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Phosphodiesterases
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
Moritz Helmstädter, Manfred Schubert-Zsilavecz
Sildenafil, the most prominent PDE-Inhibitor, is approved for the treatment of erectile dysfunction (Viagra®) and recently also for pulmonary hypertension (Revatio®). The huge success of PDE5 inhibitors in treating both ED and more recently pulmonary hypertension has been a major contributing factor in expanding pharmaceutical interest in PDEs as promising therapeutic targets (Maurice et al., 2014). Initially, it was not intended for the treatment of erectile dysfunction: Pfizer tried to develop a selective PDE5-inhibitor to promote the nitric oxide (NO)/cGMP pathway for the treatment of angina pectoris and coronary artery disease (Jackson et al., 2005). However, during early phase I trials performed in 1991 and 1992 of sildenafil, the compound revealed an adverse effect that pushed PDE5-Inhibitors into the treatment of erectile dysfunction (Jackson et al., 2005).
N-Heterocycles
Published in Navjeet Kaur, Metals and Non-Metals, 2020
Pyrazolones are used in drugs and are of pharmacological importance, for they exhibit a number of medically useful properties—anti-fungal, anti-microbial, anti-bacterial, anti-mycobacterial, anti-tumor, anti-platelet, anti-inflammatory, anti-depressant, gastric secretion stimulatory as well as anti-filarial. They also work as substrates for pigments, dyes, chelating agents and pesticides [1–3]. Moreover, pyrazolones act as inhibitors against CDK2, with remarkable activity against a number of human tumor cell lines, cannabinoid type-1 (CB1) receptor antagonists, and against tissue-nonspecific alkaline phosphatase (TNAP). In pesticide chemistry, they have come to be used as fungicides, insecticides and herbicides. Pyrazole moiety is a core structure of a wide range of biologically active compounds such as blockbuster drugs like celecoxib and sildenafil (viagra). Whereas celecoxib exhibits anti-arthritic and analgesic activities and is a powerful COX-2 inhibitor, sildenafil (viagra) is a FDA approved drug used to treat erectile dysfunction [4–5].
Cardiovascular PET-CT
Published in Yi-Hwa Liu, Albert J. Sinusas, Hybrid Imaging in Cardiovascular Medicine, 2017
Etienne Croteau, Ran Klein, Jennifer M. Renaud, Manuja Premaratne, Robert A. Dekemp
Nitrates are typically administered immediately prior to CTA for coronary vasodilatation and enhancement of image quality; 400–800 μg of sublingual nitrates is given a few minutes prior to the scan (Abbara et al. 2009). Hypotension is to be expected, but as the procedure is performed in a supine position, this is generally safe. Contraindications to nitrates include erectile dysfunction medications: sildenafil, vardenafil, or tadalafil, or sildenafil taken for pulmonary hypertension. Other contraindications relate to deleterious consequences of systemic vasodilatation. These are inferior wall MI with right ventricle involvement, pronounced hypovolemia, raised intracranial pressure, cardiac tamponade, constrictive pericarditis, severe aortic stenosis, and hypertrophic obstructive cardiomyopathy. Breath-holding at end-inspiration is important with regard to minimizing respiratory motion; explicit instructions with a practice scan are recommended.
Device profile of the Ambicor two-piece inflatable penile prosthesis for treatment of erectile dysfunction: overview of its safety and efficacy
Published in Expert Review of Medical Devices, 2021
Daniel P. Simon, Kevin Alter, Petar Bajic, Laurence A. Levine
Erectile dysfunction (ED), defined as the consistent or recurrent inability to attain and/or maintain penile erection sufficient for sexual satisfaction, is one of the most common forms of male sexual dysfunction, affecting more than half of men over age 40 years [1,2]. The prevalence of ED increases with age, and it affects more than half of men over age 40 years [2]. ED can profoundly influence quality of life for men and their partners and has been associated with anger, depression, and anxiety; in their relationships, men with ED report lower levels of satisfaction as well as decreased levels of physical and emotional intimacy [3,4]. First-line therapy for ED often consists of oral phosphodiesterase-5 inhibitors (PDE5Is), intraurethral or intracavernosal injection therapies, and/or vacuum erection devices (VEDs). In cases of refractory ED, penile prosthesis is considered the optimal method for surgical restoration of erectile function; furthermore, there is growing evidence to suggest certain patients may benefit from earlier placement of penile prosthesis, such as those with combined ED and Peyronie’s disease (PD) requiring surgical management [5,6]. Since Scott et al. introduced the first inflatable penile prosthesis (IPP) in 1973, substantial advances in prosthetic design and materials as well as improvements in surgical technique have led to the emergence of the IPP as the gold standard for the surgical treatment of ED [7].
Hyperlipidemia and male infertility
Published in Egyptian Journal of Basic and Applied Sciences, 2021
Zainab Bubakr Hamad Zubi, Hamad Abdulsalam Hamad Alfarisi
Erectile dysfunction (ED) is the failure to attain or maintain sufficient erection for satisfactory sexual intercourse [32]. There are accumulative evidences suggest the association between dyslipidaemia and ED. Amongst them is the significant correlation between total cholesterol and LDL-c with ED which justifies the importance of hyperlipidemia management in the prevention and treatment of ED [33]. In a study conducted to determine the correlation between abnormal lipid profile and ED, Rao et al., (2005) [34] reported that in 200 male patients abnormal in at least one of the lipid profile parameters, HDL-c and TC/HDL ratio are good predictors for ED. Erectile dysfunction can be attributed to the increase in levels of inflammatory cytokines, which related directly to endothelial dysfunction through nitric oxide pathway [32]. Presence of elevated levels of inflammatory cytokines leads to endothelial dysfunction. Cytokines induce impairment of endothelium-dependent relaxation of vascular beds and reduces nitric oxide release [35]. The endothelial dysfunction and vascular obstruction due to atherosclerosis caused by increased LDL-c and total cholesterol is suggested to be the final pathway leading to the clinical manifestation of ED [36].