Drugs for abdominal pain, diarrhea, and constipation Flashcards
(39 cards)
what are the Prostaglandin inhibitors? and use?
Bismuth and used for diarrhea
What are the opioid agonists and their general use
Loperamide
Diphenoxylate
Eluxadoline
diarrhea
what are the Serotonin 5Ht-3 antagonists and their general use
Alosetron
diarrhea
what are the Chloride Channel Inhibitors and their general use?
Crofelemer
diarrhea
Mechanism of Action and side effects of Loperamide?
Interferes with peristalsis (slows transit time)
Direct action on circular and longitudinal muscles of intestinal wall, slowing motility
–Slowed motility allows for fluid/electrolyte reabsorption and increasing bulk/density of feces
Side effect:
classic anticholinergic
does not exhibit opiate like effects or addiction but can cause Cardiac toxicities
Mechanism of action and side effects of Diphenoxylate
Mechanism of Action:
Believed to exert effect locally & centrally on GI smooth muscle cells; inhibits GI motility and slows excess GI propulsion
•Side effects:
Classic anticholinergic; atropine
is a synthetic opiate agonist and can cause opioid effects at high dosages so atropine is added to discourage over dosage
Indication and mechanism of action of Eluxadoline
•Mechanism of Action:
Agonist at opioid mu& kappa receptors in GI (slows peristalsis/delays digestion)
Antagonist at delta opioid receptors in GI
stomach, pancreas, biliary secretions decreased
•Indication:
Irritable Bowel Syndrome, Diarrhea-predominant subtype (IBS-D)
what are major side effects of Eluxadione and its contraindictions
Side effects:
Hepatic/Pancreatic toxicity (increased enzymes)
Pancreatitis high-risk in pts. w/o a gallbladder
–Deaths have occurred (FDA warning)
CNS-related:
sedation/euphoria/impaired cognition
Contraindications: biliary duct obstruction alcoholism history of pancreatitis severe hepatic impairment •Stop therapy if severe constipation develops and lasts 4+ days
Mechanism of action and indication for Alosetron
Selectively blocks GI-based 5HT3 receptors
Antagonism (receptor blocking) modulates regulation of visceral pain, colonic transit & GI secretions
Indications: Chronic, severe IBS-D not responsive to other conventional therapies (women)
what are the side effects and contraindications of Alosetron
Ischemic Colitis (Black Box Warning)
Physicians must enroll in prescribing program
Patients and physicians must sign a risk-benefit statement and agree to adhere to therapy plans
Additional self-training and testing by physicians to learn to appropriately diagnose IBS required
No refills without a follow-up exam by the prescriber
Contraindications:
History or Current:
GI obstruction, perforation, stricture/adhesions, toxic megacolon
Diverticulitis, Crohn’s disease, or Ulcerative colitis
Impaired intestinal circulation, thrombophlebitis or a hypercoagulable state
Severe constipation
Description and Mechanism of action of Cl- Channel Inhibitor
Description:
derived from dark red sap of Croton lechleri tree (botanical pharmaceutical)
•Mechanism of Action:
Inhibits chloride ion secretion by blocking cAMP-stimulated CFTR (cystic fibrosis transmembrane regulator) & calcium-activated (CaCC) chloride channels
channels regulate fluid secretion by intestinal epithelial cells
Indication and side effects of Crofelemer
Indication:
Non-infectious diarrhea in HIV/AIDS (for pts. on anti-retroviral therapy)
•Side Effects: GI-related Abdominal distention, elevated AST/ALT/Bilirubin Infections Respiratory/Urinary
what are the type and drug names used for abdominal pain
Antimuscarinic Agents
Hyoscyamine
Dicyclomine
what are Antimuscarinics MOA, Indication and side effects
Mechanisms of Action:
Competitively-inhibit autonomic, post-ganglionic cholinergic receptors (multiple sites)
•Indication:
Abdominal pain/spasms
•Side Effects:
Classic Anticholinergic-based
What are the Peripheral Opioid antagonists and what are their general function?
Methylnaltrexone
Naloxegol
Alvimopan
Constipation
What are the Guanylate Cyclase-C agonists and what are their general function?
Linaclotide
COnstipation
what are the Selective Chloride C2 channel activators and what are their general function
Lubiprostone
Constipation
Mechanism of action for Peripheral Opioid antagonists and which one is only used in the hospital
peripheral mu-opioid receptor antagonists
No common, significant CNS actions nor induction of withdrawal/pain symptoms
Alvimopan
What are the Indications and side effects of Peripheral Opioid antagonists
Opioid-Induced Constipation (OIC)
Alvimopan–only for accelerating time to GI recovery following bowel resection surgery with primary anastomosis (prevention of postoperative ileus)
Side effects: GI related
Alvimopan carries a risk of MI with use;
REMS program requires use only in approved institutions for max. of 15 doses
Linaclotide mechanism of action, indications and side effects
Selective guanylate cyclase-C (GC-C) Agonist
Binds to GC-C on luminal surface of intestinal epithelium & increases intracellular/extracellular concentrations of cGMP
Stimulates secretion of chloride/bicarbonate into intestinal lumenvia activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channel
•Indications:
- Irritable Bowel Syndrome-Constipation predominant subtype (IBS-C)
- Chronic Idiopathic Constipation (CIC)
•Side Effects:
GI-Related
Mechanism of action for Lubiprostone
a prostaglandin-E1(PGE-1) derivative
increases intestinal fluid secretion by activatingGI-specific chloride channels (ClC-2) in luminal cells of intestinal epithelium
Indications and side effects of Lubiprostone
Indications:
- Irritable Bowel Syndrome-Constipation predominant subtype (IBS-C) (women)
- Chronic Idiopathic Constipation (CIC)
- Opioid-Induced Constipation (OIC)
•Side Effects:
GI-related
CNS-related
What are stimulant Laxative and Cathartic agents?
Bisacodyl Castor Oil Glycerin Senna Na+Picosulfate
what are osmotic Laxatives and Cathartic agents
Lactulose Mag. citrate Polyethyleneglycol (PEG) Sorbitol (Glycerin)
