Kaletra is a fixed-dose combination antiretroviral medication containing lopinavir and ritonavir, designed for the treatment of human immunodeficiency virus (HIV-1) infection in adults and pediatric patients. As a protease inhibitor boosted by ritonavir, it plays a critical role in suppressing viral replication, improving immunological function, and delaying disease progression. It is typically used in combination with other antiretroviral agents as part of a highly active antiretroviral therapy (HAART) regimen, adhering to current clinical guidelines for HIV management.

Features

• Contains 200 mg lopinavir and 50 mg ritonavir per tablet
• Available in tablet and oral solution formulations
• Co-formulated for enhanced pharmacokinetics via CYP3A4 inhibition
• Does not require refrigeration for tablets (oral solution must be refrigerated)
• FDA-approved for treatment-naïve and treatment-experienced patients

Benefits

• Achieves and maintains viral suppression below detectable limits
• Improves CD4+ T-cell counts and immune reconstitution
• Reduces the risk of HIV-related complications and opportunistic infections
• Offers a high genetic barrier to resistance compared to some other antiretroviral classes
• Provides flexible dosing options suitable for diverse patient populations
• Supported by extensive clinical trial data demonstrating long-term efficacy and safety

Common use

Kaletra is indicated for the treatment of HIV-1 infection in combination with other antiretroviral agents. It is used in both treatment-naïve and treatment-experienced patients, including those who have developed resistance to other protease inhibitors. It is also utilized in certain scenarios for post-exposure prophylaxis (PEP) and is sometimes considered for off-label use in managing other viral infections under specialist supervision.

Dosage and direction

The recommended adult dosage is 400 mg lopinavir/100 mg ritonavir (two tablets) twice daily taken with or without food. For treatment-naïve adults, an alternative once-daily dosing of 800 mg lopinavir/200 mg ritonavir (four tablets) may be considered. Pediatric dosing is based on body weight or body surface area and must be calculated precisely. Tablets should be swallowed whole and not chewed, crushed, or split. The oral solution should be administered using the provided dosing syringe.

Precautions

• Monitor liver function tests at baseline and during treatment; use with caution in patients with hepatic impairment, including hepatitis B or C coinfection
• May cause PR interval prolongation—use cautiously in patients with pre-existing cardiac conduction abnormalities
• Pancreatitis has been reported; monitor for symptoms such as nausea, vomiting, and abdominal pain
• May increase cholesterol and triglycerides; lipid levels should be checked before and during therapy
• Use with caution in patients with hemophilia due to increased risk of bleeding

Contraindications

• Hypersensitivity to lopinavir, ritonavir, or any component of the formulation
• Coadministration with drugs highly dependent on CYP3A4 for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events (e.g., alfuzosin, amiodarone, ergot derivatives, lovastatin, simvastatin, sildenafil for pulmonary hypertension, triazolam, oral midazolam)
• Severe hepatic impairment

Possible side effect

Common side effects include diarrhea, nausea, vomiting, abdominal pain, headache, and asthenia. Less frequently, rash, insomnia, and lipid abnormalities may occur. Serious adverse reactions include pancreatitis, hepatotoxicity, cardiac conduction abnormalities, and redistribution/accumulation of body fat. Patients should report any persistent or severe symptoms to their healthcare provider.

Drug interaction

Kaletra is a potent inhibitor of CYP3A4 and CYP2D6 and may increase concentrations of drugs metabolized by these enzymes. It also induces CYP1A2, CYP2C9, CYP2C19, and glucuronosyltransferases. Significant interactions occur with:

• Anticonvulsants (e.g., carbamazepine, phenobarbital, phenytoin)
• Antimycobacterials (e.g., rifampin)
• Sedative/hypnotics (e.g., midazolam, triazolam)
• Ergot derivatives
• GI motility agents (e.g., cisapride)
• HMG-CoA reductase inhibitors (e.g., simvastatin, lovastatin)
• PDE5 inhibitors (e.g., sildenafil for pulmonary hypertension)

A comprehensive medication review is essential prior to initiation.

Missed dose

If a dose is missed within 6 hours of the scheduled time, the patient should take it as soon as possible and resume the normal dosing schedule. If more than 6 hours have passed, the missed dose should be skipped and the next dose taken at the regular time. Patients should not double the dose.

Overdose

There is no specific antidote for Kaletra overdose. Treatment should consist of general supportive measures, including monitoring of vital signs and observation of clinical status. Hemodialysis is unlikely to be beneficial due to high protein binding. If overdose is suspected, contact a poison control center or healthcare provider immediately.

Storage

Store tablets at room temperature (20–25°C or 68–77°F); excursions permitted between 15–30°C (59–86°F). Keep in the original container and protect from moisture. The oral solution must be refrigerated (2–8°C or 36–46°F) and used within 60 days if kept at room temperature. Do not freeze. Keep out of reach of children and pets.

Disclaimer

This information is intended for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider for personalized recommendations. Dosage, administration, and suitability must be evaluated by a physician familiar with the patient’s clinical history.

Reviews

Kaletra has been extensively studied in clinical trials and is regarded as a cornerstone of antiretroviral therapy by many infectious disease specialists. It is praised for its durability and high barrier to resistance, though some clinicians note gastrointestinal side effects and drug interaction challenges. Long-term real-world evidence supports its role in maintaining virologic suppression and improving quality of life for people living with HIV.