THERAPEUTICS

brands

Class

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

SULPIRIDE commonly prescribed for

(Bold for FDA approved)

• Schizophrenia
• Depression

How SULPIRIDE works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis

• Blocks dopamine 3 and 4 receptors, which may contribute to sulpiride’s actions

• Possibly blocks presynaptic dopamine 2 autoreceptors more potently at low doses, which could theoretically contribute to improving negative symptoms of schizophrenia as well as depression

How long until SULPIRIDE works

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

SIDE EFFECTS

Notable Side Effects

• Drug-induced parkinsonism, akathisia

• Prolactin elevation, galactorrhea, amenorrhea

• Sedation, dizziness, sleep disturbance, headache, impaired concentration

• Dry mouth, nausea, vomiting, constipation, anorexia

• Impotence

• Tardive dyskinesia

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

• Rare hypomania

• Palpitations, 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

• 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

common

common

What to do about SULPIRIDE 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

• Schizophrenia: 400–800 mg/day in 2 doses (oral)

• Predominantly negative symptoms: 50–300 mg/day (oral)

• Intramuscular injection: 600–800 mg/day

• Depression: 150–300 mg/day (oral)

Dosage Forms

• Different formulations may be available in different markets

• Tablet 200 mg, 400 mg, 500 mg

• Intramuscular injection 50 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

SPECIAL POPULATIONS

Renal Impairment

• Use with caution; drug may accumulate

• Sulpiride is eliminated by the renal route; in cases of severe renal insufficiency, the dose should be decreased and intermittent treatment or switching to another antipsychotic should be considered

Hepatic Impairment

• Use with caution

Cardiac Impairment

• Use with caution

Elderly

• Some patients may tolerate lower doses better

• 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 15

• 14 and older: recommended 3–5 mg/kg per day

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

• Potential risks should be weighed against the potential benefits, and sulpiride should be used only if deemed 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

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or bottle feed

• Immediate postpartum period is a high-risk time for relapse of psychosis