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PubMed1983

Comparative study of ceftriaxone and spectinomycin for treatment of uncomplicated gonorrhoea in men.

Single-dose ceftriaxone, 125 mg or 250 mg intramuscularly (IM), was compared with spectinomycin, 2 g IM, for treatment of men with uncomplicated urethral or anorectal infections due to penicillinase-negative Neisseria gonorrhoeae. Cure rates were 100% for 31 and 28 men treated with 125 mg and 250 mg ceftriaxone, respectively, and 97% for 58 men given spectinomycin. Among patients followed up for greater than or equal to 14 days, post-gonococcal urethritis occurred in 25% of 44 men treated with ceftriaxone and 19% of 47 given spectinomycin (p = NS). The geometric mean minimum inhibitory concentration of ceftriaxone for 79 pre-treatment isolates of N gonorrhoeae was 0.0058 microgram/ml, and all strains were inhibited by less than or equal to 0.063 micrograms/ml. Neither drug caused perceptible toxicity, but patient acceptance was greater for ceftriaxone than for spectinomycin. Ceftriaxone in a single dose of 125 mg is effective against uncomplicated urethral or anorectal gonorrhoea in men and may become a regimen of choice for this infection.

Cefotaxime↗
PubMed1972

Treatment of gonorrhea with spectinomycin hydrochloride: comparison with standard penicillin schedules.

Spectinomycin hydrochloride, a new parenteral antibiotic prepared from Streptomyces spectabilis, was compared with standard U.S. Public Health Service-recommended dosages of aqueous procaine penicillin G in the treatment of uncomplicated gonorrhea in 353 men and 314 women. Of the 314 women, 130 had a pretreatment positive rectal culture. All diagnoses were proven by culture on Thayer-Martin selective medium. Minimal inhibitory concentrations of both drugs were determined. Single doses of 2 and 4 g of spectinomycin were compared with 2.4 million units of procaine penicillin in males and with both 2.4 and 4.8 million units of procaine penicillin in females. Both spectinomycin schedules, 2.4 million units of penicillin in males and 4.8 million units of penicillin in females, resulted in cure rates in excess of 90%. There were no failures at the rectal site only in those women with positive rectal cultures. There was no advantage to using the larger amount of spectinomycin in either sex.

Antibiotics, Antineoplastic↗
PubMed1977

Activity of spectinomycin against anaerobes.

The in vitro inhibitory activity of spectinomycin was tested against various anaerobic bacteria. Different results were obtained with different media and with different initial pH's of the media. The highest minimum inhibitory concentrations for Bacteroides fragilis ([Formula: see text] 128 mug/ml) were obtained with the use of Wilkins-Chalgren agar (pH 7.2) and Brucella blood agar (pH 7.0). Brucella blood agar at higher pH's (7.4 and 8.0) and Mueller-Hinton and Diagnostic Sensitivity Test agars produced lower minimum inhibitory concentrations (32 and 64 mug/ml). This same relationship between spectinomycin activity and pH of the medium was, in general, observed with these media and other anaerobes, including isolates of B. melaninogenicus, Fusobacterium, gram-positive cocci, Clostridium perfringens, and C. ramosum. The variable results observed in this study and in two others make it difficult to predict the clinical usefulness of spectinomycin in the treatment of anaerobic infections. It is probably most appropriate to be guided by results obtained with Wilkins-Chalgren agar and the method proposed as a reference to the National Committee for Clinical Laboratory Standards. These results indicate that spectinomycin is not a potent inhibitor of B. fragilis or other clinically significant anaerobes.

Anaerobiosis↗
PubMed1980

Penetration of spectinomycin into cerebrospinal fluid duirng experimental meningitis.

The concentration of spectinomycin in serum and cerebrospinal fluid was compared in rabbits with and without experimental pneumococcal meningitis. When injected intravenously, spectinomycin could not be detected in the cerebrospinal fluid of normal rabbits. In rabbits with meningeal inflammation, however, spectinomycin penetrated the blood-brain barrier and produced significant cerebrospinal fluid concentrations, equal to or well above spectinomycin minimal inhibitory concentrations for many bacterial species.

Animals↗
PubMed1982

Derivatives of 4-dihydro-4-deoxy-4(R)-amino spectinomycin and their activity against susceptible and resistant Escherichia coli strains.

A number of alkyl and acyl derivatives of 4-dihydro-4-deoxy-4(R)-amino spectinomycin were tested against various Escherichia coli strains, possessing different susceptibilities to spectinomycin. The influence of the lipophilicity and the length of the side chain substituents of the derivatives was compared to both minimal inhibitory concentration values and stability to adenyltransferase. Derivatives with a chain length of more than 10 carbon atoms demonstrated a significantly higher activity against all investigated strains, whether susceptible or resistant. The same inhibitory effect was achieved with short-chain aminoacyl derivatives only against susceptible strains. Other short-chain derivatives possessed no advantage to spectinomycin. A 10-fold decrease in the affinity for adenyltransferase was achieved in compounds with a high lipophilicity (log P), i.e., in aliphatic substituted derivatives with a log P greater than 4 and in benzoyl-substituted derivatives with a log P greater than 2. Derivatives with branched alkyl chains and long side chains displayed a different mode of action than spectinomycin. They possessed strong activity against strains with an altered ribosomal binding site and a decreased influence of pH on antimicrobial activity.

Escherichia coli↗
PubMed1991

Cloning and nucleotide base sequence analysis of a spectinomycin adenyltransferase AAD(9) determinant from Enterococcus faecalis.

Enterococcus faecalis LDR55, a human clinical isolate, is resistant to tetracycline (Tcr), erythromycin (Emr), and high levels (greater than 2,000 micrograms/ml) of spectinomycin (Spr) but not streptomycin. Filter matings between strain LDR55 and E. faecalis OG1-RF produced transconjugants with the following resistance phenotypes: Tcr Emr Spr, Tcr Emr, Tcr Spr, and Tcr only but never Emr or Spr only. The genetic determinant encoding resistance to spectinomycin was cloned in Streptococcus sanguis Challis from pDL55, a 26-kb plasmid harbored by a Tcr Spr transconjugant. Subcloning experiments yielded a 1.1-kb ClaI-NdeI fragment that encoded very high-level Spr in S. sanguis (10 mg/ml) and Escherichia coli (50 mg/ml). Cell extracts of cultures obtained from Spr strains expressed adenylating activity for spectinomycin but not for streptomycin, indicating that Spr was due to an AAD(9) activity. The nucleotide base sequence of the 1.1-kb ClaI-NdeI fragment contained a single 750-base open reading frame. The protein predicted from the open reading frame consisted of 250 amino acids and had a calculated size of approximately 28,000 daltons, similar to the size estimated from maxicell analysis (29,000 daltons). The deduced amino acid sequence of the streptococcal AAD(9) was compared with that of the AAD(9) encoded by staphylococcal transposon Tn554. The two proteins shared approximately 39% amino acid identity, which was expanded to 53% when conservative amino acid changes were included. When the streptococcal protein was compared with an AAD(3")(9) protein of E. coli, the degrees of identity were 27 and 47%, on the basis of actual amino acids and conservative replacements, respectively. The cloning and nucleotide base sequence analyses of the spectinomycin AAD(9) determinant from E. faecalis that results in high-level Spr when transferred to S. sanguis or E. coli are presented.

Base Sequence↗
PubMed1980

Mutation affecting expression of spectinomycin resistance in Bacillus subtilis.

A mutation that affects the expression of spectinomycin resistance in a spectinomycin-resistant (spcA), conditionally asporogenic strain of Bacillus subtilis has been designated srm (spectinomycin resistance modifier). This mutation resulted in altered colony morphology and increased growth rate and sporulation efficiency in the presence of spectinomycin.

Bacillus subtilis↗
PubMed1983

Spectinomycin resistant gonococci.

A study was conducted examining the properties of 10 clinical isolates of spectinomycin resistant gonococci from patients attending clinics at St Mary's and St Thomas's Hospitals, London. All of the isolates produced beta-lactamase and contained plasmids of 2.6, 4.4, and 24.5 megadaltons and required proline for growth. None produced aminoglycoside modifying enzymes. Resistance to spectinomycin was transferred from some of the isolates by transformation but at a much lower frequency than resistance to streptomycin. The isolates from St Mary's Hospital were detected after therapy with spectinomycin, whereas those from St Thomas's Hospital were not. Four recent non-beta-lactamase producing gonococci isolated at St Mary's Hospital and two isolated at St Thomas's Hospital also were not related to use of spectinomycin.

Drug Resistance, Microbial↗
PubMed1975

Effect of spectinomycin on T. pallidum in incubating experimental syphilis.

Animal experiments were performed to determine if a single-dose treatment for acute gonorrhoea with 2 g. spectinomycin could cure a simultaneously acquired syphilis at a very early stage of incubation. 300 treponemes (Nichols stain T. pallidum) were inoculated intratesticularly and 3 days later spectinomycin was administered in a dose which produced spectinomycin serum levels similar to those in patients who had received a single oral dose of 2 g. This dosage of spectinomycin did not prevent the development of syphilitic orchitis or reactivity to the FTA-ABS test, but it prolonged the subclinical incubation period.

Animals↗
PubMed1977

Spectinomycin-resistant Neisseria gonorrhoeae.

Neisseria gonorrhoeae resistant to high levels of spectinomycin (more than 2,048 microng/ml), were isolated from specimens obtained from a patient with urethritis. The bacterial resistance to spectinomycin is probably due to ribosomal changes that are a result of a chromosomal mutation. If spectinomycin fails to cure gonorrhea, spectinomycin resistance should be considered.

Adult↗
PubMedDate not supplied

Treatment of chancroid with spectinomycin or co-trimoxazole.

Chancroid, the third most prevalent venereal disease in Thailand, was treated with a single 2-gm dose of spectinomycin, or two tablets of co-trimoxazole (trimethoprim-sulfamethoxazole) twice daily for seven days. The differences in cure rates between the two groups were statistically significant. The chancroidal ulcers were cured in 93.7% of 175 patients treated with spectinomycin, and in 48.2% of 168 co-trimoxazole-treated patients (P less than 0.01). The in vitro susceptibility of Haemophilus ducreyi to spectinomycin was 4 to 16 micrograms/ml and to co-trimoxazole 32 micrograms/ml or higher. Thus we found that a single-dose regimen of spectinomycin was significantly more effective than the standard seven-day regimen of co-trimoxazole for the treatment of chancroid.

Adolescent↗
PubMed1984

Comparative study of ceftriaxone and spectinomycin in the treatment of uncomplicated gonorrhea in women.

Single-dose ceftriaxone, 125 mg given intramuscularly, was compared with spectinomycin 2.0 g given intramuscularly in the treatment of women with uncomplicated gonorrhea. Cervical or anorectal gonococcal infection was eradicated in 54 (98 percent) of 55 women treated with ceftriaxone and 22 (96 percent) of 23 treated with spectinomycin. Cure rates for pharyngeal gonococcal infections were nine of 10 for ceftriaxone and four of eight for spectinomycin (p = 0.18). Neither agent eradicated concurrent Chlamydia trachomatis infection. The geometric mean minimal inhibitory concentration for ceftriaxone was 0.0038 microgram/ml for 65 pretreatment cervical isolates of beta-lactamase-negative Neisseria gonorrhoeae and all isolates were inhibited by 0.063 microgram/ml. Neither drug caused perceptible toxicity, but patient acceptance was better for ceftriaxone than for spectinomycin. A single 125 mg dose of ceftriaxone is an excellent regimen in the treatment of uncomplicated gonorrhea in women.

Adolescent↗
PubMed1983

[Biological characteristics of spectinomycin-resistant strains of the tularemia pathogen].

Sensitivity of 2 subspecies of the tularemia causative agent to spectinomycin, an aminoglycoside antibiotic, was studied in vitro. The MIC of the antibiotic with respect to strains 503/847 and Schu was 40 micrograms/ml and with respect to strain A-Cole 20 micrograms/ml. The frequency of spontaneous spectinomycin resistant mutants was low. The mutants grown on a medium containing spectinomycin in a concentration of 100 micrograms/ml were highly resistant to the antibiotic (at least 10000 micrograms/ml). By the main biological properties and virulence the spectinomycin resistant mutants did not differ from the initial strains.

Animals↗
PubMed1984

Treatment of gonorrhoea in males in the Central African Republic with spectinomycin and procaine penicillin.

Gonorrhoea has become a problem in most parts of the world, and valid recommendations for treatment are important for control of the disease. In this study in Bangui, Central African Republic, 460 male patients with gonorrhoea were randomly assigned to treatment with either 4.0 x 10(6) units of procaine penicillin plus 1 g of probenecid, or 2 g of spectinomycin. Of these patients, 91% returned for follow-up; the failure rate was 4.8% with the penicillin schedule and 6.2% with spectinomycin (difference not statistically significant). Concomitant Chlamydia trachomatis infection was found in 5% of patients, and almost all of this group developed postgonococcal urethritis.Of the 460 patients, 7 (1.5%) were infected with penicillinase-producing Neisseria gonorrhoeae (PPNG) strains. Penicillin treatment failed in these cases, while spectinomycin was highly efficacious. The failure rate for penicillin was considerably higher in infections with strains that were less sensitive to penicillin in vitro. The failure rate for spectinomycin treatment was higher in patients who were infected with a strain that was highly sensitive to penicillin.It is concluded that, once PPNG strains have been found in a country, treatment of gonorrhoea should be based on an antibiotic that cures PPNG infections. Tetracycline can be used as second-line treatment, since it will also cure C. trachomatis infection, which is much less frequently associated with gonorrhoea in Africa than in industrial countries.

Administration, Oral↗
PubMed1984

[Treatment of gonorrhea with spectinomycin and penicillin].

In an open clinical trial, spectinomycin and penicillin G were compared with regard to clinical efficacy, side effects, as well as bacteriological sensitivity in patients suffering from acute gonorrhea. The study was concerned with 176 female patients of a harbor medical practice who were frequently changing partners. 87 out of these patients were treated with spectinomycin, 89 of them with penicillin G. Smear specimens of all patients were tested microscopically; in addition, we performed bacteriological tests (as agar diffusion test, tube dilution test, beta-lactamase test). Both spectinomycin and penicillin showed a good clinical efficacy, except for one case of resistance against penicillin. Afterwards, this patient was successfully treated with spectinomycin. Apart from intermittent pain in the injection area, no side effects have been reported in either group of patients.

Administration, Oral↗
PubMed1982

Spectinomycin.

Spectinomycin is a broad-spectrum aminocyclitol antibiotic that is highly effective in the treatment of uncomplicated gonorrhea. It is the drug of choice for the treatment of gonorrhea that fails to respond to other therapy and is a good alternative drug in the treatment of penicillin-allergic patients. Spectinomycin should be considered the drug of choice in the treatment of gonorrhea in areas where penicillinase-producing strains of Neisseria gonorrhoeae are prevalent. Spectinomycin is not predictably effective in the treatment of oral pharyngeal gonorrhea but may be used in penicillin-allergic patients with disseminated gonorrhea. While spectinomycin has some activity against other human pathogens, it is unlikely that this agent will be found useful in infections other than those due to Neisseria gonorrhoeae.

Bacteria↗
PubMed1987

The molecular basis for rRNA-dependent spectinomycin resistance in Nicotiana chloroplasts.

The chloroplast genes coding for the 16S ribosomal RNA from several spectinomycin-resistant Nicotiana mutants were analyzed. Two classes of mutants were identified. In one class, a G to A base transition is found at position 1140 of the tobacco-chloroplast 16S rRNA gene, which eliminates an AatII restriction endonuclease site. This base transition is proximal to a mutation previously described for spectinomycin resistance in Escherichia coli. In the other class, a novel G to A transition is found at position 1012 of the 16S rRNA gene. Although the mutations in the two classes are 128 nucleotides apart, the secondary structure model for 16S rRNA suggests that the two mutated nucleotides are in spatial proximity on opposite sides of a conserved stem structure in the 3' region of the molecule. Phylogenetic evidence is presented linking this conserved stem with spectinomycin resistance in chloroplasts. Perturbation of the stem is proposed to be the molecular-genetic basis for rRNA-dependent spectinomycin resistance.

Journal Article↗
PubMed1998

Spectinomycin kinase from Legionella pneumophila. Characterization of substrate specificity and identification of catalytically important residues.

The bacterium Legionella pneumophila is the responsible agent for Legionnaires' disease and has recently been shown to harbor a gene encoding a kinase that confers resistance to the aminoglycoside antibiotic spectinomycin (Suter, T. M., Viswanathan, V. K., and Cianciotto, N. P. (1997) Antimicrob. Agents Chemother. 41, 1385-1388). We report the overproduction, purification, and characterization of this spectinomycin kinase from an expressing system in Escherichia coli. The purified protein shows stringent substrate specificity for spectinomycin with Km = 21.5 microM and kcat = 24.2 s-1 and does not bind other aminoglycosides including kanamycin, amikacin, neomycin, butirosin, streptomycin, or apramycin. Purification of spectinomycin phosphate followed by characterization by mass spectrometry and 1H, 13C, and 31P NMR established the site of phosphorylation to be at the hydroxyl group at position 9. Thus this enzyme is designated APH(9)-Ia (where APH is aminoglycoside kinase). The enzyme was inactivated by the electrophilic ATP analogue 5'-[p-(fluorosulfonyl)benzoyl]adenosine, consistent with a nucleophilic residue such as Lys lining the nucleotide binding pocket. Site-directed mutagenesis of Lys-52 and Asp-212 to Ala confirmed that these residues were important for catalysis, with Lys-52 playing a potential role in ATP binding and Asp-212 in phosphoryl transfer. Thio and solvent isotope effect experiments in the presence of either Mg2+ or Mn2+ were consistent with a kinetic mechanism in which phosphate transfer does not contribute significantly to the rate-limiting step. These results establish that APH(9)-Ia is a highly specific antibiotic resistance kinase and provides the requisite mechanistic information for future structural studies.

Adenosine↗