EVASIF V-245mg Santa treat chronic hepatitis B (30 tablets)
Dosage form 30 capsules
Specifications Tenofovir disoproxil
Ingredient
| Composition information | Content |
| Tenofovir disoproxil | 245mg |
Uses
Indications
Evasif 245mg drugs are indicated in the following case:
Evasif 245mg is indicated in combination with antacids of Retrovirus in the treatment of HIV -1 in adults over 18 years old.
Pharmacy
Mechanism of action
Tenofovir disoproxil fumarat is the form of Fumarat salt of the precursor of Tenofovir Disoproxil. Tenofovir Disoproxil is absorbed and transformed into the active ingredient Tenofovir, which is a nucleosid monophosphate (nucleotid). Under the catalyst of enzymes in cells through two phosphorylation reactions in both non -functioning T lymphocytes and have been activated Tenofovir into active metabolites, Tenofovir Diphosphate.
Tenofovir Diphosphate has a half -time -life that is about 10 hours in activated cells and about 50 hours in non -activated cells for peripheral single blood nuclei cells (PBMC). Tenofovir diphosphate inhibits the virus's polymerase enzyme by directly competing into the natural substrate deoxyribonucleotid and ends the DNA chain after combining DNA.
Tenofovir diphosphate is a weak inhibitor of internal polymerase polymerases α, β, and γ with dynamic inhibitor constant (ki) for polymerase α DNA (5.2 µmol/l) larger> 200 times and for polymers β and γ DNA human (corresponding to 81.7 and 59.9 µmol/l) It is for HIV reverse copy enzymes - 1 (0.02 µmol/l).
In Vitro quantitators, at high concentrations up to 300 µmol/l, Tenofovir does not show any effect on the synthesis of the DNA of the mitochondria or the lactic acid production process.
Pharmacological effects
Tenofovir has antiviral activity in vitro for retovirus and hepadnavirus.
In the concentration of twice the IC50 for wild strains, Tenofovir still maintains the activity against HIV - 1 recombinant with mutations that cause resistance to Didanosin (L74V), with Zalcitabin (T69D), and multiple nucleosid (Q151M complex).
Tenofovir activity in HIV -1 strains carrying mutations related to zidovudin seems to depend on the form and quantity of these mutations. When there is a mutation T215Y, the IC50 concentration has doubled. Of the 10 samples with diverse mutations related to zidovudin (average 3.4), the concentration of 1C50 increased by 3.7 times (about 0.8 to 8.4).
HIV - 1 resistance to many nucleosides carrying 2 mutations T69S has reduced sensitivity to Tenofovir (IC50> 10 times). Tenofovir shows the full activity against HIV strains - 1 resistance to reverse copy enzyme inhibitors that are not nucleosid, which carries K103N or Y181C mutations. Diagonal resistance to mutations that cause protease inhibitors are difficult because the enzymes of the virus have different targets.
It is selected in the test tube of HIV -1 strains of the Tenofovir sensitivity reduced from 3 to 4 times and the K65R mutation in the enzyme copied backwards. K65R mutations can also be selective for zalcitabin, didanosin, abacavir and lamivudin, and reduce sensitivity to zalcitabin, didanosin, abacavir and lamivudin (respectively 14, 4, 3 and 25 times).
Do not use Tenofovir Disoproxil Fumarat for patients who have treated Retrovirus resistant to virus infections with K65R mutations.
pharmacokinetics
tenofovir disoproxil fumarat is an ester -soluble precursor in water and in the body quickly transformed into tenofovir and formaldehyde.
In cells, Tenofovir is converted into Tenofovir Monophosphate and into Tinhofovir Diphosphate active substance.The pharmacokinetics of Tenofovir does not depend on the dose of Tenofovir Disoproxil Fumarat in the dose range from 75 to 600mg and is not affected when the dose is repeated at any dose.
absorption
After giving HIV -infected patients with Tenofovir Disoproxil Fumarat, Tenofovir Disoproxil Fumarat is quickly absorbed and transformed into Tenofovir. When taken at meals, Tenofovir Disoproxil Fumarat doses for the average value of Tenofovir concentration (%CV) CMAX, AUC0 - ∞ and cmin are 326 (36.6%) ng/ml, 3,324 (41.2%) ng.He/ml and 64.4 (39.4%) ng/mL.
Maximum serum tenofovir concentrations within 1 hour after drinking and 2 hours after drinking with food. Tenofovir's oral bioavailability from Tenofovir Disoproxil Fumarat in patients with hunger is about 25%. Take Tenofovir Disoproxil Fumarat with a high -fat meal that affects the oral bioavailability of the drug, of which Tenofovir's AUC increases by 40% and CMAX increases by about 14%.
When the patient is taken for the dose of Tenofovir Disoproxil Fumarat first at the time of eating, the average CMAX value in the average serum is between 213 to 375 ng/ ml. However, taking Tenofovir Disoproxil Fumarat and a snack does not significantly affect the pharmacokinetics of Tenofovir.
Distribution
After intravenous transmission, the distribution volume in the stable state of Tenofovir is estimated at 800 ml/kg. After taking Tenofovir Disoproxil Fumarat, Tenofovir is distributed mainly in tissues, with the highest concentration in the kidneys, liver and intestinal tract (according to preclinical studies). In test tubes, the level of cohesion with plasma or serum protein is below 0.7 and 7.2%, with Tenofovir concentration ranging from 0.01 to 25 µg/ml.
Metabolism
In vitro studies have determined that both Tenofovir Disoproxil Fumarat and Tenofovir are not metabolized through the CYP450 enzyme system. Moreover, at significantly higher concentrations (about 300 times) compared to clinical concentrations, Tenofovir does not inhibit the metabolism of the test tube but the catalyst is the main CYP450 isomers related to the biological shift of drugs in humans (CYP3A4, CYP2D6, CYP2C9, CYP2E1 or CYP1A1/2).
At 100 µg/ml concentration, Tenofovir Disoproxil Fumarat does not affect any type of CYP450, except for CYP1A1/2, which has a slight decrease (6%) but has statistical significance of metabolism of CYP1A1/2. Based on these figures, it is not possible to appear significant interactive clinical interactions between Tenofovir Disoproxil Fumarat and metabolic drugs thanks to the CYP450 system.
Elimination
Tenofovir is excreted mainly through the kidneys by both dialysis and via active transportation systems in the renal tubules with about 70-80% of intravenous doses excreted in urine in a constant form. The total clearance is estimated at 230 ml/hour/kg (about 300 ml/minute).
The renal clearance is estimated at about 160 ml/hour/kg (about 210 ml/minute), much higher than the filtration rate in the glomerular. This indicates that the active excretion through the renal tubules plays an important role in the elimination of Tenofovir. Tenofovir waste sale time after drinking is about 12 - 18 hours.
Before taking EVASIF V-245mg Santa treat chronic hepatitis B (30 tablets)
Should start treatment with a doctor with experience in treating hepatitis B or HIV virus.
How to use
take medicine after eating. In case the patient is difficult to swallow the pill, it can dissolve with at least 100 ml of filtered water, orange juice or grape juice and drink.
Dosage
Adults
recommended dose is 1 tablet/time/day.
kidney failure
Tenofovir is eliminated through the kidneys and the exposure concentration of Tenofovir increases in patients with impaired renal function. The clinical data has shown that one tablet of Tenofovir Disoproxil Fumarat daily for patients with mild renal impairment (creatinine clearance 50 - 80 ml/min). In case the patient has a creatinine clearance
The recommendations of the distance between 2 drug use based on data are limited and may not be optimal. The safety and effectiveness of the recommendations to adjust the distance between the drug use has not been clinically evaluated. Therefore, it is necessary to closely monitor clinical response to the treatment and kidney function in these patients.
Creatinine clearance (ml/minute)*
Patients with dialysis
30 - 49
10 - 29
Every 24 hours
Every 48 hours
Every 72 to 96 hours
After the end of the hemorrhage **, take one tablet per week.
** Usually once a week, assuming it is 3 times a week of separation with a period of about 4 hours for each time of separation, or after the total appraisal time is 12 hours.
There is no recommendation of dosage for patients who are not allowed to separate creatinine
What to do when using overdose?
Tenofovir can be removed by the hemorrhage, the average clearance of hematoma of Tenofovir is 134 ml/minute. Tenofovir's clearance by the abdominal separation has not been determined.
What to do when forgetting 1 dose? If the patient forgets 1 dose of Evasif 245mg after more than 12 hours and is nearly until the next dose, the patient should not use the forgotten dose and just use the next dose as usual.
If the patient vomits within 1 hour after taking EVASIF 245mg, one more tablet should be taken. If the patient vomits after more than 1 hour using EVASIF 245mg, they do not need to take another dose.
Side Effects
When using EVASIF 245mg, you may experience unwanted effects (ADR).
The suspected side effects are related to the treatment listed below by the system of organs in the body and frequency. The defined frequency is very common (> 1/10), common (> 1/100, 1/1000, 1/10000,
For HIV treatment - 1
Đánh giá về tác dụng phụ được dựa trên kinh nghiệm sử dụng thuốc sau khi đưa ra thị trường và trong hai nghiên cứu trên 653 bệnh nhân đã điều trị kháng retrovirus từ trước đang dừng tenofovir disoproxil fumarat (n = 443) hoặc placebo (n = 210) trong phác đồ kết hợp với các thuốc kháng retrovirus khác trong 24 tuần, và một nghiên cứu mù đôi có đối chứng so sánh trên 600 bệnh nhân sử dụng thuốc kháng Retrovirus was first treated with Tenofovir Disoproxil 245mg (in the form of fumarat) (n = 299) or Stavudin (n = 301) in combination with lamivudin and efavirenz for 144 weeks.
About one -third of patients are considered to have adverse effects during the treatment with Tenofovir Disoproxil Fumarat in combination with other antacids. These reactions are usually mild to medium gastrointestinal symptoms.
neurological disorders
Gastrointestinal disorders
Retrovirus combined regimens often accompanied by metabolic disorders such as hypereminemia, hypercholesteroline blood cholesterol, insulin resistance, hyperlem of blood glucose and hyperlorm blood. Retrovirus combined regimens often accompanied by the state of body fat redistribution (fat dysplasia syndrome) in HIV patients including: reducing peripheral fat and under face skin, increasing internal and abdominal fat, chest hypertrophy and accumulation of back fat (buffalo hunchback). In patients with HIV infected with severe immunodeficiency at the time of using the anti -Retrovirus (Cart) combination regimen, inflammatory reactions with or without symptoms with opportunistic pathogens may appear. In particular, in patients infected with HIV or treatment in combination with Retrovirus resistance, the risk of bone necrosis has been reported. For the treatment of hepatitis B virus Evaluation of side effects is based on the experience of using the drug after being marketed and in two studies on 641 patients with chronic hepatitis B or cirrhosis also use Tenofovir Disoproxil Fumarat 245mg (n = 426) per day or drink Adefovir Dipivoxil 10mg (n = 215) every day for 48 weeks. Gastrointestinal disorders immune system disorders Metabolic and nutrition disorders Respiratory, chest and medium disorders Gastrointestinal disease Very rare: stomach pain. Liver disorders Very rare: hepatitis. Disorders in the skin and under the skin Musculoskeletal and connective muscle disorders Renal - urinary disorders Very rare: acute renal necrosis. There are after -sales reports of nephritis and diabetes with kidney causes. Common disorders and condition at the place of use
Warnings
This drug is only used by a doctor.
Do not use overdue drugs indicated on the packaging.
Do not use the prescribed overdose.
Read the user manual carefully before use.
Notify the doctor with unwanted effects when using the drug.
If you need more information, please consult a doctor.
Contraindicated
Contraindicated in patients with hypersensitivity to Tenofovir or with any component of the drug.
Be cautious when used
Do not use Evasif tablets simultaneously with any other drug containing Tenofovir Disoproxil Fumarat.
Tenofovir disoproxil fumarat is not used in combination with adefovir.
Tenofovir disoproxil fumarat has not been studied in patients under 18 years old.
Effects on the kidneys
Tenofovir is excreted mainly through the kidneys. Tenofovir concentration in the body can increase significantly in patients with medium or severe renal impairment (Creatinin clearance
Therefore, it is necessary to adjust the distance between two medications with all patients with creatinine clearance Safety and effectiveness of tenofovir disoproxil fumarat in patients with renal failure has not been studied.
Excessive kidney failure, including cases accompanied by blood phosphate, when using Tenofovir Disoproxil Fumarat.
Monitoring the kidney function (Creatinine clearance and serum phosphate) when using Tenofovir Disoproxil Fumarat, every 4 weeks of the first year of treatment, and then every 3 months. In patients at risk or a history of kidney failure, and patients with poor kidney function, need to consider assessing more regular kidney function.
If serum phosphate concentration Be cautious when treating the interval with Tenofovir Disoproxil Fumarat with patients with creatinine clearance to
Tenofovir disoproxil fumarat has not been evaluated in patients who are taking kidney toxic drugs (such as: aminoglycosides, amphotericin B, Foscarnet, Ganciclovir, Pentamidin, Vancomycin, Cidofovir or Interleukin-2).
Avoid using Tenofovir Disoproxil Fumarat while using or stopping new kidney toxic drugs. If it is required to combine tenofovir disoproxil fumarat with kidney toxic drugs, should check the kidney function weekly.
Tenofovir disoproxil fumarat has not been clinically evaluated in patients who are taking excreted drugs through the same kidney transport system, which is 1 -person organic anion system (Hoat1) (such as: ADefovir Dipivoxil; or Cidofovir is a kidney toxic substance).
This transportation system (Hoat1) is responsible for the excretion in the renal tubules, and in part, in the excretion of the kidneys of Tenofovir, Adefovir and Cidofovir. Therefore, pharmacokinetics of these drugs may be changed if used in combination. In healthy volunteers, the single doses of Adefovir Dipivoxil combined with Tenofovir Disoproxil Fumarat does not cause any drug interaction in pharmacokinetics.
However, it is not known that the clinical safety includes the potential effects on the kidneys of the formula that combines adefovir dipivoxil and tenofovir disoproxil fumarat. The drug should only be combined when it is really necessary, and if forced to combine, the kidney function is required.
Effects on bones
In a 144 -week control clinical study compares Tenofovir Disoproxil Fumarat with Stavudin in the formula combined with Lamivudin and Efavirenz in patients with Retrovirus anti -Retrovirus for the first time, there is a mitigation of bone density in the hip and spine in both treatment groups. At 144 weeks, the decrease in bone density in the spine and transforming bone indicators compared to the beginning of research in the Tenofovir Disoproxil Fumarat treatment group is significantly greater than that of the other group.
In this group, the reduction of bone density in the hip is also significantly greater than the other group until the 96th week. However, after 144 weeks of treatment, there is no risk of increased fractures or clinical signs of bone abnormalities. The doctor should be consulted if suspected of having bone abnormalities.
Avoid using Tenofovir Disoproxil Fumarat for patients tending to carry the K65R gene mutation when treating Retrovirus resistance.
Tenofovir disoproxil fumarat has not been studied in patients over 65 years old. Almost all elderly patients have reduced renal function; Therefore, it is necessary to be cautious when treating elderly patients with Tenofovir Disoproxil Fumarat.
Lactic acid infection
There have been cases of lactic acid infections, often accompanied by fatty liver, when using nucleosid homogeneous substances. Pre -clinical and clinical data suggests that the risk of lactic acid contamination, is the side effect of the group of nucleosid homogeneous substances, for Tenofovir Disoproxil Fumarat is low. However, because Tenofovir has a nucleosid homogeneous structure, this risk cannot be excluded.
Early signs (hyperlemia of the whole body) include mild digestive symptoms (nausea, vomiting and abdominal pain), non -specific fatigue, poor appetite, weight loss, respiratory symptoms (slow and/ or deep) or neurological symptoms (including weakness). Lactic acid infection has a high mortality rate and is accompanied by pancreatitis, liver failure or kidney failure. Lactic acid infections usually appear after a few or more months of treatment.
Should stop treatment with nucleosid homogeneous substances when there are signs of hyperlactic blood and lactic acid infection/ metabolic, hypertrophy of the liver progress, or increased liver enzymes.
Be careful when using nucleosid homogeneous substances for any patient (especially obese women) with hypertrophy, hepatitis or known risk factors for liver and fatty liver disease (including certain drugs and alcohol). Patients simultaneously infected with hepatitis C and treated with alpha interferon and ribavirin may be at risk.
Need to closely monitor patients at high risk.
combined Retrovirus anti -Retrovirus is often accompanied by body fat redistribution (fat dysplasia syndrome) in HIV patients. It is still unknown for the long -term consequences of these conditions. The knowledge of the mechanism is incomplete. There is a hypothesis that there is a connection between organ fat accumulation and protease inhibitors and fat atrophy and reverse copy enzyme inhibitors. High risk of fat dysplasia syndrome is often accompanied by personal factors such as high age, and drug -related factors such as: prolonged retrovirus resistance treatment time and accompanying metabolic disorders. Clinical examination should include evaluation of physical signs of fat redistribution. It is necessary to consider the determination of plasma lipid levels and blood glucose when hungry. Clinical monitoring should be appropriate lipid disorders.
Tenofovir has the same structure as nucleosid homogeneous substances, so it is impossible to ignore the risk of fat dysplasia syndrome. However, clinical data at 144 weeks from patients with Retrovirus anti -Retrovirus first pointed out that the risk of fat dysplasia of Tenofovir Disoproxil Fumarat is lower than Stavudin when combined with Lamivudin and Efavirenz.
It is confirmed on in vito and in vivo that: nucleosid and nucleotid homosexual substances cause mitochondrial destruction to different levels. There have been reports on mitochondrial failure in HIV -negative infants who are exposed to nucleosid homogeneous substances from the uterus and/ or after birth.
The adverse reactions are reported as hematological disorders (anemia, neutrophils), metabolic disorders (hyperlem of blood lactate, hyperlase blood lipase). These reactions are usually only temporary. There have been reports on some late -starting neurological disorders (increasing muscle tone, epilepsy, abnormal behavior).
It is not known that neurological disorders are temporary or long -term. Any child exposed from the fetus with nucleosids and nucleosid homosexuals, including negative HIV children, must be clinically monitored and tested, and should be fully checked in the possibility of mitochondrial dysfunction in case of related signs or symptoms. These findings do not affect the current national recommendation of the use of antiviral drugs for pregnant women to prevent HIV transmission.
Immune recovery syndrome
In patients with HIV infected with severe immunodeficiency, at the beginning of treatment with antiviral drugs (Cart), inflammatory reactions may appear to opportunistic or disillusioned pathogens, and cause serious clinical conditions, or worsen existing symptoms.
Especially, such reactions have been observed for a few weeks or the first month of treatment. The examples of these reactions are: cytomegalovirus retinal inflammation, wide and// or localized mycobacterium infections, and pneumocystis carinii pneumonia. Any symptoms of inflammation must be evaluated and treated if necessary.Liver disease
data on safety and effectiveness is very limited in liver transplant patients.
There is very little data on the safety and effectiveness of Tenofovir Disoproxil Fumarat in patients infected with HBV with unslaced liver disease and child - pugh - turcotte (CPT)> 9. These patients are at high risk of serious side effects on the liver or kidney. Therefore, the parameters of the liver and kidneys must be closely monitored on these patients.
Hepatitis outbreaks: Spontaneous outbreaks of chronic hepatitis B are relatively common and are characterized by a sudden increase in serum ALT. After starting treatment with antiviral drugs, serum alt can increase in some patients, in patients with liver disease, the increase in serum ALT is often not accompanied by an increased concentration of serum bilirubin or liver failure. Patients with cirrhosis may be at high risk of hepatitis, thus need to be closely monitored during treatment. Outbreaks after stopping treatment: Serious acute hepatitis has also been reported in patients who have stopped hepatitis B treatment B. Promotional outbreaks after treatment are often associated with increased HBV DNA, and most seem to be self -limited. However, serious batches, including death, have been reported. The liver function must be monitored for repeated periods with both clinical monitoring and testing for at least 6 months after the treatment of hepatitis B. If appropriate, the continued treatment of hepatitis B can be guaranteed. In patients with progressive liver disease or cirrhosis, treatment should not be stopped after serious hepatitis treatment can lead to liver failure. Liver disease outbreaks are particularly serious, and sometimes death in patients with liver disease. HIV -1 co -infection and hepatitis B: Due to the risk of HIV resistance, Tenofovir Disoproxil Fumarat should only be used as part of a suitable Retrovirus resistance regimen in HIV/ HBV co -infected patients. Patients with previous liver dysfunction, including chronic hepatitis, has an abnormal liver function increase in the combination of Retrovirus anti -Retrovirus and should be followed as a standard regimen. If there are symptoms of liver disease worsens in such patients, temporary or permanent consideration should be considered. However, it should be noted that the increase in ALT may be part of the reduction of HBV during treatment with Tenofovir (see the warning warning part of hepatitis). There are no studies of Tenofovir Disoproxil about the ability to drive and operate machinery. There is no clinical data for Tenofovir Disoproxil Fumarat exposure while pregnant. Animal studies do not indicate the direct or indirect harm of Tenofovir Disoproxil Fumarat for pregnancy, fetal development, birth or development after birth. Should only use Tenofovir Disoproxil Fumarat while pregnant if the benefits are higher than the potential risk to the fetus. However, people do not know the potential risk for the development of a human fetus, so when using Tenofovir Disoproxil Fumarat for women of reproductive age, they must always combine with effective contraception. Animal studies show that: Tenofovir is excreted in milk. It is not known whether Tenofovir will excrete in human milk or not. Therefore, it is recommended that the mother being treated with Tenofovir Disoproxil Fumarat should not breastfeed. According to the general principle, it is recommended that women with HIV and hepatitis B virus should not be breastfeeding to avoid transmission of HIV and hepatitis B virus to the baby. Metabolic drugs by liver enzymes Based on the results of in vitro research and the elimination lines of Tenofovir, the metabolism of CYP450 with other drugs that is related to Tenofovir is low. Kidney elimination drugs Tenofovir is excreted through the kidneys through 2 processes of filtering and positive excretion through Anion transport (Hoat1). When using simultaneously with other competing products eliminated through the renal tubules (for example, Cidofovir and Tenofovir disoproxil fumarat), can increase the concentration of tenofovir or medication simultaneously with it. Antivirus drugs Other interactions: Combined treatment of Tenofovir Disoproxil Fumarat with Methadon, Ribavirin, Rifampicin or with birth control pills (Norgestimat, Ethinyl Estradiol) does not cause any pharmacokinetic interactions. The ability to drive and operate machinery
Pregnancy
Breastfeeding period
Drug interaction
Storage
In closed boxes, the temperature does not exceed 30 ° C.
To be out of reach of children.
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