Drugs for Diarrhea, Abdominal Pain, and Constipation Flashcards
What classes of drugs are used to treat diarrhea?
1) Prostaglandin inhibitors
2) Opioid agonists
3) Serotonin (5HT3) Antagonists
4) Chloride channel inhibitors
Bismuth which is used to treat diarrhea belongs to what class of drugs?
Prostaglandin inhibitors
Loperamide, Diphenoxylate, and Eluxadoline belong to what class of drugs?
Opioid agonists
Alosetron belongs to what class of drugs?
Serotonin (5HT3) Antagonists
Crofelemer belongs to what class of drugs?
Chloride channel inhibitors
What is the MOA of the opioid agonist loperamide?
It has direct action on what muscles of the intestinal wall that causes the above answer?
1) Interfere with peristalsis and slows motility
2) Circular and longitudinal muscles
What toxicity does loperamide cause that can lead to death?
Cardiac toxicities
Because diphenoxylate is a synthetic opiate agonist, what was added to the drug to discourage deliberate abuse?
Atropine
Diphenoxylate exerts its effect on?
This causes?
1) GI smooth muscles cells
2) Inhibits GI motility and slows excess GI propulsion
What is the classic side effect of diphenoxylate and loperamide?
Anticholinergic
Eluxadoline is an agonist at what opioid receptors in GI?
This causes what effect?
1) Mu and kappa
2) Slows peristalsis/delay digestion
Eluxadoline is an antagonist at what opioid receptor in GI?
What does it cause?
1) Delta
2) Stomach, pancreas, biliary secretions decreased
What is the specific indication for eluxadoline?
Irritable Bowel Syndrome, Diarrhea-predominant subtype (IBS-D)
When should you discontinue eluxadoline?
What side effect of eluxadoline has caused death to occur?
1) Hepatic/pancreatic enzymes dramatically increase and/or severe constipation develops and lasts 4+ days
2) Pancreatitis in patients without a gallbladder
What are some contraindications for eleuxadoline?
1) Biliary duct obstruction
2) Alcoholism
3) History of pancreatitis
4) Severe hepatic impairment
What selectively blocks GI-based 5HT3 receptors?
Alosetron
What is alosetron indicated for?
Women with chronic, severe IBS-D not responsive to other conventional therapies
What black box warning does alosetron have?
Ischemic colitis
What drug is derived from dark red sap of Croton lechleri tree?
Crofelemer
What is the MOA of crofelemer?
Inhibits chloride ion secretion by blocking cAMP stimulated CFTR and calcium activated chloride channels
What is the indication for crofelemer?
Non-infectious diarrhea in HIV/AIDS patients
What are potential side effects of crofelemer?
1) Abdominal distention
2) Elevated AST/ALT/Bilirubin
3) Respiratory/Urinary infections
What prostaglandin inhibitor is used to treat diarrhea?
Bismuth
What opioid agonists are used to treat diarrhea?
1) Loperamide
2) Diphenoxylate
3) Eluxadoline
What serotonin (5HT3) antagonist is used to treat diarrhea?
Alosetron
What Chloride channel inhibitor is used to treat diarrhea?
Crofelemer
Hyoscyamine and dicyclomine which are used for abdominal pain belong to what class of drugs?
Antimuscarinic agents
What is the MOA of the antimuscarinc agents?
Competitively-inhibits autonomic, postganglionic cholinergic receptors
What are the indications for the antimuscarinic agents?
Abdominal pain/spasms and IBS
What side effects are seen with the antimuscarinic agents?
Anticholinergic
What classes of drugs are used to treat constipation?
1) Laxative and cathartic agents
2) Peripheral opioid antagonists
3) Guanylate Cyclase-C agonists
4) Selective Chloride (C2) Channel Activators
Methylnaltrexone, Naloxegol, and Alvimopan make up what class of drugs?
Peripheral opioid antagonists
Linaclotide makes up what class of drugs?
Guanylate Cyclase-C agonists
Lubiprostone makes up what class of drugs?
Selective Chloride (C2) Channel Activators
The peripheral opioid antagonist have actions on what receptor?
Mu-opioid
Which peripheral opioid antagonist is used in the hospital only?
Alvimopan
What is the indication for peripheral opioid antagonist use?
What is the specific indication for alvimopan only?
1) Opioid-Induced Constipation (OIC)
2) Prevention of postoperative ileus after bowel resection surgery
What does alvimopan carry a risk for?
MI
What drug increases cGMP which stimulates secretion of chloride/bicarbonate into intestinal lumen via activation of CFTR ion channel?
Linaclotide
What are the indication for linaclotide?
1) IBS-Constipation (IBS-C)
2) Chronic Idiopathic Constipation (CIC)
What drug is a prostaglandin-E1 (PGE-1) derivative?
Lubiprostone
What are the indications for lubiprostone?
1) IBS-C for women
2) CIC
3) OIC
What is the MOA of lubiprostone?
Increases intestinal fluid secretion by activating GI specific chloride channels (CIC-2)
What are the peripheral Opioid Antagonists used to treat constipation?
1) Methylnaltrexone
2) Naloxegol
3) Alvimopan
What is the guanylate cyclase-C agonists used to treat constipation?
Linaclotide
What is the selective chloride (C2) channel activator used to treat constipation?
Lubiprostone
Bisacodyl, Castor Oil, Glycerin, Senna, and sodium picosulfate make up what category of laxative and cathartic agents?
Stimulants
Lactulose, Magnesium citrate, polyethylene glycol (PEG), and Sorbitol make up what category of laxative and cathartic agents?
Osmotics
Magnesium hydroxide and sodium phosphate make up what category of laxative and cathartic agents?
Salines
Dietary (Fiber/Bran/Fruits), Psyllium, Methylcellulose, and Calcium polycarbophil make up what category of laxative and cathartic agents?
Bulk forming
Docusate and Mineral oil make up what category of laxative and cathartic agents?
Stool softeners
What is the MOA of the bulk-forming/Hydrophilic colloidal agents?
What can fiber also provide support for?
How long does it usually take to take effect?
1) Increase bulk-volume and water content, thereby increasing GI motility
2) Supports colonic bacteria, fermentation, and digestion
3) Fast, 2-4 days
What adverse effects are seen with Bulk-forming agents?
What is the recommendation for this?
1) Bloating/Obstruction
2) Drink fluids
What are stool softeners also known as?
When is efficacy seen?
1) Surfactant or Emollient laxatives
2) 1-3 days
What is the MOA of anionic surfactants?
Soften/lubricate feces by increasing fluid secretion into GI tract and decreasing fluid reabsorption from GI tract
What stimulant is used for pre-colonoscopy bowel prep?
What is it metabolically converted to?
1) Sodium picosulfate
2) magnesium citrate
The stimulants are irritants to enterocytes, GI smooth muscle leading to
inflammation by?
Na+/K+-ATPase inhibition and/or increase in prostaglandin synthesis/secretion (via cAMP/GMP)
What do the stimulates promote?
Water/electrolyte accumulation in GI
What stimulant is hydrolyzed to ricinoleic acid?
Which is a tri-hydroxyl alcohol and functions as an irritant and an osmotic lubricant agent?
1) Castor oil
2) Glycerin
What is the efficacy of stimulants?
What are the contraindications?
1) 12-36 hours
2) GI obstruction/Ileus
What adverse effect can stimulants cause?
Which stimulant causes urine discoloration (yellow-brown/red-pink)?
1) Abdominal cramping
2) Senna
What is the MOA of the saline agents magnesium hydroxide and sodium phosphate?
They are hyperosmolar solutions that retain water in GI tract
What drug interactions do saline agents have?
What should be watched carefully with these interactions?
1) Diuretics
2) Electrolyte balance
When conditions should bring caution when giving saline agents?
1) Renal disease
2) CHF/HTN
What osmotic agent in large doses can be used for pre-colonoscopy bowel prep?
Polyethylene glycol
In general, osmotic agents provide effects in how many days with laxative doses?
What effect do larger doses have on catharsis?
1) 1-2 days
2) Effect occurs in hours
Which osmotic agent can also be used for severe liver disease patients such as hyperammonemia?
Lactulose
