brands

Class

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

Xolybex commonly prescribed for

(Bold for FDA approved)

How Xolybex works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis

How long until Xolybex works

• With injection, psychotic symptoms can improve within a few days, but it may take 1–2 weeks for notable improvement

• With oral formulation, 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

• Drug-induced parkinsonism

• Insomnia, restlessness, agitation, sedation

• 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

• Tachycardia

• Weight gain

• Hypomania

• Rare eosinophilia

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, 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

common

sedation

not usual

What to do about Xolybex 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 3–6 mg/day in divided doses

• Intramuscular 40–120 mg every 1–4 weeks

Dosage Forms

• Tablet 0.5 mg, 3 mg

• Injection 20 mg/mL, 100 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

Renal Impairment

• Oral: recommended to take half or less of usual adult dose

• Intramuscular: recommended dose schedule generally 10–20 mg every 15 days

Hepatic Impairment

• Use with caution

• Oral: recommended to take half or less of usual adult dose

Cardiac Impairment

• Use with caution

• Oral: recommended to take half or less of usual adult dose

Elderly

• Intramuscular: recommended initial dose generally 5 mg; recommended dose schedule generally 10–20 mg every 15 days

• Oral: recommended to take half or less of usual adult dose

• 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 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

• Not recommended for use during 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 conventional antipsychotic during pregnancy

• 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