2. • HISTORY:
• In 1891 , paul ehrlich observed the antimalarial effects
of methylene blue , a phenothiazine derivative .
• Later , the phenothiazines were developed for their
antihistaminergic properties .
• Hamon and Delay extended the use of this treatment
in psychiatric patients and uncovered its antipsychotic
activity .
• Between 1954 and 1975 about 15 antipsychotics drugs
were introduced in U.S and about 40 throughout the
world .
3. • INTRODUCTION :
Antipsychotics also known as neuroleptics or
major tranquilizers are a class of medications
primarily used to manage psychosis principally
in schizophrenia and bipolar disorder .
First generation antipsychotics known as
Typical antipsychotics were discovered in the
1950s .
Second generation drugs known as Atypical
antipsychotics, first atypical antipsychotics was
discovered in 1960s and introduced clinically in
the 1970s .
4. • DEFINITION:
Antipsychotic drugs are a class of medicines
used to treat psychosis and other mental and
emotional conditions .
5. • Classification :
Class Examples of
DRUGS
TRADE Name ORAL Dose
mg/day
Parenteral
Dose (mg)
Phenothiazines Chlorpromazine
Triflupromazine
Thioridazine
Trifluoperazine
Fluphenazine
decanoate
Megatil
Largactil
Tranchlor
Siquil
Thioril, melleril
Ridazin
Espazine
prolinate
300-1500 mg
100- 400mg
300-800mg
15-60mg
--------
50-100
IM only
30-60
IM only
1-5
IM only
25-50 IM every
1-3 weeks
7. CLASS EXAMPLES OF
DRUGS
TRADE
NAME
ORAL DOSE
(mg/day)
Parenteral
dose (mg)
Others
Risperidone
Olanzapine
Quetiapine
Ziprasidone
Reserpine
Sizodon,
sizomax
Oleanz
Qutan
Zisper
Serpasil
2-10mg
10-20mg
150-750mg
20-80mg
0.5-50mg
8. • Indications:
• Antipsychotics are mainly used in the treatment of
acute and chronic psychosis ,particularly when
accompanied by increased psychomotor activity.
a) Organic psychiatric disorder:
delirium, Dementia, Delirium tremens, etc
b) Functional disorders:
schizophrenia, schizoaffective disorders,etc
c) Mood disorders:
mania , major depression with psychotic
symptoms
9. • Childhood disorders:
Attention-deficit hyperactivity disorder,
autism.
• Neurotic and other psychiatric disorders:
Anorexia nervosa , intractable OCD , disabling
anxiety .
• Medical disorders:
Huntingtons chorea, nausea and vomiting,
eclampsia, heat stroke.
10. • Pharmacokinetics:
• Antipsychotics when administered orally are
absorbed by gastrointestinal tract with uneven
blood levels.
• They are highly bound to plasma as well as tissue
proteins .
• They are metabolized in the liver and excreted
mainly through the kidneys .
• The elimination half life varies from 10-24 hrs.
11. • Mechanism of action:
• Antipsychotic drugs block 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 (extrapyramidal
symptoms).
• Atypical antipsychotics have anti-serotonergic
anti-adregenic and antihistamine actions .
12. • Contraindications:
• Hypersensitivity(cross sensitivity may exist
among phenothiazines).
• Not to be used when CNS depression is
evident when blood dyscrasias exist , in
patients with parkinson” s disease , liver, renal
or cardiac insufficiency.
• elder, severely ill or respiratory insufficiency,
prostatic hypertrophy, or intestinal
obstruction
13. • Side effects and nursing implications:
1) Anticholinergic effects :
a) Dry mouth-
• provide sugarless candy , ice and frequent sips of
water.
• strict oral hygiene.
b) Blurred vision:
• subsides within few minutes.
• don’t drive.
• clears small items from pathways.
14. c) Constipation:
• Increase fluid intake , higer fiber diet ,
increased physical activity.
d) Urinary retention:
• Monitor intake and output ,report to if
difficulty while urinating .
2) Nausea ,gastrointestinal tract:
Administer fruit juice and concentrate must
be diluted with other liquids.
15. 3) Skin rash :
• Report appearance of any skin rash
avoid spilling of liquid concentrate on skin.
4) Sedation :
• Administer drug at bedtime.
• Don’t drive or work while drowsy or after
using sedatives
• Low dosage.
16. 5) Orthostatic hypertension:
• Rise slowly from a lying or sitting position,
monitor BP document and report if any
changes.
6) Photosensitivity:
• Wear protective sunscreens, clothing and
sunglasses while spending time outdoors.
18. 8) Reduction of seizure threshold:
• Close observation of patient with history of
seizure.
Note : THIS IS IMPORTANT WITH PATIENTS TAKING
CLOZAPINE. REPORTEDLY SEIZURES AFFECT 1% TO 5% OF
INDIVIDUALS WHO TAKE THIS DRUG.
9) Agranulocytosis:
• Relatively rare with most of the
antipsychotics drugs.
• usually occurs within the first 3 months
of RX
19. • Observe for symptoms of sore throat fever and
malaise.
• Monitor CBC if symptoms appear.
10) Extrapyramidal symptoms:
a) Pseudo-parkinsonism :
(tremor, shuffling gait, drooling, rigidity).
&
b) Akinesia(muscular weakness):
• Symptoms may appear 1to5 days following
initiation of antipsychotic medication.
• occurs most often in women ,the elderly and
dehydrated patients.
20. c)Akathesia (continuous restlessness and fidgeting):
• occurs most frequently in women ; symptoms
may occur 50-60 days following initiation of
therapy.
d) Dystonia (involuntary muscular movements[spasms] of face,
arms , legs and neck):
• occurs most often in men and patients younger
than 25 years of age .
21. 11) Tardive dyskinesia (bizarre facial and tongue
movements, stiff neck and difficulty swallowing):
• Long term therapy patients are at risk.
• Symptom are potentially irreversible.
• Drug should be withdrawn at first sign(vermiform
movements of tongue)
12) Neuroleptic malignant syndrome:
• A rare, but potentially fatal, complication with
neuroleptic drugs.
• monitor temperature and observation for
parkinsonian symptoms.
22. • Onset can occur within hours or even years after drug
initiation.
• Symptoms include severe parkinsonian muscle rigidity ,
hyperpyrexia upto 107 degree F ,tachypnea,
tachycardia , fluctuations in blood pressure ,rapid
deteriiration of mental status..
• Discontinue neuroleptic medicaton immediately.
• Monitor vital signs , degree of muscle rigidity, intake
and output and level of consciousness.
• Physician may order bromocriptine(parlodel) or
dantrolene (dantrium) to counteract the effects.
23. • Patient/Family Education:
= Patient should:
• Be cautious while driving and operating dangerous
machinery.
• Don’t stop medication after long time use.
• use sunscreens and wear protective clothing while
spending time outside.
• Report occurrence of symptoms like sore throat, severe
headache , rapid heart rate, difficulty in urinating,
twitching tremors, darkly coloured urine ,yellow skins
or eyes , skin rash or seizures.
24. • Rise slowly from sitting position to prevent
sudden drop in BP.
• Take frequent sips of water , chew sugarless gum
and maintain oral hygiene.
• Consult physician regarding smoking while on
neuroleptic therapy.
• Dress warmly in cold weather and avoid extended
exposure to very high or low temperature. Body
temperature is harder to maintain with this
medications.
25. • Stop alcohol.
• Don’t consume other medications, without physician
approval.
• Beware of risks with neuroleptic during pregnancy.
• Beware of side effects of neuroleptic drugs.
• Don’t discontinue medications immediately after
feeling well.
• Carry card or other Identification at all times
prescribed medication being taken.