Praktikum Farmakologi Minggu ke 5 Blok 19.

Perilaku dan Psikiatri

Judul bahan Praktikum :

Antipsychotic medication in schizophrenia: a review.

Bagian Farmakologi dan Terapi FK UKI

Tahun ajaran 2021/2022

9/10/2021 Bagian Farmakologi dan Terapi FK UKI 1

Tujuan dan capaian pembelajaran
• Capaian pembelajaran: Mahasiswa dapat menjelaskan Farmakodinamik, Farmakokinetik, Efek samping,
sediaan obat, cara penggantian obat antipsikosis
• Tujuan pembelajaran: Mahasiswa dapat memahami;
1. Farmakodinamik atau mekanisme kerja obat antipsikotik
2. Efek samping obat antipsikosis
3. Pemantauan obat antipsikosis
4. Lama pemberian obat antipsikosis
5. Penggantian obat antipsikosis
6. Sediaan obat antipsikosis
7. Indikasi pemberian obat antipsikosis
8. Informasi mengenai obat-obat antipsikosi yang baru

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Switching antipsychotic
• When antipsychotic are ineffectiveness or in tolerability → switching
antypsychotics.
• There are different methods for switching antipsychotic:
1. Crossover
2. Stop the first drug and switch the new drug at therapeutic dose
3. Fisrt medication is slowly discontinued and only when it is stopped
will the next medication be started.

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Sediaan obat antipsikosis
Sediaan yang ada untuk obat antipsikosis
1. Peroral
2. Injeksi kerja panjang dengan Depot

• Obat antipsikosis sediaan inj kerja panjang dg depot adalah

risperidone, paliperidone, olanzapin, aripirazole→ SGAs
• Haloperidol decanoate, flupentixol decanote, zuclopenthixol
decanote Dan fluphenazine decanoate → FGAs

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Indikasi pemberian obat antipsikosis
• Antipsikosis efektif untuk gangguan yang luar selain untuk kasus
skizoprenia.
• Indikasi lain:
• Moodstabilator
• Antimaniak
• Antidepresan
• Anxiolitik

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Bipolar affective disorder (BPAD)
• Olanzapine and quetiapine are recommended first-line treatments for
bipolar depression.
• Both quetiapine and olanzapine are associated with a rapid onset of
action in bipolar depression, with efficacy demonstrated from the first
week of treatment onwards
• In clinical practice, quetiapine is now considered more for its mood-
stabilising properties than for its antipsychotic effects. Similarly, the
antipsychotics that are indicated for acute mania are generally
recommended for maintenance therapy in BPA

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Unipolar depression
• The use of antipsychotics as augmentation treatment options in
unipolar depression and anxiety disorders is an off-label use, meaning
that this use is not formally licensed (but with a growing evidence
base to indicate the efficacy of certain antipsychotics).
• There is evidence to support the use of quetiapine, aripiprazole,
olanzapine and risperidone as antidepressant augmentation
strategies in TRD, with the best evidence existing for the use of
quetiapine and aripiprazole.

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• In psychotic depression, the combination of an antipsychotic and
antidepressant is more effective than the use of an antidepressant
alone, with olanzapine combined with fluoxetine probably the best
evidenced combination.

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Anxiety disorders
• Antipsychotic medications have long been used as augmentation
strategies for anxiety disorders, with the best evidence for their use
as selective serotonin reuptake inhibitor augmentation strategies in
obsessive compulsive disorder (OCD) and for the use of quetiapine in
generalized anxiety disorder (GAD).

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Obat antipsikotik yang generasi baru

• the heterogeneous patient response to and tolerability of

antipsychotics, there remains a need to improve the therapeutic
efficacy of available agents and to aid choice in improving treatment
tolerability for patients.
• The newer branded SGAs, asenapine and lurasidone, have less impact
on weight and metabolic parameters than older agents such as
olanzapine.

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1. Paliperidone the active both demonstrating dverse effect profile is At doses of 9–12 mg
metabolite of efficacy and similar to that of the of oral paliperidone
risperidone and is tolerability and a parent compound (equivalent to
available in oral and delay in time to risperidone, with risperidone 4–6 mg
LAI formulations relapse in increased weight gain, daily), the risk of
schizophrenia hyperprolactinaemia EPSEs is increased.
treatment of and EPSEs at higher The therapeutic dose
psychotic and manic It is not hepatically doses, along with case range is 6–9 mg once
symptoms of metabolised, making reports of tardive daily (equivalent to
schizoaffective it safe to use in dyskinesia. risperidone 3–4 mg
disorder hepatic impairment daily)
and with limited risk
of pharmacokinetic Paliperidone
drug interactions. palmitate is the LAI
formulation, which
achieves active serum
levels within days of
initiation and allows
deltoid, rather than
gluteal muscle
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2. Asenapine efficacy in the acute and
maintenance phases of
schizophrenia treatment
and in the treatment of
acute mania in BPAD, but
it is only currently licensed
for the treatment of mania
in the UK.3
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Asenapine has high
affinity for multiple
serotonin receptors,
with antagonism at 5-
HT2A, 5-HT2C and 5-
HT7 and 5-HT1A
agonism, along with
potent D2 and D3
antagonism and some
histamine (H) 1
antagonism.18
Bagian Farmakologi dan Terapi FK UKI
Asenapine is subject to Asenapine does not
first-pass metabolism require dose titration
and thus inactive if and can be dosed at 5
swallowed. It is, mg bd for acute
therefore, available schizophrenia with
only as an orally doses of up to 10 mg
disintegrating tablet, twice daily shown
meaning that it is efficacy in preventing
absorbed via oral relapses in
mucosa. schizophrenia.
Asenapine has a half-
Asenapine is subject to life of 24 h and as such
first-pass metabolism could theoretically be
and thus inactive if prescribed as a once-
swallowed. It is, daily medication
therefore, available
only as an orally It can cause akathisia
disintegrating tablet, (increased occurrence
meaning that it is at 10 mg twicedaily
absorbed via oral dosing compared with
mucosa. 5 mg twice daily),
sedation and taste12
disturbance.40
3. lurasidone licensed for the treatment of
schizophrenia35 and has
shown efficacy as an
adjunctive treatment for
bipolar depression, and it is
a licensed therapy for
bipolar depression in the
USA.
Lurasidone has full D2
antagonism and is an
antagonist at 5HT2A and
5HT7 receptors, with partial
agonism at 5-HT1A
receptors, and with low
affinity for 5HT2C, H
9/10/2021 Bagian Farmakologi dan Terapi FK UKI
Lurasidone is a once-daily Lurasidone is metabolized
prescription, simplifying its by CYP3A4 enzymes,
administration. It is dosed meaning that its dose
in adults at 37 mg once should be reduced when
daily initially and increased used with concomitant
if necessary to a maximum CYP3A4 inhibitors (e.g.
of 148 mg once daily. For diltiazem, erythromycin)
schizophrenia, a dose range
of 37–148 mg daily is
recommended, with a
lower dose range of 18.5–
120 mg daily,
recommended for bipolar
depression (lurasidone at
lower doses of 20–60 mg
daily has been shown to be
as clinically efficacious in
bipolar depression, as at
the higher dose range of
80– 100 mg/day)
13
 Terima kasih dan selamat
belajar

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