indinavir

CLINICAL USE

Protease inhibitor:Treatment of HIV infection, in combination with a nucleoside reverse transcriptase inhibitor

DOSE IN NORMAL RENAL FUNCTION

800 mg every 8 hours

PHARMACOKINETICS

Molecular weight :711.9 (as sulphate)

%Protein binding :60

%Excreted unchanged in urine : 10.4

Volume of distribution (L/kg) :14

half-life – normal/ESRD (hrs) :1.8/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function Monitor closely

10 to 20 : Dose as in normal renal function Monitor closely

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

HDF/high flux :Not dialysed. Dose as in GFR <10 mL/min

CAV/VVHD :Unlikely to be dialysed. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anti-arrhythmics: possibly increased amiodarone concentration – avoid concomitant use

Antibacterials: rifampicin increases metabolism – avoid concomitant use; increased rifabutin concentration and rifabutin reduces indinavir concentration – reduce dose of rifabutin by 50% and increase dose of indinavir; avoid with telithromycin in severe renal and hepatic failure

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

Anti-epileptics: concentration possibly reduced by carbamazepine, phenytoin, primidone and barbiturates

Antifungals: ketoconazole inhibits metabolism – reduce dose of indinavir to 600 mg every 8 hours; concentration increased by itraconazole – consider reducing indinavir

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antipsychotics: possibly increased risk of ventricular arrhythmias with pimozide and sertindole – avoid concomitant use; possibly inhibits aripiprazole metabolism – reduce aripiprazole dose

Antivirals: avoid with atazanavir; concentration reduced by efavirenz and nevirapine; with nelfinavir and darunavir, concentration of both drugs increased; concentration increased by ritonavir; saquinavir concentration increasedAnxiolytics and hypnotics: increased risk of prolonged sedation with alprazolam and midazolam – avoid concomitant useCilostazol: concentration of cilostazol possibly increased – avoid concomitant use

Ergot alkaloids: risk of ergotism – avoid concomitant useLipid-regulating drugs: increased risk of myopathy with simvastatin – avoid concomitant use; and possibly with atorvastatin5HT 1 agonists: concentration of eletriptan increased – avoid concomitant useSildenafil: concentration of sildenafil increased – reduce initial sildenafil dose

Vardenafil: concentration of vardenafil increased – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

Drink 1.5 litres of water in 24 hours .380 indinAVirGive 1 hour before, or 2 hours after food, or with a low fat meal with water

OTHER INFORMATION

If giving with didanosine, leave 1 hour between each drugMild renal insufficiency is usually due to crystalluria, but a case of interstitial nephritis has been reportedIf nephrolithiasis with flank pain occurs (with or without haematuria), temporarily stop therapy (e.g. for 1–3 days)

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