Abstract
Oral and intravenous (IV) omadacycline formulations are approved in the United States for treating acute bacterial skin and skin structure infections and community-acquired bacterial pneumonia in adults. Oral omadacycline bioavailability is 34.5%; similar exposures are obtained following 300 mg oral and 100 mg IV doses. Oral administration should be in a fasted state, with dairy products, antacids, or multivitamins avoided for ≥4 hours after dosing. Low protein binding (21%), large volume of distribution (190 L), low systemic clearance (10 L/hour), and long elimination half-life (16-17 hours) support once-daily dosing. Omadacycline is excreted unchanged in feces (81.1%) and urine (14.4%), with low potential for drug-drug interactions. Dose adjustments are unnecessary for age, sex, and renal or hepatic impairment. Pharmacokinetic-pharmacodynamic studies identify fAUC0-24/MIC ratio as the parameter that correlates with in vivo efficacy. Systemic exposure of omadacycline in epithelial lining fluid is greater than/equal to plasma concentrations in healthy adults.
References
Jul 4, 2006·The Journal of Antimicrobial Chemotherapy·Kenneth N Agwuh, Alasdair MacGowan
Aug 14, 2008·The Journal of Antimicrobial Chemotherapy·Alasdair P MacGowan
Feb 18, 2016·Transgenic Research
Jul 30, 2016·Bioorganic & Medicinal Chemistry·S Ken TanakaStephen Villano
Aug 9, 2016·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Jimmy FlarakosJames B Mangold
Oct 30, 2016·Future Microbiology·Stephen VillanoEvan Loh
Aug 20, 2016·Journal of Clinical Pharmacology·Evan TzanisEvan Loh
Nov 9, 2016·Antimicrobial Agents and Chemotherapy·Wen LinStephen Villano
Feb 6, 2017·Journal of Pharmacokinetics and Pharmacodynamics·Karen Bush, Malcolm G P Page
Feb 15, 2017·Antimicrobial Agents and Chemotherapy·Alexander J LepakDavid R Andes
Jul 9, 2017·Current Opinion in Pharmacology·Paul G Ambrose
Jul 12, 2017·Antimicrobial Agents and Chemotherapy·Mark H GotfriedKeith A Rodvold
Sep 3, 2017·Transgenic Research
Nov 22, 2017·Antimicrobial Agents and Chemotherapy·Jolene K BergStephen Villano
Nov 29, 2017·Antimicrobial Agents and Chemotherapy·Lu Ann BundrantStephen Villano
Citations
Aug 2, 2019·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·Jason C Gallagher
Aug 21, 2019·Microorganisms·Despoina KoulentiUNKNOWN SotiriosTsiodras
Nov 13, 2019·Antimicrobial Agents and Chemotherapy·Alexander J LepakDavid R Andes
Jun 10, 2020·Antimicrobial Agents and Chemotherapy·Khurshida BegumKevin W Garey
Jan 24, 2020·Drugs·George G ZhanelJames A Karlowsky
Aug 26, 2020·Antimicrobial Agents and Chemotherapy·Steven J KovacsStephen Villano
Sep 23, 2020·Future Microbiology·Teena ChopraGlenn Tillotson
Nov 13, 2020·European Journal of Drug Metabolism and Pharmacokinetics·Thomas L HuntPaul C McGovern
Dec 10, 2020·The Journal of Antimicrobial Chemotherapy·A R NoelA P MacGowan
May 1, 2021·Journal of Clinical Medicine·Annemieke BloemNelianne J Verkaik
Jun 2, 2021·Antimicrobial Agents and Chemotherapy·Bethany R QuadeLucas S Blanton
Jun 15, 2021·Antimicrobial Agents and Chemotherapy·Kavindra V SinghBarbara E Murray
Oct 7, 2021·Microbiology Spectrum·Angela CamporealeChristian G Giske