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药品详细

Triamterene(氨苯蝶啶)

化学结构式图
中文名
氨苯蝶啶
英文名
Triamterene
分子式
C12H11N7
化学名
6-phenylpteridine-2,4,7-triamine
分子量
Average: 253.2626
Monoisotopic: 253.107593387
CAS号
396-01-0
ATC分类
C03D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A pteridine that is used as a mild diuretic. [PubChem]

生产厂家
  • Wellspring pharmaceutical corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. WellSpring Pharmaceutical Corporation. Dyrenium (triamterene) capsules prescribing information. Neptune, NJ; 2001 June.
  2. Gilfrich HJ, Kremer G, Mohrke W, Mutschler E, Volger KD: Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability. Eur J Clin Pharmacol. 1983;25(2):237-41. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Pteridines
Substructures
  • Aliphatic and Aryl Amines
  • Benzene and Derivatives
  • Pyrimidines and Derivatives
  • Pyrazines
  • Heterocyclic compounds
  • Aromatic compounds
  • Pteridines
  • Imines
  • Cyanamides
适应症
药理
Indication 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.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Rapidly absorbed, with somewhat less than 50% of the oral dose reaching the urine.
Volume of distribution Not Available
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.
Route of elimination Not Available
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]
Toxicity 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.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00132 Triamterene Pathway SMP00132
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 316 °C PhysProp
water solubility 48.2 mg/L Not Available
logP 0.98 HANSCH,C ET AL. (1995)
Predicted Properties
Property Value Source
water solubility 9.63e-01 g/l ALOGPS
logP 1.21 ALOGPS
logP 1.11 ChemAxon
logS -2.4 ALOGPS
pKa (strongest acidic) 15.88 ChemAxon
pKa (strongest basic) 3.11 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 7 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 129.62 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 75.13 ChemAxon
polarizability 25.9 ChemAxon
药物相互作用
Drug Interaction
Benazepril Increased risk of hyperkalemia
Candesartan Increased risk of hyperkalemia
Captopril Increased risk of hyperkalemia
Cilazapril Increased risk of hyperkalemia
Drospirenone Increased risk of hyperkalemia
Enalapril Increased risk of hyperkalemia
Eplerenone This association presents an increased risk of hyperkalemia
Eprosartan Increased risk of hyperkalemia
Forasartan Increased risk of hyperkalemia
Fosinopril Increased risk of hyperkalemia
Indomethacin Risk of acute renal impairment with this combination
Irbesartan Increased risk of hyperkalemia
Lisinopril Increased risk of hyperkalemia
Losartan Increased risk of hyperkalemia
Moexipril Increased risk of hyperkalemia
Perindopril Increased risk of hyperkalemia
Polystyrene sulfonate Antagonism of action
Potassium Increased risk of hyperkalemia
Quinapril Increased risk of hyperkalemia
Ramipril Increased risk of hyperkalemia
Saprisartan Increased risk of hyperkalemia
Spirapril Increased risk of hyperkalemia
Tasosartan Increased risk of hyperkalemia
Telmisartan Telmisartan may increase the hyperkalemic effect of Triamterene. Monitor for increased serum potassium concentrations during concomitant therapy.
Trandolapril Increased risk of hyperkalemia. Monitor serum potassium levels.
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Valsartan Increased risk of hyperkalemia
食物相互作用
Not Available

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