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- What is efavirenz, and how does it work (mechanism of action)?
- What brand names are available for efavirenz?
- Is efavirenz available as a generic drug?
- Do I need a prescription 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 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 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.
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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).
Reference: FDA Prescribing Information
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Efavirenz (Sustiva) is a drug prescribed to treat infections with the human immunodeficiency virus (HIV). Side effects, drug interactions, warnings and precautions, and pregnancy safety should be reviewed prior to taking this drug.
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Lamivudine (3tc) (Epivir; Epivir HBV) is a drug prescribed for the treatment of HIV infection and hepatitis B infection. The most serious side include
- muscle pain,
- liver failure,
- pancreatitis, and
- liver failure.
Drug interactions, and dosage, and pregnancy and breastfeeding safety information should be reviewed prior to taking this medication.
lamivudine and zidovudine
Combivir (lamivudine and zidovudine) is a drug that is used in combination with other agents to treat HIV infection. Serious side effects include:
- Fatty liver
- Liver enlargement
- Lactic acidosis.
Drug interactions, and dosage, and pregnancy and breastfeeding information should be reviewed prior to taking this medication.
nevirapinenevirapine (Viramune, Viramune XR) is a drug used in conjunction with other anti-HIV drugs for the treatment of HIV infection. Side effects, drug interactions, pregnancy safety, and warnings and precautions should be reviewed prior to taking this medication.
stavudineStavudine (Zerit) is a medication prescribed for the treatment of HIV infection. Zerit is prescribed to be used in combination with other anti-HIV infection drugs. Side effects, drug interactions, dosage, and pregnancy safety should be reviewed prior to taking this medication.
Retrovir (zidovudine, ZDV, formerly called AZT) is a medication (oral and injectable) prescribed for the treatment of infections with HIV (human immunodeficiency virus). Side effects include:
- Weight loss
Drug interactions, dosage, and pregnancy and breastfeeding safety information, and dosing should be reviewed before taking any medication.