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Date Posted: 13:18:26 01/26/02 Sat
Author: No name
Subject: DRUGS;ETC.

WHAT IS RITONAVIR?

Ritonavir, also called Norvir, is a drug used for antiviral therapy. It is manufactured by Abbott Laboratories. Ritonavir 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 RITONAVIR?

Ritonavir was approved as an antiviral drug for adults and children with HIV infection. Most doctors start antiviral therapy when a person has some symptoms of HIV disease, has a T-cell count (CD4+ cells) below 350, or has a viral load (a measure of the amount of virus in the blood) over 30,000.

There are no absolute rules about when to start antiviral drugs. Some people want to "hit HIV hard and early", starting with the most powerful drugs to preserve the immune system. Others want to save the strongest drugs until they are needed, later in the course of HIV disease. 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.

If you take ritonavir 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.

Ritonavir makes the liver work more slowly. This can increase the blood levels of some drugs, including other protease inhibitors. Some doctors combine ritonavir with other protease inhibitors to produce better blood levels.



--------------------------------------------------------------------------------


WHAT ABOUT DRUG RESISTANCE?

The HIV virus is sloppy when it makes copies of its genetic code (RNA). 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.
If you take a protease inhibitor by itself, resistance develops within one month. When you take more than one antiviral drug at the same time, HIV mutates much more slowly and it takes much longer for resistance to develop.

Sometimes, if you develop resistance to one drug, you will also have resistance to other antiviral drugs. This is called "cross-resistance".

Resistance can develop quickly. It is very important to take protease inhibitors according to instructions, on schedule, and not to skip or reduce doses.



--------------------------------------------------------------------------------

HOW IS RITONAVIR TAKEN?

Ritonavir is taken by mouth as a liquid or capsule. The normal dose is 600 milligrams (mg) twice a day. The capsules are 100mg, so you will take 6 capsules every 12 hours. Ritonavir should be taken with meals, if possible.

Ritonavir is sometimes combined with other protease inhibitors. These combinations might use a different amount of ritonavir. Be sure you know how much ritonavir you are supposed to take.

During 1998, Abbott Laboratories noticed problems with the original ritonavir capsules. Production was stopped. Everyone taking ritonavir had to take the liquid form. Many people think the liquid version tastes bad. However, some people find the liquid more convenient. It will still be available.

Liquid ritonavir comes with a measuring cup. It takes 7.5mL (milliliters) of liquid (1-1/2 teaspoons) to equal the normal dose of 600 mg. The liquid version should not be refrigerated. Shake the bottle before taking each dose.

Your pharmacist must keep the new ritonavir soft-gel capsules refrigerated. You should keep ritonavir in your refrigerator, but it can also stay out at room temperature (below 77 degrees F, or 25 degrees C) for up to 30 days.



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WHAT ARE THE SIDE EFFECTS?

The most serious side effects of ritonavir are nausea, vomiting, gas, and diarrhea. Some people also experience tingling or numbness around the mouth, or find that foods taste strange. Side effects made almost one-third of people stop taking ritonavir.

For many people, the side effects of ritonavir lasted only 2 to 4 weeks. If they lasted beyond 4 weeks, in most cases they were permanent.

To reduce stomach upset with ritonavir, the manufacturer recommends starting with half the usual dose and increasing the drug on the following schedule:
Day 1: 300mg every 12 hours
Days 2-3: 400mg every 12 hours
Day 4: 500mg every 12 hours
Day 5 and after: 600mg every 12 hours



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HOW DOES RITONAVIR REACT WITH OTHER DRUGS?

Ritonavir is broken down by the liver. It can interact with other drugs that 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.

If you are taking ritonavir and ddI, you should take them 2-1/2 half hours apart.

Some birth control pills may not work if you are taking ritonavir. Talk to your doctor about how to prevent an unwanted pregnancy.

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 February 14, 2001

WHAT IS SAQUINAVIR?

Saquinavir, also called Fortovase or Invirase, is a drug used for antiviral therapy. It is manufactured by Roche Laboratories. Saquinavir 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 SAQUINAVIR?

Saquinavir was approved as an antiviral drug for people with HIV infection. Most doctors start antiviral therapy when a person has some symptoms of HIV disease, has a T-cell count (CD4+ cells) below 350, or has a viral load (a measure of the amount of virus in the blood) over 30,000.

There are no absolute rules about when to start antiviral drugs. Some people want to "hit HIV hard and early", starting with the most powerful drugs to preserve the immune system. Others want to save the strongest drugs until they are needed, later in the course of HIV disease. 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.

If you take saquinavir 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?

The HIV virus is sloppy when it makes copies of its genetic code (RNA). 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.

If you take a protease inhibitor by itself, resistance develops within one month. When you take more than one antiviral drug at the same time, HIV mutates much more slowly and it takes much longer for resistance to develop.

Sometimes, if you develop resistance to one drug, you will also have resistance to other antiviral drugs. This is called "cross-resistance".

Resistance can develop quickly. It is very important to take protease inhibitors according to instructions, on schedule, and not to skip or reduce doses.



--------------------------------------------------------------------------------


HOW IS SAQUINAVIR TAKEN?

The normal dose of the Saquinavir soft-gel capsule (Fortovase) is 1,200 milligrams (mg) three times a day. The capsules are 200mg, so you will take 6 capsules every 8 hours. Researchers are studying twice a day dosing of saquinavir.

Some physicians prescribe saquinavir in combination with another protease inhibitor, ritonavir. Studies are underway using a single daily dose of saquinavir taken with a small amount of ritonavir.

Saquinavir should be taken within two hours after a full meal or a large snack. Saquinavir is absorbed better (more of the drug gets into your bloodstream) if you take it after eating foods that are high in calories, fat, and protein.

NOTE: Saquinavir was initially marketed as Invirase. This formulation of the drug was not absorbed very well, and is being replaced by Fortovase.

Your pharmacist should keep saquinavir refrigerated. When you take it home, you can refrigerate it, or else keep it below 77 F or 25 C and use it within three months.



--------------------------------------------------------------------------------

WHAT ARE THE SIDE EFFECTS?

The side effects of saquinavir are usually mild. Most people can take it with no problems. However, some people get nausea, diarrhea, upset stomach, and heartburn.


--------------------------------------------------------------------------------

HOW DOES SAQUINAVIR REACT WITH OTHER DRUGS?

Saquinavir 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 several antihistamines, sedatives, and anti-fungal drugs. Make sure that your doctor knows about ALL drugs you are taking.

Some birth control pills may not work if you are taking saquinavir. Talk to your doctor about how to prevent an unwanted pregnancy.

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 February 14, 2001

WHAT IS NELFINAVIR?

Nelfinavir, also called Viracept, is a drug used for antiviral therapy. It is manufactured by Agouron Pharmaceuticals. Nelfinavir 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 NELFINAVIR?

Nelfinavir is an antiviral drug for adults and children with HIV infection. Most doctors start antiviral therapy when a person has some symptoms of HIV disease, has a T-cell count (CD4+ cells) below 350, or has a viral load (a measure of the amount of virus in the blood) is over 30,000.

There are no absolute rules about when to start antiviral drugs. Some people want to "hit HIV hard and early", starting with the most powerful drugs to preserve the immune system. Others want to save the strongest drugs until they are needed, later in the course of HIV disease. 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.

If you take nelfinavir 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?

The HIV virus is sloppy when it makes copies of its genetic code (RNA). 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.

If you take a protease inhibitor by itself, resistance develops within one month. When you take more than one antiviral drug at the same time, HIV mutates much more slowly and it takes much longer for resistance to develop.

Sometimes, if you develop resistance to one drug, you will also have resistance to other antiviral drugs. This is called "cross-resistance". Researchers are excited about nelfinavir because it appears that it will not be cross-resistant with other protease inhibitors.

Resistance can develop quickly. It is very important to take protease inhibitors according to instructions, on schedule, and not to skip or reduce doses.



--------------------------------------------------------------------------------
HOW IS NELFINAVIR TAKEN?

Nelfinavir is taken by mouth as a capsule. The normal dose is 750 milligrams (mg) three times a day. The capsules are 250mg, so you will take 3 capsules at a time.

Late in 1999, the FDA approved twice-daily dosing of nelfinavir at 1250 mg per dose. This means taking 5 capsules at a time. If you want to change how often you take nelfinavir, talk to your doctor.

The former capsules dissolved quickly and were difficult to swallow. A film-coated tablet was approved in March 2000 and replaced the old capsules.

Nelfinavir should be taken with meals. It should be stored at room temperature and protected from moisture, freezing, or excessive heat.



--------------------------------------------------------------------------------
WHAT ARE THE SIDE EFFECTS?

The most common side effects of nelfinavir are diarrhea, weakness, headache, nausea, and abdominal pain. None of these side effects seem to be very serious. The diarrhea in most cases can be controlled with over-the-counter medications.


--------------------------------------------------------------------------------
HOW DOES NELFINAVIR REACT WITH OTHER DRUGS?

Nelfinavir 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.

If you are taking nelfinavir and ddI, you should take ddI one hour before or two hours after nelfinavir.

Some birth control pills may not work if you are taking nelfinavir. Talk to your doctor about how to prevent an unwanted pregnancy.

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 February 14, 2001



WHAT IS AMPRENAVIR?
Amprenavir, also called Agenerase, is a drug used for antiviral therapy. It is manufactured by GlaxoSmithKline. Amprenavir 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 AMPRENAVIR?
Amprenavir was approved as an antiviral drug for people with HIV infection. Most doctors start antiviral therapy when a person has some symptoms of HIV disease, has a T-cell count (CD4+ cells) below 350, or has a viral load (a measure of the amount of virus in the blood) over 30,000.


There are no absolute rules about when to start antiviral drugs. Some people want to "hit HIV hard and early", starting with the most powerful drugs to preserve the immune system. Others want to save the strongest drugs until they are needed, later in the course of HIV disease. 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.

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.

Amprenavir is a sulfa drug. If you know that you are allergic to sulfa drugs, be sure to tell your doctor before taking amprenavir.

The liquid form of amprenavir contains an inactive ingredient called propylene glycol. This ingredient can cause problems for infants or children under 4 years old, pregnant women, people with liver or kidney failure, or people taking certain medications. They should not use liquid amprenavir.



--------------------------------------------------------------------------------


WHAT ABOUT DRUG RESISTANCE?
The HIV virus is sloppy when it makes copies of its genetic code (RNA). 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.

If you take a protease inhibitor by itself, resistance develops within one month. When you take more than one antiviral drug at the same time, HIV mutates much more slowly and it takes much longer for resistance to develop.

Sometimes, if you develop resistance to one drug, you 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 protease inhibitors according to instructions, on schedule, and not to skip or reduce doses.



--------------------------------------------------------------------------------


HOW IS AMPRENAVIR 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 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. The liquid form contains an inactive ingredient (propylene glycol) that should not be taken by infants or children under 4 years old, pregnant women, or people with liver or kidney failure, or people taking certain drugs.

Amprenavir 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" of amprenavir. A prodrug becomes active after it is broken down in the body. GW433908 should provide the same benefits as amprenavir with fewer pills to take.

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



--------------------------------------------------------------------------------


VITAMIN E
Amprenavir capsules contain vitamin E. The Vitamin E makes amprenavir easier for the body to absorb and makes it work better. Each 150mg capsule contains 109 International Units (IU) of Vitamin E. The normal adult dose of amprenavir 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 of amprenavir are nausea, diarrhea, vomiting, rash, numbness around the mouth, and abdominal pain. About 1% of people taking amprenavir 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 fat redistribution (lipodystrophy) the way that other protease inhibitors do.



--------------------------------------------------------------------------------


HOW DOES AMPRENAVIR 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.

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 February 14, 2001



WHAT IS LOPINAVIR?
Lopinavir is a drug used for antiviral therapy. Lopinavir used to be called ABT-378. It is manufactured by Abbott Laboratories. Lopinavir is a protease inhibitor. The amount of Lopinavir in the blood stream stays much higher if it is taken with a small amount of ritonavir, another protease inhibitor. See Fact Sheet 442 for more information on ritonavir. Kaletra is a combination of lopinavir and ritonavir in the same capsule.

Protease inhibitors 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 KALETRA?
Kaletra is an antiviral drug for adults with HIV infection. Most doctors start antiviral therapy when a person has some symptoms of HIV disease, has a T-cell count (CD4+ cells) below 350, or has a viral load (a measure of the amount of virus in the blood) over 30,000.

There are no absolute rules about when to start antiviral drugs. Some people want to "hit HIV hard and early", starting with the most powerful drugs to preserve the immune system. Others want to save the strongest drugs until they are needed, later in the course of HIV disease. 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.

If you take Kaletra 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?
The HIV virus is sloppy when it makes copies of its genetic code (RNA). 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.

If you take a protease inhibitor by itself, resistance develops within one month. When you take more than one antiviral drug at the same time, HIV mutates much more slowly and it takes much longer for resistance to develop.

Sometimes, if you develop resistance to one drug, you will also have resistance to other antiviral drugs. This is called "cross-resistance".

Doctors are excited about Kaletra because it provides blood levels that are high enough to control HIV that has already developed some resistance to other protease inhibitors.

Resistance can develop quickly. It is very important to take protease inhibitors according to instructions, on schedule, and not to skip or reduce doses.


--------------------------------------------------------------------------------


HOW IS KALETRA TAKEN?
Kaletra is taken by mouth as a capsule. Each capsule contains 133 milligrams (mg) of lopinavir and 33 mg of ritonavir. The normal dose is three capsules twice a day. Kaletra should be taken with food.

Kaletra is also available in liquid form. The adult dose is 5 milliliters (ml) twice a day.

Kaletra is approved for use by children. Their dosage is based on their body weight.

Your pharmacist should keep Kaletra refrigerated. When you take it home, you can refrigerate it, or else keep it below 77 F or 25 C and use it within two months.


--------------------------------------------------------------------------------

WHAT ARE THE SIDE EFFECTS?
The most common side effects of Kaletra are diarrhea, fatigue, headache, and nausea. None of these side effects seem to be very serious. Kaletra can increase the amount of fat (cholesterol and triglycerides) in your blood. High levels of blood fats can increase your risk of problems with your heart or pancreas.


--------------------------------------------------------------------------------


HOW DOES KALETRA REACT WITH OTHER DRUGS?
Kaletra 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.

If you are taking Kaletra and ddI, you should take ddI one hour before or two hours after Kaletra. You should also take Kaletra one hour apart from antacids.

Some birth control pills may not work if you are taking Kaletra. Talk to your doctor about how to prevent an unwanted pregnancy.

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 February 14, 2001

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