Lopinavir / Ritonavir

What it is and how it works

Mechanism of Action Lopinavir and ritonavir is a fixed-dose combination of HIV-1 antiviral drugs lopinavir and ritonavir. As co-formulated in lopinavir and ritonavir, ritonavir inhibits the CYP3A-mediated metabolism of lopinavir, thereby providing increased plasma levels of lopinavir.

Mechanism class: HIV Protease Inhibitors · Cytochrome P450 3A Inhibitors · Cytochrome P450 2D6 Inhibitors

Indications

Lopinavir and ritonavir tablets are indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients 14 days and older. Limitations of Use: • Genotypic or phenotypic testing and/or treatment history should guide the use of lopinavir and ritonavir tablets. The number of baseline lopinavir resistance-associated substitutions affects the virologic response to lopinavir and ritonavir tablets . Lopinavir and ritonavir tablets are an HIV-1 protease inhibitor indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients (14 days and older).

Dosage and administration (summary)

Tablets: May be taken with or without food, swallowed whole and not chewed, broken, or crushed. Adults : • Total recommended daily dosage is 800/200 mg given once or twice daily. • Lopinavir and ritonavir tablets can be given as once daily or twice daily regimen. See Full Prescribing Information for details. • Lopinavir and ritonavir tablets once daily dosing regimen is not recommended in: • Adult patients with three or more of the following lopinavir resistance-associated substitutions: L10F/I/R/V, K20M/N/R, L24I, L33F, M36I, I47V, G48V, I54L/T/V, V82A/C/F/S/T, and I84V. • In combination with carbamazepine, phenobarbital, or phenytoin.

Contraindications

• Lopinavir and ritonavir tablets are contraindicated in patients with previously demonstrated clinically significant hypersensitivity (e.g., toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, urticaria, angioedema) to any of its ingredients, including ritonavir.

Warnings and precautions

The following have been observed in patients receiving lopinavir and ritonavir: • The concomitant use of lopinavir and ritonavir and certain other drugs may result in known or potentially significant drug interactions. Consult the full prescribing information prior to and during treatment for potential drug interactions. ( 5.1, 7.3 ) • Toxicity in preterm neonates: Lopinavir and ritonavir oral solution should not be used in preterm neonates in the immediate postnatal period because of possible toxicities.

Pregnancy

Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to lopinavir and ritonavir during pregnancy. Physicians are encouraged to register patients by calling the Antiretroviral Pregnancy Registry at 1-800-258-4263.

Storage and supply

Lopinavir and ritonavir film coated tablets USP are available in the following strengths and package sizes: Lopinavir and Ritonavir Tablets USP, 200 mg/50 mg Yellow film coated, ovaloid tablets debossed with ‘H’ on one side and ‘70’ on other side.

Source: Lopinavir And Ritonavir (Lopinavir And Ritonavir) — US FDA prescribing information, 2021-06-03, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.