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Kaletra Oral Solution and Nelfinavir

Determining the interaction of Kaletra Oral Solution and Nelfinavir and the possibility of their joint administration.

Check result:
Kaletra Oral Solution <> Nelfinavir
Relevance: 05.01.2023 Reviewer: Shkutko P.M., M.D., in

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.

Consumer:

Talk to your doctor before using lopinavir together with nelfinavir. Combining these medications can decrease the blood levels of lopinavir, which may reduce its effectiveness in treating HIV infection. In addition, nelfinavir levels may increase and cause you to experience greater or more severe side effects. 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.

Professional:

ADJUST DOSE: Coadministration with nelfinavir may decrease the plasma concentrations of lopinavir, even in the presence of low-dose ritonavir as a pharmacokinetic booster. The proposed mechanism is nelfinavir induction of lopinavir metabolism via CYP450 3A4. In 13 healthy volunteers, administration of lopinavir-ritonavir (400 mg-100 mg capsule twice a day for 21 days) in combination with nelfinavir (1000 mg twice a day for 10 days) resulted in a 21% decrease in lopinavir peak plasma concentration (Cmax), a 27% decrease in systemic exposure (AUC), and a 38% decrease in trough plasma concentration (Cmin) compared to administration of lopinavir-ritonavir alone. Conversely, nelfinavir Cmin increased by 86%, and the Cmax, AUC and Cmin of its M8 metabolite increased by 2.4-fold, 3.5-fold and 7.5-fold, respectively, compared to administration of nelfinavir alone (1250 mg twice a day for 14 days). The clinical significance of these increases in terms of safety and efficacy is unknown.

MANAGEMENT: A dosage increase is recommended for lopinavir-ritonavir when used in combination with nelfinavir. 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 nelfinavir. 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 nelfinavir in patients under 6 months of age due to the lack of clinical data.

References
  • "Product Information. Kaletra (lopinavir-ritonavir)" Abbott Pharmaceutical, Abbott Park, IL.
  • Canadian Pharmacists Association "e-CPS. Available from: URL: http://www.pharmacists.ca/function/Subscriptions/ecps.cfm?link=eCPS_quikLink."
Kaletra Oral Solution

Generic Name: lopinavir / ritonavir

Brand name: Kaletra

Synonyms: Kaletra

Nelfinavir

Generic Name: nelfinavir

Brand name: Viracept

Synonyms: n.a.

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

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