Fixed-Dose Combination: This oral liquid contains a fixed-dose combination of two active ingredients: Lopinavir (A), an HIV protease inhibitor, and Ritonavir (B), a pharmacokinetic boosting agent.
Concentration: The liquid has a concentration of 80 mg of Lopinavir and 20 mg of Ritonavir per milliliter, which is a standard pediatric strength.
Pharmacokinetic Booster: Ritonavir is included at a low dose not for its direct antiviral effect, but to inhibit the metabolism of Lopinavir, thereby increasing its concentration in the bloodstream.
Pediatric Formulation: This liquid is specifically designed for pediatric patients (indicated by “P”), especially infants and young children who cannot swallow tablets. It often contains a flavoring agent to improve palatability.
Advantages
Accurate Weight-Based Dosing: The liquid formulation is essential for achieving precise dose adjustments for infants and children, which is critical for therapeutic effectiveness and avoiding toxicity.
Improved Adherence: The liquid format is easier for infants and young children to take compared to tablets, which improves medication compliance and treatment outcomes.
Potent Antiviral Activity: The combination of Lopinavir and Ritonavir is a powerful regimen that provides strong and sustained viral suppression, effectively reducing the HIV viral load.
Flexibility in Dosing: The oral liquid allows for flexible dosing based on the child’s age and weight, which is crucial as they grow and their medication needs change.
Uses
Pediatric HIV-1 Infection: Indicated for the treatment of HIV-1 infection in pediatric patients, including infants as young as 14 days old, as part of combination antiretroviral therapy (cART).
Prevention of Mother-to-Child Transmission: This combination is a key component of regimens used to prevent the transmission of HIV from mother to child.
Post-Exposure Prophylaxis (PEP): It can be used as a component of PEP regimens to prevent HIV infection in children following a potential exposure.
Patients with Dysphagia: The liquid formulation is also a viable option for adult patients who have difficulty swallowing pills.
Nature
Drug Classes: Lopinavir is a protease inhibitor (PI) and Ritonavir is also a PI, but it is primarily used as a cytochrome P450 (CYP450) inhibitor.
Mechanism of Action (Lopinavir): Lopinavir works by selectively inhibiting the viral enzyme protease, which is essential for the cleavage of viral polyproteins into functional proteins. This results in the production of immature, non-infectious viral particles.
Mechanism of Action (Ritonavir): At a low dose, Ritonavir is a potent inhibitor of the CYP3A4 enzyme in the liver. By blocking this enzyme, it prevents the rapid metabolism of Lopinavir, leading to higher and more sustained therapeutic concentrations.
Side Effects: A key characteristic of the oral solution is its alcohol content, which should be considered when prescribing to young children. Common side effects include gastrointestinal issues like diarrhea, nausea, and vomiting.
Storage
Temperature: The oral liquid requires refrigeration both before and after dispensing to maintain its stability and effectiveness. It should be stored at a temperature between 2∘C to 8∘C (36∘F to 46∘F).
Protection: The bottle should be kept tightly capped and protected from light.
Administration: The bottle must be shaken well before each use. A calibrated oral syringe or measuring device should always be used for accurate dosing.
Expiration Date: The medication should not be used after the expiration date on the label. Any unused portion should be properly discarded.
