Minoxidil Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R26/27/28:Sehr giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S22:Staub nicht einatmen.
Beschreibung
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.
Chemische Eigenschaften
White Crystalline Solid
Verwenden
Used as an antihypertensive and antialopecia agent. Minoxidil activates ATP-activated K+ channels
Definition
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.
Allgemeine Beschreibung
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.
Biologische Aktivität
Antihypertensive. Antialopecia agent. K + channel (K ATP ) activator.
Pharmakokinetik
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.
Clinical Use
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.
Nebenwirkungen
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.
Arzneimittelwechselwirkung
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.
Minoxidil Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
