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Antipsychotic Drugs

1) Dopamine receptor antagonists/ typical antipsychotic


Example: Haloperidol (Haldol), chlorpromazine (Largactil), trifluoperazine, sulpiride
Indications: second-line drugs for schizophrenia and other psychotic disorder.
Mechanism of action:
- Block the dopamine receptor subtype selectively (D2>D1)
- Also block the muscarinic, α1 adrenoceptor, 5-HT and histamine receptors. -> side effects

Effects:

- Block the mesolimbic and mesocortical pathway - ↓dopamine binds on D2( antipsychotic)
 ↓agitation
 ↓ paranoid idea
 ↓hallucination
 ↓ anxiety
 Mood stabilizer

Side effects:

i) Extrapyramidal symptoms (Parkinsonism, dystonia, akathisia, neuroleptic malignant syndrome)


Block the nigrostriatal pathway.
ii) Anticholinergic and antiadrenergic effects ( eg: dry mouth, constipation, blurred vision, urinary
retention, tachycardia)- 10-50%
iii) Metabolic and endocrine – block tuberoinfundibular ( inhibit PIH -> hyperprolactinemia)
Eg: weight gain, amenorrhea-galactorrhea, impotence, infertility, gynaecosmatia
iv) Sedation – 70-80%
v) Tardive dyskinesia

Dopaminergic system:

1) Tuberoinfundibular : regulation of prolactin secretion.


2) Nigrostriatal : motor coordination
3) Mesolimbic →emotion
4) Mesocortical →behaviour

2) Serotonin – dopamine antagonists (SDAs, Atypical antipsychotic drugs)


Mechanism of action:
- Block the both dopamine and serotonin receptors.
- * Risperidone – had higher affinity for D2 receptor than the others.

Common side-effects:

- Neuroleptic malignant syndrome (eg: muscular rigidity, fever, delirium, dystonia, akinesia, mutism,
diaphoresis, dysphagia, tremor, incontinence, labile blood pressure, leukocytosis and elevated creatine
phosphokinase)
 Tx: muscle relaxant. (eg: dantrolene, diazepam)
- Tardive dyskinesis ( repetitive, involuntary facial and limb movement)

Drug Pharmacokinetic Mechanism of Indications Side-effects


action
1)Risperidone i) tablet D2 = 5-HT 1) Schizophrenia Low dose:
(Risperdal) - T1/2 ~ 20hrs Improve : 1.insomnia
- OD - +ve symptoms 2.anxiety
- starting dose 3. dizziness
(hallucinations, delusions,
= 1mg 4. N&V
- maintenance disorganized thought, 5.dyspepsia and constipation
dose= 2-6mg agitation) High dose:
- max = 16mg - -ve symptoms (withdrawal, 1.Sedation
flat affect, 2.orthostatic hypotension
ii) IM Depo anhedonia,catatonia) 3. weight gain
-1x/2 weeks - cognitive impairment 4. sexual dysfunction
- starting dose 5. Hyperglycemia
=25mg (perceptual distortion, 6. dosage-dependent
-max = 50mg memory deficits, extrapyramidal effects
2)Olanzapine -tablet 5-HT >D1=D2 inattentiveness) 1. sedation
(Zypnexa) - T1/2 ~ 30hrs =α1 2. orthostatic hypotension
2) Schizophreniform disorder
- OD 3. weight gain
3) Schizoaffective disorder
- starting dose= 5- 4. sexual dysfunction
10mg 4) delusional disorder 5. hyperglycemia
-maintenance= 5) brief psychotic disorder 6. Extrapyramidal effects
10-20mg 6) manic episode
-max=20mg/day 7) MDD with psychotic
* in schizo and features
bipolar mania pt,
normally used 10-
15mg.
3)Quetiapine -tablet 1.somnolence
(Seroquel) - T1/2 ~ 6 hrs 2. dry mouth
- BD 3. postural hypotension
- starting dose= 4. dizziness
25mg BD 5. transient weight gain
-max=800mg/day 6. ↑ liver transaminase

4)Aripiprazole tablet 1.headache


(Abilify) - T1/2 ~ 75hrs 2. N&V
- OD 3. insomnia
- starting dose= 4. lightheadedness
10-15mg 5. somnolence
-maintenance=
10-30mg
-max=30mg/day

5) Clozapine tablet D4=α1 >5- 1.Sedation


(Clozaril) - T1/2 ~ 30hrs HT>D2=D1 2. weight gain
- OD 3. hypersalivation
- starting dose= 5- 4. tachycardia
10mg *clozapine is used when 5. orthostatic hypotension
-maintenance= there is drug-resistant. ( at 6. seizure, 3%
10-20mg least 2 courses of drugs) 7. agranulocytosis, <1%
-max=20mg/day *cannot be used together with
carbamazepine(Tegretol) or
drugs that cause BM
suppression.

*Maintenance monitoring for SDAs- weight, waist circumference, blood pressure, fasting blood glucose, fasting
serum lipid.

*pt started on clozapine – first 18 weeks = FBC weekly; subsequently= FBC monthly.