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- What is efavirenz, and how does it work (mechanism of action)?
- What are the uses for efavirenz?
- What are the side effects of efavirenz?
- What is the dosage for efavirenz?
- Which drugs or supplements interact with efavirenz?
- Is efavirenz safe to take if I'm pregnant or breastfeeding?
- What else should I know about efavirenz?
What is efavirenz, and how does it work (mechanism of action)?
Efavirenz is an oral medication that is used for the treatment of infections associated with the human immunodeficiency virus (HIV). Efavirenz is in a class of drugs called reverse transcriptase inhibitors, which also includes zalcitabine (Hivid), zidovudine (Retrovir), didanosine (Videx), and lamivudine (Epivir). It is in a subclass of reverse transcriptase inhibitors referred to as non-nucleoside reverse transcriptase inhibitors that includes nevirapine (Viramune), and delavirdine (Rescriptor). During infection with HIV, the HIV virus multiplies within the body's cells. The newly-formed viruses then are released from the cells and spread throughout the body where they infect other cells. In this manner, the infection continually spreads to new, uninfected cells that the body is continually producing, and HIV infection is perpetuated. When producing new viruses, the HIV virus must manufacture new DNA for each virus. Reverse transcriptase is the enzyme that the virus uses to form new DNA. Efavirenz directly inhibits the activity of reverse transcriptase and blocks the production of DNA and new viruses. Efavirenz does not kill existing HIV virus and it is not a cure for HIV. Efavirenz was approved by the FDA in 1998.
What brand names are available for efavirenz?
Is efavirenz available as a generic drug?
GENERIC AVAILABLE: No
Do I need a prescription for efavirenz?
What are the side effects of efavirenz?
The most common side effects of efavirenz are:
Other side effects include
- muscle pain (myalgia),
- abnormal heartbeats,
- liver failure,
- increased cholesterol
- increased triglyceride levels.
- abnormal dreams,
- hallucinations, and
- difficulty concentrating.
Serious psychiatric adverse effects such as depression, suicidal thoughts, manic reactions, and aggressive behavior have been reported in patients taking efavirenz. Immune reconstitution syndrome which is an inflammatory response to infection may occur in patients treated with combination antiretroviral therapy.
What is the dosage for efavirenz?
The recommended dose for adults is 600 mg daily. Efavirenz must be administered in combination with other anti-HIV drugs because the HIV virus quickly becomes resistant to treatment when efavirenz is used alone. Efavirenz should be administered on an empty stomach to improve absorption, preferably at bedtime.
Which drugs or supplements interact with efavirenz?
Efavirenz has many drug interactions because many drugs affect its breakdown and elimination by the liver. Efavirenz also affects the breakdown of other drugs by the liver. The following are some examples of drugs that interact with efavirenz.
Triazolam (Halcion), midazolam (Versed), bepridil (Vascor), pimozide (Orap), and ergot derivatives (for example, ergotamine, dihydroergotamine) should not be combined with efavirenz because efavirenz increases blood levels of these drugs, potentially causing serious adverse effects. St. John's wort should not be combined with efavirenze because it reduces blood levels of efavirenz, leading to possible loss of effectiveness.
Efavirenz increases the concentration of ritonavir (Norvir) while Ritonavir increases the concentration of efavirenz. Increased drug concentrations may result in more frequent or more serious side effects.
Is efavirenz safe to take if I'm pregnant or breastfeeding?
It is not known whether efavirenz is excreted in human breast milk. HIV-infected mothers should not breastfeed because of the risk of transmitting HIV to an infant that is not infected.
What else should I know about efavirenz?
What preparations of efavirenz are available?
Capsules: 50 and 200 mg. Tablet: 600 mg.
How should I keep efavirenz stored?
Efavirenz should be stored at room temperature, 15 C to 30 C (59 F to 86 F).
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Efavirenz (Sustiva) is a drug prescribed to treat infections associated with the human immunodeficiency virus (HIV). Review side effects, dosage, drug interactions, warnings and precautions, and pregnancy safety information prior to taking this drug.
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Related Disease Conditions
AIDS (Acquired Immunodeficiency Syndrome)
AIDS is the advanced stage of HIV infection. Symptoms and signs of AIDS include pneumonia due to Pneumocystis jiroveci, tuberculosis, toxoplasmosis, seizures, weakness, meningitis, yeast infection of the esophagus, and Kaposi's sarcoma. Anti-retroviral therapy (HAART) is used in the treatment of AIDS.
Human Immunodeficiency Virus (HIV)
HIV (human immunodeficiency virus) infection left untreated causes AIDS (acquired immunodeficiency syndrome). Still incurable, AIDS describes immune system collapse that opens the way for opportunistic infections and cancers to kill the patient. Early symptoms and signs of HIV infection include flu-like symptoms and fungal infections, but some people may not show any symptoms for years. Highly active antiretroviral therapy (ART) is the standard treatment for HIV infection. These combination drug regimens have made HIV much less deadly, but a cure or vaccine for the pandemic remains out of reach. HIV is usually transmitted through sexual contact or sharing IV drug needles, but can also infect someone through contact with infected blood. Sexual abstinence, safe sex practices, quitting IV drugs (or at least using clean needles), and proper safety equipment by clinicians and first responders can drastically reduce transmission rates for HIV/AIDS.
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