Zidovudine (AZT)

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)

Ritonavir

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

Stavudine

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

Reverse Transcriptase Inhibitors (HIV)

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)

Fusion Inhibitors

Effects Fusion inhibitors have antiviral properties against viruses. They inhibit fusion with the host cell and prevent virus entry. Indications For the treatment of viral infectious diseases. Active ingredients Enfuvirtide (Fuzeon) Umifenovir (Arbidol)

Pharmacokinetic Booster

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

Efavirenz

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

Elvitegravir

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

Enfuvirtide

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

Emtricitabine

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

Nyaope

Products Nyaope is illegally traded and consumed in South Africa. Structure and properties Nyaope consists of cheap heroin mixed or cut with other psychoactive substances, drugs, and technical substances. These include, for example, amphetamines, local anesthetics, HIV drugs, dextromethorphan, rat poison, and swimming pool cleaner. Abuse As a euphoric intoxicant. Dosage Nyaope is usually smoked … Nyaope

Integrase Inhibitors

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