Cimetidine
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Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid production.[1][7][8] It is mainly used in the treatment of heartburn and peptic ulcers.[1][8][9]
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Pronunciation | /sɪˈmɛtɪdiːn/ or /saɪˈmɛtɪdiːn/ |
Trade names | Tagamet, others |
Other names | SKF-92334[1] |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682256 |
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Routes of administration | By mouth, intramuscular injection, intravenous infusion[2] |
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Bioavailability | 60–70%[3][4] |
Protein binding | 13–25%[4][5] |
Metabolism | Liver[4] |
Metabolites | • Cimetidine sulfoxide[4] • Hydroxycimetidine[4] • Guanyl urea cimetidine[4] |
Onset of action | 30 minutes[6] |
Elimination half-life | 123 minutes (~2 hours)[5] |
Duration of action | 4–8 hours[2] |
Excretion | Urine[5] |
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ECHA InfoCard | 100.052.012 |
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Formula | C10H16N6S |
Molar mass | 252.34 g·mol−1 |
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With the development of proton pump inhibitors, such as omeprazole, approved for the same indications, cimetidine is available as an over-the-counter formulation to prevent heartburn or acid indigestion, along with the other H2-receptor antagonists.[10]
Cimetidine was developed in 1971 and came into commercial use in 1977.[11][12] Cimetidine was approved in the United Kingdom in 1976,[citation needed] and was approved in the United States by the Food and Drug Administration in 1979.[13]