$10.26 per tab
10 mg/mL (240ml bottle)
$161.78 (per 240ml)
ABC 300 mg + AZT 300 mg + 3TC 150 mg
$26.81 per tab
ABC + 3TC
ABC 600 mg + 3TC 300 mg
$35.78 per tab
Kivexa (brand name available in Europe)
ABC + 3TC
ABC 600 mg + 3TC 300 mg
*Prices represent cost per unit specified, are representative of "Average Wholesale Price" (AWP).
^Dosage is indicated in mg unless otherwise noted.
Pill burden: 2 pills/d (Ziagen, Trizivir) or 1 pill/d (Epzicom, Kivexa)
No renal dosage adjustment necessary.
No data-Usual dose likely
No data-Usual dose likely
Not a substrate, inducer, or inhibitor of CYP3A4. No interaction likely with PIs, NNRTIs, MVC, and RAL. ABC metabolized by alcohol dehydrogenase and glucoronyl transferase.
Effect of Interaction
3TC AUC decreased by 15%.
Not clinically significant. Use standard dose.
ABC AUC increased by 41%.
Clinical significance unknown. No dose adjustment recommended.
No significant interaction.
Use standard dose.
ABC AUC was decreased by 5%(NS).
Administer ABC with or without food.
Methadone clearance increased by 23%;
Monitor for methadone withdrawal, but dose adjustment unlikely to be necessary.
Decreased EVR to HCV treatment.
Suboptimal virologic suppression when ABC/TDF/3TC once daily was used as a triple nucleoside regimen without PIs or NNRTIs. However, preliminary analysis of ABC/AZT/3TC with TDF as nucleoside regimen did not show similar suboptimal results, and no evidence of drug interaction.
Decreased ABC AUC by 40%.
Clinical significance unknown. Active intracellular carbovir triphosphate not measured. Use standard dose.
Intracellular phosphorylation to active carbovir triphosphate, which competitively inhibits HIV DNA polymerase.
Well absorbed with 83% oral bioavailability.
81% metabolized by alcohol dehydrogenase and glucuronyl transferase with renal excretion of metabolites; 16% recovered in stool and 1% unchanged in urine.
Mean steady-state Cmax=3mcg/mL; AUC=6 mcg hr/mL. Intracellular levels of carbovir triphosphate 100 FM/million cells.
Serum: 1.5 hrs; intercellular (carbovir triphosphate):-12-20hrs.
Usual dose or 200 mg twice daily (limited clinical data).
Category C: rodent studies demonstrated placental passage. Teratogenic in rodent studies resulting in anasarca, skeletal malformation at 1000 mg/kg dose (35x human therapeutic levels) during organogenesis. However, rabbit studies using 8.5x human therapeutic levels did not result in fetal malformation. No adequate human data, placental passage was 32-66%.
No human data. Breast feeding is not recommended in the U.S in order to avoid post-natal transmission of HIV to the child, who may not yet be infected.
Trizivir (AZT/3TC/ABC) equivalent to unboosted IDV-based HAART regimen in pts with baseline VL < 100,000, but inferior to EFV-based HAART regimens. Since Trizivir (without a PI or NNRTI) is inferior to gold standard EFV-based regimen, it is recommended by the DHHS Guidelines only as alternative regimen when PI- or NNRTI-based regimens cannot be used. Addition of ABC to AZT/3TC/EFV did not improve virologic response in ART-naive patients. HLA-B*5701 should be ordered in all pts before starting ABC, and ABC should not be given to those who test positive. Recent data suggest decreased virologic response compared to TDF/FTC in pts with baseline VL >100,000, and possible increased risk of MI.
Comment: Randomized controled trial compared TDF/FTC and ABC/3TC in combination with EFV or boosted ATV.At a median follow-up of 60 weeks, among pts with VL >100K c/mL, the time to virologic failure was significantly shorter in the ABC/3TC group than in the TDF/FTC group (hazard ratio, 2.33; 95% confidence interval, 1.46 to 3.72; P<0.001), 57 virologic failures (14%) were observed in the ABC/3TC group versus 26 (7%) in the TDF/FTC group. In pts with VL <100K c/mL, there was no significant difference in time to virological failure between groups.
Comment: A retrospective review of D:A:D observational cohort for cardiovascular disease risks associated with NRTI use included 33,347 pts (157,912 pt-yrs of follow-up). There were 517 MIs, including 192 in pts receiving ABC-containing regimens. After adjusting for confounding risk factors, relative risk for ABC use within last 6 months was 1.9 (95% CI 1.5-2.5). There was also increased risk associated with ddI treatment, but not d4T or AZT. Greatest risk (and greatest increased risk) in pts with risk factors for cardiovascular disease. Pathophysiologic mechanism of this effect, if real, has not been identified. Other studies have not shown this risk, but they may have been under powered to show a risk of an infrequent toxicity. However, the usual caveats with observational studies apply.
Comment: Continuation of ACTG 5095 compared AZT/3TC/EFV to AZT/ABC/3TC/EFV in ART-naive pts. No significant differences between 3vs 4-drug regimens; approximately 80% of pts had VL < 50 through 3 yrs. 10% treated with AZT/3TC/ABC/EFV had ABC HSR, vs. 7% on AZT/3TC/EFV.
Comment: High rate of virologic failure in the TDF+ABC+3TC arm, with 49% experiencing virologic failure compared to 5.4% of pts taking EFV. Among TDF-treated pts for whom virologic data are available, 64% had both the K65R and M184V mutations and 36% had M184V alone. TDF/ABC/3TC is not recommended as a triple-NRTI regimen, and data minimal for use with a 4th agent.
Comment: EFV + once- or twice-daily ABC as part of an ABC/3TC backbone were equivalent, with 66% and 68% of pts achieving VL <50, respectively.
Comment: The PENTA 13 cross-over PK study evaluated ABC 8mg/kg BID vs. 16mg/kg QD in 24 HIV infected children ages 2-13 years old who had undetectable/low viral loads and stable CD4 counts. Although AUC (0-24) was comparable between QD and BID dosing, Cmin of QD ABC was lower in younger children (2-6 y/o).
Comment: ABC/3TC + EFV was non-inferior to AZT/3TC + EFV in a randomized, double-blind study involving 649 naive pts. Response rate (<50) through wk 48 was 70% and 69% in ABC and AZT group, respectively. Pts on ABC/3TC had less nausea, vomiting, fatigue, and anemia than pts taking AZT, but more HSR. ABC/3TC associated with greater increase in CD4 (209 vs 155) and CD4%.
Comment: Compared triple-NRTI regimen of AZT/3TC/ABC with 2 EFV-containing regimens, AZT/3TC + EFV and AZT/3TC/ABC + EFV. Triple-NRTI arm was stopped early because of higher rate of virologic failure vs. EFV-based regimens (21% vs 10%, p <0.001). Triple NRTI regimens should only be used as alternative in pts who cannot take PI or NNRTI-based regimens.
Comment: This study found an extraordinary association between presence of HLA-B*5701, HLA-DR7, and HLA-DQ3 alleles and HSR to ABC (OR 822 [43-15675], p<0.0001). Authors concluded that if ABC was withheld in presence of these alleles, prevalence of HSR would decrease from 9-5% to 2.5%. Positive predictive value for HSR 100%, negative predictive value 97%.
Comment: AZT/3TC + ABC was equivalent to AZT/3TC + unboosted IDV, with 51% in both group achieving VL <400 at 48 wks. Trend favoring IDV-based regimen in pts with baseline VL >100,000, with 45% vs 31% achieving <50 (a treatment difference -14% (95% CI, -27% to 0%). Although this trial demonstrated equivalency at <400 endpoint, the decreased potency at high VL suggests lower potency overall.
Comment: Retrospective review of 2752 pts enrolled in continous treatment arm of SMART evaluated cardiovascular (CV) disease risks associated with NRTI components of ARV regimens. CV risk factors comparable between groups: median age of 40, 73% males, 39% smokers, 7% had diabetes, and 4% with prior CV disease. Use of ABC associated with increased risk of MI (AHR = 4.3), CV-related death (AHR = 1.8), with signficantly increased risk seen in those with 5 or more CV risk factors.
Comment: Study randomized 1956 ABC-naive patients to standard of care or screening with HLA-B*5701 test before starting ABC. Incidence of both clinically diagnosed and immunologically confirmed HSR significantly lower in screening arm vs. control arm. No cases of immunologically confirmed HSR observed in prospective screening arm. HLA-B*5701 had a 100% sensitivity.
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