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Date Posted: 08:18:24 01/28/02 Mon
Author: TKC
Subject: Currently Approved Drugs for HIV

Currently Approved Drugs for HIV: A Comparative Chart
Protease Inhibitors (PIs)
Drug Adult Dosing Possible Side Effects Notes
Fortovase® (saquinavir soft gel capsules), by Roche Laboratories Eight 200-mg capsules, twice a day, or Six 200-mg capsules, three times a day (a total of 16-18 pills a day) Nausea; diarrhea; stomach discomfort; insomnia; headache; increased liver enzyme levels
See long-term side effects below. Take within one hour of a full meal, preferably containing at least 28 grams of fat. Should refrigerate for long-term storage (greater than 3 months), otherwise, room temperature storage is okay.
Norvir® (ritonavir), by Abbott Laboratories Six 100-mg capsules, twice a day* (a total of 12 pills a day). Start with 3 capsules, twice a day, and increase to full dose over 14 days. Nausea; vomiting; diarrhea; loss of appetite; stomach discomfort; oral tingling and numbness; increased liver enzyme levels
See long-term side effects below. Take with food. High-fat snacks may reduce side effects. Capsules and oral solution may be stored at room temperature, but should be refrigerated in hot weather. Solution can be mixed with chocolate syrup, chocolate ice cream, or Ensure® to mask the taste. Used at lower doses to enhance other protease inhibitors.
Crixivan® (indinavir), by Merck & Co. Two 400-mg capsules, every 8 hours (a total of 6 pills a day) Kidney stones (seen in 6 - 8% of patients); nausea; vomiting; diarrhea; stomach discomfort; headache; insomnia; rash; back pain
See long-term side effects below. Take on an empty stomach (no food two hours before or one hour after dosing), or with a light, low-fat snack. Drink at least 48 ounces (six 8-oz. glasses) of water daily to prevent kidney stones.
Viracept® (nelfinavir), by Agouron Pharmaceuticals Three 250-mg tablets, three times a day, or five 250-mg tablets twice a day (a total of 9-10 pills a day) Diarrhea (common); nausea; stomach discomfort; gas; rash; increased liver enzyme levels
See long-term side effects below. Take with a meal or light snack.
Agenerase™ (amprenavir), by GlaxoSmithKline Eight 150-mg capsules, twice a day (a total of 16 pills a day) Rash (seen in 20% of patients); diarrhea; nausea; vomiting; oral tingling and numbness
See long-term side effects below. Take with or without food, however high-fat meals should be avoided.
Kaletra™ (lopinavir + ritonavir), by Abbott Laboratories Three capsules, twice a day (a total of 6 pills a day). Each capsule contains 133.3 mg lopinavir + 33.3 mg ritonavir. Diarrhea (common); nausea; feeling week/tired; headache
More rarely: Pancreatitis
See long-term side effects below.
Take with a meal or light snack. If combining with Sustiva™ (efavirenz), dose should be increased to 4 capsules, twice a day (a total of 8 pills a day). Should refrigerate for long-term storage (greater than 2 months), otherwise, room temperature storage is okay.
Long-term side effects of protease inhibitors: Use of protease inhibitors may be associated with changes in blood sugar levels (and rarely, development of diabetes), elevations in blood fat levels, and changes in the way the body stores fat (including development of fat deposits in the abdomen and on the back of the shoulders as well as loss of fat in the arms, legs and face) -- see our lesson on Lipodystrophy. In addition, there have been reports of uncontrolled bleeding in hemophiliacs.
Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs)
Drug Adult Dosing Possible Side Effects Notes
Retrovir® (AZT), by GlaxoSmithKline One 300-mg tablet, twice a day* (a total of 2 pills a day) Nausea; stomach discomfort; headache; insomnia
More rarely: Muscle wasting; anemia (low red blood cell count); neutropenia (low white blood cell count)
See long-term side effects below. Taking with food may minimize stomach discomfort.
Epivir® (3TC), by GlaxoSmithKline One 150-mg tablet, twice a day* (a total of 2 pills a day) Nausea
See long-term side effects below. Take with or without food.
Combivir® (AZT+3TC), by GlaxoSmithKline One tablet (contains 300mg AZT + 150mg 3TC), twice a day (a total of 2 pills a day) Nausea; loss of appetite; headache; fatigue; stomach discomfort
More rarely: Muscle wasting; anemia (low red blood cell count); neutropenia (low white blood cell count)
See long-term side effects below.
Take with or without food, however taking it with food may minimize stomach upset.
Trizivir™ (AZT+3TC + abacavir), by GlaxoSmithKline One tablet (contains 300mg AZT + 150mg 3TC + 300mg abacavir), twice a day (a total of 2 pills a day) Similar side effects to Retrovir (AZT), Epivir (3TC), and Ziagen (abacavir), listed above. Please note Ziagen's serious allergic reactions.
See long-term side effects below. Take with or without food. Do not take Trizivir if you weigh less than 90 pounds (40 kg).
Ziagen™ (abacavir), by GlaxoSmithKline One 300-mg tablet, twice a day* (a total of 2 pills a day) Nausea; vomiting; diarrhea; loss of appetite; insomnia

Serious allergic reactions have been reported in about 3 - 5% of patients, with one death. The signs and symptoms of this reaction include fever, malaise, severe nausea, diarrhea, abdominal pain, sore throat, cough, shortness of breath, and rash. If allergic reaction is diagnosed, therapy should be discontinued and NOT restarted. Symptoms of allergic reactions usually appear within six weeks of starting therapy and resolve within 24-48 hours of stopping the drug. A rash without other signs of allergic reaction has also been reported in about 7% of patients. These rashes can usually be managed without stopping therapy.
See long-term side effects below.
Take with or without food.
Videx® (ddI): buffered versions, by Bristol-Myers Squibb Two 100-mg tablets twice a day* (a total of 4 pills a day), or Two 200-mg tablets, once a day (a total of 2 pills a day). For patients weighing less than 133 lbs. (60 kg), click here. Numbness, tingling, or pain in the hands or feet (peripheral neuropathy, seen in 15% of patients); nausea; diarrhea; headache; vomiting; rash
More rarely: Pancreatitis
See long-term side effects below. Clinical data supports twice-daily dosing as more effective. Take on an empty stomach (2 hours after & 30 minutes before a meal). Okay to take at the same time as all NRTIs, Viramune, & Sustiva. Rescriptor & Crixivan must be taken at least 1 hour prior, and Viramune can be taken 1 hour after. Kaletra should be taken at least 1 hour after, or 2 hours before. Avoid alcohol.
Videx® EC (ddI): delayed-release capsules, by Bristol-Myers Squibb One 400-mg capsule once a day. For patients weighing less than 133 lbs. (60 kg), the dose is one 250-mg capsule once a day. Numbness, tingling, or pain in the hands or feet (peripheral neuropathy, seen in 15% of patients); nausea; diarrhea; headache; vomiting; rash
More rarely: Pancreatitis
See long-term side effects below. Clinical data supports twice-daily dosing of the buffered versions of Videx as more effective. Videx EC is indicated for adults whose management requires once-daily dosing or a non-buffered version of ddI. Take Videx EC on an empty stomach (2 hours after & 1 hour before a meal). Avoid alcohol.
Zerit® (d4T), by Bristol-Myers Squibb One 40-mg capsule, every 12 hours (a total of 2 pills a day). For patients weighing less than 133 lbs. (60 kg), click here. Nausea; numbness, tingling, or pain in the hands or feet (peripheral neuropathy)
See long-term side effects below. Take with or without food.
Hivid® (ddC), by Roche Laboratories One 0.75-mg tablet, every 8 hours (a total of 3 pills a day) Numbness, tingling, or pain in the hands or feet (peripheral neuropathy, seen in 17-31% of patients); nausea; mouth ulcers
See long-term side effects below. Works best if taken on an empty stomach.
Viread™ (tenofovir DF), by Gilead Sciences One 300-mg tablet once a day. Nuasea, vomiting, diarrhea, and flatulence (intestinal gas).
See long-term side effects below.
Works best if taken with food, preferably a meal that contains some fat.
Long-term side effects of NRTIs: NRTIs have been associated with damage to the mitochondria (the cell parts that provide energy to the cell). This damage may cause low red and white blood cell counts, muscle pain and wasting (particularly in the arms and legs), fatigue, peripheral neuropathy, and more rarely, serious liver (lactic acidosis) or pancreas problems.
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Drug Adult Dosing Possible Side Effects Notes
Viramune® (nevirapine), by Roxane Laboratories One 200-mg tablet per day for 14 days, then one 200-mg tablet, twice a day*, or two 200-mg once a day (a total of 2 pills a day) Rash; stomach upset; headaches; increased liver enzyme levels

More rarely: hepatitis Take with or without food. Once daily dosing recommendation based on limited clinical data.
Rescriptor® (delavirdine), by Agouron Pharmaceuticals Two 200-mg tablets, three times a day (a total of 6 pills a day) Rash; headache; fatigue; stomach upset; elevated liver enzymes Take with or without food.
Sustiva™ (efavirenz), by Bristol-Myers Squibb Three 200-mg capsules once a day (a total of 3 pills a day) Rash; drowsiness; insomnia; confusion; inability to concentrate; dizziness; vivid dreams; nausea; stomach discomfort; fever; insomnia; elevated liver enzymes Take with or without food, however high-fat foods should be avoided. Dose should be taken at bedtime to minimize dizziness, drowsiness and impaired concentration.

*available in oral solution/mix for children or for patients who have trouble swallowing pills

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