Tìm theo
Tioconazole
Các tên gọi khác (3) :
  • Tioconazol
  • Tioconazolum
  • Vagistat-1
antifungal agents, 14 alpha demethylase inhibitors
Thuốc Gốc
Small Molecule
CAS: 65899-73-2
ATC: D01AC07, G01AF08
ĐG : Johnson & Johnson Healthcare , http://www.jnjcanada.com
CTHH: C16H13Cl3N2OS
PTK: 387.711
Tioconazole is an antifungal medication of the Imidazole class used to treat infections caused by a fungus or yeast. Tioconazole topical (skin) preparations are also available for ringworm, jock itch, athlete's foot, and tinea versicolor or "sun fungus". Tioconazole interacts with 14-alpha demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the yeast membrane. In this way, tioconazole inhibits ergosterol synthesis, resulting in increased cellular permeability.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H13Cl3N2OS
Phân tử khối
387.711
Monoisotopic mass
385.981416859
InChI
InChI=1S/C16H13Cl3N2OS/c17-12-1-2-13(14(18)7-12)15(8-21-5-4-20-10-21)22-9-11-3-6-23-16(11)19/h1-7,10,15H,8-9H2
InChI Key
InChIKey=QXHHHPZILQDDPS-UHFFFAOYSA-N
IUPAC Name
1-{2-[(2-chlorothiophen-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole
Traditional IUPAC Name
1-{2-[(2-chlorothiophen-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl}imidazole
SMILES
ClC1=C(COC(CN2C=CN=C2)C2=C(Cl)C=C(Cl)C=C2)C=CS1
Độ hòa tan
1.65e-02 g/l
logP
4.4
logS
-4.4
pKa (Strongest Basic)
6.77
PSA
27.05 Å2
Refractivity
94.53 m3·mol-1
Polarizability
36.84 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Tioconazole is a broad-spectrum imidazole antifungal agent that inhibits the growth of human pathogenic yeasts. Tioconazole exhibits fungicidal activity in vitro against Candida albicans, other species of the genus Candida, and against Torulopsis glabrata. Tioconazole prevents the growth and function of some fungal organisms by interfering with the production of substances needed to preserve the cell membrane. This drug is effective only for infections caused by fungal organisms. It will not work for bacterial or viral infections.
Cơ Chế Tác Dụng : Tioconazole is an antifungal medication of the Imidazole class used to treat infections caused by a fungus or yeast. Tioconazole topical (skin) preparations are also available for ringworm, jock itch, athlete's foot, and tinea versicolor or "sun fungus". Tioconazole interacts with 14-alpha demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the yeast membrane. In this way, tioconazole inhibits ergosterol synthesis, resulting in increased cellular permeability. Tioconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the yeast membrane. In this way, tioconazole inhibits ergosterol synthesis, resulting in increased cellular permeability. Tioconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms and the uptake of purine, impair triglyceride and/or phospholipid biosynthesis, and inhibit the movement of calcium and potassium ions across the cell membrane by blocking the ion transport pathway known as the Gardos channel.
Dược Động Học :
▧ Absorption :
Systemic absorption following a single intravaginal application of tioconazole in nonpregnant patients is negligible.
▧ Metabolism :
Orally administered tioconazole is extensively metabolized. The major metabolites are glucuronide conjugates.
Độc Tính : Symptoms of overdose include erythema, stinging, blistering, peeling, edema, pruritus, urticaria, burning, and general irritation of the skin, and cramps.
Chỉ Định : For the local treatment of vulvovaginal candidiasis (moniliasis).
Liều Lượng & Cách Dùng : Ointment - Intravaginal
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : GyneCure
  • Công ty :
    Sản phẩm biệt dược : Monistat 1
  • Công ty :
    Sản phẩm biệt dược : Trosyd
  • Công ty :
    Sản phẩm biệt dược : Trosyl
  • Công ty :
    Sản phẩm biệt dược : Vagistat-1
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01007
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5482
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508604
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08082
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00890
ChemSpider
http://www.chemspider.com/Chemical-Structure.5282.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/24385-374-82
PharmGKB
http://www.pharmgkb.org/drug/PA164746156
Wikipedia
http://en.wikipedia.org/wiki/Tioconazole
RxList
http://www.rxlist.com/cgi/generic3/tioconaz.htm
Drugs.com
http://www.drugs.com/cdi/tioconazole.html
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