Ethambutol

Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.Target: AntibacterialEthambutol 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].

Signaling Pathways >> Anti-infection >> Bacterial

Research Areas >> Infection

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

[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

[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.

Puromycin 2HCl | Geneticin | Tunicamycin | Hygromycin B | Salinomycin | Avibactam sodium | Neomycin sulfate | Vaborbactam | Methicillin SodiuM | Rifampicin | Metronidazole | Carbenicillin disodium | Ceftazidime | Eravacycline dihydrochloride | cefotaxime sodium

MOLECULAR FORMULA :

C10-H24-N2-O2

MOLECULAR WEIGHT :

204.36

WISWESSER LINE NOTATION :

Q1Y2&M2MY2&1Q -D

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

900 mg/kg/60D-I

TOXIC EFFECTS :

Liver - jaundice, cholestatic

REFERENCE :

BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 292,866,1986

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

600 mg/kg

TOXIC EFFECTS :

Peripheral Nerve and Sensation - structural change in nerve or sheath Behavioral - changes in motor activity (specific assay) Kidney, Ureter, Bladder - other changes in urine composition

REFERENCE :

BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,1105,1976

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

1200 mg/kg

TOXIC EFFECTS :

Skin and Appendages - dermatitis, other (after systemic exposure) Immunological Including Allergic - anaphylaxis

REFERENCE :

BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,1105,1976

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

8700 mg/kg

TOXIC EFFECTS :

Behavioral - convulsions or effect on seizure threshold

REFERENCE :

DPHFAK Dissertationes Pharmaceuticae et Pharmacologicae. (Warsaw, Poland) V.18-24, 1966-72. For publisher information, see PJPPAA. Volume(issue)/page/year: 23,463,1971

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1075 mg/kg

TOXIC EFFECTS :

Behavioral - convulsions or effect on seizure threshold

REFERENCE :

DPHFAK Dissertationes Pharmaceuticae et Pharmacologicae. (Warsaw, Poland) V.18-24, 1966-72. For publisher information, see PJPPAA. Volume(issue)/page/year: 23,463,1971

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

240 mg/kg

TOXIC EFFECTS :

Behavioral - convulsions or effect on seizure threshold

REFERENCE :

DPHFAK Dissertationes Pharmaceuticae et Pharmacologicae. (Warsaw, Poland) V.18-24, 1966-72. For publisher information, see PJPPAA. Volume(issue)/page/year: 23,463,1971

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - species unspecified

DOSE/DURATION :

890 mg/kg

TOXIC EFFECTS :

Lungs, Thorax, or Respiration - other changes

REFERENCE :

NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 63(3),114S,1967

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Mammal - species unspecified

DOSE/DURATION :

350 mg/kg

TOXIC EFFECTS :

Lungs, Thorax, or Respiration - other changes

REFERENCE :

NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 63(3),114S,1967