Usage
- Melitracen is primarily prescribed for the treatment of depression and anxiety. It is classified as a tricyclic antidepressant (TCA).
- Pharmacological Classification: Tricyclic Antidepressant (TCA)
- Mechanism of Action: Melitracen increases the levels of norepinephrine and serotonin, two neurotransmitters crucial for mood regulation, in the brain by inhibiting their reuptake at nerve synapses. This leads to elevated concentrations of these neurotransmitters, alleviating symptoms of depression and anxiety.
Alternate Names
- Melitracen hydrochloride is sometimes used to refer to the salt form of the drug used in formulations.
- While Melitracen itself is a generic name, it is often marketed in combination with Flupentixol under brand names like Deanxit and Melixol. Other brand names may exist regionally.
How It Works
- Pharmacodynamics: Melitracen primarily exerts its antidepressant effect by inhibiting the reuptake of serotonin and norepinephrine at presynaptic nerve terminals. This action leads to increased concentrations of these neurotransmitters in the synaptic cleft, potentiating their effects on postsynaptic receptors. It also exhibits some anticholinergic and antihistaminic properties, which contribute to some of its side effects.
- Pharmacokinetics: Melitracen is well-absorbed orally. Peak plasma concentrations are reached within approximately 4 hours. It undergoes extensive hepatic metabolism, primarily by CYP450 enzymes, and is subsequently excreted mainly through the kidneys. The half-life of Melitracen is approximately 19 hours, while the half-life of Flupentixol (when used in combination) is about 35 hours.
- Mode of Action: Melitracen blocks the reuptake pumps for serotonin and norepinephrine, located on the presynaptic neuronal membrane. This blockage prevents the removal of these neurotransmitters from the synapse, allowing them to interact with their receptors for a longer duration and increased effect.
- Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Melitracen primarily inhibits the reuptake of serotonin and norepinephrine. It may also have some affinity for histamine and muscarinic acetylcholine receptors, contributing to its side-effect profile.
- Elimination Pathways: Melitracen is metabolized in the liver via CYP450 enzymes and primarily eliminated renally.
Dosage
Standard Dosage
Adults:
- Melitracen Hydrochloride: 25 mg two to three times daily. The dose can be gradually increased to a maximum of 225 mg daily if needed.
- Flupentixol + Melitracen combination: One tablet (containing 0.5 mg Flupentixol and 10 mg Melitracen) twice daily, in the morning and at noon. In severe cases, the morning dose may be increased to two tablets. The maximum daily dose is four tablets.
Children:
- Melitracen is generally not recommended for use in children and adolescents under 18 due to a lack of data on safety and efficacy.
Special Cases:
- Elderly Patients: Initiate treatment with a reduced dose of 25-30 mg daily for Melitracen Hydrochloride or one tablet of the combination product once daily in the morning.
- Patients with Renal Impairment: Dosage adjustment may be necessary. Specific guidelines based on eGFR are lacking in the provided sources. Clinical judgment and close monitoring are advised.
- Patients with Hepatic Dysfunction: Caution should be exercised, and dosage adjustment may be required. Specific recommendations are absent in the provided sources, so clinical monitoring is crucial.
- Patients with Comorbid Conditions: Exercise caution in patients with cardiovascular disease, diabetes, glaucoma, urinary retention, and a history of seizures. Adjust dosage as needed.
Clinical Use Cases
The provided sources primarily focus on Melitracen’s use in depression and anxiety. There is no information on its use in intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. It is not indicated for such settings.
Dosage Adjustments
Dose adjustments are based on patient response, tolerability, and renal or hepatic function. Gradual dose reduction is recommended when discontinuing Melitracen to minimize withdrawal symptoms.
Side Effects
Common Side Effects:
- Dry mouth
- Constipation
- Blurred vision
- Drowsiness/fatigue
- Dizziness
- Tremor
- Insomnia
- Restlessness/agitation
- Headache
Rare but Serious Side Effects:
- Neuroleptic malignant syndrome (when used with Flupentixol)
- Seizures
- Cardiac arrhythmias (including QT prolongation)
- Suicidal thoughts or behavior
- Extrapyramidal symptoms (e.g., tardive dyskinesia, akathisia)
Long-Term Effects:
- Tardive dyskinesia (with prolonged Flupentixol combination use)
Adverse Drug Reactions (ADR):
- Serotonin syndrome (especially with concurrent MAOI use)
- Allergic reactions
- Severe hypotension
- Cardiogenic shock
Contraindications
- Hypersensitivity to Melitracen or any component of the formulation
- Recent myocardial infarction
- Any degree of atrioventricular block or cardiac rhythm disorders
- Untreated narrow-angle glaucoma
- Concomitant use or within 14 days of discontinuing MAOIs
- Coma
- Blood disorders
Drug Interactions
- MAOIs: Risk of serotonin syndrome and hypertensive crisis
- Alcohol, barbiturates, and other CNS depressants: Increased CNS depression
- Anticholinergic agents: Enhanced anticholinergic effects
- Adrenergic neuron blockers (e.g., guanethidine): Reduced antihypertensive effects
- Epinephrine and norepinephrine: Potentiates cardiovascular effects
- Levodopa: Reduced efficacy and increased cardiac side effects
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Not well-established. Use only if potential benefits outweigh the risks. Risk of neonatal withdrawal symptoms if used near term.
- Breastfeeding: Melitracen is excreted in breast milk. Use with caution, considering potential effects on the neonate.
Drug Profile Summary
- Mechanism of Action: Inhibits reuptake of serotonin and norepinephrine
- Side Effects: Dry mouth, constipation, blurred vision, drowsiness, dizziness, tremor, insomnia. Serious side effects include cardiac arrhythmias and serotonin syndrome.
- Contraindications: Hypersensitivity, recent MI, heart block, glaucoma, concurrent MAOI use.
- Drug Interactions: MAOIs, CNS depressants, anticholinergics, adrenergic blockers.
- Pregnancy & Breastfeeding: Use with caution; potential for fetal/neonatal effects.
- Dosage: Adults: 25 mg bid-tid up to 225 mg/day. Elderly: start with lower doses. Combination with flupentixol: 1 tablet bid, adjustable.
- Monitoring Parameters: Cardiac function, mental status, blood pressure, blood glucose (in diabetics).
Popular Combinations
- Flupentixol + Melitracen: This combination is used to treat depression with anxiety, apathy, or asthenia. Flupentixol is an antipsychotic that complements the antidepressant action of Melitracen.
Precautions
- General Precautions: Screen for pre-existing medical conditions like cardiovascular disease, glaucoma, diabetes, and seizure disorders.
- Specific Populations: Use with caution in pregnant or breastfeeding women, children, and the elderly.
- Lifestyle Considerations: Advise patients to avoid alcohol during Melitracen treatment due to increased CNS depression. Caution against driving or operating machinery until the effects of the medication are known.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Melitracen?
A: For adults, the usual starting dose is 25 mg two to three times daily. The dose can be gradually increased to a maximum of 225 mg per day. Elderly patients should start with a lower dose, usually 25-30 mg daily.
Q2: What conditions does Melitracen treat?
A: Melitracen is primarily used to treat depression and anxiety.
Q3: How does Melitracen work?
A: Melitracen blocks the reuptake of serotonin and norepinephrine, increasing their levels in the brain.
Q4: What are the common side effects of Melitracen?
A: Common side effects include dry mouth, constipation, blurred vision, drowsiness, dizziness, tremor, insomnia, and changes in appetite.
Q5: What are the serious side effects of Melitracen?
A: Serious side effects include cardiac arrhythmias, seizures, serotonin syndrome, and suicidal thoughts or behavior. Seek immediate medical attention if these occur.
Q6: Can Melitracen be used during pregnancy or breastfeeding?
A: Melitracen should be used with caution during pregnancy and breastfeeding. Discuss the potential risks and benefits with your doctor.
Q7: Does Melitracen interact with other medications?
A: Yes, Melitracen can interact with other medications, such as MAOIs, CNS depressants, and certain antihypertensives. Provide a complete medication list to your physician.
Q8: What should patients avoid while taking Melitracen?
A: Patients should avoid alcohol and activities requiring alertness until the drug’s effects are known. They should also inform their doctor about all other medications and supplements they are taking.
Q9: Are there any contraindications for Melitracen?
A: Yes, contraindications include hypersensitivity, recent myocardial infarction, certain heart conditions, untreated narrow-angle glaucoma, and concurrent MAOI use.
Q10: How long does it take for Melitracen to work?
A: It may take several weeks for Melitracen to reach its full therapeutic effect.
