Thiamphenicol Glycinate Hydrochloride

(BAN, USAN, rINN)

💊 Chemical information

Thiamphenicol Aminoacetate Hydrochloride; Tiamfenicolo Glicinato Cloridrato; Tianfenicol, hidrocloruro del glicinato de.
Chemical formula: C14H18Cl2N2O6S,HCl = 449.7.
CAS — 2393-92-2 (thiamphenicol glycinate); 2611-61-2 (thiamphenicol glycinate hydrochloride). ATC — J01BA02.
ATC Vet — QJ01BA02.

Pharmacopoeias.

In It.

💊 Adverse Effects and Precautions

As for Chloramphenicol. Thiamphenicol is probably more liable to cause dose-dependent reversible depression of the bone marrow than chloramphenicol but it is not usually associated with aplastic anaemia. Thiamphenicol also appears to be less likely to cause the ‘grey syndrome’ in neonates. Doses of thiamphenicol should be reduced in patients with renal impairment. It is probably not necessary to reduce doses in patients with hepatic impairment.

💊 Interactions

As for Chloramphenicol. Although thiamphenicol is not metabolised in the liver and might not be expected to be affected by drugs which induce hepatic enzymes, it is reported to inhibit hepatic microsomal enzymes and may affect the metabolism of other drugs.

💊 Antimicrobial Action

Thiamphenicol has a broad spectrum of activity resembling that of chloramphenicol. Although in general it is less active than chloramphenicol it is reported to be equally effective, and more actively bactericidal, against Haemophilus and Neisseria spp. Cross-resistance occurs between thiamphenicol and chloramphenicol. However, some strains resistant to chloramphenicol may be susceptible to thiamphenicol.

💊 Pharmacokinetics

Thiamphenicol is absorbed from the gastrointestinal tract after oral doses and peak serum concentrations of 3 to 6 micrograms/mL have been achieved about 2 hours after a 500mg dose. Thiamphenicol diffuses into the CSF, across the placenta, into breast milk, and penetrates well into the lungs. About 10% is bound to plasma proteins. The half-life of thiamphenicol is around 2 to 3 hours but unlike chloramphenicol the half-life is increased in patients with renal impairment. It is excreted in the urine, about 70% of a dose being excreted in 24 hours as unchanged drug. It undergoes little or no conjugation with glucuronic acid in the liver. A small amount is excreted in the bile and the faeces.

💊 Uses and Administration

Thiamphenicol has been used similarly to chloramphenicol in the treatment of susceptible infections, including sexually transmitted diseases. The usual adult oral dose is 1.5 g daily in divided doses; up to 3 g daily has been given initially in severe infections. A daily dose of 30 to 100 mg/kg may be used in children. Equivalent doses, expressed in terms of thiamphenicol base, may be given by intramuscular or intravenous injection as the more water soluble glycinate hydrochloride; 1.26 g of thiamphenicol glycinate hydrochloride is equivalent to about 1 g of thiamphenicol. Doses should be reduced in patients with renal impairment (see below). For the treatment of gonorrhoea, oral doses of thiamphenicol have ranged from 2.5 g daily for 1 or 2 days through to 2.5 g on the first day followed by 2 g daily on each of 4 subsequent days. The single daily dose may be most appropriate for male patients with uncomplicated gonorrhoea. Thiamphenicol glycinate hydrochloride may also be given by inhalation, or by endobronchial or intracavitary instillation. Thiamphenicol has also been used as thiamphenicol glycinate acetylcysteinate, thiamphenicol sodium glycinate isophthalolate, and thiamphenicol palmitate.

Administration in renal impairment.

Doses of thiamphenicol should be reduced in patients with renal impairment according to creatinine clearance (CC):
CC 30 to 60 mL/minute: 500 mg twice daily
CC 10 to 30 mL/minute: 500 mg once daily

💊 Preparations

Proprietary Preparations

Belg.: Fluimucil Antibiotic; Urfamycine; Braz.: Glitisol; Fr.: Thiophenicol; Hong Kong: Urfamycin; Indon.: Biothicol; Canicol; Cetathiacol; Comthycol; Conucol; Corsafen; Daiticin; Dexycol; Genicol; Ipibiofen; Kalticol; Lacophen; Lanacol; Nikolam; Nilacol; Nufathiam; Opiphen; Phenobiotic; Promixin; Renamoca; Sendicol; Thiambiotic; Thiamet; Thiamfilex; Thiamika; Thiamycin; Thislacol; Troviakol; Urfamycin; Urfekol; Venacol; Zumatab; Ital.: Fluimucil Antibiotico; Glitisol; Mex.: Tiofeniclin; Rus.: Fluimucil Antibiotic (Флуимуцил антибиотик); Spain: Fluimucil Antibiotico†; Urfamycin†; Switz.: Urfamycine; Thai.: Doqua; Thiamcin; Treomycin; Urfamycin; Turk.: Thiophenicol; Tiofen; Urfamycin. Multi-ingredient: Spain: Flumil Antibiotico; Thai.: Fluimucil Antibiotic.
Published May 08, 2019.