Baraclude - General Information
Baraclude is an oral antiviral drug used in the treatment of hepatitis B infection. It is marketed under the trade name Baraclude (BMS).
Baraclude is a guanine analogue that inhibits all three steps in the viral replication process, and the manufacturer claims that it is more efficacious than previous agents used to treat hepatitis B (lamivudine and adefovir). It was approved by the U.S. Food and Drug Administration (FDA) in March 2005.
Pharmacology of Baraclude
Baraclude is a guanosine nucleoside analogue with selective activity against hepatitis B virus (HBV). It is designed to selectively inhibit the Hepatitis B virus, blocking all three steps in the replication process. Baraclude is more efficient than an older Hepatitis B drug, lamivudine.
Baraclude for patients
BaracludeTM (BEAR ah klude)
(generic name = entecavir)
Tablets and Oral Solution
Read the Patient Information that comes with BARACLUDE before you start taking it and each time you get a refill. There may be new information. This information does not take the place of talking with your healthcare provider about your medical condition or treatment.
What is the most important information I should know about BARACLUDE?
1.Some people who have taken medicines like BARACLUDE (a nucleoside analogue) have developed a serious condition called lactic acidosis (buildup of an acid in the blood). Lactic acidosis is a medical emergency and must be treated in the hospital. Call your healthcare provider right away if you get any of the following signs of lactic acidosis.
• You feel very weak or tired.
• You have unusual (not normal) muscle pain.
• You have trouble breathing.
• You have stomach pain with nausea and vomiting.
• You feel cold,especially in your arms and legs.
• You feel dizzy or light-headed.
• You have a fast or irregular heartbeat.
2. Some people who have taken medicines like BARACLUDE have developed serious liver problems called hepatotoxicity, with liver enlargement (hepatomegaly) and fat in the liver (steatosis). Call your healthcare provider right away if you get any of the following signs of liver problems.
• Your skin or the white part of your eyes turns yellow (jaundice).
• Your urine turns dark.
• Your bowel movements (stools) turn light in color.
• You don't feel like eating food for several days or longer.
• You feel sick to your stomach (nausea).
• You have lower stomach pain.
3.Your hepatitis B infection may get worse or become very serious if you stop BARACLUDE.
• Take BARACLUDE exactly as prescribed.
• Do not run out of BARACLUDE.
• Do not stop BARACLUDE without talking to your healthcare provider.
Your healthcare provider will need to monitor your health and do regular blood tests to check your liver if you stop BARACLUDE. Tell your healthcare provider right away about any new or unusual symptoms that you notice after you stop taking BARACLUDE.
What is BARACLUDE?
BARACLUDE is a prescription medicine used for chronic infection with hepatitis B virus (HBV) in adults who also have active liver damage.
• BARACLUDE will not cure HBV.
• BARACLUDE may lower the amount of HBV in the body.
• BARACLUDE may lower the ability of HBV to multiply and infect new liver cells.
• BARACLUDE may improve the condition of your liver.
It is important to stay under your healthcare provider's care while taking BARACLUDE. Your healthcare provider will test the level of the hepatitis B virus in your blood regularly.
Does BARACLUDE lower the risk of passing HBV to others?
BARACLUDE does not stop you from spreading HBV to others by sex, sharing needles, or being exposed to your blood. Talk with your healthcare provider about safe sexual practices that protect your partner. Never share needles. Do not share personal items that can have blood or body fluids on them, like toothbrushes or razor blades. A shot (vaccine) is available to protect people at risk from becoming infected with HBV.
Who should not take BARACLUDE (entecavir)?
Do not take BARACLUDE if you are allergic to any of its ingredients. The active ingredient in BARACLUDE is entecavir. See the end of this leaflet for a complete list of ingredients in BARACLUDE. Tell your healthcare provider if you think you have had an allergic reaction to any of these ingredients.
BARACLUDE has not been studied in children and is not recommended for anyone less than 16 years old.
What should I tell my healthcare provider before I take BARACLUDE?
Tell your healthcare provider about all of your medical conditions, including if you:
• have kidney problems. You may need a lower dose of BARACLUDE.
• are pregnant or planning to become pregnant. It is not known if BARACLUDE is safe to use during pregnancy. It is not known whether BARACLUDE helps prevent a pregnant mother from passing HBV to her baby. You and your healthcare provider will need to decide if BARACLUDE is right for you. If you use BARACLUDE while you are pregnant, talk to your healthcare provider about the BARACLUDE Pregnancy Registry.
• are breast-feeding. It is not known if BARACLUDE can pass into your breast milk or if it can harm your baby. Do not breast-feed if you are taking BARACLUDE.
Tell your healthcare provider about all the medicines you take including prescription and nonprescription medicines, vitamins, and herbal supplements. BARACLUDE may interact with other medicines that leave the body through the kidneys.
Know the medicines you take. Keep a list of your medicines with you to show your healthcare provider and pharmacist.
How should I take BARACLUDE?
• Take BARACLUDE exactly as prescribed. Your healthcare provider will tell you how much BARACLUDE to take. Your dose will depend on whether you have been treated for HBV infection before and what medicine you took. The usual dose of BARACLUDE Tablets is either 0.5 mg (one white tablet) or 1 mg (one pink tablet) once daily by mouth. The usual dose of BARACLUDE Oral Solution is either 10 mL or 20 mL once daily by mouth. Your dose may be lower if you have kidney problems.
• Take BARACLUDE once a day on an empty stomach to help it work better. Empty stomach means at least 2 hours after a meal and at least 2 hours before the next meal. To help you remember to take your BARACLUDE, try to take it at the same time each day.
• If you are taking BARACLUDE Oral Solution, carefully measure your dose with the spoon provided, as follows:
1.Hold the spoon in a vertical (upright) position and fill it gradually to the mark corresponding to the prescribed dose. Holding the spoon with the volume marks facing you, check that it has been filled to the proper mark.
2.Swallow the medicine directly from the measuring spoon.
3. After each use, rinse the spoon with water and allow it to air dry.
If you lose the spoon, call your pharmacist or healthcare provider for instructions.
• Do not change your dose or stop taking BARACLUDE without talking to your healthcare provider. Your hepatitis B symptoms may get worse or become very serious if you stop taking BARACLUDE. After you stop taking BARACLUDE, it is important to stay under your healthcare provider's care. Your health-care provider will need to do regular blood tests to check your liver.
• If you forget to take BARACLUDE, take it as soon as you remember and then take your next dose at its regular time. If it is almost time for your next dose, skip the missed dose. Do not take two doses at the same time. Call your healthcare provider or pharmacist if you are not sure what to do.
• When your supply of BARACLUDE starts to run low, get more from your healthcare provider or pharmacy. Do not run out of BARACLUDE.
• If you take more than the prescribed dose of BARACLUDE, call your healthcare provider right away.
What are the possible side effects of BARACLUDE?
BARACLUDE may cause the following serious side effects (see "What is the most important information I should know about BARACLUDE?"):
• lactic acidosis and liver problems.
• a worse or very serious hepatitis if you stop taking it.
The most common side effects of BARACLUDE are headache, tiredness, dizziness, and nausea. Less common side effects include diarrhea, indigestion, vomiting, sleepiness, and trouble sleeping. In some patients, the results of blood tests that measure how the liver or pancreas is working may worsen.
These are not all the side effects of BARACLUDE. The list of side effects is not complete at this time because BARACLUDE is still under study. Report any new or continuing symptom to your healthcare provider. If you have questions about side effects, ask your healthcare provider. Your healthcare provider may be able to help you manage these side effects.
How should I store BARACLUDE?
• Store BARACLUDE Tablets or Oral Solution at room temperature, 59° to 86° F (15° to 30° C).They do not require refrigeration. Do not store BARACLUDE Tablets in a damp place such as a bathroom medicine cabinet or near the kitchen sink.
• Keep the container tightly closed. BARACLUDE Oral Solution should be stored in the original carton and protected from light.
• Throw away BARACLUDE when it is outdated or no longer needed by flushing tablets down the toilet or pouring the oral solution down the sink.
• Keep BARACLUDE and all medicines out of the reach of children and pets.
General information about BARACLUDE
Medicines are sometimes prescribed for conditions other than those described in patient information leaflets. Do not use BARACLUDE for a condition for which it was not pre-scribed. Do not give BARACLUDE to other people, even if they have the same symptoms you have. It may harm them. The leaflet summarizes the most important information about BARACLUDE. If you would like more information, talk with your healthcare provider. You can ask your healthcare provider or pharmacist for information about BARACLUDE that is written for healthcare professionals. You can also call 1-800-321-1335 or visit the BARACLUDE website at www.Baraclude.com.
What are the ingredients in BARACLUDE?
Active Ingredient: entecavir
Inactive Ingredients in BARACLUDE Tablets
lactose monohydrate, microcrystalline cellulose, crospovidone, povidone, magnesium stearate, titanium dioxide, hypromellose, polyethylene glycol 400, polysorbate 80 (0.5-mg tablet only),and iron oxide red (1-mg tablet only).
Inactive Ingredients in BARACLUDE Oral Solution
maltitol, sodium citrate, citric acid, methylparaben, propylparaben, and orange flavor.
Since entecavir is primarily eliminated by the kidneys, coadministration of BARACLUDE with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of either entecavir or the coadministered drug. Coadministration of entecavir with lamivudine, adefovir dipivoxil,or tenofovir disoproxil fumarate did not result in significant drug interactions. The effects of coadministration of BARACLUDE with other drugs that are renally eliminated or are known to affect renal function have not been evaluated, and patients should be monitored closely for adverse events when BARACLUDE is coadministered with such drugs.
BARACLUDE is contraindicated in patients with previously demonstrated hypersensitivity to entecavir or any component of the product.
Additional information about Baraclude
Baraclude Indication: For the treatment of chronic hepatitis B virus infection in adults with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease.
Mechanism Of Action: By competing with the natural substrate deoxyguanosine triphosphate, entecavir functionally inhibits all three activities of the HBV polymerase (reverse transcriptase, rt): (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA.
Drug Interactions: Not Available
Food Interactions: Take on an empty stomach.
Taking the product with a high-fat meal or a light snack reduces the maximal concentration by 44 to 46% and total exposure by 18 to 20%.
Generic Name: Entecavir
Synonyms: Not Available
Drug Category: Antiviral Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Entecavir: Baraclude;
Absorption: Absorption Following oral administration in healthy subjects, entecavir peak plasma concentrations occurred between 0.5 and 1.5 hours. In healthy subjects, the bioavailability of the tablet is 100% relative to the oral solution.
Toxicity (Overdose): Healthy subjects who received single entecavir doses up to 40 mg or multiple doses up to 20 mg/day for up to 14 days had no increase in or unexpected adverse events. If overdose occurs, the patient must be monitored for evidence of toxicity, and standard supportive treatment applied as necessary.
Protein Binding: Binding of entecavir to human serum proteins in vitro is approximately 13%.
Biotransformation: Entecavir is not a substrate, inhibitor, or inducer of the cytochrome P450 (CYP450) enzyme system. Entecavir is efficiently phosphorylated to the active triphosphate form.
Half Life: After reaching peak concentration, entecavir plasma concentrations decreased in a bi-exponential manner with a terminal elimination half-life of approximately 128-149 hours. The phosphorylated metabolite has a half-life of 15 hours.
Dosage Forms of Baraclude: Tablet Oral
Chemical IUPAC Name: 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-3H-purin-6-one
Chemical Formula: C12H15N5O3
Entecavir on Wikipedia: http://en.wikipedia.org/wiki/Entecavir
Organisms Affected: Hepatitis B virus