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H2 receptor blockers
PPIs versus H2 antagonist |
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| Treatment of bleeding peptic ulcers : A meta-analysis of 21 randomized controlled trials evaluating proton pump inhibitors for bleeding ulcers (with or without endoscopic therapy) found a significant and consistent reduction in the risk of rebleeding. In contrast, studies on H2 antagonists have generally produced disappointing results. A meta-analysis concluded that there was a possible minor benefit with intravenous H2 antagonists in bleeding gastric ulcers but no benefit with duodenal ulcers. The relative efficacy of the proton pump inhibitors may be due to their superior ability to maintain a gastric pH at a level above 6.0, and thus protect an ulcer clot from fibrinolysis. | ||||
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cimetidine (Tagamet ®)
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Active ulcer: Oral: 800 mg orally at bedtime or
300mg orally four times daily or 400 mg orally twice daily. IM/IV: 300mg
every 6 hours or 37.5 mg/hr continuous infusion. Active bleed: 37.5 mg/hr continuous IV (maximum 2400mg/day). Maintanance (duodenal ulcer prophylaxis): 400mg orally at bedtime. Gastric hypersecretory conditions: 300 to 600mg every 6 hours. Renal Dosing: >40 ml/min: no change || 20-40 ml/min: give usual dose q8h or give 75% of usual dose. || 0-20 ml/min: Usual dose q12h or give 50% of usual dose. |
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famotidine (Pepcid ® )
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Indications Therapy and treatment of duodenal ulcer, gastric ulcer, control gastric pH in critically-ill patients, symptomatic relief in gastritis, gastroesophageal reflux, active benign ulcer, and pathological hypersecretory conditions OTC labeling: Relief of heartburn, acid indigestion, and sour stomach Mechanism of Action Competitive inhibition of histamine at H2 receptors of the gastric parietal cells, which inhibits gastric acid secretion Dosing- Adults: Duodenal ulcer: Oral: Acute therapy: 40 mg/day at bedtime for 4-8 weeks; maintenance therapy: 20 mg/day at bedtime Helicobacter pylori eradication (unlabeled use): 40 mg once daily; requires combination therapy with antibiotics Gastric ulcer: Oral: Acute therapy: 40 mg/day at bedtime Hypersecretory conditions: Oral: Initial: 20 mg every 6 hours, may increase in increments up to 160 mg every 6 hours GERD: Oral: 20 mg twice daily for 6 weeks Esophagitis and accompanying symptoms due to GERD: Oral: 20 mg or 40 mg twice daily for up to 12 weeks Patients unable to take oral medication: I.V.: 20 mg every 12 hours Dosing adjustment in renal impairment: Clcr<50 mL/minute: Manufacturer recommendation: Administer 50% of dose or increase the dosing interval to every 36-48 hours (to limit potential CNS adverse effects). Supplied: Gelcap (Pepcid® AC): 10 mg Infusion [premixed in NS] (Pepcid®): 20 mg (50 mL) Injection, solution: 10 mg/mL (4 mL, 20 mL, 50 mL) [contains benzyl alcohol] Injection, solution [preservative free] (Pepcid®): 10 mg/mL (2 mL) Powder for oral suspension (Pepcid®): 40 mg/5 mL (50 mL) Tablet: 10 mg [OTC], 20 mg, 40 mg Pepcid®: 20 mg, 40 mg [film coated] Pepcid® AC: 10 mg, 20 mg Tablet, chewable (Pepcid® AC): 10 mg [contains phenylalanine 1.4 mg/tablet; mint flavor] Tablet, orally-disintegrating (Fluxid™): 20 mg, 40 mg [cherry flavor]
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nizatidine (Axid ® )
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Dosing- Adults: Duodenal ulcer: Treatment of active ulcer: 300 mg at bedtime or 150 mg twice daily Maintenance of healed ulcer: 150 mg/day at bedtime Gastric ulcer: 150 mg twice daily or 300 mg at bedtime GERD: 150 mg twice daily Meal-induced heartburn, acid indigestion, and sour stomach: 75 mg tablet [OTC] twice daily, 30 to 60 minutes prior to consuming food or beverages Helicobacter pylori eradication (unlabeled use): 150 mg twice daily; requires combination therapy Dosing adjustment in renal impairment: Active treatment: Clcr 20-50 mL/minute: 150 mg/day Clcr<20 mL/minute: 150 mg every other day Maintenance treatment: Clcr 20-50 mL/minute: 150 mg every other day Clcr<20 mL/minute: 150 mg every 3 days Supplied Capsule (Axid®): 150 mg, 300 mg Solution, oral (Axid®): 15 mg/mL (480 mL) [bubble gum flavor] Tablet (Axid® AR): 75 mg |
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ranitidine (Zantac ® )
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Indications Zantac®: Short-term and maintenance therapy of duodenal ulcer, gastric ulcer, gastroesophageal reflux, active benign ulcer, erosive esophagitis, and pathological hypersecretory conditions; as part of a multidrug regimen for H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Zantac® 75 [OTC]: Relief of heartburn, acid indigestion, and sour stomach. Mechanism of Action Competitive inhibition of histamine at H2-receptors of the gastric parietal cells, which inhibits gastric acid secretion, gastric volume, and hydrogen ion concentration are reduced. Does not affect pepsin secretion, pentagastrin-stimulated intrinsic factor secretion, or serum gastrin. Dosing- Adults: Duodenal ulcer: Oral: Treatment: 150 mg twice daily, or 300 mg once daily after the evening meal or at bedtime; maintenance: 150 mg once daily at bedtime Helicobacter pylori eradication: 150 mg twice daily; requires combination therapy Pathological hypersecretory conditions: Oral: 150 mg twice daily; adjust dose or frequency as clinically indicated; doses of up to 6 g/day have been used I.V.: Continuous infusion for Zollinger-Ellison: 1 mg/kg/hour; measure gastric acid output at 4 hours, if >10 mEq or if patient is symptomatic, increase dose in increments of 0.5 mg/kg/hour; doses of up to 2.5 mg/kg/hour have been used Gastric ulcer, benign: Oral: 150 mg twice daily; maintenance: 150 mg once daily at bedtime Erosive esophagitis: Oral: Treatment: 150 mg 4 times/day; maintenance: 150 mg twice daily Prevention of heartburn: Oral: Zantac® 75 [OTC]: 75 mg 30-60 minutes before eating food or drinking beverages which cause heartburn; maximum: 150 mg in 24 hours; do not use for more than 14 days Patients not able to take oral medication: I.M.: 50 mg every 6-8 hours I.V.: Intermittent bolus or infusion: 50 mg every 6-8 hours Continuous I.V. infusion: 6.25 mg/hour Elderly: Ulcer healing rates and incidence of adverse effects are similar in the elderly, when compared to younger patients; dosing adjustments not necessary based on age alone Dosing adjustment in renal impairment: Adults: Clcr<50 mL/minute: Oral: 150 mg every 24 hours; adjust dose cautiously if needed I.V.: 50 mg every 18-24 hours; adjust dose cautiously if needed Hemodialysis: Adjust dosing schedule so that dose coincides with the end of hemodialysis Administration Ranitidine injection may be administered I.M. or I.V.: I.M.: Injection is administered undiluted. I.V.: Must be diluted; may be administered IVP or IVPB or continuous I.V. infusion. IVP: Ranitidine (usually 50 mg) should be diluted to a total of 20 mL with NS or D5W and administered over at least 5 minutes. IVPB: Administer over 15-20 minutes. Continuous I.V. infusion: Administer at 6.25 mg/hour and titrate dosage based on gastric pH by continuous infusion over 24 hours Supplied Capsule, as hydrochloride: 150 mg, 300 mg Infusion, as hydrochloride [premixed in NaCl 0.45%; preservative free] (Zantac®): 50 mg (50 mL) Injection, solution, as hydrochloride (Zantac®): 25 mg/mL (2 mL, 6 mL, 40 mL) Syrup, as hydrochloride: 15 mg/mL (10 mL) [contains alcohol 7.5%; peppermint flavor] Zantac®: 15 mg/mL (473 mL) [contains alcohol 7.5%; peppermint flavor] Tablet, as hydrochloride: 75 mg [OTC], 150 mg, 300 mg Zantac®: 150 mg, 300 mg Zantac® 75: 75 mg TTablet, effervescent, as hydrochloride (Zantac® EFFERdose®): 25 mg [contains sodium 1.33 mEq/tablet, phenylalanine 2.81 mg/tablet, and sodium benzoate]; 150 mg [contains sodium 7.96 mEq/tablet, phenylalanine 16.84 mg/tablet, and sodium benzoate] |
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