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Perry T, editor. Therapeutics Letter. Vancouver (BC): Therapeutics Initiative; 1994-.
Therapeutics Letter 1 addresses common questions, including dosage, about H2-blockers for treatment of non-ulcer dyspepsia in adults. Other than cost, there is little difference between the four H2-blockers (Cimetidine, Famotidine, Nizatidine, and Ranitidine) available in British Columbia.
Keywords:
Cimetidine, Dyspepsia, Famotidine, Histamine H2 Antagonists, Nizatidine, /RanitidineThere are four H2-blockers available for prescription in British Columbia (see Table). These four drugs all act to reduce gastric acid secretion and are similar chemically and pharmacokineticaly; they are all eliminated mostly by the kidney and they have similar half-lives of around 2 hours.1 Despite the short half-life, they are all effective in most patients when given once daily at bed-time.1 Administration of any of the four H2-blockers results in healing after 8 weeks of therapy in 80% of the cases. The approximate clinically equivalent doses are shown in the Table reflecting some difference in potency, which is not of any clinical significance. The safety profile of all four drugs is excellent with a low percentage of patients developing side effects, requiring discontinuing the drug.1
Commonly asked questions
•. What about confusion in the elderly?
The outpatient incidence of CNS reactions including confusion is 0.2% or less. There is no evidence of a higher incidence with one H2-blocker as compared with another.2
•. What about drug interactions?
Cimetidine and to a lesser extent ranitidine have the capacity to inhibit the metabolism of some other drugs to a small usually clinically insignificant degree (10 to 30%). Cimetidine only needs to be avoided in combination with the following three drugs: warfarin, phenytoin, and theophylline.
•. What about gynecomastia?
Cimetidine is associated with a 0.3% overall incidence of gynecomastia; the risk is less with doses less than 1000 mg daily.3
•. Is it possible to switch from one H2-blocker to another?
Patients can be readily switched from one H2-blocker to another in equivalent dose without any risk to the patient.
•. How much should the dose be reduced in the elderly?
In the elderly and other patients with reduced renal function the doses used should be 1/2 to 1/4 of the usual doses.1
•. Is it safe to stop H2-blockers in patients who have been on long term maintenance therapy?
Studies have shown that many patients are inappropriately maintained on H2-blockers.4 Maintenance therapy should be limited to patients with proven recurrent peptic ulcer disease, or severe recurrent dyspepsia. The need for maintenance therapy will be markedly diminished with the appropriate eradication of Helicobacter pylori (see next Therapeutics Letter). It is safe to abruptly stop the drug in such patients. If a patient develops symptoms consistent with rebound hyperacidity the dose of the drug can be tapered over a 2–3 week period and stopped.
Conclusion
There is little difference between the various H 2 -blockers other than cost.
References
- 1.
- Feldman M., Burton ME. Histamine2 - receptor antagonists. Standard therapy for acid-peptic diseases. New England Journal of Medicine 323:1672–80, 1749–55; 1990 [PubMed: 1978250]
- 2.
- Cantú TG, Korek JS. Central nervous system reactions to histamine-2 receptor blockers. Annals of Internal Medicine 114:1027–34; 1994 [PubMed: 1674198]
- 3.
- Rodriguez LAG, Jick H. Risk of gynecomastia associated with cimetidine, omeprazole, and other antiulcer drugs. British Medical Journal 308: 503–6; 1994 [PMC free article: PMC2542783] [PubMed: 8136667]
- 4.
- Carmichael JM, Zell SC. Survey of ulcer recurrence risk factors associated with long-term cimetidine prescribing. Drug Intelligence and Clinical Pharmacy 21: 452–8; 1987 [PubMed: 3582174]
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- [Inhibition of 24-hour acidity by nizatidine].[Fortschr Med. 1989][Inhibition of 24-hour acidity by nizatidine].Dammann HG, Dreyer M, Gottlieb WR, Wolf N, Müller P, Simon B. Fortschr Med. 1989 May 10; 107(14):321-4.
- Effects of H2-receptor antagonists on gastric alcohol dehydrogenase activity.[Dig Dis Sci. 1991]Effects of H2-receptor antagonists on gastric alcohol dehydrogenase activity.Caballería J, Baraona E, Deulofeu R, Hernández-Muñoz R, Rodés J, Lieber CS. Dig Dis Sci. 1991 Dec; 36(12):1673-9.
- Neurotoxic convulsions induced by histamine H2 receptor antagonists in mice.[Toxicol Appl Pharmacol. 1996]Neurotoxic convulsions induced by histamine H2 receptor antagonists in mice.Shimokawa M, Yamamoto K, Kawakami J, Sawada Y, Iga T. Toxicol Appl Pharmacol. 1996 Feb; 136(2):317-23.
- Review Histamine Type-2 Receptor Antagonists (H2 Blockers).[LiverTox: Clinical and Researc...]Review Histamine Type-2 Receptor Antagonists (H2 Blockers).. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. 2012
- Review Clinical review of histamine2 receptor antagonists.[Arch Intern Med. 1990]Review Clinical review of histamine2 receptor antagonists.Lipsy RJ, Fennerty B, Fagan TC. Arch Intern Med. 1990 Apr; 150(4):745-51.
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