Ténofovir disoproxil comprimés treatment HIV-1 and hepatitis B (30 tablets)

Dosage form Box of 30 tablets
Specifications Tenofovir disoproxil fumarate

Ingredient

Composition information	Content
Tenofovir disoproxil fumarate	300mg

Uses

indications

Tenofovir disoproxil fumarate 300mg is indicated in the following cases:

HIV-1: Tenofovir is indicated in combination with other antiviral drugs to treat HIV-1 infection in the disease from 18 years of age.

The effectiveness of Tenofovir is based on the results of studies for patients who have never been treated before, including patients with a large number of viruses (> 100,000 copies/ ml) and studies in them. Tenofovir is used to supplement the basic treatment (mainly 3 -drug combination therapy) for patients who had previously had anti -Retrovirus drugs but failed (

Choose Tenofovir to treat patients who had previously treated anti -Retrovirus drugs must be based on viral sensitivity test results and/or patient treatment history.

Hepatitis B: Tenofovir is indicated for the treatment of chronic hepatitis B in adults with compensation liver function, with evidence of the actual activity of the virus, the concentration of alanine aminotrasferasem (ALT) continuously increases and the histological evidence of active inflammation and/or fibrosis or treatment of chronic hepatitis B in adults with liver disease.

Pharmacology

Tenofovir disoproxil fumarate is the form of Fumarate salt of the pre -substance of Tenofovir disoproxil. Tenofovir Disoproxil is absorbed and transformed into the active ingredient Tenofovir, which is a nucleoside monophosphate (nucleotide). Under the catalyst of enzymes in cells through two phosphorylation reactions in both non -functioning T cells and have been activated Tenofovir into active metabolites, Tenofovir Diphosphate.

Tenofovir Diphosphate has a half -life period of about 10 hours in activated cells and about 50 hours in cells that do not work for peripheral single blood nuclear cells (PBMC). Tenofovir diphosphate inhibits the polymerase of the virus by competing directly on the natural deoxyribonucleotide, and ends the DNA chain after combining DNA.

Tenofovir diphosphate is a weak inhibitor of internal polymerase α, β, and,, with dynamic inhibitor constant (K1) for human polymerase α DNA (5.2 μmol/l) larger> 200 times and for polymers β and human DNA (equivalent are 81.7 and 59.9 μmol/l) For HIV-1 reverse copy enzymes (0.02 μmol/). In Viro printing quantities, at high concentrations up to 300 μmol/l, Tenofovir cannot perform any effect on the synthesis of the mitochondrial DNA or the production of lactic acid production.

Dynamic pharmacokinetics

Tenofovir disoproxil fumarate is a pre -ester -soluble substance in water and in the body quickly converted into tenofovir and formaldehyde.

In cells, Tenofovir is converted into Tenofovir Monophosphate and into Tinhofovir Diphosphate active substance.

absorption:

After giving HIV -infected patients with Tenofovir Disoproxil Fumarate, Tenofovir Disoproxil Fumarate is quickly absorbed and converted into Tenofovir. The maximum serum tenofovir concentrations within 1 hour after drinking and 2 hours after drinking with food. Tenofovir's oral bioavailability from Tenofovir Disoproxil Fumarate in patients with hunger is about 25%.

Taking Tenofovir Disoproxil Fumarate with a high -fat meal that affects the oral bioavailability of the drug, of which Tenofovir's AUC increases by about 40% and CMAX increases by about 14%. However, taking Tenofovir Disoproxil Fumarate 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 to be about 800 ml/kg. After taking Tenofovir Disoproxil Fumarate, Tenofovir is distributed mainly in tissues, with the highest concentration in the kidneys, liver and intestinal tract (according to preclinical studies). In test tube, 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.

Biological shift:

In vitro studies have determined that both Tenofovir Disoproxil Fumarate and Tenofovir are not metabolized through the CYP450 enzyme system.

Era:

Tenofovir is excreted mainly through the kidneys by both dialysis and through the active transportation system in the renal tubules with about 70-80% of the intravenous dosage is excreted in the urine in a constant form.

The total clearance is estimated at 230ml/hour/kg (about 300 ml/minute).

The renal clearance is estimated at about 160ml/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 Ténofovir disoproxil comprimés treatment HIV-1 and hepatitis B (30 tablets)

How to use

Tenofovir disoproxil fumarate 300mg orally.

Therapy should be set by an experienced doctor in the treatment of HIV -infected patients.

In case of unable to swallow the drug, Tenofovir can be used in the form of dissolving tablets in at least 100 ml of water, orange juice or pressed grapes.

Dosage

Adults:

The recommended dose for HIV treatment or chronic hepatitis B treatment is taking 300 mg (1 tablet) 1 time/day with meals.

Children:

Tenofovir is not recommended for children under 18 years of age due to lack of data on safety and efficiency for this object.

Old people:

There are no data on dosage for elderly patients over 65 years old.

Patients with renal failure:

Tenofovir is excreted through the kidneys and increases tenofovir accumulation when patients with renal failure. The dose distance should be adjusted for patients with creatinine clearance

The adjustment of the dose for patients with renal impairment is based on limited data and may not be the most optimal. The safety and effectiveness of these dose adjustment guidelines have not been clinically evaluated. Therefore, clinical response to the treatment and kidney function should be closely monitored in patients with renal failure:

Creatinine clearance (ml/minute)*

30 - 49 10 - 29

Every 48 hours

Each 72-96 hours

Every 7 days after the end of the hemorrhage **

** In general, the dosage 1 time/week in the case of hemolytic refinement 3 times/week, each time about 4 hours or after a total of 12 hours of hemorrhage.

There is no suggestion for patients without hematoma with creatinine clearance

Patients with liver failure:

No dose adjustment requires patients with liver failure.

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 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 you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

When using Tenofovir Disoproxil Fumarate 300mg, you may experience unwanted effects (ADR).

Surveying adultery reactions related to treatment (at least may be related) are 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, 1/10 000,

Metabolic and nutrition disorders:

Very common: reducing blood phosphate.

Rare: Lactic acid infection.

Very common: dizziness.

Very rare: Difficulty breathing.

Gastrointestinal disorders

Very common: diarrhea, nausea, vomiting.

common: flatulence.

Rare: Pancreatitis.

Unknown: muscle disease, bone puree (both related to close tubing).

rare: renal failure, acute renal failure, renal disease in the near -coal tube (including fanconi syndrome), increased creatinine.

Very rare: acute renal necrosis.

There are after -sales reports of nephritis and diabetes that cause kidneys.

Very rare: weakness.

Retrovirus combined regimens often accompanied by metabolic disorders such as hyperglyceride blood, blood cholesterol, insulin resistance, blood glucose and hyperlorm blood.

Retrovirus combined regimens are often accompanied by a body fat redistribution (fat dysplasia syndrome) in HIV patients including peripheral fat and subcutaneous fat, increased visceral and abdominal fat, chest hypertrophy and accumulation of back neck fat (tumor).

In patients with HIV infected with severe immunodeficiency at the time of using the anti -retovirus (Cart), inflammatory reaction with or no symptoms with opportunistic pathogens may appear.

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

contraindicated

Tenofovir disoproxil fumarate 300mg contraindicated in the following cases:

Patients with hypersensitivity to Tenofovir or Tenofovir Disoproxil Fumarate.

Be cautious when used

Do not use Tenofovir tablets simultaneously with any other drug containing Tenofovir Disoproxil Fumarate.

Tenofovir Disoproxil Fumarate has not been studied in patients under 18.

Tenofovir is except mainly through the kidneys. Tenofovir concentration in the body may increase significantly in patients with medium or severe renal impairment (Creatinine clearance

It is necessary to carefully control signs of poisoning, such as impaired renal function, and changes in virus concentrations in patients with renal failure before, when the distance is started between the dose of Tenofovir Disoproxil Fumarate.

Safety and effectiveness of Tenofovir Disoproxil Fumarate in patients with renal failure has not been established.

Excessive kidney failure, including cases accompanied by a decrease in blood phosphate, when using Tenofovir Disoproxil Fumarate.

Monitoring the kidney function (clearine and serum creatinine) should be monitored) when using Tenofovir Disoproxil Fumarate, 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.

Effects on bones: Consult your doctor if you suspect bone abnormalities.

Avoid using Tenofovir Disoproxil Fumarate for patients tending to carry the K65R gene mutation when treating Retrovirus resistance.

Tenofovir disoproxil fumarate 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 Fumarate.

Patients with hepatitis B or C and treated with Retrovirus anti -Retrovirus therapy are at high risk of serious liver side effects and may cause death. In case of treatment for hepatitis B or C by combining Retrovirus resistance, it is advisable to refer to the relevant product information of these drugs.

Lactic acid infection: There have been cases of lactic acid infection, often accompanied by fatty liver, when using nucleoside homologous substances. Propertical and clinical data suggests that the risk of lactic acid contamination, is the side effect of the group of nucleoside homosexuals, for Tenofovir Disoproxil Fumarate is low. However, because Tenofovir has a nucleoside homogeneous structure, this risk cannot be excluded.

Immune recovery syndrome: HIV -infected patients with serious immunodeficiency, at the beginning of treatment with antiviral drugs (Cart), inflammatory reaction may occur for opportunistic or asymptomatic causes, and cause serious clinical conditions, or exacerbate existing symptoms. Special. Such reactions have been observed for a few weeks or the first month of treatment.

Examples of these reactions are cytomegalovirus retinal inflammation, wide and//or localized mycobacterium infections, and pneumoeystis carinii pneumonia. Any symptoms of inflammation must be evaluated and treated if necessary.

Bone necrosis: Despite the multi -factor (including the use of corticosteroids, the destruction of alcohol, severe immune system weakening, high body mass index), cases of bone necrosis have been specially reported in progressive HIV patients and/or treatment for long -term Retroviral resistance (Cart). Patients are advised to check medical examination if there are signs of joint pain, stiffness or difficulty moving.

The ability to drive and operate machinery

Tenofovir Disoproxil Fumarat tablets can cause dizziness. Patients should not drive or operate machinery if dizzy when using Tenofovir Disoproxil Fumarat tablets.

Pregnancy

There is no clinical data on the status of Tenofovir Disoproxil Fumarate exposure during pregnancy. However, people do not know the potential risk for the development of a human fetus, so when using Tenofovir Disoproxil Fumarate for women of childbearing age, they must always combine effective contraceptive measures.

The period of breastfeeding

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 is being treated with Tenofovir Disoproxil Fñimarate should not be breastfeeding.

According to the general principle, it is recommended that women who are HIV -infected with breastfeeding should not be breastfeeding to avoid transmitting HIV to their babies.

Drug interaction

Use the combination of Tenofovir Disoproxil Fumarate and Didanosine, increasing 40-60% of the didanosine body exposure concentration, which can lead to an increased risk of side effects related to Didanosine. Pancreatitis and lactic acidic cases have appeared but rare, sometimes fatal.

Didanosine dose decreased (250mg) has been tried to avoid didanosine exposure too high when combined with Tenofovir Disoproxil Fumarate, but there is a report on high rate of failure in antiviral treatment and appears resistance at an early stage with several combined formulas. Therefore, it is not recommended to combine Tenofovir Disoproxil Fumarate with Didanosine, especially in patients with high viral levels and low number of CD4 cells. If required to combine, careful supervision of patients on the effectiveness of treatment and adultery reactions related to Didanosine.

The combination treatment regimen of 3 nueleoside drugs: There are reports on high rate of failure in the antivirus and appear anti -drug strains at the early stage when Tenofovir Disoproxil Fumarate is combined with Lamivudine and Abacavir as well as combined with Lamivudine and Didanosine in the regimen once a day.

It is recommended that patients that anti -Retrovirus drugs, including Tenofovir disoproxil fumarate, can not prevent the risk of HIV spread through sex or viral blood. Need to continue using other preventive measures.

Storage

Store in the original packaging in a dry, cool place below 30 ° C. Avoid light.

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