Abacavir
Drug Info:
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Abacavir
Brand names: Ziagen™
Chemical formula:
- Drug Forms:
- Abacavir Sulfate Oral solution (below)
- Abacavir Sulfate Oral tablet
Abacavir Sulfate Oral solution
What is this medicine?
ABACAVIR (a ba KA vir) is an antiretroviral medicine. 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:
•liver disease
•an unusual or allergic reaction to abacavir, 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. Use a specially marked spoon or dropper to measure each dose. Ask your pharmacist if you do not have one. Household spoons are not accurate. 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. While this drug may be prescribed for children as young as 3 months old for selected conditions, precautions do apply.
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 may interact with this medicine?
Do not take this medicine with any of the following medications:
•alcohol or alcohol containing products
This medicine may also interact with the following medications:
•any other medicine that contains abacavir
•methadone
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.
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 problems, cough
•diarrhea
•fever or chills, sore throat
•nausea, vomiting, unusual stomach upset or pain
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•unexplained weight loss
•unusually weak or tired
•weight gain around waist, back, or thinning of face, arms, legs
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•headache
•loss of appetite
•trouble sleeping
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 20 and 25 degrees C (68 and 77 degrees F). Do not freeze. May be refrigerated. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
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.
Oxford A-Z of Medicinal Drugs:
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abacavir
An antiretroviral drug (see antiviral drugs) that prevents retrovirus replication: it is a nucleoside analogue that inhibits the action of reverse transcriptase. Abacavir is used, in combination with other antiretroviral drugs, to treat HIV infection. It is available as tablets or an oral solution on prescription only.
Side effects:
include allergic reactions (e.g. rash, fever, sore throat, breathlessness, cough; see Precautions below), fatigue, abdominal pain, vomiting, liver damage, headache, dizziness, and blood disorders.
Precautions:
abacavir should be used with caution in people with chronic hepatitis B or C or impaired liver or kidney function, and in people at high risk of cardiovascular diseases. It should not be taken by women who are breastfeeding. There is a risk of allergic reactions in some people taking abacavir; treatment should be stopped if symptoms develop.
Interactions with other drugs:
Tipranavir reduces the plasma concentration of abacavir, and the two drugs are best not taken together.
Proprietary preparations:
Ziagen; Kivexa (combined with lamivudine); Trizivir (combined with lamivudine and zidovudine).
| Azarga, Aveeno, Avandamet | |
| abatacept, abciximab, acamprosate calcium |
Wikipedia on Answers.com:
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Abacavir
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| Chemical structure of abacavir | |
| Systematic (IUPAC) name | |
| {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]cyclopent-2-en-1-yl}methanol | |
| Clinical data | |
| Trade names | Ziagen |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a699012 |
| Pregnancy cat. | B3 (AU) C (US) |
| Legal status | POM (UK) |
| Routes | Oral (solution or tablets) |
| Pharmacokinetic data | |
| Bioavailability | 83% |
| Metabolism | Hepatic |
| Half-life | 1.54 ± 0.63 h |
| Excretion | Renal (1.2% abacavir, 30% 5'-carboxylic acid metabolite, 36% 5'-glucuronide metabolite, 15% unidentified minor metabolites). Fecal (16%) |
| Identifiers | |
| CAS number | 136470-78-5  |
| ATC code | J05AF06 |
| PubChem | CID 441300 |
| DrugBank | DB01048 |
| ChemSpider | 390063 |
| UNII | WR2TIP26VS |
| KEGG | D07057 |
| ChEBI | CHEBI:421707 |
| ChEMBL | CHEMBL1380 |
| NIAID ChemDB | 028596 |
| Chemical data | |
| Formula | C14H18N6O |
| Mol. mass | 286.332 g/mol |
| SMILES | eMolecules & PubChem |
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Abacavir (ABC) English pronunciation: /ʌ.bæk.ʌ.vɪər/ (
listen) is a nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. It is available under the trade name Ziagen (ViiV Healthcare) and in the combination formulations Trizivir (abacavir, zidovudine and lamivudine) and Kivexa/Epzicom(abacavir and lamivudine) . It has been well tolerated: the main side effect is hypersensitivity, which can be severe, and in rare cases, fatal. Genetic testing can indicate whether an individual will be hypersensitive; over 90% of patients can safely take abacavir. However, in a separate study, the risk of heart attack increased by nearly 90%.[1]
Viral strains that are resistant to zidovudine (AZT) or lamivudine (3TC) are generally sensitive to abacavir, whereas some strains that are resistant to AZT and 3TC are not as sensitive to abacavir.
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Contents
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Clinical indications
Abacavir tablets and oral solution, in combination with other antiretroviral agents, are indicated for the treatment of HIV-1 infection.
Abacavir should always be used in combination with other antiretroviral agents. Abacavir should not be added as a single agent when antiretroviral regimens are changed due to loss of virologic response.
Side effects
Fatal hypersensitivity reactions have been associated with therapy with abacavir. Symptoms of hypersensitivity include fever, skin rash, fatigue, gastrointestinal symptoms such as nausea, vomiting, diarrhea or abdominal pain and respiratory symptoms such as pharyngitis, dyspnea, or cough.
Hypersensitivity is strongly associated with HLA-B*57:01[2][3][4] for which testing is now available in most western countries. There is a strong relationship with race: the prevalence of HLA-B*57:01 in some Indian ethnic groups is up to 10%, but is 0% in Japan; the prevalence is 5–7% in western Europe. Screening for the HLA-B*57:01 has been convincingly shown to reduce the incidence of abacavir hypersensitivity reactions[5][6] Abacavir binds specificially to the peptide-binding groove of HLA-B*57:01 and thereby alters the spectrum of peptides that bind to this molecule. This in turn leads to aberrant CD8 T-cell responses to self antigens which probably explain the side effect.[7]
A new FDA alert concerning abacavir and abacavir containing medications was issued on July 24, 2008. FDA informed that based on data from two studies they support a recommendation for pre-therapy screening for the presence of the HLA-B*57:01 allele and the selection of alternative therapy in positive subjects. Genetic tests for HLA-B*57:01 are available and all patients should be screened for the HLA-B*57:01 allele before starting or restarting treatment with abacavir or abacavir containing medications. Development of clinically suspected abacavir HSR requires immediate and permanent discontinuation of abacavir therapy in all patients, including patients negative for HLA-B*57:01.[8]On March 1, 2011 the FDA updated the public about an ongoing safety review of abacavir and a possible increased risk of heart attack.[9]
Warnings
Patients with liver disease should be cautious about using abacavir because of the possibility that it can aggravate the condition.
The use of nucleoside drugs such as abacavir can very rarely cause lactic acidosis.
Resistance to abacavir has developed in laboratory versions of HIV which are also resistant to other HIV-specific antiretrovirals such as lamivudine, didanosine and zalcitabine. HIV strains that are resistant to protease inhibitors are not likely to be resistant to abacavir.
Redistribution or accumulation of body fat, lipodystrophy, may occur in people taking antiviral medications giving rise to central obesity, facial, arm, leg, and/ or buttock wasting, breast enlargement, and fat accumulation at the base of the neck (buffalo hump).
Abacavir is contraindicated for use in infants under 3 months of age.
Food interactions
None known
Overdosage
Little is known about the effects of Abacavir overdose. Overdose victims should be taken to a hospital emergency room for treatment and always bring the prescription bottle or container.
Mechanism of action
ABC is an analog of guanosine (a purine). Its target is the viral reverse transcriptase enzyme.
Pharmacokinetics
Abacavir is given orally and has a high bioavailability (83%). It is metabolised primarily through alcohol dehydrogenase or glucuronyl transferase. It is capable of crossing the blood–brain barrier.
History
Abacavir was approved by the Food and Drug Administration (FDA) on December 18, 1998 and is thus the fifteenth approved antiretroviral drug in the United States. Its patent expired in the United States on 2009-12-26.
References
- ^ SFGate.com
- ^ Mallal S, Phillips E, Carosi G et al (February 2008). "HLA-B*5701 screening for hypersensitivity to abacavir". N. Engl. J. Med. 358 (6): 568–79. doi:10.1056/NEJMoa0706135. PMID 18256392. http://content.nejm.org/cgi/pmidlookup?view=short&pmid=18256392&promo=ONFLNS19.
- ^ Mallal S, Nolan D, Witt C et al (2002). "Association between the presence of HLA-B*5701, HLA-DR7 and HLA-DQ3 and hypersensitivity to HIV-1 reverse transcriptase inhibitor abacavir". Lancet 359 (9308): 727–32. doi:10.1016/S0140-6736(02)07873-X. PMID 11888582.
- ^ Hetherington S, Hughes AR, Mosteller M et al (2002). "Genetic variations in HLA-B region and hypersensitivity reactions to abacavir". Lancet 359 (9312): 1121–2. doi:10.1016/S0140-6736(02)08158-8. PMID 11943262.
- ^ Rauch A, Nolan D, Martin A et al (2006). "Prospective genetic screening decreases the incidence of abacavir hypersensitivity reactions in the Western Australian HIV cohort study". Clin Infect Dis 43 (1): 99–102. doi:10.1086/504874. PMID 16758424..
- ^ Zucman D, de Truchis P, Majerholc C et al (2007). "Prospective Screening for Human Leukocyte Antigen-B*5701 Avoids Abacavir Hypersensitivity Reaction in the Ethnically Mixed French HIV Population". J Acquir Immune Defic Syndr 45 (1): 1–3. doi:10.1097/QAI.0b013e318046ea31. PMID 17356469.
- ^ Illing PT et al. 2012, Nature, doi:10.1038/nature11147
- ^ http://www.fda.gov/cder/drug/InfoSheets/HCP/abacavirHCP.htm FDA abacavir alert web access July 29, 2008.
- ^ http://www.drugs.com/fda/abacavir-ongoing-safety-review-possible-increased-risk-heart-attack-12914.html.
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