Bacterial

Absorption, Distribution and Excretion
Sodium fusidic acid tablets have a 91% oral bioavailability. Absorption of the film-coated tablets is complete when compared to a solution, however oral absorption is variable. Oral fusidic acid hemihydrate (suspension) achieved a 22.5% bioavailability in pediatric patients following a 20 milligram/kilogram dose.

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Metabolism / Metabolites
Metabolites include dicarboxylic ester/acid, 3-keto fusidic acid, hydroxy fusidic acid, glucuronide fusidic acid and a glycol metabolite.

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Biological Half-Life
Approximately 5 to 6 hours in adults.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Fusidic acid is not approved for marketing in the United States by the U.S. Food and Drug Administration, but is available in other countries as topical and systemic dosage forms. Data on excretion of fusidic acid into breastmilk are quite old and not from a well-designed study, but levels in breastmilk after intravenous fusidic acid appear to be low.
With topical products, ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking. Fusidic acid applied topically to the nipples appears to be relatively ineffective as a treatment for sore, cracked nipples.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
A small, randomized, unblinded trial of mothers with sore, cracked nipples was performed. Fusidic acid ointment applied to the nipples after each feeding was much less effective (36% vs 79%) than an oral antibiotic (cloxacillin or erythromycin for 10 days) in resolving the problem. Additionally, 43% of patients had no improvement with fusidic acid compared with 16% with oral antibiotics; 21% worsened with fusidic acid compared with 5% with oral antibiotics.

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Protein Binding
97 to 99%

[1]. A Critical Review of the Properties of Fusidic Acid and Analytical Methods for Its Determination. Crit Rev Anal Chem. 2016;46(4):352-360.

[2].Fusidic acid is an effective treatment against Toxoplasma gondii and Listeria monocytogenes in vitro, but not in mice. Parasitol Res. 2013;112(11):3859-3863.

Fusidic acid is a steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum. It has a role as a protein synthesis inhibitor, an EC 2.7.1.33 (pantothenate kinase) inhibitor and an Escherichia coli metabolite. It is a 3alpha-hydroxy steroid, an 11alpha-hydroxy steroid, a sterol ester, a steroid acid, an alpha,beta-unsaturated monocarboxylic acid and a steroid antibiotic. It is a conjugate acid of a fusidate. It derives from a hydride of a 5alpha-cholestane.
An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed) It acts by inhibiting translocation during protein synthesis. It is often used topically in creams and eyedrops but is available in systemic formulations including tablets and injections.
Fusidic acid has been reported in Stilbella aciculosa, Microsporum canis, and other organisms with data available.
Fusidic Acid is a bacteriostatic antibiotic derived from the fungus Fusidium coccineum and used as a topical medication to treat skin infections. Fusidic acid acts as a bacterial protein synthesis inhibitor by preventing the turnover of elongation factor G (EF-G) from the ribosome. Fusidic acid is effective primarily on gram-positive bacteria.
An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.
See also: Fusidate Sodium (active moiety of).

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Drug Indication
For the treatment of bacterial infections.

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Mechanism of Action
Fusidic acid works by interfering with bacterial protein synthesis, specifically by preventing the translocation of the elongation factor G (EF-G) from the ribosome. It also can inhibit chloramphenicol acetyltransferase enzymes.

C31H48O6

516.7092

516.345

C, 72.06; H, 9.36; O, 18.58

6990-06-3

Fusidic acid sodium salt;751-94-0;Fusidic acid-d6

3000226

Solid powder

1.2±0.1 g/cm3

635.6±55.0 °C at 760 mmHg

190-192ºC

197.7±25.0 °C

0.0±4.2 mmHg at 25°C

1.558

6.41

104.06

3

6

6

37

994

10

O([H])[C@]1([H])C([H])([H])[C@@]2([H])/C(=C(/C(=O)O[H])\C([H])([H])C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])/[C@]([H])(C([H])([H])[C@]2(C([H])([H])[H])[C@@]2(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]3([H])[C@]([H])(C([H])([H])[H])[C@@]([H])(C([H])([H])C([H])([H])[C@]3(C([H])([H])[H])[C@@]21[H])O[H])OC(C([H])([H])[H])=O

IECPWNUMDGFDKC-CDSRIIBBSA-N

InChI=1S/C31H48O6/c1-17(2)9-8-10-20(28(35)36)26-22-15-24(34)27-29(5)13-12-23(33)18(3)21(29)11-14-30(27,6)31(22,7)16-25(26)37-19(4)32/h9,18,21-25,27,33-34H,8,10-16H2,1-7H3,(H,35,36)/b26-20-/t18-,21?,22-,23+,24+,25-,27-,29-,30-,31-/m0/s1

(Z)-2-((3R,4S,8S,9S,10S,11R,13R,14S,16S)-16-acetoxy-3,11-dihydroxy-4,8,10,14-tetramethylhexadecahydro-17H-cyclopenta[a]phenanthren-17-ylidene)-6-methylhept-5-enoic acid

Anhydrous Fusidic Acid; Fucidin; Fucidine; SQ-16603; CEM-102; SQ 16603; CEM 102; SQ16603; CEM102

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 本产品在运输和储存过程中需避光。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~193.53 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (4.84 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (4.84 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 3 中的溶解度: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (4.84 mM)

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。