• Monday July 13,2020

lopinavir

Lopinavir is a medicine used in the treatment of HIV infection, acting as a protease inhibitor. The HIV protease inhibitor is used in combination with the product Ritonavir from AbbVie and is known in the market under the trade name Kaletra®. The drug was approved by the responsible EU Commission in 2001.

What is Lopinavir?

Lopinavir is a medicine used in the treatment of HIV infection, acting as a protease inhibitor.

Lopinavir has the function of a protease inhibitor and is used in the treatment of HIV infection. The drug is suitable both for therapy of adults and children who are at least two years or older. The common drug combination called Kaletra® is approved in adults and children. Clinical trials and trials have shown lopinavir to be more effective than comparable drugs.

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 has been approved in Switzerland in 2000. From a chemical point of view, lopinavir is a white or even yellowish-white powder. This powder is hardly soluble in water.

Pharmacological action

Lopinavir is an HIV protease inhibitor that reduces the processing of viral progenitor proteins re-formed by the HI virus into fully functional enzymes and structural proteins. Through this mechanism of action, the drug inhibits the multiplication 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 possible concentration of the drug in the plasma of the blood would be too low to produce a therapeutic effect. For this reason, the substance is usually used with ritonavir in a fixed combination.

Ritonavir is a medicine that belongs to the same group as lopinavir. In this compound, ritonavir plays the role of a second protease inhibitor, which prevents the degradation mechanism of lopinavir or the cytochrome P450 monooxygenases. This allows the organism to have a higher concentration of lopinavir sufficient to effectively reduce 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.

Basically, lopinavir is rapidly metabolized by the cytochrome system in the liver. This hepatic degradation of the active ingredient is slowed down by the additional administration of the HIV protease inhibitor ritonavir greatly in its speed. As a result, lopinavir is able to work longer.

The majority of the active substance binds to proteins in the blood. In addition, a combination with the so-called nucleoside reverse transcriptase inhibitors is possible.

The lopinavir binds to the viral HIV protease. This is important for the propagation and spread of the virus. The drug restricts viral enzymes, interfering with the proliferation. As a result, the viral load for the organism of the affected patient decreases 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 multiplication of the HIV virus.

The corresponding effects arise from the fact that lopinavir reduces the viral protease. This takes on a special meaning and function in the maturation and multiplication of the virus.

As a rule, the drug is taken once or twice a day. Mostly, the drug is given in the form of film-coated tablets, which are taken either together with meals or independently. The syrup should be taken with meals.

Risks & Side Effects

When taking lopinavir many adverse reactions are possible. The most common side effects include abdominal pain, diarrhea, vomiting, nausea and a general feeling of weakness. In addition, sweating, rash, headache and insomnia are common.

Abnormal stools, flatulence and other gastrointestinal disturbances also occur in part. Sometimes blood tests show elevated levels of triglycerides and cholesterol. In addition, allergies and reactions of the central nervous system are possible.

Patients who suffer from cardiac arrhythmias, structural heart disease, or a poorly circulated heart are particularly at risk from taking lopinavir.

In addition, interactions with other substances and medicines are possible. The reduction of enzymes in the liver not only increases the concentration of protease inhibitors in the blood, but also those of drugs that break down in the same way. These include, for example, antiarrhythmics, benzodiazepines or ergot alkaloids.

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