#5 GI pharmacology 10/06/06
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- main causes of peptic ulcer disease?
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1) increase in attack factors = H. pylori, acid, pepsin
2) decrease in defense factors = < mucous barrier - two besic approaches to therapy?
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1) to decrease the acidity and/or peptic activity
2) to enhance the resistance of the mucosa or to protect the base of the ulcer - how to decrease the acidity and/or peptic activity?
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1) by blocking secretion of acid and/or pepsin
2) neutralization of HCL or inactivation of pepsin
3) eradicating H.pylori - drugs to decrease attack
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1) proton pump inhibitors
2) H2-antihistamines
3) antacids
4) antimuscarinics
5) prostaglandins
6) antibiotics
7) antidepressants - proton pump inhibitors (PPI)
-
1) Omeprazole (Prilosec) = prototype
2) Lansoprazole (Prevacid)
3) Rabeprazole (Aciphex)
4) Esomeprazole (Nexium)
5) Pantoprazole (Protonix) - 2) H2-antihistamines
-
1) Cimetidine (Tagamet)
2) Ranitidine (Zantac)
3) Famotidine (Pepcid)
4) Nizatidine (Axid) - 3) antacids
-
1) Mg (OH)2
2) Al (OH)3
3) CaCO3
4) NaHCO3 - 4) antimuscarinics
-
1) Glycopyrrolate (RObinul)
2) Dicyclomine (Bentyl)
3) Methscopolamine (Pamine)
4) Propantheline (Pro-Banthine) - 5) Prostaglandin
- 1) Misoprostol (Cytotec)
- 6) Antibiotics
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1) Metronidazole (Flagyl)
2) Tetracycline
3) Clarithromycin (Biaxin)
4) Amoxicillin (Amoxil) - 7) antidepressant
- 1) Tricyclics
- proton pump involves?
- H/K-ATPase
- ATPase appears to be?
- unique, and is not known to be in other cells = devoid of SE
- Omeprazole (Prilosec)
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1) prototype inhibitor
2) irreversibly inhibits the ATPase - irreversible inhibition of ATPase cause?
-
1) profound inhibition of gastric acid secretion (95-100%) for several days
2) GI bacterial overgrowth
3) diarrhea
4) subsequent colonization of the resp. tract - reversible inhibitor of the pump?
- Lansoprazole (Prevacid) = gastric acid suppression is not prolonged
- drugs which will be decreased in their absorption?
-
1) ketoconazole
2) ampicillin
3) digoxin
4) iron salts - PPI inhibit metabolism of these drugs
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1) phenytoin
2) warfarin
3) diazepam - SE of PPI
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1) headache
2) diarrhea
3) abd. pain
well tolerated - a major fraction of gastric acid is secreted in response to the activation of?
-
1) H2-histamine receptors on parietal cell memb. and
2) the subsequent activation of adenylate cyclase - H2-antihistamines have pronounced effects on both?
- acid and pepsin secretion
- acid and pepsin secretion is elecited by?
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1) histamine
2) gastrin
3) caffeine
4) food
5) insulin
6) vagus stimulation - H2-antihistamines do not directly affect?
-
1) gastrin secretion
2) GI motility
3) LES pressure - H2-antihistamines are most effective when taken at?
- bedtime
- H2-antihistamine OTC for?
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1) acid indigestion
2) sour stomach
3) heartburn - drugs to increase defense
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1) ulcer coating
2) steroid congeners
3) prostaglandins
4) antacids - 1) ulcer coating
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1) Sucralfate (Carafate)
2) Bismuth compounds (Pepto-Bismol)
3) Graviscon - 2) steroid congeners
- 1) Carbenoxolone
- 3) Prostaglandins
- 1) Misoprostol (Cytotec)
- 4) Antacids
- 1) Al(OH)3
- Sucralfate (Carafate)
-
1) a complex of sulfated sucrose and aluminum hydroxide
2) for duodenal ulcers
3) bind to free protein in the base of ulcer craters
4) forms a complex which protects from acid, pepsin, and bile salts
5) stimulate local production of PG-E - SE of Sucralfate
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1) metalic taste
2) mausea
3) constipation
4) < absorption of some drugs - Bismuth subsalicylate (Pepto-Bismol)
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1) selectively bind to ulcers
2) providing a coating and protection from acid and pepsin
3) stimu. mucus production
4) increase PG synthesis
5) to eradicate H.pylori - tripotassium dicitrato-bismuthate
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1) available in Europe
2) a stable colloidal complex - SE of bismuth compounds
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1) black stools
2) black tongue
3) OD of salicylates - Gaviscon
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1) antacid
2) contains alginate
3) protects the mucosa and impaired gastric reflux
4) for GERD - Carbenoxolone
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1) synth. derevative of glycyrrhizic acid
2) > production , secretion, and viscosity of mucus
3) widely used in Europe
4) for gastric and duodenal ulcers - SE of Carbenoxolone
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1) mineralocorticoid activity
2) Na and water retention
3) HTN
4) hypokalemia - Misoprostol (Cytotec)
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1) PG-E1 analog
2) > mucus and HCO3 production
3) < acid production
4) only for ulcer pt who cannot discontinue NSAID use - antacids
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1) neutralize H ion
2) mucosal protection
3) bind injurious substances
4) weak bases, form salt and water
5) > pH to 3.5-4.5
6) consists of metal salts - acid neutralizing capacity (ANC)
- the # of mEq of HCL that can be brought to pH 3.5 in 15 min
- antacids are used for?
-
1) dyspepsia
2) adjuncts to other tx for PUD - magnesium hydroxide
-
1) high neutralizing capacity
2) SE = diarrhea and hyperMg - Aluminum hydroxide
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1) high neut. capacity
2) SE = constipation and hypoPhos
3) SE = decrease bone mass - Calcium carbonate
-
1) moderate neut. capacity
2) liberation of CO2 = abd. distention, nausea, flatulence, belching - large doses of Ca carbonate cause?
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1) transient hyperCa
2) rebound acid secretion
3) milk-alkali syndrome
4) nephrolithiasis - sodium bicarbonate
-
1) high neut.capacity
2) SE = syst. alkalosis, fluid retention, acid rebound, CO2 liberation
3) not for chronic use - Simethicone
- added to some antacids, help to relieve gas
- for eradication of H. pylori
- 1) ranitidine bismuth citrate (tritec) + clarithromycin (Biaxin)
- HELIDAC pack
- tetracycline or amoxicillin + metronidazole + pepto-bismol
- eradication of H.pylori
- omeprazole + clarithromycin
- GERDs
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1) a functional decrease in the tome of LES
2) HCL and bile acids into the esophagus = ulcer, erosive esophagitis
3) heartburn = regurge and dyspepsia - anticholinergics
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1) decrease LES tone
2) never be used for reflux esophagitis - medications that decrease LES tone?
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1) theophylline
2) progesterone
3) nitrates
4) Ca channel blocker - prokinetic agents
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1) favor motion and can improve GI proplusion
2) increase gastric emptying - neural regulation of gastric motility
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1) acetylcholine
2) dopamine
3) serotonin - gastric motility can be stimulated by?
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1) D2 antagonists
2) 5-HT3 antagonists
3) 5-HT4 agonists - motilin receptors
-
1) in small intestine
2) potential target for prolinetic agents
3) erythromycin also stimulate motilin receptors - Metoclopramide (Reglan)
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1) prokinetic
2) 5-HT3 antagonists
3) may act as a D2 antagonists
4) cholinomimetic effect
5) crosses the BBB - SE of reglan
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1) extrapyramidal symptoms
2) depression
3) hyperprolactemia
4) hervousness
5) dystonia
6) abd. cramping
7) anticholinergic SE - Domperidone (Motilium)
-
1) non-US
2) prokinetic
3) D2 antagonist
4) Tx for gastric hypomotility in diabetics - benefit of Domperidone?
- does not cross BBB (no extrapyramidal SE) and is not anticholinergic, and better tolerated
- anti-emetics
-
antagonists of
1) serotonin
2) dopamine
3) acetylcholine
4) histamine - 5-HT3 antagonists
- 1) receptor in GI tract
- N/V believed to be triggered by release of serotonin from ?
- the enterochromaffin cells of the small intestine which then activates 5-HT3 receptors on vagal afferents, triggering the vomiting reflex
- Ondansetron (Zofran)SE
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1) well tolerated
2) HA
3) constipation
4) dizziness - benefit of ondansetron
- not an antagonist of dopamine receptors = no extrapyramidal SE
- Granisetron HCL (Kytril)
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1) for chemo-induced emesis
2) 5-HT3 antagonist - which medication is given with Granisetron HCl to improve acute antiemetic effecacy?
- Dexamethasone
- Alosetron (Lotronex)
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1) 5-HT3 antagonist
2) severe potential GI SE - Alosetron is only approved for last chance in women with?
- irritable bowel syndrome
- other 5-HT3 antagonists
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1) Dolasetron (Anzemet)
2) Palonosetron (Aloxi) - D2 antagonists
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1) Benzamides
2) Metoclopromide (Reglan)
3) Trimethobenzamide (Tigan)
4) Domperidone
5) Phenothiazine
6) Butyrophenones
7) Chlorpromazine (Thorazine)
8) Prochlorperazine (Compazine) - SE of phenothiazine
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1) hypotension
2) sedation
3) extrapyramidal movement disorders - Prochlorperazine (Compazine) IM cause
- dystonias
- Butyrophenones
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1) D2 antagonists
2) Haloperidol (Haldol)
3) Droperidol (Inapsine)
4) for CA chemo.
5) less sedation and hypotension - Corticosteroids
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1) antiemetic
2) Dexamethasone and other glucocorticoids
3) for moderately emetogenic chemo.
4) reduce SE, diarrhea - Cannabinoids
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1) anti-emetic
2) Delta-9-tetrahydrocannabinol
3) for chemo. - SE of cannabinoids
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1) hallucinations
2) disorientation
3) vertigo - tx of motion sickness
- histamine H1-receptor antagonists with anticholinergic + antimuscarinic
- Benzodiazepines
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1) antiemetic
2) Lorazepam (Ativan)
3) Alprazolam (Xanax)