Adult: Available preparation:
Flupentixol 0.5 mg and melitracen 10 mg tab
1 tab bid (morning and noon). May increase morning dose to 2 tabs in severe cases. Max: 4 tabs daily. Elderly: 1 tab once daily (morning). May increase to 1 tab bid (morning and noon) in severe cases.
Contraindications
Altered consciousness due to any cause (e.g. alcohol or drug intoxication), coma; blood disorders; recent MI, atrioventricular block (any degree), cardiac rhythm disorder, coronary artery disease, circulatory collapse; untreated narrow-angle glaucoma; phaeochromocytoma. Concomitant use or within 14 days of discontinuing MAOIs.
Special Precautions
Patient with urinary retention, CV disease; hyperthyroidism, diabetes; organic brain disorder, history of or at risk of seizures; glaucoma; prolactin-dependent tumours (e.g. breast cancer); hereditary disorder of galactose intolerance, congenital lactase deficiency, glucose-galactose malabsorption. Patients undergoing surgery. Severe hepatic impairment. Elderly. Pregnancy and lactation. Not recommended for use in excitable, overactive, or manic patients. Avoid abrupt withdrawal.
This drug may cause drowsiness, dizziness or blurred vision, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood glucose; suicidal ideation and unusual changes in behaviour at the beginning of therapy. Monitor for signs and symptoms of neuroleptic malignant syndrome (e.g. mental status changes, fever, muscle rigidity, and/or autonomic instability). Evaluate venous thromboembolism risk prior to and during therapy.
Overdosage
Symptoms: Anticholinergic effects (e.g. tachycardia, mydriasis, mucosal dryness, urinary retention, intestinal hypomotility), somnolence, irritability, agitation, hallucinations, convulsions, fever, depressed level of consciousness, respiratory depression, coma, cardiac symptoms (e.g. arrhythmias, cardiac failure, hypotension, cardiogenic shock), hypokalaemia, metabolic shock. Management: Symptomatic and supportive treatment. May perform gastric lavage and may give activated charcoal even at a late stage of oral ingestion; continuous ECG monitoring for 3-5 days; institute measures to support CV and respiratory system. May treat convulsions with diazepam; extrapyramidal disorder with biperiden. Admit patient to hospital.
Drug Interactions
Increased risk of arrhythmias and hypotension with anaesthetics. May diminish the antihypertensive effect of guanethidine, reserpine, clonidine, betanidine, and methyldopa. May potentiate the adverse effects of anticholinergic agents specifically the effects on the eyes, CNS, bowel and bladder (e.g. paralytic ileus, hyperpyrexia). May enhance the CNS depressant effect of barbiturates and other CNS depressants. May reduce the effect of levodopa and increase the risk of cardiac side effects.
Flupentixol: Increased risk of neurotoxicity with lithium. Enhanced QTc prolonging effect with QT prolonging agents (e.g. quinidine, sotalol, thioridazine, erythromycin, terfenadine, moxifloxacin).
Melitracen: May potentiate the CV effect of epinephrine, norepinephrine, ephedrine, isoprenaline, phenylephrine, and phenylpropanolamine (contained in local and general anaesthetics and nasal decongestants). Potentially Fatal: May cause hypertensive crises when given with MAOIs.
Melitracen: Concomitant administration with MAOIs may cause serotonin syndrome.
Food Interaction
May enhance the CNS depressant effect of alcohol.
Action
Description: Mechanism of Action: Flupentixol is a thioxanthene-derivative antipsychotic with anxiolytic and antidepressant properties which at low doses acts as an antagonist at dopamine (specifically, D1 and D2), serotonin (5-HT2), adrenaline (α-1), and histamine (H1) receptors.
Melitracen is a TCA with activating properties at low doses. It increases the synaptic concentration of serotonin and/or norepinephrine in the CNS. Pharmacokinetics: Absorption: Flupentixol: Readily absorbed from the gastrointestinal tract. Bioavailability: Approx 40%. Time to peak plasma concentration: Approx 4 hours.
Melitracen: Time to peak plasma concentration: 4 hours. Distribution: Flupentixol: Widely distributed in the body. Crosses the placenta and blood-brain barrier; enters breast milk (small amount). Volume of distribution: 14.1 L/kg. Plasma protein binding: Approx 99%. Metabolism: Flupentixol: Extensively metabolised in the liver via sulphoxidation, side chain N-dealkylation, and glucuronic acid conjugation into inactive metabolites.
Melitracen: Metabolised via demethylation and hydroxylation into litracen (active metabolite). Excretion: Flupentixol: Mainly via faeces (as metabolites); urine (small amounts). Elimination half-life: Approx 35 hours.
Melitracen: Mainly via faeces; urine. Elimination half-life: 19 hours (ranging from 12-24 hours).
Chemical Structure
Flupentixol Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5281881, Flupentixol. https://pubchem.ncbi.nlm.nih.gov/compound/cis-Flupentixol. Accessed Dec. 21, 2020.
Melitracen Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 25382, Melitracen. https://pubchem.ncbi.nlm.nih.gov/compound/Melitracen. Accessed Dec. 28, 2021.
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