1. ANTI-PSYCHOTIC DRUGS
(NEUROLEPTICS)
DR.FOUZIA

2. PSYCHOSIS
Psychosis is a symptom of mental illnesses characterized by a distorted
or nonexistent sense of reality.
1-Delusions
2-Hallucinations
3-Deranged thought process
4-Clear sensorium

3. PSYCHOSIS
Dopamine Excess  Psychosis
Schizophrenia:
Syndrome characterized by massive disruption of thinking, mood and
behavior and poor ability to filter various types of stimuli.
Positive symptoms:
Delusions, Hallucinations and illusions
Negative symptoms:
Diminished sociability, Poverty of speech

4. CLASSIFICATION OF ANTIPSHYCHOTICS
A-Typical antipsychotic agents
(Classic drugs)
D2 Antagonist
•Chlorpromazine (prototypical drug)
•Thioridazine
•Fluphenazine
•Thiothixene
•Haloperidol

5. CLASSIFICATION OF ANTIPSHYCHOTICS
B- Atypical antipsychotic agents
(Newer agents)
5-HT2 Antagonist
•Clozapine
•Olanzapine
•Quetiapine
•Risperidone
•Ziprasidone
•Aripiprazole

6. RECEPTORS BLOCKED BY ANTIPSHYCHOTICS
Dopamine receptors:
D2 ↓ c AMP
Serotonin receptors:
5-HT2

7. MECHANISM OF ACTION OF ANTIPSHYCHOTICS
A-Typical antipsychotic agents (Classic drugs)
Block mainly D2-Receptor
α1
H1 Blocked by Chlorpromazine (prototypical drug)
M
B- Atypical antipsychotic agents (Newer agents)
Block mainly 5-HT2-Receptor
Less effect on D2-Receptor

8. PHARMACOLOGICAL EFFECTS OF CHLORPROMAZINE
1-Antipsychotic effects:
↓ “positive” symptoms
2-Extrapyramidal effects:
Blockade of D2-R
Dystonias
Parkinson-like symptoms
Akathisia (motor restlessness)
Tardive dyskinesia

9. PHARMACOLOGICAL EFFECTS OF CHLORPROMAZINE
3-Antiemetic effects:
Blocking D2-R of CTZ
4-Anticholinergic effects:
Blurred vision, Dry mouth, Constipation, Urinary retention.
5-Blockade of α1-receptors
Orthostatic hypotension
6-Pitutary D2-receptor blockage
↑Prolactin release  Hyperprolactinemia
7-H1-receptor Blockage
Sedation

10. THERAPEUTIC INDICATIONS
A-PSYCHIATRIC USES
1-Schizophrenia: Primary indication for antipsychotics
2-Schizoaffective Disorders
3-Bipolar affective disorder
4-Acute bipolar depression
5-To control agitation with schizophrenia and bipolar disorder
6-Tourette’s Syndrome
7- Alzheimer’ disease

11. THERAPEUTIC INDICATIONS
B-NON-PSYCHIATRIC USES
1- Anti-emetic
Prochlorperazine
2- Pruritus
Chlorpromazine
3- Preoperative sedative
Promethazine
4- Neurolept analgesia
Droperidol + Fentanyl (Opioid)
5- Intractable hiccups Chlorpromazine

12. ADVERSE EFFECTS
A-Reversible neurologic effects
1-Dose-dependent EPS
2-Akathisia and dystonias
B-Tardive dyskinesia
C- Autonomic effects
Anticholinergic , α1 blockade
D-Endocrine and metabolic effects
1-↑Prolactin secretion (Typical)
2-Weight gain, hyperglycemia, hyperlipidemia (Atypical)

13. ADVERSE EFFECTS
E- Neuroleptic malignant syndrome
•Neuroleptic malignant syndrome (NMS) is a life-threatening idiosyncratic reaction
to antipsychotic drugs characterized by fever, altered mental status, muscle rigidity, and
autonomic dysfunction.
•Symptoms include very high fever (102 to 104 degrees F), irregular pulse, accelerated heartbeat
(tachycardia), increased rate of respiration (tachypnea), muscle rigidity, altered mental status,
autonomic nervous system dysfunction resulting in high or low blood pressure
F- Sedation
G-Miscellaneous toxicities
1-Retinal deposits (Visual impairment)
2-Prolong the QT interval
3- Agranulocytosis (1–2%)

14. COMAPRISON OF TYPICALAND ATYPICAL DRUGS
TYPICAL
1-Block D2 receptor
2-High Incidence of EPS
3-For positive symptoms only
4-↑ incidence of tardive dyskinesia
5-↑ prolactin secretion
6-↑ incidence of sexual
disturbances
7- Not effective in resistant cases
8-Non-psychiatric uses
ATYPICAL
1-Block 5HT-2 receptor
2-Low incidence of EPS
3-For positive and negative
symptoms
4-↓ incidence of tardive dyskinesia
5- Less effects on prolactin secretion
6- ↓incidence of sexual disturbances
7- Effective in resistant cases
(Clozapine)
8-No non-psychiatric uses