XERAVA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XERAVA (XERAVA).
Eravacycline is a tetracycline-class antibacterial that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, preventing aminoacyl-tRNA from attaching to the A-site. It exhibits activity against a broad range of Gram-positive, Gram-negative, and anaerobic bacteria, including many tetracycline-resistant strains due to modifications circumventing common resistance mechanisms.
| Metabolism | Primarily metabolized by CYP3A4 and flavin-containing monooxygenase (FMO) to multiple metabolites; also undergoes non-CYP-mediated metabolism including glucuronidation. |
| Excretion | Fecal (approximately 80-90% as unchanged drug); renal (less than 1% as unchanged drug). |
| Half-life | Terminal elimination half-life is approximately 42 hours (range 30-60 hours) in healthy subjects; prolonged in elderly patients and those with severe hepatic impairment. |
| Protein binding | Approximately 90% bound to human plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution at steady state is approximately 1.26 L/kg (range 0.54-2.08 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Not applicable (intravenous administration only); absolute bioavailability is 100% when administered intravenously. |
| Onset of Action | Intravenous administration: Clinical response observed within 24-48 hours; maximum serum concentrations achieved by end of 1-hour infusion. |
| Duration of Action | Duration of clinical effect is sustained for the entire treatment course; once-daily dosing maintains therapeutic concentrations; clinical cure rates assessed at test of cure visit (7-14 days after last dose). |
200 mg intravenously over 60 minutes every 12 hours
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for GFR ≥ 30 mL/min. For GFR < 30 mL/min, not recommended due to lack of data. |
| Liver impairment | No dose adjustment required for Child-Pugh A or B. For Child-Pugh C, use with caution due to lack of data. |
| Pediatric use | Safety and effectiveness in pediatric patients have not been established. |
| Geriatric use | No dose adjustment required based on age, but monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XERAVA (XERAVA).
| Breastfeeding | Unknown if eravacycline is excreted in human breast milk. Tetracyclines are known to be excreted and may cause adverse effects (tooth discoloration, bone growth inhibition) in nursing infants. Decision to breastfeed should consider importance of drug to mother and potential infant risks. M/P ratio not determined. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal studies, eravacycline caused fetal toxicity (reduced fetal weight, skeletal variations) at maternal toxic doses. Tetracyclines, including eravacycline, may cause permanent tooth discoloration and reversible bone growth inhibition in the fetus when used during the second and third trimesters. Avoid use during pregnancy unless benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Known hypersensitivity to eravacycline or any tetracycline-class antibiotic"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis have been reported","Tooth discoloration and enamel hypoplasia when used during tooth development","Inhibition of bone growth when used in children under 8 years or during pregnancy","Photosensitivity manifested by exaggerated sunburn reaction","Potential for Clostridium difficile-associated diarrhea","Hepatic impairment monitoring recommended in patients with liver disease"] |
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| Fetal Monitoring | Monitor for signs of hepatotoxicity and pancreatitis. Assess renal function periodically. No specific fetal monitoring required beyond routine prenatal care. Advise patient to report any signs of liver injury or allergic reactions. |
| Fertility Effects | No human data on fertility effects. Animal studies (rats) showed no adverse effects on mating, fertility, or reproductive performance at clinically relevant exposures. |