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, increasing CD4 cell counts, and reducing HIV-related morbidity and mortality. It is indicated for use in combination with other antiretroviral agents as part of a comprehensive HIV management strategy. Kaletra is formulated to offer high genetic barrier to resistance and is a cornerstone in both treatment-naïve and treatment-experienced patient regimens.

Features

• Contains lopinavir 200 mg and ritonavir 50 mg per tablet
• Available as film-coated tablets and oral solution
• Ritonavir acts as a pharmacokinetic enhancer (booster)
• Does not require refrigeration for tablets (oral solution must be refrigerated)
• Can be taken with or without food
• Manufactured under strict quality control standards

Benefits

• Effectively suppresses HIV-1 viral load to undetectable levels
• Helps restore and maintain immune function by increasing CD4+ T-cell counts
• Reduces the risk of HIV transmission to others when viral load is suppressed
• Offers a high barrier to resistance, supporting long-term treatment success
• Provides flexible dosing options suitable for diverse patient populations
• Contributes to improved quality of life and long-term survival for people living with HIV

Common use

Kaletra is used as part of combination antiretroviral therapy for the treatment of HIV-1 infection. It is prescribed for both treatment-naïve and treatment-experienced patients, including pediatric patients aged 14 days and older. The medication may be used in special populations such as pregnant individuals with HIV to prevent perinatal transmission. It is often included in second-line regimens when initial treatment fails or when resistance to other antiretroviral classes is detected.

Dosage and direction

Adults: The recommended dosage is 400 mg lopinavir/100 mg ritonavir (2 tablets) twice daily or 800 mg lopinavir/200 mg ritonavir (4 tablets) once daily in treatment-naïve adults. Once-daily dosing is not recommended for treatment-experienced adults or those with baseline resistance mutations.

Pediatric patients: Dosage is based on body weight or body surface area:

• 15-40 kg: 10 mg lopinavir/2.5 mg ritonavir per kg twice daily

• 40 kg: Adult dosage

• Maximum dose: 400 mg lopinavir/100 mg ritonavir twice daily

Tablets should be swallowed whole with water. The oral solution should be administered using the provided dosing syringe. If a dose is missed, it should be taken as soon as possible unless it is almost time for the next dose.

Precautions

• Monitor liver function tests regularly, particularly in patients with pre-existing liver disease
• Use with caution in patients with known cardiac conduction abnormalities or structural heart disease
• Pancreatitis has been reported; monitor for symptoms including nausea, vomiting, and abdominal pain
• May cause exacerbation of chronic hepatitis B or C co-infection
• May increase cholesterol and triglyceride levels; lipid monitoring recommended
• Use with caution in elderly patients due to increased likelihood of decreased hepatic, renal, or cardiac function
• Not recommended for patients with severe renal impairment

Contraindications

• Hypersensitivity to lopinavir, ritonavir, or any component of the formulation
• Coadministration with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events:
  • Alfuzosin
  • Dihydroergotamine, ergotamine, methylergonovine
  • Lovastatin, simvastatin
  • Midazolam, triazolam (oral)
  • Pimozide
  • Sildenafil (for pulmonary arterial hypertension)
  • St. John’s wort

Possible side effect

Common (≥1%):

• Diarrhea
• Nausea
• Vomiting
• Abdominal pain
• Headache
• Rash
• Asthenia

Less common:

• Increased cholesterol and triglycerides
• Pancreatitis
• Hepatotoxicity
• Insulin resistance
• Fat redistribution
• PR interval prolongation

Rare but serious:

• Severe skin reactions
• Hepatitis
• Cardiac conduction abnormalities
• New onset or exacerbation of diabetes mellitus

Drug interaction

Kaletra is a potent inhibitor of CYP3A4 and CYP2D6 and may increase plasma concentrations of drugs metabolized by these enzymes. Significant interactions include:

• Anticonvulsants: Carbamazepine, phenobarbital, phenytoin may decrease lopinavir concentrations
• Antimycobacterials: Rifampin is contraindicated; rifabutin dose reduction required
• Sedatives/hypnotics: Contraindicated with midazolam, triazolam
• Ergot derivatives: Contraindicated
• GI motility agents: Cisapride contraindicated
• Neuroleptics: Pimozide contraindicated
• HMG-CoA reductase inhibitors: Lovastatin, simvastatin contraindicated; use atorvastatin, rosuvastatin with caution
• Phosphodiesterase-5 inhibitors: Dose adjustment required for sildenafil, tadalafil, vardenafil
• Oral contraceptives: Alternative contraception recommended

Missed dose

If a dose is missed within 6 hours of the scheduled time, take the missed dose immediately. If more than 6 hours have passed, skip the missed dose and resume the regular dosing schedule. Do not double the next dose to make up for a missed dose.

Overdose

There is limited experience with Kaletra overdose. Reported events include asymptomatic PR interval prolongation and transient ALT elevations. Treatment should consist of general supportive measures including monitoring of vital signs and ECG. Since lopinavir is highly protein-bound, dialysis is unlikely to be beneficial. If overdose occurs, contact a poison control center or healthcare provider immediately.

Storage

Tablets: Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F). Keep in original container and protect from moisture.

Oral solution: Store refrigerated at 2-8°C (36-46°F). Do not freeze. If stored at room temperature (up to 25°C/77°F), use within 2 months. Keep tightly closed.

Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is 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. Individual patient needs may vary, and treatment decisions should be made in consultation with a physician experienced in HIV management. The full prescribing information should be consulted before initiating therapy.

Reviews

“Kaletra has been a reliable component of our HIV treatment arsenal for years. Its high barrier to resistance makes it particularly valuable in treatment-experienced patients. While gastrointestinal side effects can be challenging initially, they often subside with continued use.” - Infectious Disease Specialist, 15 years experience

“As a clinician working in resource-limited settings, the stability of Kaletra tablets without refrigeration requirements has been crucial for patient adherence and program implementation. The once-daily dosing option has further improved treatment acceptance among our patients.” - HIV Program Director, Sub-Saharan Africa

“After developing resistance to my initial regimen, Kaletra in combination with other antiretrovirals successfully suppressed my viral load to undetectable levels within three months. The side effects were manageable with supportive care, and I’ve maintained viral suppression for over five years.” - Patient living with HIV, 42 years old