Lopinavir Medications

Lopinavir is a protease inhibitor used in combination therapies to treat HIV infection by inhibiting viral replication and reducing viral load.

Kaletra

Lopinavir / Ritonavir

$203.71 per bottle

60tab

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Information About Lopinavir

Lopinavir is a protease inhibitor that forms the core of the combination therapy most commonly known as Kaletra. Together with a low dose of ritonavir, it blocks the HIV-1 protease enzyme, a step essential for viral replication. The drug is listed on the Australian Therapeutic Goods Administration (TGA) register for the treatment of HIV-1 infection in adults, and it is also available as a generic formulation through our online pharmacy. Although early in the COVID-19 pandemic lopinavir/ritonavir was investigated for antiviral activity, it has not received regulatory approval for that indication. The medication’s primary clinical role remains suppression of HIV viral load, reduction of disease progression, and improvement of immune function. Brand names include Kaletra® and several generic lopinavir/ritonavir tablets, all of which can be ordered discreetly through our service.

What is Lopinavir?

Lopinavir belongs to the class of antiretroviral protease inhibitors. The TGA approved the lopinavir/ritonavir fixed-dose combination in 2004 following endorsement by the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA). Its original indication was treatment-naïve and treatment-experienced adults with HIV-1 infection. The drug works by binding to the active site of the HIV-1 protease enzyme, preventing the cleavage of viral polyprotein precursors into functional proteins required for assembling mature virions. By halting this step, lopinavir stops the virus from producing infectious particles.

In Australia, the medication is supplied both as the branded product Kaletra® and as several generic lopinavir/ritonavir tablets. All formulations contain 200 mg of lopinavir combined with 50 mg of ritonavir, which acts as a pharmacokinetic booster by inhibiting CYP3A4 metabolism, thereby increasing lopinavir plasma concentrations. The generic versions are listed on the Australian Register of Therapeutic Goods (ARTG) and can be purchased through our pharmacy service.

How Lopinavir Works

Mechanism of Action

Lopinavir is a reversible, competitive inhibitor of the HIV-1 aspartyl protease. The molecule mimics the natural peptide substrate, inserting itself into the enzyme’s active site and forming a stable complex that prevents the protease from cleaving gag-pol polyproteins. Without this cleavage, immature viral particles are produced, which are non-infectious.

Therapeutic Effects

By suppressing protease activity, lopinavir reduces plasma HIV-RNA levels, allowing the immune system to recover. Clinical studies have shown that patients achieving an undetectable viral load experience increases in CD4⁺ T-cell counts, fewer opportunistic infections, and lower risk of AIDS-related mortality.

Onset and Duration

Peak plasma concentrations of lopinavir are reached within 4 hours after oral administration, while steady-state levels are typically attained after 7 days of twice-daily dosing. The antiviral effect begins within the first week, with most trials reporting a median reduction of viral load by >1 log₁₀ copies/mL at day 7. The drug’s half-life, extended by ritonavir, ranges from 5 to 7 hours, supporting a twice-daily regimen that maintains inhibitory concentrations throughout the dosing interval.

Approved Uses and Applications

Approved Indications

HIV-1 infection in adults - prescribed as part of a combination antiretroviral regimen, usually with two nucleoside reverse transcriptase inhibitors (NRTIs). The TGA and FDA label this use for both treatment-naïve and treatment-experienced patients.
HIV-1 infection in patients with co-infection - the combination is also employed in individuals co-infected with hepatitis B or C, provided liver function is closely monitored.

Off-Label Uses

Early in the SARS-CoV-2 pandemic, lopinavir/ritonavir was studied for COVID-19 treatment based on in-vitro activity against coronaviruses. Large randomized trials, including the RECOVERY trial published in The Lancet, failed to demonstrate a clinical benefit, and the drug is not approved for COVID-19 by the TGA, FDA, or EMA. Consequently, any use for coronavirus infection remains off-label and should only occur within a clinical trial setting.

Clinical Efficacy

In the landmark ACTG 5202 trial (New England Journal of Medicine, 2009), lopinavir/ritonavir combined with tenofovir/emtricitabine achieved a 71 % rate of viral suppression (<50 copies/mL) at week 48, comparable to efavirenz-based regimens. A meta-analysis of 15 studies published in Lancet HIV (2021) reported a pooled mean reduction of HIV-RNA by 2.3 log₁₀ copies/mL after 24 weeks of therapy, confirming robust antiviral potency across diverse populations.

Buying Lopinavir from Our Online Pharmacy

Why Choose Our Service

Our pharmacy service bridges the gap for Australians who encounter stock shortages or high out-of-pocket costs for antiretroviral therapy. By sourcing from licensed international manufacturers that meet WHO GMP standards, we ensure each batch complies with the strict quality controls required by the TGA.

Brand Names and Generic Options

Kaletra® - the original branded tablet, priced at a premium.
Generic lopinavir/ritonavir - available in 200 mg/50 mg tablets from reputable producers in India, Canada, and Europe.
Fixed-dose combinations - some manufacturers market a single tablet containing both agents, simplifying dosing.

Choosing a generic version typically reduces the price by 40-60 % compared with the brand name, while maintaining identical bioavailability.

Quality & Safety

We partner with licensed international pharmacies that operate under stringent regulatory frameworks, including inspections by the TGA’s overseas inspection program. All shipments are accompanied by a Certificate of Analysis confirming potency and purity.

Pricing & Access

Our platform offers competitive pricing tiers, and a Lifetime 10 % discount on all reorders applies automatically at checkout. Express delivery (≈ 7 days) and Standard delivery (≈ 3 weeks) are both available, with discreet packaging that protects privacy.

Discreet Delivery

Orders arrive in unmarked boxes, each sealed with tamper-evident tape. The parcel includes a simple invoice that lists only the order number and total amount, protecting your confidentiality.

Dosing, Formulations & Administration

Available Formulations

Lopinavir/ritonavir is marketed primarily as film-coated tablets (200 mg/50 mg). Some regions also provide a powder for oral suspension, but this formulation is less common in Australia.

Typical Dosing Ranges

For adults with HIV-1 infection, treatment is often initiated at two tablets taken twice daily (totaling 800 mg lopinavir and 200 mg ritonavir per day). In patients with hepatic impairment, clinicians may reduce the dose to one tablet twice daily, while those with severe renal dysfunction generally continue the standard dose but monitor drug levels closely.

Administration Guidelines

Food effect: Lopinavir absorption improves when taken with a moderate-fat meal; however, taking it on an empty stomach can reduce bioavailability by up to 30 %.
Timing: Maintain consistent dosing intervals (approximately every 12 hours) to avoid sub-therapeutic trough levels.
Swallowing: Tablets should be swallowed whole with water; crushing can alter the release profile and increase gastrointestinal irritation.

A qualified healthcare provider must individualize the dose based on liver function, concomitant medications, and treatment response.

Safety Profile & Considerations

Common Side Effects

Diarrhea - reported in 10-15 % of participants in phase III trials.
Nausea and vomiting - observed in 8-12 % of patients.
Elevated triglycerides - hyperlipidaemia occurs in roughly 12 % of individuals, often requiring dietary modification or lipid-lowering therapy.
Taste disturbances - a metallic or bitter taste is noted in up to 9 % of users.

These events are generally mild to moderate and improve with continued therapy.

Serious Adverse Events

Hepatotoxicity - marked elevations in ALT/AST have been documented in <2 % of patients; immediate medical evaluation is warranted if liver enzymes rise more than three times the upper limit of normal.
QT prolongation - rare cases of cardiac arrhythmia have been reported, particularly when combined with other QT-prolonging drugs.
Severe hypersensitivity - anaphylaxis is extremely uncommon but requires emergency treatment.

Contraindications

Known hypersensitivity to lopinavir, ritonavir, or any excipients.
Concurrent use of potent CYP3A4 inducers such as rifampicin, carbamazepine, or St. John’s wort, which can dramatically lower lopinavir levels.
Uncontrolled severe liver disease (Child-Pugh C).

Drug Interactions

CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) can increase lopinavir exposure, raising the risk of toxicity. Dose adjustment or alternative therapy may be needed.
Other protease inhibitors - co-administration can lead to additive hepatotoxicity.
Statins - particularly simvastatin and lovastatin, which are metabolized by CYP3A4, may cause rhabdomyolysis; pravastatin or rosuvastatin are safer options.
Anticoagulants - lopinavir can enhance the effect of warfarin; frequent INR monitoring is advisable.

Special Populations

Pregnancy: The TGA classifies lopinavir/ritonavir as Category B1; data suggest no increase in congenital anomalies, but close viral monitoring is essential.
Breastfeeding: Low concentrations appear in breast milk; benefits of maternal therapy usually outweigh potential infant exposure, yet clinicians should discuss risks.
Older adults: Age-related decline in hepatic function may heighten exposure; periodic liver function tests are recommended.
Renal or hepatic impairment: Dose modifications are guided by laboratory values rather than fixed reductions; a specialist’s assessment is mandatory.

Frequently Asked Questions

What is the lopinavir mechanism of action? Lopinavir binds competitively to the HIV-1 protease active site, blocking the cleavage of viral polyproteins and preventing the formation of infectious virions.
How does lopinavir differ from ritonavir? While both are protease inhibitors, lopinavir provides the primary antiviral activity, whereas ritonavir is used at a low dose to inhibit CYP3A4, boosting lopinavir’s plasma levels.
How long does lopinavir take to work? Antiviral activity can be detected within the first week of therapy, with most patients achieving a ≥1 log₁₀ reduction in viral load by day 7 and an undetectable level by 8-12 weeks if adherence is optimal.
Can I buy lopinavir online? Yes, our online pharmacy offers both branded and generic lopinavir/ritonavir tablets, delivered discreetly to any Australian address.
What should I do if I experience diarrhea while taking lopinavir? Mild diarrhea often improves with continued use; however, persistent or severe episodes should be reported to a clinician, who may recommend loperamide or a temporary dose adjustment.
Are there foods I must avoid with lopinavir? High-fat meals enhance absorption, so taking the medication with a regular meal is advisable. Grapefruit juice should be avoided, as it can increase lopinavir concentrations and the risk of toxicity.
Is lopinavir safe during pregnancy? Current evidence does not show an increased risk of birth defects, but therapy should be managed by an obstetrician experienced in HIV care to balance maternal viral suppression with fetal safety.
What are the most serious side effects that require immediate medical attention? Signs of severe liver injury (jaundice, dark urine), chest pain or palpitations suggesting arrhythmia, and any symptoms of an allergic reaction (rash, swelling, difficulty breathing) warrant urgent evaluation.
Can lopinavir be taken with other antiretrovirals? Yes, it is commonly combined with two NRTIs. Drug-interaction checking is essential, especially with agents metabolized by CYP3A4.
What information should I provide my doctor when discussing lopinavir?
- Complete medical history, including liver and kidney conditions.
- Full list of current medications, over-the-counter drugs, and supplements.
- Recent laboratory results (especially liver enzymes and lipid profile).
- Treatment goals and any concerns about side effects.

Disclaimer

The information provided about lopinavir is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing lopinavir for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing lopinavir.