Heartburn & Dyspepsia: Drugs Only Flashcards
Heartburn: Pharmacologic Therapy
- Antacids
- Histamine type 2 receptor antagonists (H2RAs)
- Proton pump inhibitors (PPIs)
- Bismuth subsalicylate
Antacids: MoA, FOR, Salts
- Neutralize gastric acid; act as buffering agents in GI tract
- FOR: Temporary and rapid relief of mild, infrequent heartburn
- Contain one of the following salts (all interchangeable):
• Magnesium (hydroxide, carbonate, or trisilicate)
• Aluminum (hydroxide or phosphate)
• Calcium carbonate
• Sodium bicarbonate
Avoid Antacids IF…
• Avoid antacid-aspirin combination products due to risk of serious bleed, especially in following patients:
- ≥60 years old
- History of stomach ulcers or bleeding problems
- Using anticoagulants, systemic steroids, or NSAIDs
- Consume ≥3 alcoholic beverages daily
Antacids: AE
- Mg2+ → diarrhea (avoid if CrCl <30 mL/min d/t toxicity)
- Al → constipation, hypophosphatemia (avoid if CrCl <30 mL/min)
- Ca2+ → belching and flatulence, constipation
• NaHCO3 → belching and flatulence
- Avoid in renal failure, HF, cirrhosis, pregnancy, and sodium-restricted diets
• If taking calcium supplement
- Avoid Ca2+ and NaHCO3 antacids
- Avoid Ca2+ antacid in renal failure
Antacids: Counseling
- Use product-specific doses, repeat in 1-2 hours if needed
- Food slows absorption (longer relief with food)
- Chew tablets well and drink 8 oz water
- Do not use >2x/week or >2 weeks
H2RAs: MoA, FOR
- Decrease fasting / food-stimulated gastric acid secretion and gastric volume by inhibiting histamine on the histamine type 2 receptor of the parietal cell
- Effective in relieving fasting and nocturnal symptoms
• FOR: mild-moderate, infrequent, or episodic heartburn and for prevention of heartburn associated with acid indigestion and dyspepsia
H2RAs: Counseling
• Reduce dose if impaired RENAL function (half dose in CrCl <50 mL/min) and in elderly
- Take at onset of sx or 30-60 min prior to anticipated heartburn, no more than 2x/day
- Tolerance may develop if taken daily (vs PRN)
H2RAs: Brands
- Tagament HB, Cimetidine
- Pepcid AC/Zantac 360, Famotidine
- Pepcid MAX, Zantac MAX, Famotidine
^ ALL 1 tab with water, max 2 tabs
- Pepcid Complete/Tums: Famotidine + Ca carb + mag OH (chew 1 tab, max 2)
H2RAs: AE & Interactions
• Adverse effects
- Headache, diarrhea, constipation, dizziness, drowsiness
- Thrombocytopenia is rare (and reversible)
- Cimetidine has weak anti-androgenic effects
• Drug interactions
- Cimetidine has many!!! Increases concentration of nifedipine (CCB) - monitor
- May decrease absorption of pH-dependent drugs: itraconazole, ketonazole, iron sulfate, calcium carbonate
PPIs: MoA, FOR
- Inhibit H+/K+ ATPase (proton pump)
- Irreversibly block the final step in gastric secretion, thus providing a greater prolonged and potent effect
- Indicated for frequent heartburn with symptoms ≥2 days/week or when not responding to non-rx H2RAs
- Not intended for immediate relief or occasional and acute episodes of heartburn and dyspepsia
PPIs: Counseling
- Onset: 2-3 hours, may take 1-4 days for complete relief
- Do not chew or crush tablets/capsules
- Only inhibit proton pumps that actively secrete acid so most effective 30-60 min before meal (preferably before breakfast)
- Limit to 14 days of use, no more than every 4 months
PPIs: AE
- Uncommon but may include diarrhea, constipation, headache
- Rebound acid reflux upon abruptly discontinuing after long term use
- May increase risk of traveler’s diarrhea by altering glut flora
PPIs: Interactions
• Omeprazole and esomeprazole
- May inhibit metabolism of clopidogrel via CYP 2C19 (check provider)
- May inhibit metabolism resulting in increased concentration of cilostazol and diazepam
• Avoid concurrent use
• Lansoprazole may be a safer alternative
Bismuth Subsalicylate (BSS)
- Indicated for heartburn, dyspepsia, indigestion, nausea, and diarrhea
- FDA approved for upset stomach (belching, gas) due to overindulgence in food and drink
- Topical effect on stomach mucosa
- Adult dose: 262-525 mg every 30-60 minutes as needed
- Not recommended for children or patients with renal failure or salicylate sensitivities
- May turn stool and/or tongue black
Elderly
- Avoid cimetidine; avoid H2RAs in those with or at high risk for delirium