THERAPEUTICS

brands

Class

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

HALOPERIDOL commonly prescribed for

(Bold for FDA approved)

• Manifestations of psychotic disorders (oral, immediate-release injection)
• Tics and vocal utterances in Tourette’s syndrome (oral, immediate-release injection)
• Second-line treatment of severe behavior problems in children of combative, explosive hyperexcitability (oral)
• Second-line short-term treatment of hyperactive children (oral)
• Treatment of schizophrenic patients who require prolonged parenteral antipsychotic therapy (depot intramuscular decanoate)

• Bipolar disorder
• Behavioral disturbances in dementias
• Delirium (with lorazepam)

How HALOPERIDOL works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis and possibly combative, explosive, and hyperactive behaviors

• Blocks dopamine 2 receptors in the nigrostriatal pathway, improving tics and other symptoms in Tourette’s syndrome

How long until HALOPERIDOL 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

• 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, urinary retention, blurred vision

• Decreased sweating

• Hypotension, tachycardia, hypertension

• Weight gain

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 seizures

• Rare jaundice, agranulocytosis, leukopenia

• 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

not usual

not usual

sedation

not usual

not usual

What to do about HALOPERIDOL 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

• 1–40 mg/day orally

• Immediate-release injection 2–5 mg each dose

• Decanoate injection 10–20 times the previous daily dose of oral antipsychotic (see Haloperidol Decanoate section after Pearls for dosing and use)

Dosage Forms

• Tablet 0.5 mg scored, 1 mg scored, 2 mg scored, 5 mg scored, 10 mg scored, 20 mg scored

• Concentrate 2 mg/mL

• Injection 5 mg/mL (immediate-release)

• Decanoate injection 50 mg/mL, 100 mg/mL

long term use

• Often used for long-term maintenance

• 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 because of risk of orthostatic hypertension

• Possible increased risk of QTc prolongation or torsade de pointes at higher doses or with intravenous administration

Elderly

• Lower doses should be used and patient should be monitored closely

• Elderly patients may be more susceptible to respiratory side effects and hypotension

• 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

• Safety and efficacy have not been established; not intended for use under age 3

• Oral: initial 0.5 mg/day; target dose 0.05–0.15 mg/kg per day for psychotic disorders; 0.05–0.075 mg/kg per day for nonpsychotic disorders

• 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 conventional antipsychotic during pregnancy

• Reports of limb deformity in infants whose mothers took haloperidol during pregnancy

• Haloperidol should generally not be used during the first trimester

• Haloperidol 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