Inhibits chloride ion secretion by _blocking cAMP stimulated CFTR _ and _ calcium activated chloride channels_

[Pharm] Diarrhea, Abdominal pain, Constipation Flashcards by Jaime Weber

What are the 4 classes of drugs you would prescribe for DIARRHEA?

Prostaglandin inhibitors

Opioid agonists

Serotonin antagonists

Chloride channel inhibitors

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What is the prostaglandin inhibitor you would prescribe for DIARRHEA?

Bismuth

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What are the (3) opioid agonists that you would prescribe for DIARRHEA?

Loperamide

Diphenoxylate

Eluxadoline

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What is the (1) serotonin antagonist you would prescribe for DIARRHEA?

Alosetron

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What is the (1) chloride channel inhibitor you would prescribe for DIARRHEA?

Crofelemer

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What is the GENERAL MOA of opioid agonists for treating diarrhea?

Anti-propulsive

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What is one of the clever designs put into diphenoxylate to prevent opioid abuse?

Diphenoxylate (opioid agonist) has a small quantity of ATROPINE added to discourage deliberate abuse/over-dosage of drug

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What is the one drug that has a unique indication within the opioid agonist category?

What is that indication?

Eluxadoline

Irritable bowel syndrome, diarrhea predominant subtype [IBS-D]

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What is the major side effect of eluxadoline?

Pancreatitis!!!!

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MOA of alosetron?

Selectively blocks GI BASED 5HT3 receptors

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Indication for alosetron?

Chronic, severe IBS-D that are NOT RESPONSIVE to other conventional therapies in WOMEN

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What are the major side effects associated with ALOSETRON?

GI related = dyspepsia

BLACK BOX = ISCHEMIC COLITIS

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MOA of crofelemer?

Inhibits

chloride ion secretion

blocking cAMP stimulated CFTR* and *calcium activated chloride channels

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What is the super unique indication for CROFELEMER?

Non infectious diarrhea in HIV/AIDS pts that are on ANTI-RETROVIRAL THERAPY

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What is the ONE class of drugs used for abdominal pain?

Antimuscarinic agents

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What are the (3) antimuscarinic agents used in treatment of abdominal pain?

Hyoscyamine

Dicyclomine

Clidinium/Chlordiazepoxide

Side effects of antimuscarinics?

Classic anticholinergic based

Dry mouth

Urinary retention

Constipation

Drowsiness

Mental confusion

Blurred vision

What are the (4) classes of drugs used for treating CONSTIPATION?

Peripheral opioid antagonists

Guanylate Cyclase-C Agonists

Selective Chloride (C2) Channel Activators

Laxative and Cathartic Agents

MOA of LINACLOTHIDE?

Selective guanylate cyclase-C (GC-C) agonist

Stimulates secretion of chloride/bicarb into the intestinal lumen, this results in increased intestinal fluid and accelerated transit

What are the indications for LINACLOTIDE?

Irritable bowel syndrome-constipation predominant subtype [IBS-C]

Chronic idiopathic constipation [CIC]

MOA of LUPIPROSTONE?

Prostaglandin E1 derivative

Increases intestinal fluid secretion by activating GI specific CHLORIDE CHANNELS (CIC-2) in the luminal cells of intestinal epithelium

What is the “claim to fame” indication for LUBIPROSTONE?

Opioid induced constipation (OIC)

(*also treats IBS-C and CIC)

MOA of Methylnaltrexone?

Peripheral MU-OPIOD receptor ANTAGONIST

(MethylnaltrexOne) blocks Mu-Opioid

Indications for methylnaltrexone?

Opioid induced constipation (OIC)

What is the ONE indication for **ALVIMOPAN?**

PREVENTION OF **POST OPERATIVE ILEUS**

What is the **BLACK BOX WARNING** of **ALVIMOPAN?**

RISK OF **MI** Must enter a risk mitigation systmic process (REMS) in order to prescribe

What would be a great class of drugs to prescribe for your patient that complains of: "I poop once every other day, but when I do...MAN it's hard and painful to pass..." Help me

STOOL SOFTENER

What is the one **stimulant** given **pre-colonoscopy for bowel prep?**

Sodium picosulfate

What is the MOA of **stimulants (irritants)?**

IRRITANT to **enterocytes, GI smooth muscle** which leads to **INFLAMMATION** This inflammation leads to an increase in **prostaglandin synthesis**

Contraindications of **stimulants?**

GI obstruction/Ileus/Impaction

What is the MOA of **saline agents?**

Mg/Phosphate ions poorly absorbed... Osmotically retain water in GI tract

What **OSMOTIC** agent is used for **severe liver disease?**

Lactulose

What is the **osmotic agent** that when given at **HIGH DOSES** is used for bowel prep prior to GI scopes?

Polyethylene glycol (PEG-3350)

What are the two drugs given for **pre-colonoscopy bowel prep?** State what type of drug and dose

**Sodium Picosulfate** (low dose, stimulant) **Polyethylene glycol** (high dose; osmotic)