Peringatan Keamanan

The most common adverse reactions (incidence ? 3%) are infusion site reactions, nausea, and vomiting FDA label. 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 FDA label.

The following are various side effects that may occur due to eravacycline use FDA label:

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 FDA label.

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) FDA label.

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 FDA label.

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 FDA label.

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 FDA label.

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 FDA label.

Eravacycline

DB12329

small molecule approved investigational

Deskripsi

Eravacycline, 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, ?-lactam/?-lactamase inhibitors, multidrug-resistant strains, and carbapenem-resistant Enterobacteriaceae, and the majority of anaerobic pathogens A38683. It was first approved by the FDA on August 27, 2018 L4540. Eravacycline has demonstrated superior potency to that of antibiotics that are currently being marketed for intraabdominal infections A38727.

Struktur Molekul 2D

Berat 558.563
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life is 20 hours [FDA label].
Volume Distribusi The volume of distribution at steady-state is approximately 321 L [FDA label].
Klirens (Clearance) 17.82 L/min (standard deviation of 3.4) [A38685].

Absorpsi

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 FDA label.

Metabolisme

Eravacycline is metabolized primarily by CYP3A4- and FMO-mediated oxidation FDA label.

Rute Eliminasi

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 FDA label.

Interaksi Makanan

1 Data
  • 1. 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.

Interaksi Obat

324 Data
Mecamylamine Eravacycline may increase the neuromuscular blocking activities of Mecamylamine.
Mipomersen Eravacycline may increase the hepatotoxic activities of Mipomersen.
Flucloxacillin The therapeutic efficacy of Flucloxacillin can be decreased when used in combination with Eravacycline.
Piperacillin The therapeutic efficacy of Piperacillin can be decreased when used in combination with Eravacycline.
Ampicillin The therapeutic efficacy of Ampicillin can be decreased when used in combination with Eravacycline.
Phenoxymethylpenicillin The therapeutic efficacy of Phenoxymethylpenicillin can be decreased when used in combination with Eravacycline.
Dicloxacillin The therapeutic efficacy of Dicloxacillin can be decreased when used in combination with Eravacycline.
Carbenicillin The therapeutic efficacy of Carbenicillin can be decreased when used in combination with Eravacycline.
Nafcillin The therapeutic efficacy of Nafcillin can be decreased when used in combination with Eravacycline.
Oxacillin The therapeutic efficacy of Oxacillin can be decreased when used in combination with Eravacycline.
Hetacillin The therapeutic efficacy of Hetacillin can be decreased when used in combination with Eravacycline.
Benzylpenicilloyl polylysine The therapeutic efficacy of Benzylpenicilloyl polylysine can be decreased when used in combination with Eravacycline.
Mezlocillin The therapeutic efficacy of Mezlocillin can be decreased when used in combination with Eravacycline.
Cyclacillin The therapeutic efficacy of Cyclacillin can be decreased when used in combination with Eravacycline.
Benzylpenicillin The therapeutic efficacy of Benzylpenicillin can be decreased when used in combination with Eravacycline.
Amoxicillin The therapeutic efficacy of Amoxicillin can be decreased when used in combination with Eravacycline.
Azlocillin The therapeutic efficacy of Azlocillin can be decreased when used in combination with Eravacycline.
Cloxacillin The therapeutic efficacy of Cloxacillin can be decreased when used in combination with Eravacycline.
Amdinocillin The therapeutic efficacy of Amdinocillin can be decreased when used in combination with Eravacycline.
Bacampicillin The therapeutic efficacy of Bacampicillin can be decreased when used in combination with Eravacycline.
Meticillin The therapeutic efficacy of Meticillin can be decreased when used in combination with Eravacycline.
Pivampicillin The therapeutic efficacy of Pivampicillin can be decreased when used in combination with Eravacycline.
Pivmecillinam The therapeutic efficacy of Pivmecillinam can be decreased when used in combination with Eravacycline.
Ticarcillin The therapeutic efficacy of Ticarcillin can be decreased when used in combination with Eravacycline.
Azidocillin The therapeutic efficacy of Azidocillin can be decreased when used in combination with Eravacycline.
Carindacillin The therapeutic efficacy of Carindacillin can be decreased when used in combination with Eravacycline.
Procaine benzylpenicillin The therapeutic efficacy of Procaine benzylpenicillin can be decreased when used in combination with Eravacycline.
Sultamicillin The therapeutic efficacy of Sultamicillin can be decreased when used in combination with Eravacycline.
Temocillin The therapeutic efficacy of Temocillin can be decreased when used in combination with Eravacycline.
Epicillin The therapeutic efficacy of Epicillin can be decreased when used in combination with Eravacycline.
Pheneticillin The therapeutic efficacy of Pheneticillin can be decreased when used in combination with Eravacycline.
Carfecillin The therapeutic efficacy of Carfecillin can be decreased when used in combination with Eravacycline.
Propicillin The therapeutic efficacy of Propicillin can be decreased when used in combination with Eravacycline.
Clometocillin The therapeutic efficacy of Clometocillin can be decreased when used in combination with Eravacycline.
Sulbenicillin The therapeutic efficacy of Sulbenicillin can be decreased when used in combination with Eravacycline.
Penamecillin The therapeutic efficacy of Penamecillin can be decreased when used in combination with Eravacycline.
Talampicillin The therapeutic efficacy of Talampicillin can be decreased when used in combination with Eravacycline.
Aspoxicillin The therapeutic efficacy of Aspoxicillin can be decreased when used in combination with Eravacycline.
Metampicillin The therapeutic efficacy of Metampicillin can be decreased when used in combination with Eravacycline.
Bismuth subcitrate potassium The serum concentration of Eravacycline can be decreased when it is combined with Bismuth subcitrate potassium.
Zinc Zinc can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc trihydroxide Zinc trihydroxide can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc Substituted Heme C Zinc Substituted Heme C can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Polaprezinc Polaprezinc can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc oxide Zinc oxide can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc sulfate Zinc sulfate can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc citrate Zinc citrate can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc picolinate Zinc picolinate can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc gluconate Zinc gluconate can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetylcysteine zinc Acetylcysteine zinc can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc ascorbate Zinc ascorbate can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc acetate Zinc acetate can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc glycinate Zinc glycinate can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc chloride Zinc chloride can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc sulfate, unspecified form Zinc sulfate, unspecified form can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc cation Zinc cation can cause a decrease in the absorption of Eravacycline resulting in a reduced serum concentration and potentially a decrease in efficacy.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Eravacycline.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Eravacycline.
Altrenogest The serum concentration of Altrenogest can be decreased when it is combined with Eravacycline.
Gestonorone The serum concentration of Gestonorone can be decreased when it is combined with Eravacycline.
Methylestrenolone The serum concentration of Methylestrenolone can be decreased when it is combined with Eravacycline.
Norgestrienone The serum concentration of Norgestrienone can be decreased when it is combined with Eravacycline.
Norethindrone enanthate The serum concentration of Norethindrone enanthate can be decreased when it is combined with Eravacycline.
Quingestanol acetate The serum concentration of Quingestanol acetate can be decreased when it is combined with Eravacycline.
Progesterone The serum concentration of Progesterone can be decreased when it is combined with Eravacycline.
Medroxyprogesterone acetate The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Eravacycline.
Norgestimate The serum concentration of Norgestimate can be decreased when it is combined with Eravacycline.
Etonogestrel The serum concentration of Etonogestrel can be decreased when it is combined with Eravacycline.
Desogestrel The serum concentration of Desogestrel can be decreased when it is combined with Eravacycline.
Megestrol acetate The serum concentration of Megestrol acetate can be decreased when it is combined with Eravacycline.
Levonorgestrel The serum concentration of Levonorgestrel can be decreased when it is combined with Eravacycline.
Dydrogesterone The serum concentration of Dydrogesterone can be decreased when it is combined with Eravacycline.
Norethisterone The serum concentration of Norethisterone can be decreased when it is combined with Eravacycline.
Ethynodiol diacetate The serum concentration of Ethynodiol diacetate can be decreased when it is combined with Eravacycline.
Allylestrenol The serum concentration of Allylestrenol can be decreased when it is combined with Eravacycline.
Cyproterone acetate The serum concentration of Cyproterone acetate can be decreased when it is combined with Eravacycline.
Norelgestromin The serum concentration of Norelgestromin can be decreased when it is combined with Eravacycline.
Gestodene The serum concentration of Gestodene can be decreased when it is combined with Eravacycline.
Hydroxyprogesterone caproate The serum concentration of Hydroxyprogesterone caproate can be decreased when it is combined with Eravacycline.
Dienogest The serum concentration of Dienogest can be decreased when it is combined with Eravacycline.
Medrogestone The serum concentration of Medrogestone can be decreased when it is combined with Eravacycline.
Norethynodrel The serum concentration of Norethynodrel can be decreased when it is combined with Eravacycline.
Norgestrel The serum concentration of Norgestrel can be decreased when it is combined with Eravacycline.
Gestrinone The serum concentration of Gestrinone can be decreased when it is combined with Eravacycline.
Nomegestrol The serum concentration of Nomegestrol can be decreased when it is combined with Eravacycline.
Lynestrenol The serum concentration of Lynestrenol can be decreased when it is combined with Eravacycline.
Chlormadinone The serum concentration of Chlormadinone can be decreased when it is combined with Eravacycline.
Promegestone The serum concentration of Promegestone can be decreased when it is combined with Eravacycline.
Quingestanol The serum concentration of Quingestanol can be decreased when it is combined with Eravacycline.
Demegestone The serum concentration of Demegestone can be decreased when it is combined with Eravacycline.
Etynodiol The serum concentration of Etynodiol can be decreased when it is combined with Eravacycline.
Nomegestrol acetate The serum concentration of Nomegestrol acetate can be decreased when it is combined with Eravacycline.
Hydroxyprogesterone The serum concentration of Hydroxyprogesterone can be decreased when it is combined with Eravacycline.
Drospirenone The serum concentration of Drospirenone can be decreased when it is combined with Eravacycline.
Algestone acetophenide The serum concentration of Algestone acetophenide can be decreased when it is combined with Eravacycline.
Technetium Tc-99m oxidronate Eravacycline may decrease effectiveness of Technetium Tc-99m oxidronate as a diagnostic agent.
Pitolisant The serum concentration of Eravacycline can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Eravacycline can be increased when combined with Metreleptin.
Dicoumarol Eravacycline may increase the anticoagulant activities of Dicoumarol.
Phenindione Eravacycline may increase the anticoagulant activities of Phenindione.

Target Protein

30S ribosomal protein S4 rpsD

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27851857
    Solomkin J, Evans D, Slepavicius A, Lee P, Marsh A, Tsai L, Sutcliffe JA, Horn P: Assessing the Efficacy and Safety of Eravacycline vs Ertapenem in Complicated Intra-abdominal Infections in the Investigating Gram-Negative Infections Treated With Eravacycline (IGNITE 1) Trial: A Randomized Clinical Trial. JAMA Surg. 2017 Mar 1;152(3):224-232. doi: 10.1001/jamasurg.2016.4237.
  • PMID: 24468780
    Connors KP, Housman ST, Pope JS, Russomanno J, Salerno E, Shore E, Redican S, Nicolau DP: Phase I, open-label, safety and pharmacokinetic study to assess bronchopulmonary disposition of intravenous eravacycline in healthy men and women. Antimicrob Agents Chemother. 2014;58(4):2113-8. doi: 10.1128/AAC.02036-13. Epub 2014 Jan 27.
  • PMID: 29869646
    Thakare R, Dasgupta A, Chopra S: Eravacycline for the treatment of patients with bacterial infections. Drugs Today (Barc). 2018 Apr;54(4):245-254. doi: 10.1358/dot.2018.54.4.2800623.

Contoh Produk & Brand

Produk: 7 • International brands: 0
Produk
  • Xerava
    Injection, powder, lyophilized, for solution • 100 mg/1 • Intravenous • US • Approved
  • Xerava
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Xerava
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Xerava
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Xerava
    Injection, powder, lyophilized, for solution • 50 mg/1 • Intravenous • US • Approved
  • Xerava
    Injection, powder, for solution • 50 mg • Intravenous • EU • Approved
  • Xerava
    Injection, powder, for solution • 50 mg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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