Alprostadil
Encyclopedia
Prostaglandin E1 known pharmaceutically as alprostadil, is a prostaglandin
. It is a drug used in the treatment of erectile dysfunction
and has vasodilatory
properties.
as urethral
suppositories
and in injectable form. The suppositories are sold under the brand name MUSE (Medicated Urethral Suppository for Erection). The injectable forms are Edex and Caverject. 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.
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.
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.
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).
For gastrointestinal applications, see misoprostol
.
Prostaglandin
A prostaglandin is any member of a group of lipid compounds that are derived enzymatically from fatty acids and have important functions in the animal body. Every prostaglandin contains 20 carbon atoms, including a 5-carbon ring....
. It is a drug used in the treatment of erectile dysfunction
Erectile dysfunction
Erectile dysfunction is sexual dysfunction characterized by the inability to develop or maintain an erection of the penis during sexual performance....
and has vasodilatory
Vasodilation
Vasodilation refers to the widening of blood vessels resulting from relaxation of smooth muscle cells within the vessel walls, particularly in the large arteries, smaller arterioles and large veins. The process is essentially the opposite of vasoconstriction, or the narrowing of blood vessels. When...
properties.
Sexual dysfunction
Alprostadil is sold in the United StatesUnited States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
as urethral
Urethra
In anatomy, the urethra is a tube that connects the urinary bladder to the genitals for the removal of fluids out of the body. In males, the urethra travels through the penis, and carries semen as well as urine...
suppositories
Suppository
A suppository is a drug delivery system that is inserted into the rectum , vagina or urethra , where it dissolves.They are used to deliver both systemically-acting and locally-acting medications....
and in injectable form. The suppositories are sold under the brand name MUSE (Medicated Urethral Suppository for Erection). The injectable forms are Edex and Caverject. 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
Corpus cavernosum penis
The corpus cavernosum penis is one of a pair of sponge-like regions of erectile tissue which contain most of the blood in the penis during penile erection...
.
Apricus Biosciences
Apricus Biosciences
Apricus Biosciences is a San Diego based pharmaceutical company which develops products utilizing a permeation enhancer, the NexACT drug delivery technology to enable multi-route administration of compounds across numerous therapeutic classes....
is developing proprietary drugs; Vitaros for men with erectile dysfunction
Erectile dysfunction
Erectile dysfunction is sexual dysfunction characterized by the inability to develop or maintain an erection of the penis during sexual performance....
, Femprox for female sexual arousal disorder
Female sexual arousal disorder
Female sexual arousal disorder , commonly referred to as frigidity, is a disorder characterized by a persistent or recurrent inability to attain sexual arousal or to maintain arousal until the completion of a sexual activity. The diagnosis can also refer to an inadequate lubrication-swelling...
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.
Alprostadil is also available as a generic. The major cost is that it must be mixed by a compounding pharmacy
Compounding
Compounding is the mixing of drugs by a compounding pharmacist to fit the unique needs of a patient...
and supplies of alprostadil may be difficult to obtain. There are different formulations, including Bimix and Trimix
Trimix (injection)
Trimix is an injectable three-drug cocktail used to treat erectile dysfunction. The active ingredients in the mixture are usually alprostadil, papaverine, and phentolamine. The injection must be compounded by a pharmacy and administered via intracavernosal injection. Trimix is typically compounded...
, which may include papaverine
Papaverine
Papaverine is an opium alkaloid antispasmodic drug, used primarily in the treatment of visceral spasm, vasospasm , and occasionally in the treatment of erectile dysfunction...
and/or phentolamine
Phentolamine
Phentolamine is a reversible nonselective alpha-adrenergic antagonist. -Mechanism:Its primary action is vasodilation due to α1 blockade....
. 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.
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.
Other uses
Alprostadil is also used in maintaining a patent ductus arteriosusPatent ductus arteriosus
Patent ductus arteriosus is a congenital disorder in the heart wherein a neonate's ductus arteriosus fails to close after birth. Early symptoms are uncommon, but in the first year of life include increased work of breathing and poor weight gain...
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).
For gastrointestinal applications, see misoprostol
Misoprostol
Misoprostol is a drug that is used for the prevention of non steroidal anti inflammatory drug induced gastric ulcers, for early abortion, to treat missed miscarriage, and to induce labor. The latter use is controversial in the United States. Misoprostol was invented and marketed by G.D...
.