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Lamivudine

 
Dental Dictionary: lamivudine
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n
3TC

trade name: Epivir; drug class: antiviral, nucleoside analog; action: inhibition of HIV reverse transcriptase; also inhibits RNA- and DNA-dependent DNA polymerase; use: in combination with zidovudine for the treatment of HIV infection.

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Drug Info: Abacavir; Lamivudine, 3TC
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Brand names: Epzicom™

Chemical formula:



Abacavir Sulfate, Lamivudine Oral tablet

What is this medicine?

ABACAVIR; LAMIVUDINE, 3TC (a ba KA vir; la MI vyoo deen) is two antiretroviral medicines in one tablet. It is used with other medicines to treat HIV. This medicine is not a cure for HIV. It will not stop the spread of HIV to others.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•kidney disease
•liver disease
•an unusual or allergic reaction to abacavir, lamivudine, 3TC, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. You may take this medicine with or without food. Take your medicine at regular intervals. Do not take your medicine more often than directed. For your anti-HIV therapy to work as well as possible, take each dose exactly as prescribed. Do not skip doses or stop your medicine even if you feel better. Skipping doses may make the HIV virus resistant to this medicine and other medicines. Do not stop taking except on your doctor's advice.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

This does not apply.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•alcohol or alcohol containing products
•any medicine that contains emtricitabine
•zalcitabine, ddC

This medicine may also interact with the following medications:
•any other medicine that contains abacavir or lamivudine
•interferon
•methadone
•nelfinavir
•ribavirin
•sulfamethoxazole; trimethoprim, SMX-TMP

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular check ups. Discuss any new symptoms with your doctor. You will need to have important blood work done while on this medicine.

HIV is spread to others through sexual or blood contact. Talk to your doctor about how to stop the spread of HIV.

If you have hepatitis B and HIV, talk to your doctor if you plan to stop this medicine. The symptoms of hepatitis B may get worse if you stop this medicine.

A small number of people may have a severe allergy to this medicine. Some symptoms are a skin rash, fever, nausea, vomiting, stomach pain, severe tiredness, aches, or generally feeling sick. A list of these symptoms is on the Warning Card given to you by your pharmacist. You should carry this Warning Card with you. If you have these symptoms while taking this medicine, stop the medicine and call your doctor right away.

If you stop this medicine because you ran out of medicine or because you may have had an allergic reaction, talk to your doctor. Do not restart this medicine without your doctor's advice. Severe hypersensitivity reactions can occur within hours and may include life-threatening hypotension and death.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing difficulties, cough
•depressed mood
•fever, chills, sore throat, infection
•muscle pain or weakness
•nausea, vomiting, unusual stomach upset or pain
•pain, tingling, numbness in the hands or feet
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•unexplained weight loss
•unusually weak or tired
•yellowing of the skin or eyes

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•headache
•diarrhea
•difficulty sleeping
•dizziness
•loss of appetite
•runny, stuffy nose
•trouble sleeping
•weight gain around waist, back, or thinning of face, arms, legs

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 9/1/2004 2:57:00 PM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Wikipedia: Lamivudine
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Lamivudine
Systematic (IUPAC) name
4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1,2-dihydropyrimidin-2-one
Identifiers
CAS number 134678-17-4
ATC code J05AF05
PubChem 60825
DrugBank APRD00681
Chemical data
Formula C8H11N3O3S 
Mol. mass 229.26 g/mol
SMILES eMolecules & PubChem
Synonyms L-2',3'-dideoxy-3'-thiacytidine
Pharmacokinetic data
Bioavailability 86%
Protein binding Less than 36%
Metabolism  ?
Half life 5 to 7 hours
Excretion Renal (circa 70%)
Therapeutic considerations
Pregnancy cat.

B3(AU) C(US)
Legal status

POM(UK) ℞-only(US)
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Lamivudine (2',3'-dideoxy-3'-thiacytidine, commonly called 3TC) is a potent nucleoside analog reverse transcriptase inhibitor (nRTI).

It is marketed by GlaxoSmithKline with the brand names Zeffix, Heptovir, Epivir, and Epivir-HBV.

Lamivudine has been used for treatment of chronic hepatitis B at a lower dose than for treatment of HIV. It improves the seroconversion of e-antigen positive hepatitis B and also improves histology staging of the liver. Long term use of lamivudine unfortunately leads to emergence of a resistant hepatitis B virus (YMDD) mutant. Despite this, lamivudine is still used widely as it is well tolerated.

Contents

History

Lamivudine was invented by Bernard Belleau while at work at McGill University and Nghe Nguyen-Ga at the Montreal-based IAF BioChem International, Inc. laboratories in 1989. Initially designed as an antiviral agent, the drug's effectiveness for treating HIV in combination with AZT was discovered by Yung-Chi (Tommy) Cheng at Yale University. The drug was later licensed to the British pharmaceutical company Glaxo for a 14 percent royalty.

Lamivudine was approved by the Food and Drug Administration (FDA) on November 17, 1995 for use with zidovudine (AZT) and again in 2002 as a once-a-day dosed medication. The fifth antiretroviral drug on the market, it was the last NRTI for three years while the approval process switched to protease inhibitors. According to the manufacturer's 2004 annual report, its patent will expire in the United States in 2010 and in Europe in 2011.

Mechanism of action

Lamivudine is an analogue of cytidine. It can inhibit both types (1 and 2) of HIV reverse transcriptase and also the reverse transcriptase of hepatitis B. It needs to be phosphorylated to its triphosphate form before it is active. 3TC-triphosphate also inhibits cellular DNA polymerase.

Lamivudine is administered orally, and it is rapidly absorbed with a bio-availability of over 80%. Some research suggests that lamivudine can cross the blood-brain barrier. Lamivudine is often given in combination with zidovudine, with which it is highly synergistic. Lamivudine treatment has been shown to restore zidovudine sensitivity of previously resistant HIV. Several mutagenicity tests show that lamivudine should not show mutagenic activity in therapeutic doses.

Physical interaction with Tenofovir DF

Lamivudine shows brownish coloration with tenofovir disoproxil fumarate, reason behind this is still unknown.

Resistance

See also: resistance mutation

In HIV, high level resistance is associated with the M184V/I mutation in the reverse transcriptase gene. GlaxoSmithKline claimed that the M184V mutation reduces "viral fitness", because of the finding that continued lamivudine treatment causes the HIV viral load to rebound but at a much lower level, and that withdrawal of lamivudine results in a higher viral load rebound with rapid loss of the M184V mutation; GSK therefore argued that there may be benefit in continuing lamivudine treatment even in the presence of high level resistance, because the resistant virus is "less fit". The COLATE study has suggested that there is no benefit to continuing lamivudine treatment in patients with lamivudine resistance.[1] A better explanation of the data is that lamivudine continues to have a partial anti-viral effect even in the presence of the M184V mutation.

In hepatitis B, lamivudine resistance was first described in the YMDD locus of the HBV reverse transcriptase gene. The HBV reverse transcriptase gene is 344 amino acids long and occupies codons 349 to 692 on the viral genome. The most commonly encountered resistance mutations are M204V/I/S. The change in amino acid sequence from YMDD to YIDD results in a 3.2 fold reduction in the error rate of the reverste transcriptase, which correlates with a significant growth disadvantage of the virus. Other resistance mutations are L80V/I, V173L and L180M.[2]

Dosing

For adults with HIV (or children over 12), the dose is 300mg once daily, or 150mg twice a day. Lamivudine is never used on its own in the treatment of HIV.

For the treatment of adults with hepatitis B, the dose is 100mg once daily. If co-infected with HIV, then the dose is as for HIV.

For a child 3 months to 12 years old, about 1.4-2 mg per lb. of body weight twice a day, no more than 150 mg per dose.

Overdosage

Little is known about the effects of overdosage with lamivudine.

Presentation

Epivir logo
  • Epivir 150 mg or 300 mg tablets (GlaxoSmithKline; US and UK) for the treatment of HIV;
  • Epivir-HBV 100 mg tablets (GlaxoSmithKline; US only) for the treatment of hepatitis B;
  • Zeffix 100 mg tablets (GlaxoSmithKline; UK only) for the treatment of hepatitis B.

Lamivudine is also available in fixed combinations with other HIV drugs:

References

  1. ^ Fox Z, Dragsted UB, Gerstoft J, et al. (2006). "A randomized trial to evaluate continuation versus discontinuation of lamivudine in individuals failing a lamivudine-containing regimen: The COLATE trial". Antiviral Therapy 11: 761–70. PMID 17310820. 
  2. ^ Koziel MJ, Peters MG (2007). "Viral hepatitis in HIV infection". N Engl J Med 356 (14): 1445–54. doi:10.1056/NEJMra065142. 

External links


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This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 

 

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