Usage
Flupenthixol + Melitracen is prescribed for various types of depression, including:
- Psychogenic depression
- Depressive neurosis
- Masked depression
- Psychosomatic affections accompanied by anxiety and apathy
- Menopausal depression
- Depression in alcoholics and drug addicts
It is also used in the maintenance treatment of psychogenic depressions and other psychoses and is helpful in managing anxiety disorders.
Pharmacological Classification: This combination drug falls under the category of atypical antipsychotics combined with tricyclic antidepressants (TCAs).
Mechanism of Action: Flupenthixol, the antipsychotic component, primarily acts as a dopamine receptor antagonist, blocking D1 and D2 receptors in the brain, particularly in the mesolimbic system. This action helps manage psychotic symptoms and stabilize mood. Melitracen, the tricyclic antidepressant component, inhibits the reuptake of serotonin and norepinephrine, thereby increasing their levels in the synaptic cleft and improving mood and alleviating depressive symptoms.
Alternate Names
Flupenthixol + Melitracen is also known as Flupentixol + Melitracen. It is marketed under various brand names, including Deanxit and others, differing based on region and manufacturer.
How It Works
Pharmacodynamics: Flupenthixol, by blocking dopamine receptors, particularly in the mesolimbic pathway, reduces psychotic symptoms like delusions and hallucinations. Its anxiolytic effect is attributed to its impact on dopamine and serotonin receptors. Melitracen, by inhibiting serotonin and norepinephrine reuptake, increases their concentration in the synaptic cleft, thus improving mood, reducing anxiety, and promoting emotional well-being.
Pharmacokinetics:
- Absorption: Both components are well-absorbed orally. Maximum serum concentration is reached in about 4 hours after oral administration.
- Metabolism: Flupenthixol undergoes extensive hepatic metabolism via sulphoxidation, side-chain N-dealkylation, and glucuronic acid conjugation. Melitracen is metabolized via demethylation and hydroxylation, forming an active metabolite called litracen.
- Elimination: Flupenthixol is primarily eliminated in the faeces, with a small amount in urine. Its elimination half-life is around 35 hours. Melitracen is mainly eliminated via faeces and has an elimination half-life of about 19 hours.
Mode of Action: Flupenthixol binds to and blocks dopamine D1 and D2 receptors. Melitracen inhibits the presynaptic reuptake of serotonin and norepinephrine.
Elimination Pathways: Primarily hepatic for both drugs. Flupenthixol is mainly excreted in faeces as metabolites, while Melitracen is excreted via both faeces and urine.
Dosage
Standard Dosage
Adults:
The standard dose is one tablet twice daily (morning and noon). In severe cases, the morning dose may be increased to two tablets. The maximum daily dose is four tablets.
Children:
This combination is not recommended for use in children under 18 years of age.
Special Cases:
- Elderly Patients: Start with one tablet in the morning. Increase to one tablet twice daily in severe cases.
- Patients with Renal Impairment: Dose adjustments may be necessary, but specific guidelines are limited. Monitor renal function and adjust based on clinical response and tolerability.
- Patients with Hepatic Dysfunction: Dose adjustments may be necessary. Initiate with a lower dose and monitor liver function tests.
- Patients with Comorbid Conditions: Carefully consider the potential for drug interactions with other medications the patient might be taking. Caution is advised in patients with cardiovascular disease, diabetes, or other relevant comorbidities.
Clinical Use Cases
Dosage adjustments for intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations are not specifically defined for this combination. Dosage should be adjusted based on the individual patient’s needs and clinical condition.
Dosage Adjustments
Dosage modifications are required for elderly patients and those with hepatic or renal impairment. Start with a lower dose and titrate according to clinical response and tolerability.
Side Effects
Common Side Effects:
- Dry mouth
- Constipation
- Dizziness
- Tremor
- Insomnia
- Fatigue
- Restlessness
- Agitation
- Blurred vision
Rare but Serious Side Effects:
- Extrapyramidal symptoms (e.g., tardive dyskinesia, akathisia, dystonia)
- Neuroleptic malignant syndrome
- QT prolongation
- Venous thromboembolism
- Suicidal ideation
- Hypomania
Long-Term Effects:
Tardive dyskinesia is a potential long-term side effect associated with Flupenthixol. Regular monitoring is crucial for early detection.
Adverse Drug Reactions (ADR):
Any signs of neuroleptic malignant syndrome (NMS) (e.g., high fever, muscle rigidity, altered mental status), severe extrapyramidal symptoms, cardiac arrhythmias, or suicidal thoughts require immediate medical intervention.
Contraindications
- Hypersensitivity to either Flupenthixol or Melitracen
- Recent myocardial infarction
- Atrioventricular block (any degree)
- Cardiac rhythm disorders
- Coronary artery disease
- Circulatory collapse
- Untreated narrow-angle glaucoma
- Phaeochromocytoma
- Concomitant use or within 14 days of discontinuing MAOIs
- Coma
Drug Interactions
Flupenthixol + Melitracen may interact with:
- Alcohol (increases sedative effects)
- MAOIs (risk of serotonin syndrome)
- CNS depressants (additive sedative effects)
- Anticholinergic drugs (additive anticholinergic effects)
- Guanethidine and similar antihypertensives (reduced antihypertensive effect)
- Epinephrine, norepinephrine, and other sympathomimetics (potentiated cardiovascular effects)
- Levodopa (reduced efficacy of Levodopa)
- QT prolonging agents (increased risk of QT prolongation)
Pregnancy and Breastfeeding
Flupenthixol + Melitracen is generally not recommended during pregnancy and breastfeeding. If the benefits outweigh the risks, close monitoring of both the mother and the infant is required. Flupentixol is excreted in small amounts in breast milk.
Drug Profile Summary
- Mechanism of Action: Flupenthixol: Dopamine receptor antagonist; Melitracen: Serotonin and norepinephrine reuptake inhibitor.
- Side Effects: Dry mouth, constipation, dizziness, tremor, insomnia, extrapyramidal symptoms, NMS, QT prolongation.
- Contraindications: Hypersensitivity, recent MI, heart block, glaucoma, phaeochromocytoma, concomitant MAOI use.
- Drug Interactions: Alcohol, MAOIs, CNS depressants, anticholinergics, guanethidine, sympathomimetics.
- Pregnancy & Breastfeeding: Not generally recommended.
- Dosage: Adults: 1 tablet BID, max 4/day. Elderly: 1 tablet daily, max 2/day.
- Monitoring Parameters: Liver function tests, ECG, monitor for extrapyramidal symptoms and NMS.
Popular Combinations
There are no widely established “popular combinations” for Flupenthixol + Melitracen as it is already a combination product. Other medications might be added to address specific symptoms or comorbidities based on individual patient needs, always considering potential interactions.
Precautions
- General Precautions: Screen patients for pre-existing medical conditions, allergies, and concomitant medications.
- Specific Populations: Not recommended during pregnancy and breastfeeding unless absolutely necessary and the benefits clearly outweigh the risks. Use with caution in the elderly. Not recommended for children.
- Lifestyle Considerations: Avoid alcohol. Caution when driving or operating machinery due to potential drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Flupenthixol + Melitracen?
A: Adults: One tablet twice daily, morning and noon. This can be increased to a maximum of four tablets per day in severe cases. Elderly patients: One tablet daily, increasing to two tablets in severe cases, if needed.
Q2: What are the common side effects?
A: Common side effects include dry mouth, constipation, dizziness, tremor, insomnia, fatigue, restlessness, agitation, and blurred vision.
Q3: What are the serious side effects I should watch out for?
A: Serious side effects include extrapyramidal symptoms, neuroleptic malignant syndrome, QT prolongation, venous thromboembolism, and suicidal ideation.
Q4: Can this medication be used during pregnancy or breastfeeding?
A: It is generally not recommended. The potential risks and benefits should be carefully evaluated.
Q5: What are the contraindications to using Flupenthixol + Melitracen?
A: Contraindications include hypersensitivity to either drug, recent myocardial infarction, heart block, glaucoma, phaeochromocytoma, and concomitant use of MAOIs.
Q6: How does this combination drug work?
A: Flupenthixol blocks dopamine receptors, and Melitracen inhibits serotonin and norepinephrine reuptake, working together to improve mood and reduce anxiety and psychotic symptoms.
Q7: What should I do if a patient experiences side effects?
A: Mild side effects might resolve on their own. If side effects are persistent or severe, dosage adjustment or discontinuation might be necessary. Contact a psychiatrist or relevant specialist immediately if severe side effects like NMS appear.
Q8: Are there any specific monitoring parameters for this drug?
A: Monitoring parameters might include liver function tests, ECG, and vigilance for extrapyramidal symptoms and neuroleptic malignant syndrome. Regular psychiatric evaluations are also essential.
Q9: What is the role of Flupenthixol in this combination?
A: Flupenthixol, as an antipsychotic, manages psychotic symptoms and provides anxiolytic effects.
Q10: What is the role of Melitracen in this combination?
A: Melitracen, as an antidepressant, elevates mood and reduces the symptoms of depression.
