Triumeq Generic Name & Formulations
Legal Class
Rx
General Description
Abacavir 600mg, dolutegravir 50mg, lamivudine 300mg; tabs.
Pharmacological Class
Nucleoside reverse transcriptase inhibitors (NRTIs) + integrase strand transfer inhibitor (INSTI).
See Also
How Supplied
Tabs—30; PD—90 (w. dosing cup)
Manufacturer
Generic Availability
NO
Mechanism of Action
Dolutegravir inhibits HIV integrase by binding to the integrase active site and
blocking the strand transfer step of retroviral DNA integration which is essential for the HIV replication cycle. Abacavir is converted to the active metabolite, carbovir triphosphate, which inhibits the activity of HIV-1 reverse transcriptase both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Lamivudine is converted to its active metabolite, lamivudine triphosphate, which inhibits reverse transcriptase via DNA chain termination after incorporation of the nucleotide analogue.
Triumeq Indications
Indications
HIV-1 infection in patients aged ≥3 months and weighing ≥6kg.
Limitations of Use
Not recommended alone in patients with resistance-associated integrase substitutions or suspected INSTI resistance due to insufficient dolutegravir dose in Triumeq and Triumeq PD in these subpopulations.
Triumeq Dosage and Administration
Adult
≥25kg: 1 tab once daily. Concomitant efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, rifampin: give additional dolutegravir 50mg separated by 12hrs from Triumeq.
Children
<3mos or <6kg: not established. 6–<25kg: use Triumeq PD only.
Triumeq Contraindications
Contraindications
Presence of HLA-B*5701 allele. Previous hypersensitivity reaction to any of the components. Concomitant dofetilide. Moderate or severe hepatic impairment.
Triumeq Boxed Warnings
Boxed Warning
Hypersensitivity reactions. Exacerbation of hepatitis B.
Triumeq Warnings/Precautions
Warnings/Precautions
Tabs and tabs for oral susp are not interchangeable on a mg per mg basis. Screen for presence of HLA-B*5701 allele prior to starting therapy or reinitiation; if (+), abacavir is contraindicated. Discontinue immediately if hypersensitivity is suspected, regardless of HLA-B*5701 status and even when other diagnoses are possible. If hypersensitivity cannot be ruled out, do not restart. If stopped for reasons other than hypersensitivity, restart only if medical care can be readily accessed. Test for the presence of HBV infection in all patients prior to or when initiating therapy. Lamivudine not established for chronic HBV infection; if treatment is initiated in patients co-infected with HIV and HBV, additional treatment should be considered for chronic HBV (if not, use alternative regimen). Monitor closely for severe acute exacerbations of HBV in patients co-infected with HBV and HIV for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection); if appropriate, initiate anti-hepatitis B therapy may be warranted. Increased risk for worsening/development of elevated transaminases in patients with underlying hepatitis B or C; monitor for hepatotoxicity. Suspend if lactic acidosis or pronounced hepatotoxicity (eg, hepatomegaly, steatosis) occurs. Underlying risk of coronary heart disease (eg, hypertension, hyperlipidemia, diabetes, smoking). Renal impairment (CrCl <30mL/min): not recommended; if lamivudine dose reduction is required, use individual components; (CrCl 30–49mL/min): monitor for hematologic toxicities; if new or worsening neutropenia or anemia develop, adjust lamivudine dose. Mild hepatic impairment: not recommended; if abacavir dose reduction is required, use individual components. Women. Obesity. Elderly. Embryo-fetal toxicity: increased risk of neural tube defects (assess risks/benefits; consider alternative treatment at time of conception through 1st trimester or if pregnancy is confirmed). Pregnancy: exclude status prior to initiation. Advise females of reproductive potential to use effective contraception. Nursing mothers: not recommended.
Triumeq Pharmacokinetics
Absorption
Peak plasma concentrations are reached at 2–3 hours postdose (dolutegravir).
Distribution
Plasma protein bound: ~50% (abacavir); ≥98.9% (dolutegravir); low (lamivudine). Volume of distribution: 17.4 L (dolutegravir).
Elimination
Renal. Half-life: 1.54 ± 0.63 hours (abacavir); ~14 hours (dolutegravir); 13–19 hours (lamivudine). Total clearance: 0.80 ± 0.24 L/h/kg (abacavir); 1.0 L/h (dolutegravir); 398.5 ± 69.1 mL per min (lamivudine).
Triumeq Interactions
Interactions
Dolutegravir may be affected by drugs that induce or inhibit UGT1A1, CYP3A, UGT1A3, UGT1A9, BCRP, and P-gp enzymes or transporters. Avoid concomitant nevirapine, oxcarbazepine, phenytoin, phenobarbital, St. John’s wort. Concomitant etravirine without atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir: not recommended. Concomitant efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, rifampin: requires extra dolutegravir dose (see Adults and Children). May potentiate drugs eliminated via OCT2 or MATE1 (eg, dofetilide, dalfampridine, metformin). Avoid concomitant sorbitol-containing products. Concomitant cation-containing antacids, laxatives, sucralfate, buffered drugs, or oral iron/calcium supplements (also can give together with a meal): give Triumeq or Triumeq PD 2hrs before or 6hrs after. Ethanol may increase abacavir levels. Abacavir may antagonize methadone. Potentiates riociguat; may need to reduce riociguat dose.
Triumeq Adverse Reactions
Adverse Reactions
Insomnia, headache, fatigue; hypersensitivity reactions (may be fatal), hepatotoxicity, immune reconstitution syndrome.
Triumeq Clinical Trials
See Literature
Triumeq Note
Not Applicable
Triumeq Patient Counseling
See Literature