Drugs for Diarrhea, Abd Pain, Constipation Flashcards
What drugs belong to the opioid receptor agonist drugs for diarrhea?
Loperamide
Diphenoxylate
Eluxadoline
If a person was trying to get that opioid buzz, what drug would not get them there?
loperamide
related but does not produce analgesic/euphoric effects
What is a toxicity issue associated with loperamide
cardiac toxicities
What is the MOA of loperamide
interferes with peristalsis by interfering with the muscles -> slow motility allows more water and electrolyte reabsorption
what are common side effects of loperamide?
anticholinergic sx
what drug has atropine added to it to discourage drug abuse?
diphenoxylate
opioid effects seen at very high doses
What side effects are associated with diphenoxylate
atropine OD and anticholinergic effects
what is the MOA of Eluxadoline?
agonist at mu and kappa opioid receptors
antagonist at delta opioid receptors
– decreased stomach, pancreas, biliary secretions
What disease process indicates the use of eluxadoline
IBS - Diarrhea subtype
What are the side effects associated with eluxadoline?
hepatic/pancreatic toxicity
– increased in those without gallbladder
CNS effects
–sedation, euphoria, impaired cognition
What are contraindications of eluxadoline?
biliary duct obstruction
alcoholism
pancreatitis history
severe hepatic impairment
STOP if sever constipation >4 days
Which drugs belong to the Serotonin Antagonist drugs
Alosetron
what is the mechanism of Alosetron
blocks 5HT3 receptors
What condition indicates the use of Alosetron
Chronic, severe IBS-D not responsive to other conventional therapies (women)
What is the black box warning associated with Alosetron
Ischemic Colitis
- -prescribing program
- -sign risk-benefit
- -no refills without follow up
What are the contraindications associated with alosetron
GI obstruction, perf, stricture, adhesions, toxic megacolon
Diverticulitis, Crohn’s disease, ulcerative colitis
hypercoagulability
Severe constipation -> DC immediately
What class of medication does crofelemer belong to?
Cl- channel inhibitors
What is the mechanism of action of crofelemer?
inhibits chloride channels CFTR and CaCC -> no fluid following ions into the lumen
What is the indication for using crofelemer
non infection diarrhea in HIV/AIDS
What are some side effects associated with crofelemer
GI-related: abdominal distention, elev AST/ALT/Bilirubin
Infections: respiratory/urinary
What class of medication is used for abdominal pain in IBS
antimuscarinics
What drugs belong to the antimuscarinic class
Hyoscyamine
Dicyclomine
what is the MOA of antimuscarinics
completely inhibit autonomic, post-ganglion cholinergic receptors
What is the indication for the use of antimuscarinics
Abdominal pain/spasms
What are side effects associated with the antimuscarinics
Classic anticholinergic sx
What Drugs belong to the peripheral opioid antagonists
Methylnaltrexone
Naloxegol
Alvimopan
Which peripheral opioid antagonist is the only one with IV route
Methylnaltrexone
all have PO
In what instances are peripheral opioid antagonists indicated?
Opioid induced constipation
In what specific situation is Alvimopan indicated
only for accelerating time to GI recovery following bowel resection (prevents post-op ileus)
What is the warning associated with Alvimopan?
risk of MI
REMS program requires use in approved institutions with max 15 doses
What is the mechanism of action of Linaclotide
guanylate cyclase-c agonist
binds on intestinal epithelium -> increases cGMP
stimulates secretion of Cl/Bicarb via CFTR
what circumstances indicate the use of linaclotide
IBS-C
Chronic idiopathic constipation
What is the MOA of lubiprostone
prostaglandin-E1 derivative
-increases fluid secretions by activating GI specific chloride channels CIC-2 in luminal cells of intestinal epithelium
What conditions indicate the use of lubiprostone
IBS-C (women)
Chronic idiopathic constipation
Opioid induced constipation
What medications belong to the bulk-forming/hydrophilic colloidal agents class
Fiber/Bran
Psyllium
Methylcellulose
Calcium Polycarbophil
How do the bulk-forming/hydrophilic agents work
increase bulk volume and water content
supports colonic bacteria
what are some of the adverse effects of the bulk forming agents
bloating/obstruction
What drugs do the bulk-forming agents interact with
LOTS of interactions
what are stool softeners also known as and give examples
Surfactant or emollient
- docusate salts
- mineral oil
How do anionic stool softeners soften and lubricate feces
increase fluid secretion
decrease fluid reabsorption
Which drugs fall under the stimulants (irritants) class of laxatives
Senna Bisacodyl Castor oil Glycerine Sodium Picosulfate
Which stimulant (irritant) is used for pre-colonoscopy bowel prep?
Sodium Picosulfate
metabolically converted to magnesium citrate.
What is the mechanism of action of the stimulant irritants
stimulate peristalsis by causing inflammation -> increase in prostaglandin
What are the adverse effects of the stimulant irritants
Abdominal cramping Urine discoloration (senna - yellow/brown red/pink)
-contraindicated in GI obstruction
What belongs in the saline agents class
magnesium salts
sodium phosphate
What is the MOA of saline agents
magnesium/phosphate ions are poorly absorbed
– hyper osmolar solutions draw water into bowel
What drugs do saline agents interact with
Diuretics
caution in renal disease and CHF
What drugs belong in the osmotic agents
Lactulose
Magnesium Citrate
Sorbitol
Polyethylene glycol
how do osmotic agents work?
draw water into the intestine
Which osmotic agent is used in sever liver disease
Lactulose (changes pH and trapps ammonia)
What are the adverse effects of osmotic agents
Electrolyte disturbances
GI
What drug is used in large amounts to prep for GI scopes and radiological procedures
polyethylene glycol
