Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The increasing number of beta-lactam antibiotic-resistant infections has led to the development of an alternative treatment: the combination of a beta-lactam antibiotic with an irreversible, suicide-type, beta-lactamase inhibitor. Such a combination, sulbactam/ampicillin, was used in clinical trials at 4 European and 1 American centres to treat severely ill patients with lower respiratory tract infections including bronchiectasis, pneumonia and purulent tracheobronchitis. The sulbactam/ampicillin combination was assessed for safety, efficacy and tolerance in a total of 91 patients. Investigators from all 5 centres reported satisfactory bacteriological and clinical results. The combination agent either cured or improved the condition of virtually all patients who were evaluated. The few side effects reported mainly involved pain at the injection site. A review of these studies indicates that therapy with sulbactam/ampicillin effectively treats lower respiratory tract infections in severely ill patients without causing serious adverse reactions.
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PMID:Sulbactam/ampicillin in the treatment of lower respiratory infections. 306 54

Conditions have been established where the deactivation of the beta-lactamase from Staphylococcus aureus PC1 by the penicillin substrate, quinacillin, is close to complete but fully reversible. The temperature-dependence of the rate of re-activation indicated a half-life of about 170 min for the deactivated state at 0 degrees C. Measurement of the relative viscosity of mixtures of enzyme and quinacillin at 8.4 degrees C ruled out any significant difference in shape or solvation between the deactivated and the normal enzyme. C.d. measurements of the deactivated protein, separated from excess quinacillin, showed that the quinacillin side-chain chromophore was bound in an asymmetric environment. The ellipticity associated with the bound quinacillin chromophore decreased with the same first-order rate constant as that for reappearance of enzyme activity. These findings support the accumulation of a deactivated state that contains bound quinacillin or a derivative. Quinacillin caused a 3-fold increase in the rate of 3H exchange-out (at a rate that was low compared with that for the substantially unfolded or expanded protein). However, there was rapid exchange-out of about 50 3H atoms on addition of 1 M-urea to the deactivated enzyme, whereas the same concentration had no effect on the exchange-out of 3H from native enzyme. The interpretation that quinacillin increases the susceptibility of the native state to unfolding in the presence of urea is supported by the demonstration that SO4(2)- ions decreased the rate and extent of deactivation but had no effect on the rate of re-activation, as predicted from the observation that SO4(2)- ions, in competition with urea, stabilize the native state relative to the partially unfolded state H [Mitchinson & Pain (1985) J. Mol. Biol. 184, 331-342].
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PMID:Reversible deactivation of beta-lactamase by quinacillin. Extent of the conformational change in the isolated transitory complex. 349 97

Acute otitis media and chronic otitis media with effusion are generally caused in children by the bacteria found in the nasopharynx. In growing numbers of young patients, beta-lactamase-producing strains of Branhamella catarrhalis and Staphylococcus aureus have recently emerged as causative organisms. The antimicrobial agent selected for treatment should be effective against whatever pathogens have been associated with failures of symptomatic treatment in the community. Acute or chronic sinusitis in children is overlooked and poorly understood because so many children have frequent episodes of upper respiratory infection. To relieve acute symptoms and prevent suppurative complications, antimicrobial treatment is indicated. Children with persistent pain or fever may require surgical intervention and/or treatment with another antimicrobial agent. Recurrent acute sinusitis needs further evaluation and may be associated with a tooth abscess or cystic fibrosis.
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PMID:Update on antimicrobial therapy for otitis media and sinusitis in children. 391 21

Clinical effects of spectinomycin (Trobicin, 2 g. i.m., once a day) and ampicillin (1 g/day, p.o., in 4 divided doses, for 2 days) given in combination on acute gonorrhea in female patients were studied, and sensitivity of isolated gonococci to each of these antibiotics was determined. 1. Clinical effects were evaluated by cultures of gonococci from discharge collected at 72 hours after spectinomycin administration and 12 hours after the last dose of ampicillin and both subjective and objective clinical findings. Among 20 cases of gonorrhea treated, 12 cases (60.0%) proved excellent in therapeutic results, 6 cases (30.0%) good, 1 case fair and 1 case produced no response. The success rate comprising excellent and good was 90.0%. The only side effect reported was pain of injection site in 1 case on 3 days after initiation of treatment, but no induration was noted. 2. MICs of spectinomycin and ampicillin for gonococci collected from the 20 cases were determined. Spectinomycin showed MICs of 6.25 approximately 12.5 micrograms/ml against 10(8) CFU/ml and 3.13 approximately 12.5 micrograms/ml against 10(8) CFU/ml. These values were below the blood concentration obtained at 6 hours after intramuscular administration of 2 g of spectinomycin. Ampicillin had MICs of 0.1 approximately 25 micrograms/ml against 10(8) CFU/ml and 0.1 approximately 3.13 micrograms/ml against 10(6) CFU/ml. Five strains, MICs of which were 6.25 approximately 25 micrograms/ml against 10(8) CFU/ml, were beta-lactamase-producing.
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PMID:[Spectinomycin therapy in combination with ampicillin in female patients with acute gonorrhea]. 621 6

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.
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PMID:[Treatment of gonorrhea with spectinomycin and penicillin]. 623 85

Patients with uncomplicated gonorrhea due to beta-lactamase-negative Neisseria gonorrhoeae were treated with cefotaxime (1.0 g given im in a single dose) or with aqueous procaine penicillin G (APPG; 4.8 x 10(6) units given im) plus probenecid (1.0 g given orally). Genital or rectal gonococcal infection was cured in 51 (93%) of 55 patients given cefotaxime and in 23 (96%) of 24 patients given APPG plus probenecid. Gonococcal isolates from homosexual men were less susceptible to cefotaxime (geometric mean MIC, 0.021 microgram/ml) than were strains isolated from heterosexual men (geometric mean MIC, 0.012 microgram/ml; P less than 0.05). Genital infection with Chlamydia trachomatis persisted in four of eight patients given cefotaxime and was first detected after treatment in three others. Of 23 men with gonococcal urethritis who were treated with cefotaxime and followed for 11--30 days, ten (43%) developed postgonococcal urethritis; five of these were associated with chlamydial infection. Administration of cefotaxime or APPG caused equal pain, but cefotaxime was better tolerated because of the need for only one injection. Cefotaxime and APPG plus probenecid are comparable for treatment of uncomplicated genital and rectal infection with beta-lactamase-negative N. gonorrhoeae.
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PMID:Treatment of uncomplicated gonorrhea with cefotaxime. 627 Aug 34

Young men with uncomplicated gonococcal urethritis were treated with 1 gram of cefonicid given intramuscularly plus 1 gram of probenecid by mouth. Of 53 evaluable patients, 33 (62%) had penicillinase-producing Neisseria gonorrhoeae. All but one of these patients were cured. All men who had penicillin-sensitive infections were cured. Cefonicid was highly effective in the treatment of both penicillin-sensitive and penicillin-resistant N gonorrhoeae. Other than moderate pain at the site of injection, there were no adverse side effects. Cefonicid can be added to the group of newer cephalosporins that are effective in the treatment of gonococcal urethritis caused by either penicillin-sensitive or penicillin-resistant strains.
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PMID:Cefonicid as therapy for uncomplicated gonococcal urethritis caused by penicillinase-producing Neisseria gonorrhoeae. 642 48

Bacterial infections of the upper respiratory airways are common. Some of these infections are caused by anaerobic bacteria and Staphylococcus aureus and may constitute considerable therapeutical problems. Chronic suppurative otitis media may sometimes give rise to serious osteitis of surrounding bone structures, sigmoid sinus thrombosis and intracranial abscesses. The causative microorganisms are mostly anaerobes. Many paranasal sinus infections are also due to anaerobic bacteria. These infections can rapidly cause irreversible damage of the sinus mucosa and eventually spread intracranially. Purulent parotitis is mostly seen in elderly and seriously ill patients. In the majority of the cases bacterial cultures reveal beta-lactamase-producing S. aureus. Infections of the teeth in the mandible sometimes spread into the floor of the mouth and may extend down into the throat and mediastinum. If not properly treated these anaerobic infections will prove fatal. Chronic osteomyelitis of the mandible is increasing in frequency and constitute serious therapeutical problems. Many patients cannot be protected against painful and disabling relapses. Anaerobic bacteria, emanating from the normal oropharyngeal flora, play an important part in the pathogenesis of this disorder. Retropharyngeal, parapharyngeal as well as peritonsillar infections and abscesses are mostly caused by anaerobes and demand adequate surgical and antibacterial therapy. In malignant tumors of the ear, nose or throat, anaerobic infections often deteriorate the conditions as inflammatory oedema increases the volume of the tumor and the pain of the patients. Cutaneous infections of the face and auricles caused by S. aureus may constitute therapeutical problems.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Clindamycin in the upper respiratory tract infections. 659 20

Cefpiramide (CPM) was given to 4 patients with respiratory tract infection (H. influenzae 3 cases, P. aeruginosa 1 case), 1 patient with enteritis (enteropathogenic E. coli) and 1 patient with sepsis (E. cloacae). Bacteriological eradication was observed in 5 cases (83.3%), and clinical effectiveness was 66.7%. Serum concentration of CPM at a dose of 15 mg/kg after intravenous drip-infusion for 30 minutes was 105 micrograms/ml at the end of infusion and 67 micrograms/ml at 1 hour. Bacteriological eradication by the administration of CPM was rapidly occurred in 3 strains of H. influenzae including 1 strain of beta-lactamase producing ABPC-resistant one, and 1 strain of P. aeruginosa in the sputum. One patient aged 2 years and 5 months with pneumonia was cured by the treatment of CPM as an outpatient. No side effects were observed except 1 case of vascular pain. It was concluded that CPM is a useful drug for the treatment of bacterial infections in children.
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PMID:[Clinical evaluation of cefpiramide in 6 cases of infection in children]. 665 37

Ro 13-9904, a new broad-spectrum, beta-lactamase-resistant, cephalosporin, was given as a single i.m. injection at doses of 500, 250, and 125 mg in 3 groups of male patients each consisting of 10, 6, and 6 patients respectively, suffering from uncomplicated acute but recurrent gonococcal urethritis. All patients were cured both clinically and bacteriologically without relapsing after a 7-day follow-up. 11 patients suffering from chronic urinary tract infections without flow obstruction but with underlying chronic pyelonephritis in 6, were treated for 7 days with 500 mg of Ro 13-9904 i.m., every 12 h. E. coli and P. mirabilis were the main isolated pathogens. Treatment was successful in all with only one bacteriological relapse during the follow-up period. The drug's tolerance was satisfactory except for moderate local pain in most of the patients.
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PMID:Antibacterial activity of Ro 13-9904 and preliminary experience in gonorrhoea and chronic urinary tract infections. 701 52


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