Flupenxol

Flupentixol decanoate.

Each mL contains: Flupentixol Decanoate 20 mg.

Pharmacotherapeutic group: Neuroleptics (antipsychotics). ATC code: N05AF01.
Pharmacology: Pharmacodynamics: Flupentixol is a non-sedating antipsychotic drug of the thioxanthene group. Its primary pharmacological action is dopamine blockade. Flupentixol has a high affinity for D1 and D2 receptors. Flupentixol Injection contains the decanoic ester of flupentixol in thin vegetable oil.
Pharmacokinetics: After intramuscular injection, the ester is slowly released from the oil depot and is rapidly hydrolysed to release flupentixol. Flupentixol is widely distributed in the body and extensively metabolized in the liver. Peak circulating levels occur around 7 days after administration.

It is used in the treatment of schizophrenia and other psychoses, especially with symptoms eg, apathy, inertia, withdrawal, anxiety and energy. 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.
Flupentixol 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.

Overdosage may cause somnolence or even coma, extrapyramidal symptoms, convulsions, hypotension, shock, hyper or hypothermia. ECG changes, QT prolongation, Torsade de Pointes, cardiac arrest and ventricular arrhythmias have been reported when administered in overdose together with drugs known to affect the heart.
Treatment is symptomatic and supportive, with measures aimed at supporting the respiratory and cardiovascular systems. The following specific measures may be employed if required.
Anticholinergic antiparkinson drugs if extrapyramidal symptoms occur.
Sedation (with benzodiazepines) in the unlikely event of agitation or excitement or convulsions.
Noradrenaline in saline intravenous drip if the patient is in shock. Adrenaline must not be given.

Hypersensitivity to the active substance or to any of the excipients. Circulatory collapse, depressed level of consciousness due to any cause (e.g. intoxication with alcohol, barbiturates or opiates), coma. Not recommended for excitable or agitated patients.

Patients on long-term therapy should be monitored carefully. Flupentixol 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.

Flupentixol should not be administered during pregnancy unless the expected benefit to the patient outweighs the theoretical risk to the fetus. The newborns of mothers treated with neuroleptics in late pregnancy, or labor, may show signs of intoxication eg, lethargy, tremor and hyperexcitability and have a low Apgar score.

Significant: Extrapyramidal symptoms (e.g. akathisia, dystonia, tardive dyskinesia), QT prolongation, VTE, cerebrovascular events, anticholinergic effects (e.g. xerostomia, blurred vision, constipation, urinary retention), blood dyscrasias (e.g. agranulocytosis, neutropenia, leucopenia, thrombocytopenia), diabetic ketoacidosis, oesophageal dysmotility and aspiration, falls, orthostatic hypotension, impaired core body temperature regulation, increased prolactin levels; withdrawal symptoms. Rarely, lens opacity.
Cardiac disorders: Palpitation, tachycardia.
Eye disorders: Abnormal vision, accommodation disorder.
Gastrointestinal disorders: Nausea, vomiting, dyspepsia, diarrhoea, sialorrhoea.
General disorders and administration site conditions: Fatigue, asthenia.
Investigations: Increased weight.
Metabolism and nutrition disorders: Increased appetite.
Musculoskeletal and connective tissue disorders: Myalgia.
Nervous system disorders: Dizziness, drowsiness, headache, hyper- or hypokinesia, tremor.
Psychiatric disorders: Depression, insomnia, nervousness, agitation, disturbance in attention.
Renal and urinary disorders: Micturition disorder.
Reproductive system and breast disorders: Decreased libido.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Hyperhidrosis, pruritus.
Potentially Fatal: Suicidal thoughts or attempts, arrhythmias, neuroleptic malignant syndrome.

May potentiate the effects of other CNS depressants, barbiturates, general anaesthetics, and anticoagulants. May increase risk of QT interval prolongation with class Ia and III antiarrhythmics (e.g. quinidine, sotalol), erythromycin, moxifloxacin, cisapride, thioridazine, and thiazide diuretics. May prolong the action of neuromuscular blocking agents. May potentiate the anticholinergic effects of atropine. May increase risk of extrapyramidal effects with metoclopramide and piperazine. May enhance the hypotensive effects of hydralazine, doxazosin, and methyldopa. May reverse the antihypertensive effects of guanethidine. Increased risk of neurotoxicity with lithium and sibutramine. Efficacy of adrenergic agents, levodopa and anticonvulsants may be impaired. May inhibit the metabolism of TCAs; antagonise the effects of epinephrine and sympathomimetics. Insulin and glucose responses may be modified by flupentixol.

Store at temperatures not exceeding 30°C.

Antipsychotics

N05AF01 - flupentixol ; Belongs to the class of thioxanthene derivatives antipsychotics.

Rx