Lopinavir
Lopinavir.JPG

Lopinavir

CLINICAL USE

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

DOSE IN NORMAL RENAL FUNCTION

3 capsules twice daily (in combination with ritonavir, Kaletra), or 5 mL twice daily

PHARMACOKINETICS

  • Molecular weight                           :628.8
  • %Protein binding                           :98–99
  • %Excreted unchanged in urine     : 2.2
  • Volume of distribution (L/kg)       :0.5
  • half-life – normal/ESRD (hrs)      :5–6/12–17

    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. Monitor closely

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unlikely to be dialysed. Dose as in GFR <10 mL/min
  • HD                     :Unlikely to be dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unlikely to be dialysed. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Antibacterials: concentration reduced by rifampicin – 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
  • Anti-epileptics: concentration possibly reduced by carbamazepine, phenytoin and primidone
  • Antimalarials: avoid concomitant use with artemether/lumefantrine
  • Antipsychotics: possibly inhibits metabolism of aripiprazole – reduce dose of aripiprazole; increased concentration of sertindole (increased risk of ventricular arrhythmias) – avoid concomitant use
  • Antivirals: amprenavir concentration reduced, concentration reduced by efavirenz, tipranavir and nelfinavir; active metabolite of nelfinavir increased; concentration possibly reduced by nevirapine; concentration of saquinavir and tenofovir increased; concentration increased by darunavir and darunavir concentration reducedBarbiturates: concentration reduced by phenobarbital
  • Ciclosporin: may increase concentration of ciclosporinCilostazol: possibly increases concentration of cilostazol – avoid concomitant useSirolimus: may increase concentration of sirolimusStatins: increased risk of myopathy with atorvastatin; possibly increased risk of myopathy with simvastatin – avoid concomitant use
  • Tacrolimus: may increase concentration of tacrolimus

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    Take with food

    OTHER INFORMATION

    3 capsules = 5 mL of oral solution .



    See how to identify renal failure stages according to GFR calculation

    See how to diagnose irreversible renal disease

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