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Trifluoperazine Hydrochloride

 

Drug Nomenclature

Synonyms: Trifluoperazin hydrochlorid; Trifluoperazina, hidrocloruro de; Trifluoperazinhidroklorid; Trifluoperazinhydroklorid; Trifluoperazini Hydrochloridum; Trifluoperazino hidrochloridas; Trifluoriperatsiinihydrokloridi; Triphthazinum
BAN: Trifluoperazine Hydrochloride [BANM]
INN: Trifluoperazine Hydrochloride [rINNM (en)]
INN: Hidrocloruro de trifluoperazina [rINNM (es)]
INN: Trifluopérazine, Chlorhydrate de [rINNM (fr)]
INN: Trifluoperazini Hydrochloridum [rINNM (la)]
INN: Трифлуоперазина Гидрохлорид [rINNM (ru)]
Chemical name: 10-[3-(4-Methylpiperazin-1-yl)propyl]-2-trifluoromethylphenothiazine dihydrochloride
Molecular formula: C21H24F3N3S,2HCl =480.4
CAS: 117-89-5 (trifluoperazine); 440-17-5 (trifluoperazine hydrochloride)
ATC code: N05AB06

Pharmacopoeias. In China, Europe, and US.

European Pharmacopoeia, 6th ed. (Trifluoperazine Hydrochloride). A white to pale yellow, hygroscopic, crystalline powder. Freely soluble in water soluble in alcohol practically insoluble in ether. A 10% solution in water has a pH of 1.6 to 2.5. Protect from light.

The United States Pharmacopeia 31, 2008 (Trifluoperazine Hydrochloride). A white to pale yellow, practically odourless, crystalline powder. Soluble 1 in 3.5 of water, 1 in 11 of alcohol, and 1 in 100 of chloroform insoluble in ether and in benzene. pHof a 1 in 20 solution is between 1.7 and 2.6. Store in airtight containers at a temperature of 25°, excursions permitted between 15° and 30°. Protect from light.

Adverse Effects, Treatment, and Precautions

As for Chlorpromazine. Trifluoperazine is less likely to cause sedation, hypotension, hypothermia, or antimuscarinic effects but is associated with a higher incidence of extrapyramidal effects particularly when the daily dose exceeds 6 mg.

Breast feeding. The American Academy of Pediatrics considers that, although the effect of trifluoperazine on breast-fed infants is unknown, its use by mothers during breast feeding may be of concern since antipsychotic drugs do appear in breast milk and thus could conceivably alter CNS function in the infant both in the short and long term.

Interactions

As for Chlorpromazine.

Trifluoperazine Hydrochloride10mg

Pharmacokinetics

Trifluoperazine hydrochloride is readily absorbed from the gastrointestinal tract after oral doses peak plasma concentrations are attained 1.5 to 6 hours after inges-tion and bioavailability is subject to interindividual variation. It is highly bound to plasma proteins. The elimination of trifluoperazine is multiphasic and the terminal half-life is about 22 hours. The major metabolite is the possibly active N-oxide. Other metabolites include the sulfoxide and the 7-hydroxy derivative. Trifluoperazine is distributed into breast milk.

Uses and Administration

Trifluoperazine is a phenothiazine antipsychotic with general properties similar to those of chlorpromazine. It has a piperazine side-chain.

Trifluoperazine is used in the treatment of a variety of psychiatric disorders including schizophrenia, severe anxiety, and disturbed behaviour. It is also used for the control of nausea and vomiting.

Trifluoperazine is given as the hydrochloride but doses are expressed in terms of the base. Trifluoperazine 1 mg is equivalent to about 1.2 mg of trifluoperazine hydrochloride. A modified-release preparation is also available in some countries. Trifluoperazine should be given in reduced dosage to elderly or debilitated patients.

The usual initial oral dose for the treatment of schizophrenia and other psychoses is 2 to 5 mg twice daily, gradually increased to a usual range of 15 to 20 mg daily in severe or resistant psychoses daily doses of 40 mg or more have been given. For the control of acute psychotic symptoms it may be given by deep intramuscular injection in a dose of 1 to 2 mg, repeated if necessary every 4 to 6 hours more than 6 mg daily is rarely required. The initial oral dose for use in children is up to 5 mg daily in divided doses adjusted according to age, body-weight, and response, or 1 mg given once or twice daily by intramuscular injection.

For the control of nausea and vomiting the usual adult oral dose is 1 or 2 mg twice daily up to 6 mg daily may be given in divided doses. Children aged 3 to 5 years may be given up to 1 mg daily in divided doses this may be increased to a maximum of 4 mg daily in children aged 6 to 12 years.

When used as an adjunct in the short-term management of severe anxiety disorders doses are similar to those used for the control of nausea and vomiting.

Schizophrenia. A systematic review of the use of trifluoperazine for schizophrenia concluded that it appeared to be of similar efficacy to other commonly used classical antipsychotics with a similar profile of adverse effects. However, there did not appear to be good evidence for claims that it was effective for schizophrenia at low doses.

Preparations

BP 2008: Trifluoperazine Tablets

The United States Pharmacopeia 31, 2008: Trifluoperazine Hydrochloride Injection; Trifluoperazine Hydrochloride Syrup; Trifluoperazine Hydrochloride Tablets.

Proprietary Preparations

Argentina: Stelazine

Australia: Stelazine

Brazil: Stelazine

Greece: Stelazine, Stelium

India: Trinicalm

Indonesia: Stelazine

Ireland: Stelazine

Italy: Modalina

Mexico: Flupazine, Stelazine

New Zealand: Stelazine

South Africa: Stelazine, Terflurazine

Spain: Eskazine

Thailand: Psyrazine, Triflumed, Triozine, Triplex

Turkey: Stilizan

United Kingdom: Stelazine

Venezuela: Leptazine Taclorpil

Multi-ingredient

Argentina: Cuait; D Cuait N; Stelapar

Brazil: Stelapar

Canada: Stelabid

India: Sycot; Trinicalm Forte; Trinicalm Plus

Italy: Parmodalin

Mexico: Stelabid

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