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216 Cards in this Set
- Front
- Back
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Proton pump inhibitors
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Esomeprazole
Lansoprazole Omeprazole |
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H2 receptor antagonists
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Cimetidine
Famotidine Ranitidine |
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Misc GI agents
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Sucralfate
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Neutralizing antacids
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Aluminum hydroxide
Calcium carbonate Magnesium hydroxide Magnesium trisilicate |
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M1 antagonist
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Pirenzepine
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Prokinetic agents
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Bethanechol
Cisapride Erythromycin Metoclopramide Neostigmine Tegaserod |
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Osmotic cathartics
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Magnesium citrate
Magnesium hydroxide Magnesium sulfate Polyethylene glycol |
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Osmotic laxatives
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Lactulose
Mannitol Sorbitol |
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Wetting agents
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Docusate
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Irritant laxatives
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Bisacodyl
Castor oil Glycerin |
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Bulk-forming laxatives
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Methylcellulose
Polycarbophil Psyllium |
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Antidiarrheal agents
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Bismuth subsalicylate
Diphenoxylate Loperamide Octreotide |
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Antiemetic agents
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Diphenhydramine
Dimenhydrinate Dolasetron Hydroxyzine Granisetron Metocloperamide Ondansetron Palonosetron Promethazine |
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Emetic agents
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Apomorphine
Ipecac |
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Bowel disease
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6-mercaptopurine
Budesonide Alosetron Azathioprine Mesalamine Olsalazine Sulfasalazine |
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Esomeprazole
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Proton pump inhibitor
covelantly modifies active site of H/K ATPase prodrug requires acid activation - acid labile lower acid secretion 90%, need 2-5 days interacts with warfarin, diazepam, cyclosporine |
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Lansoprazole
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Proton pump inhibitor
covelantly modifies active site of H/K ATPase prodrug requires acid activation - acid labile lower acid secretion 90%, need 2-5 days interacts with warfarin, diazepam, cyclosporine |
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Omeprazole
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Proton pump inhibitor
covelantly modifies active site of H/K ATPase prodrug requires acid activation - acid labile lower acid secretion 90%, need 2-5 days interacts with warfarin, diazepam, cyclosporine Unique- Omep. inh. clearance of disulfram and phenytoin, inc. clearance of imipramine, antipsychotics, tacrine and theophylline |
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Cimetadine
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H2 blocker
blocks base level of acid secretion by ECL cells decrease acid by 70% good for nocturnal acid, duodenal ulcers tolerance/rebound long term use cimet. decrease testosterone binding (decreased sperm, imp, gynecomastia), hydroxylation of estradiol (galactorrhea) |
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Famotidine
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H2 blocker
blocks base level of acid secretion by ECL cells decrease acid by 70% good for nocturnal acid, duodenal ulcers tolerance/rebound |
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Ranitidine
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H2 blocker
blocks base level of acid secretion by ECL cells decrease acid by 70% good for nocturnal acid, duodenal ulcers tolerance/rebound |
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Sucralfate
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Misc GI agent
makes a sticky pH neutral polymer coating stress ulcers, sticks better to duodenal ulcers acid activated, take before food, avoid PPI's and atacids Side FX: contsipation |
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Aluminum hydroxide
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Neutralizing antacid
slow acting delays emptying, slows motility Rebound acid secretion constipation, nausea, binds tetracyclines, poss. PO4 loss |
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Calcium carbonate
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Neutralizing antacid
rebound acid secretion |
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Magnesium hydroxide
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Neutralizing antacid
fast acting rebound acid secretion contraindicated in renal disease |
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Magnesium trisilicate
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Neutralizing antacid
fast acting rebound acid secretion silica is absorbed and may form renal stones contraindicated in renal disease |
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Pirenzapine
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M1 antagonist
blocks basal secretion from ECL cells ~as effective as low dose of histamine blocker |
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H. pylori treatment
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acid neut., antibacterials, cytoprotection, (eg: Proton pump inhibitor, 2 antibiotics, bismuth)
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Bethanechol
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Prokinetic agent
activates M2 and M3 receptors SDFX: bradycardia, flushing, diarreah, cramps, salivation, blurred vision |
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Neostigmine
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Prokinetic agent
Acetylcholinesterase inhibitor Used acutely to counter an ileus |
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Metoclopramide
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Prokinetic agent
Dopamine receptor antagonist increases lower esophageal tone and upper GI motility laxative, used for nausea and vomiting in dysmotility syndromes, antiemetic SDFX: dystonias, parkinsoniasm, tardice dyskinesia w/ chronic use |
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Tegaserod
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Prokinetic agent
partial serotonin 5-HT4 agonist in gut used for females with IBS, improves lower bowel motility mildly effective, SDFX diarreah and headache |
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Cisapride
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DON'T USE - NOW OFF MARKET
Prokinetic agent 50HT4 receptor and adenylate cyclase stimulant used for GERB SDFX: fatal arrhythmias, interactss with k+ channel |
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Erythromycin
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Prokinetic agent
macrolide antibiotics are motilin agonists macrolide antibiotics cause gastric dumping - can move bezoars and improve emptying with ilieus, scleroderma, and pseudo-obstructions fast dumps painful - not chronic use |
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Magnesium citrate
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Osmotic cathartic
cause water retention Mg may stimulate CCK receptors and increase motility cause bowel emptying with frequent watery stool |
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Magnesium hydroxide
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Osmotic cathartic (milk of magnesia)
cause water retention Mg may stimulate CCK receptors and increase motility cause bowel emptying with frequent watery stool |
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Magnesium sulfate
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Osmotic cathartic
cause water retention Mg may stimulate CCK receptors and increase motility cause bowel emptying with frequent watery stool |
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Polyethylene glycol
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Osmotic cathartic
cause water retention cause bowel emptying with frequent watery stool |
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Lactulose
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Osmotic laxative
draw water into gut used for constipation with opioid use and vincristine lactulose uniquely drops luminal pH by bacterial fermentation and can trap NH4 from hepatic disease and detox colon |
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Mannitol
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Osmotic laxative
draw water into gut used for constipation with opioid use and vincristine |
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Sorbitol
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Osmotic laxative
draw water into gut used for constipation with opioid use and vincristine |
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Docusate
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Stool wetting agent
surfactant that allows mixing of fatty substances and water stool softer- does not increase frequency |
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Bisacodyl
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Irritant laxative
oral or rectal don't chew or mix with milk or antacids - ensure tablet reaches site of action in small intestine and avoid gastric irritation od causes catharsis |
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Castor oil
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Irritant laxative
used as cathartic, laxative, to induce labor made from castor bean (also makes ricin) speeds small bowel motility 4 ml laxative, 16 ml catharsis |
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Glycerin
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Irritant laxative
suppository hydroscopic agent and lubricant |
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methylcellulose
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bulk-forming laxative
wall-paper paste, hydroxycut fiber based regular soft stools may adsorb other drugs may exacerbate intestinal obstructions |
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Psyllium
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bulk-forming laxative
grass-seed husk fiber based regular soft stools may adsorb other drugs may exacerbate intestinal obstructions |
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Polycarbophil
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bulk-forming laxative
fiber based regular soft stools may adsorb other drugs may exacerbate intestinal obstructions |
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Diphenoxylate
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Anti-diarrheal agent
opioid, piperidine derivitave can have CNS effects, packed with atropine to discourage abuse |
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Loperamide
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Anti-diarrheal agent
mu-opioid receptor agonist stops bowel motility - 40-50x more potent than morphine does not enter CNS |
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Octreotide
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Anti-diarrheal agent
parenteral octopeptide to combat secratory diarrhea from hormone secreting tumors used for post surgical gastric dumping & diarrhea assoc w/chemo SDFX: nausea, bloat, inj site pain, long term use assoc w/gallstones |
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Bismuth Salicylate
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Anti-diarrheal agent
clay and oil of wintergreen salicylate released in stomach, absorbed systematically |
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ondansetron
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anti-emetic
serotonin receptor agonist/ antagonist serotonin promotes gut motility acts centrally on CTZ and STN, peripherally in small intestine excretion thru liver 3.9 hours |
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granisetran
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anti-emetic
serotonin receptor antagonist serotonin promotes gut motility acts centrally on CTZ and STN, peripherally in small intestine excretion thru liver 9-11.6 hrs |
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Dolasetron
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anti-emetic
serotonin receptor antagonist serotonin promotes gut motility acts centrally on CTZ and STN, peripherally in small intestine excretion thru liver 7-9 hrs |
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Palonosetron
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anti-emetic
serotonin receptor antagonist - highest affinity serotonin promotes gut motility acts centrally on CTZ and STN, peripherally in small intestine Parenteral only excretion BY KIDNEY 40 hrs |
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Metoclopramide
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Anti-emetic
dopamine receptor antagonist strongly affect CTZ D2 receptors, inc forward motility stops emesis, promotes defecation preferred for chemo nausea SDFX: dissociative dysphoria, parkinsonian effects |
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Promethazine
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Anti-emetic
dopamine receptor antagonist strongly affect CTZ D2 receptors, inc forward motility stops emesis, promotes defecation preferred for chemo nausea SDFX: dissociative dysphoria, parkinsonian effects |
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Hydroxyzine
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Anti-emetic
antihistamine, H1-receptor antagonist motion sickness, post-op act on brainstem and vestibular apparatus |
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Diphenhydramine
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Anti-emetic
antihistamine, H1-receptor antagonist motion sickness, post-op act on brainstem and vestibular apparatus |
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Diphenhydrinate
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Anti-emetic
antihistamine, H1-receptor antagonist salt of diphenhydrinate motion sickness, post-op act on brainstem and vestibular apparatus |
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Apomorphine
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emetic agent
acts locally and on CTZ given sub-Q largely superseded by activated charcoal |
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Mesalamine
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Inflammatory bowel disease
5- aminoslaicylic acid delayed release capsules to jejunum inhibition of TNF-alpha, NF-kappa beta UC- acute flare-ups, maintaining remission Crohn's useful for flare-ups headache, dyspepsia, skin rash, diarrhea |
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Ipecac
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emetic agent
acts on CTZ given orally shortly after ingestion of toxin largely superseded by activated charcoal because of danger of choking |
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Sulfasalazine
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Inflammatory bowel disease
cleaved by colonic bacterial enzymes to yield mesalamine (5-ASA) inhibition of TNF-alpha, NF-kappa beta UC- acute flare-ups, maintaining remission Crohn's useful for flare-ups most SDFX - sulfa group: headaches, nausea, fatigue, allergic |
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Olsalazine
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Inflammatory bowel disease
cleaved by colonic bacterial enzymes to yield mesalamine (5-ASA) inhibition of TNF-alpha, NF-kappa beta UC- acute flare-ups, maintaining remission Crohn's useful for flare-ups headache, dyspepsia, skin rash, diarrhea |
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Prednisone
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Inflammatory bowel disease
glucocorticoid taget general immune response acute exacerbation, severe disease 40% responsive, 40% dependent, 20% do not respond SDFX: immunosupression, endocrine disruption |
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Budesonide
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Inflammatory bowel disease
glucocorticoid 200x more potent than predisone, 1/10 as available, most removed by first pass - topical in bowel taget general immune response acute exacerbation, severe disease 40% responsive, 40% dependent, 20% do not respond SDFX: immunosupression, endocrine disruption |
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6-mercaptopurine
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Inflammatory bowel disease
inhibits DNA synthesis maintain remission in UC and Crohns SDFX: pancreatitis, rash, fever, arthralgias, bone marrow sup, nausea, vom |
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Azathioprine
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Inflammatory bowel disease
converted to 6-mercaptopurine inhibits DNA synthesis maintain remission in UC and Crohns SDFX: pancreatitis, rash, fever, arthralgias, bone marrow sup, nausea, vom |
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Alosetron
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Irritable bowel syndrome
5-HT3 antagonist used for diarrheal prominant IBS |
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Anticoagulants
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heparin sulfate
-protamine sulfate (heparin antagonist) warfarin -menadione (vitamin K, warfarin antidote) |
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Low molecular weight heparins
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Dalteparin
Enoxaparin Fondaparinux |
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Direct thrombin inhibitors
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Argatroban
Bivalirudin Lepirudin |
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Thrombolytics
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Tissue plasminogen activator
Streptokinase Urokinase |
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Antiplatelet drugs
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Abciximab
Aspirin Clopidogrel Ticlopidine Tirofiban |
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Heparin
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Anticoagulant
variable polysaccharide IV(immediate)/subQ (30 min delay) inhibits thrombin, Xa, IXa (not VIIa) therapy monitored by PTT toxicity: bleeding, clotting, thrombocytopenia (counterindication), hyperkalemia Antagonists: stop infusion, protamine sulfate |
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Dalteparin
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Anticoagulant
Low molecular weight heparin uniform activity |
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Enoxaparin
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Anticoagulant
Low molecular weight heparin uniform activity |
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Fondaparinux
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Anticoagulant
Low molecular weight heparin uniform activity smallest - won't bind platelets |
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Argatroban
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Direct thrombin inhibitor
independant of ATII short acting, hepatically cleared use when heparin is needed, heparin induced thrombocytopenia |
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Lepirudin
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Direct thrombin inhibitor
independent of ATII recombinant hirudin, renally cleared anticoagulation in heparin induced thrombocytopenia |
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Bivalirudin
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Direct thrombin inhibitor
independent of ATII synthetic analog of hirudin anticoagulation in heparin induced thrombocytopenia |
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Warfarin
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Anticoagulant
ant K dependent gamma-carboxylation of II, VII, IX, and the end. anticoags C and S INR used to monitor can be given orally highly bound to albumin inac. by liver and kidney - 40 hr t.5 reduce dose for liver failure MANY drug interactions vitamin K antagonizes toxicities: bleeding (esp if NSAIDS), teratogen, skin necrosis antidotes - fresh frozen plasma, K |
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Streptokinase
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Thrombolytic
47 kDa, act after 1:1 complex with plasminogen - large dose needed to overcome neutr. antibodies t.5 30 min nonspecific- induce systemic fibrinolytic state, consume fibrinogen adverse: excessive bleeding, anaphylaxis, fever, can only use for one period of time |
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Urokinase
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Thrombolytic
54 kDa from human cells, no abs rapidly met by liver, t.5 10-15 min can be used multiple times, expensive nonspecific- induce systemic fibrinolytic state, consume fibrinogen adverse: excessive bleeding, no allergies |
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Tissue plasminogen activator
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Thrombolytic
70 kDa, recombinant, no Abs rapidly met in liver, t.5 3 min continuous infusuin most expensive nonspecific- induce systemic fibrinolytic state, consume fibrinogen adverse: excessive bleeding, no allergies |
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Aspirin
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Antiplatelet drug
irreversibly inhibits cyclooxygenase permanently inactivates platelets (lifespan ~10 days) bleeding, gastritis |
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Clopidogrel
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Antiplatelet drug
oral, long duration, long onset prevent platelet aggregation similar to clopidogrel with fewer toxicities |
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Ticlopidine
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Antiplatelet drug
oral, long duration, long onset prodrug, binds to platelet purinergic receptors that evoke aggregation prevent thrombosis in cerebral vascular disease toxicity: neutropenia in 1% patients |
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Abciximab
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Antiplatelet drug
c7E3 antibody - chimeric human-mouse Ab binds to platelet glycoprotein IIb/IIIa receptors and inhibits fibrinogen binding to platelets and aggregation |
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Tirofiban
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Antiplatelet drug
small molecule inhibitor of IIb/IIIa on platelets given IV continuous infusion, very short duration of action |
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AT1 antagonists (ARBs)
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candesartan
irbesartan losartan valsartan |
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ACE inhibitors
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captopril
enalapril lisinopril |
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Serotonin agonists
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sumatriptan
zolmitriptan |
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Serotonin partial agonists
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ergonovine
ergotamine methysergide |
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Serotonin antagonists
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cyproheptadine
ketanserin |
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Losartan
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AT1 antagonists (ARBs)
competitive potent nonpeptide AT1 lack some of the side effects of ACE inhibitors don't affect kininase II |
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Valsartan
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AT1 antagonists (ARBs)
competitive potent nonpeptide AT1 lack some of the side effects of ACE inhibitors don't affect kininase II |
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Irbesartan
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AT1 antagonists (ARBs)
competitive potent nonpeptide AT1 lack some of the side effects of ACE inhibitors don't affect kininase II |
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Candesartan
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AT1 antagonists (ARBs)
competitive potent nonpeptide AT1 lack some of the side effects of ACE inhibitors don't affect kininase II |
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Captopril
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ACE inhibitor
antihypertensive, essential hypertensive works in pts without elevated renin or AngII MI, HF SDFX: cough, hypotension, hyperkalemia, acute renal failure in pts with renal insufficiency |
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Enlapril
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ACE inhibitor
antihypertensive, essential hypertensive works in pts without elevated renin or AngII MI, HF SDFX: cough, hypotension, hyperkalemia, acute renal failure in pts with renal insufficiency |
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Lisinopril
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ACE inhibitor
antihypertensive, essential hypertensive works in pts without elevated renin or AngII MI, HF SDFX: cough, hypotension, hyperkalemia, acute renal failure in pts with renal insufficiency |
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Cyproheptadine
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Serotonin receptor antagonist
nonselective 5HT1/2 antagonist tx symptoms from carcinoid tumors sd FX like H1 histamin r antagonists |
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Ketanserin
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Serotonin receptor antagonist
5HT2 selective lowers arterial pressure in htn blocking 5HT2 on vasc sm muscle, and blocking alpha1 adrenergic r on vsm |
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Ergonovine
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Serotonin receptor partial agonist
partial 5HT agonist, weak antagonist diagnostic vasospastic angina used to control postpartum bleeding |
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Ergotamine
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Serotonin receptor partial agonist
partial 5HT2 agonist VSM stimulant Tx acute migraines, postpartum bleeding |
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Methysergide
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Serotonin receptor partial agonist
5-T2/1 receptors VSM stimulant Tx symptoms of carcinoid tumors |
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Sumatriptan
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Serotonin agonist
does not cross BBB 5HT1(b,d,f) agonist only acute migraines, cluster headaches inhibits release of inflammatory peptides, vasoconstriction |
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Zolmitriptan
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Serotonin agonist
crosses BBB 5HT1(b,d,f) agonist only acute migraines, cluster headaches inhibits release of inflammatory peptides, vasoconstriction |
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ACE Inhibitors
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captopril
enalapril lisinopril quinapril |
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AT1 antagonists (ARBs)
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candesartan
losartan valsartan |
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Diuretics
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Butemanide
Furosemide Metolazone Thiazides Torsemide |
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Beta receptor antagonists
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Bisoprolol
Carvedilol Metoprolol |
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Cardiac glycosides
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Digoxin
Digitoxin |
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Aldosterone antagonists
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Eplerenone
Spironolactone |
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Vasodilators
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Hydralazine
Isosorbide Nitroglycerin |
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Beta agonists
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Dobutamine
Dopamine |
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PDE inhibitors
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Inamrinone
Milrinone |
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Drugs that reduce mortality in HF
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ACEI
ARB beta-blockers |
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Captopril
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ACE inhibitor
first line for heart failure - imp survival suppress AngII/AngIII/aldosterone reduce afterload; inc SV, CO; stop na/water retention; stop hypertrophy contraind: renal failure, pregnancy, adv rxn SDFX: hypotension, hyperkalemia, cough, renal failure |
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Enalapril
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ACE inhibitor
first line for heart failure - imp survival suppress AngII/AngIII/aldosterone reduce afterload; inc SV, CO; stop na/water retention; stop hypertrophy contraind: renal failure, pregnancy, adv rxn SDFX: hypotension, hyperkalemia, cough, renal failure |
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Lisinopril
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ACE inhibitor
first line for heart failure - imp survival suppress AngII/AngIII/aldosterone reduce afterload; inc SV, CO; stop na/water retention; stop hypertrophy contraind: renal failure, pregnancy, adv rxn SDFX: hypotension, hyperkalemia, cough, renal failure |
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Quinapril
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ACE inhibitor
first line for heart failure - imp survival suppress AngII/AngIII/aldosterone reduce afterload; inc SV, CO; stop na/water retention; stop hypertrophy contraind: renal failure, pregnancy, adv rxn SDFX: hypotension, hyperkalemia, cough, renal failure |
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Candesartan
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AT1 antagonists (ARBs)
suppresses effects of AngII/III, does not prevent bradykinin degradation (as ACEI do) alternative to ACEI, same risks except no risk of cough and angioedema comparable mortality benefit |
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Losartan
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AT1 antagonists (ARBs)
suppresses effects of AngII/III, does not prevent bradykinin degradation (as ACEI do) alternative to ACEI, same risks except no risk of cough and angioedema comparable mortality benefit |
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Valsartan
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AT1 antagonists (ARBs)
suppresses effects of AngII/III, does not prevent bradykinin degradation (as ACEI do) alternative to ACEI, same risks except no risk of cough and angioedema comparable mortality benefit |
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Bumetanide
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Diuretic (loop diuretic)
preferred to manage congestive symptoms of HF, inh Na/Cl retention reduce fluid volume and preload adv effects: electrolyte and fluid depletion, hypotension, azotemia |
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Furosemide
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Diuretic (loop diuretic)
preferred to manage congestive symptoms of HF, inh Na/Cl retention reduce fluid volume and preload adv effects: electrolyte and fluid depletion, hypotension, azotemia |
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Metolazone
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Diuretic (act in distal tubules)
lesser effect in pts with renal failure manage congestive symptoms of HF inh Na/Cl retention reduce fluid volume and preload adv effects: electrolyte and fluid depletion, hypotension, azotemia |
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Thiazides
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Diuretic (act in distal tubules)
lesser effect in pts with renal failure manage congestive symptoms of HF inh Na/Cl retention reduce fluid volume and preload adv effects: electrolyte and fluid depletion, hypotension, azotemia |
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Torsemide
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Diuretic (loop diuretic)
preferred to manage congestive symptoms of HF, inh Na/Cl retention reduce fluid volume and preload adv effects: electrolyte and fluid depletion, hypotension, azotemia |
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Bisoprolol
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beta receptor antagonist (beta1)
mortality benefit in HF prevent remodeling of heart, anti-arrhythmic benefit, imp Ca handling SDFX: fluid ret, fatigue, bradycardia, hypotension |
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Carvedilol
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beta receptor antagonist (alpha1, beta 1 and 2)
mortality benefit in HF prevent remodeling of heart, anti-arrhythmic benefit, imp Ca handling SDFX: fluid ret, fatigue, bradycardia, hypotension |
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Metoprolol
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beta receptor antagonist (beta1)
mortality benefit in HF prevent remodeling of heart, anti-arrhythmic benefit, imp Ca handling SDFX: fluid ret, fatigue, bradycardia, hypotension |
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Digoxin
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Cardiac glycoside
naturally occuring steroid no longer first line increase force of cardiac contraction by inc Ca, inc CO inhibition of Na/KATPase sensitizes cardiac baroreceptors Reduces renal Na reabsorption - reduces renin release Risks: arrhythmias, GI, CNS, muscle |
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Digitoxin
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Cardiac glycoside
naturally occuring steroid similar to digoxin, rarely used no longer first line increase force of cardiac contraction by inc Ca, inc CO inhibition of Na/KATPase sensitizes cardiac baroreceptors Reduces renal Na reabsorption - reduces renin release Risks: arrhythmias, GI, CNS, muscle |
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Eplerenone
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Aldosterone antagonist
reduce mortality in class III/IV HF Risk: life threatening hyperkalemia |
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Spironolactone
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Aldosterone antagonist
reduce mortality in class III/IV HF Risk: life threatening hyperkalemia |
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Hydralazine
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Vasodilator
arterial vasodilator reduce renal vascular resistance hemodynamic improvement with isosorbide - BIDL - increase survival but not as well as ACEI SDFX: headache, GI |
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Isosorbide
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Vasodilator
short acting (dinitrate) or long acting (mononitrate venodilation by supplying NO reduce preload, less effective arteriodilator used with hydralazine nitrate tolerance risks: headache, hypotension |
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Nitroglycerin
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Vasodilator
quick acting vasoactive NO source IV in acute MI nitrate tolerance |
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Dopamine
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Beta agonist
intermediate rate: b receptors, increase contractility high infusion: a receptors, stim art & venous constriction tachycardia may provoke ischemia in pts w/CAD |
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Dobutamine
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Beta agonist
choice for pts w/systolic dysfunction does not activate dopamine receptors stim b1 (inotropic) and b2 (vasodilation) receptors tolerance after several days |
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Inamrinone
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PDE inhibitor
short term support if circulation in advanced heart failure stim contraction and accelerate myocardial relaxation by inc cAMP |
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Milrinone
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PDE inhibitor
short term support if circulation in advanced heart failure stim contraction and accelerate myocardial relaxation by inc cAMP fewer side effects, more PDE3 selective |
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Bile acid sequestrants
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cholestyramine
colestipol |
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HMG CoA reductase inhibitors
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atorvastatin
fluvastatin lovastatin simvastatin pravastatin |
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Fibric acids
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clofibrate
gemfibrozil |
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Miscellaneous atherosclerosis agents
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ezetimibe
nicotinic acid probucol |
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Cholestyramine
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Bile acid sequestrant
safe and effective - large catioinic insoluble resins bind bile acids and prevent reabsorption increase LDL reuptake, increase hepatic VLDL production, inc triglycerides SDFX: dyspesia, const, decreased absorption of drugs |
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Colestipol
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Bile acid sequestrant
safe and effective - large catioinic insoluble resins bind bile acids and prevent reabsorption increase LDL reuptake, increase hepatic VLDL production, inc triglycerides SDFX: dyspesia, const, decreased absorption of drugs |
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Nicotinic acid
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Niacin
water soluble vitamin (part of NAD) inhibits VLDL secretion, ultimitly decreases LDL production decreases triglycerides more than cholesterol no effect on bile SDFX: glucose intolerance, hyperuricemia, ulcer, SRelease & hepatic dysfunction |
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Lovastatin
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HMG CoA reductase inhibitor
competetively inhibit decrease cholesterol synthesis, upregulate LDL r, decrease LDL first pass metabolism, mild hepatotoxicity, rhabdomyolysis |
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Simvastatin
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HMG CoA reductase inhibitor
competetively inhibit decrease cholesterol synthesis, upregulate LDL r, decrease LDL first pass metabolism, mild hepatotoxicity, rhabdomyolysis |
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Pravastatin
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HMG CoA reductase inhibitor
competetively inhibit decrease cholesterol synthesis, upregulate LDL r, decrease LDL first pass metabolism, mild hepatotoxicity, rhabdomyolysis |
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Fluvastatin
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HMG CoA reductase inhibitor
competetively inhibit decrease cholesterol synthesis, upregulate LDL r, decrease LDL first pass metabolism, mild hepatotoxicity, rhabdomyolysis |
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Atorvastatin
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HMG CoA reductase inhibitor
competetively inhibit decrease cholesterol synthesis, upregulate LDL r, decrease LDL first pass metabolism, mild hepatotoxicity, rhabdomyolysis |
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Gemfibrozil
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Fibric acid
increase activity of lipoprotein lipase clears chylomycrons and VLDL quickly lowers triglycerides (VLDL) and raises HDL cholesterol SDFX: GI, hepatic, myositis |
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Clofibrate
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Fibric acid
increase activity of lipoprotein lipase clears chylomycrons and VLDL quickly lowers triglycerides (VLDL) and raises HDL cholesterol SDFX: GI, hepatic, myositis |
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Probucol
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cholesterol reduction
increases LDL catabolism, binds to LDL, blocks LDL oxidation SDFX: prolongs QT interval (ventricular arrythmias), lower HDL |
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Ezetimibe
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cholesterol reduction
absorbed and glucuronidated excreted into bile & feces impairs intestinal absorption of cholesterol |
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High LDL drug therapy
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1. Bile acid sequestrants
2. Nicotinic acid or HMG CoA reductase inhibitor 3. Combo of 1 & 2 |
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High LDL and triglycerides drug therapy
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1. Weight loss, alcohol restriction
2. Nicotinic acid or gemfibrozil 3. Bile acid sequestration or HMG CoA reductase inhibitors in combo with 2 4. Combo of any two: nicotinic acid, gemfibrozil, or HMG CoA reductase, increased risk of toxicity |
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High triglyceride (nl LDL) drug therapy
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1. Weight loss, alcohol restriction
2. Gemfibrozil or nicotinic acid |
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Low HDL drug therapy
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1. Diet, excercise, stop smoking
2. Nicotinic acid or gemfibrozil (no studies for benefit) |
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Na+ channel blockers
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Disopyramide
Procainamide Quinidine Lidocaine Flecainide Propafenone |
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K+ channel blockers
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Amiodarone
Dofetilide Sotalol |
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Ca2+ channel blockers
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Diltiazem
Verapamil |
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Beta blockers
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Esmolol
Propanolol |
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Cardiac glycosides
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Digitalis
Digoxin |
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Miscellaneous arrhythmia drugs
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Adenosine
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Procainamide
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Na channel blockers
Most atrial and ventricular arrhythmias slows upstroke and duration of cardiac APs. depress SA &AV, prolongs refractory period (QRS) preferentiall binds open and inactive NA channels avoid long term therapy - lupus-related effects, accumulation of NAPA metabolite in renal failure |
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Lidocaine
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Na channel blocker
IV only, DOC for ventricular tachycardia, prevention of v. fib in MI not for atrial/AV shortens phase 3 repol, decreases duration of APs, shortens QRS, greater effects on purkinje and ventricular fibers associates w/open and inactive channels, dissoc. from resting, raises excitability threshold renal disease no effect (liver metab) Toxicity: least cardiotoxic, CNS, well tolerated generally |
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Flecainide
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Na channel blocker
used for supraventricular arrhythmias, suppresses premature ventricular contractions, not for pts w/ vent. tachyarrhythmias from MI open and inactive Na channels, slow dissoc., decrease in conductance, inc AP threshold Prolongs phase 0 depol w/ou affecting duration, no effect on QT/refract period toxicity: narrow index, CHF, CNS, arrhythmias |
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Amiodarone
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K channel blocker
3-10 day t.5, hepatic act/excr, 35-65% nonavailability low dose- use to maintain nl rhythm in atrial fib prevention of vent. tachycardia pediatric arrhythmias oral/iv slow down phase 3 repol, increase duration of AP, prolong QT/refractory period toxicity: "last resort drugs" accumulation in tissues, thyroid, liver, photodermatitis |
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Dofetilide
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K channel blocker
low dose- use to maintain nl rhythm in atrial fib prevention of vent. tachycardia pediatric arrhythmias oral/iv slow down phase 3 repol, increase duration of AP, prolong QT/refractory period toxicity: "last resort drugs" accumulation in tissues, thyroid, liver, photodermatitis |
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Sotalol
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K channel blocker
12 hr t.5, 100% bioavail, renal excr low dose- use to maintain nl rhythm in atrial fib prevention of vent. tachycardia pediatric arrhythmias oral/iv slow down phase 3 repol, increase duration of AP, prolong QT/refractory period toxicity: "last resort drugs" accumulation in tissues, thyroid, liver, photodermatitis |
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Verapamil
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Ca channel blocker
oral/iv 7 hr t.5, liver met. supraventricular tachyarrhythmias, antianginal, reduce ventricular rate in atrial fib slows down phase 4 depol, increase SA and AV APs blocks open and inac. L-type C channels prolongs PR int/refractory period toxicity: constipation, edema, nervousness |
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Diltiazem
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Ca channel blocker
oral/iv 7 hr t.5, liver met. supraventricular tachyarrhythmias, antianginal, reduce ventricular rate in atrial fib slows down phase 4 depol, increase SA and AV APs blocks open and inac. L-type C channels prolongs PR int/refractory period toxicity: constipation, edema, nervousness |
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Propranolol
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Beta-adrenergic blocker
supraventricular tachycardias, prevention of recurrent MI prolongs AV node conductance by inhibition of PKA-dependant facilitation of L-type Ca channels |
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Esmolol
|
Beta-adrenergic blocker
supraventricular tachycardias, prevention of recurrent MI prolongs AV node conductance by inhibition of PKA-dependant facilitation of L-type Ca channels |
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Adenosine
|
Antiarrhythmic
used for acute supraventricular tachycardia rapid IV bolus - elim w/in seconds prolongs AV node conductance by act. of K/Ach currents and inhibition of L-type Ca channels |
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Digoxin
|
Cardiac glycoside
inhibits Na/K/ATPase - inotropic effect used for supraventricular tachycardias, esp in HF patients prolongs refractory period, sensitizes baororeceptors (vagal tone), reduces AV node conduction |
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Digitalis
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Cardiac glycoside
inhibits Na/K/ATPase - inotropic effect used for supraventricular tachycardias, esp in HF patients prolongs refractory period, sensitizes baororeceptors (vagal tone), reduces AV node conduction |
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Selective beta antagonists
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acebutolol
atenolol esmolol metoprolol |
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Non-selective beta antagonists
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Naldolol
Pindolol Propanolol Timolol |
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PDE5 inhibitors
|
Tadalafil
Sildenafil Vardenafil |
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Ca channel blockers
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Verapamil
Diltiazem |
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Dihydropyridines
Ca channel blockers |
Amlodipine
Felodipine Nicardipine Nifedipine Nimodipine |
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Nitrovasodilators
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Isosorbide dinitrate
Nitroglycerin Nitroprusside sodium |
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Miscellaneous Antianginals
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Aspirin
Clopidogrel Ranolazine |
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Nitroglycerin
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Nitrovasodilator
first pass hepatic metabolism dilate arteries, venodilator, decrease platelet activation Nitrate tolerance - cease 8-12 hours SDFX: headache, hypotension, reflex tachycardia, GI/oral irritant, no PPD5 inhibitors |
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Isosorbide dinitrate
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Nitrovasodilator
3-5 hrs, admin 3-4x daily dilate arteries, venodilator, decrease platelet activation SDFX: headache, hypotension, reflex tachycardia, GI/oral irritant, no PPD5 inhibitors |
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Nitroprusside sodium
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Nitrovasodilator
dilate arteries, venodilator, decrease platelet activation SDFX: headache, hypotension, reflex tachycardia, GI/oral irritant, no PPD5 inhibitors |
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Nitrate-PDE5 interaction
|
excess NO, excess cGMP,VSM relaxation, enhanced fall in blood pressure
contraindication |
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Acebutolol
|
Cardioselective (b1) beta-antagonist
DOC for angina, in combination with nitrates b1 receptors- sinus node decrease HR & contractility & renin release Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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Atenolol
|
Cardioselective (b1) beta-antagonist
DOC for angina, in combination with nitrates b1 receptors- sinus node decrease HR & contractility & renin release Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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Esmolol
|
Cardioselective (b1) beta-antagonist
DOC for angina, in combination with nitrates b1 receptors- sinus node decrease HR & contractility & renin release Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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Metoprolol
|
Cardioselective (b1) beta-antagonist
DOC for angina, in combination with nitrates b1 receptors- sinus node decrease HR & contractility & renin release Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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nadolol
|
Non-selective (b1 &b2) beta-antagonist
b1 receptors block- sinus node decrease HR & contractility & renin release b2 receptor block- vasoconstriction, bronchoconstriction, impaired glycogenolysis Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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pindolol
|
Non-selective (b1 &b2) beta-antagonist
b1 receptors block- sinus node decrease HR & contractility & renin release b2 receptor block- vasoconstriction, bronchoconstriction, impaired glycogenolysis Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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propanolol
|
Non-selective (b1 &b2) beta-antagonist
b1 receptors block- sinus node decrease HR & contractility & renin release b2 receptor block- vasoconstriction, bronchoconstriction, impaired glycogenolysis Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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timolol
|
Non-selective (b1 &b2) beta-antagonist
b1 receptors block- sinus node decrease HR & contractility & renin release b2 receptor block- vasoconstriction, bronchoconstriction, impaired glycogenolysis Adverse effects: bronchospasm, hyperglycemia, hyperlipidemia, impotence containdications: asthma, bradycardia, AV block, insulin dept diabetes |
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Diltiazem
|
Ca channel blocker
angina, Htn, supraventricular arrhythmias avoid in HF decrease contractility of cardiac myocytes - block L-type Ca channels reduce O2 demand, increase O2 supply (dilate arteries) SDFX: hypotension, dizziness, gingival inf, HF, bradycardia, arrhythmias |
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Verapamil
|
Ca channel blocker
angina, Htn, supraventricular arrhythmias ESPECIALLY avoid in HF decrease contractility of cardiac myocytes - block L-type Ca channels reduce O2 demand, increase O2 supply (dilate arteries) SDFX: hypotension, dizziness, gingival inf, HF, bradycardia, arrhythmias |
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Amlodipine
|
Ca channel blocker- dyhydropyridine
angina,htn relax arteries, minimal effect on veins less negative inotropic effect SDFX: dizziness, hypotension, peripheral edema, gingival inflammation |
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|
Felodipine
|
Ca channel blocker- dyhydropyridine
angina,htn relax arteries, minimal effect on veins less negative inotropic effect SDFX: dizziness, hypotension, peripheral edema, gingival inflammation |
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|
Nicardipine
|
Ca channel blocker- dyhydropyridine
angina,htn relax arteries, minimal effect on veins SDFX: dizziness, hypotension, peripheral edema, gingival inflammation |
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|
Nifedipine
|
Ca channel blocker- dyhydropyridine
relax arteries, minimal effect on veins can worsen outcome in acute MI and should not be used |
|
|
Nimodipine
|
Ca channel blocker- dyhydropyridine
relax arteries, minimal effect on veins ONLY used in subarachnoid hemorrhage to prevent post repair vasospasm |
|
|
Ranolazine
|
new antianginal
used for chronic refractory angina partial fatty acid oxidation inhibitor inhibits late sodium current - reduces Na and Ca overload in ischemic myocytes improves exercise tolerance no negative chronotropic, inotropic effects minimal HR/BP effects can add to nitroglycerin and beta blockers |
|
|
Stable angina drug therapy
|
acute: sublingual nitroglycerin
Chronic: beta-blockers, aspirin, statins ca channel blockers if not beta blockers |
|
|
Unstable angina drug therapy
|
Nitrates, beta blockers, statins, aspirin, heparin
|
|
|
Clopidogrel
|
Antiplatelet
irreversible ADP antagonist at P2 receptors - prevents platelet aggregation use in combo with aspirin in acute coronary syndrome, MI, stroke SDFX: neutropenia |
