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perphenazine (Trilafon)
Tradename: Trilafon.
Indications:
1) symptomatic management of psychotic disorders
2) chemotherapy-induced nausea & vomiting
Contraindications:
1) narrow-angle glaucoma
2) bone marrow suppression
3) severe liver disease
4) severe cardiac disease
Caution:
1) seizure disorder
2) safety in children < 12 years of age has not been established
Dosage:
1) 5 mg IM/IV every 6 hours
- dilute IV injection to 0.5 mg/mL with normal saline & infuse at 1 mg/min
2) 4-8 mg PO TID with water or juice
3) elderly: 2-12 mg daily [4]
Tabs: 2, 4, 8, 16 mg.
Liquid: 16 mg/5 mL.
Injection: 5 mg/mL (1 mL)
Pharmacokinetics:
1) see chlorpromazine
2) metabolized in the liver by cyt P450 2D6
Adverse effects:
1) common (> 10%)
- pseudoparkinsonism, akathisia, dystonia, hypotension, pigmentary retinopathy, tardive dyskinesia (persistent), constipation, decreased sweating, dizziness, orthostatic hypotension, nasal congestion
2) less common (1-10%)
- difficulty urinating, photosensitivity, rash, changes in menstrual cycle, ejaculatory dysfunction, changes in libido, breast pain, weight gain, nausea/vomiting, epigastric pain, trembling of fingers
3) uncommon (< 1%)
- agranulocytosis, cholestatic jaundice, neuroleptic malignant syndrome, priapism, blue-gray discoloration of the skin, impairment of temperature regulation, galactorrhea, leukopenia, hepatotoxicity, changes in the cornea & lens
4) other
- low sedation
- low anticholinergic effects
- low orthostatic hypotension effects
- high incidence of extrapyramidal symptoms
- pseudoparkinsonism
- dystonias
- akathisia
- neuroleptic malignant syndrome (rare)
- tardive dyskinesia (persistent)
- QT prolongation
- direct myocardial depression
- lowering of seizure threshold
5) black box warning [3]
- increased risk of hyperglycemia
- increased risk of cerebrovascular events
- increased risk of mortality in patients with dementia
Drug interactions:
1) see chlorpromazine
2) avoid terfenadine, astemizole & other agents which prolong the QT interval
3) perphenazine inhibits cyt P450 2D6
a) inhibits its own metabolism
b) may increase levels & effects of drugs metabolized by cyt P450 2D6
4) any drug that inhibits cyt P450 2D6 may increase levels of perphenazine [4]
Mechanism of action: high-potency antipsychotic agent
Interactions
drug interactions
drug adverse effects (more general classes)
Related
cytochrome P450 2D6 (cytochrome P450 2D, cytochrome P450 DB1, debrisoquine-4-hydroxylase, CYP2D6)
General
antipsychotic agent
phenothiazine
Properties
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Geriatric Review Syllabus, 8th edition (GRS8)
Durso SC and Sullivan GN (eds)
American Geriatrics Society, 2013
Component-of
amitriptyline/perphenazine (Etrafon, Triavil)