Staxyn ODT

Name: Staxyn ODT

What is vardenafil, and how does it work (mechanism of action)?

Vardenafil is an oral drug that is used to treat impotence, the inability to attain or maintain a penile erection. It has a mechanism of action that is similar to sildenafil (Viagra), and tadalafil (Cialis). Penile erection is caused by the engorgement of the penis with blood. This engorgement occurs when the blood vessels delivering blood to the penis increase in size and increase the delivery of blood to the penis. At the same time, the blood vessels carrying blood away from the penis decrease in size and decrease the removal of blood from the penis. Sexual stimulation that leads to the engorgement and erection causes the production and release of nitric oxide in the penis. Nitric oxide then activates the enzyme, guanylate cyclase to produce cyclic guanosine monophosphate (cGMP). The cGMP is primarily responsible for increasing and decreasing the size of the blood vessels carrying blood to and from the penis, respectively. Vardenafil prevents an enzyme called phosphodiesterase-5 (PDE-5) from destroying cGMP so that cGMP persists longer. The longer cGMP persists, the more prolonged the engorgement of the penis. Vardenafil was approved by the FDA in August 2003.

What brand names are available for vardenafil?

Levitra, Staxyn ODT

Is vardenafil available as a generic drug?

GENERIC AVAILABLE: No

Do I need a prescription for vardenafil?

Yes

Pharmacology

Mechanism of Action

Sexual stimulation causes nitric oxide to be released in corpus cavernosum, and nitric oxide activates guanylate cyclase, which in turn increases cyclic guanosine monophosphate (cGMP), thus causing smooth-muscle relaxation; PDE-5 inhibitors enhance smooth muscle-relaxing effects of nitric oxide in corpus cavernosum by inhibiting degradation of cGMP

Absorption

Rapidly absorbed

Bioavailability: 15%

Onset: 60 min

Peak plasma time: 30-120 min

Peak plasma concentration: 8-19% lower for ODT than for film-coated tablet

Distribution

Protein bound: 95%

Vd: 208 L

Metabolism

Metabolized in liver by CYP3A4 and (in minor amounts) CYP2C9

Metabolites: M1 (active; plasma concentration 26% of parent compound)

Elimination

Half-life: 3-6 hr

Total body clearance: 56 L/hr

Excretion: Feces (95%), urine (5%)

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