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The Journal of Antimicrobial... Nov 1998
Review
Topics: Administration, Oral; Anti-Bacterial Agents; Clinical Trials as Topic; Double-Blind Method; Humans; Prospective Studies; Randomized Controlled Trials as Topic; Respiratory Tract Infections; Spiramycin; Tissue Distribution
PubMed: 9848439
DOI: 10.1093/jac/42.5.572 -
Casopis Lekaru Ceskych Jan 1994Spiramycin is a 16-membered ring macrolide (antibiotic). It was discovered in 1952 as a product of Streptomyces ambofaciens. As a preparation for oral administration it... (Review)
Review
Spiramycin is a 16-membered ring macrolide (antibiotic). It was discovered in 1952 as a product of Streptomyces ambofaciens. As a preparation for oral administration it has been used since 1955, in 1987 also the parenteral form was introduced into practice. The antibacterial action involves inhibition of protein synthesis in the bacterial cell during translocation. Resistance to spiramycin can develop by several mechanisms and its prevalence is to a considerable extent proportional to the frequency of prescription in a given area. The antibacterial spectrum comprises Gram-positive cocci and rods, Gram-negative cocci and also Legionellae, mycoplasmas, chlamydiae, some types of spirochetes, Toxoplasma gondii and Cryptosporidium sp., Enterobacteria, pseudomonads and pathogenic moulds are resistant. Its action is mainly bacteriostatic, on highly sensitive strains it exerts a bactericide action. As compared with erythromycin, it is in vitro weight for weight 5 to 20 less effective, an equipotential therapeutic dose is, however, only double. This difference between the effectiveness in vitro and in vivo is explained above all by the great affinity of spiramycin to tissues where it achieves concentrations many times higher than serum levels. An important part is played also by the slow release of the antibiotic from the tissue compartment, the marked action on microbes in sub-inhibition concentrations and the relatively long persisting post-antibiotic effect. Its great advantage is the exceptionally favourable tolerance-gastrointestinal and general. It is available for parenteral and oral administration.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Humans; Spiramycin
PubMed: 8131182
DOI: No ID Found -
Canadian Medical Association Journal May 1958
Topics: Anti-Bacterial Agents; Antibiotics, Antitubercular; Dermatologic Agents; Humans; Spiramycin
PubMed: 13523517
DOI: No ID Found -
British Medical Journal Mar 1956
Topics: Anti-Bacterial Agents; Antibiotics, Antitubercular; Dermatologic Agents; Pneumonia; Spiramycin
PubMed: 13293407
DOI: No ID Found -
Molecules (Basel, Switzerland) May 2022Drug repurposing is a simple concept with a long history, and is a paradigm shift that can significantly reduce the costs and accelerate the process of bringing a new...
Drug repurposing is a simple concept with a long history, and is a paradigm shift that can significantly reduce the costs and accelerate the process of bringing a new small-molecule drug into clinical practice. We attempted to uncover a new application of spiramycin, an old medication that was classically prescribed for toxoplasmosis and various other soft-tissue infections; specifically, we initiated a study on the anti-inflammatory capacity of spiramycin. For this purpose, we used murine macrophage RAW 264.7 as a model for this experiment and investigated the anti-inflammatory effects of spiramycin by inhibiting the production of pro-inflammatory mediators and cytokines. In the present study, we demonstrated that spiramycin significantly decreased nitric oxide (NO), interleukin (IL)-1β, and IL-6 levels in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Spiramycin also inhibited the expression of NO synthase (iNOS), potentially explaining the spiramycin-induced decrease in NO production. In addition, spiramycin inhibited the phosphorylation of mitogen-activated protein kinases (MAPKs); extracellular signal-regulated kinase (ERK) and c-Jun N terminal kinase (JNK) as well as the inactivation and subsequent nuclear translocation of nuclear factor κB (NF-κB). This indicated that spiramycin attenuates macrophages' secretion of IL-6, IL-1β, and NO, inducing iNOS expression via the inhibition of the NF-κB and MAPK signaling pathways. Finally, we tested the potential application of spiramycin as a topical material by human skin primary irritation tests. It was performed on the normal skin (upper back) of 31 volunteers to determine whether 100 μM and μM of spiramycin had irritation or sensitization potential. In these assays, spiramycin did not induce any adverse reactions. In conclusion, our results demonstrate that spiramycin can effectively attenuate the activation of macrophages, suggesting that spiramycin could be a potential candidate for drug repositioning as a topical anti-inflammatory agent.
Topics: Animals; Anti-Inflammatory Agents; Extracellular Signal-Regulated MAP Kinases; Humans; Inflammation; Interleukin-6; Lipopolysaccharides; Macrophages; Mice; NF-kappa B; Nitric Oxide; RAW 264.7 Cells; Spiramycin
PubMed: 35630676
DOI: 10.3390/molecules27103202 -
Clinical Pharmacokinetics Apr 1998The absolute bioavailability of oral spiramycin is generally within the range of 30 to 40%. After a 1 g oral dose, the maximum serum drug concentration was found to be... (Review)
Review
The absolute bioavailability of oral spiramycin is generally within the range of 30 to 40%. After a 1 g oral dose, the maximum serum drug concentration was found to be within the range 0.4 to 1.4 mg/L. The tissue distribution of spiramycin is extensive. The volume of distribution is in excess of 300 L, and concentrations achieved in bone, muscle, respiratory tract and saliva exceed those found in serum. The intracellular penetration of spiramycin is also rapid and extensive, with the concentrations in alveolar macrophages 10 to 20 times greater than simultaneous serum concentrations. Spiramycin is less metabolised than some of the other macrolides. The renal excretion of spiramycin is low, with 4 to 20% of the dose being excreted by this route. High concentrations of spiramycin are achieved in bile, which is an important route of elimination. The serum elimination half-life of spiramycin is between 6.2 and 7.7 hours. Of significance to clinicians may be the finding that spiramycin is highly concentrated in the respiratory tract and other tissues and macrophages. The post-antibiotic effect of spiramycin is significant and this effect is more prolonged than that of erythromycin against Staphylococcus aureus. Spiramycin has also been shown to greatly reduce the capacity of strains of Gram-positive cocci to adhere to human buccal cells.
Topics: Animals; Anti-Bacterial Agents; Bacterial Adhesion; Dose-Response Relationship, Drug; Humans; Spiramycin; Tissue Distribution
PubMed: 9571302
DOI: 10.2165/00003088-199834040-00003 -
European Journal of Medical Research Dec 2021We aimed to investigate the effect of antepartum treatment with spiramycin with or without subsequent pyrimethamine-sulfonamide-folinic acid, compared to no treatment,... (Meta-Analysis)
Meta-Analysis Review
PURPOSE
We aimed to investigate the effect of antepartum treatment with spiramycin with or without subsequent pyrimethamine-sulfonamide-folinic acid, compared to no treatment, on the rate of mother-to-child transmission (MTCT) of Toxoplasma gondii (T. gondii) and incidence/severity of sequelae in the offspring.
METHODS
Embase and PubMed were searched for literature on spiramycin in pregnant women suspected/diagnosed with T. gondii infection. Meta-analyses were performed using random-effects model.
RESULTS
Thirty-three studies (32 cohorts and 1 cross-sectional study), with a total of 15,406 mothers and 15,250 offspring, were pooled for analyses. The MTCT rate for all treated patients was significantly lower than the untreated [19.5% (95% CI 14-25.5%) versus 50.7% (95% CI 31.2-70%), p < 0.001]. The transmission rate in patients on spiramycin monotherapy was also significantly lower than untreated [17.6% (95% CI 9.9-26.8%) versus 50.7% (95% CI 31.2-70%), p < 0.001].
CONCLUSION
Results indicate significant reduction in MTCT rates following spiramycin treatment of suspected/diagnosed maternal T. gondii infection.
Topics: Anti-Bacterial Agents; Female; Humans; Neglected Diseases; Observational Studies as Topic; Pregnancy; Pregnancy Complications, Infectious; Spiramycin
PubMed: 34895348
DOI: 10.1186/s40001-021-00606-7 -
European Review For Medical and... Mar 2023Through a cell culture test, we analyzed the cytotoxic effects of topical spiramycin on NIH/3T3 fibroblast cells.
OBJECTIVE
Through a cell culture test, we analyzed the cytotoxic effects of topical spiramycin on NIH/3T3 fibroblast cells.
MATERIALS AND METHODS
Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% fetal bovine serum and 1% penicillin/streptomycin was used for the growth of NIH/3T3 fibroblast cells in a 5% CO2 incubator. Spiramycin's cytotoxicity was measured using the MTT assay. 5,000 NIH/3T3 cells per well of a 96-well plate were seeded in each well, and the cells were treated with spiramycin (3.13-100 μM) for 24, 48 and 72 hours while the plates were incubated at 37°C in a humidified 5% CO2 atmosphere. First, 105 NIH/3T3 cells were seeded onto coverslips in 6-well plates for morphological analysis of both untreated and spiramycin-treated cells. For 24 hours, NIH/3T3 cells were exposed to a 100 μM dosage of spiramycin. The cells in the control group were grown in complete growth media alone.
RESULTS
Spiramycin was non-toxic to NIH/3T3 fibroblast cells in a MTT test. The concentration of spiramycin used to stimulate cell growth increased as the concentration was increased. After 24 and 48 hours of treatment with 100 μM NIH/3T3, the cells showed the most significant increase in size. Cell viability was shown to be significantly reduced at spiramycin doses of 50 and 100 μM. All MTT findings revealed that spiramycin enhanced cell viability and was not harmful to the fibroblast cells for short-term application of 24 and 48 hours but lowered the viability of fibroblast cells at the doses of 50 and 100 μM for long-term application duration of 72 hours. Confocal micrographs showed that spiramycin treatment did not affect the cytoskeleton or nucleus of fibroblast cells, in contrast to the control NIH/3T3 cells. Both untreated and treated with spiramycin, fibroblast cells were found to be fusiform and compact, with their nuclei remaining unaltered and unreduced in size.
CONCLUSIONS
It was concluded that spiramycin has a beneficial effect on fibroblast cells and is safe for use over short periods. Spiramycin reduced fibroblast cell viability when applied for 72 hours. Confocal micrographs showed that fibroblast cell skeletons and nuclei were unharmed and undamaged, that cell shapes were fusiform and compact, and that nuclei were neither broken nor shrunken. Topical spiramycin could be recommended for septorhinoplasty procedures due to anti-inflammatory effects for short-term usage if clinical trials will confirm experimental data.
Topics: Animals; Mice; Spiramycin; Carbon Dioxide; Fibroblasts; NIH 3T3 Cells; Cell Culture Techniques
PubMed: 36971220
DOI: 10.26355/eurrev_202303_31701 -
Journal of Hepatology Nov 1992
Topics: Chemical and Drug Induced Liver Injury; Cholestasis, Intrahepatic; Female; Humans; Middle Aged; Spiramycin
PubMed: 1487619
DOI: 10.1016/s0168-8278(05)80677-4 -
The Annals of Pharmacotherapy Dec 2002
Topics: Anti-Bacterial Agents; Chemical and Drug Induced Liver Injury; Female; Humans; Liver Diseases; Middle Aged; Spiramycin
PubMed: 12452764
DOI: 10.1345/aph.1C158