Tìm theo
Propylthiouracil
Các tên gọi khác (14 ) :
  • 2-Mercapto-6-propyl-4-pyrimidone
  • 2-Mercapto-6-propylpyrimid-4-one
  • 2-Thio-4-oxo-6-propyl-1,3-pyrimidine
  • 2-Thio-6-propyl-1,3-pyrimidin-4-one
  • 2,3-dihydro-6-Propyl-2-thioxo-4(1H)-pyrimidinone
  • 4-Propyl-2-thiouracil
  • 6-Propyl-2-thio-2,4(1H,3H)pyrimidinedione
  • 6-Propyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one
  • 6-Propylthiouracil
  • 6-Thio-4-propyluracil
  • Propiltiouracilo
  • Propylthiouracil
  • Propylthiouracile
  • Propylthiouracilum
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 51-52-5
ATC: H03BA02
ĐG : Actavis Group , http://www.actavis.com
CTHH: C7H10N2OS
PTK: 170.232
A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C7H10N2OS
Phân tử khối
170.232
Monoisotopic mass
170.051383642
InChI
InChI=1S/C7H10N2OS/c1-2-3-5-4-6(10)9-7(11)8-5/h4H,2-3H2,1H3,(H2,8,9,10,11)
InChI Key
InChIKey=KNAHARQHSZJURB-UHFFFAOYSA-N
IUPAC Name
6-propyl-2-sulfanylidene-1,2,3,4-tetrahydropyrimidin-4-one
Traditional IUPAC Name
propylthiouracil
SMILES
CCCC1=CC(=O)NC(=S)N1
Độ tan chảy
219 °C
Độ hòa tan
1200 mg/L (at 25 °C)
logP
0.4
logS
-2.15
pKa (strongest acidic)
8.09
pKa (Strongest Basic)
-2.7
PSA
41.13 Å2
Refractivity
48.9 m3·mol-1
Polarizability
17.79 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
1
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Propylthiouracil is a thiourea antithyroid agent. Grave's disease is the most common cause of hyperthyroidism. It is an autoimmune disease where an individual's own antibodies attach to thyroid stimulating hormone receptors within cells of the thyroid gland and then trigger overproduction of thyroid hormone. The two thyroid hormones manufactured by the thyroid gland, thyroxine (T4) and triiodothyronine (T3), are formed by combining iodine and a protein called thyroglobulin with the assistance of an enzyme called peroxidase. PTU inhibits iodine and peroxidase from their normal interactions with thyroglobulin to form T4 and T3. This action decreases thyroid hormone production. PTU also interferes with the conversion of T4 to T3, and, since T3 is more potent than T4, this also reduces the activity of thyroid hormones. The actions and use of propylthiouracil are similar to those of methimazole.
Cơ Chế Tác Dụng : A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534) Propylthiouracil binds to thyroid peroxidase and thereby inhibits the conversion of iodide to iodine. Thyroid peroxidase normally converts iodide to iodine (via hydrogen peroxide as a cofactor) and also catalyzes the incorporation of the resulting iodide molecule onto both the 3 and/or 5 positions of the phenol rings of tyrosines found in thyroglobulin. Thyroglobulin is degraded to produce thyroxine (T4) and tri-iodothyronine (T3), which are the main hormones produced by the thyroid gland. Therefore propylthiouracil effectively inhibits the production of new thyroid hormones.
Dược Động Học :
▧ Absorption :
Well absorbed following oral administration.
▧ Protein binding :
82%
▧ Route of Elimination :
Propylthiouracil is readily absorbed and is extensively metabolized. Approximately 35% of the drug is excreted in the urine, in intact and conjugated forms, within 24 hours.
▧ Half Life :
2 hours
Độc Tính : Oral, rat: LD50 = 1250 mg/kg.
Chỉ Định : Used to manage hyperthyroidism which is due to an overactive thyroid gland (Grave's disease).
Tương Tác Thuốc :
  • Acenocoumarol The anti-thyroid agent, propylthiouracil, may decrease the anticoagulant effect of acenocoumarol.
  • Anisindione The anti-thyroid agent, propylthiouracil, may decrease the anticoagulant effect of anisindione.
  • Dicoumarol The anti-thyroid agent, propylthiouracil, may decrease the anticoagulant effect of dicumarol.
  • Digoxin The antithyroid agent may increase the effect of digoxin.
  • Warfarin Propylthiouracil may decrease the anticoagulant effect of warfarin. Monitor for changes in the therapeutic and adverse effects of warfarin if propylthiouracil is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Bu Kwang
    Sản phẩm biệt dược : Antiroid
  • Công ty : Pfizer
    Sản phẩm biệt dược : Propil
  • Công ty : Biolab
    Sản phẩm biệt dược : Propilracil
  • Công ty : Admeda
    Sản phẩm biệt dược : Propycil
  • Công ty : Paladin
    Sản phẩm biệt dược : Propyl-Thyracil
  • Công ty : Actavis
    Sản phẩm biệt dược : Propylthiouracil
  • Công ty : Genopharm
    Sản phẩm biệt dược : Proracyl
  • Công ty : Phafag
    Sản phẩm biệt dược : Prothiucil
  • Công ty : Uni-Pharma
    Sản phẩm biệt dược : Prothuril
  • Công ty : Alkaloid
    Sản phẩm biệt dược : PTU
  • Sản phẩm biệt dược : Thiuragyl
  • Công ty : Sun-Farm
    Sản phẩm biệt dược : Thyrosan
  • Công ty : Nevada Pharma
    Sản phẩm biệt dược : Tiotil
  • Công ty : Metlen
    Sản phẩm biệt dược : Tirostat
  • Công ty : Pharmasant
    Sản phẩm biệt dược : Uracil
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00550
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=657298
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505181
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07569
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00562
ChemSpider
http://www.chemspider.com/Chemical-Structure.571424.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/67253-651-10
PharmGKB
http://www.pharmgkb.org/drug/PA451156
Wikipedia
http://en.wikipedia.org/wiki/Propylthiouracil
Drugs.com
http://www.drugs.com/cdi/propylthiouracil.html
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