Ranitidine Bismuth Citrate

(BAN, USAN)
Synonyms: A complex of ranitidine and bismuth citrate; GR-122311X; Ranitidin Bizmut Sitrat; Ranitidin Bizmutreks; Ranitidina y bismuto, citrato de; Ranitidine Bismutrex. N-[2-({5-[(Dimethylamino)methyl]furfuryl}thio)-ethyl]N′-methyl-2-nitro-1,1-ethenediamine, compound with bismuth(3+) citrate (1:1).
Cyrillic synonym: Ранитидин Висмут Цитрат.

💊 Chemical information

Chemical formula: C13H22N4O3S,C6H5BiO7 = 712.5.
CAS — 128345-62-0.
ATC — A02BA07.
ATC Vet — QA02BA07.

💊 Adverse Effects and Precautions

Ranitidine bismuth citrate would be expected to combine the adverse effects of both bismuth compounds and ranitidine. Blackening of the tongue and faeces is common, and gastrointestinal disturbances, headache, mild anaemia, and altered liver enzyme values have been reported. Rarely, hypersensitivity reactions (including anaphylaxis), have occurred. Ranitidine bismuth citrate should not be given to patients with moderate to severe renal impairment. It is not suitable for longterm or maintenance therapy because of the risk of bismuth accumulation. As with other antisecretory drugs, the possibility of malignancy should be considered when giving ranitidine bismuth citrate to patients with gastric ulcers since the drug may mask symptoms and delay diagnosis.

💊 Interactions

Ranitidine bismuth citrate would be expected to have the interactions of bismuth compounds, and ranitidine.

💊 Pharmacokinetics

After oral doses, ranitidine bismuth citrate dissociates into its ranitidine and bismuth components in the stomach. For the pharmacokinetics of ranitidine, and for those of bismuth.
1. Lacey LF, et al. Comparative pharmacokinetics of bismuth from ranitidine bismuth citrate (GR122311X), a novel anti-ulcerant and tripotassium dicitrato bismuthate (TDB). Eur J Clin Pharmacol 1994; 47: 177–80
2. Koch KM, et al. Pharmacokinetics of bismuth and ranitidine following single doses of ranitidine bismuth citrate. Br J Clin Pharmacol 1996; 42: 201–5
3. Koch KM, et al. Pharmacokinetics of bismuth and ranitidine following multiple doses of ranitidine bismuth citrate. Br J Clin Pharmacol 1996; 42: 207–11.

💊 Uses and Administration

Ranitidine bismuth citrate is a complex of ranitidine with bismuth and citrate, which releases ranitidine and bismuth in the gastrointestinal tract and therefore possesses both the actions of the bismuth compounds and of ranitidine. It has been used in the management of peptic ulcer disease, and may be given with antibacterials for the eradication of Helicobacter pylori infection and the prevention of relapse of peptic ulcer disease. Doses are 400 mg twice daily orally; treatment has usually been given for 4 to 8 weeks for duodenal ulceration and for 8 weeks for benign gastric ulceration. Ranitidine bismuth citrate should not be used for maintenance therapy, and a maximum of 16 weeks of treatment (two 8-week courses or four 4-week courses) may be given in a 12-month period. For duodenal ulceration where H. pylori infection is present, ranitidine bismuth citrate has been given as part of a 7-day triple therapy regimen, typically combined with any two of clarithromycin 500 mg twice daily, amoxicillin 1 g twice daily, or metronidazole 400 mg twice daily. Alternatively, a 14-day dual therapy regimen of ranitidine bismuth citrate combined with clarithromycin 500 mg two or three times daily has been used. In both regimens ranitidine bismuth citrate alone may be continued to a total of 28 days.
1. Bardhan KD, et al. GR122311X (ranitidine bismuth citrate), a new drug for the treatment of duodenal ulcer. Aliment Pharmacol Ther 1995; 9: 497–506
2. Peterson WL, et al. Ranitidine bismuth citrate plus clarithromycin is effective for healing duodenal ulcers, eradicating H.pylori and reducing ulcer recurrence. Aliment Pharmacol Ther 1996; 10: 251–61
3. Anonymous. Pylorid, H. pylori and peptic ulcer. Drug Ther Bull 1996; 34: 69–70
4. van der Wouden EJ, et al. One-week triple therapy with ranitidine bismuth citrate, clarithromycin and metronidazole versus two-week dual therapy with ranitidine bismuth citrate and clarithromycin for Helicobacter pylori infection: a randomized, clinical trial. Am J Gastroenterol 1998; 93: 1228–31.

💊 Preparations

Proprietary Preparations

Arg.: Pylorid†; Austria: Helirad; Pylorisin; Belg.: Pylorid†; Braz.: Pylorid; Cz.: Eradipak†; Denm.: Pylorid†; Fin.: Pylorid; Gr.: Pylorid; Hong Kong: Pylorid†; Hung.: Pylorid†; Irl.: Pylorid†; Ital.: Elicodil†; Pylorid; Mex.: Azanplus; Neth.: Pylorid†; Norw.: Pylorid; Port.: Pylorid†; Spain: Pylorid; Switz.: Pylorid†; Thai.: Pylorid†; Turk.: Pylorid; UK: Pylorid†; Venez.: Pylorid. Multi-ingredient: Austral.: Pylorid-KA.
Published March 10, 2019.