Epivir

Nucleoside Reverse Transcriptase Inhibitor

Common Name: lamivudine or 3TC

Brand Name: Epivir

Class: nucleoside analog (also called nucleoside reverse transcriptase inhibitor, NRTI, or nuke)

Standard dose: One 300 mg tablet once a day (or one 150 mg tablet twice daily), with no food restrictions (may be taken with or without food). Dose is lowered for people with kidney impairment and in children, to 4 mg/kg/day (a kilogram equals 2.2 pounds). A strawberry/banana-flavored liquid is also available. Take missed dose as soon as possible, but do not double up on your next dose.

AWP: $424.98 / month for 300 mg, $113.34 / month for 240 ml bottle

Manufacturer contact: GlaxoSmithKline,
www.treathiv.com, 1 (888) 825-5249

AIDSInfo:
1 (800) HIV-0440 (448-0440), www.aidsinfo.nih.gov

Potential side effects and toxicity: This remains one of the most easily tolerated HIV medications. Side effects (rarely seen) may include headache, nausea, vomiting, diarrhea, fever, fatigue, hair loss, insomnia, malaise (general ill feeling), nasal symptoms, cough, peripheral neuropathy, low white blood cells, and anemia.

Rare but potentially fatal toxicity with all NRTIs: hepatomegaly with steatosis (enlarged, fatty liver) and lactic acidosis (accumulation of lactate in the blood and abnormal acid-base balance). Lactic acidosis has been seen in patients taking NRTIs, but is more common and more severe in women, people who are obese, and people who have been taking NRTIs for a long time; it is more common in people with liver disease, but can occur in people without a history of liver damage. People with lactic acidosis may experience persistent fatigue, abdominal pain or distension, nausea/vomiting, difficulty breathing or shortness of breath, and enlarged, fatty liver. Pancreatitis (inflammation of the pancreas) can be life-threatening and may cause pain in the stomach and back, along with nausea, vomiting, and bleeding. Children should be watched for signs of pancreatitis.

Potential drug interactions: No significant drug interactions. Do not take Epzicom, Combivir, Trizivir, Truvada, Atripla, or Epivir-HBV while taking Epivir, since they contain Epivir or medication equivalent to Epivir.

Tips: Exciting benefit: drug resistance that the virus develops against Epivir -- the M184V mutation -- makes the virus less fit to replicate and has even been shown to keep T-cells from dropping during a treatment interruption as much as they would have otherwise. It is also approved for treatment of hepatitis B virus (HBV), under the brand name Epivir-HBV. So if you have hepatitis B and HIV, this drug works for both diseases, but make sure you are taking Epivir at HIV doses -- always ask your doctor or pharmacist. Worsening of hepatitis B (HBV) in people co-infected with HIV/HBV has occurred when Epivir was discontinued. These patients should be closely monitored by their physician. Epivir is also available combined with Retrovir (zidovudine, AZT), called Combivir (one tablet twice a day), in a once daily formula with Ziagen (Epzicom, one tablet daily), and in a triple combination with both Retrovir and Ziagen (Trizivir, one tablet twice a day). Please see package insert for more complete potential side effects and interactions.

Doctor

Epivir (lamivudine, known to most as 3TC) was first synthesized in 1989 by a Canadian biochemical firm that licensed the drug to GSK (Glaxo at the time) for a share of sales. 3TC was approved by the FDA in 1995 for twice-daily dosing and again in 2002 for once-daily dosing. Epivir is also approved for hepatitis B infection and is a component of the fixed dose combinations Combivir, Trizivir, and Epzicom. This antiretroviral agent, or its close "relative" emtricitabine [Emtriva], forms the nucleoside backbone for virtually all HAART regimens used in our clinic. We have found 3TC to be the best tolerated of all the antiretroviral agents. This does not mean there are no adverse events associated with 3TC use. On occasion we have seen bone marrow toxicity (anemia and low white cells), and have also diagnosed pancreatitis (reported with use of 3TC) in one of our patients on the drug. In Ugandan children, pancreatitis is seen with a little more frequency. Because of the tolerability of Epivir, I have found it easy to forget that it must be dose adjusted in individuals who have reduced kidney function. Failure to dose adjust 3TC may lead to increased levels of the drug in the blood and an increase in adverse events. Resistance to 3TC can occur rapidly (that's the bad part). The 3TC signature M184V mutation, however, may improve the antivretroviral activity of AZT and tenofovir and the mutated virus is less able to produce more copies of itself (that's the good part). Tolerability of 3TC and the resistance benefits makes it a key component of any HAART regimen. It's the best damn drug in town! -- Frank M. Graziano, M.D., Ph.D.

Activist

Almost the Energizer Bunny of ARVs, Epivir just keeps going and going. It is contained in Combivir, Trizivir, and Epzicom; can be taken as a single nuke with a PI (usually boosted with ritonavir [Norvir]) or NNRTI-containing regimen; and, is FDA-approved to treat hepatitis B. HIV tends to develop resistance to Epivir quickly (the M184V gene mutation), but even that turns out to be a good thing. This specific gene mutation weakens HIV "viral fitness," rendering HIV less able to make copies of itself. Thus Epivir remains effective in a back-handed sort of way, which accounts for why it is still so widely used. -- Morris Jackson

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