APA (American Psychiatric Association)

merekomendasikan bahwa pasien skizofrenia yang

gejalanya membaik dengan pengobatan antipsikotik terus
diobati dengan obat antipsikotik. Untuk individu dengan
diagnosis skizofrenia yang gejalanya membaik dengan
pengobatan antipsikotik, ada sejumlah manfaat untuk
perawatan pemeliharaan, termasuk pengurangan risiko
kekambuhan, rehospitalization, dan kematian. Namun,
bila diberikan dalam jangka panjang obat antipsikotik
juga dikaitkan dengan insiden peningkatan berat badan,
sedasi, dan movement disorder. Untuk mengurangi risiko
ini perlu intervensi pencegahan (misalnya, intervensi
awal untuk penambahan berat badan, skrining untuk
kelainan lipid dan glukosa) dan pemantauan yang cermat
untuk efek samping pengobatan. Namun demikian,
seiring berjalannya pengobatan, kelebihan dan
kekurangan melanjutkan pengobatan dengan obat
antipsikotik harus ditinjau ulang dengan pasien dalam
konteks pengambilan keputusan bersama, ada baiknya
untuk menyertakan anggota keluarga atau wali pasien.

Terlepas dari manfaat pengobatan antipsikotik lanjutan

untuk sebagian besar pasien, mempertahankan kepatuhan
terhadap pengobatan antipsikotik bisa jadi sulit.
Hambatan, fasilitator, dan motivator kepatuhan
pengobatan akan berbeda untuk setiap pasien.
Melibatkan anggota keluarga atau orang lain yang
mendukung dapat membantu dalam mendorong
kepatuhan.

Penting juga untuk menilai manfaat berkelanjutan dan

efek samping pengobatan yang mungkin
mengindikasikan perlunya penyesuaian dosis obat atau
perubahan obat. Dosis obat yang optimal adalah yang
memberikan manfaat pengobatan terbaik namun masih
dapat ditoleransi dalam hal efek samping pengobatan.
Untuk beberapa pasien, penyesuaian dosis akan
diperlukan selama pengobatan untuk menjaga
keseimbangan ini. Faktor-faktor seperti penambahan atau
penghentian obat yang berinteraksi, perubahan status
merokok, perubahan massa tubuh pasien, perubahan
status ginjal atau hati, atau perubahan dalam penyerapan
obat dapat mempengaruhi farmakokinetik obat dan
memerlukan peningkatan atau penurunan dalam dosis
obat. Jika suatu pengobatan memerlukan penghentian
segera, pengurangan dosis secara bertahap lebih
disarankan dengan pemantauan ketat untuk gejala-gejala
yang berulang. 

Diskusi pengambilan keputusan bersama dengan pasien

harus mempertimbangkan tujuan pemulihan pasien,
manfaat potensial dari perubahan obat atau pengurangan
dosis dalam hal perubahan atau pengurangan efek
samping, dan potensi bahaya dari perubahan obat atau
pengurangan dosis. Perjalanan longitudinal episode
pasien dan kepastian diagnosis juga harus
dipertimbangkan. Mungkin ada beberapa individu
dengan episode psikosis singkat atau diagnosis psikotik
yang tidak pasti (misalnya, kemungkinan psikosis akibat
zat atau psikosis terkait suasana hati) yang mungkin tidak
memerlukan perawatan antipsikotik lanjutan. Di sisi lain,
individu dengan gejala kronis, kekambuhan berulang,
dan gambaran diagnostik skizofrenia yang jelas
kemungkinan akan memiliki hasil yang lebih buruk jika
pengobatan dihentikan.
Tabel 1 Antipsychotic medications: available oral and short-acting intramuscular
formulations and dosing considerations
Available Initial Typical Maximum Comments
U.S. dose dose daily dose
formulation (mg/da range (mg/day)
s (mg, y) (mg/day)
unless
otherwise
noted)

First-generation antipsychotics 

Chlorpromazine Tablet: 10, 25-100 200-800 Oral: Jangan menyuntikkan secara

25, 50, 100, 1,000– subkutan. Gunakan dosis IM
200 Short- 2,000 yang jauh lebih rendah
acting daripada dosis oral karena
injection metabolisme oral first-pass
 (HCl): signifikan
25/mL (1
mL, 2 mL) 

Fluphenazine Tablet: 1, 2.5-10 6-20 Oral: 40 Dosis Short-acting IM adalah

2.5, 5, 10 IM:10 33% -50% dari dosis oral.
Oral Encerkan konsentrat oral
concentrate: segera sebelum digunakan
5/mL(120 untuk memastikan
mL) palatabilitas dan stabilitas.
Elixir: 2.5/5
mL (60 mL)
Short-acting
injection
(HCl):
2.5/mL (10
mL) 
Haloperidol Tablet: 0.5, 1-15 5-20 Oral: 100  2–5 mg IM dapat diberikan
1, 2, 5, 10, IM: 20 setiap 4–8 jam.
20
Oral
concentrate:
2/mL (5
mL, 15 mL,
120 mL)
Short-acting
injection
(lactate):
5/mL (1
mL, 10
mL) 

Loxapine Capsule: 5, 20 60-100^h Oral: 250 

10, 25, 50  Aerosol: 10
 Aerosol
powder
breathactiva
ted
inhalation:
10

Molindone Tablet: 5, 50-75 30-110^h 225

10, 25

Perphenazine Tablet: 2, 4, 8-16 8-32 64

8, 16

Pimozide Tablet: 1, 2  0.5-2 2-4 10 Pimozide tidak memiliki

indikasi FDA (Food and
Drug Administration) untuk
skizofrenia tetapi kadang-
kadang digunakan untuk
 mengobati gangguan delusi
seperti parasitosis delusional.
Hindari penggunaan bersama
penginduksi atau penghambat
CYP1A2 atau CYP3A4.
Lakukan genotipe CYP2D6
jika dosis yang digunakan
lebih dari 4 mg / hari. Pada
pemetabolisme CYP2D6
yang buruk, jangan berikan
lebih dari 4 mg / hari dan
jangan menambah dosis lebih
awal dari 14 hari.

Thioridazine Tablet: 10, 150- 300– 800

25, 50, 100 300 800^h
Thiothixene Capsule: 1, 6-10 15-30 60
2, 5, 10

Trifluoperazine Tablet: 1, 2, 4-10 15-20 50

5, 10 

Second-generation antipsychotics

Aripiprazole Tablet: 2, 5, 10-15 10-15 30

10, 15, 20,
30 
Tablet,
disintegratin
g: 10, 15
Tablet with
ingestible
event
marker
 (Mycite): 2,
5, 10, 15,
20, 30
Solution:
1/mL (150
mL)

Asenapine Tablet, 10 20 20 Pertimbangkan penyesuaian

sublingual: dosis pada perokok dan
2.5, 5, 10 dengan penggunaan CYP1A2
inhibitor secara bersamaan.
Jangan membelah,
menghancurkan, atau
menelan. Tempatkan di
bawah lidah dan biarkan larut
sepenuhnya. Jangan makan
atau minum selama 10 menit
 setelah pemberian untuk
memastikan penyerapan.

Asenapine Transdermal 3.8 3.8–7.6 7,6 Pertimbangkan penyesuaian

system: 3.8 dosis pada perokok dan
mg/ 24 dengan penggunaan
hours, 5.7 penghambat CYP1A2 secara
mg/24 bersamaan.
hours, 7.6 Oleskan pada kulit yang
mg/24 hours bersih, kering, dan utuh di
lengan atas, punggung atas,
perut, atau pinggul; putar
situs saat menerapkan sistem
transdermal baru. Jangan di
potong.

Brexpiprazole Tablet: 1 2–4 4 Sesuaikan dosis jika

 0.25, 0.5, 1, metabolisme CYP2D6 buruk
2, 3, 4 atau dengan penggunaan
bersamaan
CYP2D6 inhibitors, strong
CYP3A4 inhibitors, or strong
CYP3A4 inducers.

Cariprazine Capsule: 1,5 1.5–6 6^i Sesuaikan dosis dengan

1.5, 3, 4.5, 6 penggunan bersama dengan
strong CYP3A4 inhibitor or
inducer.

Clozapine Tablet: 25, 12,5-25 300– 900 Saat memulai clozapine,

50, 100, 200 450^e tingkatkan dosis 25-50 mg /
Tablet, hari selama 2 minggu,
disintegratin kemudian peningkatan
g: 12.5, 25, selanjutnya tidak melebihi
100, 150, 100 mg hingga dua kali
200 seminggu. Untuk
Oral penghentian pengobatan
suspension: selama 2 hari atau lebih,
50/mL (100 mulai ulang dengan 12,5 mg
mL) sekali atau dua kali sehari.
Retitasi dapat terjadi lebih
cepat dibandingkan dengan
pengobatan awal. Dengan
penghentian pengobatan lebih
dari 30 hari, rekomendasi
untuk titrasi awal dan
frekuensi pemantauan harus
diikuti. Sesuaikan dosis
dengan penggunaan bersama
strong CYP1A2 inhibitors
and with strong CYP3A4
 inducers. Merokok
mengurangi keefektivan
clozapine melalui induksi
CYP1A2.

Iloperidone Tablet: 1, 2, 2 12-24 24 Sesuaikan dosis dengan

4, 6, 8, 10, penggunaan bersama strong
12 CYP2D6 or CYP3A4 dan
kurangi dosis hingga 50%
pada metabolisme CYP2D6
yang buruk.

Lurasidone Tablet: 20, 40 40-120 160 Berikan dengan makanan

40, 60, 80, (≥350 kalori). Sesuaikan
120 dosis untuk penggunaan
bersamaan dengan strong
CYP3A4 inhibitors or
 inducers.

Olanzapine Tablet: 2.5, 5-10 10-20 20^k Formulasi IM kerja pendek

5, 7.5, 10, digunakan terutama untuk
15, 20 agitasi, dengan dosis biasa
Tablet, 2,5-10 mg IM dan dosis
disintegratin maksimum 30 mg/hari.
g: 5, 10, 15, Berikan IM perlahan, masuk
20 Short- ke dalam otot. Jangan
acting IM gunakan secara subkutan.
powder for Penggunaan olanzapine IM
solution: secara bersamaan dengan
10/2 mL benzodiazepin parenteral
tidak dianjurkan karena
berpotensi menimbulkan
sedasi ive berlebihan dan
depresi kardiorespirasi.
Perokok mungkin
memerlukan dosis harian
30% lebih besar daripada
bukan perokok karena
induksi CYP1A2. Wanita
mungkin membutuhkan dosis
harian yang lebih rendah.
Waktu paruh eliminasi IM
adalah ~1.5 kali lebih besar
pada orang tua. Tablet
terlarut oral larut dengan
cepat di dalam air liur dan
dapat ditelan dengan atau
tanpa cairan. Olanzapine
dapat diberikan dengan atau
tanpa makanan / makanan.
Paliperidone Tablet, 6 3-12 12 Jika melebihi 6 mg sehari,
extended dianjurkan peningkatan 3
release: 1.5, mg/hari dengan interval lebih
3, 6, 9 dari 5 hari, hingga
maksimum 12 mg/hari.
Jangan membelah atau
menghancurkan tablet.
Penggunaan extended-release
tablet tidak dianjurkan pada
gangguan penyempitan
gastrointestinal parah yang
sudah ada sebelumnya.

Quetiapine Tablet, Immedi 400-800 800 Jangan membelah atau

immediate ate menghancurkan extended-
release: 25, release: release tablets. Immediate-
50, 100, 50 release tablets dipengaruhi
 200, 300, Extende oleh makanan, sedangkan
400 d extended-release tablets
Tablet, release: dipengaruhi secara signifikan
extended 300 oleh makanan berlemak
release: 50, tinggi. Berikan extended-
150, 200, release tablets tanpa makanan
300, 400. atau dengan <300 kalori.
Retitrate untuk celah dalam
perawatan lebih dari 1
minggu. Sesuaikan dosis
dengan penggunaan
bersamaan strong CYP3A4
inhibitors or inducers.

Risperidone Tablet: 2 2-8 8^1 Fraksi risperidon bebas

0.25, 0.5, 1, ditingkatkan pada gangguan
2, 3, 4 hati, dan dosis awal adalah
Tablet, 0,5 mg dua kali sehari, yang
disintegratin dapat ditingkatkan dengan
g: 0.25, 0.5, peningkatan 0,5 mg atau
1, 2, 3, 4 kurang, diberikan dua kali
Oral sehari. Pada gangguan ginjal
solution: atau hati, tingkatkan interval
1/mL (30 1 minggu atau lebih untuk
mL) dosis >1,5 mg dua kali sehari.
Sesuaikan dosis dengan
penggunaan bersama dengan
inducers or inhibitors of
CYP2D6. Periksa label untuk
cairan yang kompatibel
dengan larutan oral. Jangan
membelah atau
menghancurkan tablet
penghancur oral. Beri tahu
 pasien dengan fenilketonuria
bahwa tablet disintegrasi oral
mengandung fenilalanin.

Ziprasidone Capsule: 20, 40 80-160 320 Berikan kapsul dengan

40, 60, 80 makanan >500 kalori. Tidak
Solution ada data yang menyarankan
reconstitute peningkatan kemanjuran pada
d, IM: 20 dosis yang lebih tinggi.
Formulasi IM short-acting
digunakan terutama untuk
agitasi, dengan dosis biasa 20
mg/hari dan dosis maksimum
40 mg/hari.
Tabel 2 Antipsychotic medications: pharmacokinetics/pharmacodynamics of oral and
short-acting intramuscular formulations
Oral Time Protein Eliminatio Excretion Hepatic Renal
bioav to bindin n half-life Impairmen Impairment
ailabi peak g in adults t
lity level
First-generation antipsychotics
Chlorpromazin 32% 2,8 90%- Biphasic: Primarily Use with Use with
e hour 99% initial 2 renal caution caution,
s hours, (<1% as not
terminal 30 unchange dialyzable
hours d drug)
Fluphenazine 2.7% Oral: 99% 4.4-16.4 Renal Contraindi Use with
2 hours and cated by caution
hour fecal; manufactur
s exact er
IM: proportio
 1.5-2 n unclear
hour
s
Haloperidol 60%- Oral: 89%- 14-37 15% No dose No dose
70% 2-6 93% hours fecal, adjustment adjustment
hour 30% noted noted
s renal
IM: (1% as
20 unchange
minu d drug)
tes
Laxopine 99% 1.5-3 97% Biphasic: Renal No dose No dose
hour initial 5 and fecal adjustment adjustment
s hours, noted noted
terminal 19
hours
Molindone Uncl 1.5 76% 1.5 hours Renal Use with No dose
ear hour and fecal caution adjustment
 s noted
Perphenazine 20%- Perp 91%- Perphenazi 5% fecal, Contraindi Use with
40% hena 99% ne: 9-12 70% cated in caution
zine: hours renal liver
1-3 7- damage
hour hydroxyper
s phenazine:
7- 10-19
hydr hours
oxyp
erph
enazi
ne:
2-4
hour
s
Pimozide ≥50 6-8 99% 55 hours Primary Use with No dose
% hour renal caution adjustment
 s noted
Thioridazine 25%- 1-4 96%- 21-24 Minimal Use with No dose
33% hour 99% hours renal caution adjustment
s noted
Thiotixene ~50 1-2 90% 34 hours Feces No dose No dose
%; hour (unchang adjustment adjustment
errati s ed drug noted noted
c and
absor metaboli
ption es)
Trifluoperazine Errati 1.5-6 90%- 3-12 hours Renal Contraindi No dose
c hour 99% cated in adjustment
absor s hepatic noted
ption disease
Second-generation antipsychotics
Aripiprazole 87% 3-5 >99% 75 hours, 55% No dose No dose
hour 94 hours fecal, adjustment adjustment
s dehy- 25% noted noted
 droaripipra renal
-zole 146
hours in
poor
CYP2D6
metabolizer
s
Asenapine 35% 0.5- 95% 24 hours 40% Contraindi- No dose
1.5 fecal, cated in se- adjustment
hour 50% vere s noted
s renal hepatic
impairment
(Child-
Pugh class
C)
Asenapine Not Not 95% 24 hours 40% Contraindi- No dose
appli avail fecal, cated in se- adjustment
cable able 50% vere s noted
 renal hepatic
impairment
(Child-
Pugh class
C)
Brexpiprazole 95% 4 <99% 91 hours 46% Moderate use
hour fecal, to severe maximum
s 25% impairment dosage of 2
renal (Child- mg/day in
Pugh class MDD and
B or C): 3 mg/day
use in
maximum schizophre
dosage of 2 nia
mg/day in
MDD and
3 mg/day
in
 schizophre
nia
Cariprazine High 3-6 91%- Cariprazine 21% Severe Not rec-
hour 97% : 2–4 days renal impairment ommended
s (Child-
Pugh class
C): not
recommen
ded
Clozapine 27%- 2,2- 97% 4–66 hours 30% Significant Significant
60% 2,5 (steady fecal, impairment impairment
hour state 12 50% : dose : dose
s hours) renal reduction reduction
(rang may be may be
e: 1- necessary necessary
6
hour
s)
Iloperidone 96% 2-4 92%- Extensive ~20% Moderate No dose
hour 97% metabolizer fecal, impairment adjustment
s s: ~50% : use with noted
iloperidone renal caution
18 hours, Severe
P88 26 impairment
hours, P95 : not
23 hours recommen
ded
Lurasidone 9- 1-3 99% Lurasidone ~80% Moderate Initial 20
19% hour 18-40 fecal, to severe mg/day,
s hours ~9% hepatic maximum
renal impairment dose 80
(Child- mg/day
Pugh class
B and class
C): use 20
mg/ day
 initially ,
with
maximum
dose of 80
mg/ day
and 40
mg/day,
respectivel
y
Olanzapine >57 Oral: 93% 30 hours 30% Use with Not
% 6 fecal, caution removed
hour 57% by dialysis
s renal
IM
: 15-
45
minu
tes
Paliperidone 28% 24 74% 23 hours; 11% Mild to Not
hour 24-51 fecal, moderate; recommen
s hours with 80% no ded for
renal renal adjustment CrCl <10
impairment necessary. mL/min-
(CrCl <80 Severe: not ute; for
mL/minute studied CrCl 10–
) 49
mL/minute
and CrCl
50–79
mL/min-
ute, use
maximum
dosage of 3
mg/day
and 6 mg/
day,
 respec-
tively
Quetiapine 100 Imm 83% Quetiapine: 20% Immediate No dose
% ediat 6–7 hours fecal, release: adjustment
e Norquetiap 73% initial 25 s noted
relea ine : 12 renal mg/ day
se: hours dose,
1.5 increase by
hour 25–50 mg/
s day to
Exte effective
nd dose
ed Extended
relea release:
se: 6 initial 50
hour mg/day,
s increase by
50 mg/day
 to effective
dose
Risperidone Abso 1 90% Risperidon 14% Mild or Mild or
lute: hour e: 3–20 fecal, moderate moderate
70% hours 70% impairment impairment
Table 9-hydroxy- renal (Child- (CrCl ≥ 30
t risperidone Pugh class mL/minute
relati : 21–30 A or B): ): reduce
ve to hours reduce dose
oral dose Severe
soluti Severe impairment
on: impairment (CrCl <30
94% (Child- mL/minute
Pugh class ): initial
C): initial 0.5 mg
0.5 mg twice a
twice a day day,
, increase increase by
 by no more no more
than 0.5 than 0.5
mg twice a mg twice a
day; may day; may
increase to increase to
total dosage >1.
dosage 5 mg twice
>1.5 mg a day at 1
twice a day week or
at 1 week greater.
or greater
Ziprasidone Oral Oral: >99% Oral: 7 66% Use with No oral
with 6-8 hours fecal, caution dose
food: hour IM: 2–5 20% adjustment
60% s hours renal s noted
IM: >99 IM
100 % formulatio
% IM: n contains
 60 a renally
minu cleared
tes excipient,
cyclodextri
n; use with
caution

Tabel 3 Antipsychotic medications: relative side effects of oral formulations

Akathi Par Dysto Tardiv Hyperprolacti Anticholin sedati
sia kins nia e nemia ergic on
onis dyskin
m esia
First-generation antipsychotics
Chlorpromazine ++ ++ ++ +++ + +++ +++
Fluphenazine +++ +++ +++ +++ +++ + +
Haloperidol +++ +++ +++ +++ +++ + +
Loxapine ++ ++ ++ ++ ++ ++ ++
Molindone ++ ++ ++ ++ ++ + ++
Perphenazine ++ ++ ++ ++ ++ ++ ++
Pimozide +++ +++ ++ +++ +++ + +
Thioridazine + + + + ++ +++ +++
Thiothixene +++ +++ +++ +++ +++ + +
Trifluoperazine ++ ++ ++ ++ ++ ++ +
Second-generation Antipsichotics
Aripiprazole ++ + + + + + +
Asenapine ++ + ++ ++ ++ + ++
Brexpiprazole ++ + + + + + ++
Cariprazine ++ + + + + ++ ++
Clozapine + + + + + +++ +++
Iloperidone + + + + ++ + ++
Lurasidone ++ ++ ++ ++ + + ++
Olanzapine ++ ++ + + ++ ++ +++
Paliperidone ++ ++ ++ ++ +++ + +
Quetiapine + + + + + ++ +++
Risperidone ++ ++ ++ ++ +++ + ++
Ziprasidone ++ + + + ++ + ++

Tabel 4 Antipsychotic medications: relative side effects of oral formulations (continued)

Seizure Ort QT Weight Hyp Gluco Comments
s host prolo gain erli se
asis ngatio pide abnor
n mia maliti
es
First-generation antipsychotics
Chlorpromazine ++ +++ +++ ++ + ++
Fluphenazine + + ++ ++ ++ +
Haloperidol + + ++ ++ + +
Loxapine + ++ ++ + + +
Molindone + + ++ + + +
Perphenazine + ++ ++ ++ + +
Pimozide +++ + +++ + + +
Thioridazine ++ +++ +++ ++ + + Pigmentary
retinopathy; high rates
of sexual dysfunction;
avoid use if QTc
interval is >450 msec
or with concomitant
use of drugs that
prolong the QTc
interval or inhibit
CYP2D6
Thiothixene +++ + ++ + + +
Trifluoperazine + + ++ ++ + +
Second-generation Antipsichotics
Aripiprazole + + + + + + FDA safety alert for
impulse control
 disorders (e.g.,
gambling, binge
eating); may reduce
hyperprolactinemia
with other
antipsychotics
Asenapine + ++ ++ ++ ++ ++ Oral hypoesthesia
Brexpiprazole + + ++ + ++ +
Cariprazine + + ++ ++ + +
Clozapine +++ +++ ++ +++ +++ +++ Increased salivation
common ; high rate of
sexual dysfunction;
sever e constipation
and paralytic ileus
possib le; fever can
occur with initiation;
myocardi tis is
infrequent;
 cardiomyopathy and
severe neutropenia are
rare
Iloperidone + +++ +++ ++ + ++
+ + + + ++ ++ Dose-related
Lurasidone creatinine increase in
some patients
Olanzapine ++ ++ ++ +++ +++ +++
Paliperidone + ++ ++ ++ ++ +
Quetiapine ++ ++ ++ ++ +++ ++
Risperidone + ++ ++ ++ + ++ Intraoperative floppy
iris syndrome reported
Ziprasidone + ++ +++ + + +
Tabel 5 Long-acting injectable antipsyichotic medications: availability and ijection-related
consideration
Availbale How Injection site Reactions Comments
strengths supplied and at injection
(mg, technique site
unless
otherwise
noted)
First-generation antipsychotics
Fluphenazi 25/mL (5 Vial, Deep IM Skin Monitor for hypotension. In
ne mL) sesame gluteal or reactions sesame oil, be alert for
oil deltoid reported allergy. For
vehicle injection; detailedinstructions on
with use of needle size and product
1.2% Ztrack handling, refer to labeling
benzyl technique
alcohol recommende
 d
Haloperidol 50/mL (1 Vial, Deep IM Inflammati Do not administer more than
mL, 5 sesame gluteal or on and 3 mL per injection site. In
mL), oil deltoid nodules sesame oil, be alert for
100/mL (1 vehicle injection; reported, allergy. For detailed
mL, 5 mL) with use of Z- especially instructions on needle size,
1.2% track with dose refer to labeling
benzyl technique >100
alcoho recommende mg/mL
d
Second-generation antipsychotics
Aripiprazol 300, 400 Kit with Slow IM Occasional Rotate injection sites. Do not
e either injection redness, massage muscle after
monohydra prefilled into gluteal swelling, injection. For detailed
te syringe or deltoid induration instructions on needle size
or muscle (mild to and product reconstitution,
single- moderate) refer to labeling.
use vial
Aripiprazol 675/2.4 Kit with IM deltoid Common: Only to be used as a single
e lauroxil mL prefilled or gluteal pain dose to initiate Aristada
syringe muscle Infrequent: treatment or to reinitiate
induration, treatment following a missed
swelling, dose of Aristada. Not for
redness repeat dosing. Not
interchangeable with
Aristada. Avoid concomitant
injection of Aristada Initio
and Aristada into the same
deltoid or gluteal muscle.
Refer to labeling for detailed
instructions on injection site,
needle length, and
instructions to ensure a
uniform suspension.
Aripiprazol 441/1.6 Kit with IM deltoid Common: Not interchangeable with
e lauroxil mL, prefilled or gluteal pain Aristada Initio. Avoid
 662/2.4 syringe muscle for Infrequent: concomitant injection of
mL, 882 441 mg IM induration, Aristada Initio and Aristada
/3.2 mL, gluteal swelling, into the same deltoid or
1,064/3.9 muscle for redness gluteal muscle. Refer to
mL 662 mg, 882 labeling for detailed
mg, or 1,064 instructions on injection site,
mg needle length, and
instructions to ensure a
uniform suspension.
Olanzapine 210, 300, Kit with Deep IM Infrequent Because of risk of
405 vial gluteal induration postinjection delirium/
containin injection or mass at sedation syndrome, must be
g diluent only; do not injection given in a registered health
and vial administer site care facility with ready
with subcutaneou access to emergency
powder sly response services, and
for patient must be observed for
reconstit at least 3 hours postinjection
 uting and accompanied on
suspensi discharge. Requires use of
on FDA REMS program
(www.zyprexarelprevv
program.com/public/Default.
aspx). Do not massage
muscle after injection. The
combined effects of age,
smoking, and biological sex
may lead to significant
pharmacokinetic differences.
For detailed instructions on
product handling and
reconstitution, refer to
labeling.

Paliperidon 39/0.25 Kit with IM only; Occasional The two initial deltoid IM
e palmitate mL, 78/0.5 prefilled slow, deep redness, injections help attain
 mL, syringe IM deltoid swelling, therapeutic concentrations
117/0.75 injection for induration rapidly. Alternate deltoid
mL, 156/1 first 2 doses, injections (right and left
mL, then deep deltoid muscle). For detailed
234/1.5 deltoid or instructions on needle size
mL gluteal and product reconstitution,
injection refer to labeling.
(upper outer
quadrant)
thereafter
Paliperidon 273/0.875 Kit with IM only; Infrequent Shake prefilled syringe for
e palmitate mL, 410/ prefilled slow, deep redness or 15 seconds within 5 minutes
1.315 mL, syringe IM deltoid swelling prior to administration. For
546/1.75 or gluteal detailed instructions on
mL, injection needle size, product
819/2.625 handling, and reconstitution,
mL refer to labeling.
Risperidon 12.5, 25, Kit with Deep IM Occasional Alternate injection sites.
e 37.5, 50 prefilled injection redness, Refrigerate and store at 2°C–
syringe into the swelling, 8°C and protect from light.
and vial deltoid or induration Vial should come to room
for gluteal temperature for at least 30
reconstit (upper outer minutes before
ution quadrant) reconstituting. May be
storedat 25°C for up to 7
days prior to administration.
For detailed instructions on
product handling and
reconstitution, refer to
labeling.
90/0.6 mL, Kit with Abdominal Lump at Alternate injection sites.
120/0.8 prefilled subcutaneou injection Inject only in area without
mL syringes s injection site may skin conditions, irritation,
containin only persist for reddening, bruising,
g several infection, or scarring; do not
powder weeks rub or massage injection
 and sites. Store at 2°C–8°C and
diluent protect from light. Allow
package to come to room
temperature for at least 15
minutes before injection. For
detailed instructions on
product handling and
reconstitution, refer to
labeling.

Tabel 6 Long-acting injectable antipsyichotic medications: dosing

Dose Initial Typical Maximu Dosing Need for Comments
conversi dose dose m dose frequency initial oral
ons (mg) (mg) (mg) suppleme
ntation
First-generation antipsychotics
Fluphen For each 6.25– 6.25–25 100 2–4 Decrease Increase in
azine 10 25 every 2– weeks oral dose 12.5 mg
mg/day every 2 4 weeks by half increments if
oral, give weeks after first doses >50
12.5 mg injection, mg are
decanoat then needed
e every 3 discontinu
weeks e with
second
injection
Haloperi For each Determ 50–200 450/mont 4 weeks Taper and If initial dose
dol 5 mg/day ined by (10–15 h discontinu is >100 mg,
oral, give oral times e after two split into two
50–75 dose previous to three injections
mg and/ or oral injections separated by
decanoat risk of dose) 3–7 days.
e every 4 relapse
weeks up to a
 maxim
um of
100 mg
Second-generation antipsychotics
Aripipra Not 400 400 400/mont Monthly Continue Follow
zole applicabl h oral for 14 labeling if
monohy e days after scheduled
drate initial injections are
injection missed. Dose
adjust for
poor
CYP2D6
metabolizers,
for those
taking
CYP2D6
and/or
CYP3A4
 inhibitors, or
because of
adverse
effects.
Avoid use
with
CYP3A4
inducers.
Aripipra Not 675 675 675 Single Must be For patients
zole applicabl dose to administer who have
lauroxil e initiate ed in never taken
Aristada conjunctio aripiprazole,
treatment n with one establish
or 30 mg tolerability
reinitiate dose of with oral
treatment oral aripiprazole
after a aripiprazo before use.
missed le Aristada
 Aristada Initio and
dose. Not Aristada are
for not
repeated interchangea
dosing ble. See
labeling for
dose
adjustments.
Aripipra 10 Monthl Monthly 882/mont Monthly: Aristada
zole mg/day y: 441, : 441, h 441, 662, Initio and
lauroxil orally, 662, 662, 882 882 Aristada are
give 441 882 not
mg interchangea
IM/mont ble. The first
h Aristada
injection
15 Every 6 Every 6 Every 6 may be given
mg/day weeks: weeks: weeks: on the same
orally, 882 882 882 day as
give 662 Aristada
mg/mont Initio or up
h IM, to 10 days
882 mg thereafter.
IM every
6 weeks,
or 1,064
mg IM
every 2
months
20 Every 2 Every 2 Every 2
mg/day months months: months:
or : 1,064 1,064 1,064
greater
orally,
give 882
mg/
 month
IM
Olanzapi 10 Determ 150 mg, 300 mg 2–4 Not Give 150 mg
ne mg/day ined by 210 mg, every 2 weeks required every 4
orally, oral or 300 weeks or weeks in
210 mg dose mg 405 mg patients who
every 2 every 2 every 4 may have
weeks weeks weeks sensitivity to
for four or 300 side effects
doses or mg or or slower
405 mg 405 mg metabolism.
every 4 every 4 Smokers
weeks weeks may require
15 a greater
mg/day daily dose
orally, than
300 mg nonsmokers,
every 2 and women
 weeks may need
for four lower daily
doses 20 doses than
mg/day expected
orally,
300 mg
every 2
weeks
Paliperid 3 mg 234 mg 78–234 234 Monthly Not Contains
one oral IM on mg mg/month required range of
palmitat paliperid day 1 monthly particle sizes
e one,give and 156 beginnin for rapid and
39–78 mg IM g at delayed
mg IM 6 1 week week 5 absorption.
mg oral, later, For changes
give 117 both to oral or
mg IM 9 adminis other LAI to
mg oral, tered in Sustenna, see
 give 156 the labeling.
mg IM deltoid Doses are
12 mg muscle expressed as
oral, give amount of
234 mg paliperidone
IM palmitate
rather than as
paliperidone.
Avoid using
with a strong
inducer of
CYP3A4
and/or P-
glycoprotein.
Paliperid Conversi Depend 273–819 819/3 Every 3 Not Change to
one on from ent on months months applicable Trinza after
palmitat monthly last at least four
e Invega dose of Invega
Sustenna monthl Sustenna
to every y doses (with
3- month paliperi two doses at
injection done same
s of strength). For
Invega changes from
Trinza: IM Trinza to
78 mg, oral or to IM
give 273 Sustenna, see
mg 117 labeling.
mg, give Doses are
410 mg expressed as
156 mg, amount of
give 546 paliperidone
mg 234 palmitate
mg, give rather than as
819 mg paliperidone.
Avoid using
 with a strong
inducer of
CYP3A4
and/ or P-
glycoprotein.

Risperid Oral 25 25–50 50 every 2 weeks Continue Upward dose

one risperido every 2 every 2 2 weeks oral for 3 adjustment
ne to weeks weeks weeks (21 should not be
Risperda days) made more
l Consta frequently
IM: than every 4
≤3 weeks.
mg/day,
give 25
mg/2
weeks >3
to ≤5
 mg/day,
give 37.5
mg/ 2
weeks >5
mg/day,
give 50
mg/2
weeks
Risperid Oral Determ 90–120 120/mont Monthly Neither a May not be
one risperido ined by monthly h loading appropriate
ne to oral dose nor for patients
subcutan dose oral taking less
eous overlap is than 3 mg or
risperido needed more than 4
ne ex- mg of oral
tended risperidone
release: daily. Adjust
dose with
 concomitant
CYP2D6
inhibitors or
CYP3A4
inducers.

Tabel 7 Long-acting injectable antipsyichotic medications: pharmacological characteristics

Time to peak Time to steady Elimination half-life
plasma level state
First-generation antipsychotics
Fluphenazine 8-10 hours 2 months 6–9 days for single injection and
14–26 days for multiple doses
Haloperidol 6 days 3-4 months 21 days
Second-generation antipsychotics
Aripiprazole 4 days (deltoid); By fourth dose 300 mg: 29.9 days 400 mg: 46.5
monohydrate 5-7 days (gluteal) days (400 mg) with gluteal injection
Aripiprazole 16-35 days Not applicable 15-18 days
lauroxil (median 27 days)
Aripiprazole Not available 4 months 53.9-57.2 days
lauroxil
Olanzapine 7 days 3 30 days
months
Paliperidone 13 days 2-3 months 25–49 days; increased in renal
palmitate disease
Paliperidone 30-33 days Not applicable 84–95 days with deltoid injection;
palmitate 118–139 days with gluteal
injection; increased in renal disease
Risperidone 29-31 days 2 months 3–6 days; increased in renal or
hepatic disease
Risperidone Two peaks: 4-6 2 months 9-11 days
hours and 10-14
days