Atazanavir
Atazanavir Uses, Dosage, Side Effects, Food Interaction and all others data.
Atazanavir (formerly known as BMS-232632) is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). Atazanavir is distinguished from other PIs in that it can be given once-daily (rather than requiring multiple doses per day) and has lesser effects on the patient's lipid profile (the amounts of cholesterol and other fatty substances in the blood). Like other protease inhibitors, it is used only in combination with other HIV medications. The U.S. Food and Drug Administration (FDA) approved atazanavir on June 20, 2003.
Atazanavir (ATV) is an azapeptide HIV-1 protease inhibitor (PI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. 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. Atazanivir is pharmacologically related but structurally different from other protease inhibitors and other currently available antiretrovirals.
| Trade Name | Atazanavir |
| Availability | Prescription only |
| Generic | Atazanavir |
| Atazanavir Other Names | Atazanavir, Atazanavirum |
| Related Drugs | Biktarvy, Truvada, tenofovir, ritonavir, zidovudine, abacavir, emtricitabine, Complera, Atripla, Stribild |
| Weight | 150mg, 200mg, 300mg, 50mg |
| Type | Capsule, Oral Capsule, Oral Powder For Reconstitution |
| Formula | C38H52N6O7 |
| Weight | Average: 704.8555 Monoisotopic: 704.389748048 |
| Protein binding | 86% bound to human serum proteins (alpha-1-acid glycoprotein and albumin). Protein binding is independent of concentration. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Dr, Reddys Laboratories (UK) Ltd |
| Available Country | United Kingdom, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Atazanavir is an antiviral protease inhibitor used in combination with other antiretrovirals for the treatment of HIV.
Used in combination with other antiretroviral agents for the treatment of HIV-1 infection, as well as postexposure prophylaxis of HIV infection in individuals who have had occupational or nonoccupational exposure to potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission.
Atazanavir is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How Atazanavir works
Atazanavir selectively inhibits the virus-specific processing of viral Gag and Gag-Pol polyproteins in HIV-1 infected cells by binding to the active site of HIV-1 protease, thus preventing the formation of mature virions. Atazanavir is not active against HIV-2.
Food Interaction
- Take with food. Food increases product absorption and reduces pharmacokinetic variability.
[Moderate] ADJUST DOSING INTERVAL: Administration of atazanavir with food enhances oral bioavailability and reduces pharmacokinetic variability.
According to the manufacturer, administration with a light meal increased the peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of a single 400 mg dose of atazanavir by 57% and 70%, respectively, relative to the fasting state.
Administration with a high-fat meal resulted in a mean increase of 35% in atazanavir AUC and no change in Cmax compared to fasting.
The coefficient of variation of AUC and Cmax decreased by approximately one-half when given with either a light or high-fat meal compared to the fasting state.
MANAGEMENT: To ensure maximal oral absorption, atazanavir should be administered with or immediately after a meal.
Atazanavir Cholesterol interaction
[Moderate] Hyperlipidemia has been observed in 10% of patients receiving ritonavir during clinical trials.
Increases of 30% to 40% from baseline have been reported for total cholesterol and 200% to 300% or more for triglycerides.
These effects have also been reported during postmarketing experience with other protease inhibitors (PIs) but may be the most dramatic with ritonavir.
The clinical significance of these elevations is unclear.
Severe hyperlipidemia is known to sometimes cause pancreatitis.
In addition, some patients have reportedly developed symptomatic atherosclerosis and coronary artery disease after initiating PI treatment.
Patients with preexisting hyperlipidemia may require closer monitoring during PI therapy, and adjustments made accordingly in their lipid-lowering regimen.
PI therapy should be administered cautiously in patients with coronary artery disease or a history of ischemic heart disease.
Atazanavir Drug Interaction
Major: quetiapine, quetiapineModerate: emtricitabine / tenofovir, emtricitabine / tenofovirUnknown: copper gluconate, copper gluconate, acetaminophen, acetaminophen, bioflavonoids, bioflavonoids, riboflavin, riboflavin, pyridoxine, pyridoxine, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, phytonadione, phytonadione
Atazanavir Disease Interaction
Major: heart block, nephrolithiasis, renal impairment, hemophiliaModerate: liver disease, PKU, hyperglycemia, hyperlipidemia
Elimination Route
Atazanavir is rapidly absorbed with a Tmax of approximately 2.5 hours. Administration of atazanavir with food enhances bioavailability and reduces pharmacokinetic variability. Oral bioavailability is 60-68%.
Half Life
Elimination half-life in adults (healthy and HIV infected) is approximately 7 hours (following a 400 mg daily dose with a light meal). Elimination half-life in hepatically impaired is 12.1 hours (following a single 400 mg dose).
Innovators Monograph
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