Агенераза

Агенераза Uses, Dosage, Side Effects, Food Interaction and all others data.

Агенераза is a protease inhibitor used to treat HIV infection.

Агенераза is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. 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. Агенераза 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.

Trade Name Агенераза
Availability Discontinued
Generic Amprenavir
Amprenavir Other Names Amprenavir, Amprénavir, Amprenavirum
Related Drugs Biktarvy, Truvada, tenofovir, ritonavir, Complera, Atripla, Stribild
Type
Formula C25H35N3O6S
Weight Average: 505.627
Monoisotopic: 505.224656557
Protein binding

Very high (90%). Amprenavir has the highest affinity for alpha(1)-acid glycoprotein.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country Russia
Last Updated: September 19, 2023 at 7:00 am
Агенераза
Агенераза

Uses

Агенераза is a protease inhibitor used to treat HIV infection.

For the treatment of HIV-1 infection in combination with other antiretroviral agents.

How Агенераза works

Агенераза inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Food Interaction

  • Avoid alcohol. Drug impairs alcohol metabolism.
  • Avoid fatty foods.
  • Take with or without food.

[Moderate] GENERALLY AVOID: Administration with a high-fat meal may decrease the oral bioavailability of amprenavir.

The mechanism is unknown.

In healthy volunteers, consumption of a standardized high-fat meal decreased the peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of amprenavir (1200 mg single oral dose) by 36% and 21%, respectively, compared to administration in the fasted state.

The time to reach Cmax (Tmax) was increased 44% following a high-fat meal.

Grapefruit juice does not appear to significantly affect the pharmacokinetics of amprenavir.

In 12 healthy volunteers, administration with grapefruit juice (200 mL) decreased the mean peak plasma concentration (Cmax) of amprenavir (1200 mg single oral dose) by 22% compared to water.

The median time to reach Cmax (Tmax) was prolonged from 0.75 to 1.13 hours.

These pharmacokinetic changes are not thought to be clinically significant, since antiretroviral response is more closely associated with systemic exposure (AUC) and trough plasma concentration (Cmin), which were not affected in the study.

MANAGEMENT: Агенераза may be taken with or without food, but should not be taken with a high-fat meal.

Агенераза 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.

Elimination Route

Rapidly absorbed after oral administration in HIV-1-infected patients with a time to peak concentration (Tmax) typically between 1 and 2 hours after a single oral dose. The absolute oral bioavailability of amprenavir in humans has not been established.

Half Life

7.1-10.6 hours

Innovators Monograph

You find simplified version here Агенераза

*** Taking medicines without doctor's advice can cause long-term problems.
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