ANTIPSYCHOTIC

1. CHEMISTRY OFANTIPSYCHOTIC AGENTS
Presentation by
Abhishek Ghara
I M. Pharm
Dept. Pharmaceutical Chemistry

2. Psychotic Disorders
Psychotic disorders are severe mental disorders that cause abnormal
thinking and perceptions.
People with psychoses lose touch with reality.
They make it hard for someone to think clearly, make good judgments,
respond emotionally, communicate effectively, understand reality, and
behave appropriately.
Schizophrenia is one type of psychotic disorder. People with bipolar
disorder may also have psychotic symptoms. Other problems that can
cause psychosis include alcohol and some drugs, brain tumors, brain
infections, and stroke.

3. Symptoms
Two of the main symptoms are delusions and hallucinations.
Delusions are false beliefs, such as thinking that someone is plotting
against you or that the TV is sending you secret messages.
Hallucinations are false perceptions, such as hearing, seeing, or feeling
something that is not there.
When symptoms are severe, people with psychotic disorders have
trouble staying in touch with reality and often are unable to handle daily
life.

4. Classification of antipsychotic drug
1. Phenothiazine derivatives : Promazine, Chlorpromazine,
Triflupromazine
2. Thiothixene derivatives : Chlorprothixene, Thiothixene
3. Butyrophenone derivatives : Haloperidol, Droperidol
4. Diphenylbutyl piperidine : Pimozide
5. Dibenzoxazepine : Loxapine
6. Dihydroindole : Molidone

5. Mechanism of action
All typical antipsychotic agents currently
employed clinically block post synaptic
dopaminergic D2 receptors in the mesolimbic and
cortex regions of the brain and act as a
competetive antagonist of dopamine. The blokade
of D2 receptors is thought to be responsible for
decreasing the positive symptoms of
schizophrenia.
Central dopamine receptors are subdivided into
D1 , D2 and according to some sources, D3
receptors. These receptors have a high affinity for
dopamine, but they differ in selectivity to
neuroleptics of various chemical classes.
Adenylyl cyclase is involved which is
responsible for the conversion of adenosine
triphosphate to cyclic adenosine monophosphate
(cAMP).

6. Phenothiazine derivatives
Synthesis

7. SAR

8. Thiothixene derivatives
Synthesis of thiothixene

9. Butyrophenone derivatives
Synthesis of droperidol

10. SAR of butyrophenone

11. Diphenylbutyl piperidine
Synthesis of pimozide

12. Dibenzoxazepine
Synthesis of loxapine

13. Dihydroindole
Synthesis of molindone