CLINICAL USE

Protease inhibitor:Treatment of HIV-1 infection in combination other antiretrovirals

DOSE IN NORMAL RENAL FUNCTION

600 mg twice dailyAs low dose booster with other protease inhibitors: 100–200 mg once or twice daily

PHARMACOKINETICS

  • Molecular weight                           :720.9
  • %Protein binding                           :98–99
  • %Excreted unchanged in urine     : 3.5
  • Volume of distribution (L/kg)       :0.4
  • half-life – normal/ESRD (hrs)      :3–5/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 in normal renal function
  • HD                     :Not dialysed. Dose as in normal renal function
  • HDF/high flux   :Not dialysed. Dose as in normal renal function
  • CAV/VVHD      :Unlikely to be dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsAlfuzosin: avoid concomitant use

  • Analgesics: opioid and NSAID levels may be increased (risk of toxicity) – avoid dextropropoxyphene and piroxicam; methadone and pethidine levels reduced; increased fentanyl and toxic pethidine metabolite concentration – avoid with pethidine
  • Anti-arrhythmics: increased concentration of amiodarone, flecainide and propafenone (increased risk of ventricular arrhythmias) – avoid concomitant use; possible increased risk of arrhythmias with disopyramide and mexiletine
  • Antibacterials: rifabutin concentration increased (risk of uveitis) – avoid; concentration of clarithromycin and other macrolides increased – reduce dose of clarithromycin in renal impairment; concentration of both drugs may be increased in combination with fusidic acid; avoid with telithromycin in renal and hepatic failure
  • Anticoagulants: anticoagulant effect of coumarins and phenindione possibly increased; effect of warfarin may be enhanced or reduced
  • Antidepressants: SSRIs and tricyclic concentrations possibly increased; concentration reduced by St John’s wort; possibly reduced paroxetine concentration; increased side effects with trazodone
  • Anti-epileptics: carbamazepine and phenytoin concentration may be increased; concentration reduced by phenytoin
  • Antifungals: in combination with itraconazole or ketoconazole concentration of both drugs may be increased; concentration increased by fluconazole; voriconazole concentration reduced – avoid
  • Antimalarials: avoid concomitant use with artemether/lumefantrine
  • Antipsychotics: concentration of pimozide, sertindole, clozapine and possibly other antipsychotics may be increased (risk of toxicity) – avoid concomitant use; possibly inhibits metabolism of aripiprazole – reduce aripiprazole dose; olanzapine concentration reduced
  • Antivirals: levels of both nelfinavir and ritonavir may be increased if used in combination; amprenavir, indinavir and saquinavir levels increased; increased risk of toxicity with efavirenz – monitor LFTs
    Anxiolytics and hypnotics: levels of many of them increased (risk of extreme sedation and respiratory depression) – avoid alprazolam, diazepam, flurazepam, midazolam, zolpidem; concentration of buspirone increasedBupropion: bupropion levels increased (risk of toxicity) – avoid
  • Calcium-channel blockers: levels of blockers possibly increased – avoid with lercanidipine.
  • Ciclosporin: levels possibly increased by ritonavir
    Cilostazol: concentration of cilostazol possibly increased – avoid concomitant use
    Corticosteroids: possibly increased corticosteroid concentration; increased concentration of inhaled/intranasal budesonide and fluticasone
  • Diuretics: eplerenone concentration increased – avoid concomitant use
  • Ergot alkaloids: risk of ergotism – avoid Ivabradine: ivabradine concentration possibly increased – avoid concomitant useLipid-lowering drugs: increased risk of myopathy with simvastatin – avoid; possibly increased risk of myopathy with atorvastatin
    Oestrogens and progestogens: metabolism accelerated (contraceptive effect reduced)5HT 1 agonists: concentration of eletriptan increased – avoidSildenafil: concentrations of sildenafil significantly increased – avoid
    Theophylline: metabolism accelerated, theophylline levels reduced
  • Tacrolimus: levels possibly increased by ritonavir
  • Vardenafil: possibly increased vardenafil concentration – avoid concomitant use

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Administer with food .

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