Tenifo Atra drugs treat HIV-1 infection, hepatitis B (1 blister x 10 tablets)

Dosage form Box of 1 blister x 10 tablets
Specifications Tenofovir disoproxil fumarat

Ingredient

Composition information	Content
Tenofovir disoproxil fumarat	300mg

Uses

Indications

Tenifo drug are indicated in the following cases:

Combined with other antiviral drugs to treat HIV-1 infection in adult patients aged 18 and over

The effectiveness of tenifo is based on the results of research studies for patients who have never been treated before, including patients with large amounts of viruses (> 100,000 copies/ml) and studies in which Tenifo is used to be added to the basic treatment (mainly combined therapy for 3 drugs for patients who had previously been anti -Retrovirus treatment but failed (

Tenifo is indicated for the treatment of hepatitis B in adults where the liver function is offset, with evidence of the human activity of the virus, the concentration of alanine aminotrasferase (ALT) increases continuously and the histological evidence of active or fibrosis. This indication is based mainly on histological, virus, biochemical and serinist in adult patients who have not been treated with nucleoside with chronic hepatitis B HBeAg positive and negative HBeAg with clear liver function.

Pharmacokic

Tenofovir disoproxil fumarate is an acyclic nucleoside phosphonate diester similar to adenosine monophosphate. Initially, Tenofovir Disoproxil Fumarate needs hydrolysis to convert to Tenofovir and then, phosphorylation by enzymes of cells converted into Tenofovir Diphosphate. Tenofovir diphosphate inhibits the enzyme activity to copy HIV-1 reverse by replacing the natural substrate of Deoxyadenosine 5 ', and ends the DNA chain after merging DNA. Tenofovir diphosphate weak inhibits DNA polymerases α, β in mammals and DNA polymerase γ mitochondria.

pharmacokinetic

absorption

Tenifo in water forms the diester form of the active ingredient Tenofovir disoproxil fumarate. Tenofovir Disoproxil Fumarate's hunger and oral biology is approximately 25%. After taking Tenifo 300mg doses in patients with HIV-1 at an empty stomach, the peak concentration of the serum is achieved after about 1 ± 0.4 hours. CMAX and AUC are 296 ± 90 ng/ml and 2287 ± 685ng/ml/hour, in order.

The pharmacological properties of Tenofovir Disoproxil Fumarate shown in the tenifo dose are about 75 to 600mg larger and does not work in the repeated dose.

Distribution

In Vitro testing, the cohesion of tenofovir disoproxil fumarate with serum or plasma protein is smaller than 0.7 and 7.2%, in order, tenofovir disoproxil fumarate level varies from 0.01 to 25µg/ml. The distribution volume at the peak concentration is 1.3 ± 0.6L/kg and 1.2 ± 0.4L/kg, and using Tenofovir Disoproxil Fumarate intravenously, 1.0mg/kg and 3.0mg/kg.

Metabolism and elimination

In Vitro test shows both tenofovir disoproxil or tenofovir is not the substrate of the CYP450 enzyme.

After the Tenofovir intravenous injection, about 70-80% of the dose found in urine in the form of unchanged Tenofovir Disoproxil Fumarate within 72 hours. After taking Tenifo doses, Tenofovir Disoproxil Fumarate is about 17 hours. After taking Tenifo multi -dose 300mg at a time/day (in full conditions), 32 ± 10% of the dose is found in urine for more than 24 hours. Tenofovir is eliminated by a combination of glomerular filtration and excreted through the renal tubules. Therefore, there may be competition on elimination with substances that are also excreted through the kidneys.

Before taking Tenifo Atra drugs treat HIV-1 infection, hepatitis B (1 blister x 10 tablets)

How to use

oral drugs. If the patient is not swallowed, it can be used in the form of dissolving tablets in at least 100ml of water, orange juice or pressed grapes.

Dosage

therapy should be given by an experienced doctor in the treatment of HIV -infected patients.

Adults

The recommended dose is taking 300mg (1 capsule) 1 time/day with meals.

Children

Tenifo is not recommended for children under 18 years of age for lack of data on safety and effectiveness for this object.

Older people

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

Patients with renal failure

Tenofovir is excreted through the kidneys and accumulates tenofovir when patients with renal failure. Dosage distance should be adjusted for patients with creatinine clearance

Creatinine clearance (ml/minute) *

30 - 49 10 - 29 bottle. There is no suggestion for patients with creatinine clearance 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 overdose? Tenofovir can eliminate blood apart, the average clearance of Tenofovir through hemorrhage appraisal is about 134ml/min. Eliminating tenofovir by peritoneal separation has not been studied.

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 Tenifo drugs , you may experience unwanted effects (ADR).

Evaluation of harmful reactions based on Marketing studies and 2 studies on 653 patients who had previously used for Tenofovir Disoproxil Fumarate (N = 443) or placebo (N = 210) in the legal therapy combined with Retrovirus anti -antacids for 24 weeks and also in an unprecedented patient with a pre -treated patient with Tenofroxil, Ten -Erra Fumarate 300 mg (n = 299) or Stavudine (n = 301) in combinations of lamivudine and efavirenz for 144 weeks.

approximately 1/3 of patients have side effects while treating with Tenofovir Disoproxil Fumarate combined with Retrovirus antacids. These counter -reactions are often mild to medium digestive reactions. Side effects are still suspicious (may be related to the treatment listed below based on the absolute ratio group. For each group, the unwanted effect is presented in the order of gradually decreasing: Very frequent ratio (> 1/10), regular (> 1/100, 1/1000, 1/10,000, Metabolism and nutrition

Very frequent: reducing blood phosphate.

Rarely: Lactic acid infection.

Central nervous system

Very often: dizziness.

Respiratory system, chest, mediastinum

Very rare: Difficulty breathing.

digestive system

Very frequent: diarrhea, nausea, vomiting.

regularly: flatulence.

rarely: pancreatitis.

liver

rarely: increase transaminase.

Very rarely: hepatitis.

Skin and subcutaneously

rarely: Red rash.

musculoskeletal

Unknown: muscle disease, bone puree (both related to near renal tubular disease).

Kidney and urinary tract

rarely: kidney failure , acute renal failure, near renal tubular disease (including fanconi syndrome), increased creatinine.

Very rare: acute renal necrosis.

Unknown: nephritis (including interstitial nephritis), diabetes due to kidneys.

General disorders

Very rare: weakness.

approximately 1% of patients with Tenofovir Disoproxil Fumarate treatment must stop treatment due to gastrointestinal side effects. Combined therapy combined antiviral drugs are related to metabolic abnormalities such as hyperglyceride blood, hypercholesterolemia, insulin resistance, hyperlem of blood glucose and hyperlorm blood. The combination of antacids of Retrovirus is related to the body's fat distribution (lipid dysplasia) on HIV -infected patients including subcutaneous and peripheral fat, increased fat in the abdomen and internal organs, hypertrophy of the mammary gland and accumulation of fat in the back (back tumor).

In a 144 -week control study for patients who have never treated Retrovirus anti -Retrovirus previously comparing Tenofovir Disoproxil Fumarate with Stavudine in combination with Lamivudine and Efavirenz, patients with Tenofovir Disoproxil Fumarate have lower lipid dysplasia than Stavudine patient group. Tenofovir Disoproxil Fumarate also causes rapid triglycerides and average total cholesterol than Stavudine.

For patients with HIV -infected immunodeficiency at the time of establishing a combination of antiviral drugs (Cart), the respondent respondent has an opportunity or an opportunity for opportunities that may arise. There have been reports on cases of bone necrosis when establishing a combination of Retrovirus (Cart), especially for patients who have known the risks, causing HIV progression or prolonged drug accumulation. The rate of this case is not known.

Instructions on how to handle ADR

Notify the doctor the unwanted effects encountered when taking the drug.

Warnings

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

Contraindicated

Tenifo drug contraindicated in the following cases:

Patients with active ingredients or any ingredients of the drug.

Be cautious when used

Tenifo is not used with any other drug that contains Tenofovir disoproxil fumarate.

Tenofovir disoproxil fumarate has not been studied in patients under 18 years old.

Tenofovir disoproxil fumarate is mainly regulated by the kidneys. Tenofovir accumulation may increase with patients with medium and severe renal impairment (creatinine clearance

Patients with renal impairment, may include hypoglycemia, which has been reported when using Tenofovir Disoproxil Fumarate.

Need to monitor kidney function (creatinine clearance and serum phosphate) before taking Tenifo, every 4 weeks in the first 1 year of treatment, and every 3 months later. For patients at risk or a history of renal failure and patients with renal failure, should consider closer monitoring. If serum phosphate concentration Consider stopping treatment for patients with creatinine clearance lower than 50ml/minute or serum phosphate level

Tenofovir disoproxil fumarate has not been clinically evaluated for patients who are using the drug excreted by the kidneys by the same shipping factor (Hota1- Element of organic anion 1) (such as Adefovir Dipivoxil, Cidofovir are known factors that are toxic to the kidneys). This shipping factor (Hoat1) can be responsible for excreting through the renal tubules and a part of the kidney excretion of Tenofovir, Adefovir and Cidofovir. Therefore, pharmacokinetics of these drugs may be changed if they are used simultaneously.

In healthy volunteers, a single dose of Adefovir Dipivoxil along with Tenofovir Disoproxil Fumarate does not cause significant interaction with pharmacokinetics. However, clinical safety includes the ability to affect the kidneys when combined with Adefovir Dipivoxil and Tenofovir Disoproxil Fumarate. Unless it is really necessary, the combination of these drugs is not recommended, but if inevitably, it is necessary to monitor the weekly kidney function.

In a 144 -week controlled study compares Tenofovir Disoproxil Fumarate with Stavudin in a combination of Lamivudin and Efavirenz in treatment for non -Retrovirus resistant patients, slightly reducing bone density in the hip and spine has been recorded in two treatment groups. Reducing mineral density in the spine and changing the bone structure of the bone increases significantly in the group of patients using Tenofovir Disoproxil Fumarate in a 144 -week study. Reducing mineral density in the hip bone increased significantly in this group of patients in 96 weeks. However, there is no risk of fracture or have clinical abnormal evidence after 144 weeks. If you suspect bone abnormalities, you should consult with experienced physicians.

Tenofovir disoproxil fumarate should be avoided in patients who have treated Retrovirus resistant to the K65R mutant hidden strain.

Tenofovir Disoproxil Fumarate has not been studied in elderly patients over 65 years old. Older patients often have renal failure, so be careful when using Tenofovir Disoproxil Fumarate for this object.

Liver disease

Tenofovir and Tenofovir Disoproxil Fumarate are not metabolized by liver enzymes. A pharmacokinetic study was conducted in non -HIV -infected patients with different levels of liver failure. There is no significant kinetic change recorded in these patients.

Safety and effectiveness of tenofovir disoproxil fumarate is limited to patients with liver dysfunction. Patients with chronic hepatitis B or C are treated for combination of antiviral drugs to increase the risk of hepatitis and liver death. In the case of combining antiviral drugs to treat hepatitis B or C, it is necessary to carefully refer to information about each drug. Patients with previous liver dysfunction, including chronic hepatitis, increased the risk of liver function abnormalities during treatment combined with Retrovirus anti -Retrovirus drugs and should be monitored for the standard process. If there is evidence that exacerbates liver disease in these patients, it is necessary to consider stopping treatment.

Lactic acid infection

Lactic acid infection, often combined with fatty liver disease, has been reported when using similar drugs nucleosid. Precipable and clinical data shows the risk of lactic acid infection, a type of impact of nucleosid -similar drugs, which is low with tenofovir disoproxil fumarate. However, because Tenofovir has a structure related to nucleosid medications, this risk cannot be excluded. Early symptoms (hyperlorm symptoms) include digestive symptoms (nausea, vomiting and abdominal pain), nonsense discomfort, loss of appetite, weight loss, respiratory symptoms (fast breathing or deep breathing) or neurological symptoms (including machinery control). Lactic acid infection can cause high death and may be associated with pancreatitis, liver failure or renal failure. Lactic acid infection usually occurs after a few months of treatment.

Treatment with nucleosid medications should be stopped when there are symptoms of hyperlage lactate and metabolic lactic infection, liver progression, or rapid increase in the concentration of aminotransferase. Caution should be careful when treating similar drugs nucleosid for any patient (especially obese women) with large liver, hepatitis or other risk factors for liver disease and fatty liver disease (including some drugs and alcohol).

Patients infected with hepatitis C are treated with Alpha Interferon and Ribavirin may have special risks. Patients who are likely to increase risks should be closely monitored. Retrovirus combined therapy is related to the redistribution of fat (lipid dysplasia) in the body of HIV -infected patients. The results of the research lasting on these cases are currently unknown. The mechanism of this is also unclear. There has been a hypothesis about a relationship between visceral fat accumulation and protease inhibition and fatty elimination and nucleoside reverse copy inhibition. The risk of high lipid dysplasia is associated with a number of special factors such as old age, and drug -related factors such as prolonged treatment of Retrovirus and related to metabolic disorders. Clinical tests should include evaluation of physical signs of fat redistribution in the body.

Consider the quick test of lipid levels in serum and blood glucose. Lipid disorders should be properly treated depending on clinical. Tenofovir is structured related to nucleoside drugs so the risk of lipid disorders cannot be excluded. However, the data of a 144 -week clinical study with patients who do not use Retrovirus resistance shows the risk of lipid disorders with tenofovir disoproxil fumarate with stavudine when combined with Lamivudine and Efavirenz.

Similar to nucleoside and nucleotide drugs have been shown to in vitro and in vivo, causing damage to mitochondria at different degrees. There have been reports on mitochondrial disorders in children who are not infected with HIV in the uterus or babies due to nucleoside medications. The harmful effects are mainly reported as blood disorders (anemia, neutropenia), metabolic disorders (hyperlactemia, hyperlipse of blood). These phenomena are often transient. Some late neurological disorders have been reported (increasing tone, convulsions, abnormal behaviors). It is not known that these disorders will be transient or prolonged.

The fetus in the uterus of the mother uses similar drugs nucleoside, even the fetus is not infected with HIV, should be monitored both clinically and tested and should also check the likelihood of chromosomal disorders when symptoms and signs are related. These results currently do not affect the recommendations when using Retrovirus resistance for pregnant women to prevent mother -to -child transmission.

Immune reaction syndrome

For patients with HIV -infected immunodeficiency at the time of establishing a Retrovirus (Cart) combined therapy, asymptomatic inflammatory reactions or opportunistic pathogens may arise and cause serious clinical conditions or worsen symptoms. Such reactions usually occur within a few weeks or the first few months to set up cartons. Patients are advised to check medical examination if there are signs of joint pain, stiffness or difficulty moving.

Combining the treatment of Tenofovir Disoproxil Fumarate and Didanosine, increasing 40 - 60% of the Didanosine accumulation in the body, increasing the risk of harmful effects related to Didanosine. Rarely occurs pancreatitis and lactic acid infection, sometimes death is reported. Didanosine dose reduction (down to 250mg) has been tested to avoid excessive accumulation of Didanosine in case of combination with Tenofovir Disoproxil Fumarate, but this is related to reports in several combined therapy tests showing the failure rate in virus treatment and higher resistance at the head phase.

Combining the treatment of Tenofovir Disoproxil Fumarate and Didanosine chlorine so it is not recommended, especially for patients with a high number of viruses and low number of CD4 cells. If the combination therapy is really necessary, the patient should be carefully monitored for the harmful reactions of Didanosine. Combining 3 nucleoside drugs: There are reports on high ratio of failure virus treatment and fast resistance when tenofovir disoproxil fumarate is combined with lamivudine and abacavir.

as well as combined with lamivudine and didanosine at a dose 1 time/day. Patients should be advised that anti -Retrovirus, including Tenofovir Disoproxil Fumarate, is not shown to prevent the possibility of HIV transmission to others (direct genital traces or blood sugar infection). The necessary protection measures are required during the use of the drug. Tenifo contains lactose monohydrate. Pediatric patients with genetic galactose intolerance due to lagl lactase deficiency, or galactose-glucose absorption abnormal should not take this medicine.

The ability to drive and operate machinery

There are no studies on the effects of drugs on driving and operating machinery. However, patients should be informed that the dizziness has been notified during the use of Tenofovir.

Pregnancy

There is no clinical information about the use of tenofovir disoproxil fumarate on pregnant people. Animal studies do not indirect or indirectly the harmful effects of tenofovir disoproxil fumarate for pregnant women, fetal development, childbirth or development of infants. Tenofovir Disoproxil Fumarate should only be used during pregnancy if the benefits bring higher risk to the fetus.

Despite the unknown fetal risks, the use of Tenofovir disoproxil fumarate for people who are likely to be pregnant must be combined with effective contraception.

Breastfeeding period

Animal studies show that Tenofovir is excreted in milk. It is not known whether Tenofovir will be excreted in human milk. Therefore, people who are using Tenofovir should not breastfeed. A general principle, women who are infected with HIV should not breastfeed to avoid HIV transmission to the child.

Medicinal interaction

Medicine interactive studies are only performed on adults. Based on the in vitro research results and the known metabolic path of Tenofovir, indirect interaction via CYP450 is related to Tenofovir and other drugs. Tenofovir is excreted through the kidneys, through both glomerular filtration and positive excretion through organic anion transport factors (Hoat1). Combining Tenofovir Disoproxil Fumarate with other drugs that are also positive through the kidneys thanks to the factor of Hoat1 (such as Cidofovir) that can cause increased tenofovir concentration or of the combined treatment.

Combined with other antiviral drugs

Emtricitabine, Lamivudine, Indinavir, Efavirenz, Nelfinavir and Saquinavir (Ritonavir derivatives) combine treatment with Tenofovir Disoproxil Fumarate without clinical value interactions.

When Tenofovir Disoproxil Fumarate is used in combination with Lopinavir/Ritonavir, there is no change in pharmacokinetics of Lopinavir and Ritonavir. Tenofovir's AUC increased by approximately 30% when Tenofovir Disoproxil Fumarate is used in combination with Lopinavir Ritonavir. Higher Tenofovir concentration is related to the harmful effects of Tenofovir, including renal disorders.

When the Didanosine intestine is taken 2 hours before or at the same time, Tenofovir Disoproxil Fumarate, the AUC of the Didanosine increases an average of 48% and 60% respectively. The average AUC of Didanosine increased by 44% when used before Tenofovir 1 hour. In both cases, Tenofovir pharmacokinetic parameters use have a change. Therefore, it is not advisable to combine tenofovir disoproxil fumarate and didanosine. When Tenofovir Disoproxil Fumarate is used with Atazanavir, reducing the level of Atazanavir is recorded by 25% and 40% AUC and CMIN, respectively, with acanavir content is 400 mg).

When Ritonavir combined with Atazanavir, there is no influence of Tenofovir on Atazanavir, CMIN decreases slightly, while AUC drops similarly to the above case (down 25% and 26% AUC and Cmin at a dose of 300/100mg respectively). Combining Atazanavir/Ritonavir with Tenofovir Disoproxil Fumarate causing Tenofovir accumulation. Higher Tenofovir concentration is related to the harmful effects of Tenofovir, including renal disorders. Combining Atazanavir/Ritonavir treatment with Tenofovir Disoproxil Fumarate has been shown by a clinical study.

Other interactions

Combining Tenofovir Disoproxil Fumarate, Methazone, Ribavirin, Rifampicin, Adefovir Dipivoxil or contraceptive hormones containing Norgestimate/Ethinyl Estradiol does not cause pharmacokinetic interaction. Tenofovir Disoproxil Fumarate is taken with food, due to the bioavailable food of Tenofovir.

Storage

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

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