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PubMedDate not supplied

Tissue fluid penetration and anti-treponemal activity of trospectomycin (a new spectinomycin analog) in the rabbit syphilis model.

The antitreponemal activity of trospectomycin (a novel 6'-propyl analog of spectinomycin) was correlated with concentrations in serum and tissue chamber fluid in a cutaneously-infected rabbit model of syphilis. After single-dose intramuscular (im) injections of trospectomycin, spectinomycin hydrochloride, and aqueous procaine penicillin G(APPG), concentrations of the drugs in paired specimens of serum and tissue fluid were determined and correlated with response of Treponema pallidum-infected lesions. Lesions responded most rapidly in APPG-treated animals. Rapid response correlated with more prolonged levels of APPG in both serum and tissue fluid. Trospectomycin, when given in single doses exceeding 40 mg/kg, surpassed penicillin in peak serum levels (greater than 60 micrograms/ml at 1 hr) but not in duration of activity. Higher and prolonged concentrations of trospectomycin in tissue fluid correlated with more effective clearance of treponemes from cutaneous lesions. Animals treated with less than 40 mg of trospectomycin/kg or with 20-80 mg/kg of the parent compound (spectinomycin hydrochloride) had cutaneous lesions that were persistently darkfield-positive, as confirmed by three or more consecutive smears.

Animals↗
PubMed1977

In vitro activity of spectinomycin against recent urinary tract isolates.

The susceptibilities to spectinomycin of 303 recent urinary tract isolates were determined and compared to the susceptibilities of those strains to ampicillin, tetracycline, and gentamicin. Based on minimal inhibitory concentrations, 84% of Escherichia coli, Klebsiella, and Enterobacter, 31% of other Enterobacteriaceae, 7% of Staphylococcus aureus and Streptococcus (including enterococci), and 0% of Pseudomonas aeruginosa were susceptible to concentrations of spectinomycin that are easily surpassed in serum (</=32 mug/ml); 90% of all organisms tested other than P. aeruginosa were susceptible to concentrations that are easily surpassed in urine (</=128 mug/ml). Spectinomycin was active against more isolates than either ampicillin or tetracycline but against fewer isolates than gentamicin. Disk diffusion susceptibility tests did not reliably distinguish susceptible from resistant isolates with any of the four antibiotics studied.

Anti-Bacterial Agents↗
PubMed1984

In vitro activities of the spectinomycin analog U-63366 and four quinolone derivatives against Neisseria gonorrhoeae.

The in vitro activities of the new spectinomycin analog U-63366 and four new quinolone derivatives, rosoxacin, norfloxacin, ofloxacin, and ciprofloxacin, were compared with those of penicillin, tetracycline, thiamphenicol, cefotaxime, ceftriaxone, and spectinomycin against 222 beta-lactamase-negative and 25 beta-lactamase-positive Neisseria gonorrhoeae strains. U-63366 was more active than spectinomycin, inhibiting 90% of the strains at a concentration of 2 mg/liter. Among the quinolone derivatives, ciprofloxacin was the most active compound in vitro (90% MIC, 0.002 mg/liter), followed by ofloxacin (90% MIC, 0.008 mg/liter), norfloxacin (90% MIC, 0.015 mg/liter), and rosoxacin (90% MIC, 0.03 mg/liter).

4-Quinolones↗
PubMed1986

Comparative study of cefoperazone and spectinomycin for treatment of uncomplicated gonorrhea in men.

Beta-lactamase-negative Neisseria gonorrhoeae infections were treated with single-dose cefoperazone (0.5 or 1.0 g) or spectinomycin (2.0 g). Anogenital infections were cured in 36 (83%) of 43 volunteers given 0.5 g of cefoperazone, 61 of 61 volunteers given 1.0 g of cefoperazone, and 99 of 100 volunteers given spectinomycin. The cefoperazone geometric mean MIC for 242 isolates was 0.028 microgram/ml. Cefoperazone (1.0 g) and spectinomycin (2.0 g) are comparable for the therapy of anogenital gonorrhea in men.

Adolescent↗
PubMed1988

Spectinomycin disk zone diameter as a predictor of outcome in clinical treatment of gonorrhea.

The MICs for 41 Neisseria gonorrhoeae strains from patients receiving spectinomycin treatment were determined by the agar dilution method and compared with the zones of inhibition produced by disks containing 100 micrograms of spectinomycin. Our data demonstrated a good correlation between the two methods. Moreover, a zone of inhibition of less than or equal to 15 mm was a good predictor of clinical treatment failures with spectinomycin.

Drug Resistance, Microbial↗
PubMed1997

Isolation of a gene encoding a novel spectinomycin phosphotransferase from Legionella pneumophila.

A gene capable of conferring spectinomycin resistance was isolated from Legionella pneumophila, the agent of Legionnaires' disease. The gene (aph) encoded a 36-kDa protein which has similarity to aminoglycoside phosphotransferases. Biochemical analysis confirmed that aph encodes a phosphotransferase which modifies spectinomycin but not hygromycin, kanamycin, or streptomycin. The strain that was the source of aph demonstrated resistance to spectinomycin, and Southern hybridizations determined that aph also exists in other legionellae.

Amino Acid Sequence↗
PubMed1974

Comparison of spectinomycin hydrochloride and aqueous procaine penicillin G in the treatment of uncomplicated gonorrhea.

Men and women with uncomplicated gonorrhea were randomly assigned to receive aqueous procaine penicillin G (2,400,000 U for men; 2,400,000 U daily for 2 days for women) or spectinomycin hydrochloride (2.0 g for men; 4.0 g for women). Among men who returned for post-treatment evaluation within 10 days, treatment failures were noted among 16 (20.3%) of 79 men who received penicillin and 8 (9.5%) of 84 men who received spectinomycin (P < 0.1). Similarly, 6 (13.3%) of 45 women who received penicillin and 3 (6.5%) of 46 women who received spectinomycin had positive endocervical cultures for Neisseria gonorrhoeae at the time of the post-treatment examination (P = not significant).

Female↗
PubMed1970

In vitro activity of lincomycin and spectinomycin against serotypes of avian mycoplasma.

Twenty strains of avian mycoplasma, representing 12 serotypes, were tested in vitro for their susceptibility to the action of lincomycin and spectinomycin alone and in combination. They varied in their sensitivity pattern. The ranges of minimal inhibitory concentration were 1 to 20 mug/ml for lincomycin or spectinomycin alone and 0.5/1 to 3/6 mug/ml for the lincomycin and spectinomycin combination. The ranges of minimal lethal concentration were greater with either single antibiotic than with the antibiotic combination. The amount of each antibiotic required to achieve mycoplasmacidal action of the relatively resistant strains was less with the antibiotic combination than with the single antibiotics.

Air Sacs↗
PubMed1983

Spectinomycin resistance due to a mutation in an rRNA operon of Escherichia coli.

A spectinomycin resistance mutation was isolated in an Escherichia coli rRNA operon (rrnH) located on a multicopy plasmid. Cell-free protein-synthesizing extracts made from cells containing the plasmid were partially resistant to spectinomycin. Although spectinomycin is an aminoglycoside antibiotic, the mutation did not confer resistance to any other aminoglycoside antibiotic tested.

Aminoglycosides↗
PubMed1989

Standardization of disk diffusion and agar dilution susceptibility tests for Neisseria gonorrhoeae: interpretive criteria and quality control guidelines for ceftriaxone, penicillin, spectinomycin, and tetracycline.

A six-laboratory study developed a standardized method for determining the susceptibilities of Neisseria gonorrhoeae strains to penicillin, tetracycline, spectinomycin, and ceftriaxone. Three quality control organisms were also selected, and quality assurance guidelines were initially generated for the disk diffusion and agar dilution methods. The medium recommended for gonococcal susceptibility testing was GC agar with a defined "XV-like" supplement. The supplement should be free of cysteine, a component implicated in the inactivation of some newer beta-lactam compounds. Penicillin, tetracycline, spectinomycin, and ceftriaxone were stable in agar plates stored at 3 to 5 degrees C for at least 2 weeks. Numerous GC agar and drug disk lots were used during the trials without significant variation in test results. Several other gonococcal strains were recommended for additional medium quality assurance. The disk quality control zone limits were established for N. gonorrhoeae ATCC 49226 (formerly CDC F-18) and Staphylococcus aureus ATCC 25923. MIC quality control ranges were also developed for N. gonorrhoeae ATCC 49226 and S. aureus ATCC 29213. The interpretive criteria for penicillin were as follows: susceptibility, greater than or equal to 47 mm (diameter of inhibition zone) (less than or equal to 0.06 micrograms/ml [MIC]); resistance, less than or equal to 26 mm (greater than or equal to 2 micrograms/ml). For tetracycline they were as follows: susceptibility, greater than or equal to 38 mm (less than or equal to 0.25 microgram/ml); resistance, less than or equal to 30 mm (greater than or equal to 2 micrograms/ml). For spectinomycin they were as follows: susceptibility, >/= 18 mm (</= 32 micrograms/ml); resistance, </= 14 mm (>/= 128 micrograms/ml). For ceftriaxone susceptibility, the criterion was >/= 35 mm (</= 0.25 micrograms/ml) with no other category. Criteria of </= 19 mm for plasmid-mediated resistances to penicillin and tetracycline were also confirmed. The false-susceptibility errors were </= 1% with these criteria.

Ceftriaxone↗
PubMed1977

Treatment of uncomplicated gonorrhoea with spectinomycin hydrochloride (Trobicin).

110 patients with uncomplicated gonococcal urethritis were treated with 2 g spectinomycin (Trobicin) intramuscularly. Seventy-five patients were available for follow-up and there was only one treatment failure, giving a cure rate of 98-6%. Of the 99 gonococcal isolates, 59 were sensitive to 5 microng/ml of spectinomycin or less and 40 were sensitive to 10 microng/ml. In a small sample of patients 2 g spectinomycin intramuscularly produced a serum concentration averaging 100 microng/ml after one hour.

Gonorrhea↗
PubMed1977

Spectinomycin hydrochloride in the treatment of gonorrhoea: Its effect on associated Chlamydia trachomatis infections.

Sixty-three heterosexual men were successfully treated with a single injection of spectinomycin hydrochloride 2 g for urethral infections with Neisseria gonorrhoeae. Chlamydia trachomatis was recovered from the urethra of 11 of these men both before and after treatment. In six men, the organism was isolated after but not before treatment. No isolates were obtained from the remaining men either before or after treatment. All 17 of the men who yielded C. trachomatis developed post-gonococcal urethritis. Eight of 46 men from whom no isolate was obtained in their cultures developed post-gonococcal urethritis. Seventeen of 50 women successfully treated with spectinomycin for cervical infections with N. gonorrhoeae yielded isolates of C. trachomatis both before and after treatment. The organism was isolated from five women before but not after treatment, and from four women after but not before treatment. In 24 women culture for C. trachomatis was negative both before and after treatment. Spectinomycin hydrochloride in the dosage used rarely eliminated C. trachomatis from the genital tract of either men or women; in this respect it resembled two other drugs commonly used for the treatment of gonorrhoea-pencillin and ampicillin.

Chlamydia Infections↗
PubMed1980

Sensitivity of Neisseria gonorrhoeae to spectinomycin and thiamphenicol.

Between 1966 and 1978 the sensitivities of strains of Neisseria gonorrhoeae (70-80 strains in each year) to penicillin, thiamphenicol, and spectinomycin were tested. For penicillin the proportion of less sensitive strains increased from 21% in 1976 to 41% in 1978 and for thiamphenicol from 10% to 18% over the same period. All the strains proved to be sensitive to spectinomycin. A significant correlation in the degree of sensitivity was observed between penicillin and thiamphenicol but not between penicillin and spectinomycin.

Microbial Sensitivity Tests↗
PubMed1982

Treatment of uncomplicated gonorrhoea in women. Comparison of rosoxacin and spectinomycin.

A comparative study of the new antibacterial agent, rosoxacin, a quinoline derivative, with spectinomycin was made in women with uncomplicated cervical, urethral, pharyngeal, and rectal gonorrhoea. Rosoxacin was given in three oral regimens: 200 mg in a single dose, 300 mg in a single dose, and 300 mg in two doses of 150 mg four hours apart. All culture results 72 hours after administration were negative for Neisseria gonorrhoeae in all 81 women compared with 107 of 109 who received 2 g spectinomycin intramuscularly. Thirty-five of the women successfully treated with rosoxacin harboured penicillinase-producing strains of N gonorrhoeae (PPNG) and 46 non-penicillinase-producing (non-PPNG) strains. Fifty of the women treated with spectinomycin had PPNG strains and 59 non-PPNG strains. Mild self-limiting side effects, principally dizziness, occurred in varying frequency with rosoxacin, but these were difficult to evaluate owing to the characteristics of the patient population and the conditions under which the study was conducted.

4-Quinolones↗
PubMed1985

Randomised comparative study of ceftriaxone and spectinomycin in gonorrhoea.

From 26 April to 30 June 1983 a total of 200 men with uncomplicated gonococcal urethritis were randomly treated with either 2 g spectinomycin or 250 mg ceftriaxone, both administered intramuscularly. Of 197 isolates tested for the presence of the enzyme beta lactamase, 91 (46.2%) were positive (PPNG) and 106 (53.8%) were non-PPNG strains. All 93 patients treated with spectinomycin and followed up and 97 treated with ceftriaxone and followed up were cured. Ceftriaxone 250 mg administered by intramuscular injection is highly effective in treating gonococcal infections caused by both PPNG and non-PPNG strains and is an appropriate alternative to spectinomycin.

Cefotaxime↗
PubMed2000

Comparison of in vitro activity of danofloxacin, florfenicol, oxytetracycline, spectinomycin and tilmicosin against recent field isolates of Mycoplasma bovis.

The minimum inhibitory concentrations (MICS) and minimum mycoplasmacidal concentrations (MMCs) of danofloxacin, florfenicol, oxytetracycline, spectinomycin and tilmicosin against 62 recent British field isolates of Mycoplasma bovis were determined in vitro by a broth microdilution method. The isolates were most susceptible todanofloxacin with MIC90 and MMC90 values of 0.5 microg/ml and 1.0 microg/ml, respectively. They were less susceptible to florfenicol with a MIC90 of 16 microg/ml and MMC90 of 32 microg/ml. Oxytetracycline and spectinomycin had only a limited effect against the majority of isolates tested with MIC50s of 32 microg/ml and 4 microg/ml, respectively and MIC90s of 64 microg/ml and more than 128 microg/ml, respectively. Nearly 20 per cent of the isolates were highly resistant to spectinomycin, and tilmicosin was ineffective, with 92 per cent of the isolates having MIC values of 128 microg/ml or greater. There was no evidence of resistance by M bovis to danofloxacin.

Animals↗
PubMed1983

Randomized prospective study of the comparative efficacy of spectinomycin and gentamicin in urinary tract infections.

A prospective, randomized study was undertaken in 32 hospitalized patients with urinary tract infections to compare the efficacy of spectinomycin versus gentamicin. Spectinomycin was found to be of equal efficacy if not more efficacious in eradicating Escherichia coli, Klebsiella and Proteus mirabilis in our patient population. No significant side-effects were noted. A review of the literature with emphasis on the use of spectinomycin in infections other than anogenital gonorrhea is made.

Adult↗
PubMed1976

Effect of spectinomycin on peptide chain initiation.

Spectinomycin inhibits the formation and causes dissociation of performed specific cell-free initiation complexes prepared with the trinucleotide A-U-G or R17 phage RNA, fmet-RNAF and either 30S ribosomal subunits or 70S ribosomes. Both the initiation factor and the Mg2+-induced processes are subject to inhibition by spectinomycin. The only exception is the Mg2+-induced 70S initiation system formed with A-U-G which is stimulated by spectinomycin.

Cell-Free System↗