Pharmacology Flashcards
List the Histamine 2 Blockers
1) Cimetidine
2) Ranitidine
3) Famotidine
4) Nizatidine
Mechanism of H2 Blockers
Reversible block of histamine H2-reeptors –> Decreased H+ secretion via parietal cells
Indications of H2 Blockers
1) Peptic Ulcer
2) Gastritis
3) Mild Esophageal Reflex
H2 Blocker Relative Contraindication
Pregnancy
Cimetidine is a ___ inhibitor and has ___ effects
P-450
Antiandrogenic Effects
List the Antiandrogenic Effects of Cimetidine
1) Gynecomastia in Men
2) Galactorrhea in Women
Ranitidine and Cimetidine have effects on kidneys by decreasing the secretion of _____,
Creatinine
List the PPIs
Lansoprazole Dexlansoprazole Omeprazole Esomeprazole Pantoprazole Rabeprazole
Mechanism of PPIs
Covalently binds sulfhydryl groups of H+/K+ ATPase of parietal cells
Indications of PPIs
1) Peptic Ulcer
2) Gastritis
3) Zollinger-Ellison Syndrome
4) Component of H. Pylori Therapy
5) Stress Ulcer Prophylaxis
Relative contraindication of PPI
Pregnancy
Adverse Effects of PPI’s
1) Increased C. Difficle infection risk
2) Pneumonia
3) AKI
4) Vitamin B12 Malabsorption
5) Decreased Ca2+ and Mg2+ Absorption (Osteoporosis)
Omeprazole is a ____ inhibitor and has many drug interactions
CYP450
Sucralfate Indications
1) Increase Ulcer Healing
2) Duodenal Ulcer
Contraindications of Sucralfate
1) Severe Renal Failure (due to aluminum) - pts should also avoid antacids
Mechanism of Sucralfate
1) Provides physical protection
2) Allows HCO3- secretion to reestablish pH gradient in mucous layer
Sucralfate should not be given with ___ and ___ because it requires an acidic enviroment.
1) PPI
2) H2 Blockers
Adverse Effects of Sucralfate
1) Constipation (Aluminum Hydroxide)
Since sucralfate has many drug interactions you’ll want to take this medication as well as Bismuth ___ after other medication.
2 hours
Bismuth (Subsalicylate) Indications
1) Travelers Diarrhea
2) Combination Therapy for H. Pylori Gastritis
Relative Contraindications of Bismuth
1) Antiplatelet and Anticoagulants
2) Severe Renal Failure
Absolute Contraindications of Bismuth
1) GI bleeding
2) Salicylate Hypersensitivity
Bismuth Mechanism
1) Prevent Microbial attachment to mucosa
2) Inactivation of Enterotoxins
3) Disruption of bacterial cell wall
Adverse Effects of Bismuth
1) Constipation
2) Black/Dark (regularly-formed) stools
Misoprostol (PGE analog) Mechanism
1) Increase Production and Secretion of Gastric Mucous Barrier
2) Decrease Acid Production (Parietal Cell)
Indications of Misoprostol
Prevention of NSAID-induced peptic ulcers
Off-label usage of Misoprostol
1) Cervical Ripening
2) Post-partum Hemorrhaging
3) Pregnancy Termination
Contraindications of Misoprostol
1) Pregnancy
2) IBD (AVOID)
List the Serotonin (5-HT3) Receptor Antagonists
1) Dolasetron
2) Granisetron
3) Ondansetron
4) Palonosetron
Mechanism of action of 5-HT3 receptor antagonists
Blocks 5-HT3 Receptors at vagal nerve terminals and to CTZ
Ondansetron is most commonly used for ____
Mild N/V
Indications for 5-HT3 Blockers
1) CINV
2) RINV
3) PONV
4) NVP
5) Mild N/V
____ and ____ are 5-HT3 Blockers that are used for delayed CINV as a single dose
1) Palonosetron
2) Sustained-Release Formulation of Granisetron
Adverse Effects of 5-HT3 Blockers
1) Serotonin Syndrome
2) Dose-dependent QT Prolongation (Torsade’s)
5-HT3 Blockers Drug interaction
Antiarrhythmics/QT-prolonging agents
Which 5-HT3 blocker has the highest risk of death
Dolasetron
List the Neurokinin (NKI) Receptor Antagonists
1) Aprepitant
2) Fosaprepitant
3) Netupitant
4) Fosnetupitant
5) Rolapitant
MOA of Neurokinin (NK1) Receptor Antagonists
Blockade of NK1 (Substances P) receptors in CTZ/VC
Indications of NK1 receptors Blockers
CINV (most effective when used in combination)
Which of the NK1 Blockers have the longest half lives
1) Netupitant
2) Rolapitant
List the Histamine (H1) Receptor Antagonists
1) Diphenhydramine
2) Dimenhydrinate
3) Hydroxyzine
4) Meclizine
5) Cyclizine
6) Doxylamine
MOA of Histamine receptor antagonists
Block H1 receptors in VC and Vestibular System
Indications of H1 Blockers
1) PONV
2) NVP ( Doxylamine/B6)
3) Motion Sickness/Vertigo (Meclizine and Cyclizine)
4) CINV (Add on therapy)
5) RINV (Add on therapy)
6) Mild N/V
Adverse Effects of H1 Blockers
Anticholinergics Effects
- Drowsiness (CNS Depression)
- Dry Mouth
- Constipation
- Urinary Retention
- Blurred Vision
- Decreased BP
What is the initial therapy for NVP?
Doxylamine w/ Pyridoxine
List the Dopamine D2 Receptor Antagonists
1) Prochlorperazine
2) Olanzapine
3) Metoclopramide
4) Amisulpride
Primary MOA of D2 Receptor Blockers
1) D2 receptor blockade in CTZ
Metoclopramide is a ___ receptor blocker. What additional MOA does it have?
1) Stimulates ACh actions in GI
- Enhances GI motility (Dysmotility use)
- Increases Lower Esophageal Sphincter Tone
Indication for Amisulpride
PONV (IV FORM)
List the indications for D2 Receptor Blockers
1) PONV (Amisulpride)
2) NVP
3) Gastroparesis/Dysmotility (Metoclopramide)
4) CINV and RINV
General adverse effects of D2 Blockers
1) Drowsiness (All agents)
2) Hypotension (primarily from IV route)
Adverse Effects of Prochlorperazine
1) Drowsiness
2) Constipation
3) Urinary Retention
4) Blurred Vision
Amisulpride Adverse Effects
1) Hypokalemia
2) Hyperprolactinemia
3) Chills
List the Muscarinic Receptor Antagonists
Scopolamine
MOA of Scopolamine
Blocks ACh-stimulated muscarinic receptors from vestibular nuclei and reticular formation to VC
Indication of Scopolamine
1) Motion Sickness
2) End-of-life care for excessive secretions
Adverse Effects of Scopolamine
1) Drowsiness
2) Dry Mouth
3) Constipation
4) Urinary Retention
5) Blurred Vision
Scopolamine can be worn as a transdermal scope patch that lasts ____
72 hours
List the Cannabinoid Receptor Agonists
1) Dronabinol
2) Nabilone
MOA of cannabinoid Receptor Agonists
Stimulates CB1 (central) and CB2 (peripheral) cannabinoid receptors in VC/CTZ
- Decreases excitability of neurons
- Minimizes serotonin release from vagal afferent terminals
Indications of Cannabinoid Receptor Agonists
1) CINV (reserved for treatment-resistant scenarios) can be used as an add on
2) Appetite Stimulation
Describe H. Pylori Treatment
1) Triple therapy (14 days) - all agents 2x day
* ** Only for low Clarithromycin resistance areas and No prior exposure to Clarithromycin
- PPI
- Clarithromycin
- Amoxicillin or Metronidazole
Describe Quadruple Therapy of H. Pylori
1) PPI twice/day all other agents four times/day
- PPI
- Metronidazole
- Amoxicillin (Tetracycline; esp for PCN allergy)
- Bismuth Subsalicylate
Describe the substitutions for Quadruple Therapy of H. Pylori
1) Clarithromycin for Bismuth
2) Levofloxacin for failed eradication
Treatment for Clostridium Difficle
1) ORAL Vancomycin (Fidaxomicin = alternative)
2) I.V. Metronidazole (for severe disease + Oral Vancomycin)
Campylobacter Jejuni Treatment
Azithromycin (Ciprofloxacin = alternative)
Salmonella Spp. Treatment
Ciprofloxacin/Levofloxacin (Azithromycin (alternative)
Shigella Spp. Treatment
Ciprofloxacin/Levofloxacin (Azithromycin = Alternative)