4.01 GI Pharm: IBD, IBS, Antiemetics, Etc. Flashcards
Anionic surfactant that may block water reabsorption
Docusate MOA
Docusate ADSE?
Diarrhea, stomach pain, cramping
How long does it take for Docusate to kick in? ADME considerations?
24-72 hours Oral
10-20 min Suppository
Generally mild way to treat patients for constipation? Not strong enough for patients on opioids
Docusate
Stimulates the peristalsis by directly irritating the smooth muscle of intestine (intramural plexus) alters water and electrolyte secretion producing net intestinal fluid accumulation and laxation?
Bisacodyl
Stimulates the peristalsis by directly irritating the smooth muscle of intestine (intramural plexus) alters water and electrolyte secretion producing net intestinal fluid accumulation and laxation?
Bisacodyl
Abdominal cramps, long term use = electrolyte disturbances, rectal irritation?
Bisacodyl
Used for acute constipation, bowel prep for procedures, opioid induced constipation?
Bisacodyl
What are the Bisacodyl contraindications?
Bowel obstruction, severe dehydration, acute surgical abdomen, rectal bleeding
Long term use could lead to lazy bowel syndrome, dependence, and electrolyte imbalances?
Bisacodyl
Bicycling fatty acid that acts locally on apical luminal portion of intestine as a chloride channel activated on CIC-2 increasing intestinal fluid secretion and intestinal motility
Lubiprostone
Laxative that is poorly absorbed and could have ADSE including diarrhea and comes CNS (Headache)?
Lubiprostone
What is used to treat chronic idiopathic constipation, opioid induced constipation, and IBS with constipation (women)?
Lubiprostone (W) and Linaclotide
Bind and agonize guanylate cyclase-c on luminal surface of intestinal epithelium resulting in chloride and bicarb secretion into intestinal lumen?
Linaclotide
What is the Linaclotide BBW?
Children under 2 years old due to dehydration concerns
Catalyzes hydrolysis of Gb-3 and other glycosphingolipids
A-galactosidase
Used to treat the X-linked lysosomal storage disorder Fabry Disease?
A - galactosidase
Numerous ADSE including peripheral edema, inclusion reactions, seroconversion, hypersensitivity reactions**
A galactosidase
A galactosidase ADME?
IV (parenteral)
Enzyme to break down lactose and taken orally with milk products?
Lactase
Isolated from porcine pancreatic glands, contains lipase, amylase and proteases?
Pancrelipase
Used to treat pancreatic insufficiencies?
Pancrelipase
How do you take Pancrelipase?
With food to aid digestion since coated in enteric capsule
What are some anti diarrheal options?
Loperamide or Diphenoxylate
Opioid agonist that minimally crosses BBB OTC?
Loperamide
Opioid agonist that will cross in higher doses and mixed with atropine?
Diphenoxylate
When shouldn’t you use opioids as anti diarrheal?
High fever, bloody diarrhea, septicemia
Most common treatment for gallstones?
Laparoscopic cholecystectomy
What should you be thinking as treatment for recurrent gallstones for patients?
Statins and ezetimibe
What is an nonsurgical option to treat very Iill patients with gallstones or to prevent the formation in overweight people losing weight very quickly?
Ursodiol
Decreases cholesterol content of bile by reducing the secretin of cholesterol from the liver?
Ursodiol
Ursodiol is used for gallstones of what size?
< 20mm
Ursodiol ADSE?
Headache, dizziness, diarrhea, constipation, nausea, back pain, upper respiratory tract infections
When will gallstones be unresponsive to Ursodiol?
When they are calcified
What is the Ursodiol effectiveness ?
50% when 10mg/kg/day for 12-24 months
What are drugs that you can use to reduce portal pressure and treat variceal hemorrhages?
Octreotide or terlipressin
Somatostatin agonist that inhibits secretion of CCK, gastrin, GH, insulin, VIP, 5-HT to reduce portal and splanchnic blood flow?
Octreotide
Due to the impaired pancreatic secretions it may cause steatorrhea and fat soluble vitamin deficiencies alongside nausea, abdominal pain, flatulence, and gall stones?
octreotide
How long would you use octreotide?
7 days or less, not long term
What can you use to treat IBS?
Dietary Alterations*, then treat symptoms like diarrhea/constipation with normal drugs, can do low dose Anticholinergics or Alosetron (Severe diarrhea)
selective 5-HT3 antagonist (direct channel)
Alosetron
Approved for treatment for women with severe diarrhea predominant IBS who failed to conventional treatment?
Alosetron
BBW for Alosetron?
Ischemic colitis and serious constipation complications
Alosetron ADME?
Oral, extensive metabolism, urinary excretion
Drugs to treat IBD generally?
Anti inflammatories
Used to treat mild IBD?
5-ASA
Used to treat severe IBD?
Natalizumab
MOA uncertain with some COX inhibition, some NF-kB inhibition, mainly topical*
5-ASA (aminosalicylates)
Anti-integrity therapy that blocks a4 integrity subunit on circulating inflammatory cells blocking ability for T cells to migrate/adhere in the gut area?
Natalizumab
Used especially to treat Crohn’s disease?
Natalizumab
Natalizumab ADSE?
Multifocal leukoencephalopathy (JC virus), Infusion reactions, opportunistic infections
Why are 5-HT3 antagonists useful as antiemetic?
Blacks afferent vagal stimulation/signaling
Why are benzos effective as an antiemetic?
It helps anticipatory vomiting from emesis responses to needles, IV bags, etc.
Used to treat motion sickness like on a boat?
Scopolamine
5-Ht3 Antagonist?
Ondansetron
What is used for chemo/radiation or postoperative nausea/vomiting and much be continuously delivered as it has a short half like (3-4hrs)?
Ondansetron
Ondansetron ADSE?
Headache, dizziness, constipation, small QT interval increase
Neurokinin receptor antagonist, blockade of the NK1 receptor in postrema area
Aprepitant
Neurokinin receptor antagonist
Aprepitant
What is used in combination with 5-HT3 antagonists for acute and delayed nausea/vomiting from highly emetogenic chemo regimens?
Aprepitant
Neurokinin receptor antagonist Aprepitant ADSE?
Drug-drug interactions (CYP3A4), fatigue, dizziness, diarrhea
Used for highly emetogenic chemo regiments especially for DELAYED nausea and vomiting
Aprepitant
Likely activation of CB1 resulting in increased appetite and antiemetic effects?
Cannabinoids = dronabinol (THC)
When is dronabinol (THC) administered?
Prior to chemo and 2-4 hours after waters
Euphoria, dysphoria, sedation, hallucinations, dry mouth, increased appetite?
Dronabinol (THC)