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Cimetidine is rapidly absorbed regardless of route of administration. [7] The oral bioavailability of cimetidine is 60 to 70%. [5] [6] The onset of action of cimetidine when taken orally is 30 minutes, [8] and peak levels occur within 1 to 3 hours. [5] Cimetidine is widely distributed throughout all tissues. [7]
Cimetidine was the first drug ever to reach more than $1 billion a year in sales, thus making it the first blockbuster drug. [ 26 ] In the pharmaceutical industry, a blockbuster drug is one that achieves acceptance by prescribing physicians as a therapeutic standard for, most commonly, a highly prevalent chronic (rather than acute) condition.
Cimetidine was the prototypical histamine H 2 receptor antagonist from which later drugs were developed. Cimetidine was the culmination of a project at Smith, Kline & French (SK&F; now GlaxoSmithKline) by James W. Black, C. Robin Ganellin, and others to develop a histamine receptor antagonist that would suppress stomach acid secretion.
This is often called linear pharmacokinetics, as the change in concentration over time can be expressed as a linear differential equation =. Assuming a single IV bolus dose resulting in a concentration C initial {\displaystyle C_{\text{initial}}} at time t = 0 {\displaystyle t=0} , the equation can be solved to give C = C initial × e − k el ...
Nizatidine was developed by Eli Lilly, and was first marketed in 1988. [3] It is considered to be equipotent with ranitidine and differs by the substitution of a thiazole ring in place of the furan ring in ranitidine.
[50] Rauws and Tytgat describe cure of duodenal ulcer by eradication of H. pylori using Borody's triple therapy combination. [51] Triple-therapy, modernized to a proton pump inhibitor and two antibiotics, soon becomes first line therapy for eradication. World Congress of Gastroenterology recommends eradicating H. pylori to cure duodenal ulcers ...
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Notable drugs that experience a significant first pass effect are buprenorphine, chlorpromazine, cimetidine, diazepam, ethanol (drinking alcohol), imipramine, insulin, lidocaine, midazolam, morphine, pethidine, propranolol, and tetrahydrocannabinol (THC). First-pass metabolism is not to be confused with Phase I metabolism, which is a separate ...
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