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SADIA 
NOREEN 
ROLL # 09 
ADCP
ANTIPSYCHOTIC 
DRUGS 
(NEUROLEPTICS)
3 
SOME DEFINITIONS 
• Antipsychotics (also known as neuroleptics or major 
tranquilizers) are a class of medication used manage 
psychosis (including delusions, hallucinations, or 
disordered thought), in particular in schizophrenia and 
bipolar disorder, and are increasingly being used in the 
management of non-psychotic disorders (ATC code N05A). 
The word neuroleptic originates from the Greek 
word lepsis ("seizure" or "fit"). 
– Typical neuroleptic: older agents fitting this 
description 
– Atypical neuroleptic: newer agents: 
antipsychotic efficacy with reduced or no 
neurologic side effects
4 
Medical uses 
Schizophrenia 
 Bipolar disorder 
 Dementia 
 Unipolar Depression 
 Other
5 
All neuroleptics are equally 
effective in treating psychoses, 
including schizophrenia, but differ in 
their tolerability. 
All neuroleptics block one or more 
types of DOPAMINE receptor, but 
differ in their other neurochemical 
effects. 
All neuroleptics show a significant 
delay before they become effective. 
All neuroleptics produce significant 
adverse effects.
6 
GENERAL CHARACTERISTICS OF 
TYPICAL NEUROLEPTICS 
The older, typical 
neuroleptics are effective 
antipsychotic agents with 
neurologic side effects 
involving the 
extrapyramidal motor 
system. 
Typical neuroleptics 
block the dopamine-2 
receptor.
7 
Typical neuroleptics do not 
produce a general depression of the 
CNS, e.g. respiratory depression 
Abuse, addiction, physical 
dependence do not develop to 
typical neuroleptics.
8 
Typical neuroleptics are 
generally more effective 
against positive (active) 
symptoms of schizophrenia 
than the negative (passive) 
symptoms.
9 
Positive/active symptoms include 
thought disturbances, delusions, 
hallucinations 
Negative/passive symptoms 
include social withdrawal, loss of 
drive, diminished affect, paucity of 
speech. impaired personal hygiene
10 
THERAPEUTIC EFFECTS OF 
TYPICAL NEUROLEPTICS 
Relapse, recurrence of symptoms 
is common ( approx. 50% within 
two years). 
Noncompliance is common. 
Adverse effects are common.
ADVERSE EFFECTS OF TYPICAL 
• Anticholinergic (antimuscarinic) side 
effects: 
– Dry mouth, blurred vision, constipation, urinary 
11/02/14 
NEUROLEPTICS 
retention(release), impotence (power less) 
PELTON-C-2 Constellation 
Workshop-IID 11
12 
RECEPTOR BLOCKADE IN THE 
BASAL GANGLIA RESULTS IN 
EXTRAPYRAMIDAL MOTOR 
SIDE EFFECTS (EPS). 
DYSTONIA 
NEUROLEPTIC MALIGNANT 
SYNDROME 
PARKINSONISM 
TARDIVE DYSKINESIA
13 
Increased prolactin secretion 
(common with all; from 
dopamine blockade) 
Weight gain (common, 
antihistamine effect) 
Photosensitivity (v. common 
w/ phenothiazines) 
Lowered seizure threshold 
(common with all) 
Leucopenia (rare; w/ 
phenothiazines) 
Retinal pigmentopathy (rare; 
w/ phenothiazines
14
MECHANISMS OF ACTION 
OF TYPICAL NEUROLEPTICS 
DOPAMINE-2 receptor blockade 
in meso-limbic and meso-cortical 
systems for antipsychotic effect. 
DOPAMINE-2 receptor blockade 
in basal ganglia (nigro-striatal 
system) for EPS 
DOPAMINE-2 receptor 
supersensitivity in nigrostriatal 
system for tardive dyskinesia
LONG LONG TERM TERM EFFECTS EFFECTS OF OF D2 
D2 
RECEPTOR RECEPTOR BLOCKADE: 
BLOCKADE: 
Dopamine neurons reduce 
activity. 
Postsynaptic D-2 receptor 
numbers increase (compensatory 
response). 
When D2 blockade is reduced, 
DA neurons start again firing and 
stimulate increased no. of receptors 
tardive dyskinesia
MANAGEMENT OF EPS(extera 
pyramidalSymptoms) 
oDystonia and parkinsonism: anticholinergic 
antiparkinson drugs 
oNeuroleptic malignant syndrome: muscle 
relaxants, DA agonists, supportive 
oAkathisia:( an often distressing sense of inner 
restlessness). benzodiazepines, propranolol 
oTardive dyskinesia: increase neuroleptic dose; 
switch to clozapine
GENERAL CHARACTERISTICS OF 
ATYPICAL NEUROLEPTICS 
Effective antipsychotic agents with 
greatly reduced or absent EPS, esp. 
reduced Parkinsonism and tardive 
dyskinesia 
All atypical neuroleptics block 
dopamine and serotonin receptors; 
other neurochemical effects differ 
Are effective against positive and 
negative symptoms of schizophrenia; 
and in patients refractory to typical 
neuroleptics
Blockade of alpha-1 adrenergic 
receptors 
Blockade of muscarinic 
cholinergic receptors 
Blockade of histamine-1 
receptors
oSame therapeutic 
effectiveness 
oSame side effect 
profile
HYPOTHESIZED MECHANISMS OF 
ACTION OF ATYPICAL NEUROLEPTICS 
Combination of Dopamine-4 and 
Serotonin-2 receptor blockade in 
cortical and limbic areas. 
Combination of Dopamine-2 and 
Serotonin-2 receptor blockade (esp. 
risperidone)
Antipsychotics 
are prescribed one at a time. In 
cases in which single antipsychotics 
are tried alone, and when one of 
those three cases was Clozapine 
(Clozapine is usually used only in 
patients that have not responded to 
other anti-psychotic treatments ) if 
possible, then two antipsychotics 
may be prescribed at the same 
time.
•Thank 
s

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Anti-psychotic Drugs or neuroleptics slides

  • 1. SADIA NOREEN ROLL # 09 ADCP
  • 3. 3 SOME DEFINITIONS • Antipsychotics (also known as neuroleptics or major tranquilizers) are a class of medication used manage psychosis (including delusions, hallucinations, or disordered thought), in particular in schizophrenia and bipolar disorder, and are increasingly being used in the management of non-psychotic disorders (ATC code N05A). The word neuroleptic originates from the Greek word lepsis ("seizure" or "fit"). – Typical neuroleptic: older agents fitting this description – Atypical neuroleptic: newer agents: antipsychotic efficacy with reduced or no neurologic side effects
  • 4. 4 Medical uses Schizophrenia  Bipolar disorder  Dementia  Unipolar Depression  Other
  • 5. 5 All neuroleptics are equally effective in treating psychoses, including schizophrenia, but differ in their tolerability. All neuroleptics block one or more types of DOPAMINE receptor, but differ in their other neurochemical effects. All neuroleptics show a significant delay before they become effective. All neuroleptics produce significant adverse effects.
  • 6. 6 GENERAL CHARACTERISTICS OF TYPICAL NEUROLEPTICS The older, typical neuroleptics are effective antipsychotic agents with neurologic side effects involving the extrapyramidal motor system. Typical neuroleptics block the dopamine-2 receptor.
  • 7. 7 Typical neuroleptics do not produce a general depression of the CNS, e.g. respiratory depression Abuse, addiction, physical dependence do not develop to typical neuroleptics.
  • 8. 8 Typical neuroleptics are generally more effective against positive (active) symptoms of schizophrenia than the negative (passive) symptoms.
  • 9. 9 Positive/active symptoms include thought disturbances, delusions, hallucinations Negative/passive symptoms include social withdrawal, loss of drive, diminished affect, paucity of speech. impaired personal hygiene
  • 10. 10 THERAPEUTIC EFFECTS OF TYPICAL NEUROLEPTICS Relapse, recurrence of symptoms is common ( approx. 50% within two years). Noncompliance is common. Adverse effects are common.
  • 11. ADVERSE EFFECTS OF TYPICAL • Anticholinergic (antimuscarinic) side effects: – Dry mouth, blurred vision, constipation, urinary 11/02/14 NEUROLEPTICS retention(release), impotence (power less) PELTON-C-2 Constellation Workshop-IID 11
  • 12. 12 RECEPTOR BLOCKADE IN THE BASAL GANGLIA RESULTS IN EXTRAPYRAMIDAL MOTOR SIDE EFFECTS (EPS). DYSTONIA NEUROLEPTIC MALIGNANT SYNDROME PARKINSONISM TARDIVE DYSKINESIA
  • 13. 13 Increased prolactin secretion (common with all; from dopamine blockade) Weight gain (common, antihistamine effect) Photosensitivity (v. common w/ phenothiazines) Lowered seizure threshold (common with all) Leucopenia (rare; w/ phenothiazines) Retinal pigmentopathy (rare; w/ phenothiazines
  • 14. 14
  • 15. MECHANISMS OF ACTION OF TYPICAL NEUROLEPTICS DOPAMINE-2 receptor blockade in meso-limbic and meso-cortical systems for antipsychotic effect. DOPAMINE-2 receptor blockade in basal ganglia (nigro-striatal system) for EPS DOPAMINE-2 receptor supersensitivity in nigrostriatal system for tardive dyskinesia
  • 16. LONG LONG TERM TERM EFFECTS EFFECTS OF OF D2 D2 RECEPTOR RECEPTOR BLOCKADE: BLOCKADE: Dopamine neurons reduce activity. Postsynaptic D-2 receptor numbers increase (compensatory response). When D2 blockade is reduced, DA neurons start again firing and stimulate increased no. of receptors tardive dyskinesia
  • 17. MANAGEMENT OF EPS(extera pyramidalSymptoms) oDystonia and parkinsonism: anticholinergic antiparkinson drugs oNeuroleptic malignant syndrome: muscle relaxants, DA agonists, supportive oAkathisia:( an often distressing sense of inner restlessness). benzodiazepines, propranolol oTardive dyskinesia: increase neuroleptic dose; switch to clozapine
  • 18.
  • 19. GENERAL CHARACTERISTICS OF ATYPICAL NEUROLEPTICS Effective antipsychotic agents with greatly reduced or absent EPS, esp. reduced Parkinsonism and tardive dyskinesia All atypical neuroleptics block dopamine and serotonin receptors; other neurochemical effects differ Are effective against positive and negative symptoms of schizophrenia; and in patients refractory to typical neuroleptics
  • 20. Blockade of alpha-1 adrenergic receptors Blockade of muscarinic cholinergic receptors Blockade of histamine-1 receptors
  • 21. oSame therapeutic effectiveness oSame side effect profile
  • 22. HYPOTHESIZED MECHANISMS OF ACTION OF ATYPICAL NEUROLEPTICS Combination of Dopamine-4 and Serotonin-2 receptor blockade in cortical and limbic areas. Combination of Dopamine-2 and Serotonin-2 receptor blockade (esp. risperidone)
  • 23.
  • 24.
  • 25. Antipsychotics are prescribed one at a time. In cases in which single antipsychotics are tried alone, and when one of those three cases was Clozapine (Clozapine is usually used only in patients that have not responded to other anti-psychotic treatments ) if possible, then two antipsychotics may be prescribed at the same time.