At Lopinavir is a drug that is used in the treatment of HIV infections and acts as a protease inhibitor. The HIV protease inhibitor is used in combination with the product ritonavir from AbbVie and is known on the market under the trade name Kaletra®. The drug received approval from the responsible EU Commission in 2001.
What is Lopinavir?
Lopinavir acts as a protease inhibitor and is used to treat HIV infection. The drug is suitable for both adults and children who are at least two years old or older. The common combination of active ingredients called Kaletra® is approved for adults and children. Clinical studies and tests have shown that lopinavir is more effective than comparable active ingredients.
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 was approved 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 effect
Lopinavir is an HIV protease inhibitor that reduces the processing of viral precursor proteins, which are newly formed by the HI virus, into fully functional enzymes and structural proteins. Through this mechanism of action, the drug inhibits the reproduction of the HI virus.
Due to the cytochrome P450 system, the substance lopinavir is metabolized by the human body in a relatively short time. If lopinavir is administered alone, the potential concentration of the drug in the plasma of the blood would be too low to have a therapeutic effect. For this reason, the substance is usually used in a fixed combination with ritonavir.
Ritonavir is a medicine that belongs to the same group as lopinavir. In this connection, ritonavir takes on the role of a second protease inhibitor, which prevents the breakdown mechanism of lopinavir or the cytochrome P450 monooxygenases. This makes it possible that a higher concentration of lopinavir is present in the body, which is sufficient for an effective reduction of the HIV proteases.
One advantage of this strategy lies in the drastic reduction in the dose for the patient concerned, so that significantly fewer tablets have to be consumed.
Basically, lopinavir is rapidly broken down by the cytochrome system in the liver. This hepatic breakdown of the active ingredient is greatly slowed down by the additional administration of the HIV protease inhibitor ritonavir. This enables the lopinavir to last longer.
Most of the active ingredient binds to proteins in the blood. In addition, a combination with what are known as nucleoside reverse transcriptase inhibitors is also possible.
The lopinavir binds to the HIV viral protease. This is important for the virus to multiply and spread. The drug curbs viral enzymes so that reproduction is disturbed. As a result, the viral load for the affected patient's organism drops sharply.
Medical application & use
The active ingredient lopinavir is used to treat infections with the HIV-1 virus as part of an antiretroviral combination therapy. Lopinavir is an antiviral agent that belongs to the category of so-called HIV protease inhibitors and stops the HIV virus from multiplying.
The corresponding effects result from the fact that lopinavir reduces the viral protease. This assumes a special meaning and function in the maturation and reproduction of the virus.
As a rule, the drug is taken once or twice a day. The drug is usually administered in the form of film-coated tablets that are taken either with or without meals. The syrup is to be taken with meals.
Risks & side effects
Numerous undesirable side effects are possible when taking lopinavir. The most common side effects include abdominal pain, diarrhea, vomiting, nausea, and a general feeling of weakness. In addition, there are often sweating, rashes, headaches and insomnia.
Abnormal stool, flatulence and other gastrointestinal disorders also occur in some cases. Occasionally, blood tests show increased levels of triglycerides and cholesterol. In addition, allergies and reactions of the central nervous system are possible.
Patients who suffer from cardiac arrhythmias, a structural heart disease or a poorly supplied heart are particularly at risk when taking lopinavir.
Interactions with other substances and drugs are also possible. The lowering of enzymes in the liver increases not only the concentration of protease inhibitors in the blood, but also that of drugs, which are broken down in the same way. These include, for example, antiarrhythmics, benzodiazepines or ergot alkaloids.
