Tìm theo
Terconazole
Các tên gọi khác (1) :
  • Terazol 3
antifungal agents
Thuốc Gốc
Small Molecule
CAS: 67915-31-5
ATC: G01AG02
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C26H31Cl2N5O3
PTK: 532.462
Terconazole is an anti-fungal medication, primarily used to treat vaginal fungal infections. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H31Cl2N5O3
Phân tử khối
532.462
Monoisotopic mass
531.180395297
InChI
InChI=1S/C26H31Cl2N5O3/c1-19(2)31-9-11-32(12-10-31)21-4-6-22(7-5-21)34-14-23-15-35-26(36-23,16-33-18-29-17-30-33)24-8-3-20(27)13-25(24)28/h3-8,13,17-19,23H,9-12,14-16H2,1-2H3/t23-,26-/m0/s1
InChI Key
InChIKey=BLSQLHNBWJLIBQ-OZXSUGGESA-N
IUPAC Name
1-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)-4-(propan-2-yl)piperazine
Traditional IUPAC Name
terconazole
SMILES
CC(C)N1CCN(CC1)C1=CC=C(OC[C@H]2CO[C@@](CN3C=NC=N3)(O2)C2=C(Cl)C=C(Cl)C=C2)C=C1
Độ tan chảy
126.3 °C
Độ hòa tan
1.16e-02 g/l
logP
4.5
logS
-4.7
pKa (Strongest Basic)
8.41
PSA
64.88 Å2
Refractivity
153.19 m3·mol-1
Polarizability
56.15 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
7
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
5
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Terconazole is a triazole antifungal agent available for intravaginal use. It is structurally related to imidazole-derivative antifungal agents, although terconazole and other triazoles have 3 nitrogens in the azole ring. By inhibiting the 14-alpha-demethylase (lanosterol 14-alpha-demethylase), Terconazole inhibits ergosterol synthesis. Depletion of ergosterol in fungal membrane disrupts the structure and many functions of fungal membrane leading to inhibition of fungal growth.
Cơ Chế Tác Dụng : Terconazole is an anti-fungal medication, primarily used to treat vaginal fungal infections. [Wikipedia] Terconazole may exert its antifungal activity by disrupting normal fungal cell membrane permeability. Terconazole and other triazole antifungal agents inhibit cytochrome P450 14-alpha-demethylase in susceptible fungi, which leads to the accumulation of lanosterol and other methylated sterols and a decrease in ergosterol concentration. Depletion of ergosterol in the membrane disrupts the structure and function of the fungal cell leading to a decrease or inhibition of fungal growth.
Dược Động Học :
▧ Absorption :
Following intravaginal administration of terconazole in humans, absorption ranged from 5-8% in three hysterectomized subjects and 12-16% in two non-hysterectomized subjects with tubal ligations
▧ Protein binding :
94.9%
▧ Metabolism :
Systemically absorbed drug appears to be rapidly and extensively metabolized. Terconazole primarily undergoes oxidatative N- and O-dealkylation, dioxolane ring cleavage, and conjugation.
▧ Route of Elimination :
Following oral (30 mg) administration of 14C-labelled terconazole, excretion of radioactivity was both by renal (32-56%) and fecal (47-52%) routes.
▧ Half Life :
6.9 hours (range 4.0-11.3)
Độc Tính : The oral LD50 values were found to be 1741 and 849 mg/kg for the male and female in rat.
Chỉ Định : For the treatment of candidiasis (a yeast-like fungal infection) of the vulva and vagina.
Liều Lượng & Cách Dùng : Bead - Intravaginal
Cream - Intravaginal
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Terazol
  • Công ty :
    Sản phẩm biệt dược : Terazol 3
  • Công ty :
    Sản phẩm biệt dược : Zazole
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00251
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441383
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505257
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08080
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00888
ChemSpider
http://www.chemspider.com/Chemical-Structure.390122.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0168-0347-20
PharmGKB
http://www.pharmgkb.org/drug/PA164768834
Wikipedia
http://en.wikipedia.org/wiki/Terconazole
RxList
http://www.rxlist.com/cgi/generic/tercon.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ter1436.shtml
Drugs.com
http://www.drugs.com/cdi/terconazole-cream.html
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