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At least 19 recordsLinked to original sources
PubMed1991

Comparison of bacteriostatic and bactericidal activity of isoniazid and ethionamide against Mycobacterium avium and Mycobacterium tuberculosis.

Minimal inhibitory and bactericidal concentrations (MIC and MBC) of isoniazid and ethionamide were determined in 7H12 broth in experiments with 68 Mycobacterium avium strains and 14 wild drug-susceptible M. tuberculosis strains. MICs of isoniazid for M. tuberculosis were from 0.025 to 0.05 microgram/ml, and for M. avium from 0.6 to greater than 10.0 micrograms/ml. MICs of ethionamide for M. tuberculosis were from 0.3 to 1.25 micrograms/ml, and 42.7% of M. avium strains were within the same range. Isoniazid and ethionamide were highly bactericidal against M. tuberculosis, but they had very low bactericidal activity against M. avium.

Colony Count, Microbial↗
PubMed1990

[In-vitro susceptibility of Mycobacterium avium complex to isoniazid and ethionamide].

In this study, it was investigated whether or not Mycobacterium avium complex strains were inhibited by such low concentrations of isoniazid and ethionamide as possible in blood. The inhibitory concentrations were determined by the "Actual Count" method (Tsukamura, M.: Japan J. Tuberc. 12: 46-54, 1964), in which the inhibitory concentration was measured as a concentration that can inhibit the growth of 'countable' colony-forming units. The ratio of strains which were inhibited by such low concentrations as 0.2 microgram/ml isoniazid or 5 micrograms/ml ethionamide was 14%. The result suggests that there are some strains in which isoniazid or ethionamide are clinically effective, though their prevalence was low (14%).

Ethionamide↗
PubMed1991

Improved high-performance liquid chromatographic assay for the determination of ethionamide in serum.

A solid-phase extraction (SPE) method was developed to simplify the preparation of human serum prior to high-performance liquid chromatography of ethionamide (ETA). Octadecyl SPE columns were used. Serum constituents were removed from the column with water, and ETA was eluted with methanol. Samples were evaporated to dryness, reconstituted in mobile phase, and assayed. The method is reproducible, with a recovery of ETA of 64%, comparable to the more tedious liquid-liquid extraction method for ETA.

Chromatography, High Pressure Liquid↗
PubMed1992

Mycolic acid synthesis: a target for ethionamide in mycobacteria?

Striking structural analogies exist between the two specific antimycobacterial drugs ethionamide (ETH) and isoniazid (INH), and they share several inhibitory properties in susceptible species of mycobacteria. The effect of ETH on mycolic acid synthesis was studied in whole cells and in cell extracts of various species, since this synthesis is one direct target for INH, as we recently demonstrated in cell extracts of Mycobacterium aurum. It was shown in the present study that there is not a direct relationship between ETH susceptibility and mycolic acid inhibition. This observation could explain the lack of cross-resistance between the two drugs. The presence of ETH disturbed mycolic acid synthesis in both resistant and susceptible mycobacteria. Synthesis of oxygenated species of mycolic acid was inhibited, while that of diunsaturated acids was either slightly altered or even increased. In contrast, INH inhibited the synthesis of all kinds of mycolic acids in the same way in all susceptible strains and had no effect on mycolic acid synthesis in resistant strains. In the presence of ETH, the unsaturated mycolic acid molecules presented a methyl end different from the usual one. These data strongly suggest that the normal unsaturated mycolic acid species are not the precursors of the oxygenated types. Moreover, they show that ETH probably acts early in the pathway leading to oxygenated mycolic acid.

Drug Resistance, Microbial↗
PubMed1991

Pharmacokinetic evaluation of ethionamide suppositories.

The absorption and elimination of ethionamide (ETA) after oral tablets and rectal suppositories were determined in 12 healthy, adult male volunteers. A randomized, double-blind, double-dummy, crossover design was used. Treatments compared 250-mg ETA tablets and a placebo suppository to a 500-mg ETA suppository and two placebo tablets, given 7 days apart. Blood samples were collected at predetermined intervals for 12 hours after the dose. Serum concentrations of ETA were determined using high-performance liquid chromatography. The area under the serum concentration-time curve was used to compare the relative bioavailability of ETA from the two preparations. Relative bioavailability after rectal administration was 57.3% of that after oral administration. The maximum serum concentration after rectal administration was 33% of that after oral administration. Higher doses of ETA and serum concentration monitoring are recommended whenever the suppositories are used.

Administration, Oral↗
PubMedDate not supplied

[Sensitivity to dapsone, sulfamethoxypyridazine and ethionamide of mycobacterium leprae taken from patients treated by the drugs].

Suspensions of M. leprae from skin biopsies of patients treated with dapsone (DDS) (four cases), sulfamethoxypyridazine (SMP) (six cases), and ethionamide (ETH) (seven cases), were inoculated into mouse foot pads and their sensitivity for the different drugs determined. Two strains were DDS resistant. Resistance appeared after 13 and 14 years respectively after the start of treatment. Five strains were isolated from patients treated with SMP. Relapses during sulfonamide treatment are considered to be due to the low effective serum concentrations reached by SMP, a situation which is aggravated by irregularities in drug intake. Fortunately all strains were sensitive to SMP and DDS as well. Four strains were ETH resistant. ETH resistance at the present moment reaches 4% and appeared in two cases six years after the start of treatment. It is concluded that SMP is not indicated for the treatment of multibacillary leprosy and that ETH can be used only in association with other drugs during the introductory phase of treatment of multibacillary forms of leprosy.

Animals↗