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PHARM_GI Flashcards

1
Q

How do the bulk forming laxatives work?

A

increase delivery of water to colon, decrease pressure in sigmoid colon, net result is more formed stools

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2
Q

how does docusate (colace) work?

A

anionic surfactant, stool softener, used to reduce strain of defecation

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3
Q

what are the adverse effects of docusate (colace)?

A

can irritate the intestinal mucosa & increase intestinal absorption of other drugs (use only short term)

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4
Q

how does castor oil work?

A

surfactant laxative that is rapid acting and effective anionic surfactant that produces catharsis, stimulates intestinal peristalsis

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5
Q

what are the AEs of castor oil?

A

colic
dehydration
electrolyte imbalance with overdose
can induce uterine contraction in pregnant women

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6
Q

on what part of the GI tract do the stimulant laxatives work on?

A

mostly large bowel

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7
Q

how do stimulant laxatives work?

A
  • increase permeability of intestinal mucosa
  • increase back diffusion of water and electrolytes
  • increase propulsive contractility of colon by stim. colonic myenteric plexus
  • stimulate PG synth. & increase intestinal secretions
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8
Q

what is the most potent class of laxatives?

A

stimulant laxatives

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9
Q

name the stimulant laxatives

A

diphenylmethanes (bisacodyl)

anthraquinones (senokot)

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10
Q

bisacodyl (dulcolax) MOA

A

prodrug that is converted by enteric bacteria into the desacetyl active form, acts as stimulant laxative

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11
Q

anthraquinones (senokot) MOA

A

stimulant laxative that is natural derivatives of senna plant, more gentle than synthetic drugs
-act by promoting colonic motility

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12
Q

what happens if you overdose on bisacodyl?

A

can cause excessive fluid & electrolyte loss, intestinal enterocyte damage leading to colonic inflammatory response

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13
Q

large doses of anthraquinones (senokot) can cause what?

A

can cause abd. pain, nephritis, melanotic pigmentation of colonic mucosa, abnormal color of urine

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14
Q

what is GOLYTELY used for?

A

Polyethylene glycol electrolyte soln used for colonoscopy for complete evacuation

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15
Q

name the 2 laxatives used in IBS

A

lubiprostone

linaclotide

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16
Q

how does lubiprostone work?

A

activates Cl- channels (in PKA independent fashion), increases intestinal fluid secretion and motility and alleviates the symptoms associated with chronic idiopathic constipation (used in IBS for constipation)

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17
Q

what are the 3 different kinds of antidiarrheal agents?

A
  1. agents that absorb water (metamucil)
  2. adsorbers of etiologial factors in the lumen (e.g. pepto-bismol)
  3. agents that alter intestinal motility (opiates)
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18
Q

how does bismuth subsalicylate work?

A

adsorb harmful bacteria, viruses, or toxin

19
Q

what drug is an effective treatment for preventing Traveler’s diarrhea and also treats H. pylori infections?

A

bismuth subsalicylate

20
Q

how do opiates work as antidiarrheal agents?

A

decrease salivary, gastric, & intestinal gland secretions
decrease motility of the stomach & intestines
increase muscle tone
increase tone of muscle sphincters including EAS “reduces urgency”
The overall effect is increasing the contact time between ingested matter and the reabsorbtive intestinal epithelium

21
Q

this drug interacts with intestinal opioid receptors and binds to & inhibits the calcium binding protein calmodulin

A

loperamide (anti-diarrheal)

22
Q

what is the purpose of using anticholinergics as antidiarrheal agents?

A

used for this b/c they are anti-spasmodic

23
Q

what drug is prophylactic only for motion sickness arising from short or long exposure to severe motion

A

scopolamine

24
Q

scopolamine MOA

A

scopolamine is anticholinergic that blocks the activation of muscarinic receptors to ACh. (Cochlear sensation of motion is projected via cholinergic fibers of the auditory nerve to the CTZ)

25
Q

how is scopolamine administered?

A

patch placed near ear

26
Q

what are some of the side effects of using scopolamine?

A

sedation, drowsiness, dry mouth

27
Q

which antidopaminergic blocks therapeutic induced activation of D2 receptors in the CTZ? Also inhibits gastric emptying

A

metoclopramide

28
Q

how do H1 antihistamines work in the treatment of motion sickness?

A

older H1 antihistamines also have anticholinergic effects

29
Q

name the 2 piperazines that are H1 antihistamines

A

cyclizine (OTC)

meclizine

30
Q

which H1 antihistamine has a depressant effect on hyperstimulation of labyrinthine function and is used for vestibular disturbances?

A

meclizine

31
Q

how are antidopaminergics effective antiemetics?

A

they block dopamine receptors in the trigger zone (CTZ)

32
Q

which drug is a centrally acting anticholinergic as well as antidopaminergic and is used for N/V & intractable hiccups?

A

chlorpromazine

33
Q

which antidopaminergic drug blocks receptors in the CTZ and is clinically used post-op for N/V?

A

droperidol

34
Q

which antiemetic antidopaminergic drug is given prophylactically to chemo pts to prevent post-op nausea and vomiting?

A

metoclopramide

35
Q

how are serotonin antagonists effective antiemetics?

A

5-HT antagnoists block 5-HT3 receptors in the stomach and small intestines
-block 5-HT3 receptors in the CTZ that are intimately involved in stimulating the VC to produce emesis

36
Q

which class of antiemetics are the most effective to date?

A

5-HT antagonists

37
Q

which drug is more potent than ondansetron?

A

granisetron (anti-emetic)

38
Q

which 5-HT3 antagonist has the longest half life?

A

dolasetron (anti-emetic)

39
Q

what is the purpose of using corticosteroids, dronabinol, benzodiazepine or aprepitant, in addition to a classic antiemetic drug?

A

these 3 are used to increase the potency of antiemetic drugs and reduce the dose of each individual agent and also reduce the significance of their combined side effects

40
Q

which drug is a substance P/ NK1 receptor antagonist?

A

aprepitant (anti-emetic)

41
Q

which drug is used as an adjunct drug for preventing emesis induced by cytotoxic chemotherapy, crosses the BBB & inhibits emesis via central actions

A

aprepitant (anti-emetic)

42
Q

which class of drugs is used as an adjunct to other antiemetic regimens and is effective for anticipatory vomiting bc they cause somnolence & amnesia lasting for hours?

A

benzodiazepines

43
Q

which class of drugs is considered the foundation for antiemetic therapy?

A

5-HT3 receptor antagonist

GI (12 decks)

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