Comparative Pharmacology
Head-to-head clinical analysis: ETRAFON 2 25 versus MELLARIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ETRAFON 2 25 versus MELLARIL.
ETRAFON 2-25 vs MELLARIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Combination of perphenazine (a typical antipsychotic) and amitriptyline (a tricyclic antidepressant). Perphenazine blocks postsynaptic dopamine D2 receptors in the mesolimbic system, also antagonizes alpha-adrenergic, histaminergic, and muscarinic receptors. Amitriptyline inhibits reuptake of serotonin and norepinephrine at the presynaptic neuronal membrane, enhancing serotonergic and noradrenergic neurotransmission.
Thioridazine is a phenothiazine antipsychotic that blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors, and also blocks alpha-adrenergic receptors, histamine H1 receptors, and muscarinic M1 receptors.
One tablet (2 mg perphenazine, 25 mg amitriptyline) orally three or four times daily. Maintenance: 2-4 tablets daily.
Typical adult dose: 10-25 mg orally 3 times daily. Maximum dose: 200 mg/day.
None Documented
None Documented
Perphenazine: 8-12 hours (terminal); amitriptyline: 15-24 hours (terminal), with nortriptyline active metabolite half-life 18-44 hours. Steady-state achieved in 4-7 days.
Terminal elimination half-life 21-24 hours; steady-state achieved within 5-7 days
Renal: approximately 25-50% as metabolites and unchanged drug; biliary/fecal: 10-25% as metabolites; the remainder is extensively metabolized via hepatic pathways.
Primarily renal (70-80% as metabolites, <1% unchanged); biliary/fecal (20-30%)
Category C
Category C
Antipsychotic/Antidepressant Combination
Antipsychotic