1 Star2 Stars3 Stars4 Stars5 Stars (No Ratings Yet)
blankLoading...

Fluphenazine

Drug Approvals

(British Approved Name, rINN)

Synonyms: Flufenatsiini; Flufenazin; Flufenazina; Fluphenazinum
BAN: Fluphenazine
INN: Fluphenazine [rINN (en)]
INN: Flufenazina [rINN (es)]
INN: Fluphénazine [rINN (fr)]
INN: Fluphenazinum [rINN (la)]
INN: Флуфеназин [rINN (ru)]
Chemical name: 2-{4-[3-(2-Trifluoromethylphenothiazin-10-yl)propyl]piperazin-1-yl}ethanol
Molecular formula: C22H26F3N3OS =437.5
CAS: 69-23-8
ATC code: N05AB02

Drug Approvals

Synonyms: Flufenatsiinidekanoaatti; Flufenazin-dekanoát; Flufenazina, decanoato de; Flufenazindekanoat; Flufenazine-dekanoát; Flufenazino dekanoatas; Fluphenazini Decanoas
BAN: Fluphenazine Decanoate [BANM]
INN: Fluphenazine Decanoate [rINNM (en)]
INN: Decanoato de flufenazina [rINNM (es)]
INN: Fluphénazine, Décanoate de [rINNM (fr)]
INN: Fluphenazini Decanoas [rINNM (la)]
INN: Флуфеназина Деканоат [rINNM (ru)]
Molecular formula: C32H44F3N3O2S =591.8
CAS: 5002-47-1
ATC code: N05AB02
Read code: y022z

(British Approved Name Modified, rINNM)

Pharmacopoeias. In China, Europe, International, and US.

 

European Pharmacopoeia, 6th ed. (Fluphenazine Decanoate). A pale yellow viscous liquid or a yellow solid. Practically insoluble in water very soluble in dehydrated alcohol and in dichloromethane freely soluble in methyl alcohol. Protect from light.

The United States Pharmacopeia 31, 2008 (Fluphenazine Decanoate). Store in airtight containers. Protect from light.

(British Approved Name Modified, rINNM)

Drug Nomenclature

Synonyms: Flufenatsiinienantaatti; Flufenazin-enantát; Flufenazina, enantato de; Flufenazinenantat; Flufenazino enantatas; Fluphenazine Enanthate; Fluphenazine Heptanoate; Fluphenazini Enantas
BAN: Fluphenazine Enantate [BANM]
INN: Fluphenazine Enantate [rINNM (en)]
INN: Enantato de flufenazina [rINNM (es)]
INN: Fluphénazine, Enantate de [rINNM (fr)]
INN: Fluphenazini Enantas [rINNM (la)]
INN: Флуфеназина Енантат [rINNM (ru)]
Molecular formula: C29H38F3N3O2S =549.7
CAS: 2746-81-8
ATC code: N05AB02
Read code: y00Fx

INNs in main languages (French, Latin, Russian, and Spanish):

Pharmacopoeias. In Europe, International, Japan, and US.

Fluphenazine125mg

European Pharmacopoeia, 6th ed. (Fluphenazine Enantate). A pale yellow viscous liquid or a yellow solid. Practically insoluble in water very soluble in dehydrated alcohol and in dichloromethane freely soluble in methyl alcohol. Protect from light.

The United States Pharmacopeia 31, 2008 (Fluphenazine Enanthate). A pale yellow to yellow-orange, clear to slightly turbid, viscous liquid having a characteristic odour. Insoluble in water soluble 1 in less than 1 of alcohol and of chloroform and 1 in 2 of ether. Stable in air at room temperature but unstable in strong light. Store in airtight containers. Protect from light.

Drug Approvals

(British Approved Name Modified, rINNM)

Synonyms: Flufenatsiinihydrokloridi; Flufenazin-dihydrochlorid; Flufenazin-hidroklorid; Flufenazina, hidrocloruro de; Flufenazinhydroklorid; Flufenazino hidrochloridas; Fluphenazine Dihydrochloride; Fluphenazini Dihydrochloridum; Fluphenazini Hydrochloridum
BAN: Fluphenazine Hydrochloride [BANM]
INN: Fluphenazine Hydrochloride [rINNM (en)]
INN: Hidrocloruro de flufenazina [rINNM (es)]
INN: Fluphénazine, Chlorhydrate de [rINNM (fr)]
INN: Fluphenazini Hydrochloridum [rINNM (la)]
INN: Флуфеназина Гидрохлорид [rINNM (ru)]
Molecular formula: C22H26F3N3OS,2HCl =510.4
CAS: 146-56-5
ATC code: N05AB02
Read code: y00Fb

Pharmacopoeias. In China, Europe, International, and US.

 

European Pharmacopoeia, 6th ed. (Fluphenazine Dihydrochloride). A white or almost white, crystalline powder. Freely soluble in water slightly soluble in alcohol and in dichloromethane. A 5% solution in water has a pH of 1.9 to 2.4. Protect from light.

The United States Pharmacopeia 31, 2008 (Fluphenazine Hydrochloride). A white or nearly white, odourless crystalline powder. Soluble 1 in 1.4 of water and 1 in 6.7 of alcohol slightly soluble in acetone and in chloroform practically insoluble in ether and in benzene. Store in airtight containers. Protect from light.

Adverse Effects and Treatment

As for Chlorpromazine. Fluphenazine is less likely to cause sedation, hypotension, or antimuscarinic effects but is associated with a higher incidence of extrapyramidal effects.

Convulsions. For mention of fluphenazine as one of the antipsychotics suitable for patients at risk of seizures.

Effects on the liver. A patient developed jaundice 17 days after the first of 3 injections of a depot antipsychotic containing fluphenazine decanoate given over a 2-week period. The patient developed indicators of severe liver toxicity, with extreme hyper-bilirubinaemia and raised liver enzyme values, and remained very ill for the next 4 months. The patient showed cross-sensitivity to haloperidol but not to flupentixol. See also under Chlorpromazine.

Overdosage. A patient who took about 30 fluphenazine hydrochloride 2.5-mg tablets was treated with gastric lavage. Twenty hours after hospital admission he had difficulty in breathing due to spasm of the respiratory muscles other very severe extrapyramidal adverse effects were also present. Muscle spasm was controlled by diazepam.

There were few adverse effects in a patient given intramuscular fluphenazine decanoate 50 mg every 4 hours, instead of the intended 4 weeks, to a total of 1050 mg. About 3 weeks after the period of overdosage the patient had some degree of hypothermia and tachycardia, and after a further week parkinsonian signs appeared. No specific treatment was given.

Precautions

As for Chlorpromazine. Fluphenazine may exacerbate depression and therefore it is contra-indicated in severely depressed patients.

Pregnancy. A neonate delivered to a mother who had received fluphenazine hydrochloride 10 to 20 mg daily throughout pregnancy had nasal congestion with severe rhinorrhoea, respiratory distress, vomiting, and extrapyramidal symptoms. Respiratory symptoms appeared to respond to pseudoephedrine.

Interactions

As for Chlorpromazine.

Pharmacokinetics

Fluphenazine hydrochloride is absorbed after oral doses, and has a reported plasma half-life of 14.7 hours after oral doses. Fluphenazine decanoate and fluphenazine enantate are very slowly absorbed from the site of subcutaneous or intramuscular injection. They both gradually release fluphenazine into the body and are therefore suitable for use as depot injections. The plasma half-life of fluphenazine decanoate has been reported to be 6 to 9 days after intramuscular injection.

References to the pharmacokinetics of fluphenazine. The plasma half-life of fluphenazine after a single dose was 14.7 hours in 1 patient given the hydrochloride orally and 14.9 and 15.3 hours in 2 patients given the hydrochloride by intramuscular injection. The half-life was 3.6 and 3.7 days in 2 patients given the enantate intramuscularly and 9.6 and 6.8 days in 2 patients given the decanoate intramuscularly. Peak plasma-fluphenazine concentrations occurred earlier in patients given fluphenazine decanoate compared with those who received the enantate. Fluphenazine sulfoxide and 7-hydroxyfluphenazine were identified in the urine and faeces.

Uses and Administration

Fluphenazine is a phenothiazine with general properties similar to those of chlorpromazine. It has a piperazine side-chain. Fluphenazine is used in the treatment of psychiatric disorders including schizophrenia, mania (see Bipolar Disorder, severe anxiety, and behavioural disturbances. Fluphenazine is given as the hydrochloride by mouth or sometimes by intramuscular injection for both routes, doses are expressed in terms of fluphenazine hydrochloride. The longer-acting decanoate or enantate esters of fluphenazine are given by intramuscular or sometimes subcutaneous injection for both esters, doses are expressed in terms of the ester.

The usual initial oral dose of the hydrochloride for the treatment of schizophrenia, mania, and other psychoses is 2.5 to 10 mg daily in two or three divided doses the dose is then increased according to response up to a usual maximum of 20 mg daily, although higher doses have occasionally been given. Dosage may subsequently be reduced to a usual maintenance dose of 1 to 5 mg daily. A lower initial dose of 1 to 2.5 mg daily, increased according to response up to a maximum of 10 mg daily, is recommended in the elderly. Treatment is sometimes started with an initial intramuscular injection of 1.25 mg of the hydrochloride adjusted thereafter according to response. The usual initial intramuscular daily dose is 2.5 to 10 mg given in divided doses every 6 to 8 hours. In general the required parenteral doses of fluphenazine hydrochloride have been found to be about one-third to one-half of those given orally. When symptoms are controlled, oral maintenance therapy may be substituted.

The long-acting decanoate or enantate esters of fluphenazine are usually given by deep intramuscular injection and are used mainly for the maintenance treatment of patients with schizophrenia or other chronic psychoses. The onset of action is usually within 1 to 3 days of injection and significant effects on psychosis are usually evident within 2 to 4 days. An initial dose of fluphenazine decanoate 12.5 mg (6.25 mg in the elderly) is given intramuscularly. Subsequent adjustments in the amounts and the dosage interval should be made according to the patient’s response the amounts required may range from 12.5 to 100 mg and the intervals required may range from 2 weeks to 5 or 6 weeks. Lower doses may be possible in some patients (see Schizophrenia, below). If doses greater than 50 mg are considered necessary, cautious increments should be made in steps of 12.5 mg. The enantate ester of fluphenazine has been given in a similar dose range at intervals of 1 to 3 weeks.

Fluphenazine hydrochloride has also been given orally in initial doses of 1 mg twice daily, increased if necessary to 2 mg twice daily, for the short-term adjunctive management of severe anxiety or behavioural disturbances.

Schizophrenia. References to fluphenazine decanoate in schizophrenia indicating that low doses (10 mg or less every 2 weeks) may be effective in some patients. Use of standard doses at greater intervals (6 weeks) has also been tried. A systematic review of the use of depot fluphenazine in schizophrenia found little advantage over oral use in terms of compliance. Another systematic review considered that although oral fluphenazine is inexpensive and widely available, other drugs may be preferable because of its adverse effects.

Tourette’s syndrome. Fluphenazine has been tried as an alternative to standard dopamine antagonists such as haloperidol or pimozide in the symptomatic management of Tourette’s syndrome.

Preparations

British Pharmacopoeia 2008: Fluphenazine Decanoate Injection; Fluphenazine Tablets

The United States Pharmacopeia 31, 2008: Fluphenazine Decanoate Injection; Fluphenazine Enanthate Injection; Fluphenazine Hydrochloride Elixir; Fluphenazine Hydrochloride Injection; Fluphenazine Hydrochloride Oral Solution; Fluphenazine Hydrochloride Tablets.

Proprietary Preparations

 

Australia: Anatensolf Modecate

Austria: Dapotum

Belgium: Sevinol

Brazil: Flufenan

Canada: Modecate Moditen

Chile: Modecate

Czech Republic: Moditen

Denmark: Padnol Siqualone

Finland: Padnol Siqualone

France: Modecate Moditen

Germany: Dapotum Lyogen Lyorodin Omca

Hong Kong: Modecate

Hungary: Moditen

India: Anatensol Fludecan

Indonesia: Anatensol Modecate

Ireland: Modecate

Israel: Fludecate

Italy: Anatensol Moditen

Malaysia: Deca

Mexico: Siqualine

The Netherlands: Anatensol Moditen

Norway: Siqualone

New Zealand: Anatensol Modecate

Philippines: Modezine Shrizine Sydepres

Portugal: Anatensol Cenilene Phenazin

Russia: Moditen

South Africa: Fludecate Modecate

Singapore: Modecate

Spain: Modecate

Sweden: Padnol Siqualone

Switzerland: Dapotum

Thailand: Deca Fluzine Pharnazine Phenazine Potensone

Turkey: Prolixin

United Kingdom: Modecate Moditen

USA: Prolixin

Venezuela: Moditen

 

Multi-ingredient

 

Brazil: Diserim

Chile: Motitrel

Indonesia: Motival

Ireland: Motival

Italy: Dominans

Mexico: Motival

South Africa: Motival

Thailand: Cetavol

United Kingdom: Motival

Leave a Reply

  Subscribe  
Notify of