POSITIVELY AWARE MARCH/APRIL 2011
brand name: Zerit
common name: stavudine or d4T
class: Nucleoside analog reverse transcriptase inhibitor
(nucleoside analog, NRTI, or nuke)
manufacturer: Bristol-Myers Squibb | www.bms.com, (800) 321-1335
Standard dose: One 40 mg capsule twice a day for people weighing 132 pounds or more, or one 30 mg capsule twice a day for people weighing less; with or without food, with no dietary restrictions. Zerit is also available in 15 mg, 20 mg, 30 mg and 40 mg capsules and a powder for oral solution; check for food restrictions. Dose reduction needed in people with kidney problems. Generic available. Take missed dose as soon as possible, unless it is almost time for your next dose. Do not double up on your next dose.
AWP: $474.41 (generic $411.16) / month for 40 mg capsules
Potential side effects and toxicity
Peripheral neuropathy (tingling, burning, numbness or pain in the hands or feet) may go away once Zerit is stopped, but can be painful and permanently debilitating if not treated in time. Caregivers of young children should be instructed regarding noticing and reporting peripheral neuropathy. Additive lipoatrophy (facial wasting) and mitochondrial toxicities can occur when combined with Videx. Adverse reactions and serious laboratory abnormalities in children were similar in type and frequency to those seen in adults. Other side effects may include headache, chills/fever, malaise (general ill feeling), insomnia, anxiety, depression, rash, upset stomach (nausea and vomiting), diarrhea, and abdominal pain. Rare but potentially serious toxicity with all NRTIs: enlarged, fatty liver (hepatomegaly with steatosis) and lactic acidosis (accumulation of lactate in the blood and abnormal acid-base balance). Lactic acidosis may cause persistent fatigue, abdominal pain or distension, nausea/vomiting, difficulty breathing or shortness of breath, and enlarged liver. Pancreatitis (inflammation of the pancreas) can be life-threatening and may cause pain in the stomach and back, along with nausea, vomiting, and blood in the urine. Risks for pancreatitis include higher than recommended doses of NRTIs, advanced HIV, and alcohol use. Stop all HIV medications and see a health care provider right away. Your physician will check for pancreatitis by doing blood tests. People with a history of peripheral neuropathy, pancreatitis, or heavy alcohol use should avoid Zerit. Lipoatrophy, fat loss in the face and limbs (arms and legs) and, to a lesser degree, lipohypertrophy (such as “buffalo hump” and increased abdominal fat) has been associated with Zerit. Zerit and Retrovir (zidovudine, AZT) are the HIV drugs most implicated by studies as causing lipoatrophy. Zerit also seems to be implicated in blood lipid (fat) increases, particularly triglycerides.
Potential drug interactions
When used in combination with Zerit, drugs such as Fungizone (amphotericin B), Foscavir (foscarnet), dapsone, and Videx/Videx EC may increase the risk of developing peri-pheral neuropathy. Cytovene (ganciclovir), valganciclovir (Valcyte), intravenous Pentam (pentamidine), and Videx (ddI) may increase the risk of pancreatitis. Should be used with caution by people with pre-existing bone marrow suppression, kidney problems, or peripheral neuropathy. Retrovir (zidovudine, AZT) and Zerit should not be used together due to evidence that one limits the other’s effectiveness. Because of additive neurotoxicity, if possible, Zerit should not be combined with Videx.
More information
Zerit is rarely used in the U.S., due to its toxicity and the availability of newer medi-cations. Contact your health care provider right away if peripheral neuropathy is suspected, but do not stop taking medication unless directed to do so by your health care provider. Studies show that Zerit crosses the blood-brain barrier to a useful degree, which may be beneficial for patients at risk for neurological damage (such as dementia) from HIV. Zerit is associated with facial wasting, peripheral neuropathy, and pancreatitis, and many leading HIV advocates are adamant that it should be avoided because of these serious, and relatively common, toxicities. See package insert for more complete information on potential side effects and interactions.
Doctor’s comments
There aren’t any good reasons to use this toxic drug anymore. Even resource-limited countries, where it has been used widely because of its low cost, are trying to move away from d4T. It can cause neuropathy, lipoatrophy, lactic acidosis, and hepatic steatosis (fatty infiltration of the liver). The originally approved dose (40 mg twice a day) was clearly too high, but while d4T might be safer at lower doses, why bother? —Joel Gallant, MD, MPH
Activist’s comments
Once considered an improvement over AZT, painful neuropathy and lipoatrophy (fat loss in the face, limbs, and buttocks) has made this drug a thing of the past in the developed world. Because it’s no longer profitable here, its low cost makes it a backbone of many regimens in the rest of the world—condemning HIVers to suffer the pain and disfigurement all over again when better, but more expensive, alternatives are available. —Jeff Taylor
