NUZYRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NUZYRA (NUZYRA).
Omadacycline is a aminomethylcycline antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, blocking aminoacyl-tRNA binding to the A site.
| Metabolism | Minimal hepatic metabolism; not significantly metabolized by CYP enzymes. Excreted primarily unchanged in urine and feces. |
| Excretion | Fecal (approximately 76%) as unchanged drug; renal (approximately 14%) as unchanged drug; biliary excretion is minimal. |
| Half-life | Terminal elimination half-life is approximately 17-21 hours; supports once-daily dosing. |
| Protein binding | 80-90% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Approximately 7-10 L/kg; indicates extensive tissue distribution, exceeding total body water. |
| Bioavailability | Oral: approximately 34% (fasting) to 62% (with high-fat meal); food significantly increases absorption. |
| Onset of Action | Intravenous: clinical effect observed within 24-48 hours; Oral: similar onset after IV to oral transition. |
| Duration of Action | Sustained for 24 hours with once-daily dosing; clinical duration extends beyond half-life due to prolonged post-antibiotic effect. |
200 mg intravenously once on day 1, then 100 mg IV once daily; or 200 mg orally once on day 1, then 100 mg orally once daily.
| Dosage form | POWDER |
| Renal impairment | For CrCl 30-49 mL/min: 200 mg IV/PO once on day 1, then 100 mg IV/PO once every 48 hours. For CrCl <30 mL/min (including dialysis): 200 mg IV/PO once on day 1, then 100 mg IV/PO once every 48 hours. For hemodialysis: administer after dialysis. |
| Liver impairment | Child-Pugh Class B or C: no dose adjustment recommended; use with caution. No specific dose adjustment provided in labeling. |
| Pediatric use | Safety and efficacy not established in pediatric patients below 18 years of age. |
| Geriatric use | No specific dose adjustment required; monitor renal function and consider age-related decline in CrCl for dosing adjustments. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NUZYRA (NUZYRA).
| Breastfeeding | It is not known whether omadacycline is excreted in human milk. However, other tetracyclines are excreted in breast milk. Because of the potential for serious adverse reactions in nursing infants, including dental discoloration and inhibition of bone growth, women should not breastfeed during treatment with NUZYRA and for 4 days after the last dose. M/P ratio is unknown. |
| Teratogenic Risk | NUZYRA (omadacycline) is a tetracycline-class antibiotic. Tetracyclines can cause fetal harm when administered to a pregnant woman. Use during the second and third trimesters may cause reversible inhibition of bone growth and permanent discoloration of teeth (yellow-gray-brown). Use during the first trimester is associated with an increased risk of neural tube defects and other malformations. Omadacycline is contraindicated in pregnant women. |
■ FDA Black Box Warning
No boxed warning.
| Serious Effects |
["Hypersensitivity to omadacycline or any tetracycline-class antibiotic"]
| Precautions | ["Tooth discoloration and enamel hypoplasia with use during tooth development","Inhibition of bone growth in premature infants and children under 8 years","Clostridioides difficile-associated diarrhea","Photosensitivity reactions","Potential for microbial overgrowth","Tetracycline class effects (e.g., antianabolic action leading to increased BUN, azotemia, hyperphosphatemia, and acidosis)"] |
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| Fetal Monitoring | Monitor maternal liver function tests and renal function periodically. For fetal monitoring, ultrasound assessment may be considered if exposure occurs during the first trimester. No specific fetal monitoring is required but assess for potential tetracycline-associated effects in neonates. |
| Fertility Effects | In animal studies, omadacycline did not impair fertility in rats. However, tetracyclines may affect spermatogenesis in males at high doses. Clinical data on human fertility are lacking. |