Clinical Information
Gen. Code and Des.
29188 alprostadil URETHRAL SUPP.URETH 500 MCG
GCN and Des.
2297 alprostadil URETHRAL SUPP.URETH 500 MCG
Strength
500MCG
Dose Form
SUPPOSITORY, URETHRAL
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
24129200 VASODILATING AGENTS, MISCELLANEOUS
Active Ingredients
704 alprostadil 745653
MUSE- alprostadil suppository
Meda Pharmaceuticals Inc.
DESCRIPTION
MUSE� (alprostadil) is a single-use, medicated transurethral system for the delivery of alprostadil to the male urethra. Alprostadil is suspended in polyethylene glycol 1450 (as excipient) and is formed into a medicated pellet (micro-suppository measuring 1.4 mm in diameter by 3 mm or 6 mm in length) that resides in the tip of a translucent hollow applicator. MUSE is administered by inserting the applicator stem into the urethra after urination. The pellet containing alprostadil is delivered by depressing the applicator button (see Figure 1). The components of the delivery system are constructed of medical grade polypropylene. Each MUSE system is packaged in an individual foil pouch. Diagram of the MUSE Transurethral System
The active ingredient in MUSE is alprostadil, which is chemically identical to the naturally occurring eicosanoid, prostaglandin E1 (PGE1 ). The chemical name for alprostadil is prost-13-en-1-oic acid, 11,15-dihydroxy-9-oxo-(11?,13E,15S)-(1R,2R,3R)-3-hydroxy-2-[(E)-(3S)-3-hydroxy-1-octenyl]-5-oxo-cyclopentane heptanoic acid, and the molecular weight is 354.49. The empirical formula is C20 H34 O5 . The structural formula of alprostadil is represented below:
Structural Formula
Alprostadil is a white to off-white crystalline powder with a melting point between 115� and 116�C. Its solubility at 35�C is 8000 mcg per 100 mL double-distilled water. The inactive ingredient in MUSE is polyethylene glycol 1450, USP. There are no other active agents or excipients in MUSE.
MUSE is available in 4 dosage strengths: 125 mcg, 250 mcg, 500 mcg, and 1000 mcg.
CLINICAL PHARMACOLOGY
Mechanism of Action: Prostaglandin E1 is a naturally occurring acidic lipid that is synthesized from fatty acid precursors by most mammalian tissues and has a variety of pharmacologic effects. Human seminal fluid is a rich source of prostaglandins, including PGE1 and PGE2 , and the total concentration of prostaglandins in ejaculate has been estimated to be approximately 100�200 mcg/mL. In vitro, alprostadil (PGE1 ) has been shown to cause dose-dependent smooth muscle relaxation in isolated corpus cavernosum and corpus spongiosum preparations. Additionally, vasodilation has been demonstrated in isolated cavernosal artery segments that were pre-contracted with either norepinephrine or prostaglandin F2 ? . When alprostadil was injected into the corpus cavernosum of pigtail monkeys in vivo, dose-dependent increases in cavernosal artery blood flow were observed. INDICATIONS AND USAGE
MUSE is indicated for the treatment of erectile dysfunction. Studies that established benefit demonstrated improvements in success rates for sexual intercourse compared with similarly administered placebo.
