lopinavir / ritonavir

Detailed Prescribing Information

Without boosting: 3-4 soft gel capsules twice a day with food

With boosting: 3 soft gel capsules + 1x100 mg ritonavir, both twice a day with food

Antiretroviral Naïve patients only - single daily dosing (approved 4.29.2005): 4 x 200/50 tablets or 6 caps (133/33) as a single dose with food

Also perioral paresthesia, hepatitis, fat redistribution, hyperlipidemia, Type 2 diabetes
There appears to be a small chance (4%) of nephrolithiasis associated with lopinavir/ritonavir.

Lopinavir/ritonavir produces the following interactions:

Increases tenofovir levels significantly (~30%) in two studies with 1.8% of subjects developing renal insufficiency and 1 patient developed Fanconi syndrome
Increases indinavir (consider use 600 twice a day of indinavir)

Increases saquinavir (consider 800 mg twice a day of saquinavir)

Increases antiarrhythmic levels (use drug level monitoring)

Increases clarithromycin levels (decrease clarithromycin for Ccr < 60 cc/hr)

Increases ketoconazole, itraconazole levels

Increases rifabutin levels (decrease rifabutin to 150 mg every other day and monitor closely for toxicity and consider further dosing reduction)

Increases dihydropyridine calcium channel blocker levels

Increases intraconazole levels
Increases tadalafil levels significantly: use tadalafil (Cialis) with caution at reduced doses of 10 mg every 72 hours with increased monitoring for adverse events
Increases vardenafil levels significantly; Use vardenafil (Levitra) with caution at reduced doses of no more than 2.5 mg every 72 hours with increased monitoring for adverse events
Increases fluticasone levels such that adrenal suppression or Cushing's syndrome may develop

Decreases atovaquone levels

Decreases dexamethasone levels

Increases sildenafil levels (decrease dose of sildenafil to 25 mg every other day maximum frequency)

Decreases methadone levels - withdrawal may be precipitated

Decreases oral contraceptive levels (use additional contraceptive method)

Variably affects anticoagulation: monitor anticoagulation with warfarin closely

Lopinavir/ritonavir is affected by the following:

Lopinavir levels are decreased very significantly by amprenavir and fosamprenavir

Lopinavir levels decreased by nevirapine and efavirenz (increase Kaletra to 4 caps twice a day with food)

Delavirdine increases lopinavir levels

Fosamprenavir decreases lopinavir levels by 60% and fosamprenavir levels are decreased by up to 70% by lopinavir

Anticonvulsants decrease lopinavir levels (avoid use)

Concomitant fosamprenavir or amprenavir are not recommended (at least until much more data is available 6/2004)
Due to markedly increased fluticasone levels avoid use of Flonase or other fluticasone containing medications if possible.
Do not use single daily dosing in antiretroviral-experienced patients