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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.
A study of the United Kingdom General Practice Research Database, which contains over 80,000 men, found that the relative risk of gynecomastia in cimetidine users was 7.2 relative to non-users. [52] People taking a dosage of cimetidine of greater than or equal to 1,000 mg showed more than 40 times the risk of gynecomastia than non-users. [ 52 ]
When these medications are used long term, the lowest effective dose should be taken. [4] They may also be taken only when symptoms occur in those with frequent problems. [5] Proton-pump inhibitors are named using the suffix "-prazole". There is a purported correlation (but no proven causal link) between the use of PPIs and the risk of dementia ...
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.
Ranitidine has 10% of the affinity that cimetidine has to CYP450, so it causes fewer side effects, but other H 2 blockers famotidine and nizatidine have no CYP450 significant interactions. [ 131 ] Ranitidine was introduced in 1981, and was the world's biggest-selling prescription drug by 1987. [ 132 ]
Therefore, PPIs are often routinely prescribed for cirrhotic patients to treat GERD and prevent variceal bleeding. However, it has been recently shown that long term use of PPIs in patients with cirrhosis increases the risk of SBP and is associated with the development of clinical decompensation and liver-related death during long-term follow ...
[9] [10] This use is on the label in the UK and some other countries. It is also used off-label in the treatment of cyclical vomiting syndrome in infants; the only evidence for this use comes from retrospective studies. [11] Cyproheptadine is sometimes used off-label to improve akathisia in people on antipsychotic medications. [12]
Use appears to be safe in pregnancy and breastfeeding. [6] How it works is unclear but is believed to involve binding to the ulcer and protecting it from further damage. [3] [6] Sucralfate was approved for medical use in the United States in 1981. [3] It is available as a generic medication.