Cis (Z)-flupentixol decanoate.
Cis(Z)-flupentixol decanoate is a potent nonsedative neuroleptic of the thioxanthene group with a rapid onset of antipsychotic, alerting and anxiolytic effects. The antipsychotic effect of neuroleptics is normally related to their dopamine receptor-blocking effect, which seems to release a chain reaction as other transmitter systems are influenced as well. Its alerting effect makes it particularly useful in the treatment of psychotic patients, who are withdrawn, apathetic, anergic or depressed, or in whom neuroleptics with a marked sedative effect cause fatigue or drowsiness.
In patients who refuse to take drugs and in outpatients who are unreliable in taking oral medication on their own, it is advantageous to change to cis(Z)-flupentixol decanoate which permits continuous antipsychotic treatment and thus prevents the frequent relapses caused by failure to take oral medication.
Pharmacokinetics: Pharmacokinetic and clinical studies have shown that cis(Z)-flupentixol injections can be given with intervals of 2-4 weeks. Its maximum serum concentration is reached by the end of the 1st week after injection. After enzymatic breakdown, the active component, cis(Z)-flupentixol, is distributed, metabolized and excreted as described previously.
The serum concentration curve declines exponentially with a half-life of 17 days reflecting the rate of release from the depot.
Schizophrenia and allied psychoses, especially with symptoms eg, apathy, inertia, withdrawal, anxiety and anergy. Paraphrenia. Oligophrenic and epileptic patients with mental deviations.
Dosage should be individually adjusted according to the condition. In general, small doses should be used initially and increased to the optimal effective level as rapidly as possible based on the therapeutic response.
Schizophrenia and Allied Psychoses: Maintenance treatment of chronic schizophrenia and other chronic psychoses: 20-40 mg (1-2 mL) every 2nd-4th week.
Fluanxol Depot is administered by IM injection into the upper outer quadrant of the buttock.
Dosage and interval between injections should be adjusted according to therapeutic response.
Treatment is symptomatic and supportive. If the drug has been swallowed, gastric lavage should be carried out immediately and activated charcoal may be administered. Measures aimed at supporting the respiratory and cardiovascular systems should be instituted; epinephrine must not be used for such patients.
Extremely excitable and overactive patients. Acute barbiturate, alcohol and opiate poisoning. Like other psychotropics, Fluanxol Depot should preferably not be given during pregnancy.
Patients on long-term therapy should be monitored carefully. Fluanxol Depot should be used with caution in patients with convulsive disorders or advanced hepatic, renal or cardiovascular disease.
Effects on the Ability to Drive or Operate Machinery: The ability to drive a car or operate machinery may be affected. Therefore, caution should be exercised initially, until the individual's reaction to treatment is known. If previously the patient has been treated with neuroleptics with sedative effect, these should be withdrawn gradually.
Like other psychotropics, Fluanxol Depot should preferably not be given during pregnancy.
Extrapyramidal symptoms may occur, especially during the early phase of treatment. In most cases these side effects can be satisfactorily controlled by reduction of dosage and/or antiparkinsonian drugs. The routine prophylactic use of antiparkinsonian medication is not recommended. Tardive dyskinesias, which can be more or less persistent, may occur very occasionally in patients on long-term therapy. Antiparkinsonian drugs do not alleviate these symptoms. Reduction in dosage or discontinuation of therapy is recommended.
Psychic: Transient insomnia, especially when the patient is switched over from sedative neuroleptics. At high dosage a sedative effect may occur in the occasional patient.
Autonomic and Cardiovascular: Very rare in the therapeutic dosage range.
Liver: Transient, mild alterations in liver function tests may occur.
Fluanxol Depot may enhance the response to alcohol and the effects of barbiturates and other CNS depressants. It should not be given concomitantly with guanethidine or similarly acting compounds, since neuroleptics may block the antihypertensive effect of these compounds. Fluanxol Depot may lower the effect of adrenergic drugs and concomitant use of metoclopramide and piperazine increases the risk of extrapyramidal symptoms.
N05AF01 - flupentixol ; Belongs to the class of thioxanthene derivatives antipsychotics.
Depot inj (amp) 20 mg/mL x 1 mL x 10's, 2 mL x 10's.