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GI drugs Flashcards

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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
cannabinoids indications
wasting related to AIDS, cancer
26
neurokinin-1-receptor antagonist
aprepitant
27
aprepitant adverse effects
fatigue, dizziness, diarrhea
28
aprepitant indications
cytostatic-induced; combo tx
29
adjunct antiemetic drugs
benzodiazepines, atropine, scopolamine, erythromycin (prokinetic)
30
benzodiazepines antiemetic indications
anticipatory vomiting
31
erythromycin moa
macrolide antibiotic, motilin agonist
32
erythromycin uses
diabetic gastroparesis, postoperative GI atony -> prokinetic
33
metoclopramide moa
central D2 antagonist (dopamine); peripheral M1 agonist
34
metoclopramide uses
antiemetic, gerd, diabetic gastroparesis -> prokinetic
35
metoclopramide pk
oral, im, iv, rectal
36
metoclopramide pd
antiemetic; prokinetic (GI)
37
metoclopramide adverse effects
extrapyramidal symptoms, esp in children; restlessness; drowsiness; with prolonged, high dose -> galactorrhea, gynaecomastia, parkinsonoid
38
most important therapy for diarrhea
drinking balanced fluid to maintain kidney fxn
39
diarrhea-causing drugs
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
drugs for diarrhea treatment
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
loperamide moa
mainly peripheral; opioid receptor agonist; OTC drug
42
loperamide pk
oral
43
loperamide pd
inhibits intestinal fluid secretion; inc intestinal fluid absorption; inc tonic (non-propulsive) intestinal smooth muscle tone
44
loperamide adverse effects
constipation; kids, high dose - opioid-like adverse effects
45
loperamide contraindications
ileus, subileus, fever, antibiotics-associated diarrhea, megacolon, pregnancy, lactation
46
ineffective drugs used for diarrhea
activated charcoal tablets; pektin; kaolin -> placebo, irritable bowel syndrome, 'stool freaks'; drugs w/serious adverse effects -> antibiotics/septics in OTC preps, tannin
47
constipation-causing drugs
ALL opioids - strong; anticholinergics (antidepressants, phenothiazines, antiparkinson drugs); ganglionic blockers; calcium channel antagonists; k-wasting diuretics; 'irritant'-type laxatives (chronic abuse)
48
types of laxatives
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
peptic ulcer drugs
proton pump inhibitors; H2-antagonists; antimicrobial agents; antacids; others - (anticholinergics), prostaglandins, mucosal protective agents (rare)
50
H2 receptor antagonists
cimetidine, ranitidine, famotidine, nizatidine
51
cimetidine characteristics
prototype drug; many pk interactions (cyt p450 inhibition - warfarin, phenytoin, theophylline); antiandrogenic effects; GYNAECOMASTIA
52
ranitidine characteristics
more POTENT; longer duration; no antiandrogenic effects; no gynaecomastia
53
famotidine + nizatidine characteristics
further improved potency, duration; nizatidine - 100% bioavail
54
cimetidine, ranitidine, famotidine, nizatidine pk
oral, IV
55
cimetidine, ranitidine, famotidine, nizatidine adverse effects
mild; headache, diarrhea, muscular pain, confusion
56
proton pump inhibitors (PPI)
omeprazole, lansoprazole, pantoprazole
57
omeprazole, lansoprazole, pantoprazole pk
oral, iv, prodrugs -> activated after secretion from gastric mucosal cells into acid canaliculi
58
omeprazole, lansoprazole, pantoprazole pd
IRREVERSIBLE! binding of proton pump; dose-dependent, complete inhibition of basal and stimulated acid secretion; long duration (up to 3d)
59
omeprazole, lansoprazole, pantoprazole adverse effects
mostly secondary to anacidity (gastric bacterial flora, aspiration pneumonia w/assisted resp)
60
antacids characteristics
weak base + HCL = salt + water; immediate relief from hyperacidity
61
antacids categories
absorbable/poorly absorbable - best in combos; laxative/constipative
62
antacids pd
SHORT duration (~2h); need large qty's - not suitable for ulcers; repeat at short intervals for lasting effect
63
antacids adverse effects
alkalosis (absorble antacids); interference w/absorption of other drugs (chelation, adsorption)
64
typical poorly-absorbable antacid combinations
aluminumhydroxide (promotes constipation); magnesiumhydroxide (promotes laxation)
65
simethicone
de-foaming agent; takes off surface tension -> defoam -> dec bloating
66
misoprostol moa
stable analogue of prostaglandin E1
67
misoprostol pd
cytoprotective; only clinically effective in doses that also inhibit acid secretion
68
misoprostol uses
prevention of ulcers induced by NSAIDs - protects mostly the stomach
69
misoprostol adverse effects
not well tolerated; all ae's associated w/PGs seen - nausea, diarrhea, abdominal cramps, uterine contractions
70
misoprostol contraindications
PREGNANCY
71
sucralfate characteristics
coating agent; combo aluminumhydroxide, sulfated sucrose
72
sucralfate pk
topical action; little systemic absorption
73
sucralfate pd
coats ulcer ground in acidic environment; stimulates PG synth; ineffective when combo w/antacids
74
sucralfate uses
longterm maintenance therapy to prevent recurrence
75
therapeutic issues: peptic ulcer disease
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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