Amitriptyline/perphenazine (Duo-Vil, Etrafon, Triavil, Triptafen) is a formulation that contains the tricyclic antidepressant amitriptyline and the medium-potency typical (first-generation) antipsychotic, perphenazine. In the United States amitriptyline/perphenazine is marketed by Mylan Pharmaceuticals Inc. and Remedy Repack Inc.[1][2]
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Amitriptyline | Tricyclic antidepressant |
Perphenazine | Typical antipsychotic |
Clinical data | |
Trade names | Duo-Vil, Etrafon, Triavil, Triptafen |
AHFS/Drugs.com | Consumer Drug Information |
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Routes of administration | Oral |
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In the United States amitriptyline/perphenazine is indicated for the treatment of patients with:[1][2][3]
Binding affinities (Ki [nM]; for human cloned receptors when available)[5][6][7]
Molecular target | Amitriptyline | Nortriptyline (Amitriptyline's active metabolite) | Perphenazine | Notes |
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SERT | 3.13 | 16.5 | ? | It is this and its NET-inhibiting action is believed to give amitriptyline its antidepressant action. |
NET | 22.4 | 4.37 | ? | See above. |
DAT | 5380 | 3100 | ? | |
5-HT1A | 450 | 294 | 421 | Binding for human brain receptors had to be substituted in amitriptyline (AMI) and nortriptyline's (NOR) cases |
5-HT2A | 4.3 | 5 | 5.6 | Binding for cloned rat receptors had to be substituted for AMI & NOR. Binding to this receptor is believed to be what gives the newer (atypical) antipsychotics, clozapine, quetiapine, olanzapine, ziprasidone, risperidone, sertindole and zotepine their lower extrapyramidal side effect (EPS) liability. |
5-HT2C | 6.15 | 8.5 | 132 | (Binding) As above. This action is believed to be partly responsible for the lower EPS liability of newer antipsychotics and also responsible for their higher weight gain liability compared to most typical antipsychotics. |
5-HT6 | 103 | 148 | 17 | Cloned rat receptor was substituted for NOR's binding. |
5-HT7 | 114 | ? | 23 | Cloned rat receptor was substituted for AMI. |
α1A | 24 | 55 | 10 | Human brain receptors were substituted for AMI and NOR. |
α2A | 690 | 2030 | 810.5 | As above. |
D2 | 1460 | 2570 | 0.16 | As above. |
D3 | 206 | ? | 0.13 | Human receptors (their source was undefined) had to be substituted for AMI. |
H1 | 1.1 | 15.1 | 8 | This receptor is at least partly responsible for the sedating effects of these three drugs and hence this combination product. Possibly also partly responsible for their weight gain liability. |
M1 | 12.9 | 40 | 1500 | This is the main receptor responsible for the anticholinergic side effects mentioned above. |
M3 | 25.9 | 50 | 1848 | This receptor is believed to be partly responsible for the metabolic adverse effects of the atypical antipsychotics. |
σ | 300 | 2000 | 31.5 | All three values are for binding to the guinea pig brain receptors. |