Amitriptyline/perphenazine

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Amitriptyline/perphenazine
Amitriptyline.svg
Perphenazine2DACS.svg
Combination of
Amitriptyline Tricyclic antidepressant
Perphenazine Typical antipsychotic
Clinical data
Trade names Duo-Vil, Etrafon, Triavil, Triptafen
AHFS/Drugs.com Consumer Drug Information
License data
Routes of
administration
Oral
Legal status
Legal status
Identifiers
CAS Number
KEGG

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]

Contents

Medical uses

In the United States amitriptyline/perphenazine is indicated for the treatment of patients with: [1] [2] [3]

Adverse effects

Common (>1% incidence) adverse effects include
[1] [2] [4]
  • Blurred vision
  • Constipation
  • Dry mouth
  • Nasal congestion
Unknown frequency adverse effects include
[1] [2] [4]
Uncommon/Rare adverse effects include
[1] [2] [4]
  • Muscle rigidity
  • Tremors
  • Mental status change (e.g., hallucinations, agitation, stupor, confusion, etc.)
  • Hyperthermia
  • Autonomic instability (e.g., tachycardia, high blood pressure, diaphoresis, diarrhoea, etc.)

Pharmacology

Binding affinities (Ki [nM]; for human cloned receptors when available) [5] [6] [7]

Molecular targetAmitriptyline Nortriptyline (Amitriptyline's active metabolite)PerphenazineNotes
SERT 3.1316.5 ?It is this and its NET-inhibiting action is believed to give amitriptyline its antidepressant action.
NET 22.44.37 ?See above.
DAT 53803100 ?
5-HT1A 450294421Binding for human brain receptors had to be substituted in amitriptyline (AMI) and nortriptyline's (NOR) cases
5-HT2A 4.355.6Binding 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 6.158.5132(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 10314817Cloned rat receptor was substituted for NOR's binding.
5-HT7 114 ?23Cloned rat receptor was substituted for AMI.
α1A 245510Human brain receptors were substituted for AMI and NOR.
α2A 6902030810.5As above.
D2 146025700.16As above.
D3 206 ?0.13Human receptors (their source was undefined) had to be substituted for AMI.
H1 1.115.18This 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 12.9401500This is the main receptor responsible for the anticholinergic side effects mentioned above.
M3 25.9501848This receptor is believed to be partly responsible for the metabolic adverse effects of the atypical antipsychotics.
σ 300200031.5All three values are for binding to the guinea pig brain receptors.

See also

Related Research Articles

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Flupentixol (INN), also known as flupenthixol, marketed under brand names such as Depixol and Fluanxol is a typical antipsychotic drug of the thioxanthene class. It was introduced in 1965 by Lundbeck. In addition to single drug preparations, it is also available as flupentixol/melitracen—a combination product containing both melitracen and flupentixol . Flupentixol is not approved for use in the United States. It is, however, approved for use in the UK, Australia, Canada, Russian Federation, South Africa, New Zealand, Philippines, Iran, Germany, and various other countries.

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References

  1. 1 2 3 4 5 "PERPHENAZINE AND AMITRIPTYLINE HYDROCHLORIDE tablet, film coated [Mylan Pharmaceuticals Inc.]". DailyMed. National Library of Medicine. Retrieved 7 October 2013.
  2. 1 2 3 4 5 "PERPHENAZINE AND AMITRIPTYLINE HYDROCHLORIDE tablet [REMEDYREPACK INC. ]". DailyMed. National Library of Medicine. Retrieved 7 October 2013.
  3. amitriptyline/perphenazine (Rx) - Etrafon, Triptafen, Triavil [Internet]. Medscape Reference. [cited 2013 Oct 7]. Available from: http://reference.medscape.com/drug/etrafon-triptafen-amitriptyline-perphenazine-342946
  4. 1 2 3 Truven Health Analytics, Inc. DRUGDEX® System (Internet) [cited 2013 Oct 7]. Greenwood Village, CO: Thomsen Healthcare; 2013.
  5. National Institute of Mental Health. PDSD Ki Database (Internet) [cited 2013 Oct 7]. Chapel Hill (NC): University of North Carolina. 1998-2013. Available from: "PDSP Database - UNC". Archived from the original on 2013-11-08. Retrieved 2013-12-01.
  6. Brunton L, Chabner B, Knollman B (2010). Goodman and Gilman's The Pharmacological Basis of Therapeutics (Twelfth ed.). McGraw Hill Professional.
  7. Taylor D, Paton C, Kapur S, Taylor D (2012). The Maudsley prescribing guidelines in psychiatry (11th ed.). Chichester, West Sussex: John Wiley & Sons.