Kaletra is a fixed-dose combination antiretroviral medication containing lopinavir and ritonavir, designed for the treatment of human immunodeficiency virus type 1 (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 indicated for use in combination with other antiretroviral agents as part of a comprehensive HIV management strategy. Kaletra is formulated to offer consistent pharmacokinetics and has been extensively studied in diverse patient populations, including treatment-naïve and treatment-experienced individuals.

Features

• Contains 200 mg lopinavir and 50 mg ritonavir per tablet
• Available as oral tablets and oral solution formulations
• Does not require refrigeration for tablet form
• Can be taken with or without food
• Co-formulated with ritonavir to enhance lopinavir bioavailability
• Manufactured under strict quality control standards

Benefits

• Provides potent suppression of HIV-1 replication, leading to undetectable viral loads
• Helps restore and preserve CD4+ T-cell counts, improving immune function
• Reduces the risk of HIV-related complications and disease progression
• Offers a well-established resistance profile with high barrier to resistance development
• Supports adherence through convenient twice-daily dosing in most cases
• Enables flexible administration regardless of meal timing

Common use

Kaletra is primarily used as part of combination antiretroviral therapy for the treatment of HIV-1 infection. It is prescribed for both treatment-naïve patients initiating therapy and treatment-experienced patients who may have developed resistance to other protease inhibitors. The medication is commonly used in scenarios where boosted protease inhibitor therapy is indicated, particularly when drug interactions or resistance patterns make other options less suitable. Clinical guidelines frequently recommend Kaletra-based regimens for patients with certain comorbidities or those requiring concomitant medications that are compatible with its metabolic profile.

Dosage and direction

Adult patients: The recommended dosage is 400 mg lopinavir/100 mg ritonavir (two tablets) twice daily. For treatment-naïve patients, once-daily dosing (800 mg lopinavir/200 mg ritonavir) may be considered. Pediatric patients: Dosage is based on body weight or body surface area, with specific calculations provided in prescribing information. Tablets should be swallowed whole and not chewed, broken, or crushed. The oral solution should be administered using the provided dosing syringe. Dosage adjustments are required for patients with hepatic impairment and those taking certain concomitant medications that affect CYP3A4 metabolism.

Precautions

Kaletra should be used with caution in patients with pre-existing liver disease, including hepatitis B or C co-infection, due to risk of hepatotoxicity. Monitor liver enzymes before and during treatment. Use cautiously in patients with cardiac conduction abnormalities or structural heart disease, as PR interval prolongation has been observed. Pancreatitis has been reported; monitor for symptoms particularly in patients with history of pancreatitis or elevated triglycerides. May cause redistribution/accumulation of body fat. Use with caution in patients with hemophilia due to potential increased bleeding risk. Contains alcohol; oral solution should be used cautiously in patients with alcohol dependence.

Contraindications

Kaletra is contraindicated in patients with known hypersensitivity to lopinavir, ritonavir, or any component of the formulation. Concomitant use with drugs highly dependent on CYP3A4 for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events is contraindicated. These include alfuzosin, amiodarone, dihydroergotamine, ergotamine, methylergonovine, cisapride, lovastatin, simvastatin, pimozide, sildenafil (for pulmonary arterial hypertension), triazolam, oral midazolam, and ranolazine. Contraindicated with lurasidone and voriconazole.

Possible side effect

Common: Diarrhea, nausea, vomiting, abdominal pain, headache, insomnia, rash, asthenia. Metabolic: Hypercholesterolemia, hypertriglyceridemia, insulin resistance, hyperglycemia. Gastrointestinal: Pancreatitis, increased amylase. Hepatic: Elevated transaminases, hepatitis. Cardiac: PR interval prolongation. Dermatological: Severe skin reactions including Stevens-Johnson syndrome. Other: Lipodystrophy, immune reconstitution syndrome, increased bleeding in hemophiliacs.

Drug interaction

Kaletra is a potent inhibitor of CYP3A4 and CYP2D6 and may increase concentrations of drugs metabolized by these enzymes. Significant interactions occur with: Antiarrythmics (amiodarone, flecainide, propafenone), Anticoagulants (warfarin), Anticonvulsants (carbamazepine, phenobarbital, phenytoin), Antifungals (voriconazole), Ergot derivatives, GI motility agents (cisapride), Neuroleptics (pimozide), Sedatives/hypnotics (midazolam, triazolam), Statins (lovastatin, simvastatin), PDE5 inhibitors, and Immunosuppressants. Also interacts with other antiretrovirals including NNRTIs and other PIs.

Missed dose

If a dose is missed within 6 hours of the scheduled time, the patient should take the missed dose immediately and then resume the regular dosing schedule. If more than 6 hours have passed, the patient should skip the missed dose and resume the regular dosing schedule. Do not double the next dose to make up for a missed dose. Consistent adherence is critical to maintain viral suppression and prevent development of resistance.

Overdose

There is limited experience with Kaletra overdose. Maximum reported daily dose was 24 tablets (4800/1200 mg lopinavir/ritonavir) with no serious adverse events. However, overdose may increase the frequency and severity of adverse effects including gastrointestinal symptoms, electrolyte imbalances, and hepatotoxicity. Treatment should be supportive and symptomatic, including monitoring of vital signs and ECG. Since Kaletra is highly protein-bound, dialysis is unlikely to be beneficial. Contact poison control center for latest guidance.

Storage

Tablets: Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F). Keep in original container to protect from moisture. Oral solution: Store refrigerated at 2°C to 8°C (36°F to 46°F). May be stored at room temperature (up to 25°C/77°F) for up to 2 months. Avoid exposure to excessive heat. Keep out of reach of children. Do not use after expiration date printed on packaging.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Kaletra is a prescription medication that should only be used under the supervision of a qualified healthcare provider. Treatment decisions should be based on individual patient characteristics, viral resistance testing, and current treatment guidelines. The prescribing physician should be consulted for complete information regarding indications, dosage, administration, and monitoring requirements. Adverse event reporting should be directed to the appropriate regulatory authorities.

Reviews

Clinical trials and real-world experience demonstrate Kaletra’s efficacy in achieving and maintaining viral suppression. In study M98-863, 75% of treatment-naïve patients receiving Kaletra-based regimen achieved HIV RNA <400 copies/mL at 48 weeks compared to 62% in comparator group. Long-term data show sustained virological response in many patients for over 5 years. Physicians note its reliability in treatment-experienced patients with some PI resistance. Some clinicians report gastrointestinal side effects as a challenge to adherence in certain patients. The fixed-dose combination and pharmacokinetic profile are frequently cited advantages over earlier protease inhibitors.