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Drug overview for ENTECAVIR (entecavir):
Generic name: entecavir (en-TEK-a-vir)
Drug class: Oral Antivirals for Chronic Hepatitis B
Therapeutic class: Anti-Infective Agents
Entecavir, a synthetic purine nucleoside analog derived from guanine, is an antiviral agent that is active against human hepatitis B virus (HBV).
No enhanced Uses information available for this drug.
Generic name: entecavir (en-TEK-a-vir)
Drug class: Oral Antivirals for Chronic Hepatitis B
Therapeutic class: Anti-Infective Agents
Entecavir, a synthetic purine nucleoside analog derived from guanine, is an antiviral agent that is active against human hepatitis B virus (HBV).
No enhanced Uses information available for this drug.
DRUG IMAGES
ENTECAVIR 1 MG TABLET
ENTECAVIR 0.5 MG TABLET
The following indications for ENTECAVIR (entecavir) have been approved by the FDA:
Indications:
Chronic hepatitis B
Lamivudine-refractory chronic hepatitis B
Professional Synonyms:
Chronic hepatitis B virus infection
Chronic hepatitis due to HBV
Indications:
Chronic hepatitis B
Lamivudine-refractory chronic hepatitis B
Professional Synonyms:
Chronic hepatitis B virus infection
Chronic hepatitis due to HBV
The following dosing information is available for ENTECAVIR (entecavir):
No enhanced Dosing information available for this drug.
Entecavir is administered orally (as tablets or oral solution). Because the presence of food in the GI tract may decrease the rate and extent of absorption, entecavir should be administered on an empty stomach at least 2 hours before or 2 hours after meals. Administer the oral solution using the supplied oral dosing spoon according to the patient instructions provided by the manufacturer.
The oral solution contains 0.05 mg of entecavir per mL; do not dilute or mix the solution with water or any other liquid. Refer to the full prescribing information for specific instructions for administration of the oral solution.
Store entecavir tablets and oral solution at 25oC (excursions permitted between 15-30oC); the tablets should be stored in a tightly-closed container. Store both the tablets and the oral solution in the outer carton to protect from light. After opening, the oral solution can be used up to the expiration date on the bottle.
The oral solution contains 0.05 mg of entecavir per mL; do not dilute or mix the solution with water or any other liquid. Refer to the full prescribing information for specific instructions for administration of the oral solution.
Store entecavir tablets and oral solution at 25oC (excursions permitted between 15-30oC); the tablets should be stored in a tightly-closed container. Store both the tablets and the oral solution in the outer carton to protect from light. After opening, the oral solution can be used up to the expiration date on the bottle.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| ENTECAVIR 0.5 MG TABLET | Maintenance | Adults take 1 tablet (0.5 mg) by oral route once daily 1 hour before a meal or 2 hours after a meal |
| ENTECAVIR 1 MG TABLET | Maintenance | Adults take 1 tablet (1 mg) by oral route once daily 1 hour before a meal or 2 hours after a meal |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| ENTECAVIR 0.5 MG TABLET | Maintenance | Adults take 1 tablet (0.5 mg) by oral route once daily 1 hour before a meal or 2 hours after a meal |
| ENTECAVIR 1 MG TABLET | Maintenance | Adults take 1 tablet (1 mg) by oral route once daily 1 hour before a meal or2 hours after a meal |
The following drug interaction information is available for ENTECAVIR (entecavir):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for ENTECAVIR (entecavir):
Drug contraindication overview.
None.
None.
There are 0 contraindications.
There are 6 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Chronic kidney disease stage 3A (moderate) GFR 45-59 ml/min |
| Chronic kidney disease stage 3B (moderate) GFR 30-44 ml/min |
| Chronic kidney disease stage 4 (severe) GFR 15-29 ml/min |
| Chronic kidney disease stage 5 (failure) GFr<15 ml/min |
| Lactic acidosis |
| Steatosis of liver |
There are 2 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Drug resistance to anti-retroviral therapy |
| Kidney disease with likely reduction in glomerular filtration rate (GFr) |
The following adverse reaction information is available for ENTECAVIR (entecavir):
Adverse reaction overview.
The most common adverse effects (>=3%, all severity grades) in adults were headache, fatigue, dizziness, and nausea. Adverse effects observed in pediatric patients were consistent with those observed in adults.
The most common adverse effects (>=3%, all severity grades) in adults were headache, fatigue, dizziness, and nausea. Adverse effects observed in pediatric patients were consistent with those observed in adults.
There are 10 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Abnormal hepatic function tests Hematuria Lactic acidosis |
Glycosuria Hyperbilirubinemia |
| Rare/Very Rare |
|---|
|
Anaphylaxis Hepatomegaly Hyperglycemia Steatosis of liver Thrombocytopenic disorder |
There are 13 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Alopecia Dizziness Drowsy Fatigue Headache disorder Nausea Skin rash |
Acute abdominal pain Diarrhea Dysgeusia Vomiting |
| Rare/Very Rare |
|---|
|
Dyspepsia Insomnia |
The following precautions are available for ENTECAVIR (entecavir):
Safety and efficacy of were evaluated in clinical trials of pediatric patients >=2 years of age with HBeAg-positive chronic HBV infection and compensated liver disease. Steady-state pharmacokinetics of entecavir were evaluated in pediatric patients 2 to <18 years of age with compensated liver disease. Entecavir exposures in nucleoside inhibitor-naive children receiving the oral solution in a dosage of 0.015
mg/kg (<=0.5 mg) once daily were similar to exposures observed in adults receiving a 0.5-mg tablet once daily. Exposures in lamivudine-experienced children receiving the oral solution in a dosage of 0.03
mg/kg (<=1 mg) once daily were similar to exposures observed in adults receiving a 1-mg tablet once daily. There are limited data available on the use of entecavir in lamivudine-experienced pediatric patients; use entecavir in these patients only if potential benefits justify potential risks. Since some pediatric patients may require long-term or lifetime management of chronic active HBV infection, consider the impact of entecavir use on future treatment options. Safety and efficacy of entecavir have not been established in pediatric patients <2 years of age; entecavir has not been evaluated in these patients since treatment of HBV is rarely required in this age group.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
mg/kg (<=0.5 mg) once daily were similar to exposures observed in adults receiving a 0.5-mg tablet once daily. Exposures in lamivudine-experienced children receiving the oral solution in a dosage of 0.03
mg/kg (<=1 mg) once daily were similar to exposures observed in adults receiving a 1-mg tablet once daily. There are limited data available on the use of entecavir in lamivudine-experienced pediatric patients; use entecavir in these patients only if potential benefits justify potential risks. Since some pediatric patients may require long-term or lifetime management of chronic active HBV infection, consider the impact of entecavir use on future treatment options. Safety and efficacy of entecavir have not been established in pediatric patients <2 years of age; entecavir has not been evaluated in these patients since treatment of HBV is rarely required in this age group.
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
A pregnancy exposure registry (the Antiretroviral Pregnancy Registry (APR)) monitors maternal-fetal outcomes of pregnant women exposed to entecavir; clinicians are encouraged to enroll patients in the registry by calling 800-258-4263. Prospective data from the APR are insufficient to adequately evaluate the risk of birth defects, miscarriage, or adverse maternal or fetal outcomes. The limited number of entecavir exposures reported to the APR is not sufficient to inform a risk assessment in comparison to a reference population.
The rate of miscarriage is not reported in the APR. In animal reproduction studies, there was no evidence of developmental toxicities in rats or rabbits at systemic entecavir exposures approximately 28 or 212 times, respectively, human exposures achieved at the maximum recommended human dose (MRHD) of 1 mg daily. In a pre/postnatal development study, no adverse effects on the offspring were observed when entecavir (<=30 mg/kg per day) was administered orally to pregnant rats from gestation day 6 to lactation/post-partum day 20, resulting in exposures >94 times those in humans at the MRHD.
The rate of miscarriage is not reported in the APR. In animal reproduction studies, there was no evidence of developmental toxicities in rats or rabbits at systemic entecavir exposures approximately 28 or 212 times, respectively, human exposures achieved at the maximum recommended human dose (MRHD) of 1 mg daily. In a pre/postnatal development study, no adverse effects on the offspring were observed when entecavir (<=30 mg/kg per day) was administered orally to pregnant rats from gestation day 6 to lactation/post-partum day 20, resulting in exposures >94 times those in humans at the MRHD.
It is not known whether entecavir is distributed into human milk, affects human milk production, or has effects on the breastfed infant. Entecavir was present in milk when administered to lactating rats. Consider the benefits of breastfeeding and the importance of entecavir to the mother along with the potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition.
Select dosage of entecavir for geriatric patients with caution due to possible age-related decreases in renal function; monitoring renal function also may be helpful. Clinical studies did not include sufficient numbers of patients >=65 years of age to determine whether they respond differently to entecavir than younger adults. Entecavir is substantially excreted by the kidneys, and the risk of entecavir-induced toxicity may be increased in patients with impaired renal function.
The area under the plasma concentration-time curve (AUC) of entecavir is increased compared with younger adults, possibly as the result of age-related changes in renal function. Since geriatric patients may be more likely to have decreased renal function, select dosage with caution; it also may be useful to monitor renal function in geriatric patients.
The area under the plasma concentration-time curve (AUC) of entecavir is increased compared with younger adults, possibly as the result of age-related changes in renal function. Since geriatric patients may be more likely to have decreased renal function, select dosage with caution; it also may be useful to monitor renal function in geriatric patients.
The following prioritized warning is available for ENTECAVIR (entecavir):
WARNING: Rarely, entecavir may cause serious (possibly fatal) liver problems and lactic acid build-up in the blood (lactic acidosis). Get medical help right away if you have any of the following symptoms: nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine, unusual tiredness/weakness, deep/fast breathing, unusual drowsiness, unusual muscle pain, feeling cold in your arms/legs, fast/irregular heartbeat. These side effects may occur more often in women and obese patients.
Your hepatitis B infection may get worse if you stop taking entecavir. Do not stop this medication without talking to your doctor. Your doctor will do blood tests to check your liver for several months after you stop entecavir.
This medication is not recommended if you have both HIV and hepatitis B and are not receiving effective treatment for HIV. This drug does not treat HIV, and it can cause certain HIV medications to become ineffective. Get an HIV test before starting this medication, and get tested again anytime you may have become infected. Consult your doctor for more details.
WARNING: Rarely, entecavir may cause serious (possibly fatal) liver problems and lactic acid build-up in the blood (lactic acidosis). Get medical help right away if you have any of the following symptoms: nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine, unusual tiredness/weakness, deep/fast breathing, unusual drowsiness, unusual muscle pain, feeling cold in your arms/legs, fast/irregular heartbeat. These side effects may occur more often in women and obese patients.
Your hepatitis B infection may get worse if you stop taking entecavir. Do not stop this medication without talking to your doctor. Your doctor will do blood tests to check your liver for several months after you stop entecavir.
This medication is not recommended if you have both HIV and hepatitis B and are not receiving effective treatment for HIV. This drug does not treat HIV, and it can cause certain HIV medications to become ineffective. Get an HIV test before starting this medication, and get tested again anytime you may have become infected. Consult your doctor for more details.
The following icd codes are available for ENTECAVIR (entecavir)'s list of indications:
| Chronic hepatitis B | |
| B18.0 | Chronic viral hepatitis B with delta-agent |
| B18.1 | Chronic viral hepatitis B without delta-agent |
| Lamivudine-refractory chronic hepatitis B | |
| B18.0 | Chronic viral hepatitis B with delta-agent |
| B18.1 | Chronic viral hepatitis B without delta-agent |
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