blonaserin drug description

1. Dr.tushar talhan
Psychiatry resident
Pdmmc amravati.

2. INTRODUCTION
 Blonanserin was developed as a novel
antipsychotic drug in Japan and was approved in
Japan in 2008 and Korea in 2009 for the
treatment of schizophrenia.
 Blonanserin belongs to a series of 4-phenyl-2-(1-
piperazinyl) pyridines.
 It has high affinity for D2 and D3 receptor and
serotonin 5HT2a receptor.
 Low affinity for 5HT2c, α1,H1, M1 receptor.

3. pharmacokinetics
 Orally absorb rapidly.
 Bioaviability -85%.
 Elimination half life10-16hrs.
 Eliminate mainly by urine-59%,faces30%.
 Max plasma conc. Reach in 2 hrs.
 Metabolite by CYP3A4.

4. Drug intraction
o Metabolise by CYP3a4.
o Drugs which are potent enzyme inhibitor may increase its
conc. So contraindicated e.g. ketoconazole,
erythromycin, clarithromycin,etc.
o Enzyme inducer decreases its effect e.g. phyntoin,
carbamazepine.
o Alcohol and barbiturate may enhances depressant effect.

5. Primary targets
 Positive symptoms of psycosis
(delusion,hallucination)
 Negative symptoms of psychosis
 Cognitive symptoms
 Mood symptoms
 Unstable mood
 Aggressive symptoms.

6. uses
 Schizophrenia
 Acute mania
 Other psychotic disorder
 Bipolar maintainance
 Bipolar depression
 T/t resistant depression.
 Behavioral disturbance in demnetia
 Behavioral disturbance in children and
adloscent.

7. dosing
 form- tab 2mg, 4mg, 8mg. Powder 20mg /1gm
 Initial dose- 8mg/day divided in 2 doses.
 Maintainance-8-16mg/day divided in 2 doses.
 Max-24mg/day.
 Should taken after meal.
 Can be taken at bed time.
 Can be shifted to single daily dose at bed
time.(pt stibilise).

8. Continue…..
 No habit form.
 Special population:
 Cardiac and renal impairment - no study done
 Hepatic impariment – use cautiosly.
 Elderly- use lower doses, risk of CVE, and
death.
 Children- safety and efficacy not established.
 Pregnancy – no studies.
 Breastfeeding- either discontinue drug or bottle
fed.

9. ADE
 Oral blonaserin was generally well tolerated.
 ADR are mild to moderate in severity.
 75% recipient experienced ADR.
MC- parkinson syndrome(35%)
Akathesia(24%)
Insomnia(22%)
increase prolactin level(19%)
Urinary retention
Sedation is commonly observe.

10. schizophrenia
 it reduces positive symptoms.( not eliminate)
 Improve negative symptoms.
 Improve aggressive, cognitive and affective
symptoms in schizophrenia.
 No total remission
 5-15% pt experienced overall improvement
of >50-60% on stable 1 yr of t/t.
 Psychotic symptoms may improve in 1 week.
 May take several week
 Recommended to wait 4-6 wk to determine
efficacy of drug

11. antipsychotics
 blonanserin was well tolerated and had equal
efficacy to haloperidol and risperidone in terms
of positive symptoms and depressive
symptoms in patients with chronic
schizophrenia.
 It was also superior to haloperidol in
improving negative symptoms
 Compared with risperidone blonnserin is more
tolerable with a better safety profile,
particularly with respect to prolactin elevation.
Hyperprolactinemia, weight gain, increased
appetite, orthostatic hypotension, increased
more frequently with Risperidone.

12.  In Blonanserin group and the
risperidone group, the change in PANSS
total score was equal. In addition,
positive symptoms, negative symptoms
subscale score, including the variation in
the two groups were not significantly
different