Atazanavir

CLINICAL USE

Protease inhibitor:

HIV infection, in combination with other antiretroviral 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 increased plasma levels of amiodarone and lidocaine

Antibacterials: concentration of both drugs 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 by St John’s wort – avoid concomitant use

Antimalarials: avoid concomitant administration with artemether/ lumefantrine

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

Antivirals: concentration reduced by efavirenz –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: concentration of diltiazem increased – reduce dose of diltiazem; possibly increased verapamil concentration

Ciclosporin: possibly increased concentration of ciclosporin

Cytotoxics: possibly inhibits metabolism of irinotecan – increased risk of toxicity

Ergot alkaloids: possibly increased concentration of ergot alkaloids – avoid concomitant use Oestrogens: increased concentration of ethinylestradiol – avoid concomitant use Sildenafil: possibly increased side effects of sildenafil

Sirolimus: possibly increased concentration 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 increased concentration of tacrolimus

Ulcer-healing drugs: concentration significantly 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

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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