Posted in Pharmaceutical materials, Pharmaceutical Raw Materials 30. Dec, 2011 · Edit
Caspofungin for the echinocandin antifungal agents, is glucan synthase inhibitors, can inhibit ß-1 ,3-d-glucan synthesis, thereby interfering with fungal cell wall synthesis. This product has a broad-spectrum antifungal activity against Candida albicans, Candida tropicalis, Candida glabrata, Candida krusei and other good antibacterial activity against Aspergillus fumigatus, Aspergillus flavus, Aspergillus terreus and Aspergillus and aspergillosis other than several filamentous fungi and dimorphic fungi have antibacterial activity.
Pharmacokinetics
Blood concentration of this product with increasing intravenous doses (from 5mg to 100mg) and increased linearly. Single-dose intravenous caspofungin 70mg, the mean blood concentration of 12.4μg/ml, 24h after 1.42μg/ml, elimination half-life 9.29h. The product of the serum protein binding rate (about 96%). In the liver, kidney and colorectal tissue drug concentrations were significantly higher than the plasma, small intestine, lung and spleen and plasma concentrations similar to the heart, brain and plasma concentrations lower than the concentration of the thigh. Elimination half-life of 9 ~ 10h. This product is mainly metabolized in the liver, the feces and urine. About 1.4% of the dose excreted in the urine from the prototype. The product enters the human body 97% and albumin by hydrolysis and N-acetylation and slowly metabolized.
Indications
This product is used in the treatment of Candida sepsis and the following Candida infections: intra-abdominal abscess, peritonitis and intra-abdominal infections; esophageal candidiasis; refractory or intolerant of other treatments such as amphotericin B, amphotericin B liposome and / or itraconazole therapy of invasive aspergillosis. Also used for febrile neutropenic patients with fungal infections.
Adverse reactions
1 general fever, headache, abdominal pain 2. Digestive tract, nausea, vomiting, diarrhea. 3. Hepatic enzyme levels. 4. Blood anemia. 5. Peripheral phlebitis, thrombophlebitis, infusion-related reactions. 6, skin rash, pruritus. 7. Common laboratory abnormalities of serum aminotransferase, bilirubin, alkaline phosphatase, serum creatinine, elevated blood urea nitrogen, serum potassium, decreased hemoglobin, hematocrit blood thin cheek.
Taboos
1. Allergic to the chemicals were banned. 2. There is no information on drug safety of children is not recommended in patients 18 years of age.
Note
1. Patients with severe liver dysfunction, there were no drugs in clinical experience.
2. This product should be a separate infusion should not be mixed with other intravenous agents.
3. This product is stable in glucose solution, it can not be diluted with glucose injection.
4. There is no report of drug overdose, the maximum dose of 100mg has been well tolerated dialysis products can not be removed.
Drug interactions
1. This product can cause blood tacrolimus concentration, the two combined should be monitoring of tacrolimus blood concentration, and adjust the dose of tacrolimus.
2. It can be used to increase the AUC of cyclosporin A, but the same blood concentration. Combination of both can occur when serum aminotransferase levels, both in combination should be avoided.
3. Rifampicin: according to Wei Secretary nevirapine, phenytoin, dexamethasone, carbamazepine can reduce the serum concentration, in combination with these drugs should be the product daily 70mg.
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