Spiramycin is white or slightly yellow powder, slightly odorous; slightly hygroscopic. Spiramycine is soluble in methanol, ethanol, acetone and ether, almost insoluble in water, and insoluble in petroleum ether. It is a macrolide antibiotic obtained from the culture medium of Streptomyces ambofaciens. Spiramycin is the acetate of acetylspiramycin. After oral administration, the acetyl group is removed to show strong antibacterial effect. Spiramycin is a strong bacteriostatic agent, and it has a bactericidal effect only at very high concentrations.
Spiramycine has a strong antibacterial effect and antibacterial post effect (PAE) in the body, can enhance the phagocytosis of phagocytes, and is widely distributed in the body. Spiramycine has a higher concentration in tissue cells than erythromycin and has less side effects than erythromycin. Spiramycine can be used to treat ear, nose, throat and respiratory infections caused by gram-positive bacteria and certain gram-negative bacteria. It is suitable for the treatment of otitis media, periodontitis, acute sinusitis and other oral cavity and ear nose throat caused by sensitive bacteria. It can also be used to treat toxoplasmosis.
Spiramycin (SPM) is a sixteen-membered macrolide antibiotic. Its acetylated derivative, acetylspiramycin, has the characteristics of high tissue concentration, low toxicity, and long vivo efficacy. It is effective for acute mastitis, lymph node inflammation and periodontitis. Omura used isotope experiments to prove that the lactone ring of SPM is composed of 5 molecules of acetic acid, 1 molecule of propionic acid, 1 molecule of butyric acid and 1 molecule of unknown precursor (two carbon units).
The biosynthesis of the lactone ring starts from a molecule of propionyl-CoA, followed by the molecules of 2-methylmalonyl-CoA. The three-carbon compounds not only act as precursors to the biosynthesis of SPM, but also induce the synthesis of propionyl-CoA carboxylase. The three mycaminoses in the molecule are derived from complete glucose molecules, the N-methyl and C-methyl groups on mycaminos are derived from methionine, and the source of the nitrogen atoms on the N-methyl group has not been fully elucidated.
Rovamycine is a macrolide antibiotic obtained from the culture medium of Streptomyces ambofaciens. Spiramycin is the acetate of acetylspiramycin. After oral administration, the acetyl group is removed to show strong antibacterial effect. Rovamycine is a strong bacteriostatic agent, and it has a bactericidal effect only at very high concentrations. Its antibacterial action mechanism is the same as that of erythromycin. By combining with the 50S subunit of the bacterial ribonucleoprotein body, it prevents the extension of the peptide chain and affects the synthesis of bacterial protein to achieve antibacterial effect.
The antibacterial spectrum of spiramycin is similar to that of erythromycin, and its antibacterial effect is not as strong as erythromycin, and its oral bioavailability is also lower than erythromycin. However, many erythromycin-resistant Staphylococcus aureus are sensitive to spiramycin. In addition, spiramycin has a better post-antibiotic effect than erythromycin.
The bacteria showed partial cross-resistance to spiramycin and erythromycin. Spiramycine has strong antibacterial activity against Staphylococcus aureus, hemolytic streptococcus, pneumococcus, diphtheria, Bacillus anthracis and Clostridium; in addition, spiramycine has strong antibacterial activity against Listeria and Catabranham Bacteria, Neisseria gonorrhoeae, Campylobacter fetus, Bacillus influenzae, Bacillus pertussis, Bacteroides, Perfringens, Propionibacterium acnes, Peptococcus and Peptostreptococcus, as well as Mycoplasma, Chlamydia, Treponema pallidum, Toxoplasma, Cryptosporidium Etc.
Oral acetylspirillum spiramycin is less affected by gastric acid, about 40% is absorbed. Oral spiramycin 100mg, 200mg, reached the peak blood concentration in 2h, respectively 0.8mg/L, 1mg/L. The drug is widely distributed after absorption. The concentration in urine, pus, bronchial secretions and lung tissue is higher than the blood concentration, and when the blood concentration drops to a minimum, there is still a high drug concentration in the tissue.
The concentration of the drug in the body is high in the lung, liver, and bile (the concentration in the bile can reach 7-10 times the serum concentration). Spiramycin can penetrate into macrophages, as well as through the placental barrier and blood-cerebrospinal fluid barrier. The concentration of cerebrospinal fluid in meningitis is 65% of the blood concentration. After the drug is absorbed, it is first metabolized in the liver to acetylspiramycin. The half-life of spiramycin is longer than that of erythromycin and acetylspiramycin, and it accumulates in the body after repeated administration.
The antibacterial spectrum of spiramycine is the same as other macrolide antibiotics. Due to slow excretion and strong tissue affinity, the antibacterial efficacy in the body is better than similar antibiotics, especially for pneumococcus and streptococcus.
On the other hand, due to slow excretion, livestock and poultry for human consumption require a longer drug withdrawal time before being slaughtered.
Spiramycine is a macrolide antibiotic. Its antibacterial spectrum is similar to erythromycin. It mainly has effects on Gram-positive bacteria and some Gram-negative bacteria, rickettsiae and large viruses, such as streptococcus, meningococcus, Bacillus pertussis, Mycoplasma pneumoniae, Bacillus diphtheria, Chlamydia trachomatis, Leptospira and Clostridium etc. Spiramycine has a strong effect on bacteria resistant to penicillin, streptomycin, tetracycline and chloramphenicol. Clinically it is mainly used for infections caused by various sensitive bacteria, such as upper respiratory tract infection, urinary tract infection, meningitis, mastitis, osteomyelitis, scarlet fever, otitis media, buccal and mouth infections and sinusitis.
Spiramycine has a strong antibacterial effect and antibacterial post effect (PAE) in vivo, which can enhance the phagocytosis of phagocytes. Acetylspiramycin is an antibiotic with antibacterial effect containing a 16-membered macrolide ring, and its effect is positive with no serious adverse reactions, and is often used as the first choice for infections such as aerobic gram-positive bacteria and anaerobic cocci, as well as a substitute for people allergic to beta lactam antibiotics.
Acetylspiramycin is the acetate of spiramycin. After oral administration, the acetyl group is removed to show strong antibacterial effect. Acetylspiramycin is a strong bacteriostatic agent, and only has a bactericidal effect at very high concentrations.
Its antibacterial action mechanism is the same as that of erythromycin. By combining with the 50S subunit of the bacterial ribonucleoprotein body, it prevents the extension of the peptide chain and affects the synthesis of bacterial protein to achieve antibacterial effect. The antibacterial activity of acetylspiramycin is similar to that of spiramycin, but its antibacterial activity is weaker than that of spiramycin. The antibacterial spectrum of acetylspiramycin is similar to that of erythromycin, and its antibacterial effect is not as strong as erythromycin, and its oral bioavailability is also lower than erythromycin. However, many erythromycin-resistant Staphylococcus aureus are sensitive to acetylspiramycin.
In addition, acetylspiramycin has a better post-antibiotic effect than erythromycin. The bacteria showed partial cross-resistance to acetylspiramycin and erythromycin. Acetylspiramycin has strong antibacterial activity against Staphylococcus aureus, Streptococcus hemolyticus, Pneumococcus, Diphtheria, Bacillus anthracis and Clostridium; In addition, Acetylspiramycin has strong antibacterial activity against Listeria and Catab, Lanhamella, Neisseria gonorrhoeae, Campylobacter fetus, Bacillus influenzae, Bacillus pertussis, Bacteroides, Perfringens, Propionibacterium acnes, Peptococcus and Peptostreptococcus, as well as Mycoplasma, Chlamydia, Treponema pallidum and Toxoplasma Spore insects.
Acetylspiramycin tablets can effectively resist Streptococcus pneumoniae, Streptococcus pyogenes, Enterobacter faecalis, etc., but also have some side effects, such as abdominal discomfort or pain, vomiting, nausea, etc., which often occur when high doses are used. However, these symptoms will not have a big impact, as long as you stop taking the drug, these symptoms will disappear. In addition, I remind you that acetylspiramycin is excreted through the hepatobiliary system, so it is not recommended for patients with hepatic insufficiency and renal insufficiency to take the drug.
Suitable for tonsillitis, bronchitis, pneumonia, pharyngitis, otitis media, skin and soft tissue infections caused by sensitive bacteria such as Staphylococcus, Streptococcus pyogenes, Streptococcus pneumoniae, Meningococcus, Neisseria gonorrhoeae, Diphtheria, Mycoplasma, Treponema pneumoniae, etc, Mastitis, cholecystitis, scarlet fever, dental and eye infections, etc.
Clinically, it is mainly used for infections caused by Staphylococcus aureus, Streptococcus, Pneumoniae Bacillus, Escherichia coli, Neisseria gonorrhoeae, such as pneumonia, bronchitis, lung abscess, scarlet fever, osteomyelitis, urethritis, mastitis, stye and lacrimal sac Yan etc.
C. Adverse reactions
The main hazards of acetylspiramycin tablets are gastrointestinal symptoms such as abdominal pain, nausea, vomiting, loss of appetite, and drug eruptions such as local or systemic rashes and itching, but these generally do not require special treatment and can recover on their own after a period of time.
However, if a severe allergic reaction occurs, such as shortness of breath, blood pressure drop, etc., it is urgent to see a doctor immediately. In addition, patients with severe liver and kidney dysfunction should not use the drug, as the drug may aggravate liver and kidney damage.
It is forbidden for patients who are allergic to spiramycine, erythromycin and other macrolides. Spiramycin can penetrate into the placenta, so it is necessary to fully weigh the pros and cons to decide whether to use it for pregnant women.
There is no data to show whether spiramycin is excreted in breast milk, but many macrolide drugs can be excreted in breast milk. So women who are breastfeeding should use this product with caution, and suspend breastfeeding if necessary. And the efficacy and safety of pediatric patients within 6 months have not been determined.
Spiramycine belongs to the macrolide antibiotics. Spiramycine and erythromycin have the same antibacterial mechanism and similar antibacterial spectrum. And spiramycin has lower antibacterial power than erythromycin. However, many bacteria resistant to erythromycin are sensitive to spiramycine, so spiramycine and erythromycin can complement each other.