Products Zidovudine is commercially available as film-coated tablets, capsules, and syrup (Retrovir AZT, combination products). It was approved in 1987 as the first AIDS drug. Structure and properties Zidovudine (C10H13N5O4, Mr = 267.2 g/mol) or 3-azido-3-deoxythymidine (AZT) is an analog of thymidine. It exists as an odorless, white to beige, crystalline substance that is soluble … Zidovudine (AZT)
Products Ritonavir is commercially available as a monopreparation in the form of film-coated tablets (Norvir). It was approved in many countries, in the United States and in the EU in 1996, and is also used as a pharmacokinetic booster in combination with antiviral agents (eg, lopinavir). Norvir syrup is no longer marketed in many countries. … Ritonavir
Products Indinavir is commercially available in capsule form (Crixivan). It has been approved in many countries since 1996. Structure and properties Indinavir (C36H47N5O4, Mr = 613.8 g/mol) is present in drugs as indinavir sulfate, a white crystalline powder that is very soluble in water. Effects Indinavir (ATC J05AE02) has antiviral properties. The effects are due … Indinavir
Products Stavudine is commercially available in capsule form (Zerit). It has been approved in many countries since 1996. Structure and properties Stavudine (C10H12N2O4, Mr = 224.2 g/mol) is a thymidine analog with a missing 3′-hydroxy group. It is a prodrug that is biotransformed intracellularly to the active metabolite stavudine triphosphate. Stavudine exists as a white … Stavudine
Effects Reverse transcriptase inhibitors (ATC J05AF) have antiviral properties against HIV. The effects are due to inhibition of the viral enzyme reverse transcriptase, which transcribes viral RNA into DNA and is important for viral replication. Structure and properties Within the drug group, two distinct classes are distinguished. The so-called nucleoside reverse transcriptase inhibitors, abbreviated NRTIs, … Reverse Transcriptase Inhibitors (HIV)
Products Abacavir is commercially available as film-coated tablets and as an oral solution (Ziagen, combination products). It has been approved in many countries since 1999. Generic versions are approved. Structure and properties Abacavir (C14H18N6O, Mr = 286.3 g/mol) is present in drugs, among other forms, as abacavir sulfate, a white crystalline powder that is soluble … Abacavir
Products Efavirenz is commercially available as film-coated tablets and as an oral solution (Stocrin, combination products, generics). It has been approved in many countries since 2001. Structure and properties Efavirenz (C14H9ClF3NO2, Mr = 315.7 g/mol) exists as a white to light pink crystalline powder that is practically insoluble in water. It has a non-nucleoside structure … Efavirenz
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 Enfuvirtide is commercially available as a powder and solvent for the preparation of a solution for injection (Fuzeon). It has been approved in many countries since 2003. Structure and properties Enfuvirtide (C 204 H 301 N 51 O 64 , M r = 4492 g/mol) is a linear synthetic peptide composed of 36 natural … Enfuvirtide
Products Emtricitabine is commercially available as a monopreparation in the form of capsules and as an oral solution (Emtriva, combination products, generics). It has been approved in many countries since 2004. Structure and properties Emtricitabine (C8H10FN3O3S, Mr = 247.2 g/mol) is a thioanalog of cytidine with a fluorine atom at the 5-position. It exists as … Emtricitabine
Effects Integrase inhibitors have antiviral against HIV viruses. They inhibit the catalytic activity of HIV integrase, which is an HIV-encoded enzyme required for viral replication. Integrase inhibition prevents integration of the HIV genome into the host cell genome during the early phase of infection. Indications For the treatment of infection with the HIV virus (HIV). … Integrase Inhibitors