Eravacyclinum
Eravacyclinum Uses, Dosage, Side Effects, Food Interaction and all others data.
Eravacyclinum, known as Xerava by Tetraphase Pharmaceuticals, is a fully synthetic fluorocycline antibiotic of the tetracycline class with activity against clinically significant gram-negative, gram-positive aerobic, and facultative bacteria. This includes most of those bacteria resistant to cephalosporins, fluoroquinolones, β-lactam/β-lactamase inhibitors, multidrug-resistant strains, and carbapenem-resistant Enterobacteriaceae, and the majority of anaerobic pathogens . It was first approved by the FDA on August 27, 2018 . Eravacyclinum has demonstrated superior potency to that of antibiotics that are currently being marketed for intraabdominal infections .
Eravacyclinum is an antibiotic that disrupts bacterial protein synthesis, treating complicated intraabdominal infections .
| Trade Name | Eravacyclinum |
| Availability | Prescription only |
| Generic | Eravacycline |
| Eravacycline Other Names | Eravacyclina, Eravacycline, Eravacyclinum |
| Related Drugs | ciprofloxacin, metronidazole, clindamycin, ceftriaxone, gentamicin |
| Type | |
| Formula | C27H31FN4O8 |
| Weight | Average: 558.563 Monoisotopic: 558.212592137 |
| Protein binding | Protein binding of eravacycline to human plasma proteins increases with increasing plasma concentrations, with 79% to 90% (bound) at plasma concentrations ranging from 100 to 10,000 ng/mL . |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Eravacyclinum is a tetracycline antibiotic used to treat complicated intra-abdominal infections.
Eravacyclinum is a tetracycline class antibacterial indicated for the treatment of complicated intra-abdominal infections in patients 18 years of age and older .
Eravacyclinum is also used to associated treatment for these conditions: Intraabdominal Infections
How Eravacyclinum works
Eravacyclinum is a fluorocycline antibacterial of the tetracycline class of antibacterial drugs. Eravacyclinum disrupts bacterial protein synthesis by binding to the 30S ribosomal subunit, preventing the incorporation of amino acid residues into elongating peptide chains. In general, eravacycline is bacteriostatic against gram-positive bacteria (e.g., Staphylococcus aureus and Enterococcus faecalis); however, in vitro bactericidal activity has been shown against certain strains of Escherichia coli and Klebsiella pneumoniae .
Toxicity
The most common adverse reactions (incidence ≥ 3%) are infusion site reactions, nausea, and vomiting . Less common (incidence ≥ 1%) adverse effects are palpitations, chest pain, acute pancreatitis, pancreatic necrosis, hypocalcemia, dizziness, dysgeusia, anxiety, insomnia, depression, pleural effusion, dyspnea, rash and hyperhidrosis .
The following are various side effects that may occur due to eravacycline use :
Hypersensitivity: Life-threatening anaphylaxis has been reported with the administration of eravacycline. Antibacterial drugs and should be avoided in patients with known hypersensitivity to tetracycline-class antibacterial drugs .
Tooth Discoloration/enamel hypoplasia: The use of this drug during tooth development (last half of pregnancy, infancy and childhood to the age of 8 years) may lead to the permanent discoloration of teeth (yellow-grey-brown) .
Inhibition of bone growth: The use of eravacycline during the second and third trimester of pregnancy, infancy and childhood until the age of 8 years old may cause reversible inhibition of bone growth. All tetracyclines form a stable calcium complex in bone-forming tissue .
Clostridium difficile-Associated diarrhea: Clostridium difficile associated diarrhea (CDAD) has been reported with use of the majority of antibacterial agents, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents changes the normal flora of the colon, leading to an overgrowth of C. difficile.
Tetracycline class adverse reactions: This drug is structurally similar to tetracycline-class antibacterial drugs and may have similar adverse reactions. Adverse reactions including photosensitivity, pseudotumor cerebri, and anti-anabolic action which has led to increased BUN, azotemia, acidosis, hyperphosphatemia, pancreatitis, and abnormal liver function tests, have been reported for other tetracycline-class antibacterial agents, and may occur with eravacycline. Discontinue eravacycline if any of these adverse reactions are suspected or observed .
Potential for microbial overgrowth: The use of eravacycline may result in overgrowth of non-susceptible organisms, including fungi. If such infections occur, discontinue eravacycline and manage with appropriate therapy .
Development of drug-resistant bacteria: Prescribing eravacycline in the absence of a proven or strongly suspected bacterial infection is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria .
Food Interaction
- Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of eravacycline. Dose adjustment may be necessary for co-administration.
Volume of Distribution
The volume of distribution at steady-state is approximately 321 L .
Elimination Route
Following single-dose intravenous administration, eravacycline AUC (area under the curve) and Cmax (maximum concentration) increase dose-proportionally for doses from 1 mg/kg - 3 mg/kg (3 times the approved dose). There is approximately 45% accumulation following intravenous dosing of 1 mg/kg every 12 hours .
Half Life
The mean elimination half-life is 20 hours .
Clearance
17.82 L/min (standard deviation of 3.4) .
Elimination Route
Following a single intravenous dose of radiolabeled eravacycline 60 mg, approximately 34% of the dose is excreted in urine and 47% in feces as unchanged eravacycline (20% in urine and 17% in feces) and metabolites .
Innovators Monograph
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