CLINICAL USE

Protease inhibitor: Treatment of HIV infected patients in combination with ritonavir and other antiretroviral agents

DOSE IN NORMAL RENAL FUNCTION

500 mg twice daily in combination with ritonavir 200 mg twice daily

PHARMACOKINETICS

  • Molecular weight                           : 602.7
  • %Protein binding                           : >99.9
  • %Excreted unchanged in urine     : 0.5
  • Volume of distribution (L/kg)       : 7.7–10.2 litres
  • half-life – normal/ESRD (hrs)      : 5.5–6/ 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                : Not dialysed. Dose as for GFR <10 mL/min
  • HD                     : Not dialysed. Dose as for GFR <10 mL/min
  • HDF/high flux   : Unknown dialysability. Dose as for GFR <10 mL/min
  • CAV/VVHD      : Not dialysed. Dose as for GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs Antacids: avoid giving for 2 hours after tipranavir administration

  • Antibacterials: plasma concentration of clarithromycin and other macrolides increased – reduce dose of clarithromycin in renal impairment; concentration increased by clarithromycin; rifabutin concentration increased (risk of uveitis) – reduce dose; concentration reduced by rifampicin – avoid concomitant use; avoid concomitant use with telithromycin in severe renal and hepatic failure
  • Antidepressants: concentration possibly reduced by St John’s wort – avoid concomitant use
  • Antimalarials: possibly increased risk of ventricular arrhythmias with artemether/ lumefantrine – avoid concomitant use
  • Antivirals: reduces concentration of abacavir, amprenavir, didanosine, lopinavir, saquinavir and zidovudine; concentration increased by atazanavir
  • Ciclosporin: levels possibly altered by tipranavir Sirolimus: levels possibly altered by tipranavir
  • Tacrolimus: levels possibly altered by tipranavir

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Administer with food; enhanced bioavailability with high fat meals .

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