トリアムテレン 化学特性,用途語,生産方法
解説
トリアムテレン，2,4,7-triamino-6-phenylpteridine．C12H11N7(253.26)．2,4,6-トリアミノ-5-ニトロソピリミジンとフェニルアセトニトリルとを反応させると得られる．黄色の結晶．融点316 ℃．λmax 356 nm(ε 21000)．鉱酸に易溶，水，有機溶媒にほとんど不溶．副腎皮質鉱質コルチコイドのアルドステロンにきっ抗して，利用作用を現す．利尿剤，降圧剤，むくみ治療剤に使用される．LD50 410 mg/kg(マウス，経口)．
効能
利尿薬, アルドステロン拮抗薬, 上皮性ナトリムチャネル遮断薬
商品名
トリテレン (京都薬品工業)
説明
Triamterene is an inhibitor of the epithelial sodium channel (ENaC; IC
50 = 4.5 μM for the rat channel).
In vivo, triamterene (0.5-32 mg/animal) enhances sodium secretion and decreases potassium secretion in adrenalectomized rats. Formulations containing triamterene have been used in the treatment of edema. This product is also available as an analytical reference standard .
化学的特性
Yellow Solid
使用
Triamterene is a potassium-sparing diuretic ie, it inhibits the urinary excretion of potassium
生物学の機能
Triamterene (Dyrenium)
results in changes in urinary electrolyte
patterns that are qualitatively similar to those produced
by spironolactone. The mechanism by which this
agents bring about the alterations in electrolyte loss,
however, is quite different. Triamterene
produces this effects whether or not aldosterone or any
other mineralocorticoid is present. The action of this
drug is clearly unrelated to endogenous mineralocorticoid
activity, and this drug is effective in adrenalectomized
patients.
一般的な説明
Odorless yellow powder or crystalline solid. Melting point 316°C. Almost tasteless at first and with a slightly bitter aftertaste. Acidified solutions give a blue fluorescence. Used as a diuretic drug.
空気と水の反応
Sensitive to light; slowly oxidized upon exposure to air. Insoluble in water.
反応プロフィール
2,4,7-Triamino-6-phenylpteridine neutralizes acids in exothermic reactions to form salts plus water. May be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen may be generated in combination with strong reducing agents, such as hydrides.
火災危険
Flash point data for 2,4,7-Triamino-6-phenylpteridine are not available; however, 2,4,7-Triamino-6-phenylpteridine is probably combustible.
作用機序
Triamterene is a pyrazine derivative that inhibits reabsorption of sodium ions without
increasing excretion of potassium ions. It exhibits the same approximate effect as spironolactone;
however, it does not competitively bind with aldosterone receptors. Its action does
not have an effect on secretion of aldosterone or its antagonists, which are a result of direct
action on renal tubules.
This potassium sparing diuretic causes a moderate increase in excretion of sodium and
bicarbonate ions in urine, and it raises excretion of potassium and ammonia ions. It has little
effect on urine volume.
臨床応用
Triamterene can be used in the treatment of congestive
heart failure, cirrhosis, and the edema caused by
secondary hyperaldosteronism. It is frequently used in
combination with other diuretics except spironolactone.
Amiloride, but not triamterene, possesses antihypertensive
effects that can add to those of the thiazides.
These K
+-sparing diuretics have low efficacy when
used alone, since only a small amount of total Na reabsorption
occurs at more distal sites of the nephron.
These compounds are used primarily in combination
with other diuretics, such as the thiazides and loop diuretics,
to prevent or correct hypokalemia. The availability
of fixed-dose mixtures of thiazides with nonsteroidal
K
+-sparing compounds has proved a rational
form of drug therapy. Both triamterene and amiloride
are available alone or in combination with hydrochlorothiazide.
副作用
Because the actions of triamterene and amiloride
are independent of plasma aldosterone levels, their prolonged
administration is likely to result in hyperkalemia.
Both amiloride and triamterene are contraindicated
in patients with hyperkalemia.Triamterene
should not be given to patients with impaired renal
function. Potassium intake must be reduced, especially
in outpatients.A folic acid deficiency has been reported
to occur occasionally following the use of triamterene.
トリアムテレン 上流と下流の製品情報
原材料
準備製品