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Tiotixene

Drug Approvals

(British Approved Name, rINN)

International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish):

Synonyms: NSC-108165; P-4657B; Thiothixene; Tiotikseeni; Tiotixen; Tiotixeno; Tiotixenum
BAN: Tiotixene
USAN: Thiothixene
INN: Tiotixene [rINN (en)]
INN: Tiotixeno [rINN (es)]
INN: Tiotixène [rINN (fr)]
INN: Tiotixenum [rINN (la)]
INN: Тиотиксен [rINN (ru)]
Chemical name: (Z)-NN-Dimethyl-9-[3-(4-methylpiperazin-1-yl)propylidene]thioxanthene-2-sulphonamide
Molecular formula: C23H29N3O2S2 =443.6
CAS: 5591-45-7; 3313-26-6 (tiotixene Z-isomer)
ATC code: N05AF04

Pharmacopoeias. In US.

The United States Pharmacopeia 31, 2008 (Thiothixene). White to tan, practically odourless, crystals. Practically insoluble in water soluble 1 in 110 of dehydrated alcohol, 1 in 2 of chloroform, and 1 in 120 of ether slightly soluble in acetone and in methyl alcohol. Store in airtight containers. Protect from light.

Drug Approvals

(British Approved Name Modified, rINNM)

International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish):

Synonyms: CP-12252-1; Thiothixene Hydrochloride; Tiotixeno, hidrocloruro de
BAN: Tiotixene Hydrochloride [BANM]
USAN: Thiothixene Hydrochloride
INN: Tiotixene Hydrochloride [rINNM (en)]
INN: Hidrocloruro de tiotixeno [rINNM (es)]
INN: Tiotixène, Chlorhydrate de [rINNM (fr)]
INN: Tiotixeni Hydrochloridum [rINNM (la)]
INN: Тиотиксена Гидрохлорид [rINNM (ru)]
Molecular formula: C23H29N3O2S2,2HCl,2H2O =552.6
CAS: 58513-59-0 (anhydrous tiotixene hydrochloride); 49746-04-5 (anhydrous tiotixene hydrochloride, Z-isomer); 22189-31-7 (tiotixene hydrochloride dihydrate); 49746-09-0 (tiotixene hydrochloride dihydrate, Z-isomer)
ATC code: N05AF04
Tiotixene

Pharmacopoeias. In US, which permits both the dihydrate and the anhydrous form.

The United States Pharmacopeia 31, 2008 (Thiothixene Hydrochloride). It is anhydrous (C23H29N3O2S2,2HCl = 516.5) or contains two molecules of water of hydration. A white or practically white crystalline powder having a slight odour. Soluble 1 in 8 of water, 1 in 270 of dehydrated alcohol, and 1 in 280 of chloroform practically insoluble in acetone, in ether, and in benzene. Store in airtight containers. Protect from light.

Stability. A combination of the stabilisers hydroxyquinoline sulfate and vanillin could protect tiotixene from photodegradation.

Adverse Effects, Treatment, and Precautions

As for Chlorpromazine. Tiotixene is less likely to cause sedation but extrapyramidal effects are more frequent.

Interactions

As for Chlorpromazine.

Pharmacokinetics

In 15 adequately controlled schizophrenic patients receiving oral tiotixene 15 to 60 mg daily in 2, 3, or 4 divided doses, plasma concentrations were found to be in the relatively narrow range of 10 to 22.5 nanograms/mL 126 to 150 minutes after the last daily dose despite the fourfold difference in dosage. Investigations in a further 5 patients indicated that peak plasma concentrations were obtained about 1 to 3 hours after a dose, indicating rapid absorption with an absorption half-time of about 30 minutes. There was an early plasma half-life of about 210 minutes and a late half-life of about 34 hours resurgence of drug concentrations in some subjects might have been due to enterohepatic recycling.

Metabolism. There has been a study indicating that tiotixene may induce its own metabolism.

Uses and Administration

Tiotixene is a thioxanthene antipsychotic with general properties similar to those of the phenothiazine, chlorpromazine. It has a piperazine side-chain. It is used in the treatment of psychoses including schizophrenia. Tiotixene is given orally as the base or hydrochloride and by intramuscular injection as the hydrochloride. Doses are expressed in terms of the base. Tiotixene 1 mg is equivalent to about 1.2 mg of tiotixene hydrochloride.

The usual initial oral dose is 2 mg three times daily (or 5 mg twice daily in more severe conditions) gradually increasing to 20 to 30 mg daily if necessary once-daily dosage may be adequate. In severe or resistant psychoses doses of up to 60 mg daily may be given. The usual initial intramuscular dose is 4 mg two to four times daily increased if necessary to a maximum of 30 mg daily. Tiotixene should be given in reduced dosage to elderly or debilitated patients.

Preparations

The United States Pharmacopeia 31, 2008: Thiothixene Capsules; Thiothixene Hydrochloride for Injection; Thiothixene Hydrochloride Injection; Thiothixene Hydrochloride Oral Solution.

Proprietary Preparations

Australia:: Navane

Canada: Navane

Hong Kong: Navane

The Netherlands: Navane

New Zealand: Thixit

USA: Navane.

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