GI Drugs Flashcards
Antacid examples
Calcium carbonate (TUMS)
Aluminum hydroxide
Magnesium hydroxide (MoM)
Maalox contains aluminum and magnesium
Antacids MOA
React locally in stomach with H+ to increase pH
Route of administration of antacids
Suspension more effective than tablets and powders
Antacids indications
Hyperacidity
reflux
Indigestion
Antacids CIs
Poor renal function
Antacids S/E
Magnesium —> diarrhea
Calcium —> Hypercalcemia, renal calculi, bloating, flatulence, belching, nausea, constipation
Aluminum —> hypophosphatemia, constipation
Antacids drug interactions
Bind to tetracycline resulting in decreased bioavailability
Which antacids are often combined
Aluminum and magnesium
Mg is rapid onset/Al is slower onset
Mg causes diarrhea/aluminum causes constipation
What is added to antacids to reduce bloating
Simethicone
H2 antagonist examples
Ranitidine / Zantac
Famotidine / Pepcid
H2 antagonist MOA
Inhibit histamine at H2 receptors of the gastric parietal cells, which reduces gastric acid secretion
H2 antagonist indications
GERD
PUD
Dyspepsia
Gastritis
H2 antagonist CIs
Caution in patients with renal impairment
Liver failure or liver disease
H2 antagonist S/E
Generally well tolerated
Common - diarrhea, headache, drowsiness, fatigue, muscle pain, constipation
Rare - CNS side effects (confusion, delirium, hallucinations, slurred speech), thrombocytopenia
disadvantages of H2 antagonists
less effective than PPIs
tolerance can develop
lots of drug interactions with Cimetidine
PPI Examples
- omeprazole / prilosec
- pantoprazole / protonix
- esomeprazole / nexium
PPI MOA
act within gastric parietal cell, inactivate the acid pump and inhibit secretion of hydrochloric acid into stomach
PPI Indications
- gastric and duodenal ulcers
- GERD
- Upper GI bleeding (Mallory Weiss)
- Zollinger-Ellison Syndrome
- H. pylori infection
PPI CIs
co-administration of other drugs
all interfere with absorption of drugs given orally that depend on gastric acid pH to be effective - vit B12, ampicillin, ketoconazole
formulation of PPIs
all have enteric coating to protect them from acidic environment until they reach small intestine for absorption - don’t break up the tablets
when to take PPIs
take 30-60 min prior to meals
PPI metabolism
liver
PPI S/E
generally well tolerated
Common: nausea, abdominal pain, constipation, diarrhea, flatulence
Less Common: hypergastrinemia –> rebound hypersecretion of gastrin if PPI stopped
Long term use: increased risk of fractures of the wrist, hip, spine (over 1 year of daily use)
benefits of PPIs
most effective for GERD - reduce acid by 85-90%
GI cytoprotectant examples
Misoprostol / Cytotec (prostaglandin analog)
Sucralfate / carafate (coating agent)
bismuch / pepto bismol (coating agent)
GI cytoprotectant MOA
protect cells in lining of stomach - either increase gastric pH or enhance mucosal barrier
sulcralfate selectively binds to necrotic tissue, covers ulcer site, acts as barrier to acid, pepsin, bile salts
Indication for misoprostol
prevention of NSAID induced ulcers
indication for sucralfate
treatment of duodenal and gastric ulcers
prevention of ulcer recrrence
indication for bismuth
adjunctive therapy in H. pylori eradication
acute diarrhea
heartburn
misoprostol CIs
- pregnancy (category X)
2. caution in patients with renal impairment
bismuth CIs
- children or teenagers with viral infections
2. may be trigger for Reye’s Syndrome - has salicylate
Misoprostol S/E
- diarrhea
- abdominal cramping
- uterine contraction (pregnancy)
sucralfate S/E
minimal systemic side effects
rarely constipation
bismuth S/E
- black, tarry stools
- discoloration of the tongue - black tongue
- constipation
- tinnitus at high doses
GI cytoprotectant drug of choice in women of child bearing age for treatment of active duodenal ulcers not caused by NSAIDs
sucralfate
patient ed on taking sucralfate
requires acidic environment to be active
don’t take antacids within 30 min of sucralfate
Dopamine antagonist examples
- metoclopramide / Regland
Dopamine antagonist MOA
increase lower esophageal sphincter tone and stimulate contractions of the stomach and small intestine
also inhibit vomiting center
Dopamine antagonist indications
- gastroparesis
- nausea/vomiting (last line in pregnant women)
- GERD that fails to respond to H2 antagonists or PPIs (3rd line)
Dopamine antagonist CIs
- patients with obstruction, perforation, or hemorrhage
- Parkinson’s Disease
- caution in patients with renal impairment
Dopamine antagonist S/E
- hyperprolactinemia - galactorrhea, gynecomastia, dysmenorrhea
- CNS effects - drowsiness, restlessness, insomnia, anxiety, agitation, depression
- extrapyramidal effects - abnormal muscle tone, parkinson-like symptoms
- tardive dyskinesia
disadvantage of metoclopramide
may decrease absorption of drugs from stomach while accelerating absorption from small intestine
serotonin antagonist examples
ondansetron / zofran
serotonin antagonist MOA
blocks serotonin 3 receptors located in vagal nerve terminals and central nervous system chemoreceptors trigger zones
serotonin antagonist indications
nausea
vomiting
IBS
serotonin antagonist S/E
generally well tolerated 1. constipation or diarrhea 2. headache 3. light-headedness Serious side effects 1. ischemic colitis 2. QT prolongation
what are serotonin antagonist good/bad for?
good - chemo induced N/V
bad - motion sickness
Antidiarrheals Examples
loperamide / imodium
loperamide MOA
inhibits peristalsis by direct effect on circular and longitudinal muscles of intestinal wall
Antidiarrheals indications
- diarrhea
- traveler’s diarrhea (due to bacteria in contaminated food/water)
- chronic diarrhea associated with IBD (w/ caution)
Antidiarrheal CIs
- acute dysentery (any blood diarrhea)
- bacterial enterocolitis (salmonella, shigella, campylobacter)
- pseudomembranous colitis
- severe IBD in which a reduction in GI motility could lead to serious sequelae such as ileus, megacolon, toxic megacolon (more likely in UC than Crohn’s)
Antidiarrheal S/E
all: constipation
opiates: CNS effects, low abuse potential
Laxative examples
- stimulants
- sennosides /senokot
- bisacodyl / dulcolax - osmotics: polypethylene glycol / Miralax
- saline: magnesium
- softeners: docusate / colace
Laxative indications
- constipation
2. as cathartics in prep for radiologic or surgical procedures
Laxative CIs
- fiber in patient with obstructive symptoms or megacolon
2. undiagnosed abdominal pain
Laxative S/E
generally well tolerated
- diarrhea (osmotic and stimulant agents)
- abdominal distention (bulk agents)
- abdominal distention, flatulence (osmotic sugars)
- electrolyte abnormalities (osmotic salts)
- mineral oil can interfere with fat soluble vitamins, elicit foreign body reaction in gut and cause lipid pneumonitis
what are osmotic sugar laxatives (ie. Miralax) useful for
treatment of constipation caused by opiates and constipation in the elderly
what else is lactulose used for
treatment of hepatic encephalopathy - decreases intestinal pH which traps ammonia w/in lumen of gut, facilitating its exit from body
Amitiza indication
- idiopathic constipation
2. IBD-C
Amitiza CIs
- severe diarrhea
2. bowel obstruction
Amitiza MOA
increases intestinal fluid secretion, causes softening of stool and increase in GI motility
Amitiza S/E
well tolerated
nausea - eat prior to taking to lessen this s/e
Methylnaltrexone / Relistor Indication
opioid induced constipation caused by long term use in chronically ill patients
Methylnaltrexone / Relistor CIs
- known or suspected GI obstruction
2. caution in nursing mothers
Methylnaltrexone / Relistor MOA
peripheral mu-opioid receptor antagonist - counteracts opioid effects like itching and constipation
*does not cross blood-brain barrier
Methylnaltrexone / Relistor S/E
- abdominal pain
- flatulence
- nausea
- diarrhea
- dizziness
what cytoprotectant do you give in hospital if pt has an ulcer
sucralfate