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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/03/18 08:50:04」(JST)

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Prostaglandin E₁ (PGE1), known pharmaceutically as alprostadil,^[1] is a prostaglandin. It is a drug used in the treatment of erectile dysfunction^[2] and has vasodilatory properties.

Medical uses

Patent ductus arteriosus

Alprostadil is also used in maintaining a patent ductus arteriosus in newborns. This is primarily useful when there is threat of premature closure of the ductus arteriosus in an infant with ductal-dependent congenital heart disease, including cyanotic lesions (e.g., pulmonary atresia/stenosis, tricuspid atresia/stenosis, transposition of the great arteries) and acyanotic lesions (e.g., coarctation of the aorta, hypoplastic left heart syndrome, critical aortic stenosis, interrupted aortic arch).

Sexual dysfunction

Alprostadil is sold in the United States as urethral suppositories and in injectable form. The suppositories are sold under the brand name MUSE.^[3] The injectable forms are Edex^[4] and Caverject.^[5] Muse delivers alprostadil as a penile suppository, inserted into the urethra, at least ten minutes before the erection will be needed. Caverject and Edex are similarly fast-acting, but instead are injected by syringe directly into the corpus cavernosum of the penis.

Apricus Biosciences is developing proprietary drugs; Vitaros for men with erectile dysfunction, Femprox for female sexual arousal disorder and RayVa for Raynaud’s phenomenon. Two Phase III studies have been completed for Vitaros, and approval has been granted in Canada. Apricus Biosciences is seeking regulatory approval in Europe, South America, and other territories. Apricus Biosciences sold the rights for Vitaros in the US to Warner Chilcott.^[6]

Alprostadil is also available as a generic. The major cost is that it must be mixed by a compounding pharmacy and supplies of alprostadil may be difficult to obtain. There are different formulations, including Bimix and Trimix, which may include papaverine and/or phentolamine. A typical mix might be 30 mg of papaverine, 2 mg of phentolamine, and 20 mcg alprostadil. As a generic, it is much less expensive than the pre-packaged injectables. It is premixed and must be kept refrigerated and the user must load a syringe with the quantity needed.

Critical limb ischemia

Alprostadil is also used for critical limb ischemia. It increases blood flow by peripheral vasodilation within 5 minutes and induces angiogenesis. It is most effective when the ankle pressure is at least 30 mmHg and at least one tibial artery is patent.

Adverse effects

Apnea
Flushing
bradycardia
hypotension
tachycardia
cardiac arrest
edema
CHF
hyperemia
second-degree heart block
shock
spasm of right ventricle infundibulum
supraventricular tachycardia
ventricular fibrillation
Fever
seizures
Cerebral bleeding
Diarrhea
Urethral pain
urethral burning
urethral bleeding/spotting
testicular pain ( Muse only)
Hematologic
DIC
bleeding
Cortical proliferation of long bones
sepsis
penile pain
prolonged erection
penile fibrosis
injection-site hematoma
penis disorder
injection-site ecchymosis ( Caverject only)
back pain
pain
pelvic pain
accidental injury ( Muse only)

Pharmacokinetics

References

^ Cawello W, Leonhardt A, Schweer H, Seyberth HW, Bonn R, Lomeli AL (September 1995). "Dose proportional pharmacokinetics of alprostadil (prostaglandin E1) in healthy volunteers following intravenous infusion". British Journal of Clinical Pharmacology 40 (3): 273–6. PMC 1365109. PMID 8527291. //www.ncbi.nlm.nih.gov/pmc/articles/PMC1365109/.
^ Harding LM, Adeniyi A, Everson R, Barker S, Ralph DJ, Baranowski AP (December 2002). "Comparison of a needle-free high-pressure injection system with needle-tipped injection of intracavernosal alprostadil for erectile dysfunction". International Journal of Impotence Research 14 (6): 498–501. doi:10.1038/sj.ijir.3900916. PMID 12494285.
^ "Muse Suppository - Facts and Comparisons". Drugs.com. http://www.drugs.com/cdi/muse-suppository.html. Retrieved 4 January 2013.
^ Edex - Facts and Comparisons Drugs.com
^ Caverject - Facts and Comparisons Drugs.com
^ Fain Hughes (2007-10-29). "NEXM: Dutton Sees Strong Speculative Buy and 12-Month Price Double". http://www.tradingmarkets.com/.site/news/Stock%20News/722371/. Retrieved 2007-11-01.

UpToDate Contents

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1. 男性性機能不全の治療 treatment of male sexual dysfunction
2. 糖尿病における勃起不全 erectile dysfunction in diabetes mellitus
3. 下肢の慢性重症下肢虚血の治療 treatment of chronic lower extremity critical limb ischemia
4. 敗血症を起こした幼児に対するアプローチ approach to the septic appearing infant
5. 新生児におけるチアノーゼ性心疾患の診断および初期マネージメント diagnosis and initial management of cyanotic heart disease in the newborn

English Journal

Drugs in early clinical development for the treatment of female sexual dysfunction.

Belkin ZR1, Krapf JM, Goldstein AT.
Expert opinion on investigational drugs.Expert Opin Investig Drugs.2015 Feb;24(2):159-67. doi: 10.1517/13543784.2015.978283. Epub 2014 Nov 6.
INTRODUCTION: There is growing recognition of female sexual dysfunction (FSD) as an important women's health concern. Despite an increased awareness of the pathophysiologic components to FSD, currently, there are no drugs approved for the most common sexual complaint in women-decreased sexual desire
PMID 25376023

A Controlled Study of Alprostadil Liposomal Preparation in the Treatment of Blue Toe Syndrome.

Xi HL1, Li R, Tian ZL, Feng S, Jia GL.
Cell biochemistry and biophysics.Cell Biochem Biophys.2014 Dec 23. [Epub ahead of print]
The aim of this study is to examine the efficacy of alprostadil liposomal preparation in the treatment of blue toe syndrome. As many as 32 patients with blue toe syndrome were randomized into the test group and a control group. Patients out of the test group were treated with alprostadil liposomal p
PMID 25534490

Effect of alprostadil combined with Diammonium glycyrrhizinate on renal interstitial fibrosis in SD rats.

Cai WY1, Gu YY2, Li AM3, Cui HQ1, Yao Y1.
Asian Pacific journal of tropical medicine.Asian Pac J Trop Med.2014 Nov;7(11):900-4. doi: 10.1016/S1995-7645(14)60157-7. Epub 2014 Oct 22.
OBJECTIVE: To observe effect of alprostadil combined with Diammonium glycyrrhizinate on renal interstitial fibrosis in SD rats.METHODS: A total of 75 SD rats were randomly divided into A, B, C, D, E groups with 15 in each group. Rats in group A served as the control group received just only but tiss
PMID 25441991

Japanese Journal

Specific Enhancement of Vascular Endothelial Growth Factor (VEGF) Production in Ischemic Region by Alprostadil : Potential Therapeutic Application in Pharmaceutical Regenerative Medicine

Inoue Hajime,Aihara Masaki,Tomioka Miyuki [他]
Journal of pharmacological sciences 122(2), 158-161, 2013-06
NAID 40019675837

Specific Enhancement of Vascular Endothelial Growth Factor (VEGF) Production in Ischemic Region by Alprostadil — Potential Therapeutic Application in Pharmaceutical Regenerative Medicine

Inoue Hajime,Aihara Masaki,Tomioka Miyuki,Watabe Yu-ichi
Journal of Pharmacological Sciences 122(2), 158-161, 2013
… Alprostadil (lipo-PGE1) is a drug delivery system preparation. … We investigated the effects of alprostadil by using the earflap ischemic model. … The following results were obtained: 1) Treatment with alprostadil significantly increased the VEGF contents in an ischemic ear; … 2) Treatment with alprostadil resulted in strongly expressed VEGF levels only in the ischemic region; …
NAID 130003362711

悪性外耳道炎の5例

三橋拓之,栗田知幸,上田祥久 [他],松田洋一,伊藤信輔,中島格
耳鼻咽喉科臨床 103(1), 15-20, 2010-01-01
… In one case, MEO was well controlled with HBO and the intravenous administration of alprostadil alfadex (PGE1), but the recurrence was severe and the patient died. …
NAID 10026216270

Related Pictures

★リンクテーブル★

リンク元	「プロスタグランジンE1」「アルプロスタジル」
拡張検索	「alprostadil alfadex」

「プロスタグランジンE1」

Prostaglandin E1
Systematic (IUPAC) name
	7-[(1R,3R)-3-hydroxy-2-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-5-oxocyclopentyl]heptanoic acid
Clinical data
MedlinePlus	a695022
Pregnancy cat.	C (US)
Legal status	?
Identifiers
CAS number	745-65-3
ATC code	C01EA01 G04BE01
PubChem	CID 149351
IUPHAR ligand	1882
DrugBank	DB00770
ChEMBL	CHEMBL495
Chemical data
Formula	C20H34O5
Mol. mass	354.481 g/mol
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