MEPARTRICIN
MEPARTRICIN
CAS: 11121-32-7
Molecular Formula: C59H86N2O19
MEPARTRICIN - Names and Identifiers
| Name | MEPARTRICIN |
| Synonyms | S-160 MEPARTRICIN |
| CAS | 11121-32-7 |
MEPARTRICIN - Physico-chemical Properties
| Molecular Formula | C59H86N2O19 |
| Molar Mass | 1127.32 |
| Storage Condition | 2-8°C |
MEPARTRICIN - Risk and Safety
| WGK Germany | 2 |
| RTECS | RW5692000 |
| Toxicity | LD50 in mice: >2 g/kg orally; 200 mg/kg i.p. (Bruzzese, 1972) |
MEPARTRICIN - References
| Background and overview | polyene macrolide antibiotics, also known as polyene antibiotics, are a class of compounds containing conjugated polyenes and hydroxy macrolides with characteristic UV absorption peaks, due to the difference in the number of conjugated double bonds can be divided into: triene, tetraene, pentene, hexene, heptene, the mechanism of action of these antibiotics mainly acts on the cell membrane ergosterol, change the permeability of cells. Polyene antibiotics have strong antibacterial activity against filamentous fungi and yeast-like bacteria. In addition, some polyene antibiotics also inhibit some pathogenic protozoa, such as Trichomonas, Amoeba, Trypanosoma, Leishmania, etc. The activity of heptaene antibiotics was stronger than that of other polyene antibiotics. Polyene antibiotics mainly include trichostatin (trichosycin), candidin (candicidin), kanamycin (hamcin), cannitracin (cannitracin), pimaricin (pimaricin), aureofuccinin (aureofucin,R-22), pecin, etc. metrimazine is a new semisynthetic Polyene Antibiotic, isolated from the medium of streptomycin aureus strain, and also produced by Streptomyces sp. The Polyene Antibiotic patrex produced by aureofaciens is prepared by methylation, and has obvious inhibitory effect on fungi and protozoa, especially on Candida albicans. This product has two types of compound preparation of unilateral preparation and the compound preparation of sodium dodecyl sulfate and the use and usage of the two are not the same. Metrimazine in the intestinal tract with androgen, estrogen, cholesterol and other sterols to form metrimazine-sterol complex, thereby preventing its absorption, therefore, it is possible to reduce the stimulating effect of hormone-like substances on prostatic epithelial cell hyperplasia for the treatment of benign prostatic hypertrophy. Sodium dodecyl sulfate is a surface-active substance that promotes the absorption of meparatrox through the intestinal mucosa. After oral administration, the plasma concentration was much higher than the minimum inhibitory concentration, and the distribution concentration was the highest in renal tissue, and the lower in liver and lung tissue. Subsequent excretion by the kidneys causes the drug to present a higher concentration in the urine to treat intestinal or vaginal candidiasis or trichomoniasis. |
| pharmacological effects | The antibacterial principle is to destroy sterols on cell membranes, interfere with their normal metabolism, and inhibit growth and reproduction. It is usually used in combination with the co-absorbent sodium dodecyl sulfate to treat fungal diseases such as vaginitis, Trichomonas vaginitis and small intestinal candidiasis caused by C.albicans. This product can also be used for the treatment of benign prostatic hyperplasia, the mechanism of action is that it is not absorbed by the intestinal mucosa and irreversibly binds to sterols in the intestinal lumen, thereby reducing the stimulation of the steroid hormone on the prostate hyperplasia. |
| toxicity studies | 1. With mice, rats and dogs as the experimental subjects, through oral and intra-duodenal administration of two kinds of drug delivery, to observe the effect of metrimazine on autonomic nervous system, central nervous system, the role of the respiratory system and the cardiovascular system and general behavioral effects, as well as on male hormones and anti-male hormones, female hormones and anti-female hormones, progesterone and anti-progesterone, the results show that, even at high doses, there was no effect on the endocrine system and none of these systems. 2. The acute toxicity test showed that the LD50 of male rats, mice and rabbits was more than 1000mg/kg. 3. Subacute toxicity and chronic toxicity experiments showed that the mice, dogs, respectively, to increase the dose of meparatrox for consecutive months, did not find any pathological changes in hematology, body fluid and liver function tests were normal morphology, histology and organ weight examination showed no change. 4. Teratological studies show that rabbits and mice during the whole pregnancy oral clinical dose of this product has no effect on fetal development and offspring, animal experiments show that this product has no mutagenic effect, histological examination showed no carcinogenic effect. |
| Clinical Study | mepitreine is an anti-deep fungal drug with high antibacterial activity against Candida fungi. The effect is similar to that of amphotericin and nystatin, and the antibacterial effect is 6-40 times stronger than that of mould and amphotericin. In vitro experiments showed that the minimum inhibitory concentration (MIC) of Candida albicans was 0.015-0.0064 μg/ml, the MIC of other Candida was 0.015-0.5 μg/ml, the MIC of Trichomonas vaginalis was 0.03-0.6 μg/ml, and the MIC of Cryptococcus neoformans was 0.015-0.3 g/mL. The drug and the fungal cell membrane on the ergodic alcohol combined with the formation of meparatrox-hydantoin complex, the formation of hollow cylindrical hydrophilic pores on the membrane, thus destroying the permeability of the cytoplasmic membrane, leakage of intracellular material causes cell death. |
| pharmacokinetics | , and maintain the level higher than the MIC; Distribution: After absorption, it is distributed in all tissues of the whole body, especially the highest concentration in the kidney, and the lower concentration in the liver and lung. metabolism and excretion: the distribution concentration of this product is higher in the kidney; It is excreted from the urine, and the unabsorbed part is excreted from the feces. 30 hours after drug withdrawal from the body to eliminate, no accumulation phenomenon. Have special effects on Candida albicans, Trichomonas also have inhibitory effect. |
| Clinical application | Candida albicans vaginitis: due to the presence of sodium dodecyl sulfate, the compound enteric-coated tablets of sodium dodecyl sulfate and sodium dodecyl sulfate have good absorption, after oral its blood concentration is much higher than the MIC, so the origin of the rectal ampulla and small intestine Candida albicans vaginitis has a high effect. Clinical trials comparing with other most commonly used topical antifungal agents (e. G., amphotericin, clomiphene, yikangwa) have shown that the anti-Candida albicans effect of metrimazine is better, its curative effect is superior to that of gram mold and Yikang. Systemic candidiasis: metrimazole has a good effect on Candida albicans infection in some immunocompromised patients. Therefore, it can be used to treat Candida albicans infection in patients with leukemia, organ transplant or cancer. Benign prostatic hyperplasia (BPH): in the intestinal tract, metrimazole forms a metrimazole complex with sterols such as androgens and estrogen cholesterol to reduce hormone levels, thereby, the stimulating effect of the hormone on the hyperplasia of prostatic epithelial cells is reduced, and thus it can be used for the treatment of benign prostatic hypertrophy. At present, the drug of choice for the treatment of benign prostatic hyperplasia. In addition, due to the characteristics of broad-spectrum, low toxicity, high efficiency and no residue, metrimazole is also widely used in the production of edible fungi such as Pleurotus ostreatus as a new type of disinfectant. |
| specification | enteric-coated tablets of meparatrox: 5 000U. Metrimazine vaginal tablets: 25000 U. |
| dosage | oral: 10000 U,12 hours, after meals, 3 days for a course of treatment. For cases of complex, refractory or drug-resistant fungal infections, the course of treatment may be extended and repeated, as appropriate. |
| adverse reactions | fewer side effects and symptoms of light, low incidence. Mainly for Nausea, stomach discomfort, abdominal distension and other gastrointestinal reactions, generally can be improved by taking after meals. |
| precautions | the effect of postprandial administration is better, which can reduce the adverse reactions. |
| contraindication | is contraindicated for those allergic to this product and accessories. |
| pregnant and lactating women | pregnant women, especially in the first 3 months of pregnancy is contraindicated. |
| Use in Children | to avoid accidental ingestion in children. |
| Main reference materials | [1] Jiang Jinliang, Zhang Shiling, chief editor of Ji Dahong. Handbook of commonly used new drugs. Jinan: Shandong Science and Technology Publishing House. 2000. Page 89-90 [2] Liu Haiying. A preliminary study on the preparation process of paroxetine. Master Thesis of East China University of Science and Technology. 2011. [3] editorial board of Chinese Medical Encyclopedia; Huang Liang. 18 pharmacology and pharmacology. Chinese medical encyclopedia. Shanghai: Shanghai Science and Technology Publishing House. 1988. P. 262. [4] Zhou Deqing, edited by Xu Shiju. Dictionary of microbiology. Tianjin: Tianjin Science and Technology Publishing House. 2005. Page 458-459 [5] Ma Zhenyou, ed. The latest handbook of dermatological drugs. Xi'an: World Book Publishing Company, Xi'an branch. 2008. Page 82-83 |
Last Update：2024-04-09 02:00:17
