THERAPEUTICS

Class

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

PIPOTHIAZINE commonly prescribed for

(Bold for FDA approved)

• Maintenance treatment of schizophrenia
• Other psychotic disorders
• Bipolar disorder

How PIPOTHIAZINE works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis

How long until PIPOTHIAZINE works

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

SIDE EFFECTS

Notable Side Effects

• Excitement, insomnia, restlessness

• Tardive dyskinesia (risk increases with duration of treatment and with dose)

• Risk of potentially irreversible involuntary dyskinetic movements may increase with cumulative dose and treatment duration

• Galactorrhea, amenorrhea

• Dry mouth, nausea, blurred vision, sweating, appetite change

• Sexual dysfunction (impotence)

• Hypotension, arrhythmia, tachycardia

• Weight gain

• Rare rash

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

• Jaundice, leukopenia

• 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

common

common

sedation

unusual

unusual

What to do about PIPOTHIAZINE 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, take 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

• 50–100 mg once a month

Dosage Forms

• Injection 50 mg/mL

long term use

• Should periodically reevaluate long-term usefulness in individual patients, but treatment may need to continue for many years

habit forming

• No

SPECIAL POPULATIONS

Renal Impairment

• Use with caution

Hepatic Impairment

• Use with caution

Cardiac Impairment

• Use with caution

Elderly

• Elderly patients do not metabolize the drug as quickly

• Dose should be reduced

• Recommended starting dose 5–10 mg

• 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

Pregnancy

• 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

• Not recommended unless absolutely necessary

• 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

• Unknown if pipothiazine is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or bottle feed