brands

Class

• Neuroscience-based Nomenclature: dopamine receptor antagonist (D-RAn)
• Conventional antipsychotic (neuroleptic, phenothiazine, dopamine 2 antagonist)

Stelazine commonly prescribed for

(Bold for FDA approved)

How Stelazine works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis

How long until Stelazine works

• Psychotic symptoms can improve within 1 week, but it may take several weeks for full effect on behavior

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 Stelazine 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

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

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