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)

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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