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GI Pharmacology
Byus-GI Pharmacology
Question | Answer |
---|---|
surface mucous and mucous neck cells | secrete mucous |
parietal cells | secrete acid and IF |
chief cells | secrete digestive enzymes |
enterochromaffin cells | secrete histamine |
G cells | secrete gastrin |
histamine | stimulates secretion of acid and IF |
gastrin | stimulates secretion of acid, pepsin, and IF |
regulation of gastric secretion-neural | ACh release directly acts on target cells and indirectly acts via release of gastrin |
regulation of gastric secretion-humoral | release of gastrin which reaches gastric gland via blood circulation |
regulation of gastric secretion-paracrine | histamine present in gastric mucosa (mast cells) and stimulates gastric glands directly |
stimulant of gastric secretion-ACh | stimulates secretion of acid, pepsing, and IF by interacting with muscarinic receptors |
stimulant of gastric secretion-gastrin | a polypeptide present in antral mucosa that stimulates secretion of acid, pepsin, and IF |
stimulant of gastric secretion-histamine | stimulates secretion of acid and IF by interacting with H2 receptors |
"other" stimulants of gastric secretion | alcohol, caffeine, insulin-induced hypoglycemia and some barbiturates |
Vitamin B12 deficiency/pernicious anemia | impairment of IF secretion |
anticholinergic agents | hyposecretory agent: reduce amount/concentration, high doses needed side effects: dry mouth, increased HR blurred vision block ACh at postganglionic parasympathetic site ex) atropine |
muscarinic cholinergic antagonist | hyposecretory agent: reduce amount/concentration, high doses needed side effects: dry mouth, increased HR blurred vision reduce basal secretion of gastric acid |
M1 antagonists | hyposecretory agent: reduce amount/concentration, high doses needed side effects: dry mouth, increased HR blurred vision produce less side effects but are less efficacious than H2 antagonists ex) pirenzepine, telenzepine |
histamine H2-receptor antagonists | hyposecretory agent: reduce amount/concentration use: reduce basal and stimulated acid secretion cimetidine reduces pain, antacid taken, improves healing of peptic ulcer side effects: increased prolactin-->gynecomastia, mental confusion, inhibits |
proton pump inhibitors | hyposecretory agent: reduce amount/concentration prodrugs converted by acidic environment to covalently bond with proton pumps use: patients with hypergastrinemia if not controlled well with H2-antagonists side effects: nausea, diarrhea, inhibi |
prostaglandins | hyposecretory agent: reduce amount/concentration non-specific reduction of basal and stimulated acid output in patients with duodenal ulcers |
acid neutralizing agents | reduce acidity in stomach with minimal effects on secretory process contain weakly basic moiety-->raises stomach pH 1)systemic: can cause metabolic acidosis 2)non-systemic: neutralize acid but poorly absorbed-->minimal effect on electrolyte balance |
sodium bicarbonate | acid neutralizing agents rapid-acting with short duration of action excess leads to systemic alkalosis side effects: acid rebound due to gastrin release-->overproduction of acid, alkalinization of urine |
calcium bicarbonate | acid neutralizing agents rapid acting with prolonged duration of action may cause hypercalcemia and positive-phosphate balance side effects: acid rebound, nausea, frequent constipation |
aluminum antacids | acid neutralizing agents slow-acting side effects: can reduce bioavailability of other drugs, can cause constipation |
magnesium antacids | acid neutralizing agents poorly soluble, excess may elevate pH to 8 or 9 side effects: causes osmotic diarrhea, neurological/neuromuscular/cardiovascular impairments if not excreted by kidney fast enough |
magnesium trisilicate | acid neutralizing agents non-systemic, non-reversible, slow acting rarely elevates pH above 3 byproduct (SiO2) is adsorbent of other drugs |
anti-inflammatory agents | reduce secretion of mucin mucosal barrier "fortifying" agents: protect lining of gastric lumen from effects of acid and pepsin ex) ACTH, cortisone, aspirin |
carbenoxolone sodium | inhibits back diffusion of H+ protects mucosal barrier from bile acids and helps heal duodenal ulcers side effects: can cause water and salt retention and hypokalemia |
prostaglandins | PGE1 analogue used to prevent ulcers in patients taking NSAIDs; ex)misoprostol PGE2-cytoprotective effect; protects gastric mucosa from ulceration and erosion |
antibiotics | acts against H. pylori antifungals and antiparasitics: bismuth, metronidazole, tetracylcine, amoxicillin, clarithromycin use two antibiotics + bismuth side effects: black color to oral cavity or feces *also considered anti-diarrheal agent |
cholestyramine, aluminum | bind bile acids |
metoclopramide | stimulates gastric emptying |
antacids | raises pH increases LES pressure |
cimetidine | inhibits acid secretion |
cholinergic drugs | acts on smooth muscle of GI and urinary tracts, increasing LES pressure ex) bethanecol |
metoclopramide-biochemistry | structural antagonist of D2 and 5-HT3 receptors depresses vomiting center by acting on brain to block dopamine and 5-HT3 receptors and stimulates gut motility |
metoclopramide-GI effects | increases muscle tension of LES improves gastric emptying |
metoclopramide-clinical use | patients who have failed to intubate the duodenum in anesthesia for emergencies in patients with chronic GER superior to antimimetics in treating nausea and vomiting |
metoclopramide-side effects | CNS side effects (bound to dopamine receptors) nervousness, restlessness, drowsiness, blocks dopamine inhibition of aldosterone, stimulates prolactin secretion-->galactorrhea |
maintenance of intestinal motility and peristalsis | layers of smooth muscles intrinsic nerves: PANS stimulatory, SANS inhibitory |
diarrhea | excessive frequency or fluidity of bowel movements |
constipation | decrease in normal frequency of bowel movement accompanied by hard stool mostly caused by poor diet (lacking fiber) |
opiates | non-specific anti-diarrheal agents decrease acid secretion and motility |
synthetic narcotics | non-specific anti-diarrheal agents slow GI motility and insoluble ex) diphenoxylate, loperamide |
anticholinergic agents | non-specific anti-diarrheal agents decrease intestinal tone, decrease peristalsis side effects: dry mouth dizziness, tachycardia, urinary retention |
adsorbents | non-specific anti-diarrheal agents may absorb undesirable constituents from solution (toxins, bacteria, viruses) ex) bismuth salts, aluminum, activated charcoal |
absorbants | non-specific anti-diarrheal agents not absorbed by GI but they absorb water and bile salt ex) dietary fiber, bran, methyl cellulose |
latobacillus cultures | non-specific anti-diarrheal agents used to restore normal bowel flora |
adrenal corticosteroids | specific anti-diarrheal agent used to treat IBD but does not necessarily cure the infection ex) hydrocortisone, prednisone |
anion exchange resins | specific anti-diarrheal agent bind bile salts and remove them ex) cholestyramine, colestipol |
bulk producers-hydrophilic | laxative with water-absorbing capacity: increase volume of intestinal content, leading to reflex peristalsis and defecation ex) pectin, bran |
bulk producers-saline | laxative with non-absorbable salts which absorb water from intestine: increase volume of intestinal content, leading to reflex peristalsis and defecation ex) magnesium salts |
fecal softener-anionic surfactants | laxative that lower surface tension and allow water to penetrate fecal material: mix with fecal mass and act as emulsifying agents to soften fecal material ex) docusate |
fecal softener-lubricant | laxative that may interfere with absorption of fat soluble substances (vitamins): mix with fecal mass and act as emulsifying agents to soften fecal material ex) mineral oil, olive oil |
stimulants-cathartics: diphenylmethane | laxatives that act on colon to stimulate myenteric plexus: alter water and electrolyte fluxes by inducing changes in motility and net absorption of water in the intestine ex) phenolphthalein |
stimulants-cathartics: anthaquinones | laxatives that act on colon: alter water and electrolyte fluxes by inducing changes in motility and net absorption of water in the intestine ex) senna, danthron |
stimulants-cathartics: castor oil | axatives that act on small intestine to reduce water absorption and shorten intestinal transit time: alter water and electrolyte fluxes by inducing changes in motility and net absorption of water in the intestine |