9/12/22, 6:53 PM Eravacycline: Drug information - UpToDate

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Eravacycline: Drug information

Copyright 1978-2022 Lexicomp, Inc. All rights reserved.

Contributor Disclosures

(For additional information see "Eravacycline: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp ( show table)

Brand Names: US
Xerava

Pharmacologic Category
Antibiotic, Tetracycline Derivative

Dosing: Adult
Collapse All

Intra-abdominal infections, complicated 

Intra-abdominal infections, complicated: IV: 1 mg/kg every 12 hours for 4 to 14

days.

Plague, treatment, bubonic or pharyngeal 

Plague (Yersinia pestis), treatment, bubonic or pharyngeal (alternative agent)

(off- label use):

Note: Consult public health officials for event-specific recommendations.

IV: 1 mg/kg every 12 hours for 10 to 14 days and for at least a few days after
clinical resolution (CDC [Nelson 2021]; Stout 2022).

Dosage adjustment for concomitant therapy: Significant drug interactions exist,

requiring dose/frequency adjustment or avoidance. Consult drug interactions database

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for more information.

Dosing: Kidney Impairment: Adult

No dosage adjustment necessary.

Dosing: Hepatic Impairment: Adult

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment

necessary

Severe impairment (Child-Pugh class C): 1 mg/kg every 12 hours on day 1, then 1 mg/kg
every 24 hours

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult
specific product labeling.

Solution Reconstituted, Intravenous [preservative free]:

Xerava: 50 mg (1 ea); 100 mg (1 ea)

Generic Equivalent Available: US

No

Administration: Adult
IV: Infuse diluted solution IV over ~60 minutes through dedicated line or via Y-site. If the
same IV line is used for sequential infusion of several drugs, flush line with NS before and
after eravacycline administration. Do not mix with other drugs or add to solutions containing
other drugs.

Use: Labeled Indications

Intra-abdominal infections, complicated: Treatment of complicated intra-abdominal

infections caused by susceptible microorganisms: Escherichia coli, Klebsiella pneumoniae,
Citrobacter freundii, Enterobacter cloacae, Klebsiella oxytoca, Enterococcus faecalis,
Enterococcus faecium, Staphylococcus aureus, Streptococcus anginosus group, Clostridium
perfringens, Bacteroides species, and Parabacteroides distasonis in patients ≥18 years.

Limitations of use: Not indicated for the treatment of complicated urinary tract
infections.

Use: Off-Label: Adult

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Plague (Yersinia pestis), treatment

Adverse Reactions
The following adverse drug reactions and incidences are derived from product labeling
unless otherwise specified.

1% to 10%:

Cardiovascular: Hypotension (1%)

Gastrointestinal: Nausea (7%), vomiting (4%), diarrhea (2%)

Local: Infusion site reaction (8%)

Miscellaneous: Wound dehiscence (1%)

<1%, postmarketing, and/or case reports: Acute pancreatitis, anaphylaxis, anxiety, chest
pain, decreased creatinine clearance, decreased white blood cell count, depression,
dizziness, dysgeusia, dyspnea, hyperhidrosis, hypersensitivity reaction, hypocalcemia,
increased amylase, increased gamma-glutamyl transferase, increased serum alanine
aminotransferase, increased serum lipase, insomnia, neutropenia, palpitations,
pancreatic necrosis, pleural effusion, prolonged partial thromboplastin time, skin rash

Contraindications
Hypersensitivity to eravacycline, tetracycline-class antibacterial drugs, or any component of
the formulation.

Warnings/Precautions

Concerns related to adverse effects:

• Anaphylactic/Hypersensitivity reactions: Life-threatening (anaphylactic) reactions

have been reported; discontinue if an allergic reaction occurs. Avoid use in patients
with known hypersensitivity to tetracyclines.

• Antianabolic effects: May be associated with antianabolic effects observed with the
tetracycline class (including increased BUN, azotemia, acidosis, and
hyperphosphatemia).

• Hepatotoxicity: May be associated with abnormal liver function tests due to

structural similarities with tetracyclines; discontinue use when suspected.

• Pancreatitis: May be associated with pancreatitis due to structural similarities with

tetracyclines.

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• Photosensitivity: May be associated with photosensitivity due to structural

similarities with tetracyclines.

• Pseudotumor cerebri: May be associated with pseudotumor cerebri due to

structural similarities with tetracyclines.

• Superinfection: Use may result in fungal or bacterial superinfection, including

Clostridioides difficile infection (CDI) and colitis; CDI has been observed >2 months
postantibiotic treatment.

Disease-related concerns:

• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage
adjustment recommended in severe hepatic impairment.

Special populations:

• Pediatric: May cause permanent tooth discoloration, enamel hypoplasia, or

reversible inhibition of bone growth; use should be avoided during tooth and bone
development (children <8 years of age).

Other warnings/precautions:

• Limitations of use: Not indicated for the treatment of complicated urinary tract
infection in adults; eravacycline failed to demonstrate efficacy in 2 randomized,
double-blind, active-controlled clinical trials.

Metabolism/Transport Effects
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on
clinically relevant drug interaction potential

Drug Interactions
(For additional information: Launch drug interactions program)

Note: Interacting drugs may not be individually listed below if they are part of a group
interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a
complete list of drug interactions by individual drug name and detailed management
recommendations, use the Lexicomp drug interactions program by clicking on the “Launch
drug interactions program” link above.

Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the

photosensitizing effect of Aminolevulinic Acid (Systemic). Risk X: Avoid combination

Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing

effect of Aminolevulinic Acid (Topical). Risk C: Monitor therapy

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Bacillus clausii: Antibiotics may diminish the therapeutic effect of Bacillus clausii.
Management: Bacillus clausii should be taken in between antibiotic doses during
concomitant therapy. Risk D: Consider therapy modification

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical).
Risk X: Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG
Vaccine (Immunization). Risk C: Monitor therapy

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine.
Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and
within 14 days following the use of oral or parenteral antibiotics. Risk X: Avoid
combination

CYP3A4 Inducers (Strong): May decrease the serum concentration of Eravacycline.

Management: Increase the eravacycline dose to 1.5 mg/kg every 12 hours when
combined with strong CYP3A4 inducers. Risk D: Consider therapy modification

Immune Checkpoint Inhibitors: Antibiotics may diminish the therapeutic effect of

Immune Checkpoint Inhibitors. Risk C: Monitor therapy

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus
and Estriol. Risk C: Monitor therapy

Lithium: Tetracyclines may increase the serum concentration of Lithium. Risk C: Monitor
therapy

Mecamylamine: Tetracyclines may enhance the neuromuscular-blocking effect of

Mecamylamine. Risk X: Avoid combination

Methoxsalen (Systemic): Photosensitizing Agents may enhance the photosensitizing

effect of Methoxsalen (Systemic). Risk C: Monitor therapy

Methoxyflurane: Tetracyclines may enhance the nephrotoxic effect of Methoxyflurane.

Risk X: Avoid combination

Mipomersen: Tetracyclines may enhance the hepatotoxic effect of Mipomersen. Risk C:

Monitor therapy

Neuromuscular-Blocking Agents: Tetracyclines may enhance the neuromuscular-

blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy

Penicillins: Tetracyclines may diminish the therapeutic effect of Penicillins. Risk C: Monitor
therapy

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Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer.

Risk C: Monitor therapy

Retinoic Acid Derivatives: Tetracyclines may enhance the adverse/toxic effect of Retinoic
Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Risk
X: Avoid combination

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium

Picosulfate. Management: Consider using an alternative product for bowel cleansing
prior to a colonoscopy in patients who have recently used or are concurrently using an
antibiotic. Risk D: Consider therapy modification

Sulfonylureas: Tetracyclines may enhance the hypoglycemic effect of Sulfonylureas. Risk

C: Monitor therapy

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine.
Only the live attenuated Ty21a strain is affected. Management: Avoid use of live
attenuated typhoid vaccine (Ty21a) in patients being treated with systemic antibacterial
agents. Postpone vaccination until 3 days after cessation of antibiotics and avoid
starting antibiotics within 3 days of last vaccine dose. Risk D: Consider therapy
modification

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of

Verteporfin. Risk C: Monitor therapy

Vitamin K Antagonists (eg, warfarin): Tetracyclines may enhance the anticoagulant effect
of Vitamin K Antagonists. Risk C: Monitor therapy

Pregnancy Considerations

Tetracyclines cross the placenta.

As a class, tetracyclines accumulate in developing teeth and long tubular bones (Mylonas
2011). Exposure during the second and third trimesters of pregnancy may cause reversible
inhibition of bone growth. Permanent discoloration of teeth (yellow, gray, brown) can occur
following in utero exposure and is more likely to occur following long-term or repeated
exposure.

Eravacycline is not one of the recommended antibiotics for the treatment of plague (Y. pestis)
in pregnant patients (CDC [Nelson 2021]).

Breastfeeding Considerations

It is not known if eravacycline is present in breast milk.

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Other tetracyclines are present in breast milk; the extent of eravacycline absorption by a
breastfeeding infant is not known. Due to the potential for serious adverse reactions in
the breastfed infant (including tooth discoloration and inhibition of bone growth),
breastfeeding is not recommended by the manufacturer during therapy or for 4 days
after the last dose.

Monitoring Parameters
Monitor hepatic function periodically. Observe for signs and symptoms of anaphylaxis
during administration.

Mechanism of Action
Eravacycline is a fluorocycline antibiotic within the tetracycline class that binds to the 30S
ribosomal subunit and prevents the incorporation of amino acid residues into elongating
peptide chains, thereby, inhibiting bacterial protein synthesis.

Pharmacokinetics

Distribution: Vdss: ~321 L (~4 L/kg) (Newman 2018)

Protein binding: 79% to 90% (increases with increasing plasma concentrations)

Metabolism: Primarily by CYP3A4- and FMO-mediated oxidation

Half-life elimination: 20 hours

Excretion: Urine: ~34% (20% as unchanged drug); Feces: 47% (17% as unchanged drug)

Pharmacokinetics: Additional Considerations

Hepatic function impairment: Cmax was 13.9%, 16.3%, and 19.7% higher and AUC was 22.9%,
37.9%, and 110.3% higher in patients with mild (Child-Pugh class A), moderate (Child-Pugh
class B), and severe (Child-Pugh class C) hepatic impairment compared to healthy subjects,
respectively.

Pricing: US

Solution (reconstituted) (Xerava Intravenous)

50 mg (per each): $63.60

100 mg (per each): $117.60

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided
as reference price only. A range is provided when more than one manufacturer's AWP price
is available and uses the low and high price reported by the manufacturers to determine the
range. The pricing data should be used for benchmarking purposes only, and as such should

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not be used alone to set or adjudicate any prices for reimbursement or purchasing functions
or considered to be an exact price for a single product and/or manufacturer. Medi-Span
expressly disclaims all warranties of any kind or nature, whether express or implied, and
assumes no liability with respect to accuracy of price or price range data published in its
solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or
consequential damages arising from use of price or price range data. Pricing data is updated
monthly.

Brand Names: International

Xerava (AT, CZ, EE, HR, HU, LT, LV, NL, PT, SK)

For country abbreviations used in Lexicomp ( show table)

Use of UpToDate is subject to the Terms of Use.

REFERENCES

1. Mylonas I. Antibiotic chemotherapy during pregnancy and lactation period: aspects for consideration. Arch
Gynecol Obstet. 2011;283(1):7-18. [PubMed 20814687]

2. Nelson CA, Meaney-Delman D, Fleck-Derderian S, Cooley KM, Yu PA, Mead PS; contributors. Antimicrobial
treatment and prophylaxis of plague: recommendations for naturally acquired infections and bioterrorism
response. MMWR Recomm Rep. 2021;70(3):1-27. doi:10.15585/mmwr.rr7003a1 [PubMed 34264565]

3. Newman JV, Zhou J, Izmailyan S, Tsai L. Randomized, double-blind, placebo-controlled studies of the safety
and pharmacokinetics of single and multiple ascending doses of eravacycline [published online August 27,
2018]. Antimicrob Agents Chemother. doi: 10.1128/AAC.01174-18 [PubMed 30150464]

4. Stout J. Clinical manifestations, diagnosis, and treatment of plague (Yersinia pestis infection). Post TW, ed.
UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed March 17, 2022.

5. US Food and Drug Administration (FDA), Center for Drug Evaluation and Research. NDA Multi-Disciplinary
Review and Evaluation – NDA 211109 Xerava (eravacycline) for injection. 2018. Available at
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211109Orig1s000MultidisciplineR.pdf. Accessed
February 8, 2019.

6. Xerava (eravacycline) [prescribing information]. Waltham, MA: Tetraphase Pharmaceuticals Inc; July 2021.
Topic 118878 Version 64.0

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