forming laxatives (for chronic) -Others (for acute) |
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Laxatives:
Agents that stimulate what... Indications to use them... |
-Intestinal peristalsis & increases movement of material
-Tx of constipation -Evacuation of bowel before surgery -Eliminate drugs or poisons |
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Bulk Laxatives:
Long term use... Osmotic or Stimulant Laxatives: Use leads to... Dependence can happen, esp in who... |
-No ADE w/ long term use
-Electrolyte abnormalities or depletion -Pts w/ renal impairment (unable to excrete osmotic substances absorbed into circulation) |
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BULK LAXATIVES:
MOA... Examples... Available in what preps... Must be taken how... How safe... Preferred for management of... |
-Absorb & retain H20 in intestinal lumen, which leads to increase in mass of intestinal material, mechanical distension of intestinal wall, stimulation of peristalsis
-Psyllium hydrophyilic mucilloid (metamucil) -Calcium polycarbophil (Fibercon) -Fiber, tabs, packets of granules -W/ full glass of H20 to avoid intestinal obstruction -Safest and most physiological laxative type -Chronic constipation |
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SURFACTANT LAXATIVES (Stool softeners):
MOA... Indications to use... Examples... |
-Helps incorporate H20 into fatty intestinal material, which softens the feces
-Constipation w/ hard dry fecal material, irritable painful stools (hemorrhoids) -If straining must be avoided (after surgery) -Docusate Na (Colace) -Docusate Ca (Surfak) |
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OSMOTIC (Saline) LAXATIVES:
MOA... Formulations available... Indications to use... Example... |
-Attract H20 in the intestinal tract, increase intraluminal pressure, stimulating peristalsis
-Oral liquids or chewable tabs -Bowel evacuation/ Constipation -Sodium phosphate (prior to surgery) -Constipation -Mg Oxide (Milk of Magnesia) |
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STIMULANT (Secretary) LAXATIVES:
MOA... Indications to use... Example... Adverse Effects... Precaution... |
-Alter fluid secretions of intestinal mucosa & stimulate peristalsis
-Constipation -Castor oil, senna or cascara -Constipation/Bowel evacuation -Bisacodyl (Dulcolax) -Abdominal cramps -Electrolyte & fluid depletion -Use as short Rx of acute constipation due to ADEs |
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Causes of Secretary Diarrhea...
Rx of diarrhea... |
-Microbial toxins
-Laxatives -Vasoactive intestinal polypeptide -Excessive bile acids -Steatorrhea- unabsorbed fats in malabsorption syndromes -Eliminate or control underlying cause -Fluid & electrolyte replacement -Antidiarrheal agents for symptomatic relief |
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Antidiarrheal Agents-
Opiods: MOA... Examples... Example of locally acting agent... It act by doing what... Effective against what... |
-Induce contraction of intestinal smooth muscle thru activation of intestinal opiod receptors
-Diphenoxylate (Lomotil) -Loperamide (Imodium) -Bismuth subsalicylate -Inhibiting intestinal secretions -Infectious diarrhea (traveler's diarrhea) |
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Drugs Used for Inflammatory Bowel Disease-
Glucocorticoids: Available how... Indications to use... Effects remission how... |
-Orally, parentally, or rectal enema
-Ulcerative Colitis -Crohn’s disease -Induces remission in both disorders, but less valuable in maintaining remission |
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Drugs Used for Inflammatory Bowel Disease-
Aminosalicylates: Indications to use... Examples... |
-Inducing & maintaining remission for IBD (UC & Crohn’s)
-Sulfasalazine & its active metabolites (Mesalamine) -Mesalamine (rectal suspension or tabs) |
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Primary therapy for IBD includes...
Immunosuppressive agents are reserved for... Example that has demonstrated value in some Crohn's cases... |
-Glucocorticoids & aminosalycylates
-Rx failures to glucocorticoids -Metronidazole |
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METRONIDAZOLE:
Works by doing what... INFLIXIMAB: Brand name... Type of drug... Given how... |
-Eradicating bacteria that contribute to mucosal inflammation
-Remicade -Monoclonal antibody to Tumor Necrosis factor (TNF). TNF involved in pathogenesis of Crohn’s. -2 hr infusion- improvement in 82% pts w/ moderate to severe Crohn’s |
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CINV stands for...
ASCO... What is no longer recommended for high emetic risk... What is preferred for moderate emetic risk... Aprepitant (Emend) recommended for what... Palonosetron (Aloxi) no longer... |
-Chemotherapy Induced Nausea and Vomiting
-American Society of Clinical Oncology -5-HT3 RA -Dexamethasone -Acute & delayed prophylaxis for high emetic chemotherapy -Identified as preferred agent for acute |
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CINV: High Risk Prophylaxis:
Aprepitant: Dose... Dexamethasone: Dose... |
-125 mg PO for D1, then 80 mg PO for D2 and 3
-12 mg IV/PO for D1, then 8 mg IV/PO QD for D2-4 |
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5-HT3 RA:
Ondansetron: Brand name... Dose... Granisetron... Dolasetron... Palonosetron... |
-Zofran
-8-12 mg IV or 16–24 mg PO D1 -Kytril -1 mg IV or 2 mg PO D1 -Anzemet -100 mg IV / PO D1 -Aloxi -0.25 mg IV D1 |
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ASCO and NCCN state that use of 5-HT2 RA is no longer recommended for...
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-Delayed CINV with highly emetogenic chemotherapy
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CINV: Moderate Risk Prophylaxis:
Day 1... |
-Aprepitant 125 mg PO
-Dexamethasone 12 mg IV or PO Then choose one 5-HT3 RA: -Ondansetron: 8–12 mg IV or 16-24mg PO -Granistron: 1mg IV or 2 mg PO -Dolansetron: 100 mg IV/PO -Palonosetron: 0.25 mg IV* If Palonosetron is used, no further 5-HT3 is required for D2-4 |
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CINV: Moderate Risk Prophylaxis:
Days 2-4: |
-Aprepitant: 80 mg on D2-3 (but only if administered on D1)
AND/OR -Dexamethasone: 8 mg PO/IV QD (preferred) OR Choose 1 5-HT3 RA: -Ondansetron: 16mg PO QD (or 8mg IV QD) -Granisetron: 1-2mg PO (or 1 mg IV QD) -Dolasetron: 100 mg PO/IV QD |
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Palonosetron: ASCO Guidelines Statements-
Palonosetron outperformed what... Primary end point was... There are no prospective trials designed specifically to prove what... Also no trial comparing palonosetron with another 5-HT3 antagonist when both are... |
-Ondansetron and dolasetron in several head-to-head comparisons
-Non-inferiority (end point was met in all studies) -Superiority of palonosetron over any other 5-HT3 antagonist -Combined appropriately w/ dexamethasone |
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PONV:
Risk is determined as low, moderate, or high based on... Type of therapy w/ low risk... Moderate risk... High risk... |
-Patient, anesthetic, and surgical factors
-Tx only strategy -Mono- or combination therapy -Combination therapy (2 or 3 agents from different classes) |
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PONV:
APREPITANT: Brand name... FDA approved dose... Evidence supports its equivalence to... Its efficacy is greater against what... Recommendations for use... |
-Emend
-40 mg dose prior to surgery -Ondansetron -Greater against vomiting than nausea -Equivalence w/ 5-HT3 RA -Cost minimization approach -Consider outpatient prescriptions (administer aprepitant 3 hours prior to surgery) |
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PONV:
PALONOSETRON: Brand name... Dose in Phase II study... Estimated $ per dose... Importance of t1/2... |
-Aloxi
-1 mcg/kg -$58 -Will longer t1/2 result in improved outcomes (0-24 hrs post-op and post discharge) |
