Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR versus DOLUTEGRAVIR SODIUM.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR versus DOLUTEGRAVIR SODIUM.
DOLUTEGRAVIR vs DOLUTEGRAVIR SODIUM
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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 HIV replication.
Integrase strand transfer inhibitor (INSTI); inhibits HIV-1 integrase, blocking viral DNA integration into host genome.
50 mg orally once daily; for integrase strand transfer inhibitor-naïve patients, 50 mg orally twice daily if coadministered with efavirenz, nevirapine, tipranavir/ritonavir, or rifampin.
50 mg orally once daily, with or without food. For INSTI-naive patients, 50 mg twice daily when co-administered with potent UDP-glucuronosyltransferase (UGT)1A1 or CYP3A inducers (e.g., efavirenz, nevirapine, tipranavir/ritonavir, rifampin).
None Documented
None Documented
Clinical Note
moderateDolutegravir + Teriflunomide
"The serum concentration of Teriflunomide can be increased when it is combined with Dolutegravir."
Clinical Note
moderateDolutegravir + Atazanavir
"The serum concentration of Atazanavir can be increased when it is combined with Dolutegravir."
Clinical Note
moderateDolutegravir + Ranolazine
"The serum concentration of Ranolazine can be increased when it is combined with Dolutegravir."
Clinical Note
moderateDolutegravir + Rolapitant
Terminal elimination half-life is approximately 14 hours (range 11-16 hours) following oral administration. This supports once-daily dosing in most patients; however, with concomitant UGT1A1/CYP3A4 inducers (e.g., efavirenz, rifampin), half-life may be reduced, necessitating twice-daily dosing.
Terminal elimination half-life is approximately 14 hours (range 11-17 hours) in healthy subjects; supports once-daily dosing. Half-life may be prolonged in severe renal impairment but no dose adjustment required.
Dolutegravir is primarily eliminated via metabolism, with approximately 53% excreted unchanged in feces and 32% in urine. Renal excretion of unchanged drug is minimal (<1%). Biliary excretion contributes to fecal elimination.
Primarily (64%) excreted unchanged in feces via biliary secretion; 31% in urine, of which 18.9% is unchanged drug and the rest as glucuronide conjugate (5.1%) and other minor metabolites. Total clearance: 0.56 L/h.
Category C
Category C
Integrase Strand Transfer Inhibitor Antiretroviral
Integrase Strand Transfer Inhibitor Antiretroviral
"The serum concentration of Rolapitant can be increased when it is combined with Dolutegravir."