Cobicistat is a medical agent that is used worldwide to treat HIV infection. It is administered exclusively in a so-called HIV combination therapy, i.e. Cobicistat is only used together with other HIV drugs. 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 that was developed to treat HIV infection. The substance is one of the younger generations of HIV medications. Cobicistat has been used in the USA since 2012. Approval in Switzerland followed shortly thereafter in 2013. In the European Union, approval was granted in 2015, where the active ingredient is marketed primarily under the trade name Tybost. In addition, use also occurs in the combination products emtricitabine, tenofovirdisoproxil and elvitegravir. The European Medicines Agency has provisionally placed Cobicistat under additional surveillance, calling on healthcare professionals to report any abnormalities. The agency should be fully and promptly informed of any previously unknown side effects. Cobicistat is white to whitish-yellow in its basic form. The substance is described in chemistry as having the molecular 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 effects on body and organs
Cobicistat merely potentiates the effects of other HIV drugs. Thus, the drug presents as a mere booster when viewed pharmacologically or pharmacokinetically. It has no efficacy against HIV. High efficacy has been demonstrated with respect to the protease inhibitors atazanavir and darunavir. Their efficacy is particularly enhanced by cobicistat. Therefore, these constitute the main field of application of cobicistat. Cobicistat achieves its effects as a booster of protease inhibitors by inhibiting the metabolic enzyme CYP 3A4. Degradation in the body occurs predominantly renally, i.e. via the kidneys. The interaction potential of cobicistat is reported in the literature to be similar to that of ritonavir.
Medicinal use and use for treatment and prevention.
Cobicistat is specifically designed to treat human immunodeficiency virus type 1 infections. Consequently, there is an indication only in diagnosed cases of HIV-1 infection. For the treatment of HIV-2 or HIV-3 infections, other drugs or active substances must be used as a matter of priority. Due to its pharmacological or pharmacokinetic properties, cobicistat is used as an enhancer of the HIV drugs atazanavir or darunavir. Cobicistat itself thus acts solely as a booster, so that the use of other drugs 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 may only be initiated by a physician who is sufficiently familiar with HIV infections as well as the corresponding therapy. Cobicistat may therefore only be dispensed by pharmacies to those receiving treatment if an appropriate certificate can be presented. When taking the drug, it is imperative to follow the doctor’s instructions. Cobicistat is sold exclusively in the form of film-coated tablets. These are about 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 boosted. Usually, however, it is not necessary to take the tablets several times a day, so once-a-day is the rule.
Risks and side effects
Cobicistat must not be taken if there is a contraindication in the form of a contraindication. This is the case if there is a known allergy or intolerance, severe kidney damage is present, or preparations are taken that contain any of the following active ingredients: Alfuzosin, Cisapride, Pimozide, Midazolam, Lovastatin, St. John’s wort, Quinidine, Rifampicin, Amiodarone, Sildenafil. This is because there are uncontrollable interactions with these agents, which reduce the safety of application and massively increase the risk of adverse effects. In addition to the risk of interactions, attention must also be paid to possible side effects.These include gastrointestinal complaints (severe nausea, diarrhea, pain after ingestion, vomiting, constipation, or a greatly increased appetite), the development of jaundice (yellowing of the skin or eyes), and skin rashes. These are usually recognizable by pustules or wheals. Itching is also not uncommon. Other side effects that may be considered include headache, dizziness, and a general feeling of discomfort and weakness. In addition, dry mouth, impaired sense of taste, and elevated bilirubin levels are also typical side effects of cobicistat. Rarely, muscle or limb pain, fever, depression, and hematuria (blood in the urine) may also occur. Because of the variety of side effects, cobicistat should be taken only if a doctor’s supervision is warranted. Also, the patient’s viral load must be examined at regularly recurring intervals to determine the success of therapy.
