Atazanavir

CLINICAL USE

Protease inhibitor:

HIV infection, in combination with otherantiretroviral drugs

DOSE IN NORMAL RENAL FUNCTION

300 mg once daily with ritonavir 100 mg once
daily

PHARMACOKINETICS

Molecular weight :
802.9 (as sulphate)

%Protein binding :
86

%Excreted unchanged in urine :
7

Volume of distribution (L/kg) :
No data

half-life – normal/ESRD (hrs) :
7/no data

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Dose as in normal renal function

<10 :
Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :
Unlikely to be dialysed. Dose as in
normal renal function

HD :
Unlikely to be dialysed. Dose as in
normal renal function

HDF/high flux :
Unlikely to be dialysed. Dose as in
normal renal function

CAV/VVHD :
Unknown dialysability. Dose as in
normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anti-arrhythmics: possibly increasedplasma levels of amiodarone and lidocaine

Antibacterials: concentration of bothdrugs increased when given with
clarithromycin; rifabutin concentration
increased – reduce dose of rifabutin;
rifampicin reduces atazanavir
concentration – avoid concomitant use;
avoid concomitant use with telithromycin
in severe renal and hepatic impairment

Antidepressants: concentration reduced bySt John’s wort – avoid concomitant use

Antimalarials: avoid concomitantadministration with artemether/
lumefantrine

Antipsychotics: possibly inhibitsmetabolism of aripiprazole – reduce
dose of aripiprazole; possibly increased
concentration of pimozide – avoid
concomitant use

Antivirals: concentration reduced byefavirenz –increase dose of atazanavir;
concentration possibly reduced by
nevirapine – avoid concomitant use;
saquinavir concentration increased;
concentration reduced by tenofovir and
tenofovir concentration possibly increased;
avoid concomitant use with indinavir
C

alcium-channel blockers: concentrationof diltiazem increased – reduce dose of
diltiazem; possibly increased verapamil
concentration

Ciclosporin: possibly increasedconcentration of ciclosporin

Cytotoxics: possibly inhibits metabolism ofirinotecan – increased risk of toxicity

Ergot alkaloids: possibly increasedconcentration of ergot alkaloids – avoid
concomitant use
Oestrogens: increased concentration of

ethinylestradiol – avoid concomitant use
Sildenafil: possibly increased side effects

of sildenafil

Sirolimus: possibly increasedconcentration of sirolimus
Statins: avoid concomitant use with

simvastatin – increased risk of myopathy;
possibly increased risk of myopathy with
atorvastatin
t is not licensed for use by anyone else.

Tacrolimus: possibly increasedconcentration of tacrolimus

Ulcer-healing drugs: concentrationsignificantly reduced by omeprazole and
esomeprazole and possibly other proton
pump inhibitors – avoid concomitant
use; concentration possibly reduced by
histamine H2 antagonists

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

Take with food

Comments

Take didanosine 2 hours after atazanavir if

used in combination

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