Clinical Information
Gen. Code and Des.
31755 alprostadil INTRACAVER VIAL 40 MCG
GCN and Des.
22962 alprostadil INTRACAVER VIAL 40 MCG
Strength
40MCG
Dose Form
VIAL (EA)
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
Inactive Ingredients
18822 rubber, unspecified
2332 sodium citrate 68042
2432 lactose 64044515
3192 benzyl alcohol 100516
CAVERJECT- alprostadil injection, powder, lyophilized, for solution
Pharmacia and Upjohn Company LLC
For Intracavernosal Use
DESCRIPTION
CAVERJECT Sterile Powder contains alprostadil as the naturally occurring form of prostaglandin E1 (PGE1 ) and is designated chemically as (11?,13E,15S)-11,15-dihydroxy-9-oxoprost-13-en-1-oic acid. The molecular weight is 354.49.
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 micrograms per 100 milliliter double distilled water. CAVERJECT is available as a sterile freeze-dried powder for intracavernosal use in four sizes: 5, 10, 20 and 40 micrograms per vial - When reconstituted as directed with 1 milliliter of bacteriostatic water for injection or sterile water, both preserved with benzyl alcohol 0.945% w/v, gives 1.13 milliliters of reconstituted solution. Each milliliter of CAVERJECT contains 5.4, 10.5, 20.5 or 41.1 micrograms of alprostadil depending on vial strength, 172 milligrams of lactose, 47 micrograms of sodium citrate and 8.4 milligrams of benzyl alcohol. The deliverable amount of alprostadil is 5, 10, 20 or 40 micrograms per milliliter because approximately 0.4 microgram for the 5 microgram strength, 0.5 microgram for the 10 and 20 microgram strengths and 1.1 microgram for the 40 microgram strength is lost due to adsorption to the vial and syringe. When necessary, the pH of alprostadil for injection was adjusted with hydrochloric acid and/or sodium hydroxide before lyophilization.
The structural formula of alprostadil is represented below:
Chemical StructureChemical StructureFigureFigureFigureFigureFigureFigureFigureFigureFigureLogo
CLINICAL PHARMACOLOGY
Alprostadil has a wide variety of pharmacological actions; vasodilation and inhibition of platelet aggregation are among the most notable of these effects. In most animal species tested, alprostadil relaxed retractor penis and corpus cavernosum urethrae in vitro. Alprostadil also relaxed isolated preparations of human corpus cavernosum and spongiosum, as well as cavernous arterial segments contracted by either noradrenaline or PGF2? in vitro. In pigtail monkeys (Macaca nemestrina), alprostadil increased cavernous arterial blood flow in vivo. The degree and duration of cavernous smooth muscle relaxation in this animal model was dose-dependent.
Alprostadil induces erection by relaxation of trabecular smooth muscle and by dilation of cavernosal arteries. This leads to expansion of lacunar spaces and entrapment of blood by compressing the venules against the tunica albuginea, a process referred to as the corporal veno-occlusive mechanism.