Tìm theo
Griseofulvin
Các tên gọi khác (18 ) :
  • (+)-griseofulvin
  • Amudane
  • Curling factor
  • Fulcin
  • Fulvicin
  • Grifulvin
  • Grisactin
  • Griseofulvin
  • Griseofulvina
  • Griseofulvine
  • Griseofulvinum
  • Grisovin
  • Grysio
  • Lamoryl
  • Likuden
  • Poncyl
  • Spirofulvin
  • Sporostatin
Thuốc điều trị bệnh da liễu
Thuốc Gốc
Small Molecule
CAS: 126-07-8
ATC: D01AA08, D01BA01
ĐG : Actavis Group , http://www.actavis.com
CTHH: C17H17ClO6
PTK: 352.766
An antifungal antibiotic. Griseofulvin may be given by mouth in the treatment of tinea infections. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H17ClO6
Phân tử khối
352.766
Monoisotopic mass
352.071365983
InChI
InChI=1S/C17H17ClO6/c1-8-5-9(19)6-12(23-4)17(8)16(20)13-10(21-2)7-11(22-3)14(18)15(13)24-17/h6-8H,5H2,1-4H3/t8-,17+/m1/s1
InChI Key
InChIKey=DDUHZTYCFQRHIY-RBHXEPJQSA-N
IUPAC Name
(2S,6'R)-7-chloro-2',4,6-trimethoxy-6'-methyl-3H-spiro[1-benzofuran-2,1'-cyclohexan]-2'-ene-3,4'-dione
Traditional IUPAC Name
griseofulvin
SMILES
COC1=CC(OC)=C(Cl)C2=C1C(=O)[C@]1(O2)[C@H](C)CC(=O)C=C1OC
Độ tan chảy
220 °C
Độ hòa tan
8.64 mg/L (at 25 °C)
logP
2.18
logS
-4.61
pKa (strongest acidic)
17.69
pKa (Strongest Basic)
-4.3
PSA
71.06 Å2
Refractivity
87.85 m3·mol-1
Polarizability
34.25 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.44
Dược Lực Học : Griseofulvin is a mycotoxic metabolic product of Penicillium spp. It was the first available oral agent for the treatment of dermatophytoses and has now been used for more than forty years. Griseofulvin is fungistatic with in vitro activity against various species of Microsporum Epidermophyton, and Trichophyton. It has no effect on bacteria or on other genera of fungi. Following oral administration, griseofulvin is deposited in the keratin precursor cells and has a greater affinity for diseased tissue. The drug is tightly bound to the new keratin which becomes highly resistant to fungal invasions. Once the keratin-Griseofulvin complex reaches the skin site of action, it binds to fungal microtubules (tubulin) thus altering fungal mitosis.
Cơ Chế Tác Dụng : An antifungal antibiotic. Griseofulvin may be given by mouth in the treatment of tinea infections. [PubChem] Griseofulvin is fungistatic, however the exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin. It binds to keratin in human cells, then once it reaches the fungal site of action, it binds to fungal microtubes thus altering the fungal process of mitosis.
Dược Động Học :
▧ Absorption :
Poorly absorbed from GI ranging from 25 to 70% of an oral dose. Absorption is significantly enhanced by administration with or after a fatty meal.
▧ Metabolism :
Primarily hepatic with major metabolites being 6-methyl-griseofulvin and its glucuronide conjugate.
▧ Half Life :
9-21 hours
Độc Tính : Side effects are minor: headaches, gastrointestinal reactions and cutaneous eruptions
Chỉ Định : For the treatment of ringworm infections of the skin, hair, and nails, namely: tinea corporis, tinea pedis, tinea cruris, tinea barbae, cradle cap or other conditions caused by Trichophyton or Microsporum fungi.
Tương Tác Thuốc :
  • Acenocoumarol Griseofulvin may decrease the anticoagulant effect of acenocoumarol.
  • Acetylsalicylic acid Griseofulvin may decrease the efficacy of acetylsalicylic acid.
  • Amobarbital The barbiturate, amobarbital, decreases the effect of griseofulvin.
  • Anisindione Griseofulvin may decrease the anticoagulant effect of anisindione.
  • Aprobarbital The barbiturate, aprobarbital, decreases the effect of griseofulvin.
  • Butabarbital The barbiturate, butabarbital, decreases the effect of griseofulvin.
  • Butalbital The barbiturate, butalbital, decreases the effect of griseofulvin.
  • Butethal The barbiturate, butethal, decreases the effect of griseofulvin.
  • Chlorotrianisene The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, chlorotrianisene.
  • Clomifene The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, conjugated estrogens.
  • Cyclosporine Griseofulvin decreases the effect of cyclosporine
  • Dicoumarol Griseofulvin may decrease the anticoagulant effect of dicumarol.
  • Diethylstilbestrol The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, diethylstilbestrol.
  • Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, decreases the effect of griseofulvin.
  • Estradiol The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estradiol.
  • Estriol The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estriol.
  • Estrone The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estrone.
  • Estropipate The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estropipate.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Heptabarbital The barbiturate, heptabarbital, decreases the effect of griseofulvin.
  • Hexobarbital The barbiturate, hexobarbital, decreases the effect of griseofulvin.
  • Liraglutide Cmax may be increased.
  • Medroxyprogesterone Acetate The enzyme inducer, griseofulvin, may decrease the effect of the hormone, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, griseofulvin, may decrease the effect of the hormone, megestrol.
  • Mestranol This product may cause a slight decrease of contraceptive effect
  • Methohexital The barbiturate, methohexital, decreases the effect of griseofulvin.
  • Methylphenobarbital The barbiturate, methylphenobarbital, decreases the effect of griseofulvin.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Pentobarbital The barbiturate, pentobarbital, decreases the effect of griseofulvin.
  • Phenobarbital The barbiturate, phenobarbital, decreases the effect of griseofulvin.
  • Primidone The barbiturate, primidone, decreases the effect of griseofulvin.
  • Quinestrol The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, quinestrol.
  • Quinidine barbiturate The barbiturate, quinidine barbiturate, decreases the effect of griseofulvin.
  • Secobarbital The barbiturate, secobarbital, decreases the effect of griseofulvin.
  • Talbutal The barbiturate, talbutal, decreases the effect of griseofulvin.
  • Ulipristal Concomitant therapy with strong CYP3A4 inducers may decrease plasma concentrations of ulipristal and ultimately its effectiveness. Avoid combination therapy.
  • Warfarin Griseofulvin may decrease the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Suspension - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Crivicin
  • Công ty : Cepharma
    Sản phẩm biệt dược : Fulcin
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Fulvicin
  • Công ty : McNeil
    Sản phẩm biệt dược : Grifulvin
  • Sản phẩm biệt dược : Grifulvin V
  • Công ty : Pedinol
    Sản phẩm biệt dược : Gris-PEG
  • Công ty :
    Sản phẩm biệt dược : Grisactin
  • Công ty :
    Sản phẩm biệt dược : Grison-250
  • Công ty : Fujisawa
    Sản phẩm biệt dược : Grisovin
  • Công ty : Lovens
    Sản phẩm biệt dược : Lamoryl
  • Công ty : Sanofi
    Sản phẩm biệt dược : Likuden
  • Công ty : Takeda
    Sản phẩm biệt dược : Poncyl
  • Công ty :
    Sản phẩm biệt dược : S-Fulvin
  • Công ty :
    Sản phẩm biệt dược : Spirofulvin
  • Công ty : Schering
    Sản phẩm biệt dược : Sporostatin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00400
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441140
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508437
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06686
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00209
ChemSpider
http://www.chemspider.com/Chemical-Structure.389934.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=31775
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/10147-0810-4
PharmGKB
http://www.pharmgkb.org/drug/PA449814
Wikipedia
http://en.wikipedia.org/wiki/Griseofulvin
RxList
http://www.rxlist.com/cgi/generic3/griseofulvin.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/gri1190.shtml
Drugs.com
http://www.drugs.com/cdi/griseofulvin-microsize.html
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