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Лопинавир

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Лопинавир

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Treatment option:

Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

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Overview of Лопинавир

Quick Facts Description
Active ingredient Lopinavir (with Ritonavir booster)
Form Film-coated tablets, Oral solution
Pharmacological class Antiretroviral Agent (Protease Inhibitor)
Common use Management of HIV-1 infection
Origin Synthetic Organic Compound

Lopinavir: Pharmacological Class and Composition

Lopinavir (Лопинавир) is a synthetic anti-retroviral agent that belongs to the protease inhibitor (PI) pharmacological class, a designation clinically recognized across international guidelines. It is exclusively prescribed as a fixed-dose combination product for oral administration, always containing two active ingredients: Lopinavir itself and the necessary enhancer, Ritonavir (Ритонавир).

The inclusion of Ritonavir in a low dose is a key differentiating feature of this agent, as it acts as a pharmacokinetic enhancer or "booster," inhibiting the breakdown of Lopinavir by liver enzymes. This co-formulation strategy ensures high systemic exposure to the primary drug. The combination is recognized for its role in global therapy. Available forms, such as film-coated tablets and a specific oral solution, highlight its formulation designed to serve diverse patient groups, including pediatric patients.


Principle of Action and Main Purpose

The primary purpose of the Lopinavir/Ritonavir combination is to achieve and sustain viral suppression by significantly reducing the amount of Human Immunodeficiency Virus (HIV) in the body. The fundamental action involves the selective inhibition of the HIV protease enzyme. This unique enzymatic target is critical because the enzyme is required by the virus to cleave its large protein precursors into the functional components necessary to construct mature, infectious viral particles.

By actively blocking this enzymatic process, the medication prevents the virus from maturing and spreading effectively to other cells. This potent antiviral activity leads to a profound reduction in the patient's viral load, which is the key measure of therapeutic success. This capacity for robust viral control has positioned Lopinavir/Ritonavir as an important option for patients undergoing antiretroviral therapy, offering a verified path to managing the HIV infection and preventing the progression to Acquired Immunodeficiency Syndrome (AIDS).

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What side effects are possible with Лопинавир?

Possible Side Effects and Safety Information

The safety profile for Lopinavir/Ritonavir is officially defined by government regulatory agencies, classifying adverse reactions primarily by frequency and the body system affected. These classifications are based on findings from clinical trials and post-marketing surveillance.

Official Adverse Reaction Categories

Frequency Classification Key Adverse Reactions (Examples)
Very Common (ge 1/10) Diarrhoea, Nausea
Common (ge 1/100 to < 1/10) Vomiting, Headache, Elevated Liver Enzymes, Rash, Elevated Lipids

Adverse effects are documented across multiple System-Organ Classes, including Gastrointestinal Disorders, Hepatobiliary Disorders, Metabolism and Nutrition Disorders (e.g., changes in blood sugar and fat), and Cardiac Disorders (e.g., PR and QT interval prolongation).

Serious Safety Considerations

Regulatory warnings highlight the risk of Serious Adverse Reactions, which include severe Hepatotoxicity (liver damage, including fatal cases), Pancreatitis, and severe Cutaneous Reactions like Stevens-Johnson Syndrome ( SJS). The FDA and EMA specifically note the risk of Cardiac Conduction Abnormalities.

Population and Duration-Related Safety

Specific safety considerations are noted for certain populations, such as a contraindication in patients with severe Hepatic Impairment. The official safety information also links some events to treatment duration: Immune Reconstitution Inflammatory Syndrome ( IRIS) is typically seen at the start of therapy, while Lipodystrophy and Osteonecrosis are associated with long-term exposure to antiretrovirals. The use of this medicine is restricted with certain other drugs due to the potential for serious or life-threatening drug interactions.

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Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Lopinavir/Ritonavir outlines specific documented manifestations and mandatory emergency actions related to overexposure. Serious outcomes reported include the potential for cardiac toxicity (such as arrhythmias and cardiac failure) and acute renal failure, particularly documented in post-marketing cases. In infants and neonates, the oral solution has been associated with severe, sometimes fatal, toxicities including CNS depression, seizures, and hyperosmolality.

Immediate medical attention is required for any suspected overdose. A Certified Poison Control Center should be consulted for current management information. Treatment is based entirely on general supportive measures and continuous monitoring of vital signs.

Overdose Contextual Constraints Official Regulatory Statement
Antidote Availability No specific antidote is known.
Procedural Limitation Dialysis (haemodialysis) is unlikely to be beneficial due to high plasma protein binding.

These statements confirm that management is symptomatic and supportive, with the drug's properties limiting the effectiveness of standard drug removal procedures.

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Therapeutic Uses of Лопинавир

What Лопинавир Treats: Main Uses and Benefits

Lopinavir/Ritonavir is commonly used to help with the chronic management of Human Immunodeficiency Virus (HIV-1) infection, and may assist in supporting long-term health stability. This combination medication may assist in managing systemic viral activity, which is considered relevant for easing the overall symptomatic burden of the disease and maintaining stability in these conditions.

The agent is commonly used to help with conditions marked by increased physiological stress related to HIV. Primary indications include the management of HIV-1 infection in adults and children, used in both antiretroviral-naïve patients (those starting therapy) and antiretroviral-experienced patients. Managing systemic viral activity helps support the body's immune health. This approach supports general well-being during symptomatic phases, contributing to the maintenance of a sense of stability when symptoms are more noticeable.

Quick Fact Relief for Symptom
Primary Goal Symptoms related to systemic imbalance
Long-Term Benefit Supports functional stability
Context Treatment-Experienced Status (Applied when supportive symptom management is appropriate)

Regulatory References

  1. NIH MedlinePlus Drug Information
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Eligibility and Restrictions for Use

Who Can and Cannot Use Лопинавир (Lopinavir/Ritonavir)

The population eligibility for Лопинавир is strictly defined by regulatory authorities to ensure patient safety and appropriate use.

Absolute Contraindications

The medicine is contraindicated and must not be used in individuals with a known hypersensitivity to lopinavir, ritonavir, or any component of the formulation. It is also prohibited for patients with severe hepatic impairment (Child-Pugh Class C). Additionally, co-administration with certain drugs that are heavily reliant on the CYP3A enzyme for clearance is strictly forbidden due to the risk of serious complications.


Age and Physiological Restrictions

Age Eligibility

The medicine is approved for use in adults and pediatric patients 14 days of age and older. Use is not recommended in infants younger than 14 days. Older adults (65+ years) should use the medicine with caution, often requiring closer monitoring.

Special Conditions

Patients with mild to moderate hepatic impairment require close monitoring and use with caution. For pregnancy, use is generally allowed, but it is not recommended for women who are breastfeeding due to the risk of HIV transmission and potential adverse effects on the infant. Caution is also advised for patients with a history of pre-existing cardiac disease or conduction system abnormalities.

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What should I know about interactions with other medicines?

The interaction profile for Lopinavir/Ritonavir is primarily defined by its effects as a powerful inhibitor of the CYP3A enzyme system, which controls the metabolism of many other medicines. This leads directly to the most critical interaction classification: contraindicated combinations.


Contraindicated Combinations

Co-administration is prohibited with drugs highly dependent on CYP3A for clearance, where elevated plasma concentrations could lead to serious or life-threatening reactions. These restricted agents include certain antiarrhythmics (e.g., Dronedarone, Amiodarone), HMG-CoA Reductase Inhibitors (e.g., Simvastatin, Lovastatin), and specific sedatives (e.g., oral Midazolam, Triazolam). Potent CYP3A inducers, such as the herbal product St. John's Wort, are also contraindicated because they significantly reduce Lopinavir exposure, which risks loss of virologic response.


Population and Administration Restrictions

Lopinavir's pharmacokinetic activity also includes documented inhibition of transporters like P-gp and OATP1B1/3. The medication is contraindicated in severe hepatic insufficiency due to the official documentation of increased Lopinavir exposure in this patient population. The oral solution formulation has specific restrictions: it must be taken with food to ensure adequate absorption and is contraindicated with Disulfiram or Metronidazole due to its alcohol content. Additionally, the liquid formulation requires mandatory timing separation when co-administered with Didanosine.

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Mechanism of Action

Lopinavir functions as a peptidomimetic inhibitor, primarily targeting the Human Immunodeficiency Virus type 1 (HIV-1) protease enzyme. This biological target is a dimeric aspartic protease essential for viral maturation. Lopinavir selectively binds to the active site of the protease, mimicking the peptide sequence normally cleaved by the enzyme. The drug incorporates a non-cleavable hydroxyethylene scaffold, which competitively inhibits the enzyme's catalytic activity.

Intracellularly, this inhibition prevents the proteolysis of the viral Gag and Gag-Pol polyproteins. Consequently, the viral particle assembly process is interrupted, leading to the formation and release of morphologically immature and non-infectious virions from the host cell. This disruption of the replication cycle limits the systemic propagation of the virus. The co-administration with ritonavir inhibits the host hepatic cytochrome P450 3A (CYP3A) isoenzymes, reducing lopinavir's oxidative metabolism and maintaining elevated plasma concentrations of the active inhibitor.

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Dosage and Administration Information

How to Use Lopinavir/Ritonavir

Lopinavir is used as a fixed-dose combination with the pharmacokinetic booster Ritonavir, following established administration protocols. The medication is delivered via the oral route, available as film-coated tablets (typically 200 mg Lopinavir / 50 mg Ritonavir) and an oral solution.


Dosing and Administration Schedule

The standard adult regimen is Lopinavir 400 mg / Ritonavir 100 mg. This amount is administered twice daily (BID) for many patients, while a once-daily (QD) regimen (800 mg / 200 mg) is used for specific treatment-naïve adults. The medication is intended for long-term, sustained administration as part of a combination regimen.

Dosage Form Contextual Administration Rule
Film-Coated Tablets May be taken with or without food; must be swallowed whole and not crushed.
Oral Solution Must be taken with food to ensure proper absorption.

Population-Specific Use and Missed Doses

For pediatric patients, the dose is calculated based on body surface area (BSA) or weight. Special consideration is also applied in cases of severe hepatic impairment, where dosage adjustment may be required. If a dose is missed, standard procedure involves taking the dose as soon as possible, unless the time is near the next scheduled dose, in which case the missed dose is skipped. The overall procedural structure defines the standardized timing and handling required to maintain the necessary drug levels over an indefinite course of treatment.

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Recent Clinical Evidence

Research evidence / Overview of studies for Lopinavir

Lopinavir for treating HIV-1 infection

Lopinavir has been extensively studied for the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection. The main type of research conducted involves large, carefully designed studies called randomized controlled trials (RCTs). These studies compare lopinavir, usually combined with a boosting agent and other HIV medicines, against different combination regimens to see what outcomes are observed.

The primary finding from decades of research is that Lopinavir-based regimens have been the subject of research exploring their association with control of the HIV virus, with findings often reporting a low or undetectable level of the virus in the blood. Studies have explored its use both in people who are new to treatment (antiretroviral-naive patients) and in those who have previously taken other HIV medications (treatment-experienced patients). Research has also explored variations in the study protocol, and findings indicated that both approaches were associated with similar findings for viral control in studies involving many adults starting treatment for the first time.

Researchers have also explored different combinations of drugs with lopinavir, including regimens that simplify the number of co-administered medicines. The evidence generally indicates that lopinavir-based regimens were associated with viral suppression in studies and research suggested a low likelihood of the virus developing resistance to lopinavir itself. For specific populations, studies have successfully evaluated different formulations, such as easy-to-use oral pellets, for use in infants and young children living with HIV, reporting results consistent with viral control in this group. What remains less certain is the long-term findings from studies comparing lopinavir-based regimens with different regimens in all patient groups, as research into treatment options continues to evolve.


Lopinavir for Coronaviruses (including COVID-19)

Given that lopinavir was developed to treat a viral infection, researchers explored its use against coronaviruses, including SARS-CoV-2 (the virus that causes COVID-19). The types of studies conducted for this indication varied widely, ranging from small observational studies to very large, international randomized controlled trials (RCTs). These studies mostly compared lopinavir (often combined with a boosting agent) to standard supportive care in patients who were sick enough to be admitted to the hospital.

For patients hospitalized with COVID-19, the large-scale, high-quality research generally indicated that adding lopinavir to the usual hospital care were not associated with a notable change in the chances of survival or the length of time patients stayed in the hospital. These findings were consistent across different patient groups. Research has also explored whether giving lopinavir very early in the course of COVID-19 to non-hospitalized patients might be associated with symptom resolution, but findings suggested that lopinavir was not observed to significantly accelerate the improvement of symptoms. Overall, the research on lopinavir for COVID-19 indicated that the medicine was not associated with a measured difference in study endpoints for people with the disease in these studies.

Key Studies & References Efficacy and Safety of Lopinavir/Ritonavir for Treatment of COVID-19: A Systematic Review and Meta-Analysis

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Frequently Asked Questions (FAQ)

Common questions about Лопинавир (FAQ)

Q: Is this medication available as a generic, and does it go by any other brand names?

A: The medication, which contains the active ingredients lopinavir and ritonavir, is available as a generic formulation. The product was originally marketed under the brand name Kaletra. This status and the composition of the medicine are detailed in official regulatory documents.

Q: Can I take common pain relievers (like ibuprofen or acetaminophen) with this drug?

A: Official product information indicates that lopinavir/ritonavir can significantly alter the plasma concentrations of many other drugs. This means there is a potential for drug interactions with common pain relievers. Official documents state the necessity of reviewing all potential drug interactions with a healthcare provider before making any changes to treatment.

Q: Are there any warnings about driving or operating heavy machinery?

A: The official product information notes that certain adverse reactions have been reported in clinical trials. These include dizziness and asthenia (a feeling of lack or loss of strength). These potential effects may warrant caution when driving or operating machinery, as described in the official safety information.

Q: Is therapeutic drug monitoring (blood level testing) required during treatment?

A: While standard dosing is generally considered effective for most patients, official guidelines or research indicates that monitoring lopinavir drug concentrations may be considered during treatment. This practice, known as therapeutic drug monitoring, is sometimes suggested for certain patient populations, such as women who are pregnant, to help ensure the desired viral response is sustained.

Q: Does this medicine affect mood, anxiety, or sleep?

A: Yes, the official safety documentation mentions that the drug may affect the nervous system and mental health. Psychiatric adverse reactions reported in clinical studies include anxiety, depression, and insomnia (trouble with sleeping). This information is reported in the adverse reactions section of the drug’s regulatory label.

Q: Is there a warning about stopping the medication suddenly (discontinuation)?

A: Regulatory patient counseling information describes the risk of altering the dose or discontinuing therapy without healthcare supervision. Stopping the medication suddenly can cause the amount of HIV-1 virus in the blood to increase. This elevated viral load may also lead to the virus becoming resistant to the medication over time.

Q: Does the tablet formulation contain lactose or any other common allergens?

A: The official prescribing information lists all inactive ingredients in the tablet formulation, which includes excipients like lactose. It is noted that hypersensitivity (an allergic reaction) to the active substances or any component of the formulation is a stated contraindication. For individuals with known allergies or intolerances, the full ingredient list is available in the official prescribing information for review.

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How should Лопинавир be stored and disposed of?

Storage and Disposal of Lopinavir/Ritonavir

Official storage conditions for Lopinavir/Ritonavir differ by dosage form and must be followed to maintain stability. Keep all medication out of the sight and reach of children.


Storage Requirements

Dosage Form Mandatory Storage Condition
Film-Coated Tablets Store at controlled room temperature (20 C to 25 C); protect from light and excess moisture. Keep in the original container with the cap tightly closed.
Oral Solution Store preferably in a refrigerator (2 C to 8 C). Do not freeze. If stored at room temperature (below 25 C), it must be used within 42 days (6 weeks) or 2 months.

Disposal

Dispose of unused or expired medicine according to local regulations. Regulatory guidance instructs against flushing the medicine down a toilet or pouring it into a drain unless specifically advised by a healthcare professional.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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