Cobicistat

Cobicistat is a medicinal substance that is used worldwide to treat HIV infections. The award takes place exclusively in a so-called HIV combination therapy, i. H. Cobicistat is only used with other HIV medicines. This enables a holistic fight against the virus, since cobicistat itself has no independent effectiveness against HI viruses.

What is cobicistat?

Cobicistat is a medicine that was developed to treat HIV infection. The substance is one of the younger generations of HIV drugs. Cobicistat has been used in the USA since 2012. Approval in Switzerland followed shortly afterwards in 2013. In the European Union, approval was granted in 2015. There the active ingredient is mainly marketed under the trade name Tybost®.

It is also used in the combined preparations emtricitabine, tenofovir disoproxil and elvitegravir.

The European Medicines Agency placed Cobicistat under additional surveillance for the time being, which is why medical professionals are called upon to report any abnormalities. The authority is to be informed comprehensively and promptly about previously unknown side effects.

Cobicistat is white to yellowish-white in its basic form. In chemistry, the substance is described by the empirical formula C 40 - H 53 - N 7 - O 5 - S 2, M r, which corresponds to a moral mass of 776.0 g / mol.

Pharmacological effect on the body and organs

Cobicistat only increases the effects of other HIV preparations. From a pharmacological or pharmacokinetic point of view, the drug is a mere booster. It is not itself effective against HIV.

The protease inhibitors atazanavir and darunavir were shown to be highly effective. Their effectiveness is particularly enhanced by cobicistat. This is why these form the main field of application for Cobicistat. Cobicistat achieves its effects as a booster of protease inhibitors by inhibiting the metabolic enzyme CYP 3A4.

The breakdown in the body takes place mainly renally, i.e. via the kidneys. The potential for interaction with cobicistat is described in the literature as similar to that of ritonavir.

Medical application & use for treatment & prevention

Cobicistat was specially developed to treat infections with the human immunodeficiency virus type 1. Consequently, there is only an indication in diagnosed cases of HIV-1 infection. For the treatment of HIV-2 or HIV-3 infections, priority should be given to other drugs or active ingredients.

Because of its pharmacological and pharmacokinetic properties, cobicistat is used as an amplifier for the HIV drugs atazanavir or darunavir. Cobicistat itself acts solely as a booster, so that further medication is always required to bring about the desired treatment success.

Due to its complexity and intense effect, Cobicistat is subject to pharmacy and prescription requirements. Treatment should only be started by a doctor who is sufficiently familiar with HIV infections and the corresponding therapy. Cobicistat may therefore only be issued to the patient by pharmacies if a corresponding certificate can be presented.

When taking it, it is imperative to pay attention to the medical instructions. Cobicistat is only sold in the form of film-coated tablets. These are approx. 10 mm in size, orange and round. They may only be taken orally with food. The exact dosage of the booster depends on whether the effect of atazanavir or darunavir is to be increased. However, it is usually not necessary to take the tablets several times a day, so taking them once a day is the norm.

Risks & side effects

Cobicistat should not be taken if there is a contraindication in the form of a contraindication. This is the case if an allergy or intolerance is known, severe kidney damage is present or preparations are taken that contain one of the following active ingredients: alfuzosin, cisapride, pimozide, midazolam, lovastatin, St. John's wort, quinidine, rifampicin, amiodarone, sildenafil. Because with these active ingredients there are uncontrollable interactions which reduce the safety of use and massively increase the risk of undesirable effects.

In addition to the risk of interactions, attention should also be paid to possible side effects. These include u. a. Symptoms of the gastrointestinal tract (severe nausea, diarrhea, pain after eating, vomiting, constipation or a greatly increased appetite), the development of jaundice (jaundice, which is a yellowish discoloration of the skin or eyes) and rashes. These can usually be recognized by pustules or wheals. Itching is also not unusual.

Other possible side effects include headache, dizziness and a general feeling of malaise and weakness. In addition, dry mouth, impaired taste and increased bilirubin levels are typical side effects of cobicistat.

Rarely, muscle or limb pain, fever, depression and hematuria (blood in the urine) can also occur.

Due to the large number of side effects, Cobicistat may only be taken if a medical check-up is guaranteed. The patient's viral load must also be examined at regularly recurring intervals in order to be able to determine the success of the therapy.