Amitriptyline/perphenazine

Amitriptyline/perphenazine
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
Pregnancy
category
  • US: D (Evidence of risk)
Routes of
administration
Oral
Legal status
Legal status
Identifiers
CAS Number 8015-22-3

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]

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]
- Galactorrhea — the release of milk that is not associated with pregnancy of breastfeeding
- Gynaecomastia — the development of breast tissue in males
- Disturbances in menstrual cycle
- Sexual dysfunction
Uncommon/Rare adverse effects include
[1][2][4]
- Muscle rigidity
- Tremors
- Mental status change (e.g. hallucinations, agitation, stupor, confusion, etc.)
- Hyperthermia — elevated body temperature
- 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]

Macromolecule Amitriptyline Nortriptyline
(Amitriptyline's active metabolite)
Perphenazine Notes
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.

See also

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: "Archived copy". Archived from the original on 2013-11-08. Retrieved 2013-12-01.
  6. Brunton L, Chabner B, Knollman B. Goodman and Gilman’s The Pharmacological Basis of Therapeutics, Twelfth Edition. McGraw Hill Professional; 2010.
  7. Taylor D, Paton C, Kapur S, Taylor D. The Maudsley prescribing guidelines in psychiatry. 11th ed. Chichester, West Sussex: John Wiley & Sons; 2012.


This article is issued from Wikipedia - version of the 10/11/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.