Atazanavir

CLINICAL USE


Protease inhibitor:

  • HIV infection, in combination with other

    antiretroviral drugs

    DOSE IN NORMAL RENAL FUNCTION


    300 mg once daily with ritonavir 100 mg once
    daily

    PHARMACOKINETICS


  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    802.9 (as sulphate)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    86
  • %Excreted unchanged in urine &nbsp &nbsp :
    7
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
    No data
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
    7/no data

    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:
    Unknown dialysability. Dose as in
    normal renal function

    IMPORTANT DRUG INTERACTIONS


    Potentially hazardous interactions with other drugs

  • Anti-arrhythmics: possibly increased

    plasma levels of amiodarone and lidocaine

  • Antibacterials: concentration of both

    drugs increased when given with
    clarithromycin; rifabutin concentration
    increased – reduce dose of rifabutin;
    rifampicin reduces atazanavir
    concentration – avoid concomitant use;
    avoid concomitant use with telithromycin
    in severe renal and hepatic impairment

  • Antidepressants: concentration reduced by

    St John’s wort – avoid concomitant use

  • Antimalarials: avoid concomitant

    administration with artemether/
    lumefantrine

  • Antipsychotics: possibly inhibits

    metabolism of aripiprazole – reduce
    dose of aripiprazole; possibly increased
    concentration of pimozide – avoid
    concomitant use

  • Antivirals: concentration reduced by

    efavirenz –increase dose of atazanavir;
    concentration possibly reduced by
    nevirapine – avoid concomitant use;
    saquinavir concentration increased;
    concentration reduced by tenofovir and
    tenofovir concentration possibly increased;
    avoid concomitant use with indinavir
    C

  • alcium-channel blockers: concentration

    of diltiazem increased – reduce dose of
    diltiazem; possibly increased verapamil
    concentration

  • Ciclosporin: possibly increased

    concentration of ciclosporin

  • Cytotoxics: possibly inhibits metabolism of

    irinotecan – increased risk of toxicity

  • Ergot alkaloids: possibly increased

    concentration of ergot alkaloids – avoid
    concomitant use
    Oestrogens: increased concentration of

    ethinylestradiol – avoid concomitant use
    Sildenafil: possibly increased side effects

    of sildenafil

  • Sirolimus: possibly increased

    concentration of sirolimus
    Statins: avoid concomitant use with

    simvastatin – increased risk of myopathy;
    possibly increased risk of myopathy with
    atorvastatin
    t is not licensed for use by anyone else.

  • Tacrolimus: possibly increased

    concentration of tacrolimus

  • Ulcer-healing drugs: concentration

    significantly reduced by omeprazole and
    esomeprazole and possibly other proton
    pump inhibitors – avoid concomitant
    use; concentration possibly reduced by
    histamine H2 antagonists

    ADMINISTRATION


    Reconstition



    Route


    Oral

    Rate of Administration


    Take with food

    Comments


    Take didanosine 2 hours after atazanavir if

    used in combination