ZUCLOPENTHIXOL

brands

Class

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

ZUCLOPENTHIXOL commonly prescribed for

(Bold for FDA approved)

How ZUCLOPENTHIXOL works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis

How long until ZUCLOPENTHIXOL works

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

• For oral formulation, psychotic symptoms can improve within 1 week, but may take several weeks for full effect on behavior

Notable Side Effects

• Drug-induced parkinsonism

• 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

• Priapism

• Galactorrhea, amenorrhea

• Rare lens opacity

• Sedation, dizziness

• Dry mouth, constipation, vision problems

• Hypotension

• 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 neutropenia

• Rare respiratory depression

• Rare 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

common

sedation

common

What to do about ZUCLOPENTHIXOL 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

usual dosage range

• Oral 20–60 mg/day

• Acetate 50–150 mg every 2–3 days

• Decanoate 150–300 mg every 2–4 weeks

Dosage Forms

• Tablet 10 mg, 25 mg, 40 mg

• Acetate 50 mg/mL (equivalent to zuclopenthixol 45.25 mg/mL), 100 mg/2 mL (equivalent to zuclopenthixol 45.25 mg/mL)

• Decanoate 200 mg/mL (equivalent to zuclopenthixol 144.4 mg/mL), 500 mg/mL (equivalent to zuclopenthixol 361.1 mg/mL)

long term use

• Zuclopenthixol decanoate is intended for maintenance treatment

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

habit forming

• No

Renal Impairment

• Use with caution

Hepatic Impairment

• Use with caution

Cardiac Impairment

• Use with caution

Elderly

• Some patients may tolerate lower doses better

• Maximum acetate dose 100 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

• Safety and efficacy have not been established in children under age 18

• Preliminary open-label data show that oral zuclopenthixol may be effective in reducing aggression in mentally impaired 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

• 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

• Infants of women who choose to breast feed should be monitored for possible adverse effects