Micafungin
Micafungin
CAS: 235114-32-6
Molecular Formula: C56H71N9O23S
Micafungin - Names and Identifiers
| Name | Micafungin |
| Synonyms | Micfungin MICAFUNGIN Micafungin UNII-R10H71BSWG Micafungin [INN] Micafungin (Acid) Pneumocandin A0, 1-((4R,5R)-4,5-dihydroxy-N2-(4-(5-(4-(pentyloxy)phenyl)-3-isoxazolyl)benzoyl]-L-ornithine)-4-((4S)-4-hydroxy-4-(4-hydroxy-3-(sulfooxy)phenyl)-L-threonine)- |
| CAS | 235114-32-6 |
| EINECS | 1806241-263-5 |
| InChI | InChI=1/C56H71N9O23S/c1-4-5-6-17-86-32-14-11-28(12-15-32)39-21-33(63-87-39)27-7-9-29(10-8-27)49(75)58-34-20-38(70)52(78)62-54(80)45-46(72)25(2)23-65(45)56(82)43(37(69)22-41(57)71)60-53(79)44(48(74)47(73)30-13-16-36(68)40(18-30)88-89(83,84)85)61-51(77)35-19-31(67)24-64(35)55(81)42(26(3)66)59-50(34)76/h7-16,18,21,25-26,31,34-35,37-38,42-48,52,66-70,72-74,78H,4-6,17,19-20,22-24H2,1-3H3,(H2,57,71)(H,58,75)(H,59,76)(H,60,79)(H,61,77)(H,62,80)(H,83,84,85)/t25-,26-,31+,34-,35-,37+,38+,42-,43-,44-,45-,46-,47-,48-,52+/m0/s1 |
Micafungin - Physico-chemical Properties
| Molecular Formula | C56H71N9O23S |
| Molar Mass | 1270.28 |
| Density | 1.62±0.1 g/cm3(Predicted) |
| Melting Point | >198oC (dec.) |
| Solubility | DMSO (Slightly), Methanol (Very Slightly, Heated) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | -4.46±0.18(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| Stability | Hygroscopic |
| Refractive Index | 1.706 |
Micafungin - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.787 ml | 3.936 ml | 7.872 ml |
| 5 mM | 0.157 ml | 0.787 ml | 1.574 ml |
| 10 mM | 0.079 ml | 0.394 ml | 0.787 ml |
| 5 mM | 0.016 ml | 0.079 ml | 0.157 ml |
Last Update：2024-01-02 23:10:35
Micafungin - Reference Information
| antifungal drugs | from the emergence of nystatin, amphotericin B and griseofulvin in the 1950 s and 1960 s, to 5-flucytosine, triazole and amphotericin B liposomes in the 1980 s, as well as the latest echinococcin antifungal drugs, antifungal drugs have undergone several updates and achieved rapid development. Amphotericin B has always been the gold standard for antifungal drugs, but its clinical application is limited due to obvious nephrotoxicity. Triazoles are currently commonly used antifungal drugs in clinical practice. Fluconazole has a good control effect on Candida, but it is ineffective against Aspergillus. Although the antibacterial spectrum of new triazole drugs has been broadened, they are faced with the problem of cross-resistance of azole drugs, and there are drug interactions with a variety of commonly used clinical drugs, which often makes their clinical application in a dilemma. The new generation of antifungal drugs echinocandins have a unique mechanism of action, mainly by inhibiting the synthesis of essential components 1, 3-β-D-glucan in the fungal cell wall to play an antifungal effect. Since there is no cell wall in human cells, it has no obvious toxic and side effects on human cells and has high safety. Since its clinical application, it has gradually won the recognition of clinicians because of its wide antifungal spectrum, good antifungal efficacy and outstanding drug safety. Micafungin is the second Acanthocin antifungal drug approved by the FDA after caspofungin. The antifungal mechanism is the same as that of caspofungin. The drug is resistant to Candida albicans (including fluconazole-resistant strains), Candida tropicalis, Candida glabrata, and Candida krusei have strong effects, but they have poor effects on Candida parapis. It has antibacterial effect on Aspergillus and has no bactericidal effect. It also has an effect on Pneumocystis. It is ineffective against Cryptococcus, Fusarium, Trichospora, and Conjugate. It is mainly used to treat esophageal candidiasis and prevent candida infection in patients with hematopoietic stem cell transplantation. [Clinical application] It is mainly used for refractory invasive fungal infection or invasive candidal infection and invasive aspergillus infection that cannot tolerate other antifungal drugs, as well as preventive treatment of fungal infection in patients receiving hematopoietic stem cell transplantation. The dose of adult treatment is 50~100 mg/d, and one intravenous drip is given. Severe or refractory aspergillus infection can be increased to 50~300 mg per day. [Precautions] 1. Those who are allergic to this drug or have a history of allergy are prohibited. 2. Use with caution ① Those with liver and kidney insufficiency. ②Blood diseases (such as anemia, reduced bone marrow function, etc.). 3. Effects of drugs on pregnancy Pregnant women should weigh the advantages and disadvantages of medication. 4. The effect of drugs on breastfeeding women should weigh the pros and cons of medication. Fig. 1 is the structural formula |
| clinical pharmacology | this product is used for intravenous drip. at the end of infusion, the plasma concentration reaches the maximum, and the elimination half-life is 13.9 hours. micafungin has the highest concentration in lung, liver, spleen and kidney tissues, but not detected in cerebrospinal fluid. After intravenous infusion, it is mainly metabolized in the liver and excreted in feces and urine. |
| usage | the recommended dose for the treatment of esophageal candidiasis is 150 mg per day, and the recommended dose for the prevention of candidiasis in patients undergoing hematopoietic stem cell transplantation is 50 mg per day. According to the available clinical data, the average course of treatment or prevention of the above two diseases is 15 days and 19 days respectively. The medicinal saline or 5% glucose injection is prepared and diluted. The administration time is at least 1 hour, otherwise it is easy to produce adverse reactions. |
| drug interaction | the peak blood concentration of nifedipine can be increased by 42%. if necessary, consider reducing the dose of nifedipine or stopping the drug. To increase the area under the blood concentration curve of the anti-organ rejection drug sirolimus (Sirolimus) by 21%, the dose of sirolimus should be reduced as appropriate. (2016-03-02) |
| adverse reactions | uncommon are: abnormal liver function indicators, hypokalemia, hypomagnesemia, hypophosphatemia, leukopenia and related symptoms caused by lymphopenia or neutropenia (such as oliguria, dry mouth), personality changes, myalgia or muscle spasm, numbness of hands and feet, fatigue, anorexia, bone joint pain, poor breathing, asphalt stool, chest pain, cold and heat, hoarseness, sore throat, dysuria, shortness of breath, white spots of oral mucosa, etc. Less common are anemia, hypertension, hypocalcemia, thrombocytopenia, anaphylactic shock. Liver and kidney damage and hemolytic reactions have also been reported, which increase the liver function indicators ALT, AST and renal function indicators creatinine and urea nitrogen. |
| drug preparation | can only be prepared and diluted with normal saline (replaced by 5% glucose injection). Every 50 mg of micafungin sodium is first dissolved in 5 ml of normal saline. In order to reduce the generation of foam, the glass bottle must be gently rotated and not shaken with force. Subsequently, the dissolved micafungin sodium solution was added to 100 ml of normal saline for drip administration for at least 1 h. |
Last Update：2024-04-09 02:00:07
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