Efavirenz
| Clinical data | |
|---|---|
| Pronunciation | /ɪˈfævɪrɛnz/ i-FAV-i-renz or /ˌɛfəˈvaɪrɛnz/ EF-ə-VY-renz |
| Trade names | Sustiva, Stocrin, others |
| Other names | EFV |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a699004 |
| License data | |
| Pregnancy category |
|
| Routes of administration | By mouth (capsules, tablets) |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| 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 | Single-dose: 52–76 h Multi-dose: 40–55 h |
| Excretion | Kidney (14–34%) and feces (16–61%) |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| NIAID ChemDB | |
| PDB ligand | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.149.346 |
| Chemical and physical data | |
| Formula | C14H9ClF3NO2 |
| Molar mass | 315.68 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| (verify) | |
Efavirenz (EFV), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention after a needlestick injury or other potential exposure. It is sold both by itself and in combination as efavirenz/emtricitabine/tenofovir. It is taken by mouth.
Common side effects include rash, nausea, headache, feeling tired, and trouble sleeping. Some of the rashes may be serious such as Stevens–Johnson syndrome. Other serious side effects include depression, thoughts of suicide, liver problems, and seizures. It is not safe for use during pregnancy. It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and works by blocking the function of reverse transcriptase.
Efavirenz was approved for medical use in the United States in 1998, and in the European Union in 1999. It is on the World Health Organization's List of Essential Medicines. As of 2016, it is available as a generic medication.