Lopinavir
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)       :0.5half-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/minHDF/high flux   :Unlikely to be dialysed. Dose as in GFR <10 mL/minCAV/VVHD      :Unknown dialysability. Dose as in normal renal function IMPORTANT DRUG INTERACTIONS
Potentially hazardous interactions with other drugsAntibacterials: concentration reduced by rifampicin – avoid concomitant use; avoid concomitant use with telithromycin in severe renal and hepatic impairmentAntidepressants: concentration reduced by St John’s wort – avoid concomitant useAnti-epileptics: concentration possibly reduced by carbamazepine, phenytoin and primidoneAntimalarials: avoid concomitant use with artemether/lumefantrineAntipsychotics: possibly inhibits metabolism of aripiprazole – reduce dose of aripiprazole; increased concentration of sertindole (increased risk of ventricular arrhythmias) – avoid concomitant useAntivirals: 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 phenobarbitalCiclosporin: 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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