Lopinavir

Lopinavir and ritonavir tablets are a fixed-dose combination of HIV-1 antiviral drugs lopinavir [see Microbiology ( 12.4 )] and ritonavir. As co-formulated in lopinavir and ritonavir tablets, ritonavir inhibits the CYP3A-mediated metabolism of lopinavir, thereby providing increased plasma levels of lopinavir.

• Lopinavir and ritonavir is indicated in combination with other antiretroviral agents for the treatment of HIV1 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.

• Lopinavir and ritonavir is 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. Lopinavir and ritonavir is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or lifethreatening reactions [see Drug Interactions ( 7.1 ) and Clinical Pharmacology ( 12.3 )].contraindicated

Tablets: May be taken with or without food, swallowed whole and not chewed, broken, or crushed. ( 2.1 ) Adults ( 2.3 ): Total recommended daily dosage is 800/200 mg given once or twice daily. Lopinavir and ritonavir can be given as once daily or twice daily regimen. See Full Prescribing Information for details. Lopinavir and ritonavir 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. ( 12.4 ) In combination with carbamazepine, phenobarbital, or phenytoin. ( 7.3 ) In combination with efavirenz, nevirapine, or nelfinavir. ( 12.3 ) In pregnant women. ( 2.5 , 8.1 , 12.3 ) Pediatric Patients (14 days and older) ( 2.4 ): Lopinavir and ritonavir once daily dosing regimen is not recommended in pediatric patients. Twice daily dose is based on body weight or body surface area. Concomitant Therapy in Adults and Pediatric Patients: Dose adjustments of lopinavir and ritonavir may be needed when co-administering with efavirenz, nevirapine, or nelfinavir. ( 2.3 , 2.4 , 7.3 ) Pregnancy ( 2.5 ): 400/100 mg twice daily in pregnant patients with no documented lopinavir-associated resistance substitutions. There are insufficient data to recommend a lopinavir and ritonavir dose for pregnant patients with any documented lopinavir and ritonavir -associated resistance substitutions. No dose adjustment of lopinavir and ritonavir is required for patients during the postpartum period.

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. A safe and effective dose of lopinavir and ritonaviroral solution in this patient population has not been established. ( 2.4 , 5.2) Pancreatitis: Fatalities have occurred; suspend therapy as clinically appropriate. ( 5.3 ) Hepatotoxicity: Fatalities have occurred. Monitor liver function before and during therapy, especially in patients with underlying hepatic disease, including hepatitis B and hepatitis C, or marked transaminase elevations. ( 5.4 , 8.6 ) QT interval prolongation and isolated cases of torsade de pointes have been reported although causality could not be established. Avoid use in patients with congenital long QT syndrome, those with hypokalemia, and with other drugs that prolong the QT interval. ( 5.1 , 5.5 , 12.3 ) PR interval prolongation may occur in some patients. Cases of second and third degree heart block have been reported. Use with caution in patients with pre-existing conduction system disease, ischemic heart disease, cardiomyopathy, underlying structural heart disease or when administering with other drugs that may prolong the PR interval.

The following adverse reactions are discussed in greater detail in other sections of the labeling. QT Interval Prolongation, PR Interval Prolongation [see Warnings and Precautions ( 5.5 , 5.6 )] Drug Interactions [see Warnings and Precautions ( 5.1 )] Pancreatitis [see Warnings and Precautions ( 5.3 )] Hepatotoxicity [see Warnings and Precautions ( 5.4 )] Commonly reported adverse reactions to lopinavir and ritonavir included diarrhea, nausea, vomiting, hypertriglyceridemia and hypercholesterolemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Macleods Pharma USA, Inc. at 1-888-943-3210 1-855-926-3384 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reactions rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Adverse Reactions in Adults The safety of lopinavir and ritonavir has been investigated in about 2,600 patients in Phase II-IV clinical trials, of which about 700 have received a dose of 800/200 mg (6 capsules or 4 tablets) once daily. Along with nucleoside reverse transcriptase inhibitors (NRTIs), in some studies, lopinavir and ritonavir was used in combination with efavirenz or nevirapine. In clinical studies the incidence of diarrhea in patients treated with either lopinavir and ritonavir capsules or tablets was greater in those patients treated once daily than in those patients treated twice daily.

Lactation: Breastfeeding not recommended. ( 8.2 ) 8.1 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. Risk Summary Available data from the Antiretroviral Pregnancy Registry show no difference in the risk of overall major birth defects compared to the background rate for major birth defects of 2.7% in the U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) (see Data). The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15-20%. The background risk for major birth defects and miscarriage for the indicated population is unknown. Methodological limitations of the APR include the use of MACDP as the external comparator group. The MACDP population is not disease-specific, evaluates women and infants from a limited geographic area, and does not include outcomes for births that occurred at <20 weeks gestation (see Data).

Metabolism

The pharmacokinetic properties of lopinavir are summarized in Table 13. The steady-state pharmacokinetic parameters of lopinavir are summarized in Table 14.

Overdoses with lopinavir and ritonavir oral solution have been reported. One of these reports described fatal cardiogenic shock in a 2.1 kg infant who received a single dose of 6.5 mL of lopinavir and ritonavir oral solution (520 mg lopinavir, approximately 10-fold above the recommended lopinavir dose) nine days prior. The following events have been reported in association with unintended overdoses in preterm neonates: complete AV block, cardiomyopathy, lactic acidosis, and acute renal failure [ see Warnings and Precautions ( 5.2 )]. Healthcare professionals should be aware that lopinavir and ritonavir oral solution is highly concentrated and therefore, should pay special attention to accurate calculation of the dose of lopinavir and ritonavir, transcription of the medication order, dispensing information and dosing instructions to minimize the risk for medication errors and overdose. This is especially important for infants and young children. Lopinavir and ritonavir oral solution contains approximately 42% (v/v) ethanol and approximately 15% (w/v) propylene glycol.

• Sep 15, 2000NDANDA021251Abbvie
• Oct 28, 2005NDANDA021906Abbvie
• Jun 4, 2021ANDAANDA091677Hetero Labs Ltd Iii
• Mar 21, 2022ANDAANDA213857Laurus
• Jul 25, 2024ANDAANDA204739Macleods Pharms Ltd

1. 1Drug Interaction1,3349.9%
2. 2Depression1,1338.4%
3. 3Nausea7815.8%
4. 4Drug Exposure During Pregnancy7775.8%
5. 5Diarrhoea7755.8%
6. 6Foetal Exposure During Pregnancy7505.6%
7. 7Anxiety7135.3%
8. 8Vomiting7015.2%
9. 9Pain6935.2%
10. 10Off Label Use6755.0%
11. 11Emotional Distress5784.3%
12. 12Renal Failure5414.0%
13. 13Pyrexia5263.9%
14. 14Anhedonia5103.8%
15. 15Anaemia4503.3%

Recent PubMed references pinned to Lopinavir as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• QT interval prolongation and its related factors before and after receiving lopinavir-ritonavir in the COVID-19 era: a historical cohort study.
  Virus research · 2026 · Jangjou A, Izadpanah P, Moqhadas M, et al.
  PMID 42067143DOI 10.1016/j.virusres.2026.199739
• Drug-drug interactions between lopinavir and felodipine in vitro and in vivo.
  Biochemical pharmacology · 2026 · Li W, Shen Y, Li Q, et al.
  PMID 42055143DOI 10.1016/j.bcp.2026.118012
• Lopinavir targets Leishmania topoisomerase I and its combination with Ritonavir exhibits enhanced antileishmanial efficacy in clinical isolates of Leishmania donovani.
  Acta tropica · 2026 · Mazire P, Roy A
  PMID 41946389DOI 10.1016/j.actatropica.2026.108082
• Effects of Ritonavir, Lopinavir, and Alcohol on ABC Transporters and Secretion of Bile Acid and Bilirubin in Senescent Hepatocytes.
  International journal of molecular sciences · 2026 · Chen L, Duran E, Headrick D, et al.
  PMID 41683625DOI 10.3390/ijms27031189
• Lopinavir Derivative as Potent P-gp Inhibitor Enables Delivery through HPMA Copolymer Conjugates and Overcoming Tumor Chemoresistance to Conventional Cytostatic Drugs.
  Biomacromolecules · 2026 · Starenko D, Kostka L, Behalova K, et al.
  PMID 41549969DOI 10.1021/acs.biomac.5c02097
• Tolerability of lopinavir versus dolutegravir in children and adolescents with HIV.
  AIDS (London, England) · 2026 · Blankenberger J, Devendra A, Bakaya M, et al.
  PMID 41467721DOI 10.1097/QAD.0000000000004432
• Lopinavir/ritonavir induces hepatotoxicity in HepG2 cells through inhibition of the Nrf2 pathway, resulting in oxidative stress, endoplasmic reticulum stress, and cell cycle arrest.
  Toxicology letters · 2026 · Zhou W, Dan Wang, Tu J, et al.
  PMID 41354389DOI 10.1016/j.toxlet.2025.111798
• Efficacy and safety of switching from lopinavir/ritonavir-based regimens to bictegravir/emtricitabine/tenofovir alafenamide in people living with HIV: A multicenter retrospective study.
  Virologica Sinica · 2025 · Fu J, Guo Y, Zheng G, et al.
  PMID 41115660DOI 10.1016/j.virs.2025.10.003

The 10 most recently updated of 429 ClinicalTrials.gov registrations naming Lopinavir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments
  Recruiting · Phase 4 · Interventional · 350 enrolled · Gilead Sciences
  NCT06337032updated 2026-06-10
• A Study of the Preliminary Efficacy of DARE-HPV to Treat High-risk Persistent Human Papillomavirus (hrHPV)
  Not yet recruiting · Phase 2 · Interventional · 118 enrolled · Daré Bioscience, Inc.
  NCT07601074updated 2026-06-02
• Very Early Intensive Treatment of Infants Living With HIV to Achieve HIV Remission
  Recruiting · Phase 1 · Phase 2 · Interventional · 1,120 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT02140255updated 2026-05-26
• Trial of Treatments for COVID-19 in Hospitalized Adults
  Completed · Phase 3 · Interventional · 1,552 enrolled · Institut National de la Santé Et de la Recherche Médicale, France
  NCT04315948updated 2026-05-20
• Lopinavir/Ritonavir in PLWH With High-Grade AIN
  Recruiting · Phase 1 · Interventional · 21 enrolled · University of Wisconsin, Madison
  NCT05334004updated 2026-05-15
• Study of Cobicistat-Boosted Atazanavir (ATV/co), Cobicistat-Boosted Darunavir (DRV/co) and Emtricitabine/Tenofovir Alafenamide (F/TAF) in Children With HIV
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 133 enrolled · Gilead Sciences
  NCT02016924updated 2026-04-21
• Randomised Evaluation of COVID-19 Therapy
  Recruiting · Phase 3 · Interventional · 70,000 enrolled · University of Oxford
  NCT04381936updated 2026-04-21
• Antiretroviral Treatment Taken 4 Days Per Week Versus Continuous Therapy 7/7 Days Per Week in HIV-1 Infected Patients
  Completed · Phase 3 · Interventional · 640 enrolled · ANRS, Emerging Infectious Diseases
  NCT03256422updated 2026-04-13
• Kuwa Free! - Live Free!
  Recruiting · Interventional · 700 enrolled · University of Alabama at Birmingham
  NCT05044962updated 2026-04-13
• Intensification With Enfuvirtide in Naive HIV-infected Patients (ANRS130)
  Completed · Phase 3 · Interventional · 195 enrolled · French National Agency for Research on AIDS and Viral Hepatitis
  NCT00302822updated 2026-04-07

Frequently asked questions

How does Lopinavir work?

Lopinavir and ritonavir tablets are a fixed-dose combination of HIV-1 antiviral drugs lopinavir [see Microbiology ( 12.4 )] and ritonavir. As co-formulated in lopinavir and ritonavir tablets, ritonavir inhibits the CYP3A-mediated metabolism of lopinavir, thereby providing increased plasma levels of lopinavir.

What is Lopinavir used for?

According to FDA labeling, Lopinavir carries indications including: Lopinavir and ritonavir is indicated in combination with other antiretroviral agents for the treatment of HIV1 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Lopinavir?

Lopinavir is classified as Protease Inhibitor, Cytochrome P450 3A Inducers, Cytochrome P450 3A Inhibitors, HIV Protease Inhibitors, Organic Anion Transporting Polypeptide 1B1 Inhibitors, P-Glycoprotein Inhibitors, Decreased Protein Synthesis, Increased Immunologically Active Molecule Activity.

What are the brand names for Lopinavir?

Lopinavir is marketed under brand names including Kaletra.

What are the contraindications for Lopinavir?

Lopinavir labeling lists contraindications including: Lopinavir and ritonavir is 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. Lopinavir and ritonavir is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or lifethreatening reactions [see Drug Interactions ( 7.1 ) and Clinical Pharmacology ( 12.3 )].. Always consult the full prescribing information and a clinician.