Protease Inhibitors

This family of medications is considered the strongest available medications for HIV and have the most side effects. They are used in infants or when children’s HIV is poorly controlled.

1. Ritonavir — also called norvir. This medication can be used as the only protease inhibitor of the drug panel or can be used in combination with other protease inhibitors (saquinavir) or to boost the strength of other protease inhibitors (kaletra).
1. Dosing: Ritonavir is available in a 400 mg or 600 mg blue capsule. It is also available in a liquid, but the taste is extremely bitter. This medication should be taken after eating and on a full stomach.
2. Side effects—Nausea and vomiting are the most common side effects and can often occur just with smelling or tasting the medication; other side effects include diarrhea, decreased appetite, abdominal pain, change in taste, headache, rash, fat accumulation in the body (known as lipodystrophy), and high blood sugars.
3. Medications which should not be taken with Ritonavir include rifabutin, cisapride, terfenadine, amiodarone, flecamide, and some seizure medications.
4. Discuss with your doctor before starting the medication if your child has liver or kidney problems or if you are planning to become pregnant.
5. Comment: When using the ritonavir/saquinavir combination, the medications should be taken 2 hours apart.
2. Saquinavir — also called fortovase, this medication is almost always used in combination with another drug in this family in an effort to maximize its effectiveness.
1. Dosing: Saquinavir is only available in a rather large gelatin capsule. It is pinkish in color and is usually taken three times per day. Saquinavir should be taken with a high fat meal.
2. Side effects: Include diarrhea, abdominal pain, nausea, headache, high blood sugar, rash, and fat deposits in the body.
3. Medications that should not be taken with this medication include astemizole, terfenadine, cisapride, midazolam and triazolam.
4. Medications that should be closely monitored when taking saquinavir include clarithromycin, ketoconazole, other HIV medications including viramune and other protease inhibitors, rifampin, and rifabutin. 1. Talk to your doctor before starting saquinavir if you have diabetes, are pregnant or may become pregnant.
5. Comment: If taken with ritonavir, take the two medications at least 2 hours apart.
3. Nelfinavir — also called viracept. This protease inhibitor is often used in small infants and children.
1. Dosing: Nelfinavir comes as a 250 mg tablet that is light blue in color or a powder form that can be mixed with water, milk, formula, or soft food. This medication should be taken with food, but avoid giving with acidic foods or juice such as orange or apple juice because this can cause a bitter taste.
2. Side effects: Diarrhea, nausea, fat deposits, and high levels of fat in the blood.
3. Medications which should not be taken with Nelfinavir include: cisapride, terfenadine, astemizole, amiodarone, quinidine, midazolam, or triazolam.
4. Comment: If your child is taking a fungus medication called ketoconazole or if you or your child are taking birth control pills, please notify the physician so doses can be adjusted if necessary.
4. Crixivan — also called indinavir; this medication is very potent.
1. Dosing: Crixivan is made only in capsule form and is therefore only used in patients who can swallow pills. It comes as 200 mg, 400 mg, or 800 mg off-white capsules. This medication should be taken on an empty stomach which means one hour before or two hours after a meal. Children taking crixivan should also increase their water intake while taking crixivan to decrease the chances of developing kidney stones. Adults should be cautious in drinking alcohol while taking this medication.
2. Side effects: Nausea, vomiting, diarrhea, rash, headache, kidney stones, liver irritation, fat depositis in the body, and belly pain.
3. Medications that should not be taken with crixivan include rifampin, rifabutin, INH, ketoconazole, clarithromycin, clotrimazole, quinidine, and birth control pills.
4. Before starting crixivan, inform the doctor if your child has diabetes, kidney problems, history of kidney stones, or if she is or may become pregnant.
5. Comment: Although this medication works best on an empty stomach, children who are having nausea and vomiting may do better if they take crixivan with a light, low fat snack.
5. Kaletra — (also called Lopinavir/Ritonavir combination), this drug is boosted, meaning it is kind of a super strength protease inhibitor. It is two protease inhibitors combined into one pill. It is sometimes saved for people that have been on many different medications over a long period of time but whose viral load continues to increase and whose CD4 count continues to fall. This is called salvage therapy.
1. Dosing: Kaletra is available in a liquid or soft gel capsule form. The liquid tastes very bitter and is often difficult for young children to swallow. It is often best given through a feeding tube placed in the stomach. The capsules are orange in color and are 133 mg doses. It generally takes 1 to 3 capsules to give an entire dose. This medication is given 2 times per day and should be taken on a full stomach.
2. Side effects: Nausea and vomiting, diarrhea, feeling tired, and headache.
3. Many medications should not be taken if a person is taking Kaletra including allergy products, cisapride, versed, some blood pressure medications, halcyon, viagra, lipitor, mevacor, or zocor.
4. Medications that should be monitored while taking Kaletra include seizure medications, metronidazole, and disulfram.
5. Before taking this medication, let the doctor know if your child has liver problems including hepatitis, diabetes, hemophilia, or if the patient is pregnant or may become pregnant.
6. Comment: While Kaletra may be difficult to use, it is a very good medication. Often, the nausea and vomiting will decrease after the first few days to a week of therapy.
6. Amprenivir — also called agenerase.
1. Dosing: Agenerase comes as a 50 mg or 150 mg capsule that is blue in color. It is also available as a liquid but is rarely used in children less than 4 years old. It is given twice a day and can be taken with or without food. Fatty foods should be avoided when taking this medication.
2. Side effects: Rash, diarrhea, nausea, vomiting, mood changes, deposits of fat in the body, tingling around the mouth, and changes in taste.
3. Comment: Some medications that should not be taken with agenerase include halcyon, cisapride, ergot medications used for migraine headaches, versed, and a medicine for tic problems called orap. Other medications require close monitoring when taken with agenerase, include rifabutin, ritonavir, viagra, St. John’s wort, rifampin, drugs to lower cholesterol, seizure medications, steroids, birth control pills, and vitamin E. There is a new form of Amprenavir now available called fosamprenavir that requires less numbers of pills to be taken. Ask the health care team about this option if you are on agenerase.
7. Reyataz — also known as atazanavir.
1. Dosing: Reyataz only comes in a capsule form. The capsule comes in a 200 mg size and the usual dose is 2 capsules one time per day. Reyataz can be boosted or supersized in certain people by adding Norvir to increase the strength of its effects. When boosting is appropriate, the dose is two 150 mg capsules of Reyataz and one 100 mg capsule of Norvir once a day. Reyataz should be taken with food, usually a complete nutritious meal, to ensure that the medicine is appropriately absorbed into the body.
2. Side effects: Jaundice, which is a yellowing of the skin and eyes caused by a build-up of bilirubin by the liver. It seems that the high bilirubin levels seen with Reyataz do not cause any other health issues or problems other than the yellowing.
3. Comment: Reyataz can interact with many other medications including acid reflux medications, antibiotics, chemotherapy medications, migraine medications, antihistamines including cold and allergy medications, heart and cholesterol medications, birth control pills, and even other HIV medications and herbal remedies. It is very important that the health care team and the pharmacist review all such medications before you start Reyataz since some medications should not be used with it and the doses of others may need to be changed to make sure they stay effective but are not toxic.