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Tiapride Hydrochloride

 

Drug Approvals

(British Approved Name Modified, rINNM)

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

Synonyms: FLO-1347; Tiaprid-hidroklorid; Tiaprid-hydrochlorid; Tiaprida, hidrocloruro de; Tiapridhydroklorid; Tiapridi Hydrochloridum; Tiapridihydrokloridi; Tiaprido hidrochloridas
BAN: Tiapride Hydrochloride [BANM]
INN: Tiapride Hydrochloride [rINNM (en)]
INN: Hidrocloruro de tiaprida [rINNM (es)]
INN: Tiapride, Chlorhydrate de [rINNM (fr)]
INN: Tiapridi Hydrochloridum [rINNM (la)]
INN: Тиаприда Гидрохлорид [rINNM (ru)]
Chemical name: N-(2-Diethylaminoethyl)-2-methoxy-5-methylsulphonylbenzamide hydrochloride
Molecular formula: C15H24N2O4S,HCl =364.9
CAS: 51012-32-9 (tiapride); 51012-33-0 (tiapride hydrochloride)
ATC code: N05AL03

Pharmacopoeias. In Europe.

European Pharmacopoeia, 6th ed. (Tiapride Hydrochloride). A white or almost white crystalline powder. Very soluble in water slightly soluble in dehydrated alcohol soluble in methyl alcohol. A 5% solution in water has a pH of 4.0 to 6.0.

Adverse Effects, Treatment, and Precautions

As for Chlorpromazine.

Effects on the cardiovascular system. Torsade de pointes developed after a single dose of tiapride in an elderly patient with cardiac disease, a known risk factor for such arrhythmias.

Interactions

As for Chlorpromazine.

Pharmacokinetics

Tiapride is rapidly absorbed after oral doses and peak plasma concentrations occur after 1 to 2 hours. It is excreted largely unchanged in the urine. The plasma half-life is reported to range from 3 to 4 hours. It is thought to be distributed into breast milk on the basis of animal studies.

The steady-state pharmacokinetics of tiapride have been studied in 5 elderly patients with tardive dyskinesia, and in 2 patients with Huntington’s chorea. All patients received tiapride 100 mg three times daily by mouth for 7 days. The mean peak plasma concentration of tiapride was 1.47 micrograms/mL, achieved a mean of 1.4 hours after dosing, and the mean elimination half-life was 3.8 hours. These values did not differ significantly from those previously reported in younger healthy subjects, although renal clearance was slightly lower in these patients. About half of the dose of tiapride was excreted unchanged by the kidneys a metabolite, probably N-monodesethyltiapride was detected in the urine but its identity was not confirmed.

Tiapride Hydrochloride100mg

Uses and Administration

Tiapride is a substituted benzamide with general properties similar to those of sulphide.

It is usually given as the hydrochloride in the management of behavioural disorders and to treat dyskinesias. Doses are expressed in terms of the equivalent amount of base tiapride hydrochloride 222.2 mg is equivalent to about 200 mg of tiapride. Oral doses of 200 to 400 mg daily are usually given, although higher daily doses have been used, particularly in the management of dyskinesias. Tiapride hydrochloride has also been given by intramuscular or intravenous injection.

Disturbed behaviour. For a discussion of the management of disturbed behaviour including limitations on the use of antipsychotics.

Extrapyramidal disorders. Tiapride has been tried in the treatment of antipsychotic-induced tardive dyskinesia, but, as with all antipsychotics, improvement may only be short-term.

Tiapride has also been tried in the treatment of Tourette’s syndrome.

For reference to the use of tiapride in suppressing the adverse effects of levodopa on respiration.

CHOREA. Antipsychotics have some action against choreiform movements as well as being of use to control the behavioural disturbances of Huntington’s chorea, and tiapride has been quite widely used for this purpose. For a discussion of the management of various choreas. References.

Substance dependence. An early review concluded that the role of tiapride in acute alcohol withdrawal was likely to be limited as patients at risk of severe reactions would still require adjunctive therapy for the control of hallucinations and seizures. Following detoxification, tiapride appeared to help, to some degree, to alleviate distress, improve abstinence and drinking behaviour, and facilitate reintegration within society. Interest in its use with carbamazepine continues.

Proprietary Preparations

Argentina: Etiles

Austria: Delpral

Belgium: Tiapridal

Brazil: Tiapridal

Chile: Sereprid

Czech Republic: Tiapra, Tiapridal

France: Clemental, Equilium, Tiapridal

Germany: Tiapridex

Greece: Tiapridal

Hong Kong: Tiapridal

Hungary: Tiapridal

Israel:Doparid

Italy: Italprid, Sereprile

Japan: Gramalil

The Netherlands: Betaprid, Elbaprid, Tiacob, Tiajac, Tiapridal, Tiastad, Tiazet

Poland: Tiapridal

Portugal: Normagit, Tiapridal

Russia: Tiapridal

Spain: Tiaprizal

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