TRIFLUOPERAZINE
THERAPEUTICS
Class
- Neuroscience-based Nomenclature: dopamine receptor antagonist (D-RAn)
- Conventional antipsychotic (neuroleptic, phenothiazine, dopamine 2 antagonist)
TRIFLUOPERAZINE commonly prescribed for
(Bold for FDA approved)
How TRIFLUOPERAZINE works
• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis
How long until TRIFLUOPERAZINE works
• Psychotic symptoms can improve within 1 week, but it may take several weeks for full effect on behavior
SIDE EFFECTS
Notable Side Effects
• Neuroleptic-induced deficit syndrome
• Akathisia
• Rash
• Priapism
• Drug-induced parkinsonism
• Tardive dyskinesia, tardive dystonia
• Risk of potentially irreversible involuntary dyskinetic movements may increase with cumulative dose and treatment duration
• Galactorrhea, amenorrhea
• Dizziness, sedation
• Dry mouth, constipation, blurred vision, urinary retention
• Decreased sweating
• Sexual dysfunction
• Hypotension
Life Threatening Side Effects
• Rare neuroleptic malignant syndrome may cause hyperpyrexia, muscle rigidity, delirium, and autonomic instability with elevated creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure
• Rare jaundice, agranulocytosis
• Rare seizures
• As a class, antipsychotics are associated with an increased risk of death and cerebrovascular events in elderly patients with dementia; not approved for treatment of dementia-related psychosis
weight gain

unusual
sedation

common
What to do about TRIFLUOPERAZINE side effects
Wait
• Wait
• Wait
• For drug-induced parkinsonism, add an anticholinergic agent
• Beta blockers, benzodiazepines, or serotonin 2A antagonists (e.g., mirtazapine, cyproheptadine) may reduce akathisia
• Reduce the dose
• For sedation, give at night
• Switch to an atypical antipsychotic
• Weight loss, exercise programs, and medical management for high BMIs, diabetes, dyslipidemia
• Metformin may help prevent or reverse antipsychotic-induced weight gain
DOSING AND USE
usual dosage range
• Oral: psychosis: 15–20 mg/day
Dosage Forms
• Tablet 1 mg, 2 mg, 5 mg, 10 mg
• Vial 2 mg/mL (discontinued in USA)
• Concentrate 10 mg/mL (discontinued in USA)
long term use
• Should periodically reevaluate long-term usefulness in individual patients, but treatment may need to continue for many years
• Not intended to treat anxiety long-term (i.e., longer than 12 weeks)
habit forming
• No
SPECIAL POPULATIONS
Renal Impairment
• Use with caution
Hepatic Impairment
• Not recommended for use
Cardiac Impairment
• Dose should be lowered
• Do not use parenteral administration unless necessary
Elderly
• Lower doses should be used and patient should be monitored closely
• Although conventional antipsychotics are commonly used for behavioral disturbances in dementia, no agent has been approved for treatment of elderly patients with behavioral symptoms of dementia such as agitation
• Elderly patients with dementia-related psychosis treated with antipsychotics are at an increased risk of death compared to placebo, and also have an increased risk of cerebrovascular events
Children and Adolescents
• Not recommended for use in children under age 6
• Children should be closely monitored when taking trifluoperazine
• Oral: initial 1 mg; increase gradually; maximum 15 mg/day except in older children with severe symptoms
• Intramuscular: 1 mg once or twice a day
• Generally consider second-line after atypical antipsychotics
Pregnancy
• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001
• Controlled studies have not been conducted in pregnant women
• There is a risk of abnormal muscle movements and withdrawal symptoms in newborns whose mothers took an antipsychotic during the third trimester; symptoms may include agitation, abnormally increased or decreased muscle tone, tremor, sleepiness, severe difficulty breathing, and difficulty feeding
• Reports of drug-induced parkinsonism, jaundice, hyperreflexia, hyporeflexia in infants whose mothers took a phenothiazine during pregnancy
• Trifluoperazine should only be used during pregnancy if clearly needed
• Psychotic symptoms may worsen during pregnancy and some form of treatment may be necessary
• Atypical antipsychotics may be preferable to conventional antipsychotics or anticonvulsant mood stabilizers if treatment is required during pregnancy
Breast Feeding
• Some drug is found in mother’s breast milk
• Recommended either to discontinue drug or bottle feed
Based on data Published online by Cambridge University Press
Compiled by Dr. Jash Ajmera