Efavirenz Stella 600mg medicine after HIV exposure (3 blisters x 10 tablets)
Dosage form Box of 3 blisters x 10 tablets
Specifications Efavirenz
Ingredient
| Composition information | Content |
| Efavirenz | 600mg |
Uses
Indications
Efavirenz 600 drug is indicated in the following cases:
pharmacokinetic
absorption
Efavirenz's peak in plasma (CMAX) concentration is achieved within 5 hours in normal volunteers after taking a single dose from 100 - 1600mg. The peak concentration (CMAX) and the area under the curve (AUC) increased by the dose to the dose of 1600mg. The absorption of the drug will be worse when the dose is higher than 1600mg. In people infected with HIV in a stable state, maximum concentration, minimum concentration and average AUC ratio according to the dose after daily dose of 200mg, 400mg, 600mg for several days.The time for the drug to reach the peak concentration in plasma is about 3-5 hours after each drink and the concentration of the drug in plasma reaches a stable level after 6-10 days of continuous medication. Take the only dose of Efavirenz 600mg with a meal rich in fat/energy (about 1000kcal, 500 - 600kcal from fat) increasing AUC average 28% and an average increase of cmax 79% compared to taking medicine when hungry.
Distribution
Efavirenz has a high association with plasma proteins (about 99.5 - 99.75%), mainly with albumin. In patients with HIV infection - 1 taking 1 tablet of Efavirenz 200 to 600mg once a day for at least a month, the concentration in cerebrospinal fluid changes in the range of 0.26 - 1.19% (average 0.69%) corresponding to plasma concentrations. This ratio is about 3 times higher than the amount of Efavirenz not attached to the plasma protein.
Metabolism
Efavirenz is converted mainly by CYP3A and CYP2B6 of the Cytochrom P450 system into hydroxylate metabolites, followed by the glucuronicization process of these hydroxylate metabolites. These metabolites actually have no HIV resistance - 1.
Efavirenz is an induction of CYP-450 enzymes, leading to its main metabolism. Take the dose of 200 - 400mg/day for 10 days reduces the accumulation of drugs (lower than 22 - 42%) and the final waste time is shorter than 40 - 55 hours (if the only dosage is 52 - 76 hours).
Elimination
Efavirenz has a final waste time from 52 to 76 hours after the single dose and 40 - 55 hours after the multiple dose. Research on excretion/weight balance for 1 month has been done at a dose of 400mg daily. With a daily dose, there is a radioactive isotope 14C. About 14 - 34% of radioactive substances are found in urine and 16-61% detected in feces. Most of the drugs are excreted in the urine in the form of metabolism.
Before taking Efavirenz Stella 600mg medicine after HIV exposure (3 blisters x 10 tablets)
How to use
Oral drugs.
Efavirenz 600 is recommended for hunger, preferably before going to bed.
Should take the whole tablet with water, should not break the pill.
Dosage
Adults
The recommended dose of Efavirenz 600 is 1 tablet of 600mg taken once a day, combined with protease inhibitors or enamel inhibitors that are similar to nucleosid (NRTIS).
Children
The recommended dose of Efavirenz 600 for children weighing 40kg or more is 1 tablet 600mg taken once a day. Efavirenz 600 is not suitable for children weighing under 40kg. Should use the appropriate forms for these objects.
Prevention after exposure due to occupation
Take 600mg once a day in the evening before sleeping, use in combination with 2 other antiviral drugs. Must use early within hours after exposure and use within 4 weeks.
Prevention after exposure is not caused by occupation
Take 600mg once a day in the evening before going to bed, used in combination with 2 other antiviral drugs. Must use early within 72 hours after exposure and use for 28 days.
Elderly
Efavirenz clinical studies are not enough patients aged 65 and over to determine whether their response is different from young people. In general, be careful when taking drugs for the elderly, corresponding to the rate of heart, liver, and kidney function, higher impairment, accompanying or other treatments.
kidney failure
Efavirenz's dynamic pharmacokinetics have not been studied in patients with renal failure. However,Hepatic failure
It is not recommended to use Efavirenz for patients with medium and severe liver failure (group B or C) because there is not enough data to determine the appropriate dose. Precautions when using Efavirenz for patients with mild liver failure due to excessive metabolism through CYP 450 intermediaries and inexperienced.
voriconazole
Often not prescribed with Efavirenz due to the risk of reducing voriconazole/increasing Efavirenz concentration. If you need to be used with Efavirenz, Voriconazole should be used from 200 to 400mg and used every 12 hours, Efavirenz dose should be reduced from 600 to 300mg once a day. When stopping treatment with voriconazole, it is necessary to recover the initial dose of Efavirenz.
rifampicin
If combining rifampicin with efavirenz for patients weighing 50kg or more, it is advisable to consider increasing the dose of Enfavirenz to 800mg/day.
Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.
What to do when overdose?
Some random patients taking the Efavirenz 600mg dose twice a day have been reported to increase side effects on the nervous system. A patient has not paid attention.
Overdose treatment
Extremely treatment of Efavirenz should include supporting the total status, including monitoring the patient's effectiveness and clinical condition. Drinking activated carbon can help eliminate the unattractive Efavirenz. There is no specific antidote when overdose of Efavirenz. Because Efavirenz is very much connected to protein, the hemorrhage can not remove Efavirenz from the blood.
What to do when forgetting a dose? If you have been close to the next drink, skip the forgotten dose, do not take two doses at a time.
Side Effects
When using Efavirenz 600, you may experience unwanted effects (ADR).
The most significant unexpected effects observed in patients treated with Efavirenz are:
Very common, ADR> 1/10
Common, 1/100 Neurological: Coordination and balance of cerebellum, attention disorders, dizziness, headache, drowsiness. Skin and lower tissue: itching. Uncommon, 1/1000 Rare, ADR Instructions on how to handle ADR Notify the doctor with adverse effects encountered when using the drug.
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
Contraindicated
Efavirenz 600 drug is contraindicated in the following cases:
Patients with severe liver failure (Child Pugh Group C).
Be cautious when using
rash
Light to the medium has been reported in clinical studies with Efavirenz. The appropriate antihistamine or corticosteroid drug can improve the tolerance and resolve the rash. The severe rash accompanied by blistering, peeling or ulcers was reported with a rate of less than 1% of patients treated with Efavirenz.
Diverse ratio of roses or Stevens - Johnson syndrome is about 0.1%. Efavirenz must be discontinued in patients with severe rash accompanied by blistering, peeling mucosa or fever.
Mental symptoms
Mental side effects have been reported in patients treated with Efavirenz. The risk of serious mental side effects occurs in patients with a history of mental disorders. Especially severe depression is more common in patients with a history of depression. There have been reports on severe depression, death due to suicide, hallucinations and mental disorders.
Patients should be warned that if there are symptoms such as severe depression, mental disorders or suicide intent, immediately contact the doctor to assess the possibility of symptoms whether or not to use Efavirenz, and if any, to determine whether the drug is continued to use is greater than the benefit or not.
neurological symptoms
Dizziness, insomnia, drowsiness, sleep quality and often have abnormal dreams. Neurological symptoms usually start in one to two days of treatment and usually in the first treatment, which is solved after 2-4 weeks of treatment.
epilepsy
Conference has been observed in patients using Efavirenz. Patients used in combination with anti -convulsions are often metabolized through the liver such as phenytoin, carbamazepine and phenobarbital, may require periodic concentration in plasma concentrations.
liver disease
There are several reports on liver failure reports in patients who have not had previous liver disease or known risk factors. Also consider monitoring liver enzymes for both patients without liver disease before or risk factors.
Food influence
Use Efavirenz with increased absorption and can lead to increased frequency of side effects.
recommend that Efavirenz should be hungry, preferably before going to bed.
immune activation syndrome
In HIV -infected patients with severe immunodeficiency at the time of combination of antiviral drugs (Cart), an inflammatory reaction to opportunistic or asymptomatic or remaining pathogens may arise and cause serious or serious clinical conditions. These reactions are usually observed for a few weeks or the first few months of Cart therapy.
The related inflammatory reactions are cytomegalovirus retinopathy, systemic or localized Mycobacteria infection and localized pneumonia and pneumocystis jiroveci (formerly known as Pneumocystis Carinii). Any symptoms of inflammation should be evaluated and treated when needed. Autoimmune disorders (such as Grave's disease) have also been reported in the immunosuppressant disease, however, the time of development changes more and these reactions may appear after months after the beginning of treatment.
fat and metabolic disorders
Combination therapy of antacids of Retrovirus may be related to the re -distribution of body fat in HIV -infected patients. It is not clear the long -term consequences of this impact. The mechanism of this impact is not fully known. There has been the theory of the relationship between the accumulation of organ fat, protease inhibitors, fat atrophy and nucleoside drugs inhibit the reverse copy enzyme.
Higher risk of fat dysplasia if accompanied by individual factors such as older and drug -related factors such as long -term treatment for Retrovirus and related metabolic disorders. Clinical examination should include evaluation of physical signs of fat re -distribution. Should consider lipd lipd and blood sugar when hungry. Lipid disorders should be properly treated.
bone necrosis
Despite being thought to have many causes, bone necrosis cases have been specially reported in patients with HIV -infected people who have progressed or use the long -term retrovirus resistance regimen. Patients need medical advice if there is joint pain, stiffness, and difficult movement.Special subjects
Liver disease
Efavirenz is contraindicated for patients with severe liver failure and is not recommended for patients with medium liver failure due to lack of data to determine whether to adjust the dose. Due to the widely metabolic mechanism through Efavirenz's cytochrome P450 intermediaries and limited clinical experience in patients with chronic liver disease, cautious when taking Efavirenz for patients with mild liver failure. Patients should be carefully monitored the side effects related to the dose, especially the symptoms on the nervous system. Testing should be done to evaluate liver disease in these patients in periods periodically.
The safety and effectiveness of Efavirenz has not been established in patients with significant liver disorders. Patients with chronic hepatitis B or C and treated with combination therapy for antiviral drugs will increase the risk of severe side effects and can cause death in the liver. Patients with previous liver dysfunction include chronic hepatitis that increases the abnormal frequency of liver function during the treatment of Retrovirus and patients should be monitored.If there is evidence of the worsening of liver disease or the persistent increase of transaminase in serum from 5 times or more than the upper limit of the normal concentration range, it is recommended to consider the benefits of continuing treatment with Efavirenz and potential risks due to liver toxicity in the liver. In these patients, disruption or stop treatment. In patients treated with toxic drugs on the liver, the monitoring of liver enzymes is also recommended. In the case of simultaneous use of antiviral hepatitis B or C antiviral therapy, it is necessary to consult the relevant information of these drugs.
kidney failure
Efavirenz pharmacokinetics has not been studied for patients with renal impairment, however, only less than 1% of Efavirenz dose is excreted in the form of unchanged urine, so the effect of kidney failure on Efavirenz elimination is very small. There is no experience in taking drugs in patients with severe renal impairment and should closely monitor safety in these patients.
Older people
Do not have enough older patients who are assessed in clinical studies to determine whether or not the difference is compared to young patients.
Children
The rash was reported on 26 children out of 57 (46%) treated with Efavirenz for 48 weeks and 3 children had a heavy rash. Preventive treatment should be considered for anti -histamine suitable for children before starting treatment with Efavirenz.
lactose
This drug contains lactose. Patients with rare genetic diseases are galactose intolerance, lactase deficiency, or glucose - galactose should not be used.
The ability to drive and operate machinery
Efavirenz can cause dizziness, concentration or drowsiness. Patients should avoid dangerous jobs such as driving and operating machinery if they experience these symptoms.
Pregnancy
There are 07 recovery reports on neuromable duct defects, including meningeal hernia, all mothers using Efavirenz treatment regimen (excluding combined tablets with a dose of Efavirenz) in the first 3 months of pregnancy. There are two more cases (1 case of rescue and 1 rescue shift) including events of neural tube defects that have been reported to the fixed -dose combination pills containing Efavirenz, Emtricitabin, and Tenofovir Disoproxil Fumarat.
The cause of the cause - the results between these events and the use of Efavirenz have not been established. Because the neural tube defects appear within the first 4 weeks in the fetal development process (the time when the neural tubes are closed), this risk is only related to women who use Efavirenz during the first 3 months of pregnancy.
Salvation reports on 904 pregnant women were treated with an efavirenz regimen in the first 3 months of pregnancy, resulting in 766 cases of living. A child is reported to have neuromuscular defects, and frequency and other types of defects at birth are similar to the group observed on children who are exposed to the Efavirenz -free treatment regimen, as well as the negative verification team with HIV. The rate of neural tube defects in the general population from 0.5 - 1 shift on 1,000 cases.
Details have been observed in the fetus of monkeys treated with Efavirenz.
Breastfeeding period
According to current recommendations, HIV -infected women should not breastfeed to avoid infection from mother to child. Mouse studies have shown that Efavirenz excreted milk. Mothers should stop breastfeeding.
Drug interaction
Efavirenz contact may increase when used with some drugs (such as ritonavir) or food (such as grapefruit juice) that inhibits the activity of CYP3A4 or CYP2B6. Herbal compounds or preparations (such as Ginkgo Biloba and St.-John’s Wort extract) induce these enzymes that can reduce the plasma concentrations of Efavirenz. Contraindicated to use Efavirenz with St. John’s World. Unable to simultaneously use Efavirenz with Ginkgo Biloba extract.
Children
Research on drug interaction is only done in adults.
Contraindications to simultaneously
Efavirenz is not used simultaneously with Terfenadin, Astemizol, Cisaprid, Midazolam, Triazolam, Pimozid, Beepridil or Alkaloid Mushroom Chicken (such as Ergotamin, Dihydroergotamin, Ergonovin, and MethylergoVin), due to the inhibition of these drugs that can lead to threats to serious events network.
st. John's Wort (Hypericum Perforatum)
Contrain to use Efavirenz and St. John's Wort or herbal preparation contains St. John's Wort. Efavirenz's plasma concentrations may be reduced when used simultaneously with St. John's Wort is due to the induction of drug metabolic enzymes or shipping proteins of ST. John's Wort.
If the patient is taking St. John's Wort, stopped using St. John's Wort, checking the virus concentration and Efavirenz levels if possible. Efavirenz concentration may increase when stopping St. John's Wort and may have to adjust the dose of Efavirenz. The touch impact of St. John's Wort can last for at least 2 weeks after treatment.
Storage
at temperatures below 30 ° C. Avoid direct light and wet place.
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