2. 1.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
3. 2.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. 3.DEFINITION:
Antipsychotic drugs are a class of medicines
used to treat psychosis and other mental and
emotional conditions .
Antipsychotics are those psychotropics 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 anti schizophrenic drugs.
5. 4.Classification
:Class Examples
of
DRUGS
TRADE Name ORAL
Dose
mg/day
Parentera
l Dose
(mg)
Phenothiazines Chlorpromazin
e
Triflupromazine
Megatil
Largactil
Tranchlo
r Siquil
300-1500 mg
100- 400mg
50-100
IM only
30-60
IM only
Thioridazine Thioril, melleril
Ridazin
300-800mg
Trifluoperazine Espazine 15-60mg 1-5
IM only
Fluphenazin
e
prolinate -------- 25-50 IM every
1-3 weeks
6. CLASS Examples
of
DRUGS
TRADE
NAME
ORAL DOSE
mg/day
Parenter
al dose
(mg)
Thioxanthenes Flupenthixol Fluanxol 3-40 mg
Butyrophenones Haloperidol Senorm
,
serenac
e
5-100mg 5-20 IM
only
Relinace
Diphenylbutyl Pimozido Orap 4-20mg
Piperidines Penfluoridol Flumap 20-60 mg
weekly
Indolic derivatives Molindone Mobam 50-225 mg
Dibenzoxazepines Loxapine Loxapac 25- 100mg
Atypical
antipsychotics
Clozapine Sizopin ,
lozapin
50—450mg
8. 5.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. 6.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. 7.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
12. 7.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. 8.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 juiceand 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. • Observefor 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..
• Discontinueneuroleptic 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. 9.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
afte
r feeling well.
• Carry card or other Identification at all
times prescribed medication being
taken.