Lonasen Blonanserin Tablets

1. Indications and Usage
Schizophrenia:
Treatment of schizophrenia in adults.
2. Dosage and Administration
Route of Administration:
For Oral Use ONLY.
Recommended Dosage:
Starting Dose: 4 mg twice daily (8 mg/day).
Maintenance Dose: Adjust based on clinical response; typically 8–16 mg/day.
Maximum Dose: 24 mg/day.
Critical Administration Instruction:
MUST BE TAKEN AFTER MEALS: Absorption is significantly affected by food. Must be taken after meals to ensure adequate bioavailability. Taking on an empty stomach may result in subtherapeutic levels.
Dosing Frequency:
Typically administered twice daily (BID).
3. Mechanism of Action
Receptor Profile:
Blonanserin is a selective antagonist with high affinity for dopamine D2/D3 receptors and serotonin 5-HT2A receptors.
Selectivity:
D2/D3 Antagonist: Its affinity for D2 receptors is approximately twice that of 5-HT2A receptors. This profile is similar to first-generation antipsychotics but with a lower risk of extrapyramidal symptoms.
Low Affinity: It has low affinity for Histamine (H1), Alpha-1 adrenergic, and Muscarinic (M1) receptors.
Clinical Implication: This selectivity contributes to a favorable profile regarding weight gain, sedation, and orthostatic hypotension compared to other atypical antipsychotics.
4. Safety and Warnings
Increased Mortality in Elderly with Dementia (Boxed Warning):
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death.
Suicidal Thoughts and Behaviors:
Monitor for the emergence of suicidal ideation and behavior.
Neuroleptic Malignant Syndrome (NMS):
A potentially fatal reaction characterized by hyperpyrexia, muscle rigidity, autonomic instability, and elevated CPK.
Tardive Dyskinesia:
Risk of developing abnormal involuntary movements, which may be irreversible.
Constipation and Intestinal Obstruction:
May cause severe constipation leading to paralytic ileus.
5.Adverse Reactions
Most Common:
Extrapyramidal Symptoms (EPS): Parkinsonism (tremor, rigidity, bradykinesia), Akathisia (restlessness).
Hyperprolactinemia: Elevated prolactin levels.
Insomnia, Anxiety.
Note:
Unlike many other atypical antipsychotics, Blonanserin has a lower incidence of somnolence, weight gain, and dry mouth.
6.Drug Interactions
CYP3A4 Substrate:
Blonanserin is primarily metabolized by CYP3A4.
Strong CYP3A4 Inhibitors (Contraindicated):
Contraindicated with potent inhibitors (e.g., ketoconazole, itraconazole, ritonavir) due to significantly increased blonanserin exposure.
CYP3A4 Inducers:
Caution is advised when used with inducers (e.g., phenytoin, carbamazepine, rifampin) as they may decrease blonanserin efficacy.
Adrenaline (Epinephrine):
Contraindicated. Use with adrenaline may lead to severe hypotension (reversal of epinephrine effect).
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Blonanserin.
Available Strength: 4 mg tablets.
Appearance: White tablets.
Storage: Store at 30°C (86°F); excursions permitted to 15–30°C (59–86°F).