Erektilní dysfunkce je charakterizována vysokou prevalencí. V rámci farmakoterapie je již po celé čtvrtstoletí využíváno látek navozujících reverzibilní inhibici fosfodiesterázy 5 (PDE-5), důsledkem čehož významně vzrůstá plnění kavernózních těles. Typickým představitelem této lékové skupiny je sildenafil. Vedle klasické tabletové formy může být nově využíván ve formě orálně dispergovatelného filmu.
Erectile dysfunction is characterised by a high prevalence. As part of pharmacotherapy, substances that induce reversible inhibition of phosphodiesterase 5 (PDE-5) have been used for a quarter century. Such an inhibition results in a significantly better filling of the cavernous bodies. A typical representative of this group of drugs is sildenafil. In addition to the classic tablet form, it can be used in the form of an orally dispersible film.
- Keywords
- film - léková forma,
- MeSH
- Erectile Dysfunction * drug therapy MeSH
- Phosphodiesterase 5 Inhibitors * administration & dosage pharmacology therapeutic use MeSH
- Dosage Forms MeSH
- Humans MeSH
- Sildenafil Citrate administration & dosage pharmacology therapeutic use MeSH
- Check Tag
- Humans MeSH
- Male MeSH
6 nečíslovaných stran : ilustrace ; 30 cm
Brožura se zaměřuje na terapii erektilní dysfunkce při depresi pomocí viagry. Určeno odborné veřejnosti.
- Conspectus
- Patologie. Klinická medicína
- NML Fields
- sexuologie
- psychiatrie
- farmacie a farmakologie
- NML Publication type
- brožury
In the search for new biologically active chemotypes, several sildenafil analogs were prepared and characterized. The presence of the pyrazolo[4,3-e][1,2,4]triazine core is thought to be of interest for the enzyme inhibitory activity of these compounds. The designed derivatives incorporating the sildenafil scaffold were assayed as carbonic anhydrase inhibitors, and for their cytotoxic activity against MCF-7 and K562 cell lines. The X-ray analysis of one of these model compounds was performed and its crystal structure is described/compared to that of sildenafil.
- MeSH
- K562 Cells MeSH
- Enzyme Inhibitors chemical synthesis MeSH
- Phosphodiesterase 5 Inhibitors chemical synthesis MeSH
- Crystallography, X-Ray MeSH
- Humans MeSH
- MCF-7 Cells MeSH
- Sildenafil Citrate analogs & derivatives chemical synthesis MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
UV-induced fingerprint spectroscopy (UV-IFS), a new tool in a toolbox of analytical methods, is a powerful technique registering molecule-specific changes of fluorescence induced by UV irradiation. Analysis of fluorescence spectra of a sample prior and after UV irradiation enables an identification of a sample of a drug or pharmaceutics based on a comparison with signals of known standards. Moreover, UV-IFS uncovers the presence of undesired contaminations or intentional changes of the composition. Herein, we employ UV-IFS for qualitative as well as quantitative analysis of common medicines including analgesic/antipyretic (Acetaminophen), antihistamines (Loratadine and Desloratadine), and phosphodiesterase type 5 inhibitors (Tadalafil and Sildenafil citrate). UV irradiation (λem = 254 nm) for 2 - 10 min induced significant changes of fluorescence of the studied samples and according to the unique patterns, the quality and quantity were evaluated. Limits of detection for individual active ingredients were calculated as follows: Acetaminophen = 0.1 μg·mL-1, Loratadine = 0.1 μg·mL-1, Desloratadine = 0.01 μg·mL-1, Tadalafil = 0.04 μg·mL-1 and Sildenafil = 0.2 μg·mL-1. Moreover, genuine and fake CIALIS, VIAGRA and KAMAGRA tablets were reliably identified.
- MeSH
- Loratadine * MeSH
- Acetaminophen * MeSH
- Sildenafil Citrate MeSH
- Spectrum Analysis MeSH
- Tablets MeSH
- Tadalafil MeSH
- Publication type
- Journal Article MeSH
- Keywords
- Avanafil,
- MeSH
- Diagnosis, Differential MeSH
- Erectile Dysfunction * diagnosis drug therapy MeSH
- Phosphodiesterase 5 Inhibitors administration & dosage MeSH
- Premature Ejaculation diagnosis MeSH
- Sexual Dysfunctions, Psychological drug therapy MeSH
- Sildenafil Citrate administration & dosage adverse effects MeSH
- Treatment Outcome MeSH
BACKGROUND: Phosphodiesterase-5A inhibitors (PDE5i) are sometimes used in patients with advanced heart failure with reduced ejection fraction before heart transplant or left ventricular assist device implantation to decrease right ventricular (RV) afterload and mitigate the risk of right heart failure. Conflicting evidence exists regarding the impact of these drugs on RV contractility. The aim of this study was to explore the acute effects of PDE5i on ventricular-vascular coupling and load-independent RV contractility. METHODS: Twenty-two patients underwent right heart catheterization and gated equilibrium blood pool single photon emission computed tomography, before and after 20 mg intravenous sildenafil. Single photon emission computed tomography and right heart catheterization-derived data were used to calculate RV loading and contractility. RESULTS: PDE5i induced a decrease in the right atrial pressure (-43%), pulmonary artery (PA) mean pressure (-26%), and PA wedge pressure (PAWP; -23%), with favorable reductions in pulmonary vascular resistance (-41%) and PA elastance (-40%), and increased cardiac output (+13%) (all P < 0.01). The RV ejection fraction increased with sildenafil (+20%), with no change of RV contractility (P = 0.74), indicating that the improvement in the RV ejection fraction was related to enhanced RV-PA coupling (r = 0.59, P = 0.004) by a decrease in the ventricular load. RV diastolic compliance increased with sildenafil. The decrease in the PAWP correlated with RV end-diastolic volume decrease; no relationship was observed with the change in LV transmural pressure, suggesting decreased pericardial constraint. CONCLUSIONS: Acute PDE5i administration has profound RV afterload-reducing effects, improves the RVEF, decreases RV volumes, and decreases the PAWP, predominantly through relief of pericardial constraint, without effects on RV chamber contractility. These findings support further study of PDE5i in protection of RV function in advanced heart failure with reduced ejection fraction who are at risk of RV failure.
Viagra® (sildenafil citrate) is one of the most sold drugs for erectile dysfunction treatment. The patents of Pfizer Inc. relating to sildenafil expired in Europe and Canada in 2013. At present, a generic sildenafil can be sold all over the world, except for the USA. The district court in Norfolk, VA confirmed that US patent 6,469,012 is valid and enforceable. Moreover, the additional six months of the exclusivity of Viagra® has been granted due to the clinical trial of sildenafil to be used for treatment of paediatric pulmonary arterial hypertension. Therefore the protection of Viagra® for the largest market, USA, remains till April 2020.
- MeSH
- Angina Pectoris drug therapy MeSH
- Time Factors MeSH
- Erectile Dysfunction * drug therapy MeSH
- Drug Industry MeSH
- Drug Evaluation MeSH
- Phosphodiesterase 5 Inhibitors * pharmacology therapeutic use MeSH
- Humans MeSH
- Patents as Topic MeSH
- Piperazines pharmacology therapeutic use MeSH
- Purines pharmacology therapeutic use MeSH
- Sildenafil Citrate MeSH
- Sulfones pharmacology therapeutic use MeSH
- Urological Agents MeSH
- Vasodilator Agents MeSH
- Check Tag
- Humans MeSH
[Sidenafil citrate in control of pulmonary hypertension]
Plicní hypertenze je definována zvýšením středního tlaku v plicnici a zvýšením plicní cévní rezistence. Při specifické léčbě plicní arteriální hypertenze se dosud používaly především látky ze skupiny prostanoidů a antagonistů endotelinových receptorů. Sildenafil je prakticky selektivní inhibitor fosfodiesterázy-5, která se významně vyskytuje v plicním oběhu. Podání sildenafilu vede k inhibici degradace cyklického guanosinmonofosfátu, který je druhým poslem v regulační kaskádě NO. Důsledkem je relaxace buněk hladkého svalstva v cévní stěně a vazodilatace. Sildenafil byl s úspěchem zkoušen v menších nerandomizovaných studiích u různých typů plicní hypertenze a recentně i v randomizované dvojitě slepé klinické studii SUPER-1. Sildenafil bude nepochybně standardní součástí terapeutického schématu u plicní arteriální hypertenze.
Pulmonary hypertension is defined by increased mean tension in the pulmonary artery and elevated pulmonary vascular resistance. So far pulmonary arterial hypertension has been treated primarily with prostanoids and endothelin receptor antagonists. Sildenafil is a selective inhibitor of phosphodiesterase-5, which is abundant in the pulmonary circulation. Sildenafil inhibits the breakdown of cyclic guano sine monophospate serving as a second messenger in the NO regulatory cascade. It induces vascular smooth muscle cell relaxation, thus producing vasodilatation. Sildenafil proved effective in control of pulmonary hypertension of various types when tested in small non-randomized studies and also showed efficacy in a recent randomized double blind clinical trial SUPER-1. Sildenafil will certainly become a standard part of the therapeutic scheme for pulmonary arterial hypertension.
- Keywords
- Revatio,
- MeSH
- Phosphodiesterase Inhibitors administration & dosage pharmacokinetics pharmacology MeSH
- Humans MeSH
- Hypertension, Pulmonary drug therapy MeSH
- Check Tag
- Humans MeSH
- Publication type
- Randomized Controlled Trial MeSH
