Drug information of Blonanserin

Blonanserin

Drug group:

Blonanserin is an atypical antipsychotic approved in Japan in January, 2008. It offers improved tolerability as it lacks side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As a second-generation (atypical) antipsychotic, it is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics.

Mechanism of effect

Blonanserin binds to and inhibits dopamine receptors D2 and D3 as well as the serotonin receptor 5-HT2A with high affinity 2. Blonanserin has low affinity for other dopamine and serotonin receptors as well as muscarinic, adrenergic, and histamine receptors. This reduces dopaminergic and serotonergic neurotransmission which is thought to produce a reduction in positive and negative symptoms of schizophrenia respectively.

Pharmacodynamic

Blonanserin antagonizes dopamine and serotonin receptors to reduce symptoms of schizophrenia

Pharmacokinetics

Absorption

Blonanserin has a Tmax of 1.5 h and a bioavailablity of 55% 1,2. Tmax has been observed to be prolonged and relative bioavailability increased when administered with food 1.

Volume of distribution

Blonanserin has a Vc of 9500 L and a Vt of 8560 L for a total Vd of 18060 L 1.

Protein binding

Blonanserin is over 99.7% bound to plasma proteins 2 . Serum albumin is the primary binder.

Metabolism

Blonanserin is mainly metabolized by CYP3A4 2. It undergoes hydoxylation of the cyclooctane ring as well as N-oxidation and N-deethylation of the piperazine ring. The N-deethylated and hydroxylated metabolites are active but to a lesser degree than the parent drug.
Route of elimination

57% of blonanserin is excreted in the urine and 30% in the feces 2. Only 5% of the drug in the feces is the parent drug with no parent drug excreted through the urine.

Half-life

Blonanserin has a half life of elimination of 10.7-16.2 h 2.

Clearance

Blonanserin has a clearance of 1230 L/h 1.


 

Dosage

schizophrenia:
2-8 mg daily

Drug contraindications

Hypersensitivity to this drug

Alerts

Use with caution in patients with history of seizures, Parkinson disease, Lewy body dementia, cardiovascular disease, hypovolemia, dehydration

Esophageal dysmotility and aspiration have been associated with antipsychotic use

Disruption of body temperature regulation has been attributed to antipsychotic agents

Metabolic changes

  • Atypical antipsychotic drugs have been associated with metabolic changes that may increase cardiovascular or cerebrovascular risk (eg, hyperglycemia, dyslipidemia, and body weight gain)
  • In some cases, hyperglycemia concomitant with use of atypical antipsychotics has been associated with ketoacidosis, hyperosmolar coma, or death

Points of recommendation

Store at room temperature 15-25°C

Pregnancy level

HAVE NOT BEEN ESTABLISHED

Drug forms

Lonasen. blosana . elicia . blonaser . blonitas .

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