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22 Cards in this Set
- Front
- Back
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H2 antagonist that inhibits binding of DHT to androgen receptor, inhibits metabolism of estradiol (can cause gynecomastia, impotence in men, galactorrhea in women) also effect many many CYPs
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cimetidine
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administered as prodrugs that require activation in acidic environment
Administered in enteric-coated formulations or with NaHCO3-containing formulations They are lipophilic weak bases that after intestinal absorption diffuse readily across membranes. In acidic compartments (parietal cell canaliculus) become ionized and trapped After ionization, they are rapidly converted to reactive sulfenamide cation, which forms a covalent bond with H+/K+ ATPase and irreversibly inhibits it. |
PPI's
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Sucrose complexed with sulfated Al-hydroxide
Negatively charged sucrose sulfate binds to positively charged proteins in erosions forming a physical barrier that restricts further damage Not absorbed, no systemic effects May impair absorption of other medications |
sucralfate
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PGE1 analog
Stimulates mucus and bicarbonate secretion Approved for prevention of NSAIDs-induced ulcers Not widely used due to side effects (cramping, uterine contractions) |
Prostaglandin analogs (misoprostol)
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Bismuth subsalicylate
Probably coats ulcers creating a protective layer Well tolerated, may cause black stools |
Colloidal bismuth compounds
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Antiemetic properties due to the 5-HT3 receptor blockade:
in the vomiting center and CTZ peripheral receptors on vagal and spinal afferent nerves Effective in emesis mediated by vagal stimulation (postoperative, chemotherapy) Not effective in motion sickness Well tolerated. Shown to induce prolongation of QT interval |
ondansetron
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First generation H1 antihistamine
Also has anticholinergic properties (sedating) |
Diphenhydramine
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Causes less sedation (minimal anticholinergic properties)
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Meclizine
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muscarinic receptor antagonis
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Scopolamine
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Prokinetic agent thats a muscarinic receptor agonist
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Betanechol:
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Prokinetic agent thats a AchE inhibitor
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Neostigmine
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prokinetic agents that are D2 receptor antagonists
In the GI D2 receptor inhibit cholinergic smooth muscle stimulation Increase lower esophageal sphincter pressure, enhance gastric emptying, have no effect on small intestine and colon motility Also has central antiemetic actions (blocks D2-receptors in CTZ) Adverse effects: CNS (restlessness, drowsiness, insomnia, anxiety, parkinsonian features, elevated prolactin levels) |
Metoclopramide and domperidone
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Dietary fiber
Methylcellulose (CITRUCEL) Psyllium seed husk (METAMUCIL) Indigestible, hydrophilic colloids that retain water (increases volume) and support bacterial growth Increased bacterial fermentation produces short chain fatty acids, which stimulate motility Bacterial fermentation can lead to gas production (bloating) |
Bulk-forming laxatives
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non-absorbable inorganic salts, create hyperosmotic luminal environment which increases secretion and decreases reabsorption
Mg-oxide (milk of magnesia), Na-phosphate, Mg citrate Produce bowel emptying within 1-3 hours Can produce electrolyte and fluid imbalance |
Saline” Laxatives
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Soften stool material, allowing water and lipids to penetrate
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Docusate (anionic surfactant): can be given orally or as an enema
Glycerin suppository Mineral oil |
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Stimulant laxatives (cathartics
Induce bowel movements through poorly understood mechanisms (direct Poorly absorbed Produce bowel movement 6-12 hours after ingestion Earlier concerns about potential carcinogenic effects not confirmed stimulation of enteric nervous system) |
senna and aloe
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anti diarheal agent that is hydrated magnesium aluminum silicate agents adsorb bacteria, toxins, fluid, decreasing stool liquidity
Not absorbed from the GI, no systemic effects Can affect absorption of other medications |
Kaolin
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anti diarrheal agent that ia a indigestible fruit carbohydrate
Both agents adsorb bacteria, toxins, fluid, decreasing stool liquidity Not absorbed from the GI, no systemic effects Can affect absorption of other medications |
Pectin
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opioid antidiarrheal agent that does not cross BBB, no potential for addiction, no analgesic properties)
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Loperamide
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opioid anti diarrheal agent that at higher doses can lead to opioid dependence
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Diphenoxylate
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Decrease diarrhea caused by excess bile acids (diseases of terminal ileum lead to malabsorption of bile salts
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Cholestyramine
Cholestipol |
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Somatostatin analog
Inhibits intestinal secretion and at low doses stimulates, but at high doses inhibits bowel motility |
Octreotide
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