Blonanserin
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 distributionBlonanserin has a Vc of 9500 L and a Vt of 8560 L for a total Vd of 18060 L 1.
Protein bindingBlonanserin is over 99.7% bound to plasma proteins 2 . Serum albumin is the primary binder.
MetabolismBlonanserin 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-lifeBlonanserin has a half life of elimination of 10.7-16.2 h 2.
ClearanceBlonanserin has a clearance of 1230 L/h 1.
Dosage
schizophrenia:
2-8 mg daily
Drug contraindications
Hypersensitivity to this drugSide effects
cardiovascular conditions , hypertriglyceridemia , Hyper-cholesteremia , Weight increaseInteractions
Pregabalin , Methocarbamol , Hydroxyzine , Chlordiaze poxide , Butalbital and Acetaminophen , Ramelteon , Secobarbital , Tolcapone , Quazepam , Lopinavir and Ritonavir , Cariprazine , Opium , Azathioprine , Acyclovir , Allopurinol , ampicillin , Amphotericin B , Amitriptyline , Iron Dextran Complex , revefenacin , Sacubitril , Abacavir , Baricitinib , Carmustine , magnesium chloride , Aminophenazone , Benorilate , Capreomycin , Alogliptin , Darifenacin , Mepenzolate , Terfenadine , Fesoterodine , Tegafur , Bacitracin , Azelaic acid , Ammonium chloride , Aceclofenac , Acemetacin , Amiloride , Quetiapine , Buprenorphine , Mirtazapine , Acenocoumarol , Hyoscyamine , Chromium+calcium , Solifenacin , Bisoprolol , Azelastine , Atazanavir , Vancomycin , Lithium carbonate , mebeverine , Nortriptyline , Warfarin , Capecitabine , Carbamazepine , Dicyclomine , Digoxin , Zolpidem , Selenium , Cyproheptadine , Cisplatin , Tiotropium bromid , Desipramine , Dopamine , Doxepin , Dexpanthenol , Disopyramide , Imipramine , Bleomycin , Budesonide , Propantheline , Thalidomide , Tolterodine , Amikacin , Acarbose , Acetaminophen , Oxybutynin , Ipratropium bromide , Isotretinoin , ethotoin , tucatinibAlerts
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
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