Hepariv 0.5mg Treatment of chronic hepatitis B virus infection (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Entecavir

Ingredient

Composition information	Content
Entecavir	0.5mg

Uses

Indications

Hepariv 0.5mg is indicated in the following cases:

Treatment of chronic hepatitis B virus (HBV) in adults and children from 16 years or more with HBV evidence actively copying DNA-HBV increases in the blood and increasing the persistent concentration of serum aminotransferase (ALT or AST) or having histological evidence of active liver disease. This indication is based on a response to histological, viruses, biochemistry, and serum in adults and children of 16 years or more before not taking nucleosid antiviral drugs and in adults with HBV resistant to lamivudine and HBeAg - positive or HBEAG - negative accompanied by liver function is still compensated. Use Entecavir to treat chronic hepatitis B and hepatitis B virus resistant to lamivudine.

Restricted data related to HBV and HIV -infected patients.

Pharmacokological

Entecavir is a synthetic drug similar to nucleosid purine derived from guanin with antiviral activity in humans (HBV). The drug is enzymes in phosphoryl cells to form an active metabolic substance, which is Entecavir Triphosphate. By competing with the natural substrate of Deoxyguanosin Triphosphate, Entecavir Triphosphate inhibits DNA polymerase (enzyme transcription) of hepatitis B virus in humans, thus preventing all active stages of enzymes.

Effective spectrum: Entecavir has in vitro and in vivo activity against HBV, including some HBV strains of Lamivudine resistance. The drug also works to limit In vitro against some viruses in humans, including the herpes simplex type 1 and 2 virus (HSV-1 and HSV-2), Varicella Zoster and Cytomegalovirus viruses but the drug does not prove it in clinical effect. Entecavir has a few effects on HIV-1 (Entecavir concentration needed to inhibit the copy virus about 50% [EC50] for HIV-1 ranging from 0.026 to greater than 10 micromes).

Drug resistance: When long -term treatment in some patients, some evidence shows that HBV is slow to reduce sensitivity to Entecavir. In patients who have not used nucleosid before before, for entecavir for 96 weeks, the virus returns to cause severe illness due to drug resistance that occurs less than 1% of the patient. In lamivudine resistant patients, the virus broke out due to Entecavir resistance occurred in 1% of patients after the first year of treatment and in 9% of patients in the second year of treatment.

Entecavir resistance occurs in the process of 2 steps, initially mutant M204V/i followed by replacing Amino-acid in RTI169, RTT184, STS202, or RTM250.

There are cross -resistance between a number of nucleosid -similar drugs that have anti -HBV anti -lamivudine and Telbivudin resistance, which has been reduced in sensitivity to Entecavir In Vitro. The Adenofir HBV also changes sensitivity to Entecavir that has seen in vitro. HBV isolated from lamivudin resistant patients and failed with Entecavir therapy that is still sensitive to Adenofir. Entecavir inhibits hepatitis B virus, inhibits both lamivudine and adefovir virus strains.

pharmacokinetic

absorption

The peak concentration of Entecavir in plasma in healthy objects is about 0.5 - 1.5 hours after drinking.

The effect of food on oral absorption: drink 0.5mg entecavir along with a normal meal of high fat or a snack leads to slowing absorption (1.0 - 1.5 hours when the abdomen is full compared to 0.75 hours when hungry) reduces CMAX 44 - 46% and AUC 8 - 20%.

Distribution

Based on the pharmacokinetics records of Entecavir after oral, the apparent distribution integral is estimated to be more than the total amount of water in the body, which shows that Entecavir is distributed in tissue.

On In vitro, about 13% of Entecavir associated with human serum protein.

Metabolism and elimination

There is no oxidation or acetylation metabolite in humans after drinking 14C-toecavir. Observations are not significant amounts of stage II metabolites (glucuronid and sulfate complex). Entecavir is not a substrate, an inhibitor or an induction of the cytochrom P450 enzyme system (CYP450).

After reaching the peak concentration, the Entecavir concentration in plasma decreases with the second -order exponential function with the last selling time of about 128 - 149 hours. The accumulation index of observation is about 2 times at a dose 1 time/day, this shows that the semi -cancellation time is actually about 24 hours.

Entecavir is mainly eliminated through the kidneys with non -metabolic drugs recovered in urine in a stable state of 62 - 73% of the dose. The dialysis does not depend on the dose and ranges from 360 to 471 ml/min, which shows that Entecavir has passed both glomerular filtration and sub -secretion.

Before taking Hepariv 0.5mg Treatment of chronic hepatitis B virus infection (3 blisters x 10 tablets)

How to use

oral drugs.

Take the drug at hunger, at least 2 hours before or 2 hours after the meal. Oral solution is not mixed with water or with any other liquid. Measuring spoon after drinking must be washed with water.

Dosage

Adults and children from 16 years or more of chronic HBV has never been treated with nucleosid -similar drugs

Dosage recommends taking 0.5mg 1 time daily.

adults and children from 16 years or more have a history of blood hbv during treatment of lamivudin or HBV is known to be anti -Lamivudin or telbivudin

Take 1mg of oral 1 time.

The optimal medication time is unknown but at least 1 year. Can stop treatment:

In HBeAg people - Positive, must be treated at least until the HBE serum is transferred, the HBeAg and DNA levels of HBV become negative (below the detection threshold), accompanied by the detection of HBE anti -HBE antibodies in 2 consecutive blood takes at least 3 to 6 months or until the HBS server is transferred or in case of no effect after 1 year. Most until the concentration of negative DNA-HBV (below the detection threshold) and HBS serum transfer or until it is not seen. In case of treatment lasting for more than 2 years, it is necessary to regularly reassess to determine whether the treatment is suitable for patients.

Elderly

No dose adjustment. However, it should be remembered that the kidney function is often poor in tall people.

kidney failure

Must adjust the dose based on the CLCR. Reduce the dose by using oral solution. If the solution is not available, the distance between the dose must be increased. According to the manufacturer, you should drink once a day. The patient of the hemolysis must take entecavir after the fertilizer.

Cl (ml/minute)

Recommended doses for non -use nucleosides

Recommended doses for lamivudin resistors

0.5mg 1 time

1mg 1 time

30 - 49

0.25mg orally 1 time*
or 0.5mg every 48 hours

0.5mg 1 time

10 - 29

0.15mg 1 time* or 0.5mg every 72 hours

0.3mg 1 time* or 0.5mg every 48 hours

0.05mg 1 time* or 0.5mg every 5 - 7 days

0.1mg oral 1 time* or 0.5mg 72 hours from 72 hours

liver

No dose adjustment.

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? Some people took 20mg/day for 14 days and some took 1 dose of 40mg but did not show signs of poisoning. When overdose, it is necessary to monitor the evolution to handle.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

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 Hepariv 0.5mg, you may experience unwanted effects (ADR).

In clinical trials, 3% or more patients are reported unwanted effects such as headache, fatigue, dizziness, nausea, diarrhea, indigestion, vomiting, drowsiness, and insomnia have also been reported.

Common, ADR> 1/100

Kidney: Bleeding (9%), increased creatinine (1-2%), urinary glucose (4%).

Mental: Insomnia, headache, dizziness.

digestive: vomiting, diarrhea, nausea, indigestion.

Hepatic liver: increased transaminase (> 10%), increased lipase (7%), increased amylase (2 - 3%), increased blood bilirubin (2 - 3%).

all body: tired.

Uncommon, 1/1 000

Skin: rash, hair loss.

Popular bloating.

Rare, ADR

Immune reaction.

Some cases of lactic acidic acidosis are often combined with loss of liver or another severe medical disease or are taking some other drugs. Use Entecavir an average of 96 weeks without a replacement tolerance.

The most common testing abnormalities in Entecavir clinical trial is an increase in ALT (5 times larger than normal levels: ULN), hematuria, lipase increases (at least 2.1 times ULN), glucose pulse, hyperlemin bilirubin (larger than 2 times ULN), increasing ALT (larger than 10 times ULN and 2 times the level of treatment at the beginning of the Helocons) Increasing blood glucose at hunger (over 250 mg/dl), and increased creatinine (at least 0.5 mg/dl).

Instructions on how to handle ADR

In general, light ADRs are usually out of self, without treatment. The serious hepatitis may occur after stopping anti -HBV therapy, including Entecavir. The serious batch manifested by ALT by 10 times the normal high level (ULN) and twice as serum at the beginning of treatment. The average time of severe disease occurs about 23 weeks after stopping treatment. Severe disease after stopping treatment is usually combined with HBV's DNA increase and most of themselves will recover. Most serious illness after stopping treatment in HBeAg - negative. Liver monitoring should be clinically and biochemically regularly at least 6 months after stopping treatment. If necessary, can be treated again. Severe hepatitis also encountered while being treated with HBV with Entecavir on average 4 to 5 weeks after the beginning of treatment but often ran out of treatment. Entecavir treatment must be stopped in any patient with clinical manifestations or tests that think of lactic acidic acidosis or severe liver toxicity (such as fatty liver, even if transaminase does not increase).

Warnings

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

Contraindicated

Hepariv 0.5mg contraindicated in the following cases:

Contraindicated when there is a history of hypersensitivity to Entecavir or with any component of the finished product.

Pregnant women, nursing women.

Children under 16 years old.

Caution when using

spontaneous hepatitis becomes serious or occurs and often manifests by temporary increase in alat serum concentration. After starting antiviral treatment, alat serum levels may increase in patients while HBV's DNA serum levels decrease. Among the patients treated with Entecavir, severe illnesses appear on average 4 to 5 weeks after the beginning of treatment. In patients with compensation liver disease, alat serum levels increased, often without hypoglycemia of blood bilirubin like liver disease. If the patient has cirrhosis, there is a high risk of liver and liver after getting worse. Therefore, during treatment, clinical and biochemistry must be closely monitored.

Some cases of severe illness due to the stop treatment against hepatitis B with Entecavir have been reported. The serious illness stops Entecavir often combined with increased serum DNA serum of HBV and most cases of self -out, but some cases have died. Among the previous patients who have not used nucleosides are now treated with Entecavir, severe cases appear on average 23 to 24 weeks after stopping treatment. Most cases occur in people with HBeAg - negative. Must monitor the liver regularly both clinically and biochemically at least 6 months after stopping treatment. If DNA-HBV increases or if needed, give treatment another batch.

Be cautious when treating patients with liver loss due to many auxiliary complications, at high risk of lactic acidic acidosis. Be cautious when treating Entecavir for chronic HBV infected people without detecting that person is also infected with HIV because there is a risk of HIV -resistant strains resistant to nucleosides inhibiting enzymes in reverse transcription (NRRTI). Before starting Entecavir treatment, HIV test. Because there may be a risk of NRTI -resistant HIV appearance, Entecavir should not be used to treat chronic HBV infections in HIV -infected patients.

Be cautious when using Entecavir to treat chronic hepatitis B because it can cause lactic acidic acidosis, large liver and liver fatty in patients with only nucleosid medications or in combination with other antiviral drugs. Most cases occur in women; Obesity and long -term treatment with nucleosid drugs inhibit the opposite code enzyme can also be risk factors. Caution must be used with nucleosid -similar drugs for people who are at high risk of liver disease, but lactic acidic acidosis, enlarged liver and fattyness occur in people who are not at risk. Entecavir must be stopped immediately in any patient with clinical signs and tests for lactic acidosis or severe liver poisoning even when transaminase does not increase.

Unknown about the safety and effectiveness of Entecavir for liver transplants. If you have to use Entecavir for a liver transplant that has or is taking an immunosuppressant that can affect kidney function such as cyclosporin, tacrolimus, must monitor kidney function before and during Entecavir treatment.

For tall people of 65 years or more, the experience is less enough to determine whether the response is different from the young people. Because Entecavir is mainly eliminated through the kidneys, the risk of Entecavir canxicity may increase in people with renal failure. Elderly people often have impaired renal function, need to adjust the dose according to the degree of renal failure and must monitor the kidney function.

Adjustment recommended for patients with CLCR

Entecavir does not reduce the risk of virus transmission to others, so the prevention measures must be taken.

The ability to drive and operate machinery

Be careful when used for driving objects and operating machinery.

Pregnancy

There has been no research in pregnant women and there is no data on the effect of Entecavir on HBV transmission from mother to child; The child born from HBV -infected mother is often recommended to use the HBV vaccine and hepatitis B immune globe (HBIG).

Women during labor and childbirth

There are no studies in pregnant women and there is no data on the influence of Entecavir on the transmission of HBV from mother to child. Therefore, it is advisable to use appropriate interventions to prevent the suffering from HBV in infants.

Breastfeeding period

It is unknown whether Entecavir is in breast milk or not. Stop breastfeeding or medication depending on the importance of the drug for the mother.

Drug interaction

There is no interaction that should be recommended to avoid using at the same time with Entecavir.

Effects and effects of Entecavir may increase by ganciclovir, Valganciclovir, Ribavirin.

Entecavir is not a substrate and does not inhibit or stimulate the cytochrom P450 (CYP) iszyme. Less likely to interact with pharmacological drugs with metabolic drugs caused by ISOENZYM CYP.

The drug affects the kidneys or eliminates the kidneys: has the ability to interact with pharmacological interactions with drugs that reduce the kidney function or compete with Entecavir to positive secretion through the renal tubules. Etecavir serum or combined drug may increase. Need to monitor the auxiliary complications.

With Adefovir, Lamivudin, Tenofovir, Disoproxil: no interaction.

Immunosuppressant drugs: Having the ability to interact with pharmacokinetic (Entecavir serum levels increase because the kidney function is replaced) with cyclosporin or tacrolimus. Kidney function must be monitored before and during human being (liver transplant) treatment, using cyclosporin, tacrolimus or other immunosuppressive drugs that can affect kidney function.

nucleosid and nucleosid drugs inhibit the reverse code enzyme: There is no pharmacological interaction with lamivudin or tenofovir disoproxil fumarat.

Storage

Store in closed packaging, at temperatures not more than 30 ° C, avoiding light.

oral solution after opening the vial, the solution may be used until the expiry date stated on the vial.

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