Tìm theo
Triamterene
Các tên gọi khác (8 ) :
  • 6-phenylpteridine-2,4,7-triamine
  • Dyrenium
  • Teridin
  • Triamteren
  • Triamtérène
  • Triamterene
  • Triamtereno
  • Triamterenum
diuretics, epithelial sodium channel blockers
Thuốc Gốc
Small Molecule
CAS: 396-01-0
ATC: C03DB02
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C12H11N7
PTK: 253.2626
A pteridine that is used as a mild diuretic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H11N7
Phân tử khối
253.2626
Monoisotopic mass
253.107593387
InChI
InChI=1S/C12H11N7/c13-9-7(6-4-2-1-3-5-6)16-8-10(14)18-12(15)19-11(8)17-9/h1-5H,(H6,13,14,15,17,18,19)
InChI Key
InChIKey=FNYLWPVRPXGIIP-UHFFFAOYSA-N
IUPAC Name
6-phenylpteridine-2,4,7-triamine
Traditional IUPAC Name
triamterene
SMILES
NC1=NC(N)=C2N=C(C(N)=NC2=N1)C1=CC=CC=C1
Độ tan chảy
316 °C
Độ hòa tan
48.2 mg/L
logP
0.98
logS
-2.4
pKa (strongest acidic)
15.88
pKa (Strongest Basic)
3.11
PSA
129.62 Å2
Refractivity
75.13 m3·mol-1
Polarizability
25.9 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
7
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Triamterene, a relatively weak, potassium-sparing diuretic and antihypertensive, is used in the management of hypokalemia. Triamterene is similar in action to amiloride but, unlike amiloride, increases the urinary excretion of magnesium.
Cơ Chế Tác Dụng : A pteridine that is used as a mild diuretic. [PubChem] Triamterene inhibits the epithelial sodium channels on principal cells in the late distal convoluted tubule and collecting tubule, which are responsible for 1-2% of total sodium reabsorption. As sodium reabsorption is inhibited, this increases the osmolarity in the nephron lumen and decreases the osmolarity of the interstitium. Since sodium concentration is the main driving force for water reabsorption, triamterene can achieve a modest amount of diuresis by decreasing the osmotic gradient necessary for water reabsorption from lumen to interstitium. Triamterene also has a potassium-sparing effect. Normally, the process of potassium excretion is driven by the electrochemical gradient produced by sodium reabsorption. As sodium is reabsorbed, it leaves a negative potential in the lumen, while producing a positive potential in the principal cell. This potential promotes potassium excretion through apical potassium channels. By inhibiting sodium reabsorption, triamterene also inhibits potassium excretion.
Dược Động Học :
▧ Absorption :
Rapidly absorbed, with somewhat less than 50% of the oral dose reaching the urine.
▧ Protein binding :
55-67% (93% for the OH-TA-ester metabolite)
▧ Metabolism :
Triamterene is primarily metabolized to the sulfate conjugate of hydroxytriamterene. Both the plasma and urine levels of this metabolite greatly exceed triamterene levels.
▧ Half Life :
255 minutes (188 minutes for OH-TA-ester metabolite) after IV administration.
▧ Clearance :
* 4.5 l/min [total plasma clearance] * 0.22 l/kg [renal plasma clearance]
Độc Tính : In the event of overdosage it can be theorized that electrolyte imbalance would be the major concern, with particular attention to possible hyperkalemia. Other symptoms that might be seen would be nausea and vomiting, other G.I. disturbances, and weakness. It is conceivable that some hypotension could occur. The oral LD50 in mice is 380 mg/kg.
Chỉ Định : For the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and the nephrotic syndrome; also in steroid-induced edema, idiopathic edema, and edema due to secondary hyperaldosteronism.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Kotobuki Seiyaku
    Sản phẩm biệt dược : Diuteren
  • Công ty : Goldshield
    Sản phẩm biệt dược : Dyazide
  • Công ty : Wellspring
    Sản phẩm biệt dược : Dyrenium
  • Công ty : Mercury
    Sản phẩm biệt dược : Dytac
  • Công ty : Ciiphar
    Sản phẩm biệt dược : Riyazine
  • Công ty : Kyoto Yakuhin
    Sản phẩm biệt dược : Triteren
  • Công ty : Ying Yuan
    Sản phẩm biệt dược : Urinis
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00384
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5546
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507623
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00386
ChemSpider
http://www.chemspider.com/Chemical-Structure.5345.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=6644
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/65197-002-01
PharmGKB
http://www.pharmgkb.org/drug/PA451752
Wikipedia
http://en.wikipedia.org/wiki/Triamterene
RxList
http://www.rxlist.com/cgi/generic/triamterine.htm
Drugs.com
http://www.drugs.com/triamterene.html
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