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ANTIPSIKOTIK

Apakah obat-obat
antipsikotik itu?
Obat-obat antipsikotik ialah obatobatan yang digunakan untuk
mengobati jenis gangguan jiwa yang
disebut gangguan psikotik.

Apakah gangguan psikotik


itu?
Gangguan psikotik adalah gangguan jiwa yang
memengaruhi cara orang berpikir, merasa dan
berperilaku.
Para penderita gangguan psikotik mungkin
memiliki kesulitan mengenali apa yang
sebenarnya terjadi dan apa yang sebenarnya
tidak terjadi.
Gejala gangguan psikotik dialami oleh
penderita gangguan bipolar, depresi, psikosis
yang berkaitan dengan penggunaan narkoba
dan skizofrenia.

Jenis-Jenis Psikosis
a. Psikosis Organik
adalah penyakit jiwa yang disebabkan oleh faktor-faktor fisik atau
organik, yaitu pada fungsi jaringan otak, sehingga penderita
mengalamai inkompeten secara sosial, tidak mampu bertanggung
jawab, dan gagal dalam menyesuaikan diri terhadap realitas. Contoh
psikosis jenis ini adalah : Alcoholic psychosis, Drug psychose,
Traumatic psychosis, Dementia paralytica.

b. Psikosis Fungsional
Psikosis fungsional merupakan penyakit jiwa secara fungsional yang
bersifat nonorganik, yang ditandai dengan disintegrasi kepribadian
dan ketidak mampuan dalam melakukan penyesuaian sosial. Psikosis
jenis ini dibedakan menjadi beberapa ., yaitu : schizophrenia, psikosis
mania-depresif, dan psiukosis paranoid (Kartini Kartono, 2000 : 106).

ANTIPSIKOTIK
1. tipikal
merupakan obat antipsikotik lama.
2. Atipikal
merupakan obat antipsikotik baru.

Mekanisme Kerja
Semua obat anti-psikosis merupakan obat-obat
potensial dalam memblokade reseptor dopamin dan
juga dapat memblokade reseptor kolinergik,
adrenergik dan histamin
Pada obat generasi pertama (fenotiazin dan
butirofenon), umumnya tidak terlalu selektif,
sedangkan benzamid sangat selektif dalam
memblokade reseptor dopamine D2.
Anti-psikosis atypical memblokade reseptor
dopamine dan juga serotonin 5HT2 dan beberapa
diantaranya juga dapat memblokade dopamin
sistem limbic, terutama pada striatum.

Antipsikotik tipikal
1. Phenothiazine
rantai aliphatic : Chlorpromazine
rantai
piperzine :Perphenazine,Trifluoperazi
ne Fuphenazine
rantai piperidine : Thioridazine
2. Butyrophenone : Haloperidol
3. Diphenyl-butyl-piperidine : Pimozide

Antipsikotik Atipikal
1. Benzamine : Amilsupride
2. Dibenzodiazepin : Clozapine,
Olanzapine, Quetapine, Zotepine
3. Benzosoxazole : Risperidon,
Aripirazole

Efek samping
1. Extrapiramidal:
distonia akut, parkinsonism, akatisia,
dikinesia tardiv
2. Endokrin:
galactorrhea, amenorrhea
3. Antikolinergik: hiperprolaktinemia

Kontra indikasi

Penyakit hati
penyakit darah
epilepsi
kelainan jantung
febris yang tinggi
ketergantungan alkohol
penyakit SSP dan
gangguan kesadaran

INTERAKSI OBAT

Antipsychotics + Antacids or
Sucralfate
Antacids containing aluminium/magnesium hydroxide or
magnesium trisilicate can reduce the serum levels of
chlorpromazine which would be expected to reduce the
therapeutic response. Sucralfate and an aluminium/magnesium
hydroxide antacid can reduce the absorption of sulpiride. In vitro
studies suggest that this interaction may possibly also occur
with other antacids and phenothiazines. There seem to be no
clinical studies or reports confirming the anecdotal evidence of a
possible reduction in the effects of haloperidol by antacids.
Mechanism
Chlorpromazine and other phenothiazines become adsorbed
onto these antacids,3,6 which would seem to account for the
reduced bioavailability. It is possible that adsorption also occurs
with sulpiride, but this has not been proven.

Antipsychotics +
Antiepileptics
Haloperidol plasma levels are roughly halved
by carbamazepine, phenobarbital and
phenytoin. Bromperidol, fluphenazine and
tiotixene levels are also reduced by
carbamazepine. The plasma levels of
chlorpromazine and haloperidol do not appear
to be affected by oxcarbazepine. Neurotoxicity
has been seen with haloperidol and
carbamazepine and haloperidol can raise
serum carbamazepine levels. Valproate or
valproic acid appear not to interact.

Antipsychotics +
Antiepileptics
Mechanism
Carbamazepine, phenobarbital and
phenytoin are recognised enzyme inducers,
therefore it seems highly likely that the
reduced plasma bromperidol, chlorpromazine
and haloperidol levels occur because their
metabolism by the liver is markedly increased
by these antiepileptics. Oxcarbazepine does
not appear to interact, probably because it is
not an enzyme inducer.

Antipsychotics +
Antimuscarinics
Antipsychotics and antimuscarinics are very
often given together advantageously and
uneventfully, but occasionally serious and
even life-threatening interactions occur.
These include heat stroke in hot and humid
conditions, severe constipation and adynamic
ileus, and atropine-like psychoses.
Antimuscarinics used to counteract the
extrapyramidal adverse effects of
antipsychotics may also reduce or abolish
their therapeutic effects.

Antipsychotics +
Antimuscarinics
Mechanism
Antimuscarinic (anticholinergic) drugs inhibit the parasympathetic nervous
system, which innervates the sweat glands, so that when the ambient
temperature rises the major body heat-losing mechanism can be partially or
wholly lost.28 Phenothiazines, thioxanthenes and butyrophenones may also have
some antimuscarinic effects, but additionally they impair to a varying extent the
hypothalamic thermoregulatory mechanisms that control the bodys ability to
keep a constant temperature when exposed to heat or cold. Thus, when the
ambient temperature rises, the body temperature also rises. The tricyclics can
similarly disrupt temperature control. Therefore in very hot and humid
conditions, when the need to reduce the temperature is great, the additive
effects of these drugs can make patients unable to control their temperature,4
which can be fatal. Antimuscarinic drugs also reduce peristalsis, which in the
extreme can result in total gut stasis. Additive effects can occur if two or more
antimuscarinic drugs are taken. The toxic psychoses described resemble the CNS
effects of atropine or belladonna poisoning and appear to result from the additive
effects of the drugs used. The mechanism for antipsychotic antagonism is not
understood. Animal studies suggest that the site of interaction is in the gut.19

Antipsychotics +
Bromocriptine
The concurrent use of bromocriptine
with antipsychotics can be
successful. However, one report
describes the re-emergence of
schizophrenic symptoms in a patient
when bromocriptine was added to
treatment with molindone and
imipramine. Another case reports a
rise in prolactin levels and
deterioration of vision when

Antipsychotics + Coffee or
Tea
Tea and coffee can cause some drugs
to precipitate out of solution in vitro,
but so far there is no clinical
evidence to show that this normally
affects the bioavailability of the
drugs nor that it has a detrimental
effect on treatment.

Antipsychotics + Lithium
Chlorpromazine levels can be
reduced to subtherapeutic
concentrations by lithium. The
development of severe
extrapyramidal adverse effects or
severe neurotoxicity has been seen
in one or more patients given lithium
with various antipsychotics
Sleepwalking has been described in
some patients taking

Antipsychotics + Lithium
Mechanism
Not understood. One suggestion to account for the
reduced serum levels of chlorpromazine, which is
based on animal studies,50,51 is that
chlorpromazine can be metabolised in the gut.
Therefore, if lithium delays gastric emptying, more
chlorpromazine will be metabolised before it
reaches the circulation. Just why severe
neurotoxicity and other adverse effects sometimes
develop in patients taking lithium and
antipsychotics is not understood. It is the subject
of considerable discussion and debate.9,11,12,

Antipsychotics + Orlistat
No changes in the plasma levels of
haloperidol or clozapine were seen
when orlistat was also given.

Antipsychotics + SSRIs
On the whole no significant adverse interactions
appear to occur between the antipsychotics and the
SSRIs. However, a number of case reports describe
extrapyramidal adverse effects following the use of
fluoxetine or paroxetine with an antipsychotic, and
galactorrhoea and amenorrhoea developed in one
patient given loxapine and fluvoxamine. Fluoxetine
and fluvoxamine appear to raise haloperidol levels,
which may increase adverse effects. Thioridazine
levels are expected to be increased with fluoxetine,
fluvoxamine, or paroxetine treatment with a risk of
QT interval prolongation.

Antipsychotics + Tobacco or
Cannabis
Smokers of tobacco or cannabis may possibly
need larger doses of chlorpromazine,
fluphenazine, haloperidol or tiotixene than
nonsmokers.
Mechanism
Not established. The probable reason is that
some of the components of tobacco smoke act
as enzyme inducers, which increase the rate at
which the liver metabolises these
antipsychotics, thereby reducing their serum
levels and clinical effects.