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 &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
505.6

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
90

%Excreted unchanged in urine &nbsp &nbsp :
<3

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
6

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
7.1–10.6/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 :
Not 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:
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

–

Route

Oral

Rate of Administration

–

Comments

–

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

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