brand name | preparation | manufacturer | route | form | dosage^ | cost* |
Epivir | Lamivudine (3TC) | ViiV Healthcare | oral | tablet | 150 mg, 300 mg | $7.63; $15.27 |
oral | solution | 10 mg/mL (240 mL) | $122.14 | |||
Epivir HB (for HBV infection) | Lamivudine (3TC)Route | ViiV Healthcare | oral | tablet | 100 mg | $13.66 |
oral | solution | 5 mg/mL (240 mL) | $163.97 | |||
Combivir and generic AZT/3TC | Lamivudine (3TC)/Zidovudine (AZT) | ViiV Healthcare and generic manufacturer (Aurobindo Pharma Limited) | oral | tablet | 150 mg 3TC/300 mg AZT | $16.55; generic price (TBA) |
Trizivir | Lamivudine (3TC)/Zidovudine (AZT)/Abacavir (ABC) | ViiV Healthcare | oral | tablet | ABC 300 mg + AZT 300 mg + 3TC 150 mg | $26.81 |
Epzicom | Lamivudine (3TC)/Abacavir (ABC) | ViiV Healthcare | oral | tablet | ABC 600 mg + 3TC 300 mg | $35.78 |
Kivexa (brand name available in Europe) | ABC + 3TC | ViiV Healthcare | oral | tablet | ABC 600 mg + 3TC 300 mg | variable |
*Prices represent cost per unit specified, are representative of "Average Wholesale Price" (AWP).
^Dosage is indicated in mg unless otherwise noted.
300 mg once-daily or 150 mg PO twice-daily.
Cr Clearance 30-49 mL/min: 150 mg PO once-daily ; Cr Clearance 15-29 mL/min: 150 mg x1 then 100 mg once-daily.
150 mg x1 then 25-50 mg once-daily.
50 mg x1, then 25-50 mg once-daily (post HD).
150 mg x1, then 25-50 mg once-daily (limited data).
No data consider 150 mg PO once-daily.
No pertinent drug interactions since it is not a substrate, inhibitor, or inducer of CYP450 isoforms.
Drug | Effect of Interaction | Recommendations/Comments |
3TC AUC decreased by 15%; Cmax decreased by 35%. | Not clinically significant. Use standard dose. | |
3TC: No reported interaction. Methadone: No change. | Not clinically significant. Use standard dose. | |
Nelfinavir | No effect on 3TC AUC. | Not clinically significant. Use standard doses of both. |
Trimethoprim/Sulfamethoxazole | 3TC AUC increased by 44%. | Not clinically significant. Use standard dose. |
HIV and HBV
Intracellular phosphorylation to active lamivudine triphosphate, which competitively inhibits HIV DNA polymerase.
86%
Renal excretion accounts for 71%.
36%
Cmax = 3mcg/mL; Intracellular carbovir triphosphate 100 FM/million cells.
Serum: 5-7 hrs; Intracellular:12 hrs.
Widely distributed. Vd = 1.3 L/kg.
Usual dose.
Category C: Negative carcinogenicity and teratogenicity studies in rodents. Placental passage ratio of 1.0 (newborn:mother). Well tolerated in pregnant pts.
No human data, breast milk excretion in animal studies. 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.
Comment: This open-label pilot study determined whether there was clinical or immunological benefit to continuing 3TC in pts harboring M184V mutation. Pts randomly assigned to monotherapy with 3TC 300 mg once -daily or discontinuation of all ARV drugs (TI group). By wk 48, 20 of 29 (69%) pts in TI group (69%) and 12 of 29 (41%) in the 3TC group had discontinued study because of immunological (CD4 <350) or clinical failure, which was significantly delayed in 3TC group (p = 0.018).
Comment: In vitro data suggest benefit of continuing 3TC after virological failure due to a decrease in viral fitness. This prospective randomized trial did not support this theory. At wk 48 the average decline in VL (AAUCMB) was comparable between the 2 groups (p=0.65). However, continuing 3TC despite M184V mutation may be beneficial for resistance reasons, especially in pts taking AZT, d4T, or TDF. In pts who continued 3TC, 10.7 (95% CI: 7.5, 14.0) fewer nucleotide changes in viruses containing M184V (p<0.0001) were observed.
Comment: Randomized, placebo-controlled trial in 34 centers in U.S. with 66 untreated pts with HBV given 3TC 100 mg/day for 52 wks. Statistically significant histologic improvement with 3TC treatment (52% vs. 23%), decreased levels of HBeAg(undetectable in 32% vs. 11%), and suppression of HBV DNA (44% vs. 16%). Rate of AEs same in both groups. Limitation of 3TC monotherapy is development of resistance, which occurred at rate of 15-20% per yr.
Comment: Review article outlining therapeutic efficacy, pharmacokinetic properties, and antiviral activity.
Comment: DHHS dosing recommendations for lamivudine in pediatric patients.
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