Pronunciation: (in-DIN-ah-veer SULL-fate)
Class: Protease inhibitor

Trade Names:
Crixivan
- Capsules 100 mg
- Capsules 200 mg
- Capsules 333 mg
- Capsules 400 mg

Indinavir Sulfate is an oral capsule used for the treatment of HIV (Human Immunodeficiency Virus). HIV is the virus that causes AIDS (acquired immune deficiency syndrome). CRIXIVAN is a type of HIV drug called a protease (PRO-tee-ase) inhibitor.

Pharmacology

Indinavir Sulfate is a drug that inhibits the human immunodeficiency virus (HIV) protease. HIV causes the immune system to break down so that it can no longer fight off other infections. This leads to the fatal disease known as acquired immune deficiency syndrome (AIDS). CRIXIVAN Capsules are formulated as a sulfate salt and are available for oral administration in strengths of 100, 200, and 400 mg of indinavir (corresponding to 125, 250, and 500 mg indinavir sulfate, respectively). Each capsule also contains the dormant ingredients anhydrous lactose and magnesium stearate. The capsule shell contains the following inactive ingredients and dyes:, titanium dioxide, silicon dioxide and sodium lauryl sulfate.

HIV thrives by taking over the immune system’s vital CD4 cells (white blood cells) and using their inner workings to make additional copies of it. Crixivan belongs to a class of HIV drugs called protease inhibitors, which work by interfering with an important step in the virus’s reproductive cycle. Even though Crixivan cannot eliminate HIV already present in the body, it can reduce the amount of virus available to infect other cells.

Crixivan can be taken alone or in combination with other HIV drugs such as zidovudine. Because Crixivan and zidovudine hit the virus in diverse ways, the combination is likely to be more effective than either drug alone.

Indinavir sulfate is a capsule that has a white to off-white color, hygroscopic, crystalline powder with the molecular formula C₃₆H₄₇N₅O₄•H₂SO₄ and a molecular weight of

711.88. It is very soluble in water and in methanol. Indinavir sulf

ate has the following structural formula:

Brief History of Indinavir Sulfate

The Food and Drug Administration (FDA) approved indinavir last March 13, 1996, making it the eighth approved antiretroviral. Indinavir was a lot more powerful than any prior antiretroviral drug; using it with dual NRTIs set the standard for treatment of HIV/AIDS and raised the bar on design and introduction of subsequent antiretroviral drugs. Protease inhibitors changed the very nature of the AIDS epidemic from one of a terminal illness to a somewhat manageable one.

Increasingly, it is being replaced by newer drugs that are more convenient to take and less likely to promote resistant virus, such as lopinavir or atazanavir.

Important Fact About This Drug

It is important that you drink at least six 8-ounce glasses of liquid (preferably water) daily while taking Crixivan. If you do not get enough liquid, you may develop kidney stones and have to temporarily stop taking Crixivan or even discontinue it altogether.

Dosage

Take Indinavir sulfate exactly as prescribed by your doctor. Do not share Indinavir sulfate with anyone and do not take more than your recommended dosage.

To ensure maximum absorption, do not take Crixivan with food. Instead, take it with water 1 hour before or 2 hours after a meal. (Crixivan may also be taken with liquids such as skim milk, juice, coffee, or tea, or even with a light meal such as dry toast with jelly, juice, and coffee with skim milk and sugar, or corn flakes with skim milk and sugar.)

* If you miss a dose…

Skip it and take the next dose at the regularly scheduled time. Do not double the dose.

Overdosage

There have been more than 60 reports of acute or chronic human overdosage (up to 23 times the recommended total daily dose of 2400 mg) with CRIXIVAN. The most commonly reported symptoms were renal (e.g., nephrolithiasis/urolithiasis, flank pain, hematuria) and gastrointestinal (e.g., nausea, vomiting, diarrhea).

How does it work?

CRIXIVAN is a protease inhibitor that fights HIV. CRIXIVAN can help lessen your chances of getting illnesses related with HIV. CRIXIVAN can also help lower the amount of HIV in your body (called “viral load”) and raise your CD4 (T) cell count. CRIXIVAN may not have these effects in all patients.

CRIXIVAN is usually prescribed with other anti-HIV drugs such as ZDV (also called AZT), 3TC, ddI, ddC, or d4T. CRIXIVAN works differently from these other anti-HIV drugs. Talk with your doctor about how you should take CRIXIVAN.

Possible Side Effects

Side effects cannot be anticipated. If any develop or change in intensity, inform your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking Crixivan.

Side effects may include  abdominal pain, acid regurgitation, back pain, bladder stones, changes in taste, diarrhea, dizziness, drowsiness, dry skin, fatigue, headache, itching, jaundice (yellowish skin or eyes, especially in children), kidney stones, liver problems, loss of appetite, nausea, pain in the side, rash, redistribution of body fat, sore throat or upper respiratory tract infection, vomiting, weakness.

Some patients treated with CRIXIVAN developed kidney stones. In some of these patients this led to more severe kidney problems, including kidney failure or inflammation of the kidneys or kidney infection which sometimes spread to the blood. Drinking at least six 8-ounce glasses of liquids (preferably water) each day should help reduce the chances of forming a kidney stone (see How should I take CRIXIVAN?). Call your doctor or other health care provider if you develop kidney pains (middle to lower stomach or back pain) or blood in the urine.

Some patients treated with CRIXIVAN have had rapid breakdown of red blood cells (hemolytic anemia) which in some cases was severe or resulted in death.

Some patients treated with CRIXIVAN have had liver problems including liver failure and death. Some patients had other illnesses or were taking other drugs. It is uncertain if CRIXIVAN caused these liver problems.

Diabetes and high blood sugar (hyperglycemia) have occurred in patients taking protease inhibitors. In some of these patients, this led to ketoacidosis, a serious condition caused by poorly controlled blood sugar. Some patients had diabetes before starting protease inhibitors, others did not. Some patients necessitate adjustments to their diabetes medication. Others needed new diabetes medication.

In some patients with hemophilia, increased bleeding has been reported.

Severe muscle pain and weakness have occurred in patients taking protease inhibitors, including CRIXIVAN, together with some of the cholesterol-lowering medicines called “statins”. Call your doctor if you develop severe muscle pain or weakness.

Changes in body fat have been seen in some patients taking antiretroviral therapy. These changes may include increased amount of fat in the upper back and neck (“buffalo hump”), breast, and around the trunk. Loss of fat from the legs, arms and face may also happen. The cause and long term health effects of these conditions are not known at this time.

In some patients with advanced HIV infection (AIDS), signs and symptoms of inflammation from opportunistic infections may occur when combination antiretroviral treatment is started.

How should one take this drug?

There are six important things you must do to help you benefit from CRIXIVAN:

• Take CRIXIVAN capsules every day as prescribed by your doctor. Continue taking CRIXIVAN unless your doctor tells you to stop. Take the exact amount of CRIXIVAN that your doctor tells you to take, right from the very start. To help make sure you will benefit from CRIXIVAN, you must not skip doses or take “drug holidays”. If you don’t take CRIXIVAN as prescribed, the activity of CRIXIVAN may be reduced (due to resistance).
• Take CRIXIVAN capsules every 8 hours around the clock, every day. It may be easier to remember to take CRIXIVAN if you take it at the same time every day. If you have questions about when to take CRIXIVAN, your doctor or health care provider can help you decide what schedule works for you.
• If you miss a dose by more than 2 hours, wait and then take the next dose at the regularly scheduled time. However, if you miss a dose by less than 2 hours, take your missed dose immediately. Then take your next dose at the regularly scheduled time. Do not take more or less than your prescribed dose of CRIXIVAN at any one time.
• Take CRIXIVAN with water. You can also take CRIXIVAN with other beverages such as skim or non-fat milk, juice, coffee, or tea.

Ideally, take each dose of CRIXIVAN without food but with water at least one hour before or two hours after a meal. Or you can take CRIXIVAN with a light meal. Examples of light meals include:  dry toast with jelly, juice, and coffee (with skim or non-fat milk and sugar if you want) cornflakes with skim or non-fat milk and sugar

Do not take CRIXIVAN at the same time as any meals that are high in calories, fat, and protein (for example – a bacon and egg breakfast). When taken at the same time as CRIXIVAN, these foods can interfere with CRIXIVAN being absorbed into your bloodstream and may lessen its effect.

• It is critical to drink plenty of fluids while taking CRIXIVAN. Adults should drink at least six 8-ounce glasses of liquids (preferably water) throughout the day, every day. Your health care provider will provide you further instructions on the amount of fluid that you should drink. CRIXIVAN can cause kidney stones. Having enough fluids in your body should help reduce the chances of forming a kidney stone. Call your doctor or other health care provider if you develop kidney pains (middle to lower stomach or back pain) or blood in the urine.

Does CRIXIVAN cure HIV or AIDS?

CRIXIVAN is not a cure for HIV or AIDS. People under the medications of  CRIXIVAN may still develop infections or other conditions related with HIV. Because of this, it is very important for you to remain under the care of a doctor. Although CRIXIVAN is not a cure for HIV or AIDS, CRIXIVAN can help reduce your chances of getting illnesses, including death, associated with HIV. CRIXIVAN may not have these effects in all patients.

Special warnings about Indinavir sulfate

Although Crixivan reduces the amount of HIV in the blood and increases the white blood cell count, its long-term effect on survival is still unknown. The virus remains in the body, and you will continue to face the possibility of complications, including opportunistic infections (rare infections that develop when the immune system falters) such as certain types of pneumonia, tuberculosis, and fungal infection. Therefore, it is important that you remain under the care of a doctor and keep all your follow-up appointments.

Crixivan is not a cure for HIV infection, and it does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Therefore, you should continue to avoid practices that could spread HIV.

Protease inhibitors such as Crixivan have been known to trigger diabetes (high blood sugar levels) or worsen existing diabetes. If you have diabetes, the dosages of your diabetes medications may have to be adjusted.

People who are under HIV medications may also experience a redistribution of body fat, with wasting of the face, arms, and legs, and accumulation of fat around the middle, the upper back, and breasts.

Cases of liver failure and death have occurred in patients treated with Crixivan and other medications. If you have a liver problem, particularly cirrhosis of the liver, make sure the doctor is aware of it. Kidney problems, including kidney and urinary stones, are also a possibility, so alert the doctor if you have any type of kidney disease.

Some patients have developed severe anemia (loss of red blood cells) while taking Crixivan. If this problem surfaces, you will have to stop taking the drug.

If you have hemophilia, you should also be aware that spontaneous bleeding has occurred in hemophilia victims taking protease inhibitors such as Crixivan.

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