Ethambutol  (Synonyms: 乙胺丁醇)

Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases. Target: Antibacterial Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].

204.31

C₁₀H₂₄N₂O₂

74-55-5

固体

White to off-white

乙胺丁醇；乙二胺二丁醇；乙二胺丁醇

Room temperature in continental US; may vary elsewhere.

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• [1]. Ethambutol. Tuberculosis (Edinb), 2008. 88(2): p. 102-5.  [Content Brief]

  [2]. Rastogi, N., V. Labrousse, and K.S. Goh, In vitro activities of fourteen antimicrobial agents against drug susceptible and resistant clinical isolates of Mycobacterium tuberculosis and comparative intracellular activities against the virulent H37Rv strain in human macrophages. Curr Microbiol, 1996. 33(3): p. 167-75.  [Content Brief]

  [3]. Kaur, D. and G.K. Khuller, In vitro, ex-vivo and in vivo activities of ethambutol and sparfloxacin alone and in combination against mycobacteria. Int J Antimicrob Agents, 2001. 17(1): p. 51-5.  [Content Brief]

  [4]. Kang L, Miao JX, Cao LH, Miao YY, Miao MS, Liu HJ, Xiang LL, Song YG. Total glucosides of herbaceous peony (Paeonia lactiflora Pall.) flower attenuate adenine- and ethambutol-induced hyperuricaemia in rats. J Ethnopharmacol. 2020 Oct 28;261:113054.  [Content Brief]

  [5]. Pham AQ, Doan A, Andersen M. Pyrazinamide-induced hyperuricemia. P T. 2014 Oct;39(10):695-715.  [Content Brief]

  [6]. Nusanti S, Sari RI, Siregar NC, Sidik M. The Effect of Citicoline on Ethambutol Optic Neuropathy: Histopathology and Immunohistochemistry Analysis of Retina Ganglion Cell Damage Level in Rat Model. J Ocul Pharmacol Ther. 2022 Oct;38(8):584-589.  [Content Brief]