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Fact Sheet Number 445

AMPRENAVIR (Agenerase)


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WHAT IS AMPRENAVIR?

Amprenavir is a drug used for antiviral therapy. It is also called

Agenerase®. It is manufactured by GlaxoSmithKline. It used

to be called 141W94.

Amprenavir is a protease inhibitor. These drugs prevent the protease

enzyme from working. HIV protease acts like a chemical scissors.

It cuts the raw material for HIV into specific pieces needed to

build a new virus. Protease inhibitors “gum up” these

scissors.


WHO

SHOULD TAKE IT?

Amprenavir was approved as an antiviral drug for people with HIV

infection. There are no absolute rules about when to start antiviral

drugs. You and your doctor should consider your T-cell

count, your viral load,

any symptoms you are having, and your attitude about taking HIV

medications. Fact Sheet 411

has more information about guidelines

for the use of antiviral medications.

If you take amprenavir with other antiviral drugs, you can

reduce your viral load to extremely low levels, and increase your

T-cell counts. This should mean staying healthier longer.


WHAT ABOUT DRUG

RESISTANCE?

Many new copies of HIV are mutations. They are slightly different

from the original virus. Some mutations can keep multiplying even

when you are taking an antiviral drug. When this happens, the

drug will stop working. This is called “developing resistance”

to the drug. See Fact Sheet 414

for more information on resistance.

Sometimes, if your virus develops resistance to one drug, it

will also have resistance to other antiviral drugs. This is called

“cross-resistance”. Researchers are excited about Amprenavir

because it might not be cross-resistant with other protease inhibitors.

Resistance can develop quickly. It is very important to

take antiviral medications according to instructions, on schedule,

and not to skip or reduce doses.


HOW IS IT TAKEN?

Amprenavir is taken by mouth as a capsule. The normal adult dose

is 1200 milligrams (mg) two times a day. The capsules are 150mg,

so you will take 8 capsules at a time. The dose is lower, based

on body weight, for children and people who weigh less than 50

kilograms (110 pounds).

Amprenavir was also approved in two combinations with the protease

inhibitor ritonavir:

  • 600 mg (4 capsules) of amprenavir plus 100 mg (one capsule)

    of ritonavir, taken twice a day, or

  • 1200 mg (8 capsules) of amprenavir plus 200 mg (2 capsules)

    of ritonavir, taken just once a day.

Different doses are used in some combinations. Be sure you

know how much amprenavir your doctor has prescribed for you, and

when and how to take each dose.

If you have liver problems, you may need to take a lower dose

of amprenavir.

Amprenavir is available as gelatin capsules and as a liquid.

The gelatin capsules should be kept at room temperature. If they

get too warm, they can melt. People taking the liquid form should

not drink alcoholic beverages.

It can be taken with or without food, but high-fat meals should

be avoided. Do not take antacids within one hour of taking

amprenavir.

GlaxoSmithKline is developing GW433908, a new form of amprenavir.

It is a “prodrug.” A prodrug becomes active after it

is broken down in the body. GW433908 should provide the same benefits

with fewer pills.


VITAMIN E

Amprenavir capsules contain vitamin E. The Vitamin E improves

how the drug is absorbed and how it works. Each 150mg capsule

contains 109 International Units (IU) of Vitamin E. The normal

adult dose contains 1,744 IU of vitamin E. This information can

help you decide what vitamin supplements to take.


WHAT ARE THE SIDE

EFFECTS?

The most common side effects are nausea, diarrhea, vomiting, rash,

numbness around the mouth, and abdominal pain. About 1% of people

get serious skin reactions, including Stevens-Johnson syndrome.

No other side effects seem to be very serious. The diarrhea in

most cases can be controlled with over-the-counter medications.

Amprenavir might not cause problems with high cholesterol levels

the way that other protease inhibitors do.

Amprenavir is a sulfa drug. If you are allergic to sulfa drugs,

be sure to tell your doctor.

Liquid amprenavir contains an ingredient called propylene glycol.

It can cause problems, and should not be used by the following

patients:

  • infants or children under 4 years old
  • pregnant women
  • people with liver or kidney failure
  • people taking certain medications (check with your doctor.)

HOW DOES IT REACT

WITH OTHER DRUGS?

Amprenavir is broken down by the liver and can interact with other

drugs that also use the liver. Combining these drugs can change

the amount of each drug in your bloodstream and cause an under-

or overdose. Drugs to watch out for include Viagra, several antihistamines,

sedatives, drugs to lower cholesterol and anti-fungal drugs. Make

sure that your doctor knows about ALL drugs you are taking.

Amprenavir works better if it is taken with the reverse

transcriptase inhibitor abacavir.

If you are taking amprenavir and ddI,

you should take them one hour apart. You should also take amprenavir

one hour apart from antacids.

Some birth control pills may not work if you are taking amprenavir.

Talk to your doctor about how to prevent an unwanted pregnancy.

Taking amprenavir with methadone can lower blood levels of

both drugs. Check with your doctor if you use methadone.

The herb St. John’s Wort (See

Fact Sheet 729) lowers the blood levels of some protease inhibitors.

Tell your doctor about any herbs or other supplements that you

use.


Revised August 16, 2002

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