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Abacavir
Abacavir (ABC) is a nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. It is available under the trade name Ziagen™ (GlaxoSmithKline} 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, rarely, fatal. Genetic testing can indicate whether an individual will be hypersensitive; over 90% of patients can safely take abacavir. Additional recommended knowledgeViral strains that are resistant to zidovudine (AZT) or lamivudine (3TC) are generally sensitive to abacavir, whereas strains that are resistant to AZT and 3TC are not as sensitive to abacavir.
HistoryAbacavir 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 will expire in the United States on 2009-12-26. IndicationAbacavir 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. Mechanism of actionABC is an analog of guanosine (a purine). Its target is the viral reverse transcriptase enzyme. PharmacokineticsAbacavir is given orally and has a high bioavailability (83%). It is metabolised primarily through alcohol dehydrogenase or gluconyl transferase. It is capable of crossing the blood-brain barrier. Adverse reactionsFatal 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*5701[1][2] for which testing is now available in most western countries. There is a strong relationship with race: the prevalence of HLA-B*5701 in India is 20–50%, but is 0% in Japan; the prevalence is 5–7% in western Europe. Screening for the HLA-B*5701 has been convincingly shown to reduce the incidence of abacavir hypersensitivity reactions.[3][4] Cautions and WarningsStop taking this drug at the first sign of drug allergy or sensitivity. People have died from abacavir sensitivity. People with liver disease should be cautious about using this drug because of the possibility that it can aggravate the condition. Some people have died from liver damage associated with abacavir. The use of nucleoside drugs such as abacavir can very rarely cause lactic acidosis, a fatal metabolic disturbance. Resistance to abacavir has developed in laboratort versions of HIV also resistant to lamivudine, didanosine and zalcitabine. HIV that is resistant to protease inhibitors is not likely to be resistant to abacavir. Redistribution or accumulation of body fat may occur in people taking antiviral medications including: central obesity; facial arm, leg, and/ or buttock wasting; breast enlargement; and fat accumulation at the base of the neck (buffalo hump). Abacavir cannot be used in infants under age 3 months. Food InteractionsNone known Usual DoseAdult (age 17 and over) :300mg 2 times a day Child (age 3 months - 16 years) 3.6mg per lb. of body weight twice a day, up to a maximun of 300mg in each dose. OverdosageLittle is known about the effects of abacavir overdose. Overdose victims should be taken to a hospital emergency room for treatment. ALWAYS brings the prescription bottle or container. References
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Abacavir". A list of authors is available in Wikipedia. |