Agents for Diarrhea and Constipation

Question 1

Agents for diarrhea?

Answer 1

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

Question 2

Loperamide

Answer 2

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

Question 3

Diphenoxylate class and indication?

Answer 3

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

Question 4

MOA Diphenoxylate?

Answer 4

• Exert local effect to GI sm mm andi nhibits GI motility

Question 5

Eluxadoline? MOA?

Answer 5

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

Question 6

Eluxadoline indication?

Answer 6

• IBS-D

Question 7

AE of Eluxadoline?

Answer 7

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

Question 8

Contraindications of Eluxadoline?

Answer 8

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

Question 9

Alosetron class and indication

Answer 9

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

Question 10

Alosteron MOA?

Answer 10

blocks GI based 5HT receptors

Question 11

What is the BBW for Alosteron?

Answer 11

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

Question 12

Contraindications for Alosteron?

Answer 12

• 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

Question 13

Crofelemer MOA?

Answer 13

• 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

Question 14

When is Crofelemer used?

Answer 14

• Non infectious diarrhea in HIV patientes on ARV

Question 15

Agents for Constipation?

Answer 15

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

Question 16

Methylnaltrexone, Naloxegol, Alvimopam class and MOA?

Answer 16

• Peripheral opioid antagonist- Constipation
• Peripherally actinv mu opoid receptor antagonist

Question 17

Methylnaltrexone, Naloxegol, Alvimopam indications?

Answer 17

• Opioid induced constipation

Question 18

Alvimopam is only used for _____.

Answer 18

Alvimopam only used for prevention of post op ileu

Question 19

Why can Alvimopam only be used in the hospital?

Answer 19

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

Question 20

Linaclotide class?

Answer 20

GUanylate Cyclase C agonists

Question 21

What is linaclotide MOA?

Answer 21

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

Question 22

Indications for linaclotide?

Answer 22

IBS-C

Chrobnic idiopathic constipation

Question 23

Lubiprostone MOA? Class?

Answer 23

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

Question 24

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

Answer 24

Lubiprostone

Question 25

Lubiprostone indications?

Answer 25

* IBS-C * Chronic idiopathic constipation * Opioid induced constipation

Question 26

Tegaserod class and MOA?

Answer 26

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

Question 27

Tegaserod indications?

Answer 27

* IBS-C in adult women less than 65

Question 28

Tegaserod contraindications?

Answer 28

* Hx of MI/TIA/CVA/Angina * ESRD/severe CKI * Mod to severe hepatic impairment * ischemic colitis obstruction gallbladder dz

Question 29

Absolute contraindication for stimulants?

Answer 29

Ileus

Question 30

What are the bulk forming agents used for?

Answer 30

* Increase bulk volume and water content to increase GI motility * 2-4 days to see

Question 31

Bulk forming AE's and drug drug interaction?

Answer 31

* Bloating and obstruction * needs lots of fluids cauting in CHF and renal failure * Many drug interactions

Question 32

Stool softeners other name?

Answer 32

* Surfactant or emollient laxatives * Docusate salts * Mineral oil

Question 33

Stool softener MOA?

Answer 33

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

Question 34

Loperamide FDA issued drug safety concern?

Answer 34

Cardiac toxicities leading to death