Anti Psychotic

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DRUGS USED FOR

TREATMENT PSYCHIATRIC
DISORDERS
(PSYCOTROPIC DRUGS)

Dr. TRULLY SITORUS, MSi


DEPARTMENT OF PHARMACOLOGY
& THERAPY
NEUROBEHAVIOUR SYSTEM
CASE
Mr X began haloperidol therapy for schizophrenia and
within several week developed bradykinesia, rigidity
and tremor
His psychosis were well controlled
What
Whatisisthe
themechanism
mechanismof ofaction
action
of
ofhaloperidol?
haloperidol?
Why
Whyhaloperidol
haloperidolcan
cancontrol
control
schizophrenia?
schizophrenia?
Why
Whyhe hegot
gotbradykinesia,
bradykinesia,rigidity
rigidity
and
andtremor?
tremor?
How
Howto tohandle
handlethe
theproblem?
problem?
Should
Shouldititchange
changeto toothers
othersdrugs?
drugs?
SCHIZOPHRENIA
Is a psychotic illness characterized by multiple
symptoms affecting thought preceptions and
emotion

The symptoms of SZ is divided to :


 Positive symptom

 Negative symptom
Symptoms of SZ
POSITIVE SYMPTOMS
• hallucinations
• Delusions
• Thought disorders
•Bizzare behaviour

NEGATIVE SYMPTOMS
• Poverty of speech
Which is a restrictions in the amount of spontaneous speech
• Flatteing of affect (Loss of normal expression of emotion)
• Social withdrawal
•Apathy (reduced drive, energy and interest)
• Attention deficit
PATHOGENESIS OF SZ
Hypothesis :
Neurotransmitter alternation in mesolimbic
and mesocortical areas

neurotransmitter

: dopamine
5 HT
NE
glutamate
Mechanism of action of SZ-drugs

SZ
D D D
S
S D
Drugs S S D D D
D Drugs
block block
Serotonin dopamine
Receptor receptor

Symptom
DRUGS USED FOR TREATMENT SZ
Precipitate F Non pharmacologist
How
Howtoto
treat
treatthe
the dopamine
dopamine
SZ
SZ Drugs :
others
others Dopamine antagonist

Psychotropic drugs
Neuroleptic drugs

Positive symptoms
Negative symptoms
PSYCHOTROPIC DRUGS/NEUROLEPTIC DRUGS
Class Chemical Examples
Classification
Typical Phenothiazines Chlorpromazines
Anti P Thioridazines
Fluphenazines
Butyrophenones Haloperidol
Thioxanthines Flupentixol
Atypical Dibenzodiazepin Clozapine
Olanzapine

A Psychosis Bensisoxazole Risperidone


EFFECTS
1. Antipsychotic actions
(blocking dopamin receptor in the mesolimbic
system)
 Hallucinations
 Agitation
 Sedation
 Spontaneous physical movement
Onset of action: several weeks
Do not depress intellectual function and motor
incoordination is minimal
3. Antiemetic effects
(blocking D2 dopaminergic
receptor of the CTZ of the medulla)
SIDE EFFECT OF PSYCHOTROPIC
DRUGS

Why
Why
the
theSE
SE
occurs?
occurs? The
Thedrugs
drugs
!! 1.
1. Interact
Interactwith
withDD
receptor
receptor in
in
others
othersarea.
area.
2.
2. Interact
Interactwith
with
others
others
neurotransmitte
neurotransmitte
rr
DISTRIBUTION OF DOPAMINE
Why
Why the
theSE
SE
occurs?!
occurs?!

II. NIGROSTRIATAL
Coordinate of
voluntary system
I. MESOLIMBIC :
Behaviour
Emotion III.TUBEROIFUNDI
BULUM
Memory
Prolactin
Communication secretion
DRUGS INTERACT WITH OTHERS
NEURROTRANSMITTER RECEPTORS
Why
Why
the
theSE
SE
occurs?
occurs?
!!
Why
Why the
theSE
SE
occurs?!
occurs?!

Psychotropic drugs

Dopamine Serotonin
α Adrenergik Muscarinik Histamine
receptor receptor
Clinical Extra Sedative Hypotensive
potency pyramidal
Chlorpromazine Low Medium High High

Fluphenazine High High Low Very low

Thioridazine High Medium Medium Medium

Haloperidol High Very High Low Very low

Clozapine Medium Very low Low Medium

Olanzapine High Very low Medium Low

Risperidon High Low low Low


INDICATION

I. Treatment of Schizophrenia
The neuroleptics are the only efficacious
treatment for SZ
 Typical. Are the most effective in treating positive
symptom of SZ
 Atypical. Are effective in many patient resistant to the
traditional drugs (typical) especially in treating
negative symptom of SZ
II. Prevention of severe and vomiting
 Neuroleptics are useful in the treatment of drugs-
induced nausea. (Chemotherapy for cancer)
DRUGS USED IN MOOD
DISORDERS

Dr. TRULLY SITORUS, MSi


DEPARTMENT OF PHARMACOLOGY
& THERAPY
NEUROBEHAVIOUR SYSTEM
MOOD DISORDERS
Depression :
Present as depressed mood
diminished interest in normal activities
Anorexia
Fatique
Inability to concentrate
Manic :
Characterized by expansive mood.
Inflated self esteem
Pressured speech
Flight of ideas
Insomnia
 Seorang pengacara berusia 42 th. Datang dengan
keluhan utama episode sesak nafas yang sering
timbul dan palpitasi, pada saat serangan dia merasa
mual (nausea) dan berkeringat. Serangan ini makin
sering timbul beberapa bulan terakhir ini. Gejalanya
tidak berkaitan dengan aktivitas fisik, dan cenderung
menghilang dalam beberapa menit. Pada saat itu, dia
merasa sangat takut dan mengira dia mengalami
serangan jantung.
 Pada pemeriksaan, dia terlihat kurus, letih dan agitasi.
Karena berada dalam tekanan pekerjaan, dia
mengalami gangguan tidur dan sulit berkonsentrasi.
Suasana hatinya terasa murung dan cemas mengenai
penyebab dari serangan ini. Dia tidak memiliki
keinginan untuk bunuh diri secara aktif, namun
terkadang dia berfikir kalau keluarganya akan lebih
baik tanpa dia.
PATHOGENESIS

DEPRESSION
Serotonin
Serotonin
NE
NE
Dopamine
Dopamine

Drugs that increase


serotonin
concentration

Symptom
ANTIDEPRESSAN DRUGS

1. Tricyclic antidepressants (TCAs)


Amitriptyline
Imipramine
Others
2. Selective serotonin reuptake inhibitors (SSRIs)
Fluoxetine
Sertaline
Others
3. MAOIs
Isocarboxazid
MECHANISM OF ACTION
TRICYCLIC ANTIDEPRESANTS

 Mechanism of action
1. TCAs inhibit the neuronal reuptake of
norepinephrine, and serotonin into
presynaptic nerve terminals.
2. Block of the receptor :

Serotonin α adrenergic, histamine,


muscarinic.
UPTAKE INHIBITION RECEPTOR AFFINITIES
DRUG
Histaminergi
Norepinephrine Serotonin Muscarinic Adrenergic
c

TCA ++ +++ ++ + +

SSRI 0 ++++ 0 0 0
THE ONSET OF TCA EFFECT

• Narrow therapeutic range


• Steady state achieve in 2-3 week
• The onset effect : 2-3 week
SSRIs
Mechanism of action
 Inhibition of Serotonin uptake into
presynaptic nerve terminal
Indication
 Depression :

Bulimia nervosa, obsesive-compulsive


disorders, anorexia nervosa, panic
disorder, premenstrual syndrome
TRICYCLIC ANTIDEPRESANTS

 Pharmacokinetics
Fluoxetine is a potent inhibitor of a cyt-P-
450 enzyme, metabolism other drug will
decrease.

The drugs usually give once daily in the


morning
MONOAMINE OXIDASE INHIBITOR
 Mechanism of action
Block the action of enzyme that metabolize
(degrade) monotransmitter (5HT N A
Dopamine)
The monoamine will increase
 Indication
 For depressed patients who are Unresponsive or
allerrgic to other drugs
 For depressed patient who have strong anxiety
SE :
Drowsiness, orthostatic hypotension, blurred vision,
dryness of the mouth, dysuria, constipation
TREATMENT OF BIPOLAR AFFEVTIVE
DISORDERS (BPAD)
 BPAD is characterized by Bdepression and
mania we called as manic-depressive
disorders

 Drug for treatment HB-disorders :

I. Litium
II. Carbamazepine
Gabapentine
LITHIUM SALT

The mechanism of action is unknown.

Hypothesis :
Li act by altering the cellular
concentration of IP3.

The therapeutic range is very narrow.

Side effect : Ataxia, tremors, confusion,


and convulsion
Takut mati
Takut hilang kontrol
Takut pinsan
Takut menjadi gila
Pusing Depersonalisasi
Pucat / derealisasi
Tenggorokan
terasa tersumbat
Nyeri dada Palpitasi

Mual/nausea Semburat dingin/


panas
Mulas, ingin defekasi
Sweating
Gemetar
Terasa tertusuk
jarum

Tungkai terasa
lemas
ANTIPSYCHOSIS TEST

A. Dopamine mesolimbic 1. Movement disorders


B. Dopamine tubero In 2. Infertility
C. Dopamine nigrostriatal 3. Amenorrhoea
4. Hypotensi orthostatic
D. α1 adrenergik
5. Sedation
E. Muscarinic 6. Parkinsonism
F. Histamine (Extrapyramidal)
7. Constipation
8. Gynecomastia
9. Tardive dyskinesia
10. Dry mouth
1. Amytriptilin A. Hypotensi orthostatic
2. Fluoxetine B. Extrapyramidal
3. Halloperidol disorders
4. Olanzapine C. Dry mouth,
5. Trihexyphenidil constipation
D. SSRIs
E. Anticholinergic
PATHOGENESIS OF SZ
D D D
Normal
S S

No symptom

sz
D D

D D D D D

S S S S

Positive Negative
Symptom Symptom
*EFFECT – SIDE EFFECT
RESPONS OF AP DRUGS

EFFECT SIDE EFFECT


(Primary effect) (secondary effect)

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