Definition and mechanisms A pharmacokinetic booster is an agent that improves the pharmacokinetic properties of another agent. It is a desirable drug interaction It can exert its effects at different levels (ADME): Absorption (uptake into the body). Distribution (distribution) Metabolism and first-pass metabolism (metabolization). Elimination (excretion) Pharmacokinetic enhancers can increase absorption, increase distribution to an … Pharmacokinetic Booster
Products Elvitegravir is commercially available as film-coated tablets in fixed combination with other antiretroviral agents and cobicistat (Stribild, successor: Genvoya). It has been approved in many countries since 2013. Stribild: elvitegravir, cobicistat, emtricitabine, and tenofovirdisoproxil. Genvoya: elvitegravir, cobicistat, emtricitabine and tenofoviralafenamide. Structure and properties Elvitegravir (C23H23ClFNO5, Mr = 447.9 g/mol) is a dihydroquinolone derivative. It … Elvitegravir
Products Darunavir is commercially available as film-coated tablets and as an oral suspension (Prezista). It has been approved in many countries since 2006. In 2016, a fixed-dose combination with cobicistat was approved (Rezolsta film-coated tablets). In 2018, generic versions of the tablets entered the market. Structure and properties Darunavir (C27H37N3O7S, Mr = 547.7 g/mol) is … Darunavir
Products Cobicistat is commercially available as a monopreparation (Tybost) and as a fixed combination with elvitegravir, emtricitabine, and tenofovirdisoproxil in the form of film-coated tablets (Stribild). It has been approved in many countries since 2013. Other combination products exist with darunavir (Rezolsta) and with atazanavir (Evotaz). Structure and properties Cobicistat (C40H53N7O5S2, Mr = 776.0 g/mol) … Cobicistat
CYP450 Cytochromes P450s are a family of enzymes that are of paramount importance in drug biotransformation. The most important isoenzymes for drug metabolism are: CYP1A1, CYP1A2 CYP2B6 CYP2C9, CYP2C19 CYP2D6 CYP2E1 CYP3A4, CYP3A5 and CYP3A7 The number after the abbreviation CYP stands for the family, the following letter for the subfamily and the last number … Cytochrome P450 (CYP)
Definition When two or more drugs are combined, they may affect each other. This is especially true with regard to their pharmacokinetics (ADME) and effects and adverse effects (pharmacodynamics). This phenomenon is called interaction and drug-drug interaction. Interactions are usually undesirable because they can lead to, for example, loss of efficacy, side effects, poisoning, hospitalization, … Interactions
Definition Drugs today usually contain a defined active pharmaceutical ingredient. However, numerous drugs with two or more active substances also exist. These are called combination drugs or fixed combinations. For example, Aspirin C contains both acetylsalicylic acid and vitamin C. Many blood pressure medications are combination preparations, for example perindopril + indapamide or candesartan + … Combination Products
Products Bictegravir was approved in the United States and EU in 2018 and in many countries in 2019 in fixed combination with emtricitabine and tenofoviralafenamide in the form of film-coated tablets (Biktarvy). Structure and properties Bictegravir (C21H18F3N3O5, Mr = 449.4 g/mol) exists as a white to yellowish substance. Effects Bictegravir (ATC J05AR20) has antiviral properties. … Bictegravir
Products Most HIV protease inhibitors are commercially available in tablet or capsule form. In addition, a few liquid dosage forms are available for ingestion. Saquinavir (Invirase) was the first to be lanicized in 1995. Structure and properties The first HIV protease inhibitors were modeled on the natural peptide substrate of the HIV protease. The protease … HIV Protease Inhibitor
Atazanavir is an active medical substance. It is used to treat HIV infection. What is atazanavir? Atazanavir is a medical active ingredient. It is used for the therapy of HIV infections. The drug atazanavir is commercially available in Germany under the name Reyataz. It is taken orally and is used to treat HIV infections. The … Atazanavir: Effects, Uses & Risks
Products Atazanavir is commercially available in capsule form (Reyataz). It has been approved in many countries since 2004. Generic versions were registered in 2017. Structure and properties Atazanavir (C38H52N6O7, Mr = 704.9 g/mol) is present in drugs as atazanavir sulfate, a white to slightly yellow crystalline powder that is sparingly soluble in water. Effects Atazanavir … Atazanavir
Products Various drugs containing tenofoviralafenamide are on the market worldwide. In many countries, tenofoviralafenamide was first approved in 2016 (United States: 2015). Biktarvy: bictegravir, emtricitabine, and tenofoviralafenamide (HIV). Genvoya: elvitegravir, cobicistat, emtricitabine, and tenofoviralafenamide (HIV). Descovy: emtricitabine and tenofoviralafenamide (HIV). Odefsey: emtricitabine, rilpivirine and tenofoviralafenamide (HIV). Symtuza: darunavir + cobicistat + emtricitabine + tenofoviralafenamide. Vemlidy: … Tenofoviralafenamide
