Kaletra: Advanced Protease Inhibitor for Effective HIV Management
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Synonyms | |||
Kaletra is a fixed-dose combination antiretroviral medication containing lopinavir and ritonavir, designed to suppress HIV replication and support long-term viral load control. As a cornerstone of modern highly active antiretroviral therapy (HAART) regimens, this protease inhibitor formulation demonstrates robust efficacy against HIV-1 through its unique pharmacokinetic enhancement mechanism. Clinically proven to maintain undetectable viral loads and improve CD4 cell counts, Kaletra represents a critical therapeutic option for both treatment-naïve and treatment-experienced patients. Its co-formulation ensures optimized bioavailability and consistent dosing convenience, supporting adherence to complex antiretroviral regimens.
Features
- Contains 200 mg lopinavir and 50 mg ritonavir per tablet
- Available as film-coated tablets and oral solution formulations
- Utilizes pharmacokinetic boosting via ritonavir-mediated CYP3A4 inhibition
- Manufactured under strict quality control standards compliant with FDA and EMA regulations
- Stable at room temperature (20-25°C) with protection from moisture
- Demonstrated high genetic barrier to resistance compared to earlier protease inhibitors
Benefits
- Achieves and maintains viral suppression below detectable limits (<50 copies/mL)
- Provides durable treatment response with reduced risk of virological failure
- Supports immune reconstitution through consistent CD4+ T-cell count improvements
- Offers flexible dosing options suitable for diverse patient populations
- Minimizes pill burden through fixed-dose combination technology
- Demonstrates efficacy against some nucleoside-resistant HIV strains
Common use
Kaletra is primarily indicated for the treatment of HIV-1 infection in combination with other antiretroviral agents in adults and pediatric patients (14 days and older). It is commonly prescribed as part of initial therapy regimens and for treatment-experienced patients who require regimen optimization. The medication may also be utilized in post-exposure prophylaxis protocols following potential HIV exposure, though this represents an off-label application requiring careful risk-benefit assessment. Clinical guidelines frequently recommend Kaletra for patients with specific resistance patterns or those requiring a boosted protease inhibitor approach.
Dosage and direction
Adult patients: The standard recommended dosage is 400 mg lopinavir/100 mg ritonavir (2 tablets) twice daily with food. For treatment-naïve patients, an alternative regimen of 800 mg lopinavir/200 mg ritonavir (4 tablets) once daily may be considered, though twice-daily dosing maintains more consistent plasma concentrations.
Pediatric patients: Dosage is based on body weight or body surface area:
- 15-25 kg: 200 mg lopinavir/50 mg ritonavir twice daily
- 25-35 kg: 300 mg lopinavir/75 mg ritonavir twice daily
35 kg: Adult dosage
Tablets should be swallowed whole with a meal or snack to enhance absorption. The oral solution requires precise measurement using the provided dosing syringe and must be administered with food to improve tolerability and bioavailability.
Precautions
Hepatic impairment requires careful dosage consideration and monitoring of liver function tests. Patients with hepatitis B or C coinfection may experience accelerated hepatic deterioration and require enhanced monitoring. Pancreatitis has been reported, particularly in patients with advanced HIV disease or history of pancreatitis—monitor for symptoms including nausea, vomiting, and abdominal pain. Patients may experience lipid abnormalities including elevated cholesterol and triglycerides, requiring baseline and periodic monitoring. Electrocardiogram monitoring is recommended in patients with underlying cardiac structural abnormalities or those taking other QT-prolonging medications.
Contraindications
Kaletra is contraindicated in patients with known hypersensitivity to lopinavir, ritonavir, or any component of the formulation. Coadministration with drugs highly dependent on CYP3A4 for clearance that produce elevated plasma concentrations associated with serious or life-threatening events is absolutely contraindicated. Specific prohibited medications include alfuzosin, silodosin, lovastatin, simvastatin, lurasidone, pimozide, triazolam, oral midazolam, ergot derivatives, sildenafil for pulmonary arterial hypertension, and ranolazine. Concomitant use with St. John’s wort is contraindicated due to reduced lopinavir concentrations and potential loss of virological response.
Possible side effect
Common (≥10%): Diarrhea, nausea, vomiting, abdominal pain, headache, asthenia Less common (1-10%): Rash, insomnia, elevated cholesterol/triglycerides, increased liver enzymes Rare (<1%): Pancreatitis, diabetes mellitus/hyperglycemia, fat redistribution, immune reconstitution syndrome, PR interval prolongation Laboratory abnormalities: Elevated AST/ALT, elevated total cholesterol, elevated triglycerides, hyperglycemia, elevated creatinine kinase
Most adverse reactions are mild to moderate in severity and often diminish with continued therapy. Gastrointestinal symptoms may be managed with temporary dose reduction or antiemetic therapy under medical supervision.
Drug interaction
Kaletra demonstrates extensive drug interaction potential due to potent CYP3A4 inhibition and moderate CYP2D6 inhibition. Significant interactions occur with:
- Anticonvulsants: Carbamazepine, phenobarbital, phenytoin (reduce lopinavir concentrations)
- Antimycobacterials: Rifampin (contraindicated), rifabutin (requires 75% dose reduction)
- Sedative/hypnotics: Benzodiazepines (increased sedation risk)
- Ergot derivatives: Contraindicated due to ergotism risk
- GI motility agents: Cisapride (contraindicated)
- HCV protease inhibitors: Requires careful dose adjustment and monitoring
- HMG-CoA reductase inhibitors: Lovastatin and simvastatin contraindicated
- Phosphodiesterase-5 inhibitors: Requires dose reduction and extended dosing interval
Comprehensive medication review is essential before initiation and during therapy.
Missed dose
If a dose is missed within 6 hours of the scheduled time, the patient should take the missed dose immediately with food and resume the regular dosing schedule. If more than 6 hours have passed, the patient should skip the missed dose and take the next dose at the regularly scheduled time. Patients should not double the next dose to make up for a missed dose. Consistent adherence is critical to maintain therapeutic drug levels and prevent resistance development.
Overdose
Limited data exists regarding Kaletra overdose. Maximum reported single dose includes 24 tablets (4800 mg lopinavir/1200 mg ritonavir) with associated nausea, vomiting, and diarrhea. Management should include supportive measures with attention to electrolyte balance and hydration. Activated charcoal may be administered if presented within one hour of ingestion. Lopinavir is highly protein-bound and unlikely to be significantly removed by dialysis. Contact poison control center for latest management recommendations.
Storage
Store tablets at room temperature (20-25°C) in the original container with desiccant included. Protect from excessive moisture and light. The oral solution should be stored refrigerated (2-8°C) until opened, after which it may be kept at room temperature (below 25°C) for up to 2 months. Do not freeze. Keep all medications out of reach of children and pets. Properly dispose of expired or unused medication through medication take-back programs.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient characteristics and current treatment guidelines. The prescribing physician should be consulted for complete prescribing information, including boxed warnings and medication guide. Patients should not alter their treatment regimen without medical supervision.
Reviews
Clinical trials demonstrate Kaletra’s efficacy in maintaining virological suppression, with 70-80% of treatment-naïve patients achieving viral loads <50 copies/mL at 48 weeks. The MONARK study showed 76% of patients receiving lopinavir/ritonavir monotherapy maintained viral suppression at 48 weeks. Real-world evidence supports sustained effectiveness in diverse patient populations, though gastrointestinal side effects remain a consideration. The medication continues to play a valuable role in global HIV treatment programs, particularly in resource-limited settings where once-daily dosing and heat stability provide practical advantages.