Vardenafil
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| Non-proprietary name | Vardenafil | |||||||||||||||||||||
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1 - {[3- (5-Methyl-4-oxo-7-propyl-3,4-dihydroimidazo [5,1- f ] [1,2,4] triazin-2-yl) -4-ethoxyphenyl] sulfonyl } -4-ethylpiperazine ( IUPAC ) |
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| Brief description |
almost colorless solid (vardenafil hydrochloride trihydrate) |
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| Physical state |
firmly |
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| Melting point |
218 ° C (vardenafil hydrochloride trihydrate) |
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Water: 3.5 mg l −1 (25 ° C) |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||||||||
Vardenafil is a drug that is used in the treatment of erectile dysfunction (erectile dysfunction, ED) in men. Vardenafil is orally effective and was launched in 2003 by the German company Bayer HealthCare as a tablet of 5 mg, 10 mg and 20 mg under the trade name Levitra .
Vardenafil belongs to the group of PDE-5 inhibitors . In all EU countries as well as in Liechtenstein , Switzerland and Norway , vardenafil in all available dosage forms (film-coated tablets: 5, 10, 20 mg vardenafil) is subject to prescription.
history
In 1998, sildenafil was the first PDE-5 inhibitor to be approved by the Food and Drug Administration (FDA) in the United States . In the following, further drugs for the drug treatment of erectile dysfunction were developed, which differ in application, tolerability and dosage from their predecessor. Vardenafil was researched and developed by Bayer HealthCare. In March 2003 the active ingredient received approval from the European Commission . Initially, the marketing was carried out jointly by Bayer HealthCare and GlaxoSmithKline , from 2005 Bayer HealthCare took over the rights for most markets outside the USA.
Mechanism of action
The erection is controlled by a balance between two substances in the body. The first substance, cyclic guanosine monophosphate (cGMP), a second messenger , brings about the erection: The smooth muscles in the erectile tissue of the penis relax so that blood can flow into the erectile tissue, which leads to an erection. The second substance, phosphodiesterase type 5 (PDE-5), causes the erection to subside by breaking down the first substance.
If this equilibrium is disturbed, the erection will fail or prematurely. Vardenafil inhibits PDE-5, so that the concentration of the cGMP increases. This results in an erection that lasts long enough for sexual activity to be satisfactorily performed. An erection only takes place when the man is sexually aroused, since only then is the first substance, cGMP, activated in the cells of the erectile tissue.
The effects of vardenafil last up to 12 hours. The tablet can be taken with or without food; the consumption of alcohol does not affect the pharmacokinetic properties of vardenafil.
Studies
The results of a study carried out by Valiquette et al. (2005) showed that thanks to vardenafil, the treated men achieved an erection that was sufficient for sexual intercourse in 87% of the men and led to orgasm in 83% of the cases . A study carried out by Montorsi et al. (2004) shows the rapid onset of effects of vardenafil. The data from this clinical trial show that after taking vardenafil ( 10 mg dose ) some men could get an erection after 10 minutes if they were sexually aroused. Rosen et al. (2004) have shown in their MALES studies that the reliability of the treatment for men with erectile dysfunction is the most important property for a successful ED therapy. The research results of the MALES study confirm that men consider the rapid onset of action of a PDE-5 inhibitor to be more important than the long duration of the drug's effect.
The comparative study CONFIRMED by Rubio-Arioles et al. (2006) compared the effects of vardenafil and sildenafil in 1057 impotent men. In the randomized, double-blind study carried out at different centers , two drugs against erectile dysfunction were compared with each other, with the two groups being given either sildenafil or vardenafil first. It turned out that both active ingredients are equally well tolerated. A significant majority of men reported more successfully completed sexual intercourse and better sexual intercourse satisfaction with vardenafil than with the active ingredient sildenafil. Basu & Ryder (2004) provide an overview of the treatment options for ED in diabetes patients.
Risks and Side Effects
Contraindications
Simultaneous intake of vardenafil with drugs containing nitrite or NO donors (including the scene drugs poppers ) is contraindicated. The combined effect on blood pressure threatens an acute, life-threatening drop in blood pressure.
Combinations with strong CYP-3A4 inhibitors such as HIV protease inhibitors or oral conazoles are contraindicated. Simultaneous administration of alpha blockers should be avoided (with the exception of tamsulosin ).
Apart from these contraindications, its use in patients with coronary artery disease poses a risk because sexual activity can put a lot of stress on the circulation.
Interactions
Grapefruit juice should not be taken at the same time as vardenafil, as this can affect the usual effects of vardenafil. Vardenafil can be taken with or without food. However, the effect can be delayed if a meal is difficult to digest or is extremely high in fat.
Side effects
The clinical studies as part of the approval process and monitoring show that vardenafil is well tolerated. The side effects noted were short-lived and mild to moderate in intensity. The most commonly reported side effects of vardenafil were headache , facial flushing, indigestion and rhinitis (inflammation of the lining of the nose) and dizziness . Rare and occasional side effects can also manifest themselves.
Health insurance and reimbursement
In the vast majority of cases, patients have to pay for the drug costs of Vardenafil themselves, as these are not covered by health insurance companies.
In Germany, the Social Security Code (Section 34 (1) SGB V, sentence 7) has excluded from payment by the health insurance companies since January 1, 2004 those medicinal products which are used to improve the quality of life. This also includes drugs used to treat erectile dysfunction. The cause of the fault is irrelevant. An exception is not provided.
In Switzerland, medication is paid for by the compulsory health insurances if the effectiveness has been scientifically proven in accordance with Art. 32–34 of the Health Insurance Act (KVG) , the treatment is appropriate and economical and the Federal Council or the responsible office does not rule out the assumption of the cost of the service.
In Austria the provisions in §116ff. of the General Social Insurance Act (ASVG) . In principle, the costs are only reimbursed if an illness is treated.
Individual evidence
- ^ A b The Merck Index : An Encyclopedia of Chemicals, Drugs, and Biologicals. 14th edition. Merck & Co., Whitehouse Station, NJ, USA, 2006, ISBN 0-911910-00-X , p. 1707.
- ↑ a b c Entry on formaldehyde in the Hazardous Substances Data Bank , accessed March 23, 2008.
- ↑ There is not yet a harmonized classification for this substance . A labeling of 2- {2-ethoxy-5 - [(4-ethylpiperazin-1-yl) sulfonyl] phenyl} -5-methyl-7-propylimidazo [5,1-f] [ is shown, which is derived from a self-classification by the distributor 1,2,4] triazin-4 (1H) -one in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on July 10, 2020.
- ↑ L. Valiquette, JM Young, I. Moncada, H. Porst, JG Vézina, BN Stancil, K. Edmunds, F. Montorsi: Sustained Efficacy and Safety of Vardenafil for Treatment of Erectile Dysfunction: A Randomized, Double-Blind, Placebo -Controlled Study. In: Mayo Clin Proc. 80 (10), 2005, pp. 1291-1297.
- ↑ F. Montorsi, H. Padma-Nathan, J. Buvat, H. Schwaibold, M. Beneke, E. Ulbrich, TJ Bandel, H. Porst: Earliest Time to Onset of Action Leading To Successful Sexual Intercourse with Vardenafil Determined in an At-Home Setting: A Randomized, Double-Blind, Placebo-Controlled Trial. In: J Sex Med . 1, 2004, pp. 168-178.
- ↑ RC Rosen, W. Fisher, I. Eardley, C. Niederberger, A. Nadel, M. Sands: The Multinational Men's Attitudes to Life Events and Sexuality (MALES) Study: I. Prevalence of Erectile Dysfunction and Related Health Concerns in the General population. In: Cur Med Res Opin. 20 (5), 2004, pp. 607-614.
- ↑ E. Rubio-Aurioles, H. Porst, I. Eardley, I. Goldstein: Comparing vardenafil and sildenafil in the Treatment of Men with Erectile Dysfunction and Risk Factors for Cardiovascular Disease: A Randomized, Double-blind, pooled crossover study. In: J Sex Med. 3, 2006, pp. 1037-1049.
- ^ Ansu Basu, Robert E J. Ryder: New Treatment Options for Erectile Dysfunction in Patients with Diabetes Mellitus. In: Drugs. 64 (23), 2004, pp. 2667-2688.
Trade names
Levitra ( EU , USA , CDN ), Vivanza (EU), Vilitra
