Active Ingredients

Cobicistat – Effect, Application & Risks

Cobicistat

Cobicistat is a medical agent that is used worldwide to treat HIV infections . It is only given in a so-called HIV combination therapy, ie cobicistat is only used together with other HIV medications. This enables a holistic fight against the virus , since cobicistat itself has no independent effectiveness against HI viruses .

What is cobicistat?

Cobicistat is a drug developed to treat HIV infection. The substance is one of the younger generations of HIV drugs. Cobicistat has been used in the United States since 2012. Approval in Switzerland followed shortly thereafter in 2013. Approval was granted in the European Union in 2015. The active ingredient is sold there primarily under the trade name Tybost®.

In addition, it is also used in the combination preparations emtricitabine , tenofovir disoproxil and elvitegravir .

The European Medicines Agency has temporarily placed cobicistat under additional surveillance, which is why healthcare professionals are being asked to report any abnormalities. The authority should be informed comprehensively and promptly about previously unknown side effects.

In its basic form, cobicistat is white to off-white. The substance is described in chemistry with 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 body & organs

Cobicistat only increases the effects of other HIV medicines. From a pharmacological or pharmacokinetic point of view, the drug is therefore a mere booster. It itself has no effectiveness against HIV.

A high level of effectiveness was demonstrated in relation to the protease inhibitors atazanavir and darunavir . Their effectiveness is particularly enhanced by cobicistat. Therefore, these form the main field of application of cobicistat. Cobicistat achieves its effects as a booster of protease inhibitors by inhibiting the metabolic enzyme CYP 3A4.

The degradation in the body is mainly renal, i.e. via the kidneys . The interaction potential of cobicistat is reported in the literature to be similar to that of ritonavir .

Medicinal Application & Use for Treatment & Prevention

Cobicistat is specifically designed to treat human immunodeficiency virus type 1 infection . Consequently, there is only an indication in diagnosed cases of HIV-1 infection. For the treatment of HIV-2 or HIV-3 infections, other drugs or active substances should be used as a priority.

Due to its pharmacological and pharmacokinetic properties, cobicistat is used as a booster for the HIV drugs atazanavir or darunavir. Cobicistat itself thus acts solely as a booster, so that it is always necessary to take additional medication in order to bring about the desired treatment success.

Due to its complexity and intense effects, cobicistat is pharmacy and prescription only. Treatment may only be initiated by a doctor who is sufficiently familiar with HIV infections and the corresponding therapy. As a result, cobicistat may only be dispensed to those treated by pharmacies if a corresponding certificate can be presented.

When taking it, it is imperative to follow the doctor’s 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. Usually, however, it is not necessary to take the tablets several times a day, so once-a-day dosing 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 there are uncontrollable interactions with these active ingredients, 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 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 indicated by a yellowish discoloration of the skin or eyes ) and skin rashes . These are usually recognizable by pustules or wheals . Also an itchis not exceptional.

Other possible side effects include headaches , dizziness , and a general feeling of being unwell and weak . In addition, dry mouth , a disturbed sense of taste and increased bilirubin levels are typical side effects of cobicistat.

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

Due to the large number of side effects, cobicistat may only be taken if medical supervision is guaranteed. The patient’s viral load must also be examined at regular intervals in order to be able to determine the success of the therapy.

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.