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CAS NO.23593-75-1
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C22H17ClN2 |
| Molar Mass | 344.84 |
| Density | 1.1095 (rough estimate) |
| Melting Point | 147-149°C |
| Boling Point | 501.14°C (rough estimate) |
| Flash Point | 245.5°C |
| Water Solubility | <10mg/L(25 ºC) |
| Solubility | Soluble in DMSO (25 mM), chloroform (50 mg/ml), DMF, ethyl acetate, ethanol, methanol |
| Vapor Presure | 5.42E-09mmHg at 25°C |
| Appearance | Crystallization |
| Color | White to Almost white |
| Maximum wavelength(λmax) | ['556nm(Phosphate buffer sol.)(lit.)'] |
| Merck | 14,2417 |
| pKa | pKa 4.7(EtOH 50%aq ) (Uncertain) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.5940 (estimate) |
| MDL | MFCD00057220 |
| Physical and Chemical Properties | White powder or colorless crystalline powder. Melting point 147-149 °c. Soluble in ethanol, acetone, chloroform, almost insoluble in water. Odorless, tasteless, quickly decomposed in acid solution. Clotrimazole hydrochloride, melting point 159 °c. |
| Use | Antimycotic drugs for the treatment of epidermal and deep fungal infections |
| broad-spectrum antifungal drug | clotrimazole is a synthetic pyrrole antifungal drug, which has inhibitory effect on a variety of pathogenic fungi and can also have bactericidal effect when the concentration is high. Clotrimazole inhibits the biosynthesis of fungal ergosterol and other sterols by interfering with the activity of cytochrome P450; damages the fungal cell membrane and changes its permeability, causing the leakage of important substances in the cell; it can also inhibit the triglyceride of fungi And the biosynthesis of phospholipids; this product can also inhibit the activity of oxidation and peroxidase, cause excessive accumulation of peroxides in the cell, and cause fungal subcellular structure degeneration and necrosis. Clotrimazole has a broad-spectrum antifungal activity, and has a good antibacterial effect on Epidermophyton, Trichophyton, Aspergillus, Coloring fungi, Cryptococcus and Candida, and has a good antibacterial effect on Sporothrix Schenckii, Dermatitis Bud bacteria, Costococcus, Histoplasma bacteria, etc. also have certain antibacterial activity. |
| Pharmacological activity | In vivo and in vitro, clotrimazole has a good antibacterial effect on Candida, Cryptococcus, Aspergillus, Algae, Dermatophytes, etc. The curative effect on superficial fungal disease is similar to griseofulvin, and the curative effect on deep fungal disease is similar to amphotericin B, it has a good effect on visceral pathogenic fungi such as Candida albicans, Cryptococcus neoformans, Coccidioides and Histoplasma, etc., and has a stronger effect on Candida albicans than nystatin. Fungi are not easy to develop drug resistance to this product. This product is easy to absorb internally, and can be taken orally to treat systemic and deep fungal infections, such as aspergillosis, candidiasis albicans, cryptococcosis, coccidioidomycosis, histoplasmosis (dogs, cats) and Fungal sepsis, etc. For severe deep fungal infection, it should be combined with amphotericin B. External use can also treat superficial fungal infections, such as ringworm of the crown and animal tinea corporis, ringworm. Not effective for tinea capitis. Clotrimazole is also effective against some gram-positive bacteria and trichomonas vaginalis. |
| pharmacokinetics | clotrimazole is rarely absorbed after oral administration. after 3g oral administration in adults, the blood peak concentration is only 1.29mg/L for 2 hours and 0.78mg/L for 6 hours. During continuous administration, the blood drug concentration decreases due to the induction of liver enzymes. The elimination half-life is 4.5~6 hours. Most of this product is metabolically inactivated in the liver and excreted by bile. Only a small amount (less than 1% of the dosage) is excreted from the urine in the prototype. Most of the excreted in the urine are inactive metabolites. This product has a high concentration in feces, including oral unabsorbed parts and bile excretion parts. Clotrimazole is widely distributed in the body, with a high concentration in liver and adipose tissue, and cannot penetrate the normal meninges into the cerebrospinal fluid. The serum protein binding rate of this product is 50%. |
| clinical application | clinical topical use 1% clotrimazole cream or solution to treat skin infections such as candida ringworm, tinea versicolor, tinea pedis, and onychomycosis. Clotrimazole vaginal tablets (100mg) are administered to treat vaginal infections of Candida and Trichomonas. Side effects include local irritation and burning sensation. Oral administration is used to treat deep fungal infection, but the toxic and side effects are severe, including gastrointestinal irritation, neutropenia and abnormal liver function. 1. oral administration:(1) for the treatment of oral and pharyngeal candida infection. (2) It is used for the prevention of oropharyngeal candida infection in patients with chemotherapy, immunodeficiency or deficiency. 2. Topical application:(1) Candida cutaneous infection. (2) Tinea manus, pedis, tinea cruris and tinea corporis caused by Trichophyton, Microsporum and Epidermophyton; Tinea versicolor caused by Pityrosporum. 3. Vaginal administration:(1) Vaginitis caused by Candida or other fungi. (2) Infectious leucorrhea caused by yeast. (3) the drug sensitive bacteria caused by vaginal double infection. |
| Mechanism of action | (1) By reducing the activity of cytochrome P450, it inhibits the biosynthesis of sterols such as ergosterol in the fungal cell membrane, damages the fungal cell membrane and changes Its permeability causes the leakage of important substances in the cell. (2) Clotrimazole can also inhibit the biosynthesis of fungal triacylglycerol and phospholipids. (3) It can also inhibit the activities of oxidase and peroxidase, resulting in excessive accumulation of hydrogen peroxide in cells, causing fungal subcellular structure degeneration and cell necrosis. (4) Candida albicans can inhibit its transformation from spores to invasive hyphae. |
| drug interaction | clotrimazole can inhibit the metabolism of sirolimus, dofetilide and other drugs mediated by cytochrome P450 3A4, and increase the blood concentration of these drugs. Combined use with tacrolimus and triclosa can slow down the metabolism of these drugs and increase their toxic reactions. Clotrimazole is combined with betamethasone, it can make the skin susceptible to infection or increase the chance of microbial reproduction. The possible mechanism is that the local inflammatory response is inhibited; combined with nystatin, amphotericin B and flucytosine, it has no synergistic antibacterial effect on Candida albicans; And when combined with amphotericin B, it has an antagonistic effect on pharmacodynamics. |
| adverse reactions | 1. oral administration:(1) gastrointestinal reactions: loss of appetite, nausea, vomiting, abdominal pain, diarrhea, etc. (2) Hepatotoxicity: Since most of clotrimazole is metabolized in the liver, liver damage may occur, causing elevated serum bilirubin, alkaline phosphatase and aminotransferase, which can be restored after stopping the drug. (3) Occasionally, temporary neuropsychiatric abnormalities may occur, manifested as depression, hallucinations and disorientation. Once such reactions occur, treatment must be discontinued. (4) Occasionally leukopenia. (5) Some patients can cause urethral burning after taking medicine. At this time, they should drink more water to ensure more urine output and do not need to stop taking medicine. 2, local medication occasionally local irritation, itching or burning sensation, skin may appear erythema, papules, blisters, desquamation, etc. Contact dermatitis has also been reported. 3, a small number of vaginal drug delivery can appear vaginal burning sensation, lower abdominal spastic pain, abdominal distension, frequent urination, etc. Different degrees of allergic reactions can also be seen, such as skin itching and erythema, shortness of breath, hypotension or transient sensation reduction, nausea, diarrhea, etc. |
| instructions for administration | 1. this medicine cannot be used for systemic fungal infection. Due to the poor oral absorption of this drug, adverse reactions are more common, and local external use or vaginal administration is now used. 2. When using this medicine, avoid drug contact with eyes. 3. Clotrimazole vaginal tablets are prohibited from oral use. 4. Take the lozenge of this medicine for 15-30 minutes at a time to slowly and completely dissolve the medicine. Do not chew the lozenge or swallow the whole lozenge. 5. Vaginal treatment is prohibited during menstruation. 6. If temporary neuropsychiatric abnormalities, severe gastrointestinal reactions and local skin allergic reactions occur, the drug should be stopped immediately. |
| use | broad-spectrum antifungal drugs. It is used for systemic fungal infection and also for local fungal infection. Antimycotics, used to treat epidermis and deep mycotic infections, etc. |
CAS:
23593-75-1
MF:
C22H17ClN2
MW:
344.84
EINECS:
245-764-8
MDL No.:
MFCD00057220
Melting point:
147-149°C
Boiling point:
501.14°C (rough estimate)
Density
1.1095 (rough estimate)
refractive index
1.5940 (estimate)
storage temp.
2-8°C
solubility
Soluble in chloroform, DMSO, DMF and alcohols
pka
pKa 4.7(EtOH 50%aq ) (Uncertain)
color
White to Almost white
Water Solubility
<10mg/L(25 ºC)
λmax
556nm(Phosphate buffer sol.)(lit.)
Merck
14,2417
InChI
InChI=1S/C22H17ClN2/c23-21-14-8-7-13-20(21)22(25-16-15-24-17-25,18-9-3-1-4-10-18)19-11-5-2-6-12-19/h1-17H
InChIKey
VNFPBHJOKIVQEB-UHFFFAOYSA-N
SMILES
C1N(C(C2=CC=CC=C2Cl)(C2=CC=CC=C2)C2=CC=CC=C2)C=CN=1
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.