Peringatan Keamanan

Toxicity information regarding cethromycin is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as diarrhea, nausea, vomiting, abdominal pain, and headaches. Symptomatic and supportive measures are recommended.L14006, A203369

Cethromycin

DB06419

small molecule investigational

Deskripsi

Cethromycin is a 3-keto (ketolide) derivative of erythromycin A with an 11,12-carbamate group and an O-6-linked aromatic ring system.A203369 Cethromycin represents a joint development effort by Abbott Laboratories, Taisho Pharmaceuticals, and Advanced Life Sciences, intended to be marketed under the trade name Restanza for the treatment of community-acquired pneumonia.L14006, A203369 However, after completing phase III clinical trials, it was deemed safe but not sufficiently efficacious by the FDA.A203369

Since this time, cethromycin has received FDA orphan drug designations for the prophylactic treatment of anthrax inhalation, plague due to Yersinia pestis, and tularemia due to Francisella tularensis.L13988 It has also been investigated, by itself or together with zoliflodacin, for the treatment of gonorrhea,A203432, A203495 and was recently suggested as a possible treatment for liver-stage Plasmodium sporozoite infection.A203441

Struktur Molekul 2D

Berat 765.945
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Cethromycin given in five oral doses of 150 or 300 mg has a plasma half-life of 4.85 ± 1.10 and 4.94 ± 0.66 hrs, respectively.[A203414] A single oral dose of 150 mg produced a measured half-life of 5.66 ± 0.77 hrs.[A203429]
Volume Distribusi Cethromycin given in five 150 mg oral doses had an apparent volume of distribution at the terminal elimination phase of 1433 ± 843 L, and an apparent steady-state volume of distribution of 1453 ± 997 L. The corresponding values for a 300 mg dose was 761 ± 293 L and 769 ± 272 L.[A203414] Cethromycin is known to accumulate in the epithelial lining fluid and alveolar cells,[A203414] as well as within polymorphonuclear leukocytes.[A203426]
Klirens (Clearance) Cethromycin clearance in patients receiving a once-daily oral dose of 300 mg is reported to be approximately 63 L/h.[A203414]

Absorpsi

Cethromycin displays non-linear absorption kinetics. In healthy adults administered 150 mg cethromycin orally once daily for five doses, the calculated Cmax, Tmax, and AUC0-24 values were 0.181 ± 0.084 ?g/ml, 2.01 ± 1.30 hrs, and 0.902 ± 0.469 ?g\*h/ml, respectively. Similarly, the corresponding values for a 300 mg dose were 0.500 ± 0.168 ?g/ml, 2.09 ± 0.03 hrs, and 3.067 ± 1.205 ?g\*h/ml, respectively.A203414 In another study using a single oral dose of 150 mg cethromycin, the Cmax was 318 ± 161 ng/ml, the Tmax was 1.79 ± 0.50, the AUC0-24 was 1596 ± 876 ng\*h/ml, and the AUC0-? was 1662 ± 907 ng\*h/ml.A203429

Metabolisme

Extensive studies of cethromycin metabolism have not been conducted, although one study identified seven metabolites within feces of patients administered a single 150 mg oral dose. The major recovered products were unchanged cethromycin and an inactive N-desmethyl metabolite. It is likely that most of the metabolism occurs in the liver and is mediated, at least in part, by CYP3A4.L14003

Rute Eliminasi

Cethromycin is primarily excreted by the biliary route, with 87.2% of an initial dose recovered in feces and only 7.0% in urine. Unchanged cethromycin accounted for 35.7% of the radioactivity recovered in feces and an N-desmethyl metabolite for 39.8%; the remaining radioactivity was approximately evenly divided between three minor metabolites and a group of uncharacterized additional products.L14003

Interaksi Obat

672 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Cethromycin.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Cethromycin.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Cethromycin.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Cethromycin.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Cethromycin.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Cethromycin.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Cethromycin.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Cethromycin.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Cethromycin.
Silodosin The excretion of Silodosin can be decreased when combined with Cethromycin.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Cethromycin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Cethromycin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Cethromycin.
Alfentanil The serum concentration of Alfentanil can be increased when it is combined with Cethromycin.
Buspirone The metabolism of Buspirone can be decreased when combined with Cethromycin.
Carbamazepine The metabolism of Carbamazepine can be decreased when combined with Cethromycin.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Cethromycin.
Disopyramide Cethromycin may increase the QTc-prolonging activities of Disopyramide.
Estazolam The serum concentration of Estazolam can be increased when it is combined with Cethromycin.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Cethromycin.
Quinine The serum concentration of Quinine can be increased when it is combined with Cethromycin.
Quinidine The serum concentration of Quinidine can be increased when it is combined with Cethromycin.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Cethromycin.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Cethromycin.
Sirolimus The metabolism of Sirolimus can be decreased when combined with Cethromycin.
Temsirolimus The metabolism of Temsirolimus can be decreased when combined with Cethromycin.
Terfenadine The serum concentration of Terfenadine can be increased when it is combined with Cethromycin.
Triazolam The serum concentration of Triazolam can be increased when it is combined with Cethromycin.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Cethromycin.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Cethromycin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Cethromycin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Cethromycin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Cethromycin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Cethromycin.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Cethromycin.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Cethromycin.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Cethromycin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Cethromycin.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Cethromycin.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Cethromycin.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Cethromycin.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Cethromycin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Cethromycin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Cethromycin.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Cethromycin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Cethromycin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Cethromycin.
Telaprevir The serum concentration of Telaprevir can be increased when it is combined with Cethromycin.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Cethromycin.
Vincristine The excretion of Vincristine can be decreased when combined with Cethromycin.
Vintafolide The serum concentration of Vintafolide can be increased when it is combined with Cethromycin.
Vincamine The serum concentration of Vincamine can be increased when it is combined with Cethromycin.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be increased when it is combined with Cethromycin.
Deslanoside The serum concentration of Deslanoside can be increased when it is combined with Cethromycin.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Cethromycin.
Oleandrin The serum concentration of Oleandrin can be increased when it is combined with Cethromycin.
Cymarin The serum concentration of Cymarin can be increased when it is combined with Cethromycin.
Proscillaridin The serum concentration of Proscillaridin can be increased when it is combined with Cethromycin.
Lanatoside C The serum concentration of Lanatoside C can be increased when it is combined with Cethromycin.
Gitoformate The serum concentration of Gitoformate can be increased when it is combined with Cethromycin.
Peruvoside The serum concentration of Peruvoside can be increased when it is combined with Cethromycin.
Cyclosporine The metabolism of Cyclosporine can be decreased when combined with Cethromycin.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Cethromycin.
Dicoumarol The serum concentration of Dicoumarol can be increased when it is combined with Cethromycin.
Phenindione The serum concentration of Phenindione can be increased when it is combined with Cethromycin.
Coumarin The serum concentration of Coumarin can be increased when it is combined with Cethromycin.
Tioclomarol The serum concentration of Tioclomarol can be increased when it is combined with Cethromycin.
Ethyl biscoumacetate The serum concentration of Ethyl biscoumacetate can be increased when it is combined with Cethromycin.
Diphenadione The serum concentration of Diphenadione can be increased when it is combined with Cethromycin.
4-hydroxycoumarin The serum concentration of 4-hydroxycoumarin can be increased when it is combined with Cethromycin.
Fluindione The serum concentration of Fluindione can be increased when it is combined with Cethromycin.
Clorindione The serum concentration of Clorindione can be increased when it is combined with Cethromycin.
Lumacaftor The serum concentration of Cethromycin can be decreased when it is combined with Lumacaftor.
Oxtriphylline The metabolism of Oxtriphylline can be decreased when combined with Cethromycin.
Doxofylline The metabolism of Doxofylline can be decreased when combined with Cethromycin.
Bamifylline The metabolism of Bamifylline can be decreased when combined with Cethromycin.
Acefylline The metabolism of Acefylline can be decreased when combined with Cethromycin.
Bufylline The metabolism of Bufylline can be decreased when combined with Cethromycin.
Fenethylline The metabolism of Fenethylline can be decreased when combined with Cethromycin.
Proxyphylline The metabolism of Proxyphylline can be decreased when combined with Cethromycin.
Bromotheophylline The metabolism of Bromotheophylline can be decreased when combined with Cethromycin.
Pentoxifylline The metabolism of Pentoxifylline can be decreased when combined with Cethromycin.
8-azaguanine The metabolism of 8-azaguanine can be decreased when combined with Cethromycin.
7,9-Dimethylguanine The metabolism of 7,9-Dimethylguanine can be decreased when combined with Cethromycin.
Xanthine The metabolism of Xanthine can be decreased when combined with Cethromycin.
7-Deazaguanine The metabolism of 7-Deazaguanine can be decreased when combined with Cethromycin.
Guanine The metabolism of Guanine can be decreased when combined with Cethromycin.
9-Methylguanine The metabolism of 9-Methylguanine can be decreased when combined with Cethromycin.
Peldesine The metabolism of Peldesine can be decreased when combined with Cethromycin.
Hypoxanthine The metabolism of Hypoxanthine can be decreased when combined with Cethromycin.
9-Deazaguanine The metabolism of 9-Deazaguanine can be decreased when combined with Cethromycin.
Valomaciclovir The metabolism of Valomaciclovir can be decreased when combined with Cethromycin.
3-isobutyl-1-methyl-7H-xanthine The metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Cethromycin.
Uric acid The metabolism of Uric acid can be decreased when combined with Cethromycin.
6-O-benzylguanine The metabolism of 6-O-benzylguanine can be decreased when combined with Cethromycin.
Lisofylline The metabolism of Lisofylline can be decreased when combined with Cethromycin.
Lobucavir The metabolism of Lobucavir can be decreased when combined with Cethromycin.
Cafedrine The metabolism of Cafedrine can be decreased when combined with Cethromycin.
Theodrenaline The metabolism of Theodrenaline can be decreased when combined with Cethromycin.
Etamiphylline The metabolism of Etamiphylline can be decreased when combined with Cethromycin.

Target Protein

23S ribosomal RNA

Referensi & Sumber

Synthesis reference: Yat Sun Or, Zhenkun Ma, Richard F. Clark, Daniel T. Chu, Jacob J. Plattner. "6-o-substituted ketolides having antibacterial activity". Patent WO1998009978A1, Issued March 12, 1998.
Artikel (PubMed)
  • PMID: 23463743
    Mansour H, Chahine EB, Karaoui LR, El-Lababidi RM: Cethromycin: a new ketolide antibiotic. Ann Pharmacother. 2013 Mar;47(3):368-79. doi: 10.1345/aph.1R435. Epub 2013 Mar 5.
  • PMID: 15328118
    Conte JE Jr, Golden JA, Kipps J, Zurlinden E: Steady-state plasma and intrapulmonary pharmacokinetics and pharmacodynamics of cethromycin. Antimicrob Agents Chemother. 2004 Sep;48(9):3508-15. doi: 10.1128/AAC.48.9.3508-3515.2004.
  • PMID: 12177734
    Champney WS, Pelt J: The ketolide antibiotic ABT-773 is a specific inhibitor of translation and 50S ribosomal subunit formation in Streptococcus pneumoniae cells. Curr Microbiol. 2002 Sep;45(3):155-60. doi: 10.1007/s00284-001-0110-9.
  • PMID: 15469510
    Vimberg V, Xiong L, Bailey M, Tenson T, Mankin A: Peptide-mediated macrolide resistance reveals possible specific interactions in the nascent peptide exit tunnel. Mol Microbiol. 2004 Oct;54(2):376-85. doi: 10.1111/j.1365-2958.2004.04290.x.
  • PMID: 15127365
    Edelstein PH: Pneumococcal resistance to macrolides, lincosamides, ketolides, and streptogramin B agents: molecular mechanisms and resistance phenotypes. Clin Infect Dis. 2004 May 15;38 Suppl 4:S322-7. doi: 10.1086/382687.
  • PMID: 12805263
    Garcia I, Pascual A, Ballesta S, del Castillo C, Perea EJ: Accumulation and activity of cethromycin (ABT-773) within human polymorphonuclear leucocytes. J Antimicrob Chemother. 2003 Jul;52(1):24-8. doi: 10.1093/jac/dkg290. Epub 2003 Jun 12.
  • PMID: 12604553
    Pletz MW, Preechachatchaval V, Bulitta J, Allewelt M, Burkhardt O, Lode H: ABT-773: pharmacokinetics and interactions with ranitidine and sucralfate. Antimicrob Agents Chemother. 2003 Mar;47(3):1129-31. doi: 10.1128/aac.47.3.1129-1131.2003.
  • PMID: 31106713
    Jacobsson S, Alirol E, Unemo M: In vitro activity of the ketolide cethromycin in multidrug-resistant clinical Neisseria gonorrhoeae isolates and international reference strains. J Chemother. 2019 Sep;31(5):246-251. doi: 10.1080/1120009X.2019.1615724. Epub 2019 May 20.
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Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Restanza

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