Darunavir

CLINICAL USE

Protease inhibitor:Treatment of HIV infection with 100 mg of ritonavir, in combination with other antiretroviral medication

DOSE IN NORMAL RENAL FUNCTION

600 mg twice daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :593.7 (as ethanolate)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :95

%Excreted unchanged in urine &nbsp &nbsp : 7.7

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :29.1–147.1 litres (81.1–180.9 litres with ritonavir)

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :15 (with ritonavir)/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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

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

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

CAV/VVHD &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsAntibacterials: rifabutin concentration increased – reduce dose of rifabutin; darunavir concentration reduced by rifampicin – avoid concomitant useAntidepressants: possibly reduced concentration of paroxetine and sertraline; darunavir concentration reduced by St John’s wort – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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