Flupentixol–Melitracen is a combination of two psychoactive agents flupentixol and melitracen, a tricyclic antidepressant which has antidepressant properties.

Therapeutic Class

Combined anxiolytics & anti-depressant drugs

Pharmacology

Maximum serum concentration is reached in about 4 hours after oral administration of Flupentixol-Melitracen. The half-life of Flupentixol is about 35 hours and that of Melitracen is about 19 hours.

The combination of Flupentixol-Melitracen does not seem to influence the pharmacokinetic properties of the individual compounds.

Flupenthixolprimarily acts as a neuroleptic drug. The antipsychotic effect of Flupentixol-Melitracen is achieved by mixed blockade of dopamine D1 and D2 receptors. In the mesolimbic dopamine system of the brain, this accounts for the antipsychotic action of this drug.

Flupentixol-Melitracen has other effects on CNS. In the chemoreceptor trigger zone, the dopamine blockade accounts for the antiemetic effect of the drug.

Melitracen is a tricyclic antidepressant. It blocks the neuronal re-uptake of both serotonin and nor-epinephrine in the central nervous system, thereby minimizing the symptoms of depression.

Dosage & Administration

Adults: Usually 2 tablets daily, in morning and afternoon. In severe cases, the morning dose may be increased to 2 tablets.

Elderly patients: 1 tablet in the morning.

Maintenance dose: Usually 1 tablet in the morning or as directed by the physician.

Interaction

This preparation may enhance the response to alcohol, barbiturates and other CNS depressants. Simultaneous administration of MAO-inhibitors may cause hypertensive crisis.

Overdose

Symptoms: In case of overdosage the symptoms of intoxications by melitracen, especially of anticholinergic nature, dominate. More rarely extrapyramidal symptoms due to Flupentixol-Melitracen occur. Treatment: Symptomatic and supportive.

Gastric lavage should be carried out as soon as possible and activated charcoal may be administered. Measures aimed at supporting the respiratory and cardiovascular systems should be instituted.

Epinephrine (adrenaline) must not be used for such patients. Convulsions may be treated with diazepam and extrapyramidal symptoms with biperiden.

Contraindications

It is contraindicated in the immediate recovery phase after myocardial infarction, defects in bundle-branch conduction, untreated narrow angle glaucoma and in acute alcohol, barbiturate & opioid intoxications.

Not recommended for excitable patients since its activating effect may lead to exaggeration of these characteristics.

The immediate recovery phase after myocardial infarction. Defects in bundle-branch conduction. Untreated narrow angle glaucoma. Acute alcohol, barbiturate and opiate intoxications. Flupentixol-melitracen combination should not be given to patients who have received a MAO-inhibitor within two weeks.

Not recommended for excitable or overactive patients since its activating effect may lead to exaggeration of these characteristics.

Side Effects

In the recommended doses, side effects are rare. These could be transient restlessness and insomnia.

Drowsiness, dry mouth, constipation, vomiting, dyspepsia, diarrhoea, abdominal pain, nausea, flatulence. Extrapyramidal effects, especially in the initial phase of the treatment. Tachycardia, palpitations, prolonged QT interval, hypotension.

Thrombocytopenia, neutropenia, leukopenia, agranulocytosis. Dyspnoea, myalgia, muscle rigidity, micturition disorder, urinary retention. Increased appetite and wt. Abnormal glucose tolerance and LFTs. Insomnia, depression, nervousness, agitation, libido decreased.

Pregnancy & Lactation

The safety of this drug has not been established in pregnancy and lactation. Abnormal glucose tolerance and LFTs. Insomnia, depression, nervousness, agitation, libido decreased.

Precautions & Warnings

If previously the patient has been treated with tranquilizers with sedative effect these should be withdrawn gradually.

Unsafe in porphyria. Caution when used in patients with epilepsy; Parkinson’s disease; narrow angle glaucoma; prostatic hypertrophy; hypothyroidism; hyperthyroidism; liver disease; cardiac disease or arrhythmias; severe respiratory disease; renal failure; myasthenia gravis; phaeochromocytoma.

Patients with hypersensitivity to thioxanthenes or other antipsychotics. Close monitoring for changes in behaviour, suicidal thoughts or clinical worsening during the initial part of the treatment is recommended. May impair control of diabetes; monitor blood glucose in diabetics. Withdrawal should be gradual.

Storage Conditions

Keep in a dry place away from light and heat. Keep out of the reach of children.