Amprenavirum

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

Amprenavirum is a protease inhibitor used to treat HIV infection.

Amprenavirum 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. Amprenavirum 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.

Amprenavirum
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Amprenavirum
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
Last Updated:	September 19, 2023 at 7:00 am

Uses

Amprenavirum is a protease inhibitor used to treat HIV infection.

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

How Amprenavirum works

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

Amprenavirum 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.

Amprenavirum Drug Interaction

Major: alprazolam, alprazolamModerate: flurazepam, flurazepamMinor: clotrimazole, clotrimazole, indinavir, indinavirUnknown: acetaminophen, acetaminophen, aspirin, aspirin, pseudoephedrine / triprolidine, pseudoephedrine / triprolidine, darbepoetin alfa, darbepoetin alfa, carboplatin, carboplatin, loratadine / pseudoephedrine, loratadine / pseudoephedrine

Amprenavirum Disease Interaction

Major: renal/liver disease, hemophiliaModerate: liver disease, nephrolithiasis, hyperglycemia, hyperlipidemiaMinor: vitamin K deficiency

Elimination Route

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