ZIAGEN abacavir sulfate 20 mg/mL Solution
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Abacavir is used to treat human immunodeficiency virus (HIV) infection. Abacavir is in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). It works by decreasing the amount of HIV in the blood. Although abacavir does not cure HIV, it may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses. Taking these medications and making other lifestyle changes may decrease the risk of giving the HIV virus to other people.
Read the full MedlinePlus article ↗- Abacavir works by blocking a key step HIV uses to copy itself inside your cells. But HIV is clever — if you use just one medicine, the virus can mutate and find a workaround. Using...
- What exactly does abacavir do, and why do I have to take it with other HIV medicines?
- Yes, and this one is really important. Before you start abacavir, your doctor will test you for a gene variant called HLA-B*5701. People who carry this variant are at much higher r...
- I heard there's a genetic test I need before starting — what is that about?
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🧪 Inactive Ingredients / Excipients
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UNII XF417D3PSL
Anhydrous citric acid is a sour, crystalline powder derived from citric acid with water removed. In medicines, it acts as a buffer to control pH, adds tartness to improve taste, and helps tablets disintegrate.
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Methylparaben is a preservative derived from benzoic acid that prevents growth of bacteria, fungi, and mold in medicines. It extends the product's shelf life and maintains safety during storage.
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Propylene glycol is a clear liquid derived from petroleum or vegetable sources. It acts as a solvent, humectant, and preservative in medicines, helping dissolve active ingredients and maintain product stability.
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Propylparaben is a chemical preservative used to prevent bacterial and fungal growth in medicines and personal care products. It helps extend shelf life and maintain product safety during storage.
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Saccharin sodium is an artificial sweetener made from saccharin salt. It's added to medicines to improve taste, especially in liquid formulations for children or bitter drugs.
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Sorbitol is a natural sugar alcohol derived from glucose. It serves as a sweetener, humectant, and bulking agent in medications to improve taste and help maintain moisture in the product.
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UNII B22547B95K
A salt derived from citric acid that helps maintain the proper acid-base balance in the medicine. It's used as a buffer to keep the product stable and at the right pH level.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
8 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $0.6030 | $144.72 / 240 ml |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Abacavir 20 mg/mL 31722-0562-24 | Camber | 240 ml | — | AA | FDA listed | — |
| Ziagen 20 mg/mLthis 49702-0222-48 | ViiV | 1 bottle | — | AA | FDA listed | — |
| Abacavir 20 mg/mL 64980-0405-24 | Rising | 1 bottle | — | AA | FDA listed | — |
| Abacavir 20 mg/mL 65862-0089-24 | Aurobindo | 1 bottle | — | AA | FDA listed | — |
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⏳ Availability & generic status
The FDA lists approved generic versions of this medicine, but that does not always mean a pharmacy can get one today. Patent rules, launch agreements, supply and pricing can affect when generics actually arrive.
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📊 Medicare Part D spend CMS · PART D · 2025 (Q1-Q4)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
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Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 49702-0222-48 You're viewing this | 1 BOTTLE in 1 CARTON (49702-222-48) / 240 mL in 1 BOTTLE | 1999-01-28 | Active |
🧭 About this NDC listing & data coverage
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING: HYPERSENSITIVITY REACTIONS Serious and sometimes fatal hypersensitivity reactions, with multiple organ involvement, have occurred with ZIAGEN (abacavir). Patients who carry the HLA ‑ B*5701 allele are at a higher risk of a hypersensitivity reaction to abacavir; although, hypersensitivity reactions have occurred in patients who do not carry the HLA ‑ B*5701 allele [see Warnings and Precautions ( 5.1 )] . ZIAGEN is contraindicated in patients with a prior hypersensitivity reaction to abacavir and in HLA ‑ B*5701-positive patients [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 )] .
All patients should be screened for the HLA ‑ B*5701 allele prior to initiating therapy with ZIAGEN or reinitiation of therapy with ZIAGEN, unless patients have a previously documented HLA ‑ B*5701 allele assessment. Discontinue ZIAGEN immediately if a hypersensitivity reaction is suspected, regardless of HLA-B*5701 status and even when other diagnoses are possible [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 ) ]. Following a hypersensitivity reaction to ZIAGEN, NEVER restart ZIAGEN or any other abacavir-containing product because more severe symptoms, including death can occur within hours.
Similar severe reactions have also occurred rarely following the reintroduction of abacavir-containing products in patients who have no history of abacavir hypersensitivity [see Warnings and Precautions ( 5.1 )] . WARNING: HYPERSENSITIVITY REACTIONS See full prescribing information for complete boxed warning. • Serious and sometimes fatal hypersensitivity reactions have occurred with ZIAGEN (abacavir). ( 5.1 ) • Hypersensitivity to ZIAGEN is a multi-organ clinical syndrome.
( 5.1 ) • Patients who carry the HLA-B*5701 allele are at a higher risk of experiencing a hypersensitivity reaction to abacavir. ( 5.1 ) • ZIAGEN is contraindicated in patients with a prior hypersensitivity reaction to abacavir and in HLA-B*5701-positive patients. ( 4 ) • Discontinue ZIAGEN as soon as a hypersensitivity reaction is suspected.
Regardless of HLA-B*5701 status, permanently discontinue ZIAGEN if hypersensitivity cannot be ruled out, even when other diagnoses are possible. ( 5.1 ) • Following a hypersensitivity reaction to ZIAGEN, NEVER restart ZIAGEN or any other abacavir-containing product. ( 5.1 )
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE ZIAGEN tablets and oral solution, in combination with other antiretroviral agents, are indicated for the treatment of human immunodeficiency virus (HIV-1) infection. ZIAGEN, a nucleoside analogue human immunodeficiency virus (HIV-1) reverse transcriptase inhibitor, is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION • Before initiating ZIAGEN, screen for the HLA-B*5701 allele. ( 2.1 ) • Adults: 600 mg daily, administered as either 300 mg twice daily or 600 mg once daily. ( 2.2 ) • Pediatric Patients Aged 3 Months and Older: Administered either once or twice daily. Dose should be calculated on body weight (kg) and should not exceed 600 mg daily. ( 2.3 ) • Patients with Hepatic Impairment: Mild hepatic impairment – 200 mg twice daily. ( 2.4 )
2.1Screening for HLA-B*5701 Allele prior to Starting ZIAGEN Screen for the HLA‑B*5701 allele prior to initiating therapy with ZIAGEN [see Boxed Warning, Warnings and Precautions ( 5.1 )].
2.2Recommended Dosage for Adult Patients The recommended dosage of ZIAGEN for adults is 600 mg daily, administered orally as either 300 mg twice daily or 600 mg once daily, in combination with other antiretroviral agents.
2.3Recommended Dosage for Pediatric Patients The recommended dosage of ZIAGEN oral solution in HIV-1–infected pediatric patients aged 3 months and older is 8 mg per kg orally twice daily or 16 mg per kg orally once daily (up to a maximum of 600 mg daily) in combination with other antiretroviral agents. ZIAGEN is also available as a scored tablet for HIV-1–infected pediatric patients weighing greater than or equal to 14 kg for whom a solid dosage form is appropriate. Before prescribing ZIAGEN tablets, children should be assessed for the ability to swallow tablets.
If a child is unable to reliably swallow ZIAGEN tablets, the oral solution formulation should be prescribed. The recommended oral dosage of ZIAGEN tablets for HIV-1–infected pediatric patients is presented in Table 1 . Table 1.
Dosing Recommendations for ZIAGEN Scored Tablets in Pediatric Patients a Data regarding the efficacy of once-daily dosing is limited to subjects who transitioned from twice-daily dosing to once-daily dosing after 36 weeks of treatment [see Clinical Studies ( 14.2 )]. Weight (kg) Once-Daily Dosing Regimen a Twice-Daily Dosing Regimen AM Dose PM Dose Total Daily Dose 14 to <20 1 tablet (300 mg) ½ tablet (150 mg) ½ tablet (150 mg) 300 mg ≥20 to <25 1½ tablets (450 mg) ½ tablet (150 mg) 1 tablet (300 mg) 450 mg ≥25 2 tablets (600 mg) 1 tablet (300 mg) 1 tablet (300 mg) 600 mg
2.4Recommended Dosage for Patients with Hepatic Impairment The recommended dose of ZIAGEN in patients with mild hepatic impairment (Child‑Pugh Class A) is 200 mg twice daily. To enable dose reduction, ZIAGEN oral solution (10 mL twice daily) should be used for the treatment of these patients. The safety, efficacy, and pharmacokinetic properties of abacavir have not been established in patients with moderate to severe hepatic impairment; therefore, ZIAGEN is contraindicated in these patients.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS ZIAGEN tablets contain 300 mg of abacavir as abacavir sulfate. The tablets are yellow, biconvex, scored, capsule-shaped, film-coated, and imprinted with “GX 623” on both sides. ZIAGEN oral solution contains 20 mg per mL of abacavir as abacavir sulfate.
The solution is a clear to opalescent, yellowish, strawberry-banana-flavored liquid, which may turn brown over time. • Tablets: 300 mg scored ( 3 ) • Oral Solution: 20 mg per mL ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS ZIAGEN is 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 )]. • with moderate or severe hepatic impairment [see Use in Specific Populations ( 8.6 )]. • Presence of HLA-B*5701 allele. ( 4 ) • Prior hypersensitivity reaction to abacavir. ( 4 ) • Moderate or severe hepatic impairment. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues. ( 5.2 ) • Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy. ( 5.3 )
5.1Hypersensitivity Reactions Serious and sometimes fatal hypersensitivity reactions have occurred with ZIAGEN (abacavir). These hypersensitivity reactions have included multi-organ failure and anaphylaxis and typically occurred within the first 6 weeks of treatment with ZIAGEN (median time to onset was 9 days); although abacavir hypersensitivity reactions have occurred any time during treatment [see Adverse Reactions ( 6.1 ) ]. Patients who carry the HLA-B*5701 allele are at a higher risk of abacavir hypersensitivity reactions; although, patients who do not carry the HLA‑B*5701 allele have developed hypersensitivity reactions.
Hypersensitivity to abacavir was reported in approximately 206 (8%) of 2,670 patients in 9 clinical trials with abacavir-containing products where HLA‑B*5701 screening was not performed. The incidence of suspected abacavir hypersensitivity reactions in clinical trials was 1% when subjects carrying the HLA‑B*5701 allele were excluded. In any patient treated with abacavir, the clinical diagnosis of hypersensitivity reaction must remain the basis of clinical decision making.
Due to the potential for severe, serious, and possibly fatal hypersensitivity reactions with ZIAGEN: • All patients should be screened for the HLA‑B*5701 allele prior to initiating therapy with ZIAGEN or reinitiation of therapy with ZIAGEN, unless patients have a previously documented HLA‑B*5701 allele assessment. • ZIAGEN is contraindicated in patients with a prior hypersensitivity reaction to abacavir and in HLA‑B*5701-positive patients. • Before starting ZIAGEN, review medical history for prior exposure to any abacavir-containing product.
NEVER restart ZIAGEN or any other abacavir‑containing product following a hypersensitivity reaction to abacavir, regardless of HLA‑B*5701 status. • To reduce the risk of a life-threatening hypersensitivity reaction, regardless of HLA-B*5701 status, discontinue ZIAGEN immediately if a hypersensitivity reaction is suspected, even when other diagnoses are possible (e.g., acute onset respiratory diseases such as pneumonia, bronchitis, pharyngitis, or influenza; gastroenteritis; or reactions to other medications). • If a hypersensitivity reaction cannot be ruled out, do not restart ZIAGEN or any other abacavir-containing products because more severe symptoms which may include life-threatening hypotension and death, can occur within hours. • If a hypersensitivity reaction is ruled out, patients may restart ZIAGEN.
Rarely, patients who have stopped abacavir for reasons other than symptoms of hypersensitivity have also experienced life-threatening reactions within hours of reinitiating abacavir therapy. Therefore, reintroduction of ZIAGEN or any other abacavir-containing product is recommended only if medical care can be readily accessed. • A Medication Guide and Warning Card that provide information about recognition of hypersensitivity reactions should be dispensed with each new prescription and refill.
5.2Lactic Acidosis and Severe Hepatomegaly with Steatosis Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues, including ZIAGEN. A majority of these cases have been in women. Female sex and obesity may be risk factors for the development of lactic acidosis and severe hepatomegaly with steatosis in patients treated with antiretroviral nucleoside analogues.
Treatment with ZIAGEN should be suspended in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity, which may include hepatomegaly and steatosis even in the absence of marked transaminase elevations.
5.3 Immune Reconstitut…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: • Serious and sometimes fatal hypersensitivity reactions [see Boxed Warning, Warnings and Precautions ( 5.1 )] . • Lactic acidosis and severe hepatomegaly with steatosis [see Warnings and Precautions ( 5.2 )] . • Immune reconstitution syndrome [see Warnings and Precautions ( 5.3 )] . • Myocardial infarction [see Warnings and Precautions ( 5.4 )] . • The most commonly reported adverse reactions of at least moderate intensity (incidence greater than or equal to 10%) in adult HIV-1 clinical trials were nausea, headache, malaise and fatigue, nausea and vomiting, and dreams/sleep disorders.
( 6.1 ) • The most commonly reported adverse reactions of at least moderate intensity (incidence greater than or equal to 5%) in pediatric HIV-1 clinical trials were fever and/or chills, nausea and vomiting, skin rashes, and ear/nose/throat infections. ( 6.2 ) To report SUSPECTED ADVERSE REACTIONS, contact ViiV Healthcare at 1-877-844-8872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience in Adult Subjects Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Serious and Fatal Abacavir-Associated Hypersensitivity Reactions In clinical trials, serious and sometimes fatal hypersensitivity reactions have occurred with abacavir [see Boxed Warning, Warnings and Precautions ( 5.1 )].
These reactions have been characterized by 2 or more of the following signs or symptoms: (1) fever; (2) rash; (3) gastrointestinal symptoms (including nausea, vomiting, diarrhea, or abdominal pain); (4) constitutional symptoms (including generalized malaise, fatigue, or achiness); (5) respiratory symptoms (including dyspnea, cough, or pharyngitis). Almost all abacavir hypersensitivity reactions include fever and/or rash as part of the syndrome. Other signs and symptoms have included lethargy, headache, myalgia, edema, arthralgia, and paresthesia.
Anaphylaxis, liver failure, renal failure, hypotension, adult respiratory distress syndrome, respiratory failure, myolysis, and death have occurred in association with these hypersensitivity reactions. Physical findings have included lymphadenopathy, mucous membrane lesions (conjunctivitis and mouth ulcerations), and maculopapular or urticarial rash (although some patients had other types of rashes and others did not have a rash). There were reports of erythema multiforme.
Laboratory abnormalities included elevated liver chemistries, elevated creatine phosphokinase, elevated creatinine, and lymphopenia, and abnormal chest x-ray findings (predominantly infiltrates, which were localized). Additional Adverse Reactions with Use of ZIAGEN Therapy-Naive Adults: Treatment-emergent clinical adverse reactions (rated by the investigator as moderate or severe) with a greater than or equal to 5% frequency during therapy with ZIAGEN 300 mg twice daily, lamivudine 150 mg twice daily, and efavirenz 600 mg daily compared with zidovudine 300 mg twice daily, lamivudine 150 mg twice daily, and efavirenz 600 mg daily from CNA30024 are listed in Table 2 .
Table 2. Treatment-Emergent (All Causality) Adverse Reactions of at Least Moderate Intensity (Grades 2-4, Greater than or Equal to 5% Frequency) in Therapy-Naive Adults (CNA30024 a ) through 48 Weeks of Treatment a This trial used double-blind ascertainment of suspected hypersensitivity reactions. During the blinded portion of the trial, suspected hypersensitivity to abacavir was reported by investigators in 9% of 324 subjects in the abacavir group and 3% of 325 subjects in the zidovudine group. b Ten (3%) cases of suspected drug hypersensitivity were reclassified as not being due to abacavir following unblinding.
Adverse Reaction ZIAGEN plus Lamivudine…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS • Methadone: An increased methadone dose may be required in a small number of patients. ( 7.1 ) • Riociguat: The riociguat dose may need to be reduced. ( 7.2 )
7.1Methadone 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; however, an increased methadone dose may be required in a small number of patients.
7.2Riociguat Coadministration with fixed-dose abacavir/dolutegravir/lamivudine resulted in increased riociguat exposure, which may increase the risk of riociguat adverse reactions [see Clinical Pharmacology ( 12.3 )] . The riociguat dose may need to be reduced. See full prescribing information for ADEMPAS (riociguat).
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS • Lactation: Women infected with HIV should be instructed not to breastfeed due to potential for HIV transmission. ( 8.2 )
8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ZIAGEN 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 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 to pregnant rats during organogenesis resulted in fetal malformations and other embryonic and fetal toxicities at exposures 35 times the human exposure (AUC) at the recommended clinical daily dose.
However, no adverse developmental effects were observed following oral administration of abacavir to pregnant rabbits during organogenesis, at exposures approximately 9 times the human exposure (AUC) at the recommended clinical dose (see Data) . Data Human Data: Based on prospective reports to the APR of exposures to abacavir during pregnancy resulting in live births (including over 1,300 exposed in the first trimester and over 1,300 exposed in the second/third trimester), there was no difference between the overall risk of birth defects for abacavir compared with the background birth defect rate of 2.7% in the U.S. reference population of the MACDP.
The prevalence of defects in live births was 3.2% (95% CI: 2.3% to 4.3%) following first trimester exposure to abacavir-containing regimens and 2.9% (95% CI: 2.1% to 4.0%) following second/third trimester exposure to abacavir-containing regimens. Abacavir has been shown to cross the placenta and concentrations in neonatal plasma at birth were essentially equal to those in maternal plasma at delivery [see Clinical Pharmacology ( 12.3 )] . Animal Data: Abacavir was administered orally to pregnant rats (at 100, 300, and 1,000 mg per kg per day) and rabbits (at 125, 350, or 700 mg per kg per day) during organogenesis (on Gestation Days 6 through 17 and 6 through 20, respectively).
Fetal malformations (increased incidences of fetal anasarca and skeletal malformations) or developmental toxicity (decreased fetal body weight and crown‑rump length) were observed in rats at doses up to 1,000 mg per kg per day, resulting in exposures approximately 35 times the human exposure (AUC) at the recommended daily dose. No developmental effects were observed in rats at 100 mg per kg per day, resulting in exposures (AUC) 3.5 times the human exposure at the recommended daily dose. In a fertility and early embryo-fetal development study conducted in rats (at 60, 160, or 500 mg per kg per day), embryonic and fetal toxicities (increased resorptions, decreased fetal body weights) or toxicities to the offspring (increased incidence of stillbirth and lower body weights) occurred at doses up to 500 mg per kg per day.
No developmental effects were observed in rats at 60 mg per kg per day, resulting in exposures (AUC) approximately 4 times the human exposure at the recommended daily dose. Studies in pregnant rats showed that abacavir is transferred to the fetus through the placenta. In pregnant rabbits, no developmental toxiciti…
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ZIAGEN 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 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 to pregnant rats during organogenesis resulted in fetal malformations and other embryonic and fetal toxicities at exposures 35 times the human exposure (AUC) at the recommended clinical daily dose.
However, no adverse developmental effects were observed following oral administration of abacavir to pregnant rabbits during organogenesis, at exposures approximately 9 times the human exposure (AUC) at the recommended clinical dose (see Data) . Data Human Data: Based on prospective reports to the APR of exposures to abacavir during pregnancy resulting in live births (including over 1,300 exposed in the first trimester and over 1,300 exposed in the second/third trimester), there was no difference between the overall risk of birth defects for abacavir compared with the background birth defect rate of 2.7% in the U.S. reference population of the MACDP.
The prevalence of defects in live births was 3.2% (95% CI: 2.3% to 4.3%) following first trimester exposure to abacavir-containing regimens and 2.9% (95% CI: 2.1% to 4.0%) following second/third trimester exposure to abacavir-containing regimens. Abacavir has been shown to cross the placenta and concentrations in neonatal plasma at birth were essentially equal to those in maternal plasma at delivery [see Clinical Pharmacology ( 12.3 )] . Animal Data: Abacavir was administered orally to pregnant rats (at 100, 300, and 1,000 mg per kg per day) and rabbits (at 125, 350, or 700 mg per kg per day) during organogenesis (on Gestation Days 6 through 17 and 6 through 20, respectively).
Fetal malformations (increased incidences of fetal anasarca and skeletal malformations) or developmental toxicity (decreased fetal body weight and crown‑rump length) were observed in rats at doses up to 1,000 mg per kg per day, resulting in exposures approximately 35 times the human exposure (AUC) at the recommended daily dose. No developmental effects were observed in rats at 100 mg per kg per day, resulting in exposures (AUC) 3.5 times the human exposure at the recommended daily dose. In a fertility and early embryo-fetal development study conducted in rats (at 60, 160, or 500 mg per kg per day), embryonic and fetal toxicities (increased resorptions, decreased fetal body weights) or toxicities to the offspring (increased incidence of stillbirth and lower body weights) occurred at doses up to 500 mg per kg per day.
No developmental effects were observed in rats at 60 mg per kg per day, resulting in exposures (AUC) approximately 4 times the human exposure at the recommended daily dose. Studies in pregnant rats showed that abacavir is transferred to the fetus through the placenta. In pregnant rabbits, no developmental toxicities and no increases in fetal malformations occurred at up to the highest dose evaluated, resulting in exposures (AUC) approximately 9 times the human exp…
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of ZIAGEN have been established in pediatric patients aged 3 months and older. Use of ZIAGEN is supported by pharmacokinetic trials and evidence from adequate and well-controlled trials of ZIAGEN in adults and pediatric subjects [see Dosage and Administration ( 2.3 ), Adverse Reactions ( 6.2 ), Clinical Pharmacology ( 12.3 ), Clinical Studies ( 14.2 )] .
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical trials of ZIAGEN 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 ZIAGEN in elderly patients reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
🆘 Overdosage ▾
10 OVERDOSAGE There is no known specific treatment for overdose with ZIAGEN. If overdose occurs, the patient should be monitored and standard supportive treatment applied as required. It is not known whether abacavir can be removed by peritoneal dialysis or hemodialysis.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Abacavir is an antiretroviral agent [see Microbiology ( 12.4 )] .
12.3Pharmacokinetics Pharmacokinetics in Adults The pharmacokinetic properties of abacavir were independent of dose over the range of 300 to 1,200 mg per day. Absorption: Following oral administration, abacavir is rapidly absorbed and extensively distributed. The geometric mean absolute bioavailability of the tablet was 83%.
Plasma abacavir AUC was similar following administration of the oral solution or tablets. After oral administration of 300 mg twice daily in 20 subjects, the steady-state peak serum abacavir concentration (C max ) was 3.0 ± 0.89 mcg per mL (mean ± SD) and AUC (0-12 h) was 6.02 ± 1.73 mcg•hour per mL. After oral administration of a single dose of 600 mg of abacavir in 20 subjects, C max was 4.26 ± 1.19 mcg per mL (mean ± SD) and AUC ∞ was 11.95 ± 2.51 mcg•hour per mL.
Effect of Food: Bioavailability of abacavir tablets was assessed in the fasting and fed states with no significant difference in systemic exposure (AUC ∞ ); therefore, ZIAGEN tablets may be administered with or without food. Systemic exposure to abacavir was comparable after administration of ZIAGEN oral solution and ZIAGEN tablets. Therefore, these products may be used interchangeably.
Distribution: The apparent volume of distribution after IV administration of abacavir was 0.86 ±
0.15L per kg, suggesting that abacavir distributes into extravascular space. In 3 subjects, the CSF AUC (0-6 h) to plasma abacavir AUC (0-6 h) ratio ranged from 27% to 33%. Binding of abacavir to human plasma proteins is approximately 50% and was independent of concentration.
Total blood and plasma drug-related radioactivity concentrations are identical, demonstrating that abacavir readily distributes into erythrocytes. Elimination: In single-dose trials, the observed elimination half-life (t ½ ) was 1.54 ± 0.63 hours. After intravenous administration, total clearance was 0.80 ±
0.24L per hour per kg (mean ± SD). Metabolism: In humans, abacavir is not significantly metabolized by cytochrome P450 enzymes. The primary routes of elimination of abacavir are metabolism by alcohol dehydrogenase to form the 5′-carboxylic acid and glucuronyl transferase to form the 5′-glucuronide.
The metabolites do not have antiviral activity. In vitro experiments reveal that abacavir does not inhibit human CYP3A4, CYP2D6, or CYP2C9 activity at clinically relevant concentrations. Excretion: Elimination of abacavir was quantified in a mass balance trial following administration of a 600-mg dose of 14 C-abacavir: 99% of the radioactivity was recovered, 1.2% was excreted in the urine as abacavir, 30% as the 5′-carboxylic acid metabolite, 36% as the 5′-glucuronide metabolite, and 15% as unidentified minor metabolites in the urine.
Fecal elimination accounted for 16% of the dose. Specific Populations Patients with Renal Impairment: The pharmacokinetic properties of ZIAGEN have not been determined in patients with impaired renal function. Renal excretion of unchanged abacavir is a minor route of elimination in humans.
Patients with Hepatic Impairment: The pharmacokinetics of abacavir have been studied in subjects with mild hepatic impairment (Child-Pugh Class A). Results showed that there was a mean increase of 89% in the abacavir AUC and an increase of 58% in the half-life of abacavir after a single dose of 600 mg of abacavir. The AUCs of the metabolites were not modified by mild liver disease; however, the rates of formation and elimination of the metabolites were decreased [see Contraindications ( 4 ), Use in Specific Populations ( 8.6 )] .
Pregnant Women: Abacavir pharmacokinetics were studied in 25 pregnant women during the last trimester of pregnancy receiving abacavir 300 mg twice daily. Abacavir exposure (AUC) during pregnancy was similar to those in postpartum and in HIV-infected non-pregnant historical controls. Consistent with passive diffusion of abacavir across the…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Abacavir is an antiretroviral agent [see Microbiology ( 12.4 )] .
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING ZIAGEN tablets, containing abacavir sulfate equivalent to 300 mg abacavir are yellow, biconvex, scored, capsule-shaped, film-coated, and imprinted with “GX 623” on both sides. They are packaged as follows: Bottles of 60 tablets (NDC 49702-221-18) with child-resistant closure. Store at controlled room temperature of 20° to 25°C (68° to 77°F) (see USP).
ZIAGEN oral solution is a clear to opalescent, yellowish, strawberry-banana-flavored liquid, which may turn brown over time. Each mL of the solution contains abacavir sulfate equivalent to 20 mg of abacavir. It is packaged in plastic bottles as follows: Bottles of 240 mL (NDC 49702-222-48) with child-resistant closure.
This product does not require reconstitution. Store at controlled room temperature of 20° to 25°C (68° to 77°F) (see USP). DO NOT FREEZE.
May be refrigerated.
📋 Description ▾
11 DESCRIPTION ZIAGEN is the brand name for abacavir sulfate, a synthetic carbocyclic nucleoside analogue with inhibitory activity against HIV-1. The chemical name of abacavir sulfate is ( 1 S,cis)- 4-[2-amino-6-(cyclopropylamino)-9 H -purin-9-yl]-2-cyclopentene-1-methanol sulfate (salt) (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 670.76 g per mol. It has the following structural formula: Abacavir sulfate is a white to off-white solid and is soluble in water. ZIAGEN tablets are for oral administration.
Each tablet contains abacavir sulfate equivalent to 300 mg of abacavir as active ingredient and the following inactive ingredients: colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. The tablets are coated with a film that is made of hypromellose, polysorbate 80, synthetic yellow iron oxide, titanium dioxide, and triacetin. ZIAGEN oral solution is for oral administration.
Each milliliter (1 mL) of ZIAGEN oral solution contains abacavir sulfate equivalent to 20 mg of abacavir (i.e., 20 mg per mL) as active ingredient and the following inactive ingredients: artificial strawberry and banana flavors, citric acid (anhydrous), methylparaben and propylparaben (added as preservatives), propylene glycol, saccharin sodium, sodium citrate (dihydrate), sorbitol solution, and water. In vivo, abacavir sulfate dissociates to its free base, abacavir. Dosages are expressed in terms of abacavir.
Abacavir sulfate chemical structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Medication Guide). Hypersensitivity Reactions Inform patients: • that a Medication Guide and Warning Card summarizing the symptoms of the abacavir hypersensitivity reaction and other product information will be dispensed by the pharmacist with each new prescription and refill of ZIAGEN and instruct the patient to read the Medication Guide and Warning Card every time to obtain any new information that may be present about ZIAGEN.
The complete text of the Medication Guide is reprinted at the end of this document. • to carry the Warning Card with them. • how to identify a hypersensitivity reaction [see Warnings and Precautions ( 5.1 ), Medication Guide]. • that if they develop symptoms consistent with a hypersensitivity reaction they should call their healthcare provider right away to determine if they should stop taking ZIAGEN. • that a hypersensitivity reaction can worsen and lead to hospitalization or death if ZIAGEN is not immediately discontinued. • to not restart ZIAGEN or any other abacavir‑containing product following a hypersensitivity reaction because more severe symptoms can occur within hours and may include life‑threatening hypotension and death. • that if they have a hypersensitivity reaction, they should dispose of any unused ZIAGEN to avoid restarting abacavir. • that a hypersensitivity reaction is usually reversible if it is detected promptly and ZIAGEN is stopped right away. • that if they have interrupted ZIAGEN for reasons other than symptoms of hypersensitivity (for example, those who have an interruption in drug supply), a serious or fatal hypersensitivity reaction may occur with reintroduction of abacavir. • to not restart ZIAGEN or any other abacavir‑containing product without medical consultation and only if medical care can be readily accessed by the patient or others.
Lactic Acidosis/Hepatomegaly with Steatosis Advise patients that lactic acidosis and severe hepatomegaly with steatosis have been reported with use of nucleoside analogues and other antiretrovirals. Advise patients to stop taking ZIAGEN if they develop clinical symptoms suggestive of lactic acidosis or pronounced hepatotoxicity [see Warnings and Precautions ( 5.2 )] . Immune Reconstitution Syndrome Advise patients to inform their healthcare provider immediately of any signs and symptoms of infection as inflammation from previous infection may occur soon after combination antiretroviral therapy, including when ZIAGEN is started [see Warnings and Precautions ( 5.3 )].
Pregnancy Registry Advise patients that there is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ZIAGEN during pregnancy [see Use in Specific Populations ( 8.1 )] . Lactation Instruct women with HIV-1 infection not to breastfeed because HIV-1 can be passed to the baby in the breast milk [see Use in Specific Populations ( 8.2 )] . Missed Dose Instruct patients that if they miss a dose of ZIAGEN, to take it as soon as they remember.
Advise patients not to double their next dose or take more than the prescribed dose [see Dosage and Administration ( 2 )] . Availability of Medication Guide Instruct patients to read the Medication Guide before starting ZIAGEN and to re-read it each time the prescription is renewed. Instruct patients to inform their physician or pharmacist if they develop any unusual symptom, or if any known symptom persists or worsens.
COMBIVIR, EPIVIR, and ZIAGEN are trademarks owned by or licensed to the ViiV Healthcare group of companies. The other brands listed are owned by or licensed to their respective owner and are not owned by or licensed to the ViiV Healthcare group of companies. The makers of these brands are not affiliated with and do not endorse the ViiV Healthcare group of companies or its products.
Manufactured for: ViiV Healthcare Durham, NC 27701 ©2023 ViiV Healthcare group of companies or its licensor. ZGN:16PI
💬 Medication Guide ▾
MEDICATION GUIDE ZIAGEN (ZY-uh-jen) ZIAGEN (ZY-uh-jen) (abacavir) (abacavir) tablets oral solution What is the most important information I should know about ZIAGEN? ZIAGEN can cause serious side effects, including: • Serious allergic reactions (hypersensitivity reaction) that can cause death have happened with ZIAGEN and other abacavir-containing products. Your risk of this allergic reaction is much higher if you have a gene variation called HLA‑B*5701.
Your healthcare provider can determine with a blood test if you have this gene variation. If you get a symptom from 2 or more of the following groups while taking ZIAGEN, call your healthcare provider right away to find out if you should stop taking ZIAGEN. Symptom(s) Group 1 Fever Group 2 Rash Group 3 Nausea, vomiting, diarrhea, abdominal (stomach area) pain Group 4 Generally ill feeling, extreme tiredness, or achiness Group 5 Shortness of breath, cough, sore throat A list of these symptoms is on the Warning Card your pharmacist gives you.
Carry this Warning Card with you at all times. If you stop ZIAGEN because of an allergic reaction, never take ZIAGEN (abacavir) or any other abacavir ‑ containing medicine (EPZICOM, TRIUMEQ, or TRIZIVIR) again. • If you have an allergic reaction, dispose of any unused ZIAGEN. Ask your pharmacist how to properly dispose of medicines. • If you take ZIAGEN or any other abacavir-containing medicine again after you have had an allergic reaction, within hours you may get life-threatening symptoms that may include very low blood pressure or death. • If you stop ZIAGEN for any other reason, even for a few days, and you are not allergic to ZIAGEN, talk with your healthcare provider before taking it again.
Taking ZIAGEN again can cause a serious allergic or life‑threatening reaction, even if you never had an allergic reaction to it before. If your healthcare provider tells you that you can take ZIAGEN again, start taking it when you are around medical help or people who can call a healthcare provider if you need one. What is ZIAGEN?
ZIAGEN is a prescription HIV-1 (Human Immunodeficiency Virus type 1) medicine used with other antiretroviral medicines to treat HIV-1 infection. HIV-1 is the virus that causes Acquired Immune Deficiency Syndrome (AIDS). The safety and effectiveness of ZIAGEN has not been established in children under 3 months of age.
When used with other antiretroviral medicines to treat HIV-1 infection, ZIAGEN may help: • reduce the amount of HIV-1 in your blood. This is called “viral load”. • increase the number of CD4+ (T) cells in your blood, that help fight off other infections. Reducing the amount of HIV-1 and increasing the CD4+ (T) cells in your blood may help improve your immune system.
This may reduce your risk of death or getting infections that can happen when your immune system is weak (opportunistic infections). ZIAGEN does not cure HIV-1 infection or AIDS. You must keep taking HIV-1 medicines to control HIV-1 infection and decrease HIV-related illnesses.
Who should not take ZIAGEN? Do not take ZIAGEN if you: • have a certain type of gene variation called the HLA‑B*5701 allele. Your healthcare provider will test you for this before prescribing treatment with ZIAGEN. • are allergic to abacavir or any of the ingredients in ZIAGEN.
See the end of this Medication Guide for a complete list of ingredients in ZIAGEN. • have liver problems. What should I tell my healthcare provider before taking ZIAGEN? Before you take ZIAGEN, tell your healthcare provider if you: • have been tested and know whether or not you have a particular gene variation called HLA‑B*5701. • have or have had liver problems, including hepatitis B or C virus infection. • have heart problems, smoke, or have diseases that increase your risk of heart disease such as high blood pressure, high cholesterol, or diabetes. • drink alcohol or take medicines that contain alcohol. • are pregnant or plan to become pregnant.
Talk to your healthcare provider if you are pregnant…