Amprenavir

CLINICAL USE

Protease inhibitor: HIV infection, in combination with other antiretroviral drugs

DOSE IN NORMAL RENAL FUNCTION

Capsules:

>50 kg: 1.2 g, twice a day

<50 kg: 20 mg/kg, twice a day; maximum 2.4 g daily

With ritonavir 100 mg, twice a day: >50 kg: 600 mg, twice a day Oral solution: 17 mg/kg every 8 hours; maximum 2.8 g daily

PHARMACOKINETICS

Molecular weight : 505.6

%Protein binding : 90

%Excreted unchanged in urine : <3

Volume of distribution (L/kg) : 6

half-life – normal/ESRD (hrs) : 7.1–10.6/Unchanged

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 : Not 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 increase concentration of amiodarone, flecainide, lidocaine and propafenone (increased risk of ventricular arrhythmias) – avoid concomitant use

Antibacterials: concentration of both drugs increased with erythromycin; increased concentration of rifabutin – reduce rifabutin dose; concentration significantly reduced by rifampicin – avoid concomitant use; possibly increased dapsone concentration; avoid concomitant use with telithromycin in severe renal and hepatic impairment

Antidepressants: concentration reduced by St John’s wort – avoid concomitant use; possibly increased side effects of tricyclics; possibly reduced paroxetine concentration

Antimalarials: avoid concomitant administration with artemether/ lumefantrine

Antipsychotics: possibly inhibit aripiprazole metabolism – reduce aripiprazole dose; possibly increased clozapine concentration; increased pimozide and sertindole concentration (increased risk of ventricular arrhythmias) – avoid concomitant use

Antivirals: concentration reduced by efavirenz, lopinavir and tipranavir; concentration possibly reduced by nevirapine; concentration increased by ritonavir

Anxiolytics and hypnotics: increased risk of prolonged sedation and respiratory depression with alprazolam, clonazepam, diazepam, flurazepam and midazolam

Cilostazol: possibly increased cilostazol concentration – avoid concomitant use Ergot alkaloids: increased risk of ergotism – avoid concomitant use.

Immunosuppressants: monitor ciclosporin, tacrolimus and sirolimus levels Statins: possibly increased risk of myopathy with atorvastatin; possibly increased myopathy with simvastatin – avoid concomitant use t is not licensed for use by anyone else. 54 AMPrEnAVir

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Oral solution contains vitamin E 46 units/ mL, potassium 26 micromol/mL and sodium 174 micromol/mL

Avoid oral solution in renal impairment due to possible accumulation of propylene glycol

Bioavailability of oral solution is 14–19% less than the capsules

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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