Efavirenz
Antiretroviral medication / From Wikipedia, the free encyclopedia
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Efavirenz (EFV), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS.[1] It is generally recommended for use with other antiretrovirals.[1] It may be used for prevention after a needlestick injury or other potential exposure.[1] It is sold both by itself and in combination as efavirenz/emtricitabine/tenofovir.[1] It is taken by mouth.[1]
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Pronunciation | /ɪˈfævɪrɛnz/ i-FAV-i-renz |
Trade names | Sustiva, Stocrin, others[1] |
AHFS/Drugs.com | Monograph |
MedlinePlus | a699004 |
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Routes of administration | By mouth (capsules, tablets) |
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Bioavailability | 40–45% (under fasting conditions) |
Protein binding | 99.5–99.75% |
Metabolism | Liver (CYP2A6 and CYP2B6-mediated) |
Onset of action | 3–5 hours |
Elimination half-life | 40–55 hours |
Excretion | Kidney (14–34%) and feces (16–61%) |
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ECHA InfoCard | 100.149.346 |
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Formula | C14H9ClF3NO2 |
Molar mass | 315.68 g·mol−1 |
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Common side effects include rash, nausea, headache, feeling tired, and trouble sleeping.[1] Some of the rashes may be serious such as Stevens–Johnson syndrome.[1] Other serious side effects include depression, thoughts of suicide, liver problems, and seizures.[1] It is not safe for use during pregnancy.[1] It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and works by blocking the function of reverse transcriptase.[1]
Efavirenz was approved for medical use in the United States in 1998,[1] and in the European Union in 1999.[4] It is on the World Health Organization's List of Essential Medicines.[5] As of 2016, it is available as a generic medication.[6][7]