Betaine Hydrochloride

(BANM, rINNM)

💊 Chemical information

Betaiinihydrokloridi; Betaína, hidrocloruro de; Betainhydroklorid; Betaini Hydrochloridum; Trimethylglycine Hydrochloride. (Carboxymethyl)trimethylammonium hydroxide inner salt hydrochloride.
Chemical formula: C5H11NO2,HCl = 153.6.
CAS — 590-46-5.
ATC — A09AB02.
ATC Vet — QA09AB02.

Pharmacopoeias.

In US.

USP 31

(Betaine Hydrochloride). A white crystalline powder. Soluble in water and in alcohol; practically insoluble in chloroform and in ether. A 25% solution in water has a pH of 0.8 to 1.2.

💊 Profile

Betaine is used as a methyl donor to remethylate homocysteine to methionine in the treatment of patients with homocystinuria. It is given orally in a usual dose of 3 g twice daily. Doses are adjusted according to plasma-homocysteine concentrations; up to 20 g daily has been required in some patients. In children under 3 years old, an initial dose of 100 mg/kg daily given in 2 divided doses may be used. Severe cerebral oedema and hypermethioninaemia have been reported in a few patients, and it is recommended that plasmamethionine concentrations should be monitored at the start of betaine treatment and periodically thereafter. Patients being treated for cystathionine beta-synthase deficiency may pose particular problems because betaine may further raise their already elevated methionine concentrations increasing the risk of cerebral oedema. Betaine has also been used as a variety of salts in preparations for liver and gastrointestinal disorders. The hydrochloride has been given as a source of hydrochloric acid in the treatment of hypochlorhydria.

Adverse effects.

References.
1. Devlin AM, et al. Cerebral edema associated with betaine treatment in classical homocystinuria. J Pediatr 2004; 144: 545–8.

Homocystinuria.

References.
1. Smolin LA, et al. The use of betaine for the treatment of homocystinuria. J Pediatr 1981; 99: 467–72
2. Wilcken DEL, et al. Homocystinuria—the effects of betaine in the treatment of patients not responsive to pyridoxine. N Engl J Med 1983; 309: 448–53
3. Holme E, et al. Betaine for treatment of homocystinuria caused by methylenetetrahydrofolate reductase deficiency. Arch Dis Child 1989; 64: 1061–4
4. Anonymous. Betaine for homocystinuria. Med Lett Drugs Ther 1997; 39: 12.

Liver disorders.

Betaine has also been investigated for the treatment of nonalcoholic steatohepatitis.
1. Miglio F, et al. Efficacy and safety of oral betaine glucuronate in non-alcoholic steatohepatitis: a double-blind, randomized, parallel-group, placebo-controlled prospective clinical study. Arzneimittelforschung 2000; 50: 722–7
2. Abdelmalek MF, et al. Betaine, a promising new agent for patients with nonalcoholic steatohepatitis: results of a pilot study. Am J Gastroenterol 2001; 96: 2711–7.

Pharmacokinetics.

References.
1. Schwahn BC, et al. Pharmacokinetics of oral betaine in healthy subjects and patients with homocystinuria. Br J Clin Pharmacol 2003; 55: 6–13.

💊 Preparations

Proprietary Preparations

Austral.: Cystadane; Canad.: Cystadane; Cz.: Cystadane; Israel: Cystadan; Ital.: Somatyl; Port.: Cystadane; USA: Cystadane. Multi-ingredient: Arg.: Eucos-L†; Austral.: Betaine Digestive Aid; Bioglan Digestive Zyme; Digestaid; Austria: CO Granulat; Oroacid; Belg.: Digestomen; Braz.: Aminotox†; Anekron; Betaliver†; Biohepax; Colachofra; Enterofigon; Epocler; Hepacitron†; Hepalin; Hepatobe†; Hepatox; Hormo Hepatico†; Metiocolin Composto; Necro B-6; Xantinon Complex; Cz.: Citrargine†; CO Granulat†; Fr.: Citrarginine†; Gastrobul†; Hepagrume; Nivabetol; Ornitaine; Ger.: CO Granulat†; Flacar; Unexym MD S; Gr.: Kloref; Hong Kong: Jetepar; Hung.: Betacid; Gastrobul†; Indon.: Naturica DFM; Israel: Betazim; Ital.: Citroepatina; Epabetina†; Ietepar†; Malaysia: Jetepar; Neth.: Gastrobul; Philipp.: Jetepar; S.Afr.: Kloref; Singapore: Jetepar; Switz.: Pepsi-Chlor†; UK: Enzyme Digest; Enzyme Plus; Kloref.
Published January 16, 2019.