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Chemical Compound Review

Levitra     3-[2-ethoxy-5-(4- ethylpiperazin-1...

Synonyms: Vivanza, Vardenafil, CHEMBL1520, SureCN5772, Levitra (TN), ...
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Disease relevance of Levitra


Psychiatry related information on Levitra

  • The feasibility of these enzymes as drug targets is exemplified by the commercial and clinical successes of the erectile dysfunction drugs, sildenafil (Viagra), tadalafil (Cialis), and vardenafil (Levitra) [5].
  • After 12 weeks, vardenafil-treated patients with severe ED showed a significant improvement in their self-esteem compared with patients receiving placebo (change from baseline -1.51 vs. 3.54, respectively, P = 0.036) [6].
  • All 3 doses of vardenafil were superior to placebo across all primary efficacy variables and all study time points in a broad range of patients with ED, regardless of etiology or severity [7].

High impact information on Levitra

  • It is concluded that Gln(817) is a positive determinant for PDE5 affinity for cGMP and several inhibitors; Gln(775), which perhaps restricts rotation of Gln(817) side chain, is critical for cGMP affinity but has no measurable effect on affinity for cAMP, sildenafil, or vardenafil [8].
  • Digital blood flow was measured by laser-Doppler flowmetry at room temperature and during the cold-exposure test before medical treatment, 1 hour after the initial intake, and after 2 weeks of continuous treatment (10 mg twice a day) with the novel phosphodiesterase type 5 inhibitor vardenafil [9].
  • Sildenafil and tadalafil, but not vardenafil, caused a significant reduction in the pulmonary to systemic vascular resistance ratio [10].
  • At peak exercise, vardenafil 10 mg did not alter blood pressure, heart rate, or rate-pressure product relative to placebo [11].
  • CONCLUSIONS: Vardenafil 10 mg did not impair the ability of patients with stable CAD to exercise at levels equivalent or greater than that attained during sexual intercourse (average of 2.5 to 3.3 METS) [11].

Chemical compound and disease context of Levitra


Biological context of Levitra


Anatomical context of Levitra


Associations of Levitra with other chemical compounds


Gene context of Levitra

  • The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil [20].
  • In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM [20].
  • Of the currently available treatment options for ED, the most commonly prescribed therapies are oral PDE5 inhibitors, which include sildenafil citrate (Viagra, Pfizer Inc), tadalafil (Cialis, Lilly ICOS), and vardenafil (Levitra, Bayer) [25].
  • The hypothesis was tested that vardenafil, a PDE5 inhibitor, specifically enhances coronary vasodilation during acidosis [15].
  • METHODS: In this double-blind, crossover, single-dose multicenter study, 41 men with reproducible stable exertional angina due to ischemic CAD received vardenafil 10 mg or placebo, followed by ETT (5 to 10 metabolic equivalents [METS], Bruce protocol) 1 h postdose [11].

Analytical, diagnostic and therapeutic context of Levitra


  1. Sildenafil and vardenafil, types 5 and 6 phosphodiesterase inhibitors, induce caspase-dependent apoptosis of B-chronic lymphocytic leukemia cells. Sarfati, M., Mateo, V., Baudet, S., Rubio, M., Fernandez, C., Davi, F., Binet, J.L., Delic, J., Merle-Beral, H. Blood (2003) [Pubmed]
  2. Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development. Wang, H., Liu, Y., Huai, Q., Cai, J., Zoraghi, R., Francis, S.H., Corbin, J.D., Robinson, H., Xin, Z., Lin, G., Ke, H. J. Biol. Chem. (2006) [Pubmed]
  3. Vardenafil: a review of its use in erectile dysfunction. Keating, G.M., Scott, L.J. Drugs (2003) [Pubmed]
  4. Sildenafil and vardenafil but not nitroglycerin limit myocardial infarction through opening of mitochondrial K(ATP) channels when administered at reperfusion following ischemia in rabbits. Salloum, F.N., Takenoshita, Y., Ockaili, R.A., Daoud, V.P., Chou, E., Yoshida, K., Kukreja, R.C. J. Mol. Cell. Cardiol. (2007) [Pubmed]
  5. Cyclic nucleotide phosphodiesterases: molecular regulation to clinical use. Bender, A.T., Beavo, J.A. Pharmacol. Rev. (2006) [Pubmed]
  6. Efficacy of vardenafil and influence on self-esteem and self-confidence in patients with severe erectile dysfunction. Martin-Morales, A., Meijide, F., García, N., Artes, M., Muñoz, A. The journal of sexual medicine (2007) [Pubmed]
  7. Sustained efficacy and tolerability of vardenafil, a highly potent selective phosphodiesterase type 5 inhibitor, in men with erectile dysfunction: results of a randomized, double-blind, 26-week placebo-controlled pivotal trial. Hellstrom, W.J., Gittelman, M., Karlin, G., Segerson, T., Thibonnier, M., Taylor, T., Padma-Nathan, H. Urology (2003) [Pubmed]
  8. Phosphodiesterase-5 Gln817 is critical for cGMP, vardenafil, or sildenafil affinity: its orientation impacts cGMP but not cAMP affinity. Zoraghi, R., Corbin, J.D., Francis, S.H. J. Biol. Chem. (2006) [Pubmed]
  9. Phosphodiesterase type 5 inhibition is a novel therapeutic option in Raynaud disease. Caglayan, E., Huntgeburth, M., Karasch, T., Weihrauch, J., Hunzelmann, N., Krieg, T., Erdmann, E., Rosenkranz, S. Arch. Intern. Med. (2006) [Pubmed]
  10. Differences in hemodynamic and oxygenation responses to three different phosphodiesterase-5 inhibitors in patients with pulmonary arterial hypertension: a randomized prospective study. Ghofrani, H.A., Voswinckel, R., Reichenberger, F., Olschewski, H., Haredza, P., Karadaş, B., Schermuly, R.T., Weissmann, N., Seeger, W., Grimminger, F. J. Am. Coll. Cardiol. (2004) [Pubmed]
  11. The effect of vardenafil, a potent and highly selective phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction, on the cardiovascular response to exercise in patients with coronary artery disease. Thadani, U., Smith, W., Nash, S., Bittar, N., Glasser, S., Narayan, P., Stein, R.A., Larkin, S., Mazzu, A., Tota, R., Pomerantz, K., Sundaresan, P. J. Am. Coll. Cardiol. (2002) [Pubmed]
  12. Interaction between the phosphodiesterase 5 inhibitor, tadalafil and 2 alpha-blockers, doxazosin and tamsulosin in healthy normotensive men. Kloner, R.A., Jackson, G., Emmick, J.T., Mitchell, M.I., Bedding, A., Warner, M.R., Pereira, A. J. Urol. (2004) [Pubmed]
  13. Erectile response to vardenafil in men with a history of nonresponse to sildenafil: a time-from-dosing descriptive analysis. Hatzichristou, D.G., Aliotta, P., Auerbach, S., Barkin, J., Lording, D., Murdock, M., Wilkins, H.J., McBride, T.A., Colopy, M.W., Carson, C.C. Clinical therapeutics. (2005) [Pubmed]
  14. Vardenafil reverses erectile dysfunction induced by paroxetine in rats. Angulo, J., Bischoff, E., Gabancho, S., Cuevas, P., Sáenz de Tejada, I. Int. J. Impot. Res. (2003) [Pubmed]
  15. Vardenafil increases coronary flow response to hypercapnic acidosis in isolated guinea pig heart. Brand, M., Deussen, A. Basic Res. Cardiol. (2007) [Pubmed]
  16. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Blount, M.A., Beasley, A., Zoraghi, R., Sekhar, K.R., Bessay, E.P., Francis, S.H., Corbin, J.D. Mol. Pharmacol. (2004) [Pubmed]
  17. A 46-Amino Acid Segment in Phosphodiesterase-5 GAF-B Domain Provides for High Vardenafil Potency over Sildenafil and Tadalafil and Is Involved in Phosphodiesterase-5 Dimerization. Blount, M.A., Zoraghi, R., Ke, H., Bessay, E.P., Corbin, J.D., Francis, S.H. Mol. Pharmacol. (2006) [Pubmed]
  18. New treatment options for erectile dysfunction in patients with diabetes mellitus. Basu, A., Ryder, R.E. Drugs (2004) [Pubmed]
  19. Relationship Between Vascular Damage Degrees and Endothelial Progenitor Cells in Patients with Erectile Dysfunction: Effect of Vardenafil Administration and PDE5 Expression in the Bone Marrow. Foresta, C., Caretta, N., Lana, A., De Toni, L., Biagioli, A., Vinanzi, C., Ferlin, A. Eur. Urol. (2007) [Pubmed]
  20. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Saenz de Tejada, I., Angulo, J., Cuevas, P., Fernández, A., Moncada, I., Allona, A., Lledó, E., Körschen, H.G., Niewöhner, U., Haning, H., Pages, E., Bischoff, E. Int. J. Impot. Res. (2001) [Pubmed]
  21. Accurate mass measurement using Fourier transform ion cyclotron resonance mass spectrometry for structure elucidation of designer drug analogs of tadalafil, vardenafil and sildenafil in herbal and pharmaceutical matrices. Gratz, S.R., Gamble, B.M., Flurer, R.A. Rapid Commun. Mass Spectrom. (2006) [Pubmed]
  22. Effect of high-fat breakfast and moderate-fat evening meal on the pharmacokinetics of vardenafil, an oral phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction. Rajagopalan, P., Mazzu, A., Xia, C., Dawkins, R., Sundaresan, P. Journal of clinical pharmacology. (2003) [Pubmed]
  23. Simultaneous administration of vardenafil and alcohol does not result in a pharmacodynamic or pharmacokinetic interaction in healthy male subjects. Wensing, G., Bauer, R., Unger, S., Rohde, G., Heinig, R. International journal of clinical pharmacology and therapeutics. (2006) [Pubmed]
  24. Phosphodiesterase 5 in the female pig and human urethra: morphological and functional aspects. Werkström, V., Svensson, A., Andersson, K.E., Hedlund, P. BJU Int. (2006) [Pubmed]
  25. Evaluating preference trials of oral phosphodiesterase 5 inhibitors for erectile dysfunction. Mulhall, J.P., Montorsi, F. Eur. Urol. (2006) [Pubmed]
  26. Efficacy and tolerability of vardenafil in men with mild depression and erectile dysfunction: the depression-related improvement with vardenafil for erectile response study. Rosen, R., Shabsigh, R., Berber, M., Assalian, P., Menza, M., Rodriguez-Vela, L., Porto, R., Bangerter, K., Seger, M., Montorsi, F. The American journal of psychiatry. (2006) [Pubmed]
  27. The oral efficacy of vardenafil hydrochloride for inducing penile erection in a conscious rabbit model. Bischoff, E., Niewoehner, U., Haning, H., Es Sayed, M., Schenke, T., Schlemmer, K.H. J. Urol. (2001) [Pubmed]
  28. Evidence for contamination of herbal erectile dysfunction products with phosphodiesterase type 5 inhibitors. Fleshner, N., Harvey, M., Adomat, H., Wood, C., Eberding, A., Hersey, K., Guns, E. J. Urol. (2005) [Pubmed]
  29. Vardenafil increases penile rigidity and tumescence in men with erectile dysfunction after a single oral dose. Stark, S., Sachse, R., Liedl, T., Hensen, J., Rohde, G., Wensing, G., Horstmann, R., Schrott, K.M. Eur. Urol. (2001) [Pubmed]
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