Agents for Diarrhea and Constipation Flashcards

1
Q

Agents for diarrhea?

A
  • Prostaglandin inhibitors
    • Bismuth
  • Opioid Agonists
    • Loperamide
    • Diphenoxylate
    • Eluxadoline
  • 5HT channel blockers
    • Alosteron
  • Chloride channel inhibtor
    • Crofelemer
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2
Q

Loperamide

A
  • Opioid agonsist for diarrhea
  • doesnt have analgesic opiate effects or produce dependence
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3
Q

Diphenoxylate class and indication?

A
  • Opioid agonist
  • Synthetic opiate agonist, with small amounts of atropine (an anticholinergic) to reduce abuse/overdose
  • Indicated for diarrhea
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4
Q

MOA Diphenoxylate?

A
  • Exert local effect to GI sm mm andi nhibits GI motility
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5
Q

Eluxadoline? MOA?

A
  • Opioid agonist
  • Agonist against opioid mu and kappa receptors in GI
    • also an antagonist to the delta opioid receptor in the GI
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6
Q

Eluxadoline indication?

A
  • IBS-D
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7
Q

AE of Eluxadoline?

A
  • GI related
  • Hepatic/Pancreatic toxicity
    • pancreatitis higher risk in patients w/o a gallbladder
  • CNS related
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8
Q

Contraindications of Eluxadoline?

A
  • alcoholism
  • hx of pancreatitis
  • cholecystectomy or bile duct obstruction
  • severe hepatic issue
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9
Q

Alosetron class and indication

A
  • 5HT antagonist
  • Chronic severe IBS-D after several other drugs have not worked
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10
Q

Alosteron MOA?

A

blocks GI based 5HT receptors

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11
Q

What is the BBW for Alosteron?

A
  • Ischemic colitis
  • Risk mitigation strategy- required training to prescribe this
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12
Q

Contraindications for Alosteron?

A
  • Hx or current:
    • Ischemic colitis
    • GI obstruction, perf, stricture, toxic megacolon
    • Diverticulitits, CD, UC
    • impaired circulation
    • Severe hepatic disease
    • Severe constipation, bloody diarrhea, sudden severe abd pain
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13
Q

Crofelemer MOA?

A
  • Cl channel inhibitor used for diarrhea
  • Derivevd from red sap of Croton lechleri tree
  • Inhibits cl ion secretion by blocking cAMP stimulated CFTR and calcium activated cl channels at luminal membrane of intestine
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14
Q

When is Crofelemer used?

A
  • Non infectious diarrhea in HIV patientes on ARV
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15
Q

Agents for Constipation?

A
  • Peripheral opoid antagonist
  • Guanylate Cyclase C agonist
  • Selective Cl channel activators
  • 5HT partial agonist
  • Laxative and Cathartic agents
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16
Q

Methylnaltrexone, Naloxegol, Alvimopam class and MOA?

A
  • Peripheral opioid antagonist- Constipation
  • Peripherally actinv mu opoid receptor antagonist
17
Q

Methylnaltrexone, Naloxegol, Alvimopam indications?

A
  • Opioid induced constipation
18
Q

Alvimopam is only used for _____.

A

Alvimopam only used for prevention of post op ileu

19
Q

Why can Alvimopam only be used in the hospital?

A
  • It carries a risk of MI
  • To prescribe you have to go through REMS training
  • Use less than 15 doeses
20
Q

Linaclotide class?

A

GUanylate Cyclase C agonists

21
Q

What is linaclotide MOA?

A
  • Binds GC-C on luminal surface of intestinal epi and increases intra/extracellualr cGMP which stimulates secretioni of cl and bicarb
22
Q

Indications for linaclotide?

A

IBS-C

Chrobnic idiopathic constipation

23
Q

Lubiprostone MOA? Class?

A
  • Selecctive chloride channel activator
  • Prostaglandin E1 derivative
  • Increases intestinal fluid secfretion by activating GI specific cl channels in luminal cells of intestine
24
Q

Patient on opioid and cannot stop it due to pain. What drugs will not interfere with the opioid receptors?

A

Lubiprostone

25
Q

Lubiprostone indications?

A
  • IBS-C
  • Chronic idiopathic constipation
  • Opioid induced constipation
26
Q

Tegaserod class and MOA?

A
  • Partial agonist of serotonin type 4 receptors in the GI tract
    • stimulates peristalsis and intestinal fluid secretion
    • inhibiits visceral sensitivity
27
Q

Tegaserod indications?

A
  • IBS-C in adult women less than 65
28
Q

Tegaserod contraindications?

A
  • Hx of MI/TIA/CVA/Angina
  • ESRD/severe CKI
  • Mod to severe hepatic impairment
  • ischemic colitis obstruction gallbladder dz
29
Q

Absolute contraindication for stimulants?

A

Ileus

30
Q

What are the bulk forming agents used for?

A
  • Increase bulk volume and water content to increase GI motility
  • 2-4 days to see
31
Q

Bulk forming AE’s and drug drug interaction?

A
  • Bloating and obstruction
    • needs lots of fluids cauting in CHF and renal failure
  • Many drug interactions
32
Q

Stool softeners other name?

A
  • Surfactant or emollient laxatives
  • Docusate salts
  • Mineral oil
33
Q

Stool softener MOA?

A
  • Anionic surfactants soften and lubricate feces
  • increase fluid secretion into GI tract
  • Decrease fluid reabsorption from GI tract
    • mineral oil penetrates stool to soften
34
Q

Loperamide FDA issued drug safety concern?

A

Cardiac toxicities leading to death