ANTI PSYCHOTIC DRUGS

Prologue
Synonym: Neuroleptics, Major
tranquilizers, Ataractics,
These drugs are used primarily to treat
psychotics syndromes
This syndromes present difficulty in reality
testing ability. The symptoms include
Affected awareness
Affected judgment
Insight affected
 Also presents abnormality in normal mental
activity. This includes positive symptoms and
negative symptoms.
Positive symptoms:
Incoherence
Delusions
Hallucinations
Disorganized personality

Negative symptoms:
Minimal emotional response
Disturbed process of thought
Abulia
 Psychotic syndrome happens in the
following situations;
1. Sindrom Psikosis Fungsional :
Skizofrenia, Psikosis Paranoid, Psikosis
Afektif, Psikosis Reaktif Singkat

2. Sindrom Psikosis Organik :

Sindrom Delirium, Dementia, Intoksikasi
Alkohol
 Classification of the Drugs
The anti-psychotic drugs could be divided into five major
classifications based on the structure of the drug. This
classification is of modest importance, because within
each chemical group, different side chains have profound
effects on the potencies of the drug
Phenothiazines
Chlorpromazine
Fluphenazine
Prochlrperazine
Promethazine
Thioridazine
Benzisoxazoles
Risperidone
Dibenzodiazepines
Clozapine
Butyrophenones
Haloperidol
Thioxanthenes
Thiothixene
 However have been divide to the typical
anti psychotics and the atypical anti
psychotics.
Typical Phenothiazine, Butyrophenone,
Diphenyl-butyl-piperidine
Atypical Benzamide, Dibenzodiazipine
and Benzisoxazole

Typical Atypical
Pro extrapyramidal Lower expyramidal
side effects side effects
 Mode of Action
Dopamine receptor-blocking activity in brain
All neuroleptic drugs block dopamine receptors in
brain and periphery
Clinical efficacy correlates closely with ability to block
D2 receptor in mesolimbic syatem
Action of these drugs are antagonized by agents rise
dopamine concentration (e.g L-dopa)
Serotonin blocking activity in brain
The newer atypical drug appear to exert part of their
unique action through inhibition of serotonin receptors
(S)
Shows low incidence of extrapyramidal side effects
 Action of Drug
The antipsychotic actions of neuroleptic drug
reflect blockage at dopamine and/or serotonin
receptors. However many of these agents also
block cholinergic, adrenergic and histamine
receptors causing variety of side effects
Antipsychotic action
reduces hallucination and agitation associated with
SR by blocking dopamine receptors in mesolimbic
system
Extrapyramidal effects
blocking dopamine receptor parkinsonian
symptoms, akathisia and tardive dyskinesia
 Antiemetic effect
block D2 dopeminergic receptor of
chemoreceptor trigger zone of medulla
Antimuscarinic effects
particularly thioridazine and chlorpromazine
cause anticholinergic effects blurred vission,
dry mouth, sedation, confucion and inhibition
of GI and urinary smooth muscle leads to
constipation and urinary retention
Other effects
blockade of -adrenergic orthostatic
hypotension. Also alter temperature regulating
mechanism - poikilothermia
 Absorption and Metabolism
Shows variable absorption after oral
administration
Readily pass through brain, have large
volume of distribution, binds well with
plasma protein and metabolized to many
different substance in liver
Fluphenazine decanoate and haloperidol
decanoate are slow release formulations,
administered by IM
 Adverse Effect
Sedation and psychomotor inhibition
(drowsy, reduced alertness, cognitive ability reduces)
Extrapyramidal disturbances
(acute distonia, akathisia, parkinsonian effect tremor,
bradikinesia, rigidity)
Autonomic abnormalities
(hypotension, anticholergenic/parasympatolytic: dry
mouth, difficulty in urination and constipation, blurred
vision, increased intraocular pressure, distrubance in
heart rhythm)
Endocrine disturbances
(amenorrhoea, gynecomystia)
Hematologic agranulocytosis
Malignant Neuroleptic Syndrom
 Contraindication
Liver abnormalities hepatotoxic
Abnormalities in blood
Epilepsy
Abnormalities in heart
High febris
Alcohol dependency
Conscious disturbed patients caused by
CNSdepressant
 Drug Therapeutic notes
Haloperidol Little adrenergic or muscarinic effect.
Available as slow release depot form
Fluphenazine Available as slow release depot form

Thiothixene

Thioridazine Strong muscarinic antagonist

Chlorpromazine Used infrequently because of

adverse effects
Clozapine Few extrapyrmidal effects; causes a
potentially fatal agranulcytosis in 1-
2%
Risperidone Minimal sedation, low potential for
extrapyramidal effects
 Reference
Baldessarini R.J., Tarazi F.I. Pharmacotherapy of psychosis and
mania. In: Brunton, L.L., Lazo J.S., Parker K.L., editors. Goodman
and Gilmans the pharmacological basis of therapeutics, 11th
edition. USA: Mc Graw Hill; 2006.

Mycek M.J., Harvey R.A., Champe P.C. Lippincotts illustrated

reviews: Pharmacology, 2nd edition. Philadelphia: Lippincott
Williams and Wilkins; 1997.

Rusdi Maslim. Panduan praktis penggunaan klinis obat psikotropik,

3rd edition. Jakarta: BAgian Ilmu Kedokteraan Jiwa FK Unika Atma
Jaya; 2002.