GI Pharm Flashcards
H2 Receptor Antagonists (4)
1) Cimetidine
2) Ranitidine
3) Famotidine
4) Nizatidine
When are H2 receptor antagonist effects most pronounced?
At night due to nocturnal acid secretion (which depends largely on histamine)
Nizatidine: Class? Pharmacokinetics?
1) H2 receptor Antagonist
2) Great bioavailbility dt reduced first pass hepatic metabolism
Serum half life is 1-4 hours
H+K+ ATPase
Proton pump
How often should H2 receptor antagonist be used for GERD?
<3x per week
If doctor decides to use H2 receptor antagonist for peptic ulcer, when should they be given?
At night
H2 receptor antagonist contraindicated?
Preganant women; crosses the placenta and gets into breast milk
Two H2 receptor antagonists that effect hepatic metabolism of many drugs?
Cimetidine and Ranitidine
Proton Pump Inhibitors (6)
1) Omeprazole
2) Esomprazole
3) Lansoprazole
4) dexlansoprazole
5) Pantoprazole
6) Rabeprazole
PPIs: how do they work?
1) Prodrugs!– require acid environment; activated drug binds with H, K atapase and irreversibly inactivates the enzyme
Most potent H2 receptor antagonist?
Famotidine
How should PPI be used?
On empty stomach before meals
Triple therapy of Hpylori associated ulcers?
1) PPI
2) Amoxicillin
3) Clarithromycin or metronidazole bid
PPI adverse reactions in hospitalized patients?
C. difficile
Sucralfate: Use? MOA? Drug drug interactions?
1) Ulcers
2) **Promotes mucosal defense; **Requires acidic activation
3) so do not give with PPI or H2);
Thought to selectively bind necrotic ulcer tissue and acts as barrier to acid, pepsin and bile
Drug that promotes mucosal defense? Which drugs should it not be given with?
1) Sucralfate
2) PPI or H2 antagonist
Colloidal Bismuth Compounds: MOA? Use?
1) Bind to ulcer, coat it and protect it
2) Ulcers (direct antimicrobial activity against H pylori)
(High rates of ulcer healing when combined with tetracyclines and metronidazole)
Misoprostol: MOA? Use? Contraindication?
1) Prostoglandin analog; both mucosal and acid inhibitory properties; reduces histamine stimulated cAMP production
2) NSAID induced ulcers
3) will ABORT in pregnant woman
3 functions of metoclopramide? Use? MOA? Side effects?
1a) Inc. esophageal clearance
b) Raises LES pressure
c) Inc. gastric emptying
2) used for gastric motor problems
3) DA receptor antagonist
4) Extrapyramidal
DM II patient on medication for “gastric motility” develops a tremor– drug? MOA?
Metoclopramide
Dopamine antagonist
Lubiprostone: use? MOA? side effects?
1) Inc. motility; soften stools (constipation)
2) FA derivative from prostoglandin– producing chloride rich secretions
3) Can’t use in children
Prostoglandin derivative that cannot be used in children?
Lubiprostone
Laxative used before colonoscopy
Polyethylene Glycol
Diphenoxylate and loperamide: MOA?
Inhibits ACh release
Two drugs that inhibit ACh release
Diphenoxylate and Loperamide
ACh inhibitor that has potential for addiction?
Diphenoxylate
Pain associated with IBS: drug class? Two drugs?
1) Tricyclic antidepressants
2) Amitriptyline and desipramine
Amitriptyline: Use? What is it?
1) IBS
2) Tricyclic antidepressant
Desipramine: Use? What is it?
1) IBS
2) Tricyclic antidepressant
Alosetron: Use? MOA?
1) Severe IBS with diarrhea
2) Seretonin antagonist
5-HT3 antagonist in GI tract
Alosetron
Mesalamine (5-ASA): use? MOA?
1) UC
2) Bowel specific aminosalicylate
First line treatment of mild to moderate UC?
Mesalamine (5-ASA)
Steroid that is released in distal ileum and colon?
Budesonide
Steroid with high first pass metabolism?
Budesonide
Antimetabolite used primarly for Crohn’s?
Methotrexate
Natalizumab: MOA? Side effect? use?
1) Anti integrin antibody
2) Progressive multifocal leukoencephalopathy (caused by JC virus)
3) Moderate to severe Crohn’s in patients who have failed other treatments
Anti seretonin drugs suffix?
“setron”