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
Licence data US Daily Med:link
Pregnancy cat.
Legal status
Routes Oral
Identifiers
ATC code ?

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[edit]

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

  • Moderate-severe anxiety and/or agitation and depression
  • Depression and anxiety in association with chronic physical disease
  • Schizophrenia with prominent depressive symptoms

Adverse effects[edit]

Common (>1% incidence) adverse effects include
[1][2][4]
- Blurred vision
- Constipation
- Dry mouth
- Nasal congestion
  • Increased appetite
  • Weight gain
  • Nausea
  • Dizziness
  • Headache
  • Vomiting
Unknown frequency adverse effects include
[1][2][4]
  • Diarrhoea
  • Alopecia — hair loss
  • Photophobia
  • Pigmentation
  • Eczema up to exfoliative dermatitis
  • Urticaria
  • Erythema
  • Itching
  • Photosensitivity (increased sensitivity of affected skin to sunlight)
  • Hypersalivation — excessive salivation.
  • Hyperprolactinaemia — elevated blood prolactin levels. This may present with the following symptoms:
- 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
  • Pigmentation of the cornea and lens
  • Hyperglycaemia — elevated blood glucose (sugar) levels.
  • Hypoglycaemia — low blood glucose (sugar) levels.
  • Disturbed concentration
  • Excitement
  • Anxiety
  • Insomnia
  • Restlessness
  • Nightmares
  • Weakness
  • Fatigue
  • Diaphoresis — excessive/abnormal sweating.
Uncommon/Rare adverse effects include
[1][2][4]
  • Tardive dyskinesia, an often irreversible adverse effect that usually results from chronic use antipsychotic medications, especially the high-potency first-generation antipsychotics. It is characterised by slow (hence tardive), involuntary, repetitive, purposeless muscle movements.
  • Neuroleptic malignant syndrome, a potentially fatal complication of antipsychotic drug use. It is characterised by the following symptoms:
- 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.)
  • Urinary retention — the inability to pass urine despite having urine to pass.
  • Blood dyscrasias e.g. agranulocytosis (a potentially fatal drop in white blood cell count), leukopaenia (a drop in white blood cell counts but not to as extreme an extent as agranulocytosis), neutropaenia (a drop in neutrophil [the cells of the immune system that specifically destroy bacteria] count), thrombocytopaenia (a dangerous drop in platelet [a cell found in the blood that plays a crucial role in the blood clotting process] counts), purpura (the appearance of red or purple discolourations of the skin that do not blanch when pressure is applied), eosinophilia (raised eosinophil [the cells of the immune system that specifically fights off parasites] count)
  • Hepatitis — inflammation of the liver
  • Jaundice
  • Pigmentary retinopathy
  • Anaphylactoid reactions
  • Oedema — the abnormal buildup of fluids in the tissues
  • Asthma
  • Coma
  • Seizures
  • Confusional states
  • Disorientation
  • Incoordination
  • Ataxia
  • Tremors
  • Peripheral neuropathy — nerve damage
  • Numbness, tingling and paresthesias of the extremities
  • Dysarthria
  • Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
  • Tinnitus — falsely hearing ringing in the ears.
  • Alteration in EEG patterns
  • Paralytic ileus — cessation of the peristaltic waves that propel partially digested food through the digestive tract.
  • Hyperpyrexia (elevated body temperature)
  • Disturbance of accommodation
  • Increased intraocular pressure
  • Mydriasis

Pharmacology[edit]

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.

References[edit]

  1. ^ a b c d e "PERPHENAZINE AND AMITRIPTYLINE HYDROCHLORIDE tablet, film coated [Mylan Pharmaceuticals Inc.]". DailyMed. National Library of Medicine. Retrieved 7 October 2013. 
  2. ^ a b c d e "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. ^ a b c 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: http://pdsp.med.unc.edu/pdsp.php
  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.