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106 Cards in this Set
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Urine is formed from the result of maintaining a balance between renal (kidney) reabsorption and elimination |
Kidney functions: - clear substances from blood (including ions, glucose, and water) - reabsorb elements (sodium, potassium, chloride, and bicarbonate) - excrete wastes |
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Main Indication of Diuretics - reduce the circulating fluid volume to help treat edema and hypertension |
Thiazides - the most frequently used type of diuretic - increasing excretion of water, sodium, chloride and potassium Ex: hydrochlorothiazide |
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Diuretics function and Types - increase urine excretion Categories - thiazides - loop diuretics - potassium-sparing diuretics - osmotic agents - carbonic anhydrase inhibitors |
Urinary Tract Infections (UTIs) - treated with oral antibiotics - source: Gram-Negative bacteria (primary source E.coli) - frequently accompanied by a burning sensations accompanied by frequent and painful urination (treat with analgesics: oral agents phenazopyridine (Pyridium) |
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Urinary Antispasmodic Drugs treat: - urethral spasms - renal colic - spasm of the bladder sphincter - urinary retention - kidney stones |
Urinary Antispasmodic Drugs used - irritation in urinary tract from: infection, catheterization, urinary retention or kidney stones |
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Action of Antispasmodic drug - relax the smooth muscle in the wall of the urethra and bladder - allow normal emptying of urine |
Chronic Renal Failure (CRF) - progressive destruction of kidney structures - it is NOT Reversible |
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Chronic Renal Failure (CRF) cause - progressive deterioration of glomerular filtration - tubular reabsorption - endocrine functions of kidneys - cause impaired synthesis of erythropoietin (stimulates RBC production) - can cause anemia |
Medications used to treat anemia in CRF patients = Epogen = Procrit = Aranesp |
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Benign Prostatic Hyperplasia - increase in number of cells of the prostate gland - age- related nonmalignant enlargement of prostate - characterized by formation of large discrete lesion in the periurethral region of prostate |
GI |
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Uses of thiazides include treatment of - Edema from many causes (loop diuretics more commonly used) - Hypertension (blood pressure is lowered by reducing peripheral vascular resistance and decrease fluid retention) - Prophylaxis (action taken to prevent) of calculus (stone formation in those with hypercalciuria - excess calcium in urine) |
Side effects of thiazides may include - Hypokalemia (K+ deficiency) may lead to cardiac arrhythmias; hyponatremia (low Na+ levels) ; hypercalcemia (abnormally high blood Ca2+ levels) - muscle weakness or spasm - GI reactions (e.g. anorexia, nausea, vomiting, diarrhea) - Postural hypotension, vertigo, and headache - fatigue, weakness, lethargy - skin conditions (rash and photosensitivity; rare) - Hyperglycemia and increased uric acid level |
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Precautions or Contraindications with thiazides apply to - Diabetes (may cause hyperglycemia and glycosuria) - History of gout (increased uric acid level) - Severe renal disease - Impaired liver function - Prolonged use (K+ supplements to prevent hypokalemia) - Older adults due to greater sensitivity to thiazides (may cause low Na+ levels) - patients with sulfonamide hypersensitivity |
Patient Education for patients being treated with Thiazides - diet including potassium-rich foods - low-sodium diet if diuretic is prescribed for hypertension - notifying the physician of persistent or severe side effects - administration with food (reduce gastric irritation) - administration in morning to prevent disruption of sleep from frequent urination - rising slowly from reclining position to counteract postural hypotension - limitation of alcohol consumption - consulting physician before adding new medications - necessity for regular blood test to monitor electrolyte levels |
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Interactions of thiazides may occur with - Nonsteroidal Anti-inflammatory agents (risk of renal insufficiency and reduced blood pressure control - Corticosteroids (increase K+ loss) - Lithium (causes lithium intoxication) - Hypotensive agents (potentiate blood pressure decrease) - Digoxin (increased potential for digoxin toxicity - Probenecid (blocks uric acid retention) - Antidiabetic agents (loss of diabetic control) |
Loop Diuretics - act on the loop of Henle in the kidney to inhibit sodium and chloride reabsorption; which inhibits water reabsorption back into the bloodstream = increased urine formation |
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Potent diuretics - furosemide (Lasix), bumetanide and toresmide (demadex) are not thiazides but act in similar way to increase excretion of water, sodium, chloride and potassium. - Action: more rapid and effective that thiazides, with greater Diuresis (they do not lower blood pressure as well as thiazides) |
Uses of Loop Diuretics include treatment of - edema associated with impaired renal function, heart failure, or hepatic disease - pulmonary edema - ascites caused by malignancy or cirrhosis - hypertension (if thiazide not effective, loop diuretics combined with other antihypertensives esp patient with kidney disease) |
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Side effects of loop diuretics include - fluid and electrolyte imbalance with dehydration, circulatory collapse, and chest pain - Hypokalemia with weakness( K+ supplements may be indicated esp for cardiac patients to prevent arrhythmias) hypocalcemia - Hypotension (close blood pressure checks required)- GI effects, including anorexia, nausea vomiting, diarrhea and abdominal pain. - Hyperglycemia and increased uric acid level Tinnitus, hearing impairment and blurred vision - rash, urticaria, pruritus and photosensitivity |
Precautions or contraindications with loop diuretics apply to - Cirrhosis and other liver disease - Kidney impairment - Alkalosis and Dehydration - Patients on digoxin (cardiac arrhythmias are possible unless K+ is supplemented) - Those allergic to sulfonamides - Diabetes - History of gout - Pregnancy and lactation - Patients under 18 years of age (bumetanide and Demadex) |
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Interactions of loop diuretics similar to those of thiazides - Corticosteroids (potentiate potassium loss) - Hypotensive agents (potentiation of effects) - Digoxin (increased potential for digoxin toxicity and arrhythmias) |
Additional of Loop Diuretics may include - Aminoglycosides increase chance of deafness - Indomethacin decreases diuretic effect - Salicylates with furosemide increase chance of salicylate toxicity - anticonvulsants (phenytoin) reduce diuretic effect of furosemide *patients taking loop diuretics should be instructed regarding same instructions as thiazides. |
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Potassium-Sparing Diuretics (spironolactone (Aldactone) and triamterene (Dyrenium)) - sometimes administered under conditions where potassium depletion can be dangerous - may also counteract the increased glucose and uric acid levels associated with thiazide diuretic therapy - |
Spironolactone is diuretic of choice in patients with cirrhosis* - reduce deaths in patients with severe heart failure |
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Potassium-sparing diuretics - seldom used alone - used with combine with thiazide diuretics to increase diuretic and hypotensive effects and to reduce danger of hyperkalemia (excessive potassium retention) - when combined (Aldactazide or Dyazide), supplemental K+ is usually NOT indicated but varies. |
Side effects of Potassium-Sparing Diuretics are usually mild and respond to withdrawal of drug but may include - Hyperkalemia (esp with K+ supplements) which may lead to cardiac arrhythmias - Dehydration or weakness - GI symptoms (nausea, vomiting and diarrhea) - Fatigue, lethargy, and profound weight loss - Hypotension - Gynecosmatia (enlargement of breast tissue in men) with spironolactone |
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Caution with Potassium-Sparing Diuretics indicated in patients with - renal insufficiency - cirrhosis and other liver disease - pregnancy and lactation |
Interactions may occur between potassium-sparing diuretics and - potassium supplements, Angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs) salicylates, and NSAIDs, to cause hyperkalemia |
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Osmotic Agents (e.g. mannitol) - most frequently used to reduce intracranial or intraocular pressure |
Side effects of osmotic agents can include - Fluid and electrolyte imbalance - CNS symptoms (headache, vertigo, and mental confusion) - GI symptoms, (nausea and vomiting) - Tachycardia, hypertension and hypotension - Allergic reactions - Severe pulmonary edema |
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Extreme caution is indicated and kidney and cardiovascular function should be evaluated before administration of osmotic agents to anyone with - Kidney Failure - Heart Failure - Severe Pulmonary Edema - Pregnancy and Lactation |
Patient Education for Osmotic Agents - side effects reported immediately - reassured that osmotic agents given under close medical supervision and serum electrolyte levels monitored frequently by blood test to detect adverse reactions |
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Gout - form of arthritis and metabolic disorder characterized by the accumulation of uric acid crystals in various joints (esp in big toe, ankle, knee, and elbow) tissues, sometimes kidneys, with resultant inflammation and pain |
Treatment for managing Gout includes treating - acute attacks - uric acid - lowering therapy - preventing recurrence of acute attacks |
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Acute Gout characterized by - sudden onset of pain, redness, warmth and swelling in affected joints |
Medications to treat Gout - NSAIDS and Colchicine - Uricosuric Agents - Xanthine Oxidase Inhibitors |
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NSAIDs to treat Gout - naproxen, Indomethacin, and ibuprofen (when started soon after onset of symptoms, work quickly to relieve pain -should be used cautiously with patients with kidney disease, heart disease, or risk factors for GI bleeding |
Corticosteroids (prednisone) - useful in treatment of acute gout in patients who cannot tolerate NSAIDs |
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Colchicine - not an analgesic - does not affect uric acid clearance - relieve inflammation in acute gouty arthritis (must be given within 24 hours of onset of symptoms for maximum effectiveness) - in chronic management of gout - can be used prophylactically at low does to prevent recurrent attacks of gout |
Side Effects of Colchicine limit its use and can include - rash, alopecia - GI upset, nausea, vomiting, and diarrhea (~80% of patients cannot tolerate frequent GI side effects) - blood disorders and bone marrow suppression |
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Patient Education for Colchicine - large fluid intake to facilitate excretion of uric acid crystals - avoiding alcohol (increase risk of adverse GI effects and increases serum urate [salt of uric acid] concentrations. |
Medications used to treat gout chronically include the uricosuric agents and the xanthine oxidase inhibitors = lower uric acid levels |
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Uricosuric Agents (probenecid) - act on kidneys by blocking reabsorption and promote urinary excretion of uric acid - treats chronic cases of gout and frequent disabling attacks of gouty arthritis. - have no analgesic or anti-inflammatory activity = not effective in treatment of acute gout |
During acute attacks of gout: - probenecid dosage is supplemented with colchicine (has anti-inflammatory action) |
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Probenecid - sometimes given with penicillin to potentiate the level of antibiotic in blood Ex: amoxicilllin for some gonococcal infections - also given with cefoxitin to treat acute pelvic inflammatory disease |
Side effects of probenecid are rare but may include - headache - nausea, vomiting - kidney stones and renal colic if large volume of fluids is not maintained - hypersensitivity reactions, rash, hypotension and anaphylaxis are rare |
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Precautions or contraindications for probenecid apply to patients with - history of uric acid kidney stones - history of peptic ulcer - renal impairment - hematologic disease |
Interactions may occur with - penicillins and cephalosporins, potentiating therapeutic effect of antibiotics - oral hypoglycemics, could cause hypoglycemia through potentiation - salicylates which antagonize uricosuric action - NSAIDs (probenecid decreases renal clearance) |
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Patient Education with Uricosuric agents - Drinking large amounts of fluid - Avoid taking large doses of aspirin products - taking medications at the same time only with physician's order - taking medications with food - reporting rash immediately |
Xanthine Oxidase Inhibitors - Allopurinol (Zyloprim) another medication used to treat chronic gout - class of drugs results in decreased serum and urinary levels of uric acid - has no analgesic or anti-inflammatory activity, and therefore not effective in treatment of ACUTE GOUT |
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Side Effects of allopurinol can include - Rash - allergic reactions, also fever, chills, nausea, vomiting, diarrhea, drowsiness and vertigo - severe hypersensitivity reactions (rare) but increase in older patients with renal impairment who receive allopurinol and thiazide diuretics in combination |
Precautions or Contraindications with Allopurinol apply to - impaired renal function - history of hypersensitivity reactions - liver disease - pregnancy and lactation |
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Interactions of allopurinol may occur with - Antineoplastic drugs (potentiate side effects - azathioprine, mercaptopurine) - alcohol and diuretics (increase serum urate concentrations) |
Febuxostat (Uloric) - first new oral agent approved for gout sine early 1960s. - more potent and lower risk of hypersensitivity reactions compared to allopurinol - may have higher risk of cardiovascular adverse events |
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Patient Education for allopurinol and febuxostat - drinking large quantities of fluid - taking medications after meals - stopping medication and reporting rash to physician immediately - avoiding alcohol (increase uric acid) - avoidance of purine-rich foods (liver, kidneys, shellfish and red meat) - avoiding other medications unless prescribed by physician |
Bladder Antispasmodics = frequency and urgency Frequency: having to urinate more than 8 times in 24 hours Urgency: sudden need to urinate |
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Antispasmodics (Definition) - anticholinergic in action (blocking parasympathetic nerve impulses) used to increase the capacity and decrease urgency of urinary bladder "used to reduce the strength and frequency of contractions of urinary bladder and decrease gastrointestinal motility" |
Antispasmodics relieve incontinence Incontinence: loss of bladder control |
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Antispasmodic Drugs = Tolterodine (Detrol) and oxyburtynin used to decrease bladder tone and suppress bladder contractions in patients with neurogenic bladder = result in decreased incontinence. = these drugs are used to relief symptoms such as urgency, frequency, nocturia and incontinence. (have similar adverse effects, esp in older adults. |
FDA approved OTC patch (Oxytrol for Women) 18 years or older -prescription only for men Hyoscyamine (Levsin) another anticholinergic less commonly used as antispasmodic, but adverse side effects common in older adults |
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Side Effects of bladder antispasmodic (Anticholinergic in action) can include - drying of all secretions (eyes and mouth) - Drowsiness and dizziness (headache; fatigue) - Urinary retention and constipation - Blurred Vision - Mental confusion (esp older adults) - Tachycardia, palpitations - Nausea and vomiting - Rash, urticaria and allergic reactions |
Precautions or Contraindications with bladder antispasmodics apply for - older adults - hepatic/renal disease and obstructive uropathy - Bladder or GI obstruction or ulcerative colitis - Cardiovascular disease - Prostatic hyperplasia - Children (contraindcated under 6 years. Ditropan XL is used effectively in children greater or = to 6 years) - pregnancy or lactation - narrow-angle glaucoma |
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Interactions with bladder antispasmodics may include - other anticholinergic agents (can potentiate effects with possible toxicity) - Potassium salts (risk of GI irritation) |
Mirabegron (Myrbetriq) - newest bladder antispasmodic - stimulates beta3 receptors in bladder to increase bladder capacity - provides alternative for patients who cannot tolerate side effects of anticholinergic antispasmodics. -common adverse effects: nausea, constipation, diarrhea, headache, dizziness, hypertension and sinus tachycardia. |
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Patient education for bladder antispasmodics (pg 258) |
Cholinergics Bethanechol (Urecholine) - stimulates parasympathetic nerves to bring about contraction of urinary bladder in cases of nonobstructive urinary retention (usually postoperatively or postpartum) = "Pharmacological Catheterizations" |
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Side effects of bethanechol are cholinergic action and usually dose related and can include - GI cramping, diarrhea, nausea, and vomiting - Sweating and salivation - headache and bronchial constriction - slow heartbeat or reflex tachycardia and orthostatic hypotension - urinary urgency |
Precautions or Contraindications of bethanechol include - Obstruction of the GI or urinary tract - Hyperthryoidism - Peptic ulcer and irritable bowel syndrome - Asthma - Cardiovascular disease - bradycardia - Parkinsonism and seizure disorder - Pregnancy and lactation |
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Interactions with bethanechol may occur with - other cholinergic or anticholinesterase agents (e.g. neostigmine) administered concomitantly (can potentiate effects with increased possibility of toxicity) - Quinidine or procainamide (antagonize cholinergic effect) - Atropine (antagonizes cholinergic effect - antidote in cases of cholinergic toxicity) |
Urinary Analgesics - Phenazopyridine (AZO Standard) - oral or local anesthetic for urinary tract mucosa - used for short time to relieve burning, pain, discomfort and urgency associated with cystitis (bladder inflammation) - should not be taken for more than 2 days when used with an antibacterial agent* |
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Benign Prostatic Hyperplasia (BPH) - most common benign tumor in men - involves Hyperplasia (increase in number of cells) leading to prostate enlargement (interferes with urinary flow) |
Drugs used to treat symptoms of BHP - includes those that slow prostate growth (antiandrogens) - relax the bladder smooth muscle to make easier for urine flow from bladder through urethra (alpha-blockers) |
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Antiandrogens - Finasteride (Proscar) and dutasteride (Avodart) - work by supressing prostate growth and associated urinary obstruction and manifestations Ex: urgency, nocturia and urinary hesitancy - treats BPH |
Proscar 5 mg, or Avodart 0.5 mg administered daily for min of 6-12 months - therapy appears to be suppressive rather than curative - return of hyperplasia is likely if drug is withdrawn. |
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Side effects of Antiandrogens - impotence, decreased libido, decreased ejaculate - gynecomastia (breast tenderness and enlargement) - side effects diminish after first year of treatment |
Cautions of Antiandrogens - patients should be screened first for cancer, infection or other urinary dysfunctions - can affect blood test (PSA) screens prostate cancer - Liver function abnormalities may be exacerbated - Crushed tablets and soft gelatin capsule should not be handled by pregnant women (cause fetal damage) - |
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Antiandrogens have not been associated with clinically important drug interactions |
Saw palmetto commonly used supplement for BPH - might moderately reduce some BPH symptoms - effects of co-use are not known at this time. |
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Alpha-Blockers Tamsulosin (Flomax) - blocks alpha-1 receptors found in smooth muscle in bladder neck and prostate = relax - urine rate is improved and symptoms of BPH are decreased. - first line of therapy for treatment of BPH |
Other examples of alpha-blockers - doxazosin (Cardura) - terazosin (treat hypertension and BPH) |
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Side Effects of alpha-blockers are infrequent but can include - dizziness, headache, and nasal congestion - orthostatic hypotension - Palpitations (not Flomax) - Ejaculation dysfunction, decreased libido and impotence (erectile dysfunction) |
Cautions of Alpha-blockers - serious or life-threatening sulfonamide allergy (with flomax) - notify ophthalmologist of current /previous treatment with alpha blockers (may be at risk for intraoperative floppy iris syndrome during cataract surgery |
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Interactions with Alpha-blockers may occur with - Calcium channel blockers - Other antihypertensive agents (additive hypotensive effects) |
Phosphodiesterase (PDE) Inhibitor Tadalafil (Cialis) -treats erectile dysfunction - recently approved to treat the signs and symptoms of BPH |
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Caution with PDE inhibitor - important to read instructions on product label to reduce risk of hypotension and fainting |
Loop diuretics acts directly on what part of the Kidney = Loop of Henle |
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The primary action of loop diuretics is to - increase excretion of water, sodium, chloride and potassium. |
A potential side effect of a loop diuretic is = Hypokalemia |
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Important instructions to patients on how to take his medication (for pulmonary edema) = rise slowly from inclining position |
Which medication is used prophylactically at low doses to prevent recurrent attacks of gout? = Cochicine |
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What type of intake is suggested for a patient on probenecid in order to prevent kidney stones and renal colic? = large volume of fluids |
What instructions should be given to a patient taking allopurinol? - Avoid alcohol |
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In treating BPH, a patient taking Flomax might experience which side effect? = Dizziness |
What is a symptom or condition that is characterized by having to urinate more than 8 times in 24 hours? = Frequency |
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Chapter 16 |
Gastrointestinal Drugs |
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Antacids - act by partially neutralizing gastric hydrochloric acid and widely available in many OTC preparations for relief of indigestion, heartburn and sour stomach. - supplemental agents in managing esophageal reflux |
Pyrosis (heartburn) and dyspepsia (acid indigestion) are experienced by up to 40% of pop in U.S. at least once a month |
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Antacid products may contain - aluminium - calcium carbonate - magnesium -*most antacids contain sodium ** sodium bicarbonate alone is not recommended because flatulence(acuumulation of gas), metabolic alkalosis and electrolyte imbalance with prolonged use |
Tums (calcium carbonate) - rapid acting and possess good neutralizing capacity but may cause constipation and kidney stones (if overused) |
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Generally Antacids have - short duration of action - requiring frequent administration *Magnesium and or aluminum antacids most commonly used |
Antacids Magnesium - can cause diarrhea - Aluminum causes constipation = combinations of the two: Maalox, Gelusil and Mylanta are frequently used to control frequency and consistency of bowel movements |
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Side effects with frequent use of antacids include - constipation (with aluminum or calcium carbonate antacids) - diarrhea (magnesium antacids) - Electrolyte imbalance - urinary calculi (stone formation) renal complications - osteoporosis (aluminum antacids) - Belching and flatulence (calcium carbonate and sodium bicarbonate) |
Precautions or Contraindications with antacids - Heart failure - Chronic kidney disease or history of renal calculi - Cirrhosis of liver or edema - dehydration or electrolyte imbalance - |
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*Antacids may increase/decrease absorption of other medications- may decrease effectiveness of drug = antacids should not be taken within 2hours of administering the following meds: - Anti-infectives (esp tetracyclines, quinolones and isoniazid) - Digoxin, indomethacin and iron - Salicylates and thyroid hormones - Bisphosphonates (ie.e Actonel, Fosamax) |
Antacids with following drugs may increase action and precipitate side effects: - Diazepam, (increase sedation) - Amphetamines and quinidine (increase cardiac irregularities) - Enteric-coated drugs may be released prematurely in stomach (separate doses from antacids by 2 hours) |
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Patient Education with Antacids - avoid prolonged use (no longer than 2 weeks) of OTC antacids without medical supervision because danger of masking symptoms of GI bleeding or GI malignancy and causing stomach to increase excess acid - Avoid use of antacids at same time as other medications interactions - Avoid use of antacids entirely or use with caution if patient has cardiac, renal or liver disease or fluid retention |
Patients taking medicine for managing esophageal reflux should be instructed - avoid constrictive clothing treatment of obesity (if appropriate) - reduce meal size, avoid lying down after meals - restriction of alcohol use - elimination of smoking - elevating head of bed during sleep |
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Agents for treatment of Ulcers and Gastroesophageal Reflux Disease - H2-blockers - Proton Pump Inhibitors |
H2- receptors - found in stomach H2-receptor antagonists = reduce gastric acid secretions by acting as histamine2blockers. |
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Histamine2-Blockers - agents that block the histamine receptors found in the stomach to reduce gastric acid secretions - reduce amount of gastric acid released in response to stimuli such as food and caffeine - Drugs: - cimetidine - famotidine (Pepcid) - ranitidine (Zantac) |
Histamine2-Blockers - used short term for the relief of "acid indigestion and heartburn" - Gastroesophgeal reflux disease (GERD) - esophagitis - prevention of duodenal ulcer recurrence |
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Side effects of H2-Blockers usually transient and dose related can include - diarrhea, dizziness, rash and headache - mild gynecomastia with cimetidine occurs infrequently and reversible - mental confusion (esp in older and debilitated adults; less with Pepcid) |
Precautions or contraindications with H1-blockers apply to - renal disease (may need to reduce dose and or frequency) - pregnancy - lactation |
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Interactions with cimetidine may occur with increased blood concentrations of - Warfarin (Coumadin) (also with high doses of Zantac) - Phenytoin - Beta-blockers - Benzodiazepines - Lidocaine - Theophylline (also with high doses of Zantac) - Tricyclic antidepressants - Proton pump inhibitors may interfere with effectiveness of H2-blockers when given together the H2-blocker (usually given at bed time) |
*less likelihood for drug interaction with Pepcid |
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Proton Pump Inhibitors (PPIs) - Omeprazole (Prilosec) gastric antisecretory agent (unrelated to H2-receptor antagonists) - used for short-term (4-8 weeks) symptomatic relief of GERD - used for erosive esphagitis and "heart burn" - short term treatment of confirmed gastric and duodenal ulcers |
GERD PPI is caused by excessive reflux of acidic contents into esophagus - result in irritation or injury to esophageal mucosa characterized by heartburn and acid regurgitation - Serious complications: esophageal stricture, pulmonary aspiration and esophageal cancer |
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Long-term use of PPIs for severe GERD - preventing NSAID-induced ulcers and hypersecretory conditions other drugs include: Lansoprazole (Prevacid), rabeprazole (Aciphex), pantoprazole (Protonix) and esomeprazole (Nexium) |
Side Effects of PPis can include - Diarrhea, constipation, nausea, vomiting and abdominal pain - increased risk for pneumonia or intestinal (Clostridium difficile) infection |
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Long-term use on regular basis of agents that reduce gastric acid can possibly result in - vitamin B deficiency and low Magnesium levels in blood (esp in older adults) - patients over 50 years, long term PPI particular at high doses, associated with increased risk or hip, wrist or spine fractures = potential mechanism for this PPi's interference with calcium absorption |
Interactions of PPIs may occur with - Clopidogrel (Plavix) (platelet inhibitor) - H2-blockers (decrease PPI effectiveness) - Sucralfate (delays absorption of most PPIs) - Benzodiazepines, phenytoin, and warfarin (increased serum levels) - Ampicillin, ketoconazole, iron salts, vitamin B 12, bisphophonates (results in poor bioavailability) - Food - Nexium, Prevacid and Prilosec should be given on empty stomach; Aciphex and Protonix can be give without regard to meals |
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Gastric Mucosal Agents -Misoprostol (Cytotec) - Sucralfate (Carafate) - Helicobacter Pylori Treatment |
Misoprostol (Cytotec) - synthetic form of prostaglandin E1 - inhibits gastric acid secretion and protects the mucosa from irritant effect of certain drugs (ex. NSAIDs), especially those at risk (ex: debilitated patients or older adults or those with history of gastric ulcers) *not FDA approved for treatment of gastric or duodenal ulcers that are unrelated to NSAID use |
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Side effects of Cytotec can include - Diarrhea, nausea, and abdominal pain (occur early in treatment, usually self-limiting; take with food to minimize effects) - Spontaneous abortion, possibly incomplete , with potentially dangerous uterine bleeding or maternal or fetal death |
Precautions or Contraindications for Cytotec - Women of childbearing age (unless women is capable of using effective contraceptives) - pregnant women - children under 12 |
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Interactions of Misoprostol with antacids decrease rate of absorption - recommend that antacids be given at least 2 hours away - should not be of a magnesium type (which exacerbates diarrhea) |
Sucralfate (Carafate) - inhibitor of pepsin (another antiulcer agents acts different way) - administered on an empty stomach - then reacts with hydrochloric acid in stomach to form a paste that adheres to mucosa = protecting the ulcer from irritation - the therapeutic effects of drug result from local (e.e at ulcer site) rather than systemic activity |
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Side effects of Sucralfate - rare - constipation (occasionally) |
Interactions of Sucralfate - possible with sucralfate altering absorption of certain drugs - avoid giving other drugs within 2 hours of sucralfate (esp antibiotics and antacids) - Antacids may decrease binding of sucralfate to mucosa, decreasing effectiveness (separate administration times by 30 mins) |
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-Helicobacter Pylori Treatment - bacterial infection major role in development of gastritis, gastric and duodenal ulceration and gastric cancer - treated successfully with multiple-drug regimens (over 14 days) |
Patient education on Helicobacter Pylori Treatment - avoid cigarette smoking (decrease effectiveness of med in healing of duodenal ulcers) - structuring of environment to reduce stress factors, decrease tension (facilitate healing of ulcers) - not taking antacid within 2 hours of any drug - taking med on reg basis and avoid abrupt withdrawal- could lead to rebound hypersecretion of gastric acid - taking sucralfate (Carafate) 1 hour before meals and at bedtime with food and avoid magnesium products to lessen incidence of diarrhea - Taking PPIs esomeprazole (nexium), lansoprazole (prevacid), omeprazole (prilosec) on an empty stomach; - Take Rabeprazole (Aciphex) and pantoprazole (protonix) given without regard to meals - self-medication with OTC PPis not intended for immediate relief of heartburn - PPIs available as delayed-released dosage forms (should not be chewed, broken or crushed) |
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GI Antispasmodic or Anticholinergics - Dicyclomine: anticholinergic and antimuscarinic agent used to treat irritable bowel syndrome and other functional disturbances of GI motility - help calm the bowel - GI anticholinergics work by decreasing motility (smooth muscle tone) in GI tract |
Side effects of dicylomine (esp in older adults) can include - dry mouth, constipation - blurred vision, dizziness, drowsiness - urinary retention (decreases smooth muscle tone in urinary tract) - tachycardia, palpitations - confusion (esp in older adults) |
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Precautions or Contraindications of dicyclomine - Glaucoma (narrow angle) - Obstructive GI disease and ulcerative colitis - Obstructive uropathy (BPH and bladder obstruction) - Myasthenia gravis -lactation |
Interactions of dicylomine - Phenothiazines (decreased antipsychotic effectiveness, increased anticholinergic side effects) - Tricyclic antidepressants (increased anticholinergic side effects) - Opiate agonist (additive depressive effects on GI motility or bladder function) |
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Agents for Inflammatory Bowel Disease - Salicylates - Glucocorticoids |
Inflammatory Bowel Disease (IBD) - chronic condition that causes inflammation in the lining of the GI tract - includes Crohn's disease and ulcerative colitis - abnormal defecation (may be predominant constipation of diarrhea) |
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- NO cure for IBD Treatment: strategies focus on symptom control and improvement of life Salicylates |
Salicylates - Mesalamine (Asacol, Rowasa) prodrug sulfasalazine (azulfidine) - have chemical structures similar to those of aspirin and exhibit anti-inflammatory activity in GI tract - used to manage Crohn's disease and ulcerative colitis - designed to reach ileum and colon, bypassing stomach and upper intestines *safe for long term use and well tolerated in most patients |
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Side Effects of Salicylates (often more frequent and severe with sulfasalazine) - Anorexia, nausea, vomiting, diarrhea, and dyspepsia - Abdominal pain, cramps, bloating (with rectal administration) - Headache, weakness, dizziness, and rash - Intolerance to sulfasalazine can be minimized by taking enteric-coated product (Azulfidine EN-tabs) |
Precautions and contraindications with sulfasalazine - allergy to salicylates - allergy to sulfonamides with sulfasalazine (can cause anaphylaxis or asthma attacks) - allergy to sulfites (Rowasa enema) - Renal impairment - hepatic impairment with sulfasalazine |
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Interactions with Sulfasalazine include - warfarin (increased risk of hemorrhage) - Methotrexate (increased bone marrow suppression) - Cyclosporine (decreased efficacy) - Oral diabetic agents (hypoglycemia) - Folic acid (absorption is inhibited) |
Glucocorticoids (prednisone, prednisolone, hydrocortisone enema) - treat moderate to severe active forms of IBD in patients who are inadequately controlled with salicylates - the oral steroids do not require direct contact with inflamed intestinal tissue to be effective |
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Antidiarrheal Drugs - Bismuth Subsaicylate - Opiate Agonist: Diphenoxylate with Atropine and Loperamide - Probiotics - Clostridum Difficile Infection |
Antidiarrheal agents - act in various ways to reduce the number of loose stools Drugs: bismuth subsalicylate, Opiate Agonists: Diphenoxylate with Atropine and Loperamide, Probiotics, C. Diff infection |
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Bismuth Subsalicylate -(eg.g Kaopectate, pepto-bismol) has anti-infective and antisecretory properties - a direct mucosal protective effect and weak antacid and anti-inflammatory effects - Kaopectate brand products have been reformulated several times (generic still available) |
Side effects of Bismuth subsalicylate - transient, occasional constipation - discoloration of tongue and stool (black color) - ringing in ears |
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Interactions with Bismuth subsalicylate - when these agents are administered concurrently with meds such as - Warfarin (increases bleeding) - Aspirin and methotrexate (increases toxicity) - Quinolones and tetracyclines (decreased bioavailability) |
Precautions or contraindications for Bismuth subsalicylate - Salicylate (include aspirin) hypersensitivity - Children (< 12 years) or teenagers recovering from chickenpox or influenza (risk of Reye's syndrome) - Coagulation abnormalities and ulcers - Pregnancy and Lactation |
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Patient education for Bismuth subsalicylate - avoid self medication for longer than 48 hours or if fever develops (no longer than 48 hours) - diet of bland nature (exclude rough skin apples and no sugar added) food contain natural pectin - adequate fluid intake intake of oral electrolyte products to prevent dehydration - contract physician immediately if complications develop or condition worsens and if observing blood in stool - not using Bismuth subsalicylate if allergic to salicylate (include aspirin) and in children or teens recovering from chickenpox of influenza |
Opiate Agonists: Diphenoxylate with Atropine and Loperamide (anti-diarrhea) - sowing intestinal motility, thus allowing for more reabsorption of fluid - Lomotil - combining diphenoxylate with atropine (schedule C-V controlled substance) - Loperamide (Imodium) - available various forms are OTC products except for some capsule forms (remain Rx only) |
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Side Effects of Diphenoxylate with Atropine and Loperamide can include - anticholinergic effects with Lomotil (drying of secretions, blurred vision, urinary retention, lethargy, confusion, or flushing - abdominal distention, nausea or vomiting with Lomotil or Imodium |
Precautions or Contraindications of Diphenoxylate with Atropine and Loperamide - Diarrhea caused by infection or poisoning - fever over 101 F - Young children under 3 years - pregnancy - C. difficile colitis associated with antibiotics - obstructive jaundice apply to older adults * |
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Patient Education Diphenoxylate with Atropine and Loperamide - (taking antidiarrheal drugs should be instructed regarding) - not exceeding recommended dosage; short term (48 hours) only - adequate fluid intake and bland diet - reporting side effects /complications to physician immediately or if symptoms persist or worsen |
Probiotics - living microorganisms that can alter a patient's intestinal flora and may provide benefit in numerous GI diseases - Lactobacillus acidophilus: acid-producing probiotic bacterium (several OTC forms) - help reestablish normal intestinal flora - administered orally for treatment of simple uncomplicated diarrhea caused by antibiotics, infection irritable colon, colostomy or amebiasis. |
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Probiotic types - capsules, tablets, powder, granules (taking directly or mixed with cereal, food, milk, juice or water - found in yogurt (activia) and other dairy foods for replacement of intestinal tract bacteria |
Side effects of Lactobacillus - tend to be mild and digestive (gas, bloating) in nature |
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Precautions or contraindications for Lactobacillus - anyone with high fever; weakened immune system - sensitive to milk products - long-term use, unless directly by physician - Patients with prosthetic heart valves or valvular heart disease (risk of bacteremia) |
Saccharomyces boulardii (Florastor) - a yeast used in dairy fermentation - derived from intestinal microbiota of healthy humans - is probiotic often started within 3 days of antibiotic initiation and conintued for 3 days after disontinuation to prevent diarrhea |
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Clostridium Difficile Infection (CDD) - C diff. one of the most common causes of infectious diarrhea in U.S. symptoms: may include watery diarrhea, nausea and or abdominal pain or tenederness |
Complications of Clostridium Difficile Infection - include sepsis, renal failure, toxic colitis and death - CDD is caused primarily by eradication of native intestinal flora with broad spectrum antimicrobials and overuse of PPI and H2-blocker therapy |
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Oral Medication of CDD - include metronidazole (Flagyl) or vancomycin opiates and antidiarrheal meds may decrease GI motility, thereby increasing toxins in intestines so their use should be avoided |
Antiflatulents (e.g. simethicone) - used to treat symptomatic treatment of gastric bloating and postoperative gas pains by helping break up gas bubbles in GI tract - No Side Effects, precautions and contraindications or drug interactions have been reported Education: avoid gas-forming food (onions, cabbage and beans) |
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Precautions or Contraindications apply only to infant colic because of limited information on safety to children* |
Laxative and Cathartics - Bulk-Forming Laxatives - Stool Softeners - Emollients - Saline Laxatives - Stimulant Laxatives - Osmotic Laxatives - Chloride Channel Activators |
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Laxative: promote evacuation of the intestine and are used to treat constipation - cathartics or purgatives (promote rapid evacuation of the intestine and alteration of stool consistency |
Laxative can be subdivided into 7 categories - Bulk-Forming Laxatives - Stool Softeners - Emollients- Saline Laxatives - Stimulant Laxatives - Osmotic Laxatives - Chloride Channel Activators |
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Prevention and Relief of constipation is better achieved - natural methods: high-fiber diet, adequate fluid intake, good bowel habits, and exercise - normal frequency of bowel movements varies from daily to several times a week. * when constipation occurs, cause should be identified before laxatives are used |
Bulk-Forming Laxatives (fiber supplements: psyllium, cellulose derivatives, polycarbophil and bran) - soften the stool by absorbing water and increase fecal mass to facilitate defecation - treatment of choice for simple constipation and unrelieved by natural methods (products must be dissolved or diluted according to manufacturer's directions) - proper dosage: one to three times per day - laxative effect apparent within 12-72 hours |
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Bulk-forming laxative - choice for older adults or laxative-dependent patients - useful in maintaining regularity for patients with diverticulosis - increasing bulk of stools in patients with chronic water diarrhea |
Precautions or Contraindications of Bulk-Forming Laxatives - apply to patients with acute abdominal pain, - partial bowel obstruction - dysphagia (difficulty swallowing) - esophageal obstruction |
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Patient education on Bulk-forming Laxatives - dissolve products completely in one full glass of liquid and following with another glass of fluid to prevent obstruction - administer immediately when dissolved before thickening accurs |
Stool Softeners - (Docusate) -surface-acting agents that moisten stool through a detergent action and administered orally - dosage required to soften stools varies depending on condition and patient response - choice for pregnant or nursing women and children with hard dry stools. - onset action 12-72 hours |
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Side effects of Stool Softeners - rate with occasional mild, transitory GI cramping or rash Precautions or contraindications: - acute abdominal pain or prolonged use (more than 1 week) without medical supervision - Caution: avoid stool softeners that also contain stimulant laxatives (ex: eri-Colace, Senokot-S) |
Patient Education for Stool Softeners - discontinuance with any signs of diarrhea or abdominal pain - avoid use longer than 1 week without medical supervision - interaction with mineral oil = mucosal irritation and systemic absorption of mineral oil - taking large quantities of fluids to soften stool - checking package label to be sure no cathartics included |
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Emollients: promote stool movement through intestine by softening and coating the stool - mineral oil may be administered orally and effective in 6-8 hours - sometimes administered rectally as oil-retention enema 60-120 mL |
Side effects of emollients - seepage of oil from rectum causing anal irritation - malabsorption of vitamins A,D, E and K only with prolonged use |
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Precautions or contraindications for oral mineral apply to - children under 5 years old - bedridden, debilitated, or geriatric patients - patients with dysphagia, gastric retention, or hiatal hernia - pregnancy - prolonged use - concomitant(naturally accompanied) use of stool softeners |
Patient Education on Mineral oil Emollient - avoid frequent / prolonged use - use caution if trouble swallow or with aspiration of oil (potential of lipoid pneumonitis if aspirated) never take mineral at bedtime - Interaction with docusate (stool softener) can faciliate absorption of mineral oil, possibly increasing risk of toxicity |
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Saline Laxative (e.g. milk of magnesia or citrate of magnesia) - promote secretion of water into intestinal lumen- should be taken only infrequently in single doses - should NOT be taken on a regular or repeated basis unless directed by physican - onset of action is -0.5 - 3 hours |
Side effects of Saline Laxative used for prolonged periods or in overdoses can include - electrolyte imbalance - CNS symptoms, including weakness, sedation and confusion - Edema - Cardiac, renal and hepatic complications |
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Precautions or contraindications of Saline Laxative apply to - long-term use - heart failure or other cardiac disease - Edema, cirrhosis or renal disorders - those taking diuretics - acute abdominal pain - colostomy |
Patient Education on Saline Laxative - using caution as products of different strengths - avoiding saline cathartics with certain medical conditions - avoiding frequent or regular use of saline cathartics |
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Osmotic Laxatives - Glycerin, lactulose, polyethylene glycol (PEG) and sorbitol - exert an action that draws water from tissues into the feces and reflexively stimulates evacuation - used to treat encephalopathy (brain and nervous system damage) in hepatic failure precipitated by GI bleeding and other conditions - response and side effects vary with preparation - response may take 24-48 hours |
Side effects of Osmotic Laxatives - nausea, vomiting, flatulence and abdominal cramps - Glycerin rectal suppositories or enemas usually cause evacuation of colon within (14-60 mins) Glycerin: may produce rectal irritation or cramping pain |
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Polyethylene glycol (Miralax) response -seen in 0.5 to 3 hours - two to four days of therapy may be required to produce bowel movement - side effects: similar to other drugs in this category; high doses of Miralax can cause elcetrolyte imbalances (hyponatremia, hypokalemia) with prolonged or excessive use |
Chloride Channel Activators - Lubiprostone (Amitiza) unique oral agent for treatment of constipation - increases intestinal fluid secretion by activating specific chloride channels in intestinal epithelium - alters stool consistency and promotes regular bowel movements without altering electrolyte balance or producing tolerance - most patients experience bowel movement within 24 hour of first dose |
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Side Effects of Lubiprostone (Chloride Channel Activators) - nausea and diarrhea - headache Precautions/Contraindications - severe diarrhea or bowel obstruction - renal or hepatic impairment - pregnancy and breast-feeding |
Patient Education for Chloride Channel Activators (Lubiprostone) - high fiber diet to prevent constipation (roughage) - bran, whole grain cereals, fresh fruit and veggies - adequate fluid intake - develop good bowel habits (regular and at unrushed time of day - regular exercise to develop muscle tone - avoid any laxative with acute abdominal pain, nausea, vomiting or fever - avoid laxatives if medical conditions present, unless prescribed by doctor (bulk-forming laxatives are safest in long-term) on short term, infrequent basis - reporting any prolonged constipation |
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Antiemetics - used in prevention or treatment of nausea, vomiting, vertigo or motion sickness - prevention is preferred over treatment of established nausea and vomiting Types: Anticholinergics, Antidopaminergics, Serotonin-Receptor Antagonists |
Anticholinergics: - dimenhydrinate (Dramamine) or scopolamine are used to treat prophylaxis of motion sickness - motion sickness mediated by cholinergic and histaminic receptors in inner ear - Greatest effectiveness: Transderm-Scop patch applied behind ear 4 hour before anticipated exposure to motion (do not cut patch) and effective up to 72 hours |
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Dramamine administered orally 30 mins before exposure to motion - Both dimenhydrinate (Dramamine) and scopolamine are available for IM injection in patients who have already developed motion sickness |
Meclizine (Antivert) - antihistamine used in prevention and treatment of nausea, vomiting and or vertigo associated with motion sickness - in the symptomatic treatment of vertigo associated with the vestibular system (e.g. Meniere's disease) - onset of action about 1 hour and effects persist 8-24 hours after a single oral dose -*produces fewer adverse anticholinergic effects (dry mouth, confusion, urinary retention than scopolamine) can cause drowsiness but to a lesser degree than Dramamine * not recommended for ages under 12 |
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Antidopaminergics - Dopamine-receptor antagonists interfere with stimulation of chemoreceptor trigger zone (CTZ) in brain, blocking messages to GI tract - most frequently used agents to control nausea and vomiting in this class = prochlorperazine (brand name Compazine- no longer marketed), and promethazine (Phenergan) related to phenothiazines - used for symptomatic relief and must be supplemented by restoration of fluid and electrolyte balance and determination of cause of vomiting |
Antagonism of Dopamine receptors in other areas of brain (involved movement) can lead to extrapyramidal reactions (tremors, difficulty walking and muscular rigidity) * common for this class at high doses |
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Prochlorperazine shows high incidence of extrapyramidal reactions - esp in psychiatric patients receiving phenothiazines long term or in children * not recommended for children under 12 (caution with older adults- not for long term use) |
Promethazine (Phenergan) - treatment of choice for preoperative preventive antiemetic effect or postoperative treatment for nausea and vomiting - can be given deep IM (50 mg/mL concentration) or via central line (25 mg/ mL concentration only), but never subcutaneously due to risk of serious tissue injury that may occur |
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Metoclopramide (Reglan) - dopamine-receptor antagonist unrelated to other agents - antiemetic and stimulant of upper GI motility - accelerates gastric emptying and intestinal transit - used in variety of GI motility disorders (esp gastric stasis , shot-term up to 12 weeks) treatment of GERD, and for prevention of cancer chemotherapy induced emesis. - Extrapyramidal reactions can also occur* |
Serotonin: major Neurotransmitter involved in emesis located in the gut |
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Serotonin-receptor antagonists - block serotonin receptors found centrally in the CTZ and peripherally in the intestines to control emesis. |
Ondansetron (Zofran) and dolasetron (Anzemet) used for prevention and treatment of post-operative nausea and vomiting (PONV) and for the control of chemotherapy-induced nausea and vomiting (CINV) *these agents have fewer side effects (mainly headache, dizziness, drowsiness and diarrhea) |
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Side effects of Antiemetics vary with drug and dosage but most commonly include - confusion, anxiety, restlessness (esp in older adults) - sedation, drowsiness, vertigo, weakness, and headache - diarrhea and depression (with Reglan) - dry mouth and blurred vision - Extrapyramidal reactions (involuntary movements) esp in children and older adults with antidopaminergics - cardiac arrhythmias, QT prolongation with high doses or too fast IV administration |
Precautions or contraindications with antiemetics - children and adolescent (increased risk of movement disorders) with antidopaminergics) - pregnancy and lactation - debilitated, emaciated or older adult patients (require reduced dose) - angle-closure glaucoma - prostatic hypertrophy - cardiac arrhythmias or hypertension - seizure disroders (seizure threshold lowered) - COPD and asthma (Phenergan suppresses cough reflex) |
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Interactions of antiemetics result in potentiation of a sedative effect occur with - CNS depressants including tranquiliziers, hypnotics, analgesics, antipsychotics, alcohol, muscle relaxants (potentiation of sedative effects) - Drugs that prolong QT intervals (antiarrhythmics, tricylic antidepressants, phenothiazines, atypical antipsychotics,"mycin" and quinolone antibiotics and others |
Interactions of antiemetics continued - Metoclopramide - SSRI antidepressants (serotonin syndrome with promethazine and metoclopramide) serotonin syndrome caused by excess serotonin release - lead to muscle rigidiyy, increased temp, change in blood pressure, confusion and eventually death *administer only as directed |
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Medication = Condition Nexium = GERD Antivert = Motion sickness Rowasa = Inflammatory Bowel Disease IBD Prevacid = GERD Transderm-Scop = Motion Sickness Dulcolax = Constipation (laxative) Simethicone - Flatulence (gas bloating) Imodium = Diarrhea Phenergan = Nausea and Vomiting |
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