ミノキシジル 化学特性,用途語,生産方法
外観
白色～わずかにうすい黄色, 結晶性粉末～粉末
溶解性
メタノールに溶ける。
用途
血管拡張剤、高血圧の治療の研究。
用途
ミノキシジル（Minoxidil）とは血管拡張薬として開発された成分。後に発毛効果があるとされ発毛剤に転用され。
効能
血圧降下薬, 外用発毛促進薬, ATP感受性カリウムチャネル開口薬
説明
Minoxidil is a peripheral vasodilator that directly relaxes vascular smooth musculature,
thus, lowering systolic and diastolic pressure. Its action is linked to the activation of calcium
channels. Open calcium channels cause hyperpolarization of smooth muscle cells,
which in turn, reduces the flow of calcium ions into the cell, which is necessary for supporting
vascular tonicity. However, when taking minoxidil, tachycardia, elevated renin
secretion, and water and sodium ion retention all appear simultaneously with hypotension.
化学的特性
White Crystalline Solid
使用
Used as an antihypertensive and antialopecia agent. Minoxidil activates ATP-activated K+ channels
定義
ChEBI: Minoxidil is a pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6. It has a role as a vasodilator agent and an antihypertensive agent. It is a pyrimidine N-oxide, a member of piperidines and an aminopyrimidine.
一般的な説明
Minoxidil, 2,4-diamino-6-piperidinopyrimidine-3-oxide . It is converted to minoxidil sulfate in the liver bya sulfotransferase enzyme.
The antihypertensive properties of minoxidil are similarto those of hydralazine hydrochloride, in that minoxidil candecrease arteriolar vascular resistance. Minoxidil exerts itsvasodilatory action by a direct effect on arteriolar smoothmuscle and appears to have no effect on the CNS or on theadrenergic nervous system in animals. The serum half-lifeis 4.5 hours, and the antihypertensive effect may last up to24 hours.
生物活性
Antihypertensive. Antialopecia agent. K + channel (K ATP ) activator.
薬物動態学
Minoxidil is absorbed from the GI tract and is metabolized to its active sulfate metabolite. Plasma concentrations for
minoxidil sulfate peak within 1 hour and then decline rapidly. Following an oral dose of minoxidil, its hypotensive effect
begins in 30 minutes, is maximal in 2 to 8 hours, and persists for approximately 2 to 5 days. The delayed onset of the
hypotensive effect for minoxidil is attributed to its metabolism to its active metabolite. The drug is not bound to plasma
proteins. The major metabolite for minoxidil is its N-O-glucuronide, which unlike the sulfate metabolite is inactive as a
hypotensive agent. Approximately 10 to 20% of an oral dose of minoxidil is metabolized to its active metabolite,
minoxidil O-sulfate, and approximately 20% of minoxidil is excreted unchanged.
臨床応用
Minoxidil is used for severe hypertension that is difficultto control with other antihypertensive agents. The drug hassome of the characteristic side effects of direct vasodilatorydrugs. It causes sodium and water retention and may requirecoadministration of a diuretic. Minoxidil also causes reflextachycardia, which can be controlled by use of a -adrenergicblocking agent.
Minoxidil topical solution is used to treat alopecia androgenitica(male-pattern baldness). Although the mechanismis not clearly understood, topical minoxidil is believed to increasecutaneous blood flow, which may stimulate hairgrowth. The stimulation of hair growth is attributed to vasodilationin the vicinity of application of the drug, resultingin better nourishment of the local hair follicles.
副作用
Adverse reactions include local irritation and contact dermatitis.
If the treatment is discontinued, clinical regression occurs within 3 months
to the state of hair thinning that would have occurred had the treatment
not been started. Twice-daily treatment is more efficacious than once-daily
application. Women who use the5%concentrationmay note the development
of facial hair, which is reversible on discontinuation of the medication. The
5% concentration can be more irritating than the 2% solution.
薬物相互作用
When minoxidil is administered with diuretics or other hypotensive drugs, the hypotensive effect of minoxidil increases,
and concurrent use may cause profound orthostatic hypotensive effects.
ミノキシジル 上流と下流の製品情報
原材料
準備製品