brands

Class

• Neuroscience-based Nomenclature: dopamine, serotonin receptor antagonist (DS-RAn)
• Atypical antipsychotic (serotonin– dopamine antagonist; second-generation antipsychotics; also a mood stabilizer)

SERTINDOLE commonly prescribed for

(Bold for FDA approved)

How SERTINDOLE works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis and stabilizing affective symptoms

• Blocks serotonin 2A receptors, causing enhancement of dopamine release in certain brain regions and thus reducing motor side effects and possibly improving cognitive and affective symptoms

• Serotonin 2C properties may contribute to antidepressant actions

How long until SERTINDOLE works

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

• Classically recommended to wait at least 4–6 weeks to determine efficacy of drug, but in practice some patients may require up to 16–20 weeks to show a good response, especially on negative or cognitive symptoms

Notable Side Effects

• Orthostatic hypotension

• Dizziness, dry mouth, nasal congestion

• Weight gain, peripheral edema, decreased ejaculatory volume

• May increase risk for diabetes and dyslipidemia

• Tardive dyskinesia (reduced risk compared to conventional antipsychotics)

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

Life Threatening Side Effects

• Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients taking atypical antipsychotics

• Rare neuroleptic malignant syndrome may cause hyperpyrexia, muscle rigidity, delirium, and autonomic instability with elevated creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure

• 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

• Rare seizures

weight gain

common

sedation

unusual

What to do about SERTINDOLE side effects

• Wait

• Wait

• Wait

• Anticholinergics may reduce drug-induced parkinsonism when present

• Beta blockers, benzodiazepines, or serotonin 2A antagonists (e.g., mirtazapine, cyproheptadine) may reduce akathisia

• Weight loss, exercise programs, and medical management for high BMIs, diabetes, dyslipidemia

• Metformin may help prevent or reverse antipsychotic-induced weight gain

• Switch to another atypical antipsychotic

usual dosage range

• 12–20 mg/day

Dosage Forms

• Tablet 4 mg, 12 mg, 16 mg, 20 mg

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

• Dose adjustment not generally necessary

Hepatic Impairment

• For mild to moderate impairment, use slower titration and lower maintenance dose

• Contraindicated in patients with severe hepatic impairment

Cardiac Impairment

• Drug should be used with caution because of risk of orthostatic hypotension

• Not recommended for patients with significant cardiovascular illness, including congestive heart failure, cardiac hypertrophy, arrhythmia, bradycardia, or congenital prolonged QTc syndrome

Elderly

• Use cautiously and only after thorough cardiovascular examination

• Some patients may tolerate lower doses better

• Although atypical 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 atypical 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

• Children and adolescents using sertindole may need to be monitored more often than adults and may tolerate lower doses better

Pregnancy

• Some animal studies show adverse effects; no controlled studies in humans

• 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

Breast Feeding

• Unknown if sertindole 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

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