After the discovery of sildenafil and the huge success found in the treatment of erectile dysfunction, the most important companies in the pharmaceutical market were at a great disadvantage compared to Pfizer, a company that marketed Viagra; as a result, they have steadfastly undertaken the search for new and more effective drugs that inhibit phosphodiesterase type 5, the category to which sildenafil belongs.
Vardenafil is the brainchild of three pharmaceutical giants - companies Bayer Pharmaceuticals, GlaxoSmithKline and Schering-Plow - who have "" joined forces "" to stand up to the pharmaceutical company Pfizer.
Vardenafil is a type 5 phosphodiesterase inhibitor drug used to treat erectile dysfunction.
History of vardenafil
Vardenafil is the second phosphodiesterase type 5 inhibitor drug to be marketed after obtaining Food and Drug Administration clearance for the treatment of erectile dysfunction on 19 August 2003.
Vardenafil was marketed at the same time by the three pharmaceutical companies that created it - Bayer Pharmaceuticals, GlaxoSmithKline and Schering-Plow - under the registered name of Levitra ®. to the pharmaceutical company GlaxoSmithKline the rights to market vardenafil under the name of Levitra in markets outside the United States, therefore in Italy as well as in other countries of the European Union. Today, the pharmaceutical company GlaxoSmithKline markets vardenafil under the registered name of Vivanza ®.
Due to the trade laws of the European Union, which allow parallel amounts, vardenafil in Italy and in other EU member countries. it can be found commercially under both registered names, namely Levitra (sold by Bayer Pharmaceuticals) and Vivanza (sold by GlaxoSmithKline). Recently, an orodispersible form of vardenafil was approved in the United States of America and Canada and is marketed under the registered name of Staxyn ®.
Vardenafil, rather than the result of actual research or scientific discovery, is a structural modification of the parent molecule, sildenafil (active ingredient of viagra). In fact, the chemical structure of vardenafil differs from that of sildenafil only for the different position of a nitrogen atom and for the alkyl substituent of the piperazine ring, which instead of being a methyl group, is an ethyl group, that is, it has only been added a carbon atom that absolutely does not change the pharmacokinetic and pharmacodynamic properties of vardenafil compared to sildenafil. It can in fact be noted that the pharmacological properties, side effects, the time it takes for the drug to take effect and other characteristics of vardenafil are very similar to However, despite all the similarities, vardenafil boasts a particular property that no other type 5 phosphodiesterase inhibitor possesses; vardenafil significantly increases the time it takes from the onset of vaginal penetration to ejaculation and can therefore be also used in the treatment of premature ejaculation. This advantage of vardenafil can be used to treat patients suffering from both erectile dysfunction and premature ejaculation with a single drug.
Mechanism of action
To work, vardenafil needs sufficient sexual stimulation, otherwise its intake does not produce the desired effect.
The physiological process responsible for penile erection includes the release of a certain amount of nitric oxide (NO), a molecular "messenger", into the corpus cavernosum during any sexual stimulus. Nitric oxide, in turn. , it activates an enzyme called guanylate cyclase which causes an increase in the levels of cyclic guanosine monophosphate (cGMP), causing smooth muscle relaxation in the corpus cavernosum and thus allowing large amounts of blood to flow into the penis.
Vardenafil is a type 5 phosphodiesterase (PED5) inhibitor, specific for cGMP (cyclic guanosine monophosphate); type 5 phosphodiesterase is mainly localized in the smooth muscle of the vessels of the corpora cavernosa of the penis and is the enzyme responsible for the degradation of cGMP (cyclic guanosine monophosphate); therefore the inhibition of this enzyme by vardenafil leads to a higher concentration of cGMP (cyclic guanosine monophosphate), consequently allows greater vasodilation, giving a more vigorous erection through the greater blood supply in the corpora cavernosa.
In conclusion we can say that vardenafil, being a type 5 phosphodiesterase inhibitor specific for cGMP (cyclic guanosine monophosphate), does not have a direct relaxing effect, but effectively increases the muscle relaxant effect of nitric oxide (NO). on the smooth muscle of the corpus cavernosum of the penis: when the NO / cGMP pathway is activated, as occurs during sexual stimulation, the inhibition of phosphodiesterase type 5 by vardenafil considerably increases the level of cGMP in the corpus cavernosum.
Vardenafil, like other phosphodiesterase type 5 inhibitor drugs and erectile dysfunction treatments in general, has also conquered all the internet pages, most of which offer a very simple way to get the drug, even offering to ship the drug directly. to the home of the customer concerned. Many people are attracted by the possibility of obtaining vardenafil via the internet, seduced by apparently low prices and the desire to solve their problem without consulting a doctor, thus avoiding possible embarrassment. This is obviously an attitude absolutely wrong, because the doctor is indispensable in the evaluation of the problem.For example, erectile dysfunction can be of a different nature and the drug is not necessary.
Vardenafil and other type 5 phosphodiesterase enzyme inhibitors are often sold in much lower or higher doses than recommended therapeutics, and / or in preparations that combine multiple "" miracle "drugs: similar cocktails are advertised by managers. of these websites as "" very powerful "" or "" infallible ""; in reality, such doses can seriously harm the patient's health by increasing the "entity and" incidence of the drug's side effects. Therefore, the purchase of vardenafil via the Internet without first consulting a doctor is strongly discouraged. If vardenafil is being taken by people of advanced age or who have cardiovascular disorders, a thorough and preventive medical assessment should also be performed to ensure that the administration of vardenafil does not lead to any serious side effects and does not interfere with the clinical picture of the patient.
Other articles on "Vardenafil"
- Vardenafil: dosage and method of use
- Vardenafil: contraindications and warnings
- Vardenafil: interaction with other drugs
- Vardenafil: side effects