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• Antipsychotics are those psychotropic
drugs, which are used for the treatment of
psychotic symptoms. These are also
known as neuroleptics (as they produce
neurological side-effects),major
tranquilizers, D2-receptor blockers and
antischizophrenic drugs.
– Conventional
– Atypical
CLASSIFICATION:-
Class
Examples of
drugs
Trade name
Oral dose
mg/day
Parenteral
dose (mg)
Phenothiazines Chlorpromazine Megatil 300-1500 50-100
Largactil IM only
Tranchlor
Triflupromazine Siquil 100-400 30-60 IM only
Thioridazine Thioril, Melleril 300-800
Ridazin
Trifluoperazine Espazine 15-60 1-5 IM
Fluphenazine
decanoate
prolinate - 25-50 IM
every 1-3
weeks.
Thioxanthenes Flupenthixol Fluanxol 3-40
Butyrophenones Haloperidol Senorm, serenace 5-100 5-20 IM
Relinace
Class
Examples
of drugs
Trade name
Oral dose
mg/day
Parenteral
dose (mg)
Diphenylbutyl Pimozide Orap 4-20
Piperidines Penfluridol Flumap 20-60 weekly -
Indolic
derivatives
Molindone Mobam 50-225 -
Dibenzoxazepines Loxapine Loxapac 25-100 -
Atypical
antipsychotics
Clozapine Sizopin, lozapine 50-450 -
Risperidone Sizodon, sizomax 2-10 -
Olanzapine Oleanz 10-20 -
Quetiapine Qutan 150-750 -
Ziprasidone Zisper 20-80 -
Others Reserpine Serpasil 0.5-50 -
INDICATIONS
 Organic psychiatric disorders:
• Delirium
• Dementia
• Delirium tremens
• Drug-induced psychosis & other organic mental
disorders
 Functional disorders:
• Schizophrenia
• Schizoaffective disorders
• Paranoid disorders
 Mood disorders:
• Mania
• Major depression with psychotic symptoms
 Childhood disorders:
• Attention-deficit hyperactivity disorder
• Autism
• Enuresis
• Conduct disorder
 Neurotic & other psychiatric disorders:
• Anorexia nervosa
• Intractable obsessive- compulsive disorder
• Severe, intractable & disabling anxiety
 Medical disorders:
• Huntington‘s chorea
• Intractable hiccough
• Nausea & vomiting
• Tic disorder
• Eclampsia
• Heat stroke
• Severe pain in malignancy
• Tetanus
PHARMACOKINETICS
• Antipsychotics when administered orally are
absorbed variably from the gastrointestinal
tract, with uneven blood levels.
• They are highly bound to plasma as well as
tissue proteins. Brain concentration is
higher than the plasma concentration.
• They are metabolized in the liver, & excreted
mainly through the kidneys. The elimination
half-life varies from 10 to 24 hours.
• Most of the antipsychotics tend to have a
therapeutic window. If the blood level is
below this window, the drug is ineffective. If
the blood level is higher than the upper limit
of the window, there is toxicity or the drug is
again ineffective.
Mechanism of action
• Antipsychotic drug blocks D2 receptors in the
mesolimbic and mesofrontal systems. Sedation
is caused by alpha-adrenergic blockade. Anti-
dopaminergic actions on basal ganglia are
responsible for causing EPS. Atypical
antipsychotics have antiserotonergic (5-
hydroxytryptamine ) antiadrenergic and
antihistaminergic actions. These are therefore
called serotonin-dopamine antagonists.
ADVERSE EFFECTS OF
ANTIPSYCHOTICS
1. Extrapyramidal
symptoms (EPS)
i. Neuroleptic-induced parkinsonism
• Symptoms include
rigidity, tremors,
bradykinesia, stooped
posture, drooling,
akinesia, ataxia, etc.
The disorder can be
treated with
anticholinergic agents
ii. Acute dystonia
• Dystonic movements results from a slow sustained muscular
spasm that lead to an involuntary movement.
• Dystonia can involve the neck, jaw, tongue and the entire body
(opisthotonos). There is also involvement of eyes leading to
upward lateral movement of the eye known as oculogyric crisis.
• Dystonias can be prevented by anticholinergics,
antihistaminergics, dopamine agonists, beta-adrenergic
antagonists, benzodiazepines, etc.
iii. Akathisia
• Akathisia is a subjective feeling of muscular
discomfort that can cause patients to be
agitated, restless and feel generally dysphoric.
• Akathisia can be treated with propranolol,
benzodiazepines and clonidine.
iv. Tardive Dyskinesia
• It is a delayed adverse effect of antipsychotics. It
consists of abnormal, irregular choreoathetoid
movements of the muscles of the head, limbs and
trunk. It is characterized by chewing, sucking, grimacing
and peri-oral movements
V. Neuroleptic Malignant Syndrome
• This is a rare but serious disorder occurring in a
small minority of patients taking neuroleptics,
especially high-potency compounds.
• The onset is often, but not invariably, in the first
10 days of treatment. The clinical picture
includes the rapid onset (usually over 24-
72hours) of severe motor, mental and
autonomic disorders.
• The prominent motor symptom is generalized
muscular hypertonicity.
• Stiffness of the muscles in the throat and chest
may cause dysphasia, and dyspnea. The mental
symptoms include akinetic mutism, stupor or
impaired consciousness
• Hyperpyrexia develops with evidence of autonomic
disturbances in the form of unstable blood pressure,
tachycardia, excessive sweating, salivation, and urinary
incontinence.
• In the blood, Creatinine Phospho Kinase [CPK] levels
may be raised to very high levels, and the white cell
count may be increased. Secondary features may
include pneumonia, thromboembolism, cardiovascular
collapse, and renal failure.
• The syndrome lasts for one to two weeks after stopping
the drug.
2) Autonomic side-effects: Dry mouth,
constipation, cycloplegia, mydriasis, urinary
retention, orthostatic hypotension, impotence
and impaired ejaculation.
3) Seizures
4) Sedation
5) Other effects:
• Agranulocytosis (especially for clozapine)
• Sialorrhea or increased salivation (especially
for clozapine)
• Weight gain
• Jaundice
• Dermatological effects(contact dermatitis,
photosensitive reaction)
Side effects of Atypical
Antipsychotics
• Lower incidence of tardive dyskinesia, increase the risk
of cardiovascular disease, hyperglycemia & diabetes
• Impaired sexual performance with the main difficulties
being failure to ejaculate
• Abnormal menstrual cycles & infertility in females
• In both, the breast may become enlarged and a fluid
sometimes oozes from the nipples
• Risperidone & paliperidone cause a high increase in
prolactin levels
Nurse's Responsibility
• Instruct the patient to take sips of water frequently
• A high-fiber diet, increased fluid intake and
laxatives
• Advise the patient to get up from the bed or chair
very slowly.
• Differentiate between akathisia and agitation and
inform the physician.
• Observe the patient regularly for abnormal
movements.
• Take all seizure precautions.
• Patient should be warned about driving a car or
operating machinery when first treated with
antipsychotics.
• Advise the patient to use sunscreen measures
• A patient receiving clozapine is at risk for developing
agranulocytosis.
• Teach the importance of drug compliance, side-
effects of drugs
• Seizure precautions should also be taken as
clozapine reduces seizure threshold.
ANTIPSYCHOTICS.pdf

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ANTIPSYCHOTICS.pdf

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  • 2. • Antipsychotics are those psychotropic drugs, which are used for the treatment of psychotic symptoms. These are also known as neuroleptics (as they produce neurological side-effects),major tranquilizers, D2-receptor blockers and antischizophrenic drugs. – Conventional – Atypical
  • 3. CLASSIFICATION:- Class Examples of drugs Trade name Oral dose mg/day Parenteral dose (mg) Phenothiazines Chlorpromazine Megatil 300-1500 50-100 Largactil IM only Tranchlor Triflupromazine Siquil 100-400 30-60 IM only Thioridazine Thioril, Melleril 300-800 Ridazin Trifluoperazine Espazine 15-60 1-5 IM Fluphenazine decanoate prolinate - 25-50 IM every 1-3 weeks. Thioxanthenes Flupenthixol Fluanxol 3-40 Butyrophenones Haloperidol Senorm, serenace 5-100 5-20 IM Relinace
  • 4. Class Examples of drugs Trade name Oral dose mg/day Parenteral dose (mg) Diphenylbutyl Pimozide Orap 4-20 Piperidines Penfluridol Flumap 20-60 weekly - Indolic derivatives Molindone Mobam 50-225 - Dibenzoxazepines Loxapine Loxapac 25-100 - Atypical antipsychotics Clozapine Sizopin, lozapine 50-450 - Risperidone Sizodon, sizomax 2-10 - Olanzapine Oleanz 10-20 - Quetiapine Qutan 150-750 - Ziprasidone Zisper 20-80 - Others Reserpine Serpasil 0.5-50 -
  • 5. INDICATIONS  Organic psychiatric disorders: • Delirium • Dementia • Delirium tremens • Drug-induced psychosis & other organic mental disorders  Functional disorders: • Schizophrenia • Schizoaffective disorders • Paranoid disorders
  • 6.  Mood disorders: • Mania • Major depression with psychotic symptoms  Childhood disorders: • Attention-deficit hyperactivity disorder • Autism • Enuresis • Conduct disorder  Neurotic & other psychiatric disorders: • Anorexia nervosa • Intractable obsessive- compulsive disorder • Severe, intractable & disabling anxiety
  • 7.  Medical disorders: • Huntington‘s chorea • Intractable hiccough • Nausea & vomiting • Tic disorder • Eclampsia • Heat stroke • Severe pain in malignancy • Tetanus
  • 8. PHARMACOKINETICS • Antipsychotics when administered orally are absorbed variably from the gastrointestinal tract, with uneven blood levels. • They are highly bound to plasma as well as tissue proteins. Brain concentration is higher than the plasma concentration.
  • 9. • They are metabolized in the liver, & excreted mainly through the kidneys. The elimination half-life varies from 10 to 24 hours. • Most of the antipsychotics tend to have a therapeutic window. If the blood level is below this window, the drug is ineffective. If the blood level is higher than the upper limit of the window, there is toxicity or the drug is again ineffective.
  • 10. Mechanism of action • Antipsychotic drug blocks D2 receptors in the mesolimbic and mesofrontal systems. Sedation is caused by alpha-adrenergic blockade. Anti- dopaminergic actions on basal ganglia are responsible for causing EPS. Atypical antipsychotics have antiserotonergic (5- hydroxytryptamine ) antiadrenergic and antihistaminergic actions. These are therefore called serotonin-dopamine antagonists.
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  • 12. ADVERSE EFFECTS OF ANTIPSYCHOTICS 1. Extrapyramidal symptoms (EPS)
  • 13. i. Neuroleptic-induced parkinsonism • Symptoms include rigidity, tremors, bradykinesia, stooped posture, drooling, akinesia, ataxia, etc. The disorder can be treated with anticholinergic agents
  • 14. ii. Acute dystonia • Dystonic movements results from a slow sustained muscular spasm that lead to an involuntary movement. • Dystonia can involve the neck, jaw, tongue and the entire body (opisthotonos). There is also involvement of eyes leading to upward lateral movement of the eye known as oculogyric crisis. • Dystonias can be prevented by anticholinergics, antihistaminergics, dopamine agonists, beta-adrenergic antagonists, benzodiazepines, etc.
  • 15. iii. Akathisia • Akathisia is a subjective feeling of muscular discomfort that can cause patients to be agitated, restless and feel generally dysphoric. • Akathisia can be treated with propranolol, benzodiazepines and clonidine.
  • 16. iv. Tardive Dyskinesia • It is a delayed adverse effect of antipsychotics. It consists of abnormal, irregular choreoathetoid movements of the muscles of the head, limbs and trunk. It is characterized by chewing, sucking, grimacing and peri-oral movements
  • 17. V. Neuroleptic Malignant Syndrome • This is a rare but serious disorder occurring in a small minority of patients taking neuroleptics, especially high-potency compounds. • The onset is often, but not invariably, in the first 10 days of treatment. The clinical picture includes the rapid onset (usually over 24- 72hours) of severe motor, mental and autonomic disorders.
  • 18. • The prominent motor symptom is generalized muscular hypertonicity. • Stiffness of the muscles in the throat and chest may cause dysphasia, and dyspnea. The mental symptoms include akinetic mutism, stupor or impaired consciousness
  • 19. • Hyperpyrexia develops with evidence of autonomic disturbances in the form of unstable blood pressure, tachycardia, excessive sweating, salivation, and urinary incontinence. • In the blood, Creatinine Phospho Kinase [CPK] levels may be raised to very high levels, and the white cell count may be increased. Secondary features may include pneumonia, thromboembolism, cardiovascular collapse, and renal failure. • The syndrome lasts for one to two weeks after stopping the drug.
  • 20. 2) Autonomic side-effects: Dry mouth, constipation, cycloplegia, mydriasis, urinary retention, orthostatic hypotension, impotence and impaired ejaculation. 3) Seizures 4) Sedation
  • 21. 5) Other effects: • Agranulocytosis (especially for clozapine) • Sialorrhea or increased salivation (especially for clozapine) • Weight gain • Jaundice • Dermatological effects(contact dermatitis, photosensitive reaction)
  • 22. Side effects of Atypical Antipsychotics • Lower incidence of tardive dyskinesia, increase the risk of cardiovascular disease, hyperglycemia & diabetes • Impaired sexual performance with the main difficulties being failure to ejaculate • Abnormal menstrual cycles & infertility in females • In both, the breast may become enlarged and a fluid sometimes oozes from the nipples • Risperidone & paliperidone cause a high increase in prolactin levels
  • 23. Nurse's Responsibility • Instruct the patient to take sips of water frequently • A high-fiber diet, increased fluid intake and laxatives • Advise the patient to get up from the bed or chair very slowly. • Differentiate between akathisia and agitation and inform the physician. • Observe the patient regularly for abnormal movements. • Take all seizure precautions.
  • 24. • Patient should be warned about driving a car or operating machinery when first treated with antipsychotics. • Advise the patient to use sunscreen measures • A patient receiving clozapine is at risk for developing agranulocytosis. • Teach the importance of drug compliance, side- effects of drugs • Seizure precautions should also be taken as clozapine reduces seizure threshold.