Elvitegravir

At Elvitegravir is a drug that is one of the active ingredients in integrase inhibitors. In human medicine, elvitegravir is primarily used as a drug to treat infections with the HIV-1 virus. Doctors always use the active ingredient together with other drugs that are characterized by an antiretroviral effect. Doctors often combine elvitegravir with the substance cobicistat, which is a so-called booster.

What is Elvitegravir?

Elvitegravir has a high degree of inhibition of integrase (a retroviral enzyme), which makes it suitable for treating infections with the HIV-1 virus. The pharmaceutical company Gilead Sciences developed the drug elvitegravir, which was approved as a drug by the Food and Drug Administration in 2012. Elvitegravir is mainly used for drug therapy in adult patients.

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Elvitegravir is a derivative of dihydroquinoline and appears as a powder with a white to yellowish color at room temperature. Elvitegravir is also characterized by its relatively poor solubility in water.

The active ingredient is particularly suitable for people whose HIV drug therapy is just beginning. Thus, in many cases, elvitegravir is an initial medication. Sometimes the pharmaceutical manufacturers combine elvitegravir with the active ingredient tenofovir. This combination of two drugs improves the effectiveness, while the disadvantages are partially reduced.

People infected with HIV are often given Elvitegravir as a single drug under the trade name Vitekta®. In addition, doctors often combine the active ingredient with ritonavir. Ritonavir is a pharmacological substance that is used in a wide variety of HIV drugs. Ritonavir usually acts as a booster that increases the effectiveness of the actual drug.

Pharmacological effect on the body and organs

Elvitegravir works primarily by inhibiting integrase. This means that elvitegravir is very suitable as an HIV drug. This is because elvitegravir inhibits the enzyme integrase of viruses, especially of HIV-1 viruses. Elvitegravir is somewhat less effective on HIV-2 viruses. The viruses need this enzyme in order to transfer their genetic information into the host's DNA.

In this way, elvitegravir is highly antiviral. Elvitegravir is usually used in combination with CYP inhibitors, which slow down the metabolism of elvitegravir and thereby increase its effectiveness in the body. Elvitegravir is primarily broken down by CYP3A. Therefore, simultaneous use with inducers of the enzyme should not be used. These include, for example, phenytoin or St. John's wort.

Elvitegravir has little effect on how the kidneys work. Patients take elvitegravir in tablet form. If taken at the same time as ritonavir and a meal, the active ingredient reaches the highest concentrations in the blood plasma after about four hours. Studies show that high-fat foods increase the bioavailability of elvitegravir. In the bloodstream, most of the Elvitegravir binds to the plasma proteins. The organism excretes almost 95 percent of the active ingredient in the stool. The rest of it comes out of the body with the urine. The plasma half-life of elvitegravir in combination with ritonavir is between 9 and 13 hours.

Medical application & use for treatment & prevention

Elvitegravir is an HIV-1 drug that is usually used as a fixed combination with pharmacological boosters. Patients take elvitegravir orally as a film-coated tablet. It is sufficient to consume a single tablet of the active ingredient elvitegravir per day. Elvitegravir is recommended to be taken with a meal to make it more effective.

It is mandatory to administer the active ingredient Elvitegravir together with a booster that inhibits the protease. For this reason, Elvitegravir is usually available in a fixed combination with a corresponding booster. The dose depends mainly on the protease inhibitor administered at the same time. However, doctors are currently still using the drug Elvitegravir as a reserve preparation.

Risks & side effects

Elvitegravir can sometimes have undesirable side effects that are similar to many other HIV medicines. The most common symptoms of digestive tract symptoms such as nausea, vomiting and diarrhea are caused by the administration of elvitegravir. In addition, some patients report headaches and fatigue. In addition, some people develop rashes on their skin.

The pharmaceutical manufacturers generally describe Elvitegravir as a well-tolerated drug. Therapy with the active ingredient is fundamentally excluded if the patient suffers from intolerance to the active ingredient. Even if there is resistance to elvitegravir, taking it does not make any medical sense. For pregnant and breastfeeding women, there are sometimes special requirements for therapy with elvitegravir.

Before taking elvitegravir, certain interactions with other pharmaceutical substances should be considered. Elvitegravir is metabolized primarily in the liver by the enzyme CYP3A. For this reason, simultaneous use of elvitegravir and phenytoin, rifampicin and carbamazepine must be avoided as a matter of urgency. A combination with St. John's wort should also be avoided. Elvitegravir is characterized by cross-resistance to the active ingredient raltegravir.

Elvitegravir is generally considered a reserve preparation for the drug therapy of infections with the HIV-1 virus. The clinical experience so far has been comparatively limited. The advantage of elvitegravir, however, is that one intake per day is sufficient for therapy.