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Author: Admin | 2025-04-28
AVblock, third-degree AV block, QTc interval prolongation, torsades (torsade) depointes [see WARNINGS AND PRECAUTIONS].Skin And AppendagesToxic epidermal necrolysis (TEN), Stevens-Johnsonsyndrome and erythema multiforme. Drug Interactions for Kaletra TabletsPotential For KALETRA To Affect Other DrugsLopinavir/ritonavir is an inhibitor of CYP3A and mayincrease plasma concentrations of agents that are primarily metabolized byCYP3A. Agents that are extensively metabolized by CYP3A and have high firstpass metabolism appear to be the most susceptible to large increases in AUC(> 3-fold) when co-administered with KALETRA. Thus, co-administration ofKALETRA with drugs highly dependent on CYP3A for clearance and for whichelevated plasma concentrations are associated with serious and/orlife-threatening events is contraindicated. Co-administration with other CYP3Asubstrates may require a dose adjustment or additional monitoring as shown inTable 12.Additionally, KALETRA induces glucuronidation.Published data suggest that lopinavir is an inhibitor ofOATP1B1.Potential For Other Drugs To Affect LopinavirLopinavir/ritonavir is a CYP3A substrate; therefore,drugs that induce CYP3A may decrease lopinavir plasma concentrations and reduceKALETRA's therapeutic effect. Although not observed in the KALETRA/ketoconazoledrug interaction study, co-administration of KALETRA and other drugs thatinhibit CYP3A may increase lopinavir plasma concentrations.Established And Other Potentially Significant Drug InteractionsTable 12 provides a listing of established or potentiallyclinically significant drug interactions. Alteration in dose or regimen may berecommended based on drug interaction studies or predicted interaction [see CONTRAINDICATIONS,WARNINGS AND PRECAUTIONS, CLINICALPHARMACOLOGY] for magnitude of interaction.Table 12: Established and Other PotentiallySignificant Drug Interactions Concomitant Drug Class: Drug Name Effect on Concentration of Lopinavir or Concomitant Drug Clinical Comments HIV-1 Antiviral Agents HIV-1 Protease Inhibitor: fosamprenavir/ritonavir ↓ amprenavir ↓ lopinavir An increased rate of adverse reactions has been observed with co-administration of these medications. Appropriate doses of the combinations with respect to safety and efficacy have not been established. HIV-1 Protease Inhibitor: indinavir* ↑ indinavir Decrease indinavir dose to 600 mg twice daily, when co-administered with KALETRA 400/100 mg twice daily. KALETRA once daily has not been studied in combination with indinavir. HIV-1 Protease Inhibitor: nelfinavir* ↑ nelfinavir ↑ M8 metabolite of nelfinavir ↓ lopinavir KALETRA once daily in combination with nelfinavir is not recommended [see DOSAGE AND ADMINISTRATION]. HIV-1 Protease Inhibitor: ritonavir* ↑ lopinavir Appropriate doses of additional ritonavir in combination with KALETRA with respect to safety and efficacy have not been established. HIV-1 Protease Inhibitor: saquinavir ↑ saquinavir The saquinavir dose is 1000 mg twice daily, when co-administered with KALETRA 400/100 mg twice daily. KALETRA once daily has not been studied in combination with saquinavir. HIV-1 Protease Inhibitor: tipranavir* ↓ lopinavir Co-administration with tipranavir (500 mg twice daily) and ritonavir (200 mg twice daily) is not recommended. HIV CCR5 - Antagonist: maraviroc* ↑ maraviroc When co-administered, patients should receive 150 mg twice daily of maraviroc. For further details see complete prescribing information for maraviroc. Non-nucleoside Reverse Transcriptase Inhibitors: efavirenz*, nevirapine* ↓
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