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32 Cards in this Set
- Front
- Back
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What drugs are histamine type-2 blockers?
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All end in -tidine
Cimetidine Ranitidine Famotidine Nizatidine |
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What is the MOA of the histamine type-2 blockers?
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Reversibly inhibit H2 receptors on the basolateral membrane of the parietal cell
Prompt onset of action and relief of symptoms Inhibit 20-50% of acid depending on dose and duration |
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What are the adverse effects of the histamine type-2 blockers?
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Primarily GI related - nausea, vomiting, diarrhea, constipation
Some CNS related - drowsiness, fatigue, headache High dose IV in renal compromised patients can induce worse CNS effects |
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What are the rare side effects of the H2 blockers?
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Cimetidine decreases testosterone binding to androgen receptor - gynecomastia in men and galactorrhea in women
Blood dyscrasias |
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What are the drug interactions of the H2 blockers?
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Cimetidine has lots of drug drug interactions - inhibits several CYP450 isoenzymes
Ranitidine 10% of the CYP450 inhibition of cimetidine Can inhibit absorption of agents that need an acidic pH for gastric absorption |
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What are the relative contraindications for the H2 blockers?
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Renal disease
Caution in pregnancy |
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What drugs are proton pump inhibitors (PPI's)?
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All end in -prazole
Omeprazole Esomeprazole Lansoprazole Dexlansoprazole Pantoprazole Rabeprazole |
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T or F: PPI's are acid labile pro-drugs.
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True
Have an enteric coating, delayed release |
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What is the MOA of the PPI's?
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Covalently bind to sulfhydryl groups of H+/K+ - ATPase at parietal cell secretory sites, inhibiting gastric acid secretion
Inhibit 50-90% of acid Most effective at reducing acid *Inhibits pump induced egress of gastric acid |
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What are the adverse effects of the PPI's?
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Primarily GI related - nausea/vomiting/diarrhea/constipation
Latest major risk - CDAD - clostridium difficile-associated diarrhea CNS effects Generalized myalgias, fatigue, and myopathies |
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What are the drug interactions of the PPI's?
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Omeprazole - CYP450 inhibition - many drug-drug interactions
Affect duration/elimination of other drugs Inhibit absorption of agents that need acidic pH for gastric absorption |
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What are the relative contraindications for the PPI's?
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Reduce dose in hepatic disease
Caution in pregnancy - C for omeprazole, B for all others |
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What drugs are surface acting agents?
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Sucralfate
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What is the MOA of sucralfate?
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In acid it undergoes cross-linking from interaction with stomach acid and forms a viscous, sticky polymer which adheres to epithelial cells around ulcers - prevents acid access to ulcer site
May also stimulate local prostaglandin and mucous production and growth factor *Does NOT affect pH* |
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What uses does sucralfate have?
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Duodenal ulcers
Aphthous ulcers Oral mucositis with radiation Radiation proctitis/ulcers (enema) Bile reflux gastropathy |
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What are the adverse effects of sucralfate? Contraindications?
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Adverse effect: Constipation (Al(OH)3)
Contraindication: renal failure |
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What drugs are PGE-1 analogs?
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Misoprostol
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What is the MOA of misoprostol?
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Prostaglandin E1 analog
Provides protective prostaglandins to gastric mucosa and reduces gastric acid release Less potent than H2 blockers and PPI's |
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What are the uses for misoprostol?
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Prevention of NSAID induced gastric ulcers
Off label for pregnancy terminations, cervical ripening |
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What are the adverse effects of misoprostol? Contraindications?
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Adverse effects: GI related - nausea/vomiting/diarrhea
Contraindications: Pregnancy (unless specifically used for the the off label issues) IBD |
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What are the bismuth compounds?
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Pepto-bismol
Kaopectate Lots of others |
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What is the MOA of the bismuth compounds?
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Exact is unknown
Believed to increase production of bicarb and mucous and may bind to ulcer site; also antibacterial action *Also used in combo pack for H pylori |
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What are the antibacterial properties of the bismuth compounds?
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Prevents microbial attachment to mucosa
Inactivates enterotoxins Disrupts bacterial cell wall |
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*What are the adverse effects of the bismuth compounds?
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Constipation
Black/dark stools LOTS of drug interactions |
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What are the contraindications of the bismuth compounds?
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Antiplatelets and anticoagulants
Diabetics Renal failure |
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What is a MUST for H pylori treatment?
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Combination therapy
At least 2 antibiotics Acid reducer |
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What is metronidazole?
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Pro drug activated by electron transfer process creating nitro radicals which kills the organism
H pylori antibiotic |
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What are the adverse effects of metronidazole?
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Dry mouth/nausea/vomiting
Abdominal pain Metallic taste!! Disulfiram like reaction |
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What are the drug interactions and contraindications of metronidazole?
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Induces metabolism of rifampin and several anti seizure meds
Contraindications: Alcohol CNS diseases Hepatic diseases FIrst trimester pregnancy |
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What is triple therapy for H pylori?
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BID regimen
Contains a PPI Clarithromycin Amoxicillin/metronidazole |
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What is quadruple therapy for H pylori?
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PPI
Metronidazole/clarithromycin Amoxicillin/tetracycline Bismuth subsalicylate |
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How long should PPI or H2 receptor blocker therapy be given after the 10-14 H pylori combo therapy?
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2-6 weeks for complete healing of the ulcers
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