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 &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :628.8

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :98–99

%Excreted unchanged in urine &nbsp &nbsp : 2.2

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.5

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :5–6/12–17

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. Monitor closely

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unlikely to be dialysed. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Unlikely to be dialysed. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp: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

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Route

Oral

Rate of Administration

–

Comments

Take with food

OTHER INFORMATION

3 capsules = 5 mL of oral solution .

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