Prostaglandin E1

Prostaglandin E1 속성

Prostaglandin E1 MSDS

11,15-Dihydroxy-9-oxoprost-13-en-1-oic acid

Prostaglandin E1 C화학적 특성, 용도, 생산

개요

 Alprostadil은 또한 노르 에피네프린의 신경 방출을 방지하여 노르 에피네프린의 혈관 수축 작용을 길항 할 수 있으며 비 아드레날린, 비 콜린성 혈관 확장 성 신경 전달 물질의 작용을 향상시킬 수 있습니다. ED 치료에서 알프로 스타 틸은 섬유주 평활근을 이완시키고 해면 동맥과 그 가지를 확장시킴으로써 발기를 유도합니다.

용도

Alprostadil (Prostglandin E1)은 성인 남성의 발기 부전 (ED) 치료에 사용됩니다.

개요

Prostaglandin E1 is an endogenous prostaglandin with vasodilatory, anti-platelet, and anti-hypertensive activities. It is in clinical use for the treatment of erectile dysfunction and the emergency management of infants with patent ductus arteriosus. It has also been used in the treatment of peripheral arterial occlusive disease (PAD).

화학적 성질

Crystalline Solid

용도

A primary Prostaglandin; easily crystallized from purified biological extracts. Vasodilator (peripheral)

Indications

Alprostadil (prostaglandin E₁ [PGE₁]; Edex, Topiglan) exerts a number of effects, including systemic vasodilation, inhibition of platelet aggregation, and stimulation of intestinal motility. PGE₁ relaxes isolated smooth muscle cells contracted by norepinephrine. It has become widely used in the treatment of ED. Alprostadil binds with PGE receptors and results in a cyclic adenosine monophosphate (cAMP) mediated smooth muscle relaxation. Little is known about the pharmacokinetics of PGE₁, but it is believed that as much as 80% is metabolized in one pass through the lungs. Such rapid degradation probably accounts for its lack of significant cardiovascular side effects when administered intracavernosally. PGE₁ can also be metabolized in the penis.

World Health Organization (WHO)

Alprostadil, a prostaglandin with vasodilating and platelet antiaggregatory activity, was introduced in 1984 for the treatment of chronic arterial obstruction. Intravenous administration of the drug has been associated with adverse effects that have sometimes been severe. These include allergic reactions, pulmonary oedema and cardiac insufficiency. Interactions with antihypertensive agents, vasodilators, anticoagulants and inhibitors of platelet aggregation have also occurred. This has led the German agency to modify the approved product information of alprostadil preparations to warn against these adverse effects.

Biological Functions

Prostaglandin E1 is produced endogenously to relax vascular smooth muscle and cause vasodilation by activating the adenylate cyclase/cAMP pathway. Recent studies show that the cAMP is important in the PGE1 relaxation of penile erectile tissue and vasodilation of penile resistance arteries. Moreover, agents that stimulate the release of cAMP also crossactivate the NO/cGMP cascade.

일반 설명

PGE1, Alprostadil (Prostin VR Pediatric), is a naturally occurring prostaglandin that has found particular use in maintaining a patent (opened) ductus arteriosus in infants with congenital defects that restrict pulmonary or systemic blood flow.
Alprostadil must be administered intravenously continually at a rate of approximately 0.1 μg/kg/min to maintain the patency of the ductus arteriosus until corrective surgery can be performed. Up to 80% of circulating alprostadil may be metabolized in a single pass through the lungs. Because apnea has been observed in 10% to 12% of neonates with congenital heart defects, this product should be administered only when ventilatory assistance is immediately available. Other commonly observed side effects include decreased arterial blood pressure, which should be monitored during infusion; inhibited platelet aggregation, which might aggravate bleeding tendencies; and diarrhea.

생물학적 활성

Prostaglandin with some selectivity for EP 3 and EP 4 receptors (K i values are 1.1, 2.1, 36, 10? and 33 nM for mouse EP 3 , EP 4 , EP 1 , EP 2 and IP receptors respectively). Inhibits platelet aggregation and is a vasodilator in vivo .

Mechanism of action

PGE₁ is not orally effective. Its therapeutic success depends on its being injected intracavernosally or administered transurethrally or intraurethrally. PGE₁ has also been used in combination with other agents, such as papaverine. The injection does not appear to produce any long-term side effects on penile smooth muscle. Transurethral therapy with alprostadil, such as MUSE (alprostadil urethral suppository or medicated urethral system for erection) is also an effective therapeutic technique, and there may be a role for this form of administration in selected patients with ED.The intracavernosal injection of alprostadil (e.g., alprostadil alfadex; Edex, Viridal) is safe and effective in patients with ED when sildenafil is ineffective. Both of these delivery systems have been used in the treatment of ED. MUSE can also be used in conjunction with a penile constrictor device (e.g., ACTIS).

Clinical Use

Prostaglandin E1 (PGE1; Alprostadil) is approved for the intracavernosal (Caverject, Edex)or intraurethral suppository (Muse) treatment of ED. A three-drug combination of PGE1, papaverine, and phentolamine sometimes is used as an intracavernosal injection to achieve a synergistic action. Erectile dysfunction that is medication-induced or caused by endocrine problems, such as hypogonadism or hyper- or hypothyroidism, should be evaluated and appropriately treated before PGE1 treatment is considered.

신진 대사

The major route of excretion of PGE1 metabolites is via the kidney. Its elimination half-life is 5 to 10 minutes. If any alprostadil is systemically absorbed, it is metabolized by a single pass through the lungs. The onset of action is within 10 minutes, and the time to peak effect is less than 20 minutes. The duration of action is 1 to 3 hours for the intracavernosal injection and 30 to 60 minutes for the intraurethral suppository.

Prostaglandin E1 준비 용품 및 원자재

원자재

준비 용품

Prostaglandin E1 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Guangzhou TongYi biochemistry technology Co.,LTD	+8613073028829	mack@tongyon.com	China	2996	58
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12456	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5993	58
CONTIDE BIOTECH CO.,LTD	+85253358525	xena@healthtide-api.com	China	499	58
Shanghai Daken Advanced Materials Co.,Ltd	+86-371-66670886	info@dakenam.com	China	15928	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Shanghai finete Pharmaceutical Co., Ltd.	+86-18221039705		CHINA	139	55
Hubei XinRunde Chemical Co., Ltd.	+8615102730682	bruce@xrdchem.cn	CHINA	566	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
SHANDONG ZHI SHANG CHEMICAL CO.LTD	+86 18953170293	sales@sdzschem.com	China	2931	58

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