Kaletra and Sustiva (Efavirenz Tablets)

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Talk to your doctor before using lopinavir together with efavirenz. Combining these medications can decrease the blood levels of lopinavir, which may reduce its effectiveness in treating HIV infection. Your doctor may be able to prescribe alternatives that do not interact, or you may need a dose adjustment or more frequent monitoring to safely use both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

ADJUST DOSE: Coadministration with efavirenz may decrease the plasma concentrations of lopinavir, even in the presence of low-dose ritonavir as a pharmacokinetic booster. The proposed mechanism is efavirenz induction of lopinavir metabolism via CYP450 3A4. In a parallel group study consisting of healthy, HIV-negative subjects, coadministration of lopinavir-ritonavir (400 mg-100 mg capsule twice a day) with efavirenz (600 mg once daily) for nine days resulted in a 19% relative decrease in lopinavir systemic exposure (AUC) and a 39% relative decrease in trough plasma concentration (Cmin) in 11 subjects compared to administration of lopinavir-ritonavir alone in 7 subjects. Efavirenz Cmax and AUC were also reduced by 16% each compared to administration of efavirenz alone in 12 healthy subjects. When the dosage of lopinavir-ritonavir was increased to 500 mg-125 mg (two 200 mg-50 mg tablets and one 100 mg-25 mg tablet) twice daily and coadministered with efavirenz for nine days in 19 healthy subjects, similar lopinavir concentrations were observed compared to lopinavir-ritonavir 400 mg-100 mg (two 200 mg-50 mg tablets) administered twice daily without efavirenz. By contrast, when the lopinavir-ritonavir dosage was increased to 600 mg-150 mg (three 200 mg-50 mg tablets) twice daily and coadministered with efavirenz for nine days in 23 healthy subjects, lopinavir plasma concentrations were significantly increased by approximately 35% and ritonavir concentrations by 56% to 92% compared to lopinavir-ritonavir 400 mg-100 mg (two 200 mg-50 mg tablets) administered twice daily without efavirenz. The clinical significance in terms of safety and efficacy is unknown. In healthy volunteers, lopinavir-ritonavir did not significantly affect the plasma concentrations of efavirenz. However, due to study discontinuations, there was limited power to detect changes in efavirenz pharmacokinetics in the presence of lopinavir-ritonavir.

MANAGEMENT: A dosage increase is recommended for lopinavir-ritonavir when used in combination with efavirenz. For adults, the dosage should be increased to 500 mg-125 mg (two 200 mg-50 mg tablets and one 100 mg-25 mg tablet) twice daily for the tablets and 533 mg-133 mg (6.5 mL) twice daily for the oral solution. Lopinavir-ritonavir should not be administered as a once daily regimen in combination with efavirenz. For pediatric patients 6 months to 18 years of age, the dosage should be increased to 300 mg-75 mg/m2 twice daily for the oral solution in both treatment-naive and treatment-experienced patients, not to exceed the recommended adult dosage of 533 mg-133 mg (6.5 mL) twice daily. If weight-based dosing is preferred, the recommended dosage is 13 mg-3.25 mg/kg given twice daily for patients under 15 kg and 11 mg-2.75 mg/kg given twice daily for patients 15 kg to 45 kg. Pediatric patients weighing more than 45 kg should receive the adult dosage of lopinavir-ritonavir. Please consult the manufacturer's product labeling for pediatric dosing of the tablet formulation. Lopinavir-ritonavir should not be administered in combination with efavirenz in patients under 6 months of age due to the lack of clinical data.

Kaletra

Generic Name: lopinavir / ritonavir

Brand name: Kaletra

Synonyms: n.a.

What is Kaletra?

Sustiva (Efavirenz Tablets)

Generic Name: efavirenz

Brand name: Sustiva

Synonyms: Sustiva

What is Sustiva (Efavirenz Tablets)?