eravacycline

Inhibits bacterial protein synthesis by binding to the 30S bacterial ribosome.

Therapeutic effects:

Bacteriostatic against gram-positive bacteria. Bactericidal against certain strains of Escherichia coli and Klebsiella pneumoniae.

Spectrum:

Active against some gram-positive pathogens:
- Enterococcus faecalis,
- Enterococcus faecium,
- Staphylococcus aureus,
- Streptococcus anginosus.
Active against some gram-negative pathogens:
- Citrobacter freundii,
- Enterobacter cloacae,
- Escherichia coli,
- Klebsiella oxytoca,
- Klebsiella pneumoniae.
Active against some anaerobic pathogens:
- Bacteroides spp.,
- Clostridium perfringens,
- Parabacteroides distasonis.

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Extensively distributed to tissues.

Protein Binding: 79–90% (↑ as plasma concentrations ↑).

Metabolism/Excretion: Primarily metabolized by the liver by CYP3A enzymes. 47% excreted in feces (17% as unchanged drug), 34% in urine (20% as unchanged drug).

Half-Life: 20 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	unknown	1 hr	12 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to eravacycline or other tetracycline antibiotics;
OB: Pregnancy (may lead to permanent staining of teeth and inhibition of bone growth in fetus if used during 2nd or 3rd trimester);
Lactation: Lactation;
Pedi: Children 8 yr (may lead to permanent staining of teeth and growth).

Use Cautiously in:

Severe hepatic impairment;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

Derm: photosensitivity

GI: CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), diarrhea, nausea, vomiting

GU: ↓fertility (males)

Local: infusion site reaction

Neuro: intracranial hypertension

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inducers may ↓ levels; ↑ eravacycline dose.
May ↑ effect of warfarin.

Route/Dosage ⬆ ⬇

IV (Adults ): 1 mg/kg every 12 hr for 4–14 days. Concurrent use of strong CYP3A inducer: 1.5 mg/kg every 12 hr for 4–14 days.

Hepatic Impairment

IV (Adults ): Severe hepatic impairment (Child-Pugh C): 1 mg/kg every 12 hr on Day 1, then 1 mg/kg every 24 hr starting on Day 2 (total duration of therapy = 4–14 days).

Availability ⬆ ⬇

Lyophilized powder for injection: 50 mg/vial; 100 mg/vial

Assessment ⬆ ⬇

Assess for infection (vital signs, WBC) at beginning of and during therapy.
Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results.
Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of
Clostridioides difficile
-associated diarrhea (CDAD). May begin up to several wk following cessation of therapy.
Assess for signs and symptoms of hypersensitivity reactions (rash, hives, pruritus, dyspnea swelling of face, throat, and lips) during therapy.
Assess IV site frequently; may cause thrombophlebitis.

Implementation ⬆ ⬇

Intermittent Infusion: Reconstitution: Reconstitute each vial with 5 mL of Sterile Water for Injection or 0.9% NaCl.Concentration: 50 mg vial – 10 mg/mL. 100 mg vial — 20 mg/mL. Swirl gently until dissolved; do not shake. Solution is clear, pale yellow to orange solution. Reconstituted solution is stable for 1 hr; discard if not diluted within 1 hr. Diluent: Dilute further with 0.9% NaCl.Concentration: 0.3 mg/mL with a range of 0.2–0.6 mg/mL.Infuse within 24 hr if stored at room temperature or 10 days if refrigerated. Solution is clear, light yellow to orange; do not administer solutions that are cloudy, discolored or contain particulate matter.
Rate: Infuse over 60 min. Flush line with 0.9% NaCl before and after infusion.

Patient/Family Teaching ⬆ ⬇

Explain purpose of eravacycline to patient. Emphasize the importance of completing full course of therapy and not skipping doses.
Instruct patient to notify health care professional immediately if rash, diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheals without consulting health care professionals. Diarrhea may occur as late as 2 mo after therapy.
Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Advise patient to report the signs of superinfection (black, furry overgrowth on the tongue, vaginal itching or discharge, loose or foul-smelling stools).
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: May cause tooth discoloration and inhibition of bone growth if administered during 2nd and 3rd trimesters. Advise females of reproductive potential to use a nonhormonal method of contraception while taking tetracyclines and until next menstrual period and to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during and for 4 days after last dose of eravacycline. May cause infertility in male patients.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇