Lopinavir is a drug used in the therapy of HIV infection, acting as a protease inhibitor. The HIV protease inhibitor is used in combination with AbbVie’s product ritonavir and is known on the market by the trade name Kaletra. The drug received approval from the relevant EU Commission in 2001.
What is lopinavir?
Lopinavir is a drug used in the treatment of HIV infection, acting as a protease inhibitor. Lopinavir functions as a protease inhibitor and is used in the treatment of HIV infection. The drug is suitable for the treatment of both adults and children who are at least two years old or older. The commonly used combination of active ingredients, known as Kaletra, is approved for use in adults and children. Clinical studies and trials have shown that lopinavir is more effective than comparable agents. The drug lopinavir is available both in the form of film-coated tablets and as a syrup. In the case of the syrup, it is a fixed combination with the substance ritonavir. This received approval in Switzerland in 2000. From a chemical point of view, Lopinavir is a white or yellowish white powder. This powder is hardly soluble in water.
Pharmacological action
Lopinavir is an HIV protease inhibitor that reduces the further processing of viral precursor proteins newly formed by HIV into fully functional enzymes and structural proteins. Through this mechanism of action, the drug inhibits the replication of the HI virus. Due to the cytochrome P450 system, the substance lopinavir is metabolized by the human organism in a relatively short time. If lopinavir is administered alone, the possible concentration of the drug in the plasma of the blood would be too low to bring about a therapeutic effect. For this reason, the substance is usually used with ritonavir in a fixed combination. Ritonavir is a drug that belongs to the same group as lopinavir. In this compound, ritonavir takes the role of a second protease inhibitor, which prevents the degradation mechanism of lopinavir or cytochrome P450 monooxygenases. This allows a higher concentration of lopinavir to be present in the organism, sufficient for effective reduction of HIV proteases. An advantage of this strategy is in particular the drastic reduction of the dose for the affected patient, so that significantly fewer tablets have to be consumed. In principle, lopinavir is rapidly degraded in the liver by the cytochrome system. This hepatic degradation of the active ingredient is greatly slowed in its rate by the additional administration of the HIV protease inhibitor ritonavir. As a result, the lopinavir is able to last longer. The majority of the active ingredient binds to proteins in the blood. In addition, a combination with the so-called nucleoside reverse transcriptase inhibitors is also possible. Lopinavir binds to the viral HIV protease. This is important for the reproduction and spread of the virus. The drug inhibits viral enzymes so that replication is disrupted. As a result, the viral load for the organism of the affected patient decreases sharply.
Medical application and use
The active substance lopinavir is used for the therapy of infections with the HIV-1 virus as part of combination antiretroviral therapy. Lopinavir is an antiviral agent that belongs to the category of so-called HIV protease inhibitors and stops the multiplication of the HI virus. The corresponding effects result from the fact that lopinavir reduces the viral protease. This has a special significance and function in the maturation and multiplication of the virus. As a rule, the drug is taken once or twice a day. Most often, the drug is administered in the form of film-coated tablets, which are taken either together with meals or independently. The syrup is to be taken with meals.
Risks and side effects
Numerous adverse side effects are possible as part of taking lopinavir. The most common side effects include abdominal pain, diarrhea, vomiting, nausea, and a general feeling of weakness.In addition, there is often sweating, skin rash, headache and insomnia. Abnormal stools, flatulence and other gastrointestinal disorders also sometimes occur. Sometimes blood tests show elevated levels of triglycerides and cholesterol. In addition, allergies and central nervous system reactions are possible. Patients suffering from cardiac rhythm disorders, a structural disease of the heart or a poorly perfused heart are particularly at risk when taking lopinavir. In addition, interactions with other substances and medications are possible. The reduction of enzymes in the liver increases not only the concentration of protease inhibitors in the blood, but also that of drugs that are broken down in the same way. These include, for example, antiarrhythmics, benzodiazepines, or ergot alkaloids.
