Comparative Pharmacology
Head-to-head clinical analysis: ETRAFON 2 25 versus SERENTIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ETRAFON 2 25 versus SERENTIL.
ETRAFON 2-25 vs SERENTIL
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.
SERENTIL (mesoridazine) is a phenothiazine antipsychotic that blocks postsynaptic dopamine D2 receptors in the mesolimbic system, and also exhibits alpha-adrenergic blocking, anticholinergic, and antihistaminic effects. It has high affinity for D2, 5-HT2A, and alpha-1 receptors.
One tablet (2 mg perphenazine, 25 mg amitriptyline) orally three or four times daily. Maintenance: 2-4 tablets daily.
Oral: 50–100 mg 3 times daily; maximum 400 mg/day. IM: 25 mg every 4–6 hours.
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 is approximately 24-30 hours in adults. Does not correlate well with duration of antipsychotic effect due to active metabolite formation.
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 conjugated and unconjugated metabolites) and fecal (15-20%). Biliary excretion contributes to enterohepatic circulation.
Category C
Category C
Antipsychotic/Antidepressant Combination
Antipsychotic