N

1.

Penggolong
an
Antiretrovir
al & Contoh
Nama Obat
NRTI
(Nucleoside
Reverse
Transcripta
se
Inhibitor)
Zidovudin

Farmakokinetik

A: Rapidly
absorbed. T max is
0.5 to 1.5 h. Oral
bioavailability is
64%

Farmakodinamik & Struktur

Kimia

Spektrum
Antiretrov
iral &
Indikasi

Efek Samping &

Kontraindikasi

Interaksi Obat

Gugus AZT 5-monofosfat

bergabung pada ujung 3 rantai
DNA virus & menghambat enzim
reverse transcriptase (RT)

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV
lainnya
(lamivudin,
abakavir),
mencegah
penularan
HIV dari ibu
ke janin

Efek samping:
anemia,
neutropenia, sakit
kepala, mual
Kontraindikasi:
Potentially lifethreatening
hypersensitivity to
any component.

Bekerja pada HIV RT dengan cara

menghentikan pembentukan rantai
DNA virus

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV,
terutama

Efek samping:
diare, pancreatitis,
neuropati perifer
Kontraindikasi:
Potentially lifethreatening

Adriamycin, amphotericin B,
dapsone, flucytosine, interferon,
pentamidine, vinblastine,
vincristine
May increase risk of toxicity, including
nephrotoxicity, cytotoxicity, or
hematologic toxicity.
Atovaquone, fluconazole,
methadone, probenecid, valproic
acid
May increase serum concentration and
potential toxicity of zidovudine.
Doxorubicin
May antagonize the effect of
zidovudine. Avoid use.
Experimental nucleoside analogs
May affect RBC/WBC counts or
function and may increase potential
for hematologic toxicity.
Ganciclovir
Life-threatening hematologic toxicity
may occur.
Nelfinavir, ribavirin, rifamycin,
ritonavir, stavudine
May decrease zidovudine serum
concentrations, reducing the
therapeutic effect.
Phenytoin
Phenytoin levels have been reported
to increase, decrease, or not change
with coadministration. Zidovudine Cl is
decreased.

D: It is extensively
distributed. Binding
to plasma protein is
low, less than 38%.
Apparent Vd is 1.6
L/kg
M: Hepatic
metabolism. Major
metabolites are Dglucopyranuronosylt
hymidine (GZDV)
and 3-amino-3deoxythymidine
E: Primarily
eliminated by
hepatic metabolism.
Half-life is 0.5 to 3
h. GZDV (74%) and
zidovudine (14%)
are recovered in the
urine.
2.

Didanosin

A: T

max

is 0.25 to

Allopurinol
Because allopurinol may cause
increased didanosine plasma levels,
do not coadminister.

1.5 h (buffered
formulation), 2 h
(delayed-release).
Bioavailability is
approximately 42%
(buffered
formulation). Food
decreases the C max
and AUC by
approximately 55%
when didanosine
tablets were
administered up to
2 h after a meal. C
max and AUC of the
delayed-release
capsules decreased
by approximately
46% and 19%,
respectively, in the
presence of food.
Should be taken on
an empty stomach.
D: Less than 5%
protein bound. Vd is
approximately
M: Hepatic
metabolism
E: Half-life is
approximately 1.5 h
(buffered
formulation).
Approximately 18%
recovered in the
urine (buffered
formulation). Renal
Cl is approximately
458 mL/min
(buffered
formulation) in
patients with CrCl of
at least 90 mL/min.

3.
Zalsitabin

A: Oral
bioavailability is

infeksi HIV
tingkat
lanjut,
dalam
kombinasi
dengan anti
HIV lainnya

Bekerja pada HIV RT dengan cara

Spektrum:
HIV type 1
&2
Indikasi:

hypersensitivity to
any component.

Efek samping:
neuropati perifer,
stomatitis, ruam,

Antacids
Aluminum- or magnesium-containing
antacids may potentiate adverse
reactions associated with the antacid
component of didanosine pediatric
powder.
Antiretroviral agents
Antiretroviral agents have caused fatal
lactic acidosis in women when
coadministered with didanosine.
Delavirdine, indinavir
Administer 1 h prior to didanosine to
avoid decreasing plasma levels of
delavirdine or indinavir.
Drugs that cause peripheral
neuropathy or pancreatitis
Increased risk of these toxicities.
Food
Reduces absorption of didanosine by
as much as 50%.
Fluoroquinolones, tetracyclines
Do not administer within 2 h of
didanosine.
Ganciclovir, valganciclovir
Didanosine plasma concentrations
may be elevated, increasing the risk of
toxicity.
Itraconazole, ketoconazole,
dapsone, and other drugs whose
absorption can be affected by
gastric acidity
Administer at least 2 h before
didanosine.
Methadone
May decrease didanosine plasma
levels.
Ribavirin
Risk of didanosine toxicity may be
increased. Avoid coadministration.
Tenofovir disoproxil fumarate
Didanosine plasma concentrations
may be increased, necessitating a
dose reduction in didanosine.

about 80%.
Absorption rate of a
1.5 mg oral dose
was reduced with
food. C max is 25.2
ng/mL. T max is 0.8 h.
AUC is 72 ngh/mL
D: Vd is 0.534 L/kg.
Less than 4%
protein bound. Drug
interaction involved
in binding site is
unlikely.
M: Major metabolite
is dideoxyuridine
E: Renal elimination
is the primary route
of elimination

4.

Stavudin

A: Following oral

administration,
stavudine is
rapidly absorbed,
with peak plasma
concentrations
occurring within 1
hour after dosing
D: Binding of
stavudine to
serum proteins
was negligible
over the
concentration
range of 0.01 to
11.4g/mL.
Stavudine
distributes equally
between red
blood cells and
plasma

menghentikan pembentukan rantai

DNA virus

Bekerja pada HIV RT dengan cara

menghentikan pembentukan rantai
DNA virus

infeksi HIV,
terutama
pasien
dewasa
infeksi HIV
tingkat
lanjut yang
tidak
responsive
terhadap
zidovudin,
dalam
kombinasi
dengan anti
HIV lainnya
(bukan
didanosin)
Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV,
terutama
infeksi HIV
tingkat
lanjut,
dalam
kombinasi
dengan anti
HIV lainnya

pankreatitis
Kontraindikasi:
Potentially lifethreatening
hypersensitivity to
any component.

Aminoglycosides, amphotericin,
foscarnet
May increase risk of peripheral
neuropathy and other zalcitabine
toxicities caused by decreased
clearance of zalcitabine.
Chloramphenicol, cisplatin,
dapsone, disulfiram, ethionamide,
glutethimide, gold, hydralazine,
iodoquinol, isoniazid,
metronidazole, nitrofurantoin,
phenytoin, ribavirin, vincristine
May increase risk of peripheral
neuropathy.

Efek samping:
neuropati perifer,
asidosis laktat,
sakit kepala,
ruam, mual
Kontraindikasi:

Stavudine is
contraindicated
in patients with
clinically
significant
hypersensitivity
to stavudine or
to any of the
components
contained in the
formulation

Drugs associated with

pancreatitis (eg, pentamidine)
Fatal pancreatitis has occurred,
possibly related to zalcitabine and IV
pentamidine given concurrently.
Zidovudine: Zidovudine competitively
inhibits the intracellular
phosphorylation of stavudine.
Therefore, use of zidovudine in
combination with stavudine should be
avoided.
Doxorubicin: In vitro data indicate that
the phosphorylation of stavudine is
inhibited at relevant concentrations by
doxorubicin.

M: Metabolism

plays a limited
role in the
clearance of
stavudine.
Unchanged
stavudine was the
major drugrelated
component
circulating in
plasma after an
80-mg dose of
14C-stavudine,
while metabolites
constituted minor
components of the
circulating
radioactivity. Minor
metabolites include
oxidized stavudine,
glucuronide
conjugates of
stavudine and its
oxidized metabolite,
and an Nacetylcysteine
conjugate of the
ribose after
glycosidic cleavage,
suggesting that
thymine is also a
metabolite of
stavudine
E: Following an 80mg dose of 14Cstavudine to
healthy subjects,
approximately 95%
and 3% of the total
radioactivity was
recovered in urine
and feces,
respectively.

Ribavirin: In vitro data indicate

ribavirin reduces phosphorylation of
lamivudine, stavudine, and
zidovudine. However, no
pharmacokinetic (eg, plasma
concentrations or intracellular
triphosphorylated active metabolite
concentrations) or pharmacodynamic
(eg, loss of HIV/HCV virologic
suppression) interaction was observed
when ribavirin and lamivudine (n=18),
stavudine (n=10), or zidovudine (n=6)
were coadministered as part of a
multi-drug regimen to HIV/HCV coinfected patients
Stavudine does not inhibit the major
cytochrome P450 isoforms CYP1A2,
CYP2C9, CYP2C19, CYP2D6, and
CYP3A4; therefore, it is unlikely that
clinically significant drug interactions
will occur with drugs metabolized
through these pathways.
Because stavudine is not proteinbound, it is not expected to affect the
pharmacokinetics of protein-bound
drugs

5.
Lamivudin

Radioactivity due to
parent drug in urine
and feces was
73.7% and 62.0%,
respectively. The
mean terminal
elimination half-life
is approximately 2.3
hours following
single oral doses.
Mean renal
clearance of the
parent compound is
approximately 272
mL/min, accounting
for approximately
67% of the
apparent oral
clearance

A: C

max is
approximately
1.28mcg/mL
(single dose of
100 mg). T max is
0.5 to 2h.
Absolute
bioavailability is
approximately
87%
D: Less than 36%
protein bound. Vd
is approximately
1.3 L/kg
M: Metabolism of
lamivudine is a
minor route of
elimination. The
metabolite is
trans-sulfoxide
metabolite

Bekerja pada HIV RT & HBV RT

dengan cara menghentikan
pembentukan rantai DNA virus

Spektrum:
HIV type 1
& 2, HBV
Indikasi:
infeksi HIV
& HBV,
infeksi HIV
dalam
kombinasi
dengan anti
HIV lainnya
(zidovudin
& abakavir)

Efek samping:
asidosis laktat,
hepatomegali
dengan steatosis,
sakit kepala, mual
Kontraindikasi:
Potentially lifethreatening
hypersensitivity to
any component.

Drugs with active renal secretion

via the organic cationic transport
system (eg, trimethoprim)
Lamivudine Cl may be reduced,
increasing plasma concentrations.
Interferon- and ribavirin-based
regimens
Risk of hepatic decompensation may
be increased.
Zalcitabine

Spektrum:

Lamivudine and zalcitabine may

inhibit the intracellular
phosphorylation of one another. Use in
combination is not recommended

E: The majority is
6.
Emtrisitabin

eliminated
unchanged in the
urine. Mean halflife is 5 to 7 h. Cl
is approximately
398.5 mL/min
A: Rapidly and

extensively
absorbed after
oral
administration.
Absolute
bioavailability is
about 93%
(capsules) and
75% (solution).
Postdose T max
about 1 to 2 h.
Steady-state C max
is about 1.8
mcg/mL. AUC is
about 10
mcg/mLh. Mean
steady-state
trough plasma
concentration at
24 h postdose is
0.09 mcg/mL
7.

Abakavir

HIV type 1
& 2, HBV
Indikasi:
infeksi HIV
& HBV
Merupakan derivate 5-flourinated
lamivudin, diubah ke bentuk
trifosfat oleh enzim selular. Bekerja
pada HIV RT & HBV RT dengan cara
menghentikan pembentukan rantai
DNA virus

D:M:E: Plasma t

is
approximately 10
h. Eliminated in
the urine (86%
with 13% as
putative
metabolites) and
feces (14%).

Bekerja pada HIV RT dengan cara

menghentikan pembentukan rantai
DNA virus

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV,
dalam
kombinasi
dengan anti
HIV lainnya
(zidovudin,
lamivudin)

Efek samping:
nyeri abdomen,
diare, malaise,
sakit kepala,
lipodistrofi, mual,
rhinitis, pruritus,
ruam. Jarang:
reaksi alergi,
asidosis laktat,
mimpi buruk,
parestesia,
pneumonia,
steatosis hati
Kontraindikasi:
Potentially lifethreatening
hypersensitivity to
any component.

Efek samping:
mual, muntah,
diare, reaksi
hipersensitif
(demam, malaise,
ruam), gangguan
gastrointestinal
Kontraindikasi:

Do not coadminister with Atripla or

Truvada , or drugs containing
lamivudine

Ethanol

A: Rapidly and

extensively
absorbed.
Bioavailability is
83% (tablets). C
max is
approximately 3
mcg/mL and AUC
0-12 is
approximately
6.02 mcgh/mL
D: Vd after IV
administration is
approximately
0.86 L/kg. Plasma
protein binding is
approximately
50%
M: Metabolized to
inactive metabolites
by alcohol
dehydrogenase
E: 1.2% is excreted
in the urine as
abacavir; 81% as
inactive
metabolites; 16% is
excreted in the
feces. The half-life
is approximately
1.54 h and Cl is
approximately 0.8
L/h/kg (after IV
administration).

NtRTI
(Nucleotide
Reverse
Transcripta
se

Moderate or
severe hepatic
function
impairment;
hypersensitivity
to any
component of
the product.

Increases exposure to abacavir by

decreasing the elimination and
prolonging the half-life.
Methadone
Plasma levels of methadone may be
decreased in some patients, reducing
the therapeutic effect.

8.

Inhibitor)
Tenofovir
disoproksil
fumarat

A: Tenofovir C max is
approximately 0.3
mcg/mL and AUC is
approximately 2.29
ngh/mL. T max is
approximately 1 h,
and bioavailability
is approximately
25%. Administration
following a high-fat
meal increases the
oral bioavailability,
with an increase in
AUC of
approximately 40%
and a C max increase
of approximately
14%.
D: Vd of tenofovir is
approximately 1.3
L/kg. Binding to
plasma or serum
proteins is less than
0.7% and 7.2%,
respectively
M: Tenofovir is not a
CYP-450 substrate
E: Elimination of
tenofovir is by
glomerular filtration
and tubular
secretion.
Approximately 70%
to 80% is recovered
in urine as
unchanged drug.

Bekerja pada HIV RT & HBV RT

dengan cara menghentikan
pembentukan rantai DNA virus

Spektrum:
HIV type 1
& 2 serta
berbagai
retrovirus
lainnya &
HBV
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
efavirens,
tidak boleh
dikombinasi
dengan
lamivudin
& abakavir

Efek samping:
mual, muntah,
flatulens, diare
Kontraindikasi:

None well
documented.

Atazanavir, indinavir
May increase tenofovir plasma levels.
Tenofovir may decrease plasma levels
of atazanavir and indinavir, decreasing
the therapeutic effect. Do not
administer atazanavir without ritonavir
in patients receiving tenofovir.
Didanosine
Plasma concentrations of didanosine
may be increased, increasing the risk
of adverse reactions. Reduce the
didanosine dose to 250 mg when
administered with tenofovir in adults
weighing more than 60 kg. Monitor
patients closely and administer under
fasting conditions.
Drugs that reduce renal function
or compete for active tubular
secretion (eg, acyclovir, adefovir,
cidofovir, ganciclovir)
May increase serum levels of tenofovir
and/or increase the levels of other
renally eliminated drugs. Avoid
coadministration with adefovir.
Lopinavir/Ritonavir
May increase tenofovir plasma levels.
Nephrotoxic agents
Risk of nephrotoxicity may be
increased; avoid tenofovir in patients
who are currently receiving or have
recently received nephrotoxic agents.
NSAIDs (eg, ibuprofen)

May increase the pharmacologic and

toxic effects of tenofovir. Coadminister
with caution.
Tacrolimus
Coadministration increased C
tenofovir by 13%.

9.

NNRTI
(NonNucleoside
Reverse
Transcripta
se
Inhibitor)
Nevirapin

A: Nevirapine oral
absorption is more
than 90%,
bioavailability is
93% (tablets) and
91% (oral solution),
T max is 4 h, and C
max is approximately
2 mcg/mL
D: Nevirapine
crosses the
placenta and is
found in breast
milk. Protein
binding is
approximately 60%
and is highly
lipophilic and widely
distributed.
Nevirapine Vd is
1.21L/kg (IV), and
CSF approximates
45% of
concentration in
plasma.
M: Extensively
metabolized by CYP
isozymes. In vitro
studies indicated

Bekerja pada siklus alosterik

tempat ikatan non-substrat HIV-1
RT

Spektrum:
HIV type 1
Indikasi:
infeksi HIV1 dalam
kombinasi
dengan
anti-HIV
lainnya,
terutama
NRTI

Efek samping:
ruam, demam,
fatigue, sakit
kepala,
somnolens, mual,
peningkatan
enzim hati
Kontraindikasi:

Moderate or severe
(Child-Pugh class
B or C) hepatic
impairment.

max

of

Amiodarone, carbamazepine,
cisapride, clonazepam,
cyclophosphamide, cyclosporine,
diltiazem, disopyramide,
ergotamine, ethosuximide,
fentanyl, itraconazole, lidocaine
systemic, nifedipine, sirolimus,
tacrolimus, verapamil
Plasma levels may be decreased by
nevirapine.
Clarithromycin
Clarithromycin concentrations may be
reduced, while concentrations of the
active metabolite of clarithromycin
may be increased.
Contraceptives, hormonal
Lower hormone levels and potential
contraceptive failure.
Efavirenz, methadone
Concentrations of these agents may
be decreased by nevirapine.
Fluconazole
Nevirapine concentrations may be
increased.
HMG-CoA reductase inhibitors
(eg, atorvastatin, simvastatin)
Risk of severe myopathy or
rhabdomyolysis may be increased.
Ketoconazole

that metabolism is
primarily by CYP2B6
and CYP3A4
E: Nevirapine is
eliminated in urine
(81.3%) and feces
(10.1%). Less than
3% of the parent
compound is
excreted in urine.
Autoinduction
results in a
decrease of the
half-life from 45 h
(single dose) to
approximately 25 to
30 h (multiple doses

10
.
Delavirdin

A: Rapidly
absorbed. T max
approximately 1 h.
C max approximately
35 mcM. AUC
approximately 180
mcMh.
D: Approximately
98% protein bound,
primarily albumin
M: Primarily
metabolized by
CYP3A and possibly
CYP2D6 to several
inactive
metabolites.
E: Approximately
44% excreted in
feces and
approximately 51%
in urine (less than

Bekerja pada siklus alosterik

tempat ikatan non-substrat HIV-1
RT

Spektrum:
HIV type 1
Indikasi:
infeksi HIV1 dalam
kombinasi
dengan
anti-HIV
lainnya,
terutama
NRTI

Coadministration resulted in
significant reduction in ketoconazole
plasma concentrations. Do not
coadminister ketoconazole and
nevirapine.
Protease inhibitors (eg, indinavir)
Lower protease inhibitor plasma
levels.
Rifabutin
Rifabutin concentrations may be
increased.
Rifampin, rifabutin, rosiglitazone
Lower nevirapine plasma levels.
St. John's wort
May reduce nevirapine concentrations,
resulting in loss of virologic response
and possible resistance to nevirapine
and the class of NNRTIs.
Warfarin
Plasma concentrations of warfarin
may be altered, resulting in potential
increases in coagulation time.
Efek samping:
ruam, peningkatan
tes fungsi hati,
neutropenia
Kontraindikasi:
Potentially lifethreatening
hypersensitivity to
any component.

Antacids
Antacids reduce absorption of
delavirdine. Separate doses by at least
1h.
Anticonvulsants (eg,
carbamazepine, phenobarbital,
phenytoin)
Induce hepatic metabolism of
delavirdine resulting in decreased
plasma concentrations.
Benzodiazepines (eg, alprazolam,
midazolam, triazolam)
Delavirdine may increase blood levels
of these drugs, which may produce
extreme sedation and respiratory
depression.
Cisapride, dapsone, ergot
derivatives, quinidine, rifabutin,
warfarin
Delavirdine may elevate blood levels
of these drugs, which may increase
the risk of arrhythmias or other

5% as unchanged
drug). t is
approximately 5.8
h.

11
.

Efavirenz

A: C

is 1.6 to
9.1 mcM. T max is
3to 5h. Food
significantly
increases the AUC
and C max . Should
max

Bekerja pada siklus alosterik

tempat ikatan non-substrat HIV-1
RT

Spektrum:
HIV type 1
Indikasi:
infeksi HIV1 dalam
kombinasi
dengan
anti-HIV
lainnya,
terutama
NRTI &

Efek samping:
sakit kepala,
pusing, mimpi
buruk, sulit
konsentrasi, ruam
Kontraindikasi:

Concomitant use

potentially serious adverse reactions.

Clarithromycin
Coadministration may increase blood
levels of delavirdine or clarithromycin.
Didanosine
Separate administration of didanosine
and delavirdine by at least 1 h;
coadministration results in a 20%
reduction in systemic exposure of both
drugs.
Dihydropyridine calcium channel
blockers (eg, nifedipine)
Delavirdine may elevate blood levels,
which may increase toxicity.
Fluoxetine, ketoconazole
Increased delavirdine plasma
concentrations.
H 2 antagonists (eg, cimetidine)
Concurrent use may reduce absorption
of delavirdine. Chronic use of these
drugs with delavirdine is not
recommended.
Indinavir
Delavirdine inhibits metabolism of
indinavir. Consider indinavir dosage
reduction if coadministered with
delavirdine.
Rifabutin, rifampin
Induce hepatic metabolism of
delavirdine resulting in decreased
plasma concentrations. These agents
should not be coadministered with
delavirdine.
Saquinavir
Delavirdine inhibits metabolism of
saquinavir. Monitor hepatocellular
enzymes frequently if coadministered.

Astemizole, bepridil, cisapride,

ergot derivatives, midazolam,
pimozide, triazolam
May elevate levels of these drugs,
which may increase the risk of
arrhythmias, hematologic

be taken on an
empty stomach
D: Approximately
99.5% to 99.75%
is protein bound,
predominantly to
albumin
M: Metabolized in
the liver by CYP450 (primarily
CYP3A4 and
CYP2B6) to
inactive
metabolites
E: The half-life is
52 to 76 h (single
dose) and 40to
55 h (multiple
doses).
Approximately
14% to 34% is
excreted in the
urine (less than
1% as unchanged
drug), and 16% to
61% is excreted in
the feces.

NtRTI

with astemizole,
bepridil, cisapride,
ergot derivatives,
midazolam,
pimozide, St.
John's wort,
triazolam, or
voriconazole (in
standard doses);
hypersensitivity to
any component of
the product.

abnormalities, or other potentially

serious adverse reactions.
Coadministration is contraindicated.
Atazanavir, calcium channel
blockers (eg, diltiazem,
felodipine, nicardipine, nifedipine,
verapamil), clarithromycin,
fosamprenavir, HMG-CoA
reductase inhibitors (atorvastatin,
pravastatin, simvastatin),
indinavir, itraconazole,
ketoconazole, lopinavir,
methadone, rifabutin, saquinavir,
sertraline
Efavirenz may decrease plasma
concentrations of these agents, which
could reduce their efficacy.
Carbamazepine, phenobarbital,
phenytoin
Plasma concentrations of the
anticonvulsant may decrease.
Carbamazepine, phenobarbital,
phenytoin, rifampin
May decrease plasma levels of
efavirenz, which may reduce antiviral
activity.
Ethinyl estradiol, nelfinavir,
ritonavir
Efavirenz may increase plasma
concentrations, which could increase
activity or toxicity of these agents.
Food
Efavirenz plasma concentrations may
be elevated, increasing the risk of
adverse reactions. Efavirenz should be
taken on an empty stomach,
preferably at bedtime.
Ritonavir
May increase efavirenz plasma levels,
which could increase adverse
reactions.
St. John's wort
May reduce efavirenz plasma
concentrations, which may decrease
the clinical efficacy. Coadministration
is contraindicated.

Voriconazole
Contraindicated at standard doses.
Voriconazole doses should be
increased while efavirenz doses should
be decreased.
Warfarin
Plasma concentrations may be
increased or decreased

12
.

13
.

PI
(Protease
Inhibitor)
Sakuinavir

Ritonavir

A:
D:
M:
E:

A:
D:
M:
E:

Bekerja pada tahap transisi,

menghambat enzim HIV protease
peptidomimetic

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV
lainnya
(NRTI &
beberapa PI
seperti
ritonavir)

Efek samping:
diare, mual, nyeri
abdomen
Kontraindikasi:

Bekerja pada tahap transisi,

menghambat enzim HIV protease
peptidomimetic

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV
lainnya
(NRTI &
beberapa PI
seperti
sakuinavir)

Efek samping:
mual, muntah,
diare
Kontraindikasi:

14
.

Indinavir

Nelfinavir
15
.

Amprenavir
16
.

A:
D:
M:
E:

A:
D:
M:
E:

A:
D:
M:
E:

Bekerja pada tahap transisi,

menghambat enzim HIV protease
peptidomimetic

Bekerja pada tahap transisi,

menghambat enzim HIV protease
peptidomimetic

Bekerja pada tahap transisi,

menghambat enzim HIV protease
peptidomimetic

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV
lainnya
seperti
NRTI

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV
lainnya
seperti
NRTI
Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV

Efek samping:
mual,
hiperbilirubinemia,
batu ginjal
Kontraindikasi:

Efek samping:
diare, mual,
muntah
Kontraindikasi:

Efek samping:
mual, diare, ruam,
parestesia
perioral/ oral
Kontraindikasi:

Lopinavir

lainnya
seperti
NRTI

A:
D:
M:
E:

17
.
Bekerja pada tahap transisi,
menghambat enzim HIV protease
peptidomimetic
Atazanavir

A:
D:
M:
E:

Bekerja pada tahap transisi,

menghambat enzim HIV protease
peptidomimetic

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV
lainnya
seperti
NRTI

Menghambat masuknya HIV-1 ke

dalam sel dengan cara
menghambat fusi virus ke
membrane sel: berikatan dengan
HR1 (first heptad-repeat) pada
subunit gp41 envelope glikoprotein
virus serta menghambat terjadinya

Spektrum:
HIV type 1
Indikasi:
infeksi HIV1 dalam
kombinasi
dengan

18
.

19
.

Viral Entry
Inhibitor
Enfuvirtid

A:
D:
M:
E:

Spektrum:
HIV type 1
&2
Indikasi:
infeksi HIV
dalam
kombinasi
dengan
anti-HIV
lainnya
seperti
NRTI

Efek samping:
mual, muntah,
peningkatan kadar
kolesterol & TG,
peningkatan -GT
Kontraindikasi:

Efek samping:
hiperbilirubinemia,
mual, perubahan
EKG (jarang)
Kontraindikasi:

Efek samping:
reaksi local (nyeri,
eritema, pruritus,
iritasi, nodul/
kista), eosinofilia,
pneumonia
bakterial

perubahan konformasi yang

dibutuhkan untuk fusi virus ke
membrane sel

anti-HIV
lainnya

Kontraindikasi: