【中文品名】异康唑
【药效类别】抗真菌药>咪康唑类
【通用药名】ISOCONAZOLE
【别　　名】Adestan, Fazol, Gyno-Travogen, Icaden, Nupaten, R-15454, Travocort, Travogen, Travogyn
【化学名称】 1H-Imidazole, 1-[2-(2,4-dichlorophenyl)-2-[(2,6-dichlorophenyl)methoxy]ethyl]-
【CA登记号】[27523-40-6]、[24168-96-5]
【结 构 式】

【分 子 式】C18H14Cl4N2O
【分 子 量】416.13
【收录药典】
【开发单位】Janssen
【首次上市】1979年，法国
【性　　状】
【用　　途】异康唑是一种抗真菌的咪唑衍生物。当局部应用时，异康唑具有广谱抗菌活性，包括对革兰氏阳性菌、皮真菌、酵母菌、酵母样真菌、霉菌和毛滴虫有效。

GYNO-TRAVOGEN is effective both against dermatophytes, yeasts, yeast-like fungi and moulds and against gram-positive bacteria.
Pharmacokinetics
The treatment of vaginal mycoses with GYNO-TRAVOGEN is a local therapy, which does not require effective plasma levels of isoconazole. By insertion of the ovule into the vagina, a drug depot is established. The ovule melts at body temperature and forms a viscid, oily mass, which panels the vaginal wall. A part of the drug is dissolved in the vaginal secretion and penetrates into the vaginal epithelium. In the secretion and in the epithelium, a concentration of the antimycotic distinctly above the in vitro determined minimum inhibitory and minimum biocidal concentration is maintained for several days.
After a single vaginal application of an ovule containing 600 mg radio-labelled isoconazole nitrate, the drug was absorbed to an extent of less than 5 % of the dose applied. Absorbed isoconazole nitrate is completely metabolised by the human organism. After intravenous administration of 3H-labelled isoconazole nitrate one third of radiolabelled metabolites were excreted with the urine and two thirds with the faeces, 75 % of the dose already within the first 24 hours. 2,4- dichloromandelic acid and 2-(2,6-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)-acetic acid were characterised as quantitatively most important metabolites in the urine.
Indications
Fungal infections of the vagina including mixed infections with gram-positive bacteria.
Dosage and Administration
The ovule must be inserted deep into the vagina. This is best done in the lying position in the evening before going to sleep using the enclosed applicator. During pregnancy, the applicator is not to be used. The treatment is also not to be carried out during menstruation.
Contraindications
None so far known.
Warnings and Precautions
For treatment of the external genital region or for simultaneous prophylactic treatment of the partner it is recommended to use an appropriate anti-fungal cream.
During treatment and in the following week vaginal douching should be avoided. To avoid renewed infection, personal linen (face cloth, towels, underwear - preferably of cotton) should be changed daily and boiled.
Preclinical Safety Data
The results from repeated dose toxicity studies did not indicate that particular health risks could be associated with the therapeutic use of GYNO-TRAVOGEN.
In vitro- and in vivo experiments for the detection of gene and chromosome mutations did not indicate a mutagenic potential of isoconazole. No in vivo tumorigenicity studies have been conducted. According to the present state of knowledge, there is no evidence of a tumorigenic potential of isoconazole to be derived from the results of mutagenicity tests, repeated dose toxicity studies, chemical structure and biochemical mechanism of action.
In a series of special reproduction toxicity studies, isoconazole exerted no adverse effects on any phase of the reproductive cycle. In particular, there was no evidence of a teratogenic potential.
According to the results from local tolerance studies on the skin and mucous membranes, no remarkable local irritation has to be expected under therapeutic conditions. In view of the results obtained at the rabbit eye, conjunctival irritation has to be expected after inadvertent contamination of the eye.
Pregnancy and Lactation
Use in Pregnancy
The experience with the use of isoconazole-containing preparations during pregnancy does not indicate a teratogenic risk in humans.
Use in Lactation
Because of the only slight absorption (less than 5 % of the dose administered) and the short duration of the therapy, damage to the baby from isoconazole nitrate transferred with the breast milk can be ruled out.
Adverse Effects
Local concomitant symptoms such as smarting and itching occur occasionally.
Interactions
Since GYNO-TRAVOGEN does not contain rubber-softening substances - an incompatibility with latex condoms is not to be expected.
Overdosage
According to the results from single dose toxicity studies, the active ingredient isoconazole can be classified as virtually non-toxic. No risk of acute intoxication has to be expected after a single overdose or inadvertent oral intake of one ovule.
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原产地英文商品名:GYNO-TRAVOGEN 600mg/ovule/box
原产地英文药品名:ISOCONAZOLE
原产地英文化合物名称:1H-Imidazole, 1-[2-(2,4-dichlorophenyl)-2-[(2,6-dichlorophenyl)methoxy]ethyl]-
中文参考商品译名:GYNO-TRAVOGEN 600毫克/胚珠/盒