Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Sustiva
Active ingredient: Efavirenz
Available dosage forms: 200, 500, 600 mg
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Efavirenz general information
Several years ago, efavirenz wasn’t recommended when pregnant. Appropriate studies performed to date never have demonstrated geriatric-specific issues that would confine the usefulness of efavirenz within the elderly. Consequently, efavirenz really should not be administered while pregnant. Efavirenz-based therapy might be an option following the very first trimester of pregnancy.
Liver problems might occur while you’re using this medicine. Whether this condition occurs, your personal doctor may provide you with a medicine to reduce the cholesterol and fats. This medicine might raise the degree of cholesterol and fats inside your blood. The results of some tests might be affected via this medicine.
A lot of women initiated efavirenz following the very first trimester of pregnancy. All early pregnancy losses within our study occurred within the initial 3 months following the date of the final reported menstrual period. Don’t give during pregnancy as a result of risk of fetal malformations. 1 woman started EFV to the end of the leading trimester.
Call your own doctor straight away if you or your own child have some strange feelings, thoughts, or behaviors. Tell your physician straight away if you or your own child notice any changes inside your health. For instance, if you or your own child are taking one dose daily, attempt to take it at precisely the same time every day. Please keep this in your mind, and be certain to visit different parts of our site for much more recent details!
Whenever you’re taking this medicine, it is particularly important your healthcare professional know if you’re taking any one of the medicines given below. Utilizing this medicine with any of these medicines may cause an elevated risk of certain unwanted side effects, but using both drugs might be the optimal/optimally treatment for you. In such cases, your own doctor may want to alter the dose, or alternative precautions might be necessary. Utilizing this medicine with any of these medicines is not advisable.
Eight patients within the efavirenz group and one patient within the efavirenz-free group committed suicide. The goal of the present study was supposed to compare time to suicidality with each sort of therapy. Long-term utilization of efavirenz within this study wasn’t associated with any new safety concerns. There isn’t any significant upsurge in danger of NTDs with EFV exposure.
If you really need help planning the top times to take your own medicine, check with your own doctor. Don’t take different medicines unless they’ve been discussed with your physician. Tell your physician if you or your own child get any skin rash, even just a mild rash. Keep taking efavirenz for the entire time of cure, even if you start to feel better.
Indications For curing HIV-1 infection in adults. The existence of other medical problems might affect the use of the medicine. It should be taken with several other HIV medicines. It works by lowering the quantity of HIV within the blood. This information includes only the typical doses of the medicine. This medicine has a patient information insert.
If you believe you have become pregnant when using the medicine, tell your physician without delay. Employing this medicine as long as you’re pregnant can harm your unborn baby. The aggregate of medicine you take is based on the strength of the medicine. At times the immune system will begin to fight infections which were hidden within your body, like pneumonia, herpes, or tuberculosis. In the event your dose differs, don’t change it unless your own doctor directs you to achieve that. Don’t let yourself run out of this medicine.
Instructions for use
The active substance (INN) Efavirenz (Efavirenz)
Application: HIV-1 infection (combination therapy).
Contraindications Efavirenz (Efavirenz) (-): Hypersensitivity.
Restrictions apply: can not be administered concurrently with terfenadine, astemizole, cisapride, midazolam, or triazolam and ergot alkaloids (competition efavirenz for CYP3A4 may result in inhibition of metabolism of these drugs and create the possibility of causing serious and / or life-threatening adverse events including cardiac arrhythmias, prolongation of sedation or respiratory depression).
Pregnancy and lactation: Pregnancy should be avoided in women receiving efavirenz (in experiments on primates Efavirenz crosses the placenta and is teratogenic). Before starting treatment, women of childbearing age should be tested for pregnancy and during treatment always use barrier methods of contraception in conjunction with other methods (eg, oral or other hormonal contraceptives).
In the case of pregnancy, the use of efavirenz is allowed only in cases when the potential benefit justifies the potential risk to the fetus (adequate and well-controlled studies in pregnant women has not been)
Breastfeeding is not recommended -. the potential risk of transmission and, although it is not known whether efavirenz with milk in humans is released , of possible serious side effects of efavirenz in infants. Studies in rats have shown that efavirenz excreted with the milk.
Side effects: Efavirenz has been studied in more than 2,000 patients and is usually in clinical trials was well tolerated. In controlled clinical trials, in the subgroup of 413 patients who received 600 mg / day of efavirenz in combination with protease inhibitors and / or nucleoside reverse transcriptase inhibitors, the most frequently reported adverse events of at least moderate severity, associated with treatment were:
From the nervous system and sensory organs: dizziness (9.2%), headache (6.3%), insomnia (6.1%), fatigue (5.6%), decreased concentration (5,3%).
in a controlled clinical trial in which efavirenz (600 mg) was administered in conjunction with other anti-retroviral drugs, neurological symptoms of moderate to severe degree of intensity were observed in 22.8% of patients compared to 10.1% in the control group. Severe neurological symptoms were observed in 2.9% of patients receiving efavirenz (600 mg / d), and 1.3% of patients in the control group, 2.7% of patients in connection with the treatment of neurological symptoms were reversed. These symptoms usually occur within the first 1-2 days of treatment and usually go through 2-4 weeks.
Reported serious psychiatric side effects in patients receiving efavirenz. In controlled trials, the frequency of severe psychiatric symptoms in patients treated with efavirenz, and in the control group were respectively: severe depression – 1.6 and 0.6%, suicidal ideation – 0.6 and 0.3%, non-fatal suicide attempts – 0, 4 and 0%, aggressive behavior – 0.4 and 0.3%, paranoid reactions – 0.4 and 0.3%, manic reaction – 0.1% and 0. In addition, with a frequency of more than 2% in patients treated with efavirenz, and in the control group met Depression – 15.8 and 13.1%, anxiety – 11.1 and 7.6%, nervousness – 6.3 and 2% .
From the digestive tract: nausea (10.4%), diarrhea (6.8%), rarely – indigestion, abdominal pain
From the skin. covers: rash (in the form of light or moderate maculopapular skin eruptions that appear within the first 2 weeks after initiation of treatment, most patients rash held with continued treatment for 1 month, in clinical trials on patients treated at 600 mg of efavirenz, severe rash occurred in 0.7% of patients, 1.7% due to rash treatment was canceled); erythema multiforme and Stevens – Johnson (0.14% among more than 2000 patients).
Interactions: With simultaneous use of efavirenz, are inducers of CYP3A4 in vivo . may decrease in the plasma concentration of other compounds that are substrates for CYP3A4.
Reduced AUC and Cmax of indinavir (IDV dose of 800 mg every 8 hours) at about 31 and 16%, respectively (in this regard, indinavir dose increases from 800 to 1000 mg every 8 hours, with dosage adjustment is not required efavirenz; indinavir to 1200 mg administered every 12 hours, only a limited number of patients)
Combined use of ritonavir (ritonavir – 500 mg every 12 hours, efavirenz – 1 600 mg. once daily at bedtime) in uninfected volunteers, poorly tolerated and resulted in an increase in the frequency of adverse clinical events (eg dizziness, nausea, paraesthesia) and laboratory abnormalities (elevated liver enzymes).
Reduced Cmax and AUC of saquinavir (1200 mg 3 times per day in the form of soft jelly) at 45-50 and 62% respectively.
Simultaneous reception efavirenz (1 400 mg once a day) and clarithromycin (500 mg every 12 hours) for 7 days resulted in a significant change in pharmacokinetics of clarithromycin: Cmax and AUC clarithromycin decreased by 26 and 39% respectively, and the AUC and Cmax of clarithromycin gidroksimetabolita increased by 49 and 34%, respectively. The clinical significance of these changes has not been established. Among uninfected volunteers 46% when receiving efavirenz and clarithromycin rash. In the appointment of efavirenz with clarithromycin dose adjustment of efavirenz is not required. alternative to the use of clarithromycin should be considered.
Efavirenz increases AUC of ethinyl estradiol by 37% (study only ethinylestradiol component of oral contraceptives), significant changes in Cmax of ethinyl estradiol has been noted. The clinical significance of these effects is not known. The effects of a single dose of ethinyl estradiol on the Cmax or AUC of efavirenz was observed.
Do not bind to cannabinoid receptors. In non-infected patients treated with efavirenz, marked false positive results of the analysis of urine for cannabinoids (only when using the test CEDIA DAU Multi – Level THC, which is used for screening, but tests are used to confirm positive results)
The simultaneous use. drugs metabolized mainly isozymes 2C9, 2C19 and 3A4 may lead to changes in plasma concentrations of co-administered drugs. In this regard, and may require appropriate adjustment of the dose of these drugs.
Drugs inducing activity of CYP3A4 (eg phenobarbital, rifampicin, rifabutin, etc.), Can increase the clearance of efavirenz that lowers the plasma concentration.
decreased Cmax and AUC of rifabutin (300 mg, efavirenz – 600 mg / day for 14 days) at 32 and 38%, respectively
Increased AUC and Cmax nelfinavir (NFV -. 750 mg every 8 hours, efavirenz – 600 mg during 7 days) by about 21 and 20%.
Rifamycin (600 mg / day for 7 days) reduced Cmax and AUC efavirenz (600 mg / d) for 20 and 26%, respectively.
it may increase or decrease the plasma concentration and the effects of warfarin.
In a joint application with itraconazole and ketoconazole may reduce the plasma concentration of them.
Hypericum perforatum (St. John’s wort) or preparations containing it can significantly reduce the plasma levels of efavirenz (joint use is not recommended).
Overdose: has been reported on the strengthening of neurological symptoms in patients with accidental administration of a dose of 600 mg 2 times a day. One patient observed involuntary muscle contractions
Treatment:. general supportive measures, including monitoring of vital signs and observation of the clinical condition of the patient. You can use activated carbon to remove the acceleration does not absorb the drug. A specific antidote is not known. The effectiveness of dialysis is unlikely (efavirenz actively binds with proteins).
Dosing Efavirenz (Efavirenz) (-): Inside, regardless of meals, in combination with protease inhibitors and / or nucleoside reverse transcriptase inhibitors
Adults – 600 mg 1 time. per day. Teenagers (aged 17 years) and children (. Over 3 years or body weight 13 kg), the dose is prescribed according to body weight: 13-15 kg – 200 mg; 15-20 kg – 250 mg, 20-25 kg – 300 mg, 25-32,5 kg – 350 mg, 32,5-40 kg – 400 mg 1 time per day. Children weighing more than 40 kg – 600 mg 1 time per day. Efavirenz capsules prescribed only to children who are able to swallow the capsule easily.
Caution: In patients with severe rash accompanied by blistering, desquamation, mucosal involvement, or fever, you need to cancel the EFV. With the reappointment of efavirenz is recommended that the application of appropriate antihistamines and / or corticosteroids. If you cancel the EFV treatment should also consider removing all other anti-retroviral drugs to avoid the emergence of resistant viruses. After the disappearance of the symptoms of intolerance to the intake of these antiretroviral drugs should be started simultaneously. Intermittent monotherapy and sequential re-appointment of antiretroviral drugs are not recommended due to the increased probability of occurrence of the mutant viruses resistant to these drugs.
In order to improve the tolerability of side effects in the nervous system during the first 2-4 weeks of treatment, as well as patients, continuing in the future to experience these symptoms, it is recommended to take the drug before going to sleep.
in children before treatment should consider preventing rashes appropriate antihistamines.
be wary appoint patients with hepatic insufficiency (due to intensive metabolism of efavirenz, mediated by the P450 cytochrome, and the limited experience of its use in patients with chronic liver diseases).
it is recommended to maintain constant monitoring of liver enzymes in patients with known or suspected infection with hepatitis B or C in the history and in patients receiving other medications, which may have hepatotoxic effects. In the appointment of efavirenz with ritonavir is recommended to maintain constant supervision over the activity of liver enzymes.
In the case of a persistent increase in serum transaminase levels to more than 5 times the upper limit of normal, should be weighed against the benefits of continuing treatment with the unknown risks of significant hepatotoxicity.
During treatment, continuous monitoring of cholesterol levels is recommended.
Because the potential interaction of efavirenz with oral contraceptives has not been studied fully, in addition to oral contraceptives should use a reliable method of barrier contraception.
use of efavirenz in combination with saquinavir as the sole protease inhibitor is not recommended.
Patients who had a history of mental health problems are at greater risk of serious psychiatric side effects, such as manic reactions, severe depression and suicidal thoughts. In the event of serious psychiatric side effects, the patient should be examined for the presence of these effects due to the use of efavirenz, and if the connection is established, you weigh the risks and benefits of further treatment.
Special instructions: Do not use as a single agent to treat HIV or added as a single agent after failure of other means. When efavirenz monotherapy rapidly developing viral resistance. efavirenz treatment should always be started in combination with one or more new antiretroviral drugs, which the patient has not previously received. In the selection of new anti-retroviral drugs for their use in combination with efavirenz should take into account the possibility of cross-resistant viruses.
There is no evidence that the reduction or splitting the daily dose has a beneficial effect, so it is not recommended.
Patients should be informed about the possible neurological and psychiatric reactions, as well as a potential additive effect on the central nervous system when taken with alcohol or psychotropic drugs.