HEALTHY LIFESTYLE




Fosamprenavir
Fosamprenavir.JPG

Fosamprenavir

CLINICAL USE

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

DOSE IN NORMAL RENAL FUNCTION

700 mg twice daily with ritonavir 100 mg twice daily

PHARMACOKINETICS

  • Molecular weight                           :625.7 (as calcium salt)
  • %Protein binding                           :90 (amprenavir)
  • %Excreted unchanged in urine     : <1 (amprenavir)
  • Volume of distribution (L/kg)       :6 (amprenavir)
  • half-life – normal/ESRD (hrs)      :7.7/Unchanged (amprenavir)

    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 concentration of amiodarone, flecainide, lidocaine and propafenone (increased risk of ventricular arrhythmias) – avoid concomitant use
  • Antibacterials: concentration of both drugs increased with erythromycin; increases concentration of rifabutin – reduce rifabutin dose; concentration significantly reduced by rifampicin – avoid concomitant use; possibly increases 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 increases side effects of tricyclics; possibly reduces paroxetine concentration
  • Antimalarials: avoid concomitant administration with artemether/lumefantrine
  • Antipsychotics: possibly inhibits aripiprazole metabolism – reduce aripiprazole dose; possibly increases clozapine concentration; possibly increases 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 ritonavirAnxiolytics and hypnotics: increased risk of prolonged sedation and respiratory depression with alprazolam, clonazepam, diazepam, flurazepam and midazolamCilostazol: possibly increases cilostazol concentration – avoid concomitant use
  • Ergot alkaloids: increased risk of ergotism – avoid concomitant useImmunosuppressants: monitor ciclosporin, tacrolimus and sirolimus levelsStatins: possibly increased risk of myopathy with atorvastatin; possibly increased myopathy with simvastatin – avoid concomitant use

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Prodrug of amprenavir, 700 mg of fosamprenavir is equivalent to 600 mg amprenavir.
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