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Brand Name: Epivir
Common Name: lamivudine or 3TC
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 lower for people with kidney impairment and in children and people who weigh less than 110 pounds (50 kg), 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: $347.11 / month for 300 mg
Manufacturer contact: GlaxoSmithKline,
www.treathiv.com, 1 (888) 825–5249
AIDSInfo:1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov
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| Potential side effects and toxicity: |
This remains one of the most easily tolerated HIV medications. Potential side effects/toxicities (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 is 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 nukes for a long time; and 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, and difficulty breathing or shortness of breath; and enlarged, fatty liver. Pancreatitis can be life-threatening and may cause pain in the stomach and back, along with nausea, vomiting and blood. Children should be watched for signs of pancreatitis.
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| Potential drug interactions: |
| Do not use Epivir if you are on Emtriva or Emtriva-containing product. No significant drug interactions. |
| 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. Epivir is also available combined with Retrovir (Combivir, one tablet twice-a-day), in a once-a-day formula with Ziagen (Epzicom, one tablet daily) and in a triple combination with both Retrovir and Ziagen (Trizivir, one tablet twice-a-day). |
| Doctor |
| Lamivudine (3TC) is a potent and generally well-tolerated agent that has been included in most antiretroviral regimens for the past 10 years. Its primary role in combination antiretroviral therapy is being partially eclipsed by its close cousin FTC. It can be dosed once or twice a day and is available in three fixed-dose combinations (Combivir, Epzicom, and Trizivir). A single mutation (M184V) can significantly diminish its antiviral efficacy, so use in potent combination regimens is key to preserving its effectiveness. In the setting of the M184V mutation there is still modest anti-HIV activity plus diminished fitness of the virus, as well as preserved or enhanced activity for other reverse transcriptase inhibitors (such as zidovudine) such that it is often continued even after the appearance of the M184V mutation. Since it is renally excreted, dose adjustments need to be made in the setting of significant renal failure (Cr<50 ml), which also precludes use of the fixed dose combinations. It has proven efficacy in the treatment of hepatitis B infection, but use of monotherapy (in the hepatitis B context) leads to resistance, so combination hepatitis B therapy (use of another drug such as tenofovir) is often considered in co-infected patients. —Keith Henry, MD |
| Activist |
| Epivir was the fifth drug approved to treat HIV, and is arguably one of the most steadfast in its ability to stay among the top rungs of the treatment ladder. Commonly used alone (with other ARVs) and also in GSK’s fixed dose combinations of Combivir, Epzicom and Trizivir, Epivir keeps hanging in there over the years. Although it has its drawbacks (from such potential side effects as hair loss and a quickly developing mutation called M184V), it can be a strong building block for a treatment regimen containing a PI or an NNRTI. The one interesting thing about Epivir’s signature mutation M184V is that it appears to make the virus less fit (i.e., reduces its ability to replicate effectively). The ramifications (potentially good) have not been completely fleshed out, but many docs will keep their salvage patients on this drug, even when they show resistance, just to gain the benefit that it might bring. Epivir is also used to treat chronic hepatitis B.—Cathy Olufs |
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