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perphenazine (Trilafon)

 

Classes: Antipsychotics, 1st Generation; Antipsychotics, Phenothiazine

Dosing and uses of Trilafon (perphenazine)

 

Adult dosage forms and strengths

tablets

  • 2mg
  • 4mg
  • 8mg
  • 16mg

 

Intractable Hiccoughs

8-16 mg PO qDay divided q8-12hr

Maximum: 24 mg

 

Treatment of Nausea/Vomiting

8-16 mg PO qDay divided q6-12hr

Maximum: 24 mg

 

Schizophrenia

Hospitalized patients: 8-16mg PO q6-12hr

Hospitalized patients: Not to exceed 64 mg/day divided q6-12hr

Outpatients: 4-8mg PO q8hr; reduce as soon as possible to minimum effective dose

 

Hepatic Impairment

Dose adjustment not described in manufacturer's labeling

 

Renal Impairment

Dose adjustment not described in manufacturer's labeling

 

Pediatric dosage forms and strengths

tablets

  • 2mg
  • 4mg
  • 8mg
  • 16mg

 

Intractable Hiccoughs

<12 years

  • Not recommended by manufacturer

 >12 years

  • 8-16 mg PO qDay divided q8-12hr Maximum: 24 mg

 

Schizophrenia

<12 years

  • Not recommended by manufacturer

>12 years

  • Hospitalized patients: 8-16mg PO q6-12hr
  • Hospitalized patients: Not to exceed 64 mg/day divided q6-12hr
  • Outpatients: 4-8mg PO q8hr; reduce as soon as possible to minimum effective dose

 

Geriatric dosage forms and strengths

Initiate dosing at lower end of the range

 

Intractable Hiccoughs

 8-16 mg PO qDay divided q8-12hr

Maximum: 24 mg

 

Treatment of Nausea/Vomiting 

8-16 mg PO qDay divided q6-12hr  

Maximum: 24 mg

 

Schizophrenia

Hospitalized patients: 8-16mg PO q6-12hr

Hospitalized patients: Not to exceed 64 mg/day divided q6-12hr

Outpatients: 4-8mg PO q8hr; reduce as soon as possible to minimum effective dose

 

Trilafon (perphenazine) adverse (side) effects

>10%

Akathisia (60%)

 

Frequency not defined

Confusion

Decreased gag reflex

EPs

  • Akathisia (60%)
  • Dystonia
  • Muscle stiffness
  • Neuroleptic malignant syndrome (infrequent but serious)
  • Parkinsonism
  • Tardive dyskinesia

Common

  • Anticholinergic effects
  • Sedation
  • Weight gain
  • Oligomenorrhea/amenorrhea
  • Erectile dysfunction

Less Common

  • Orthostatic hypotension (post-IM inj), tachycardia
  • Anxiety, agitation, cerebral edema, depression, dizziness, euphoria, headache, insomnia, restless, weakness
  • Anorexia, dyspepsia, constipation, ileus
  • Lens opacities (prolonged use)

Uncommon

  • ECG changes
  • Photosensitivity
  • Pruritis
  • Galactorrhea
  • Ejaculatory disorder
  • Diarrhea
  • Blood dyscrasia

Rare

  • Seizure
  • Priapism
  • Cholestatic jaundice

 

Warnings

Black box warnings

Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials. The deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature

This drug is not approved for the treatment of patients with dementia-related psychosis

 

Contraindications

Documented hypersensitivity to phenothiazines

Coma, severe hypotension, severe CNS depression, concurrency with large amounts of CNS depressants, poorly controlled seizure disorder, subcortical brain damage, myelosuppression, liver damage, blood dyscrasias

Severe cardiovascular disease

Lactation

 

Cautions

Avoid using in children with suspected Reye's syndrome

Glaucoma, prostatic hypertrophy, stenosing PUD, tardive dyskinesia, history of NMS, Parkinson's disease, hypocalcemia, renal/hepatic impairment, patients who have exhibited a severe reaction to insulin or ECT, history of seizures, asthma, respiratory tract infections, cardiovascular disease

Hypotension may be particularly severe in patients with pheochromocytoma or mitral insufficiency

Depresses hypothalamic thermoregulatory mechanism; exposure to extreme temperatures may cause hypo- or hyperthermia

In case of severe hypotension, use norepinephrine or phenylepinephrine, do NOT use epinephrine or dopamine

Antiemetic effect may obscure toxicity of chemotherapeutic drugs

May need anticholinergic antiparkinsonian agent to counter EPs

FDA Warning regarding off-label use for dementia in elderly

 

Pregnancy and lactation

Pregnancy category: C

Lactation: avoid

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Trilafon (perphenazine)

Mechanism of action

Antipsychotic that blocks postsynaptic mesolimbic dopaminergic receptors in the brain; it has moderate anticholinergic effects, weak to moderate sedative effects, strong extrapyramidal effects, and strong antiemetic activity

 

Pharmacokinetics

Peak Plasma Time: 1-3 hr; 2-4 hr (metabolite)

Half-Life: 9-12 hr (; 10-19 hr (metabolite)

Concentration: 984 pg/mL; 509 pg/mL (metabolite)

Metabolism: Hepatic P450 enzyme CYP2D6

Metabolites: 7-hydroxyperphenazine

Enzymes inhibited: CYP2D6

Excretion: Urine and feces