Fusidic
sodium fusidate
CAS: 751-94-0
Molecular Formula: C31H49NaO6
Fusidic - Names and Identifiers
Fusidic - Physico-chemical Properties
| Molecular Formula | C31H49NaO6 |
| Molar Mass | 540.72 |
| Melting Point | >200°C (dec.) |
| Boling Point | 635.6°C at 760 mmHg |
| Flash Point | 197.6°C |
| Water Solubility | Soluble in water |
| Solubility | H2O: soluble |
| Vapor Presure | 7.93E-19mmHg at 25°C |
| Appearance | neat |
| Color | White to Off-White |
| Merck | 13,4339 |
| Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
| Sensitive | Moisture & Light Sensitive |
| Use | This product is for scientific research only and shall not be used for other purposes. |
| In vivo study | Fusidin(Fusidate Sodium) can improve experimental autoimmune myocarditis by inhibiting the secretion of TNF-a. It attenuates the clinical and histological features of immune-inflammatory diabetes in mice treated with streptozotocin(SZ). This effect was found to be dose-dependent in three different strains of mice. Therefore, fusidin may have antidiabetic effects. |
Fusidic - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
| RTECS | LV5775000 |
| HS Code | 29419000 |
| Toxicity | LD50 in mice (g/kg): 0.2 i.v. (Godtfredsen, Nature 1962) |
Fusidic - Reference Information
| narrow-spectrum antibiotics | sodium fusidate is also known as sodium Brown mold, sodium fusospores, it is a narrow-spectrum antibiotic with a steroidal skeleton, which is a derivative of fusidic acid, white crystal or crystalline powder, odorless, bitter, slightly hygroscopic, soluble in water and ethanol, slightly soluble in chloroform, insoluble in copper, ether, benzene. It is successfully developed for the first time by Leo pharmaceutical company of Denmark, and its trade name is ristin. This product has strong tissue penetration, mainly metabolized in the liver, and excreted by bile, almost not excreted by the kidney, with low toxicity, by inhibiting bacterial protein synthesis to produce bactericidal effect, it has good antibacterial effect on Gram-positive bacteria and good drug resistance. At the same time, strains resistant to penicillin, methicillin and other antibiotics are still sensitive to this product, there was no cross-resistance between sodium fusidate and other antibiotics used clinically. This product is a non-cephalosporin antibiotic, so it does not need to do skin allergy test. At present, it has been widely used in clinical treatment of various infections caused by various sensitive bacteria, especially Staphylococcus, such as osteomyelitis, septicemia and endocarditis, recurrent infections of cystic fibrosis, bacterial endocarditis, Pneumonia, meningitis, diphtheria, tuberculosis, skin and soft tissue infections, Surgical and traumatic infection, etc. Intravenous administration is indicated for severe infections or infections with drug-resistant strains, as well as for MRSA infections. But because of its easy to produce drug resistance, more as an adjuvant drug. Oral treatment of Clostridium difficile-induced pseudomembranous colitis has good effect. |
| pharmacokinetics | sodium fusidate acts primarily on the ribosome of bacteria, inhibiting the displacement of mRNA, blocking protein synthesis and killing bacteria. Oral absorption is good, 2H after oral administration of 0.5g single dose, Cmax is about 14~38mg/L,0.5g,3 times/d, the fourth day blood drug concentration can reach 21~71mg/L. No drug accumulation, eating may affect absorption. Intravenous infusion of 0.5g,2H after the blood concentration of 40mg/L. High fat soluble, good tissue migration, can penetrate into the aqueous humor, prostate, Bursa fluid to effective concentration; Can also successfully penetrate the placenta, but it is difficult to penetrate the blood-cerebrospinal fluid barrier. Sodium fusidate has excellent tissue permeability and is widely distributed in the body. It is particularly important clinically that the product not only has a high concentration in tissues with abundant blood supply, but also has a high concentration even in tissues with less vascular distribution. Known in pus, sputum, soft tissue, heart, bone tissue, synovial fluid, dead bone pieces, burn scabs, brain abscesses, and intraocular, the concentration of sodium fusidate exceeded its minimum inhibitory concentration against Staphylococcus (0.03~0.16 μg/ml). Sodium fusidate is metabolized in the liver and excreted mainly by bile and almost not by the kidneys. The toxicity is extremely low, and there is no cross allergy between other antibacterial drugs used in clinic, so it can be used to treat patients who are contraindicated to other antibiotics, such as those allergic to penicillin or other antibiotics. Sodium fusidate is recommended in combination with other anti-staphylococcal agents to reduce the development of drug resistance when long-term use is required due to severe or deep infection, cephalosporins, erythromycin, aminoglycosides, lincomycin, rifampicin or vancomycin are used in combination and may achieve additive or synergistic effects. |
| adverse reactions and precautions | adverse reactions are few and mild, oral administration may have mild gastrointestinal reactions. Intravenous injection of this product may cause thrombophlebitis and venous spasm. There is a report of the increase of reversible transaminase when 1.5~3 grams per day. Individual patients have been reported to have retrograde jaundice after drug administration, which is mainly seen in high-dose intravenous administration, especially in patients with severe Staphylococcus aureus bacteremia. If jaundice continues, the drug should be stopped, serum bilirubin will return to normal. Reports of allergic reactions are very rare. due to the metabolic and excretory properties of sodium fusidate, when administered at high doses over a long period of time or in combination with other drugs with similar elimination routes (eg, lincomycin or rifampicin), patients with liver dysfunction and biliary tract abnormalities should be regularly checked for liver function. In vitro, sodium fusidate can replace bilirubin at the albumin binding site, and the clinical significance of this substitution is not clear. Neonatal use of this product is not found after the nuclear jaundice, but premature infants, jaundice, acidosis and severe illness of the newborn when using this product should pay attention to this factor. |
| biological activity | Fusidate Sodium (Fucidin, SQ-16360) is the Sodium salt form of fusidic acid, fusidic acid is a bacteriostatic antibiotic from fusporium that is used as a topical drug to treat skin infections. |
| uses | sodium fusidate produces bactericidal effects by inhibiting protein synthesis in bacteria, has a strong antibacterial effect against a range of gram-positive bacteria. Staphylococcus, including penicillin, methicillin and other antibiotic resistant strains, are highly sensitive to this product. There is no cross-resistance between sodium fusidate and other antibacterial drugs used in clinic effect: it is an antibiotic with steroid skeleton, which mainly has antibacterial effect on Gram-positive bacteria, Neisseria and Mycobacterium tuberculosis. It is used for peripheral infection caused by sensitive bacteria, especially for strains resistant to other antibiotics. Commonly used in skin and bone tissue and joints and other parts of infection and endocarditis and other packaging: 25kg carton |
Last Update：2024-04-10 22:29:15
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