New Mansoura University
Faculty of Pharmacy
Pharm D Program
Antipsychotics Drugs
Community Pharmacy
Clerkship I (PPP305)
First-Generation Antipsychotics (FGAs)
• Haloperidol (Haldol®)
• Mechanism of Action:
– High-potency D2 receptor antagonist
– Strong antipsychotic with minimal sedative and anticholinergic effects
• Dosage Forms:
Tablets, oral solution, IM injection, long-acting depot injection
• Dose Regimen:
– Oral: 1–15 mg/day
– IM (acute): 2–5 mg, may repeat every 4–8 hrs
– Depot: 50–200 mg every 4 weeks
• Administration:
– Oral or IM; depot for maintenance
• Precautions:
– High risk of extrapyramidal symptoms (EPS)
– QT prolongation, neuroleptic malignant syndrome (NMS)
– Sedation is low, suitable for agitated psychosis
• Brand Names in Egypt:
Halodol®, Haloperidol®
First-Generation Antipsychotics (FGAs)
• Chlorpromazine (Largactil®):
• Mechanism of Action:
– Low-potency D2 receptor antagonist
– Also blocks H1, M1, and alpha-1 receptors → more sedation, hypotension, anticholinergic
effects
• Dosage Forms:
Tablets, syrup, IM/IV injection
• Dose Regimen:
– Oral: 25–600 mg/day in divided doses
– IM: 25–50 mg every 4–6 hrs
• Administration:
– Oral or IM/IV in emergencies
• Precautions:
– High sedation, orthostatic hypotension, anticholinergic effects
– Moderate risk of EPS
• Brand Names in Egypt:
Largactil®, Chlorpromazine-EIPICO®
First-Generation Antipsychotics (FGAs)
• Fluphenazine :
• Mechanism of Action:
– High-potency D2 antagonist
– Similar to haloperidol but longer duration
• Dosage Forms:
Tablets, oral elixir, IM injection, depot (decanoate)
• Dose Regimen:
– Oral: 2.5–10 mg/day
– Depot: 12.5–50 mg IM every 2–3 weeks
• Administration:
– Oral or depot IM for long-term maintenance
• Precautions:
– High risk of EPS, tardive dyskinesia
– Monitor for movement disorders
• Brand Names in Egypt:
Fluphenazine Decanoate®, MOTIVAL ®
First-Generation Antipsychotics (FGAs)
• Trifluoperazine:
• Mechanism of Action:
– High-potency D2 receptor antagonist
– Used in psychosis and anxiety (low dose)
• Dosage Forms:
Tablets
• Dose Regimen:
– 5–15 mg/day for psychosis
– 1–2 mg/day for anxiety
• Administration:
– Oral
• Precautions:
– High EPS risk, akathisia, dystonia
– May elevate prolactin
• Brand Names in Egypt:
STELLASIL®, Trifluoperazine-EIPICO®
Second Generation Antipsychotics
• Risperidone (Risperdal®)
• Mechanism of Action:
– Antagonist of D2 and 5-HT2A receptors
– Modulates dopamine and serotonin pathways
• Dosage Forms:
Tablets, oral solution, IM depot injection
• Dose Regimen:
– Oral: 1–6 mg/day
– Depot: 25–50 mg IM every 2 weeks
• Administration:
– Oral once or twice daily; depot injection for maintenance
• Precautions:
– May cause hyperprolactinemia, weight gain, EPS (at high dose)
– Monitor glucose, lipids
• Brand Names in Egypt:
Risperdal®, Risdone®
Second Generation Antipsychotics
• Olanzapine
• Mechanism of Action:
– Blocks D2 and 5-HT2A receptors
– Also antagonizes H1, M1, and alpha-1 receptors
• Dosage Forms:
Tablets, orodispersible tablets, IM injection
• Dose Regimen:
– 5–20 mg/day orally
– IM: 10 mg for agitation (acute)
• Administration:
– Oral or IM; orodispersible useful for noncompliant patients
• Precautions:
– Significant weight gain, metabolic syndrome, sedation
– Avoid IM + benzodiazepine (risk of respiratory depression)
• Brand Names in Egypt:
Olapex®, Ranxapin®
Second Generation Antipsychotics
• Quetiapine (Seroquel®)
• Mechanism of Action:
– Antagonist of D2 and 5-HT2A
– Also blocks H1 (sedation) and alpha-1 (orthostasis)
• Dosage Forms:
Tablets (IR and XR)
• Dose Regimen:
– IR: 150–750 mg/day
– XR: 300–800 mg/day (usually once daily at bedtime)
• Administration:
– Oral; start low and titrate to reduce sedation
• Precautions:
– Sedation, weight gain, orthostatic hypotension
– Less EPS risk, often used in bipolar depression
• Brand Names in Egypt:
Seroquel®, Quitapex®
Second Generation Antipsychotics
• Aripiprazole :
• Mechanism of Action:
– Partial agonist at D2 and 5-HT1A receptors
– Antagonist at 5-HT2A
• Dosage Forms:
Tablets, oral solution, IM depot
• Dose Regimen:
– Oral: 10–30 mg/day
– Depot: 400 mg IM monthly
• Administration:
– Oral or IM; low risk of weight gain
• Precautions:
– Akathisia, insomnia, but minimal metabolic side effects
– Often used in depression augmentation
• Brand Names in Egypt:
Aripiprazole®, Aripiprex®
Second Generation Antipsychotics
• Clozapine :
• Mechanism of Action:
– D4 > D2 antagonist, strong 5-HT2A blockade
– Effective in treatment-resistant schizophrenia
• Dosage Forms:
Tablets
• Dose Regimen:
– Start: 12.5–25 mg/day → titrate up to 300–900 mg/day
• Administration:
– Oral only; monitor weekly CBC
• Precautions:
– Agranulocytosis (requires CBC monitoring), seizures, weight gain,
hypersalivation, myocarditis
• Brand Names in Egypt:
Clozapex®