Tipranavir.txt

CLINICAL USE

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

DOSE IN NORMAL RENAL FUNCTION

500 mg twice daily in combination with ritonavir 200 mg twice daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 602.7

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : >99.9

%Excreted unchanged in urine &nbsp &nbsp : 0.5

Volume of distribution (L/kg) &nbsp &nbsp &nbsp : 7.7–10.2 litres

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp : 5.5–6/ unchanged

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: Not dialysed. Dose as for GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : Not dialysed. Dose as for GFR <10 mL/min

HDF/high flux &nbsp : Unknown dialysability. Dose as for GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp: Not dialysed. Dose as for GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs Antacids: avoid giving for 2 hours after tipranavir administration

Antibacterials: plasma concentration of clarithromycin and other macrolides increased – reduce dose of clarithromycin in renal impairment; concentration increased by clarithromycin; rifabutin concentration increased (risk of uveitis) – reduce dose; concentration reduced by rifampicin – avoid concomitant use; avoid concomitant use with telithromycin in severe renal and hepatic failure

Antidepressants: concentration possibly reduced by St John’s wort – avoid concomitant use

Antimalarials: possibly increased risk of ventricular arrhythmias with artemether/ lumefantrine – avoid concomitant use

Antivirals: reduces concentration of abacavir, amprenavir, didanosine, lopinavir, saquinavir and zidovudine; concentration increased by atazanavir

Ciclosporin: levels possibly altered by tipranavir Sirolimus: levels possibly altered by tipranavir

Tacrolimus: levels possibly altered by tipranavir

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Administer with food; enhanced bioavailability with high fat meals .

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