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1. Pharmacology > GI: Prokinetics and Antidiarrheal > Flashcards

GI: Prokinetics and Antidiarrheal Flashcards

1
Q

Outer longitudinal muscle

A

Peristalsis (aboral movement, unidirectional)
Myenteric plexus (Cholinergic affects)
Peptide hormone (motilin)

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2
Q

Inner circular muscle

A

Segmentation contraction (narrowed lumen and mixing)
Submucosa plexus
Cholinergic and adrenergic effects

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3
Q

Risk of diarrhea

A

Peristalsis > segmentation contraction

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4
Q

Risk of constipation

A

Segmentation contraction > peristalsis

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5
Q

Drugs regulating peristalsis

A

Cholinergics
Dopamine antagonists (Ach sensitizer)
Miscellaneous
Contrain: GI obstruction!!

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6
Q

Cholinergics

A

Bethanechol, Neostigmine
Ranitidine, nizadidine
Cisapride

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7
Q

Bethanechol (urecholine) MOA

A

Cholinergic agonist
Binds to muscarinic receptors and initiates smooth muscle contraction

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8
Q

Bethanechol uses

A

Gastric emptying in horses
↑ Ileocolic contraction in cattle
↑ bladder smooth muscle contraction

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9
Q

Bethanechol adverse effects

A

Non-specific binding (pleotrophic)
Profound sid effects
Diarrhea

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10
Q

Neostigmine (prostigmin) MOA

A

Acetylcholinesterase inhibitor
Inhibits degradation of Ach (stimulating cholinergic receptors)

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11
Q

Neostigmine uses

A

Myasthenia gravis
Large colon motility (equine)

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12
Q

Ranitidine and Nizatidine MOA

A

H2 blockers and inhibits AcholE

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13
Q

Cisapride MOA

A

Enhances Ach release
Agonist for 5-HT4 receptor

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14
Q

Dopamine antagonists (Ach sensitizer)

A

Metoclopramide (reglan), doperidone

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15
Q

Metoclopramide MOA

A

Antagonist: dopamine and 5HT3 centrally
Agonist: 5HT4
↑ release of Ach

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16
Q

Metoclopramide uses

A

Stimulates upper motility after surgery
Poster operative ileus

17
Q

Domperidone MOA

A

Dopamine antagonist
Doesn’t cross BBB (↓ CNS effects compared to metoclopramide)

18
Q

Domperidone uses

A

Not used in small animals
Treats fescue toxicity and agalactia in mare

19
Q

Miscellaneous peristalsis regulators

A

Erythromycin
Lidocaine

20
Q

Erythromycin

A

Macrolide antimicrobial
Lose dose: nonspecific GI motility by ↑activation of motilin receptor
Side effects: diarrhea (horses)

21
Q

Lidocaine

A

Local anesthetic
Reduces postoperative ileus in horses

22
Q

Lidocaine MOA

A

Suppress transmission of sympathetic tone
Prevent sympathetic reflexive SC
Produce direct excitatory effects on smooth muscle of the intestine
Suppress centrally mediated hyperalgesia

23
Q

Motility Modifiers: Anticholinergics

A

Opioids
Anticholinergics
Mucosal protectants
Adsorbants

24
Q

Opioids _______ segmental contractions

A

Increase
antidiarrheal → constipation

25
Q

Anticholinergic drugs ________ both segmental contractions and peristalsis

A

Decrease

26
Q

Opioids

A

Diphynoxylate (Lomotil): not used
Loperamide (Imodium): OTC

27
Q

Opioid MOA

A

↑ segmentation and tone of GI sphincter
↓ propulsive contractions
Inhibits Ca2+ influx and ↓ calmodulin activity
Stimulates absorption of fluid, electrolytes and glucose

28
Q

Anticholinergics

A

Atropine, Scopolamine, Isopropamide

29
Q

N- Butylscopolammonium bromide

A

Colic treatment in horses
Severe forms of diarrhea
Absence of segmentation movement

30
Q

Anticholinergics MOA

A

↓ GI motility (and intestinal secretions)

31
Q

Contraindications for anticholinergics

A

Gastritis, vomiting, infectious diarrhea

32
Q

Bismuth subsalicylate (pepto bismol)

A

Mucosal protectant and adsorbent
Systemic treatment for acute diarrhea
Adsorb bacterial enterotoxins
Gastric/ intestinal protective effect
Anti-inflammatory

33
Q

Bismuth subsalicylate contraindication

A

Care in admin to cats
Deficient in glucuronyl transferase → toxic metabolic formation

34
Q

Prokinetics

A

Enhance GI transit via interaction with receptors involved in regulation of motility

35
Q

Prokinetics

A

Mosapride
Misoprostol
Colchicine

36
Q

Mosapride

A

Potent 5HT4 receptor agonist
Experimental in horses
Useful for treatment of chronic constipation

37
Q

Mu- opioid receptor antagonists

A

Peripherally acting (can’t cross BBB) on GI secretion and motility
Methylnaltrexone bromide and alvimopan (more potent)

38
Q

Methylnaltrexone bromide

A

Limited use in horses
Inhibits morphine-induced intestinal effects

39
Q

Alvimopan causes increased incidence of …

A

Myocardial infarction

1. Pharmacology (29 decks)

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