Wk4 antidiarrheals/laxatives/IBS drugs Flashcards

1
Q

Cisapride

A

Prokinetic –> increased motility

5HT4 agonist (and 5H3 ANtagonist)

Tx: diabetic gastroparesis

**restricted use dt cardiac toxicity

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2
Q

Domperidone

A

D2 receptor antagonist

increase GI motility throughout the entire GI tract

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3
Q

Macrolides (erythromycin)

A

stimulate motilin receptors directly on GI smooth muscle → initiation of migrating motor complex

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4
Q

Metoclopramide

A

D2 receptor antagonist

increase GI motility throughout the entire GI tract

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5
Q

Diphenoxylate

A

Opiate

most effective antidiarrheal

Crosses BBB so abuse potential and needs Rx

mixed with atropine to discourage abuse

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6
Q

Loperamide

A

opiate

most effective antidiarrheal

doesn’t cross BBB so available OTC

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7
Q

Cholestyramine

A

Binds bile salts

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8
Q

Colestipol

A

Binds bile salts

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9
Q

Kaolin/Pectin

A

Absorbant

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10
Q

Bismuth Subsalicylate

MOA as antidiarrheal?

A

inhibits prostaglandin and chloride secretion in the large intestine

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11
Q

Crofelmer use?

MOA?

A

HIV diarrhea

blocks CFTR –> decreases Cl- secretion

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12
Q

Octreotide MOA?

Effects at different doses?

A

Somatostatin analogue

low dose stimulates motility

high dose inhibits motility

overall decrease in secretion

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13
Q

Docusate class?

MOA?

A

Stool softener

surfactant –> softens stool by allowing mixing of aqueous and fatty substances

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14
Q

Mineral Oil Class?

MOA?

A

Stool softener

lubricates feces –> decreased water absorption from stool

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15
Q

Dietary fiber

A

increase mass of stool → distension → enteric reflexes → increased GI motility → decreased transit time through the colon

“stool stabilizers” – also less diarrhea

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16
Q

Anthraquinone

A

Contact cathartic

Stimulates peristalsis

large intestine

less potent

17
Q

Bisacodyl

A

Contact cathartic

Stimulates peristalsis

large intestine

less potent

is given as a prodrug → 6 hour latency

18
Q

Castor oil

A

Contact cathartic

Stimulates peristalsis

large AND small intestine

VERY potent

**uterine contractions

dehydration

19
Q

Linaclotide

A

activates guanylyl cyclase-C on the luminal surface of intestinal epithelial cells

increased intra- and extra-cellular cGMP activates (CFTR) → increased Cl- secretion

Tx: constipation IBS

not in pregnancy or for peds

20
Q

Lubiprostone

A

activation of chloride channel ClC-2 → more Cl- secretion → increased water content in stool

constipation IBS

NOT in PREGNANCY

21
Q

Alvimopan

A

selective μ receptor antagonists that do not cross the BBB (won’t antagonize central analgesic effects of opiate medications)

used to shorten period of postoperative ileus following small or large bowel resection (short term)

**cardiotoxicity

22
Q

Methylnaltrexone

A

selective μ receptor antagonists that do not cross the BBB (won’t antagonize central analgesic effects of opiate medications)

patients receiving palliative care for advanced illness (long term)

23
Q

Lactulose

A

Osmotic cathartic (purgative)

reduces plasma NH4 conc; tx for hepatic encephalopathy

24
Q

Magnesium hydroxide

A

Osmotic cathartic (purgative)

MOA???

25
Q

Sodium Phosphate

A

Osmotic cathartic (purgative)

MOA: increased electrolytes in colon

26
Q

Polyethylene glycol

A

Osmotic cathartic (purgative)

used for whole bowel irrigation prior to colonoscopy/endoscopy

27
Q

TCA’s

Amitriptyline, Desipramine

A

blocking NE reptake into postganglionic sympathetic neurons results in increased NE concentrations in the synapse → increased NE actions on the α2 receptor → decreased ACh release

blocking DA reuptake into enteric interneurons → increased DA concentrations in the synapse → increased D2-mediated inhibition of cholinergic smooth muscle motoneurons

Diarrhea IBS tx

28
Q

SSRIs

Fluoxetine, Paroxetine, Sertraline

A

Increased peristalsis

more 5HT in synapse –> afferent activation

Tx: constipation IBS

29
Q

Alosterone

A

Antidiarrheal

5HT3 antagonist

Tx: diarrheal IBD

**last resort, bad constipation

30
Q

Tegaserod

A

Prokinetic

selective 5HT4 agonist

Tx: constipation IBS

**last resort, big Cardiac side fx

31
Q

cause a characteristic, harmless, brown pigmentation of the colonic mucosa

A

anthraquinones

32
Q

D2 receptor antagonist

does not cross BBB

compassionate use only

not available in USA

A

Domperidone

33
Q

D2 receptor antagonist

crosses BBB

parkisonism

pituitary effects (impotence, galactorhea, menstruation disorders)

A

Metaclopramide

34
Q

Secondary MOA or tegaserod and cisapride:

A

activate cAMP-dependent chloride secretion form the colon