Vardenafil

drugbox
IUPAC_name = 4- [2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl] -
9-methyl-7-propyl- 3,5,6,8-tetrazabicyclo [4.3.0]
nona-3,7,9-trien-2-one


CAS_number = 224785-90-4
ATC_prefix = G04
ATC_suffix = BE09
ATC_supplemental =
PubChem = 110634
DrugBank = APRD00699
C=23 | H=32 | N=6 | O=4 | S=1
molecular_weight = 488.604 g/mol
bioavailability = 15%
protein_bound = 95%
metabolism = Hepatic (CYP3A4)
elimination_half-life = 4–5 hours
excretion = Biliary
pregnancy_category = B3 (Au), B (U.S.)
legal_status =
legal_AU = S4
legal_UK = POM
legal_US = Rx
routes_of_administration = Oral

Vardenafil (INN) is a PDE5 inhibitor used for treating impotence (erectile dysfunction) that is sold under the trade name Levitra (Bayer AG), (GSK), (SP) .

History

Vardenafil was co-marketed by Bayer Pharmaceuticals,GSK, and SP under the trade name "Levitra". As of 2005, the co-promotion rights of GSK on "Levitra" have been returned to Bayer in many markets outside the U.S. In Italy, Bayer sells vardenafil as "Levitra" and GSK sells it as Vivanza, thus, because of European Union trade rules, parallel imports might result in "Vivanza" sold next to "Levitra" in the E.U.

Clinical use

Vardenafil's indications and contra-indications are the same as with other PDE5 inhibitor; it is closely related in function to sildenafil (Viagra) and tadalafil (Cialis). Structurally, the difference between a vardenafil molecule and the others is a methyl group and a nitrogen atom's position. Vardenafil's relatively short effective time is comparable to sildenafil's.

Adverse drug reactions

The common, adverse drug reactions (side effects) are the same as with other PDE5 inhibitors. The frequent vardenafil-specific side effect is nausea; the infrequent side effects are: abdominal pain, back pain, photosensitivity, abnormal vision, eye pain, facial oedema, hypertension, palpitation, tachycardia, arthralgia, myalgia, rash, itch, and priapism. (Rossi, 2004)

One possibly serious, but rare, side effect with vardenafil is heart attack. Also in rare cases, vardenafil use may damage penile tissue, resulting in permanent impotence.Health Canada (2006)

On 18 October 2007, the FDA announced that a warning about possible deafness (sudden hearing loss) would be added to the drug labels of Vardenafil, and other PDE5 inhibitors. cite web | url= http://www.fda.gov/bbs/topics/NEWS/2007/NEW01730.html| title= FDA Announces Revisions to Labels for Cialis, Levitra and Viagra| author= | date= 2007-10-18| publisher= Food and Drug Administration| accessdate=2007-12-08 ]

Drug interactions

Vardenafil should not be used by men taking nitrate medications, because combining them with vardenafil might provoke potentially life-threatening hypotension (low blood pressure).

Dose forms

It is available in 2.5 mg, 5 mg, 10 mg, and 20 mg doses in round orange tablets. The normal starting dose is 10 mg (roughly equivalent to 50 mg of sildenafil). Vardenafil should be taken 1 to 2 hours prior to sexual activity, with a maximum dose frequency of once per day.In some territories, such as the UK, only certain doses may be available, i.e. 5 mg, 10 mg, and 20 mg.

See also

* PDE5 inhibitor
* Sildenafil (Viagra)
* Tadalafil (Cialis)

Notes

External links

* [http://www.levitra.com/ Official Levitra website]
* [http://www.fda.gov/cder/consumerinfo/druginfo/levitra.htm FDA's Consumer Information]
* [http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=110634 PubChem Information]