Abacavir And Lamivudine

What is Abacavir And Lamivudine?

11 DESCRIPTION Abacavir and Lamivudine Tablets USP Abacavir and lamivudine tablets USP contain the following 2 synthetic nucleoside analogues: abacavir (ZIAGEN, also a component of TRIZIVIR ® ) and lamivudine (also known as EPIVIR or 3TC) with inhibitory activity against HIV-1. Abacavir and lamivudine tablets USP are for oral administration. Each orange colored, oval shaped, biconvex, film-coated tablet contains the active ingredients 600 mg of abacavir as abacavir sulfate and 300 mg of lamivudine, and the inactive ingredients crospovidone, magnesium stearate, microcrystalline cellulose, and povidone. The tablets are coated with a film that is made of FD&C Yellow No. 6, hypromellose, polyethylene glycol, polysorbate, and titanium dioxide. Abacavir Sulfate The chemical name of abacavir sulfate is (1S,4R)- 4-[2-Amino-6-(cyclopropylamino) -9H- purin-9-yl]-2-cyclopentene-1-methanol sulfate (2:1). Abacavir sulfate is the enantiomer with 1S, 4R absolute configuration on the cyclopentene ring. It has a molecular formula of (C 14 H 18 N 6 O) 2 . H 2 SO 4 and a molecular weight of 670.74 g per mol. It has the following structural formula: Abacavir sulfate is a white to off-white solid with

Uses of Abacavir And Lamivudine

Established uses

1 INDICATIONS AND USAGE Abacavir and lamivudine tablet, a combination of abacavir and lamivudine, both nucleoside analogue HIV-1 reverse transcriptase inhibitors, is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.
( 1 ) Abacavir and lamivudine tablets, in combination with other antiretroviral agents, are indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection.

How Abacavir And Lamivudine works

In more detail: 12.1 Mechanism of Action Abacavir and lamivudine tablet is an antiretroviral agent with activity against HIV-1 [see Microbiology ( 12.4 )]. Mechanism of Action Abacavir: Abacavir is a carbocyclic synthetic nucleoside analogue. Abacavir is converted by cellular enzymes to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5'-triphosphate (dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Lamivudine: Lamivudine is a synthetic nucleoside analogue. Intracellularly lamivudine is phosphorylated to its active 5'-triphosphate metabolite, lamivudine triphosphate (3TC-TP). The principal mode of action of 3TC-TP is inhibition of RT via DNA chain termination after incorporation of the nucleotide analogue.

How to take Abacavir And Lamivudine

2 DOSAGE AND ADMINISTRATION Before initiating abacavir and lamivudine tablets, screen for the HLA-B*5701 allele because abacavir and lamivudine tablets contains abacavir. ( 2.1 ) Adults: One tablet orally once daily. ( 2.2 ) Pediatric patients weighing at least 25 kg: One tablet daily. ( 2.3 ) Because abacavir and lamivudine tablets is a fixed-dose tablet and cannot be dose adjusted, abacavir and lamivudine tablets is not recommended in patients with creatinine clearance less than 30 mL per minute or patients with hepatic impairment. ( 2.4 , 4 ) 2.1 Screening for HLA-B*5701 Allele Prior to Starting Abacavir and Lamivudine Tablets Screen for the HLA-B*5701 allele prior to initiating therapy with abacavir and lamivudine tablets [see Boxed Warning , Warnings and Precautions ( 5.1 )] . 2.2 Recommended Dosage for Adult Patients The recommended dosage of abacavir and lamivudine tablets for adults is one tablet taken orally once daily, in combination with other antiretroviral agents, with or without food. 2.3 Recommended Dosage for Pediatric Patients The recommended oral dose of abacavir and lamivudine tablets for pediatric patients weighing at least 25 kg is one tablet daily in combinati

Dosage

Follow the dose prescribed by your doctor or pharmacist. The ranges below are general information, not a personal prescription.

Adults: 2 DOSAGE AND ADMINISTRATION Before initiating abacavir and lamivudine tablets, screen for the HLA-B*5701 allele because abacavir and lamivudine tablets contains abacavir. ( 2.1 ) Adults: One tablet orally once daily. ( 2.2 ) Pediatric patients weighing at least 25 kg: One tablet daily. ( 2.3 ) Because abacavir and lamivudine tablets is a fixed-dose tablet and cannot be dose adjusted, abacavir and lamivudine tablets is not recommended in patients with creatinine clearance less than 30 mL per minute or patients with hepatic impairment. ( 2.4 , 4 ) 2.1 Screening for HLA-B*5701 Allele Prior to Starting Abacavir and Lamivudine Tablets Screen for the HLA-B*5701 allele prior to initiating therapy with abacavir and lamivudine tablets [see Boxed Warning , Warnings and Precautions ( 5.1 )] . 2.2 Recommended Dosage for Adult Patients The recommended dosage of abacavir and lamivudine tablets for adults is one tablet taken orally once daily, in combination with other antiretroviral agents, with or without food. 2.3 Recommended Dosage for Pediatric Patients The recommended oral dose of abacavir and lamivudine tablets for pediatric patients weighing at least 25 kg is one tablet daily in combinati

Side effects of Abacavir And Lamivudine

Common

6 ADVERSE REACTIONS The most commonly reported adverse reactions of at least moderate intensity (incidence greater than 5%) in an adult HIV-1 clinical trial were drug hypersensitivity, insomnia, depression/depressed mood, headache/migraine, fatigue/malaise, dizziness/vertigo, nausea, and diarrhea.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Lupin Pharmaceuticals, Inc.
at 1-800-399-2561 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
The following adverse reactions are discussed in greater detail in other sections of the labeling: Serious and sometimes fatal hypersensitivity reactions [see Boxed Warning, Warnings and Precautions ( 5.1 )].
Exacerbations of hepatitis B [see Boxed Warning, Warnings and Precautions ( 5.2 )].
Lactic acidosis and severe hepatomegaly with steatosis [see Warnings and Precautions ( 5.3 )].

Warnings and who should not take it

Who should NOT take Abacavir And Lamivudine?

4 CONTRAINDICATIONS Presence of HLA-B*5701 allele.
( 4 ) Prior hypersensitivity reaction to abacavir or lamivudine.
( 4 ) Moderate or severe hepatic impairment.
( 4 , 8.7 ) Abacavir and lamivudine tablets are contraindicated in patients: who have the HLA-B*5701 allele [see Warnings and Precautions ( 5.1 )].
with prior hypersensitivity reaction to abacavir [see Warnings and Precautions ( 5.1 )] or lamivudine.
with moderate or severe hepatic impairment [see Use in Specific Populations ( 8.7 )].

Overdose

10 OVERDOSAGE There is no known specific treatment for overdose with abacavir and lamivudine tablets. If overdose occurs, the patient should be monitored, and standard supportive treatment applied as required. Abacavir It is not known whether abacavir can be removed by peritoneal dialysis or hemodialysis. Lamivudine Because a negligible amount of lamivudine was removed via (4-hour) hemodialysis, continuous ambulatory peritoneal dialysis, and automated peritoneal dialysis, it is not known if continuous hemodialysis would provide clinical benefit in a lamivudine overdose event.

Safety at a glance

PregnancyCaution

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to abacavir and lamivudine tablets during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Available data from the (APR) show no difference in the overall risk of birth defects for abacavir or lamivudine compared with the background rate for birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population (see Data) . The APR uses the MACDP as the U.S. reference population for birth defects in the general population. The MACDP evaluates women and infants from a limited geographic area and does not include outcomes for births that occurred at less than 20 weeks gestation. The rate of miscarriage is not reported in the APR. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15% to 20%. The background risk for major birth defects and miscarriage for the indicated population is unknown. In animal reproduction studies, oral administration of abacavir

Children and elderly

Children

8.4 Pediatric Use The dosing recommendations in this population are based on the safety and efficacy established in a controlled trial conducted using either the combination of EPIVIR and ZIAGEN or abacavir and lamivudine tablets [see Dosage and Administration ( 2.3 ), Adverse Reactions ( 6.2 ), Clinical Studies ( 14.2 )] . In pediatric patients weighing less than 25 kg, use of abacavir and lamivudine as single products is recommended to achieve appropriate dosing.

Elderly

8.5 Geriatric Use Clinical trials of abacavir and lamivudine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, caution should be exercised in the administration of abacavir and lamivudine tablets in elderly patients reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy [see Dosage and Administration ( 2.4 ), Use in Specific Populations ( 8.6 , 8.7 )].

Interactions

Medicine and medicine

7 DRUG INTERACTIONS Methadone: An increased methadone dose may be required in a small number of patients.
( 7.1 ) Sorbitol: Coadministration of lamivudine and sorbitol may decrease lamivudine concentrations;
when possible, avoid chronic coadministration.
( 7.2 ) Riociguat: The riociguat dose may need to be reduced.
( 7.3 ) 7.1 Methadone In a trial of 11 HIV-1-infected subjects receiving methadone-maintenance therapy with 600 mg of ZIAGEN twice daily (twice the currently recommended dose), oral methadone clearance increased [see Clinical Pharmacology ( 12.3 )] .
This alteration will not result in a methadone dose modification in the majority of patients;

Frequently asked questions

What is Abacavir And Lamivudine used for?

1 INDICATIONS AND USAGE Abacavir and lamivudine tablet, a combination of abacavir and lamivudine, both nucleoside analogue HIV-1 reverse transcriptase inhibitors, is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection., ( 1 ) Abacavir and lamivudine tablets, in combination with other antiretroviral agents, are indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection..

How should I take Abacavir And Lamivudine?

2 DOSAGE AND ADMINISTRATION Before initiating abacavir and lamivudine tablets, screen for the HLA-B*5701 allele because abacavir and lamivudine tablets contains abacavir. ( 2.1 ) Adults: One tablet orally once daily. ( 2.2 ) Pediatric patients weighing at least 25 kg: One tablet daily. ( 2.3 ) Because abacavir and lamivudine tablets is a fixed-dose tablet and cannot be dose adjusted, abacavir and lamivudine tablets is not recommended in patients with creatinine clearance less than 30 mL per minute or patients with hepatic impairment. ( 2.4 , 4 ) 2.1 Screening for HLA-B*5701 Allele Prior to Starting Abacavir and Lamivudine Tablets Screen for the HLA-B*5701 allele prior to initiating therapy with abacavir and lamivudine tablets [see Boxed Warning , Warnings and Precautions ( 5.1 )] . 2.2 Recommended Dosage for Adult Patients The recommended dosage of abacavir and lamivudine tablets for adults is one tablet taken orally once daily, in combination with other antiretroviral agents, with or without food. 2.3 Recommended Dosage for Pediatric Patients The recommended oral dose of abacavir and lamivudine tablets for pediatric patients weighing at least 25 kg is one tablet daily in combinati

What are the common side effects?

6 ADVERSE REACTIONS The most commonly reported adverse reactions of at least moderate intensity (incidence greater than 5%) in an adult HIV-1 clinical trial were drug hypersensitivity, insomnia, depression/depressed mood, headache/migraine, fatigue/malaise, dizziness/vertigo, nausea, and diarrhea., ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Lupin Pharmaceuticals, Inc., at 1-800-399-2561 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch., The following adverse reactions are discussed in greater detail in other sections of the labeling: Serious and sometimes fatal hypersensitivity reactions [see Boxed Warning, Warnings and Precautions ( 5.1 )]., Exacerbations of hepatitis B [see Boxed Warning, Warnings and Precautions ( 5.2 )]., Lactic acidosis and severe hepatomegaly with steatosis [see Warnings and Precautions ( 5.3 )]..

Who should not take Abacavir And Lamivudine?

4 CONTRAINDICATIONS Presence of HLA-B*5701 allele.; ( 4 ) Prior hypersensitivity reaction to abacavir or lamivudine.; ( 4 ) Moderate or severe hepatic impairment.; ( 4 , 8.7 ) Abacavir and lamivudine tablets are contraindicated in patients: who have the HLA-B*5701 allele [see Warnings and Precautions ( 5.1 )].; with prior hypersensitivity reaction to abacavir [see Warnings and Precautions ( 5.1 )] or lamivudine.; with moderate or severe hepatic impairment [see Use in Specific Populations ( 8.7 )]..

Can I take Abacavir And Lamivudine during pregnancy?

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to abacavir and lamivudine tablets during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Available data from the (APR) show no difference in the overall risk of birth defects for abacavir or lamivudine compared with the background rate for birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population (see Data) . The APR uses the MACDP as the U.S. reference population for birth defects in the general population. The MACDP evaluates women and infants from a limited geographic area and does not include outcomes for births that occurred at less than 20 weeks gestation. The rate of miscarriage is not reported in the APR. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15% to 20%. The background risk for major birth defects and miscarriage for the indicated population is unknown. In animal reproduction studies, oral administration of abacavir

Can children take Abacavir And Lamivudine?

8.4 Pediatric Use The dosing recommendations in this population are based on the safety and efficacy established in a controlled trial conducted using either the combination of EPIVIR and ZIAGEN or abacavir and lamivudine tablets [see Dosage and Administration ( 2.3 ), Adverse Reactions ( 6.2 ), Clinical Studies ( 14.2 )] . In pediatric patients weighing less than 25 kg, use of abacavir and lamivudine as single products is recommended to achieve appropriate dosing.

Does Abacavir And Lamivudine interact with other medicines?

7 DRUG INTERACTIONS Methadone: An increased methadone dose may be required in a small number of patients.; ( 7.1 ) Sorbitol: Coadministration of lamivudine and sorbitol may decrease lamivudine concentrations;; when possible, avoid chronic coadministration.; ( 7.2 ) Riociguat: The riociguat dose may need to be reduced.; ( 7.3 ) 7.1 Methadone In a trial of 11 HIV-1-infected subjects receiving methadone-maintenance therapy with 600 mg of ZIAGEN twice daily (twice the currently recommended dose), oral methadone clearance increased [see Clinical Pharmacology ( 12.3 )] .; This alteration will not result in a methadone dose modification in the majority of patients;.