What is the mechanism of action of atazanavir?
Atazanavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
What is Pomeranz Fritsch synthesis of isoquinoline?
In 1893 C. Pomeranz and P. Fritsch independently described a new synthesis of isoquinoline. This prepared by heating a benzalaminoacetal generated through the condensation of benzaldehyde and 2,2-diethoxyethylamine in concentrated sulfuric acid.
What is the function of atazanavir?
Atazanavir is in a class of medications called protease inhibitors. It works by decreasing the amount of HIV in the blood. Although atazanavir does not cure HIV, it may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses such as serious infections or cancer.
Is atazanavir a competitive inhibitor?
ATV is a weak competitive inhibitor of CYP3A4 and a strong inhibitor of uridine diphosphate-glucuronosyltransferase 1A1, which is the cause of the frequent high plasma bilirubin after its administration and of its pharmacological interactions.
Why is atazanavir combined with ritonavir?
Atazanavir, which is typically administered with low-dose ritonavir (atazanavir/r), has been an important innovation in the treatment of adult HIV infection owing to its ease of dosing, virologic potency, minimal toxicity, high genetic barrier to resistance, favorable resistance profile and lower effect on lipid and …
Is atazanavir a protease inhibitors?
Atazanavir (formerly BMS-232632), an azapeptide protease inhibitor (PI), is a new human immunodeficiency virus (HIV) treatment that has recently received marketing approval from the FDA.
How is quinoline prepared by Skraup synthesis?
Quinolines may be obtained by the Skraup synthesis. This involves heating aniline or a substituted aniline with glycerol in the presence of sulphuric acid, ferrous sulphate and nitrobenzene. The reaction is complex. It involves dehydration of glycerol by means of sulphuric acid to give acrolein.
Which of the following is an application of Isoquinoline?
Isoquinolines are used in the manufacture of dyes, paints, insecticides and antifungals. It is also used as a solvent for the extraction of resins and terpenes, and as a corrosion inhibitor.
Who manufactures atazanavir?
The originator version of atazanavir, marketed as Reyataz, is manufactured by Bristol Myers Squibb.
Is atazanavir a CYP3A4 inhibitor?
Atazanavir is a known substrate and inhibitor of CYP3A4 in vitro. Therefore, medications that are also metabolized by CYP3A4 may interact with atazanavir.
What is the most common side effect of atazanavir?
The most common side effects include: nausea. headache. stomach-area pain.
How do you take atazanavir?
Take atazanavir with food. Swallow the capsules whole. Do not open the capsules. Atazanavir oral powder must be mixed with food or liquid.
Which is a modification of the Pomeranz-Fritsch reaction?
A modification of the Pomeranz–Fritsch synthesis <1983JOC3344> is used in the preparation of thieno [2,3- c]pyridine and its 2-substituted derivatives. An aryl aldehyde undergoes condensation with aminoacetaldehyde dimethyl acetal giving a Schiff base which cyclizes to form an imine product.
What is the pharmacokinetic profile of atazanavir?
Atazanavir has a pharmacokinetic profile that allows for once daily oral administration in the treatment of AIDS. Atazanavir was not associated with increases in total cholesterol, low-density lipoprotein–cholesterol or triglyceride levels after 108 weeks.
How does stavudine and atazanavir work together?
Atazanavir is a novel azapeptide protease inhibitor with high specificity for, and activity against HIV-1 protease. In combination with stavudine plus didanosine, atazanavir given once daily produces a rapid and sustained reduction in viral load in treatment-naïve patients after 48 weeks.
When to take atazanavir in combination with didanosine?
In combination with stavudine plus didanosine, atazanavir given once daily produces a rapid and sustained reduction in viral load in treatment-naïve patients after 48 weeks. Atazanavir has a pharmacokinetic profile that allows for once daily oral administration in the treatment of AIDS.