E2: GI Drugz Flashcards
MOA for antacids
Inorganic bases that neutralize HCl to form salt and H2O
List the 2 drugs in the Antacids class
Magnesium Hydroxide
Aluminum Hydroxide
What is the primary adverse effect of Magnesium Hydroxide? Aluminum Hydroxide? How can this be improved?
Mg = diarrhea Al = constipation
Combine together to cancel out these effects
What are the uses of Antacids?
Symptomatic short term relief of heartburn and GERD (or used as adjunct therapy)
Antacids are contraindicated in what pt population?
Patients w/ kidney dysfunction (can cause accumulation of toxins)
Antacids have a high potential for _____.
Drug interactions
Name the 2 drugs in the H2 blockers class.
Cimetidine
Ranitidine (Zantac)
MOA for H2 blockers
COMPETITIVE antagonists of H2
When are H2 blockers most effective? When should you educate your patients to take them?
Most effective at decreasing nocturnal acid formation
Pts should take at bedtime!
What are 4 uses of H2 blockers?
- Duodenal and gastric ulcers*
- Given w/ H1 antagonists for severe allergic rxn (decrease vasodilation)*
- Adjuncts for GERD and ZES
- Given pre-operatively in case of aspiration
*Most important
H2 blockers are metabolized by the _____ and excreted by the _____.
Metabolized by liver
Excreted by kidney
What are 3 general adverse effects of H2 blockers? What is a specific adverse effect for Cimetidine and in what how can this be used therapeutically?
- HA
- Nausea
- Confusion (elderly)
Chronic cemetidine: Anti-androgenic effects (ex: gynecomastia) - used to tx HIRSUITISM in females
Which H2 blocker can cause drug interactions? What liver enzyme does this drug inhibit?
Cimetidine inhibits CYP3A4
*Drug interactions with phenytoin, warfarin, theophylline, benzos, TCAs, etc.
Name the 2 PPIs
Omeprazole
Esomeprazole
MOA for PPIs
IRREVERSIBLY inhibit the proton pump in the final stage of gastric acid production (binds to H/K pump)
What is the DOC for GERD w/ esophagitis?
PPIs - extremely effective!
In what form are PPIs ingested into the body?
Ingested as prodrugs –> must be converted to active sulfenamide
How long does it take for the PPIs (Omeprazole, Esomeprazole) to start working? How long do their effects last once discontinued?
2-5 days to start working
Effects last 24-48 hrs upon discontinuation
Though usually minimal, what are the adverse effects of PPIs? (6)
- Nausea/Diarrhea/Abd. colic
- Increased URIs (specifically pneumonia)
Chronic use:
- Decreased Ca absorption (risk for osteoporosis)
- Hypomagnesia
- Vit B12 deficiency
- Increased risk of CKD
What liver enzyme does Omeprazole inhibit? This effects the metabolism of what 3 other drugs?
Inhibits CYP249
Decreased metabolism of phenytoin, diazepam, and warfarin
What drug is a Cytoprotective Agent? What is the MOA?
Misoprostol
MOA: Prostaglandin E1 analogue (increased secretion of mucous, decreased acid secretion)
What is the primary use of Misoprostol (cytoprotective agent)?
Prevention of NSAID-induced uclers
What drug can be used for prevention of NSAID-induced ulcers?
Misoprostol
What is the primary effect of the prokinetic agents? What 3 drugs fall under this class?
Increase GI activity
- Metoclopramide
- Bethanechol
- Erythromycin
What 2 drugs are used to tx post-surgical gastric hypomotility? Which drug is also an antiemetic?
Metoclopramide (hypomotility + antiemetic)
Bethanechol (hypomotility)
MOA for Metoclopramide (2)
D2 antagonist
Increases Ach release
(this enhances motility and tone of smooth muscle)
What are 2 adverse effects of Metoclopramide? In what population is this prokinetic agent C/I?
Extrapyramidal sxs (Parkinson's like) GI cramping + diarrhea
C/I in pregnancy (risk of methemoglobinemia)
MOA for Bethanechol
Muscarinic agonist
What drug is used to tx diabetic gastroparesis? What is the MOA of this drug?
Erythromycin (prokinetic agent)
MOA: Macrolide abx, stimulates motilin receptors
What 2 drugs are used as antismasotics/tx of IBS?
Dicyclomine
Amitriptyline
MOA for Dicyclomine. What are the adverse effects?
MOA: Blocks muscarinic receptors
SE: sedation, dry mouth, constipation, etc (basically SNS effects)
MOA for Amitriptylline in the tx of IBS? (2)
Blocks muscarinic receptors
Increased NE release stimulates alpha-2 receptors in spinal cord to DECREASE PAIN
The chemoreceptor trigger zone (vomiting center of the brain) is rich in what 4 receptor types?
5HT-3
DA
NK-1
Opioid
What are the 5 anti-nausea/anti-emetic drugs?
Ondansetron (Zofran)
Promethazine (Phenergan)/Prochlorperazine
Dronabinol (THC)
Aprepitant
MOA for Ondansetron (Zofran)
5HT-3 antagonist
MOA for Promethazine (Phenergan) and Prochlorperazine
Block D2, muscarinic, and histamine receptors
What 3 drugs can be used for chemotherapy induced N/V?
Ondansetron (Zofran) (NOT effective for motion sickness)
Dronabinol (THC) (also increases appetite!)
Aprepitant
MOA for Aprepitant. What 2 drugs is it typically combined with?
NK1 antagonist
usually combined with 5HT-3 antagonist and steroid
What are 3 adverse effects of chronic laxative use?
Electrolyte imbalances
Dependence
Alterations in bowel function
Name the bulk forming laxative. What is its MOA?
Psyllium (Metamucil)
Attracts H20, forms soft mass
What are 2 adverse effects of Psyllium? What should be included in pt education?
AE: Bloating, flatulence
Tell patient to drink plenty of water as Psyllium is high in fiber!
How do osmotic laxatives work? Name the 3 drugs included in this class.
Magnesium Hydroxide
Lactulose
Polyethylene glycol
Drugs are poorly absorbed salts and sugars in GI tract that hold onto H20 inside the intestine
What drug is used to decrease ammonia build up in pts with cirrhosis? Is this used acutely or long-term?
Lactulose
*ONLY laxative that should be used long-term!
What drug is used for colonoscopy prep? How can this be adjusted to tx constipation?
Polyethylene glycol used in LARGE amounts for colonoscopy prep
-Significantly reduced dose used for tx of constipation for up to 7 days
What drug is used as a Mucosal Agent? How does it work?
Senna
Stimulates peristalsis, enhances secretion, and inhibits water absorption
What are 5 general C/I for use of laxatives?
N/V Abd. cramps Undiagnosed abd. pain Appendicitis Intestinal obstruction
MOA for Lubiprostone (2). What is used to tx?
MOA: Prostaglandin E1 analogue; Increases intestinal fluid secretion by activating ClC-2 chloride channels
Used to soften stool and reduce sxs in WOMEN with IBS-C
MOA for Linclotide (2). What is it used to tx?
MOA: Activates guanylate cyclase C ( resulting in increased Cl secretion in intestines); Activates CFTR
Used to tx IBS-C or chronic constipation
MOA for Loperamide (imodium). What is it used to tx?
MOA: Opioid analogue, decreases peristalsis by inhibiting activity of GI tract
Anti-diarrheal med (can be given OTC due to no CNS effects)
What are 4 adverse effects of Loperamide (Imodium)?
Abd pain
Distention
Constipation
Dry mouth
In what 3 situations is the use of Imodium C/I?
Diarrhea caused by organisms that penetrate mucosa
Pts w/ ulcerative colitis
Pts w/ hx of drug abuse (opioid)
Which anti-inflammatory drug is used for tx of IBS? What is the MOA?
Sulfasalazine
MOA: Aminosalicylate; decreases inflammation, bacteria try to active it
What is the primary adverse effect of sulfasalazine? In what population is this anti-inflammatory drug C/I?
Hypersensitivity
C/I in children (potential for Reyes Syndrome)
What drug is used to tx flatulence? How does it work?
Simethicone (Gas-X)
Coats and dissipates gas to allow it to pass less noticeably