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Pharmacology > GI drugs > Flashcards

GI drugs Flashcards

1
Q

GI drugs uses

A

most common forms of: nausea/vomiting, diarrhea, constipation, gerd

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2
Q

drugs used for therapeutic emesis

A

ipecacuana; hypertonic saline; apomorphine; comm

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3
Q

ipecacuana

A

ipecac syrup; obsolete

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4
Q

use of drugs to induce emesis

A

to empty stomach after poison ingestion; alternative to/combo with gastric lavage

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5
Q

contraindications of drug-induced emesis

A

ingestion of corrosives (cleaning fluids); ingest aliphatics (petroleum -> lipid pneumonia); somnolence, unconciousness

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6
Q

adverse effects of drug-induced emesis

A

aspiration, vagal syncope, hypochloremia, hypovolemia, absorption of emetic drug (NaCl, ipecac)

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7
Q

antiemetic drugs

A

antihistamines (inhibit dopamine); phenothiazines; dopamine antagonists; 5-HT-antagonists; corticosteroids; cannabinoids (effective, illegal in some states); neurokinin-1-receptor antagonist; adjunct medications

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8
Q

antiemetic antihistamines

A

diphenhydramine, hydroxizine

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9
Q

diphenhydramine, hydroxizine adverse effects

A

sedation

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10
Q

diphenhydramine, hydroxizine indications

A

pregnancy, motion sickness

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11
Q

phenothiazines

A

perchlorphenazine, proemthazine

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12
Q

perchlorphenazine, proemthazine adverse effects

A

epm disturbances, dyskinesias, sedation

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13
Q

perchlorphenazine, proemthazine indications

A

metabolic/endocrine, cns

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14
Q

dopamine antagonists

A

metoclopramide, (domperidon) - risk of arrhythmia -> used in compounds

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15
Q

metoclopramide, (domperidon) adverse effects

A

s.a., but less pronounced

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16
Q

metoclopramide indications

A

widely used to prevent/treat moderate nausea/emesis

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17
Q

5-HT-antagonists

A

ondansetron, granisetron, tropisetron, dolasetron

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18
Q

ondansetron, granisetron, tropisetron, dolasetron adverse effects

A

CONSTIPATION (contraindicated w/opiates), headache

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19
Q

ondansetron, granisetron, tropisetron, dolasetron indications

A

cytostatic-induced EARLY vomiting

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20
Q

antiemetic corticosteroids

A

dexamethasone

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21
Q

dexamethasone adverse effects

A

none

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22
Q

dexamethasone indications

A

intracranial pressure, cytostatic-induced LATE vomiting; given together w/5-HT-antagonists

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23
Q

cannabinoids

A

marijuana, THC (dronabinol), nabilone

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24
Q

marijuana, THC, nabilone adverse effects

A

drowsiness, confusion, amotivational syndrome (prolonged use)

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25
Q

cannabinoids indications

A

wasting related to AIDS, cancer

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26
Q

neurokinin-1-receptor antagonist

A

aprepitant

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27
Q

aprepitant adverse effects

A

fatigue, dizziness, diarrhea

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28
Q

aprepitant indications

A

cytostatic-induced; combo tx

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29
Q

adjunct antiemetic drugs

A

benzodiazepines, atropine, scopolamine, erythromycin (prokinetic)

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30
Q

benzodiazepines antiemetic indications

A

anticipatory vomiting

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31
Q

erythromycin moa

A

macrolide antibiotic, motilin agonist

32
Q

erythromycin uses

A

diabetic gastroparesis, postoperative GI atony -> prokinetic

33
Q

metoclopramide moa

A

central D2 antagonist (dopamine); peripheral M1 agonist

34
Q

metoclopramide uses

A

antiemetic, gerd, diabetic gastroparesis -> prokinetic

35
Q

metoclopramide pk

A

oral, im, iv, rectal

36
Q

metoclopramide pd

A

antiemetic; prokinetic (GI)

37
Q

metoclopramide adverse effects

A

extrapyramidal symptoms, esp in children; restlessness; drowsiness; with prolonged, high dose -> galactorrhea, gynaecomastia, parkinsonoid

38
Q

most important therapy for diarrhea

A

drinking balanced fluid to maintain kidney fxn

39
Q

diarrhea-causing drugs

A

adrenergic blockers ((reserpine)); antimicrobials (tetracyclines, sulfonamides, broad spectrum) - affect flora; bile acids, fatty acids, carcinoid tumor secretions; digestive enzyme blockers (acarbose, orlistat); dietary agents (OLESTRA, some sweeteners); cardiac glycosides - sign of overdose; cholinergic agonists; laxatives; prostaglandins

40
Q

drugs for diarrhea treatment

A

peripheral opioid-receptor agonists (loperamide, diphenoxylate (combine w/atropine)); tinctura opii; somatostatin; alpha2 agonists (clonidine); adjunct meds - spasmolytic drugs; bile-acid induced diarrhea (colestyramine); clostridium-difficile associated enterocolitis (vancomycin; metronidazole)

41
Q

loperamide moa

A

mainly peripheral; opioid receptor agonist; OTC drug

42
Q

loperamide pk

A

oral

43
Q

loperamide pd

A

inhibits intestinal fluid secretion; inc intestinal fluid absorption; inc tonic (non-propulsive) intestinal smooth muscle tone

44
Q

loperamide adverse effects

A

constipation; kids, high dose - opioid-like adverse effects

45
Q

loperamide contraindications

A

ileus, subileus, fever, antibiotics-associated diarrhea, megacolon, pregnancy, lactation

46
Q

ineffective drugs used for diarrhea

A

activated charcoal tablets; pektin; kaolin -> placebo, irritable bowel syndrome, ‘stool freaks’; drugs w/serious adverse effects -> antibiotics/septics in OTC preps, tannin

47
Q

constipation-causing drugs

A

ALL opioids - strong; anticholinergics (antidepressants, phenothiazines, antiparkinson drugs); ganglionic blockers; calcium channel antagonists; k-wasting diuretics; ‘irritant’-type laxatives (chronic abuse)

48
Q

types of laxatives

A

bulk-forming agents (fiber) - bran, psyllium, methylcellulose -> distend bowel -> inc peristalsis; hyperosmolar agents - sorbitol, lactulose, polyethylenglycol (for surgery prep) -> retain water in gut; stool softening/lubricating agents - docusate sodium, glycerin, mineral oil (can cause lipid pneumonia); stimulants/irritants - bisacodyl, castor oil, phenolphtalein, anthrachinones; enema - containing any of others (helps pregnant women push)

49
Q

peptic ulcer drugs

A

proton pump inhibitors; H2-antagonists; antimicrobial agents; antacids; others - (anticholinergics), prostaglandins, mucosal protective agents (rare)

50
Q

H2 receptor antagonists

A

cimetidine, ranitidine, famotidine, nizatidine

51
Q

cimetidine characteristics

A

prototype drug; many pk interactions (cyt p450 inhibition - warfarin, phenytoin, theophylline); antiandrogenic effects; GYNAECOMASTIA

52
Q

ranitidine characteristics

A

more POTENT; longer duration; no antiandrogenic effects; no gynaecomastia

53
Q

famotidine + nizatidine characteristics

A

further improved potency, duration; nizatidine - 100% bioavail

54
Q

cimetidine, ranitidine, famotidine, nizatidine pk

A

oral, IV

55
Q

cimetidine, ranitidine, famotidine, nizatidine adverse effects

A

mild; headache, diarrhea, muscular pain, confusion

56
Q

proton pump inhibitors (PPI)

A

omeprazole, lansoprazole, pantoprazole

57
Q

omeprazole, lansoprazole, pantoprazole pk

A

oral, iv, prodrugs -> activated after secretion from gastric mucosal cells into acid canaliculi

58
Q

omeprazole, lansoprazole, pantoprazole pd

A

IRREVERSIBLE! binding of proton pump; dose-dependent, complete inhibition of basal and stimulated acid secretion; long duration (up to 3d)

59
Q

omeprazole, lansoprazole, pantoprazole adverse effects

A

mostly secondary to anacidity (gastric bacterial flora, aspiration pneumonia w/assisted resp)

60
Q

antacids characteristics

A

weak base + HCL = salt + water; immediate relief from hyperacidity

61
Q

antacids categories

A

absorbable/poorly absorbable - best in combos; laxative/constipative

62
Q

antacids pd

A

SHORT duration (~2h); need large qty’s - not suitable for ulcers; repeat at short intervals for lasting effect

63
Q

antacids adverse effects

A

alkalosis (absorble antacids); interference w/absorption of other drugs (chelation, adsorption)

64
Q

typical poorly-absorbable antacid combinations

A

aluminumhydroxide (promotes constipation); magnesiumhydroxide (promotes laxation)

65
Q

simethicone

A

de-foaming agent; takes off surface tension -> defoam -> dec bloating

66
Q

misoprostol moa

A

stable analogue of prostaglandin E1

67
Q

misoprostol pd

A

cytoprotective; only clinically effective in doses that also inhibit acid secretion

68
Q

misoprostol uses

A

prevention of ulcers induced by NSAIDs - protects mostly the stomach

69
Q

misoprostol adverse effects

A

not well tolerated; all ae’s associated w/PGs seen - nausea, diarrhea, abdominal cramps, uterine contractions

70
Q

misoprostol contraindications

A

PREGNANCY

71
Q

sucralfate characteristics

A

coating agent; combo aluminumhydroxide, sulfated sucrose

72
Q

sucralfate pk

A

topical action; little systemic absorption

73
Q

sucralfate pd

A

coats ulcer ground in acidic environment; stimulates PG synth; ineffective when combo w/antacids

74
Q

sucralfate uses

A

longterm maintenance therapy to prevent recurrence

75
Q

therapeutic issues: peptic ulcer disease

A

all tx include PPI or H2-antagonist and 2 or 3 antimicrobial agents; antimicrobials prevent recurrence (no healing); HP eradication mostly successful; antimicrobials ~10d, PPI ~6wks; symptom relief best w/PPI; healing rate same for PPI/H2-ant; no diet rec; smoking stops healing, promotes recurrence

Pharmacology (15 decks)

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