(a BAK a veer)
- Abacavir Sulfate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Ziagen: 20 mg/mL (240 mL) [contains methylparaben, propylene glycol, propylparaben, saccharin sodium; strawberry-banana flavor]
Ziagen: 300 mg [scored]
Generic: 300 mg
Brand Names: U.S.
- Antiretroviral, Reverse Transcriptase Inhibitor, Nucleoside (Anti-HIV)
Nucleoside reverse transcriptase inhibitor. Abacavir is a guanosine analogue which is phosphorylated to carbovir triphosphate which interferes with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.
Rapid and extensive absorption
Vd: 0.86 ± 0.15 L/kg; CSF to plasma AUC ratio: 27% to 33%
Hepatic via alcohol dehydrogenase and glucuronyl transferase to inactive carboxylate and glucuronide metabolites; not significantly metabolized by cytochrome P450 enzymes; intracellulary metabolized to carbovir triphosphate.
Urine: ~83% (1.2% as unchanged drug, 30% as 5'-carboxylic acid metabolite, 36% as the glucuronide, and 15% as other metabolites); feces (16% total dose)
Clearance (apparent): Single dose 8 mg/kg (Hughes 1999): Pediatric patients ≥3 months to ≤13 years: 17.84 mL/minute/kg; Adults: 10.14 mL/minute/kg
Time to Peak
Pediatric patients ≥3 months to ≤13 years: Within 1.5 hours (Hughes 1999); Adults: 0.7 to 1.7 hours
Pediatric patients ≥3 months to ≤13 years: 1 to 1.5 hours (Hughes 1999; Kline 1999)
Adults: 1.54 ± 0.63 hours
Hepatic impairment (mild): Increases half-life by 58%
Intracellular: 12 to 26 hours
Special Populations: Hepatic Function Impairment
In mild hepatic impairment (Child-Pugh score 5 to 6), AUC increased 89%.
Use: Labeled Indications
HIV-1 infection: Treatment of HIV-1 infection in combination with other antiretroviral agents
Hypersensitivity to abacavir or any component of the formulation; patients who are positive for the HLA-B*5701 allele; moderate to severe hepatic impairment
HIV-1 infection, treatment: Oral: 300 mg twice daily or 600 mg once daily in combination with other antiretroviral agents.
Refer to adult dosing.
HIV-1 infection, treatment: Oral:
Infants ≥3 months, Children, and Adolescents: Note: Efficacy of once daily dosing has only been demonstrated in patients who transitioned from twice daily dosing after 36 weeks of treatment. Some experts recommend avoiding once daily therapy for infants and young children receiving oral solution until viral load has been undetectable and CD4 have been stable for more than 6 months (HHS [pediatric 2016]).
Weight-directed dosing: Oral solution: 16 mg/kg/day in 1 or 2 divided doses (maximum: 600 mg/day). Note: Weight-band dosing may be used in certain patients weighing ≥14 kg; especially rapid growing younger children (HHS [pediatric] 2016)
Weight-band directed dosing for patients ≥14 kg: Tablets (scored 300 mg tablets), oral solution:
14 to <20 kg: 300 mg once daily or 150 mg twice daily
≥20 to <25 kg: 450 mg once daily or 150 mg in the morning and 300 mg in the evening
≥25 kg: 600 mg once daily or 300 mg twice daily
Dosing: Renal Impairment
US labeling: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
Canadian labeling: No dosage adjustment necessary. Use of 600 mg once daily dosing has not been studied.
Dosing: Hepatic Impairment
Mild impairment (Child-Pugh class A): 200 mg twice daily (oral solution is recommended).
Moderate to severe impairment (Child-Pugh class B or C): Use is contraindicated (has not been studied).
May be administered with or without food.
Store at 20°C to 25°C (68°F to 77°F). Oral solution may be refrigerated; do not freeze.
Cabozantinib: MRP2 Inhibitors may increase the serum concentration of Cabozantinib. Monitor therapy
Methadone: May diminish the therapeutic effect of Abacavir. Abacavir may decrease the serum concentration of Methadone. Monitor therapy
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Monitor therapy
Protease Inhibitors: May decrease the serum concentration of Abacavir. Monitor therapy
Rates of adverse reactions were defined during combination therapy with other antiretrovirals. Frequency not always defined. *Incidence not specifically defined but reported in the range of >10%. **Incidence not specifically defined but reported in the range of 1% to 10%.
Central nervous system: Fatigue*, headache (adults: >10%; children: 1% to 10%), malaise*, abnormal dreams**, anxiety**, chills**, depression**, dizziness**, migraine**, sleep disorder**
Dermatologic: Skin rash**
Endocrine & metabolic: Hypertriglyceridemia**, increased gamma-glutamyl transferase
Gastrointestinal: Nausea*, abdominal pain**, diarrhea (increased incidence with once daily dosing)**, gastritis**, gastrointestinal disease**, increased serum amylase**, nausea and vomiting**, vomiting**, pancreatitis
Hematologic & oncologic: Neutropenia**, thrombocytopenia**
Hepatic: Increased serum ALT**, increased serum AST**
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis and multiorgan failure; 8%; excluding subjects carrying the HLA-B*5701 allele: 1%)
Neuromuscular & skeletal: Increased creatinine phosphokinase**, musculoskeletal pain**
Respiratory: Bronchitis**, ENT infection**, pneumonia (children)**, viral respiratory tract infection**
<1% (Limited to important or life-threatening): Anemia, erythema multiforme, hepatomegaly, hepatotoxicity, hyperglycemia, immune reconstitution syndrome, lactic acidosis, leukopenia, liver steatosis, myocardial infarction, pain, redistribution of body fat, renal disease, Stevens-Johnson syndrome, toxic epidermal necrolysis
Concerns related to adverse effects:
• Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance).
• Hypersensitivity reactions: [US Boxed Warning]: Serious and sometimes fatal hypersensitivity reactions have occurred. Patients who carry the HLA-B*5701 allele are at a higher risk for a hypersensitivity reaction to abacavir, although hypersensitivity reactions have occurred in patients who do not carry the HLA-B*5701 allele. All patients should be screened for the HLA-B*5701 allele prior to initiating or reinitiation of therapy unless patients have had a previously documented HLA-B*5701 allele assessment. Discontinue abacavir if a hypersensitivity reaction is suspected. Abacavir is contraindicated in patients who have the HLA-B*5701 allele or in patients with a prior hypersensitivity reaction to abacavir. Reintroduction of any abacavir-containing product can result in life-threatening or fatal hypersensitivity reactions, even in patients who have no history of hypersensitivity to abacavir therapy. Such reactions can occur within hours. An allergy to abacavir should be documented in the medical record of allele-positive patients. Reactions usually occur within 9 days of starting abacavir; ~90% occur within 6 weeks, although these reactions may occur at any time during therapy (HHS [adult] 2015). These reactions usually include signs or symptoms from two or more of the following: Fever, skin rash, constitutional symptoms (malaise, fatigue, aches), respiratory symptoms (eg, pharyngitis, dyspnea, cough), and GI symptoms (eg, abdominal pain, diarrhea, nausea, vomiting). Other signs and symptoms include lethargy, headache, myalgia, edema, abnormal chest x-ray findings, arthralgia and paresthesia. Anaphylaxis, liver failure, renal failure, hypotension, adult respiratory distress syndrome, respiratory failure, myolysis, and death have occurred in association with hypersensitivity reactions. Physical findings (lymphadenopathy, mucous membrane lesions, and rash [maculopapular, urticarial or variable]) may occur. Erythema multiforme has also been reported. Laboratory abnormalities (eg, elevated liver function tests, elevated creatine phosphokinase, elevated creatinine, and lymphopenia) may occur. Abacavir should be permanently discontinued if hypersensitivity cannot be ruled out, even when other diagnoses are possible and regardless of HLA-B*5701 status. Abacavir SHOULD NOT be restarted because more severe symptoms may occur within hours, including LIFE-THREATENING HYPOTENSION AND DEATH. If abacavir is restarted following an interruption in therapy not associated with symptoms of a hypersensitivity reaction, carefully evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or cannot be ruled out regardless of HLA-B*5701 status. If abacavir is restarted, continually monitor for symptoms of a hypersensitivity reaction. Make the patient aware that reintroduction should only take place if medical care is readily accessible.
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
• Lactic acidosis/hepatomegaly: [U.S Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues, including fatal cases; use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis).
• Coronary heart disease: Use has been associated with an increased risk of myocardial infarction (MI) in observational studies; however, based on a meta-analysis of 26 randomized trials, the FDA has concluded there is not an increased risk. Consider using with caution in patients with risks for coronary heart disease and minimizing modifiable risk factors (eg, hypertension, hyperlipidemia, diabetes mellitus, and smoking) prior to use.
• Hepatic impairment: Use with caution and adjust dosage in patients with mild hepatic impairment (contraindicated in moderate to severe impairment).
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Dosage form specific issues:
• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated with hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP, 1997; Zar, 2007).
• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer’s labeling.
• Sorbitol: Oral solution contains sorbitol. Use oral solution with caution in patients who are fructose intolerant; may experience abdominal discomfort and/or diarrhea with administration of the oral solution.
• Appropriate use: Abacavir should always be used as a component of a multidrug regimen; concomitant use with other abacavir-containing products is not recommended. Do not use abacavir/lamivudine (plus efavirenz or plus atazanavir/ritonavir) in adolescent and adult HIV-1 patients with a pre-ART HIV RNA >100,000 copies/mL (HHS [adult] 2015).
CBC with differential, serum creatine kinase, CD4 count, HIV RNA plasma levels, serum transaminases, triglycerides, serum amylase; HLA-B*5701 genotype status prior to initiation of therapy and prior to reinitiation of therapy in patients of unknown HLA-B*5701 status; signs and symptoms of hypersensitivity
Abacavir has a high level of transfer across the human placenta. No increased risk of overall birth defects has been observed following first trimester exposure according to data collected by the antiretroviral pregnancy registry. Maternal antiretroviral therapy may increase the risk of preterm delivery, although available information is conflicting possibly due to variability of maternal factors (disease severity; initiation of therapy); however, maternal antiretroviral medication should not be withheld due to concerns of preterm birth. Information related to stillbirth, low birth weight, and small for gestational age infants is limited. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children who develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential mitochondrial dysfunction. Cases of lactic acidosis and hepatic steatosis related to mitochondrial toxicity have been reported with use of nucleoside reverse transcriptase inhibitors (NRTIs). These adverse events are similar to other rare but life-threatening syndromes which occur during pregnancy (eg, HELLP syndrome). In general nucleoside reverse transcriptase inhibitors are well tolerated and the benefits of use generally outweigh potential risk.
Combination antiretroviral therapy (cART) therapy is recommended for all HIV-infected pregnant women to keep the viral load below the limit of detection and reduce the risk of perinatal transmission. When HIV is diagnosed during pregnancy in a woman who has never received antiretroviral therapy, cART should begin as soon as possible after diagnosis. The Health and Human Services (HHS) Perinatal HIV Guidelines consider abacavir in combination with lamivudine to be a preferred NRTI backbone for initial therapy in antiretroviral-naive pregnant women (do not use in women who are positive for the HLA-B*5701 allele). This backbone is not recommended with atazanavir/ritonavir or efavirenz if pretreatment HIV RNA is >100,000 copies/mL. The pharmacokinetics of abacavir are not significantly changed by pregnancy and dose adjustment is not needed for pregnant women. In general, women who become pregnant on a stable cART regimen may continue that regimen if viral suppression is effective, appropriate drug exposure can be achieved, contraindications for use in pregnancy are not present, and the regimen is well tolerated. Monitoring during pregnancy is more frequent than in non-pregnant adults; cART should be continued postpartum.
For HIV-infected couples planning a pregnancy, maximum viral suppression with combination antiretroviral therapy (cART) is recommended prior to conception for the HIV-infected partner(s) and expert consultation is recommended; modification of therapy (if needed) and optimization of the woman’s health should be done prior to conception. HIV-infected women not planning a pregnancy may use any available type of contraception, considering possible drug interactions and contraindications of the specific method. In addition, consistent use of condoms is also recommended (even during pregnancy) to prevent transmission of HIV or other sexually transmitted diseases.
Health care providers are encouraged to enroll pregnant women exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or www.APRegistry.com). Health care providers caring for HIV-infected women and their infants may contact the National Perinatal HIV Hotline (888-448-8765) for clinical consultation (HHS [perinatal] 2016).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience vomiting, dizziness, headache, nausea, diarrhea, lack of appetite, change in body fat, insomnia, or nightmares. Have patient report immediately to prescriber signs of allergic reaction with organ failure (fever, rash, fatigue, flu-like signs, nausea, vomiting, diarrhea, abdominal pain, pharyngitis, cough, or difficulty breathing), signs of lactic acidosis (fast breathing, tachycardia, abnormal heartbeat, vomiting, fatigue, shortness of breath, severe loss of strength and energy, severe dizziness, feeling cold, or muscle pain or cramps), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of depression (suicidal ideation, anxiety, emotional instability, or confusion), angina, severe dizziness, passing out, mouth sores, enlarged lymph nodes, or signs of infection (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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- Drug class: nucleoside reverse transcriptase inhibitors (NRTIs)
Other brands: Ziagen