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1.
Chinese Journal of Cardiology ; (12): 507-512, 2020.
Article in Chinese | WPRIM | ID: wpr-941139

ABSTRACT

Objective: To develope and validate a reliable and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for determination of vardenafil concentration in plasma of rat. Methods: Plasma samples of normal Sprague-Dawley rats were collected. A Phenomenex Synergi Polar-RP 80A column (2.0 mm×50 mm, 4 µm) was used. Column temperature was set at 30 ℃. Mobile phase A was 0.1% formic acid in water; mobile phase B was 0.1% formic acid in acetonitrile. The flow rate was 0.4 ml/minutes. Quantitative determination was performed by electrospray ionization, operating in positive ion multiple reaction monitoring (MRM) mode. Cisapride was used as the internal standard. The feasibility of the method was evaluated by examining its specificity, linearity and quantitative range, precision and accuracy, matrix effects, and stability. Results: Under the selected chromatographic and mass spectrometry conditions, the monitoring ions of vardenafil and internal standard were mass-to-charge ratio(m/z) 489.3/151.2 and 466.4/234.2, the retention times of vardenafil and internal standard were 2.62 and 2.80 minutes, respectively, and the peak shape was satisfactory. The method has good linearity in the concentration range of 0.2-200 ng/ml. The intra-batch precision (%CV) and accuracy (%DEV) of vardenafil were 1.5%-9.7% and -6.8%-6.6%, respectively. The inter-batch precision and accuracy of vardenafil were 3.1% -8.4% and -3.7%-4.6%, respectively. In this sample processing method, the extraction recovery rate of vardenafil was obtained at range of 88.2%-104.6%, which met the requirements for the investigation of extraction recovery rate. In this sample processing method, the normalized matrix factor of each quality control concentration of vardenafil was 1.04, 0.85, and 1.04, and the coefficient of variation (%CV) was in the range of 1.7%-10.7%, which met the requirements for the investigation of matrix effects. Variations of short-term stability, long-term stability, and stability of 4 freeze-thaw cycles of vardenafil was within ±15%, and the coefficient of variation were within 5%. Conclusion: The high performance liquid chromatography-tandem mass spectrometry method established in this study is feasible for the measurement of concentration of vardenafil in rat plasma and this method has good specificity and high accuracy, and can be used to detect the concentration of vardenafil in rat plasma.


Subject(s)
Animals , Rats , Chromatography, Liquid , Feasibility Studies , Rats, Sprague-Dawley , Reproducibility of Results , Sensitivity and Specificity , Tandem Mass Spectrometry , Vardenafil Dihydrochloride
2.
The World Journal of Men's Health ; : 313-321, 2019.
Article in English | WPRIM | ID: wpr-761885

ABSTRACT

PURPOSE: To examine the association between phosphodiesterase type 5 (PDE5) inhibitor use and melanoma by 1) conducting a systematic review of observational studies; and 2) determining if low PDE5A gene expression in human melanoma correlated with decreased overall survival. MATERIALS AND METHODS: A systematic search of observational studies examining the association between PDE5 inhibitor use and melanoma was performed through ClinicalTrials.gov, the Cochrane Library, EMBASE, PubMed, and Web of Science databases, and seven eligible studies were identified. PDE5A gene expression was analyzed with RNA sequencing data from 471 human melanoma samples obtained from The Cancer Genome Atlas. RESULTS: Four studies reported a positive association between PDE5 inhibitor use and melanoma, and three studies found no correlation. RNA sequencing data analysis revealed that under-expression of the PDE5A gene did not impact clinical outcomes in melanoma. CONCLUSIONS: There is currently no evidence to suggest that PDE5 inhibition in patients causes increased risk for melanoma. The few observational studies that demonstrated a positive association between PDE5 inhibitor use and melanoma often failed to account for major confounders. Nonetheless, the substantial evidence implicating PDE5 inhibition in the cyclic guanosine monophosphate (cGMP)-mediated melanoma pathway warrants further investigation in the clinical setting.


Subject(s)
Humans , Gene Expression , Genome , Guanosine Monophosphate , Melanoma , Phosphodiesterase 5 Inhibitors , Sequence Analysis, RNA , Sildenafil Citrate , Statistics as Topic , Tadalafil , Vardenafil Dihydrochloride
3.
Acta cir. bras ; 30(5): 339-344, 05/2015. tab, graf
Article in English | LILACS | ID: lil-747023

ABSTRACT

PURPOSE: To investigate the effect of vardenafil in kidney of rats submitted to acute ischemia and reperfusion. METHODS: Twenty-eight rats were randomly distributed into two groups. Right nephrectomy was performed and the vardenafil group received vardenafil solution (at a concentration of 1 mg/ml in 10 mg/kg) while the control group received 0.9% saline solution (SS) one hour prior to the ligature of the left renal pedicle. After one hour of ischemia, animals were submitted to twenty-four hours of reperfusion, followed by left nephrectomy. The kidney's histological parameters evaluated on the study included vacuolar degeneration and tubular necrosis. Apoptosis was assessed by immunohistochemistry for cleaved caspase-3 using the point-counting and digital methods (Cytophotometry). Also, a biochemical analysis for creatinine was conducted. RESULTS: There were statistically significant differences between groups only with regards to the vacuolar degeneration parameter and to the cleaved caspase-3 digital method. CONCLUSION: Vardenafil showed a protective effect on the kidney of rats subjected to acute ischemia and reperfusion in this model .


Subject(s)
Animals , Male , Imidazoles/therapeutic use , Ischemia/prevention & control , Kidney/blood supply , Kidney/drug effects , /therapeutic use , Piperazines/therapeutic use , Reperfusion Injury/prevention & control , Apoptosis/drug effects , /analysis , Disease Models, Animal , Immunohistochemistry , Kidney/pathology , Random Allocation , Rats, Wistar , Reproducibility of Results , Sulfones/therapeutic use , Time Factors , Treatment Outcome , Triazines/therapeutic use , Vardenafil Dihydrochloride
4.
Chinese Journal of Cancer ; (12): 223-230, 2014.
Article in English | WPRIM | ID: wpr-320550

ABSTRACT

ABCC10, also known as multidrug-resistant protein 7 (MRP7), is the tenth member of the C subfamily of the ATP-binding cassette (ABC) superfamily. ABCC10 mediates multidrug resistance (MDR) in cancer cells by preventing the intracellular accumulation of certain antitumor drugs. The ABCC10 transporter is a 171-kDa protein that is localized on the basolateral cell membrane. ABCC10 is a broad-specificity transporter of xenobiotics, including antitumor drugs, such as taxanes, epothilone B, vinca alkaloids, and cytarabine, as well as modulators of the estrogen pathway, such as tamoxifen. In recent years, ABCC10 inhibitors, including cepharanthine, lapatinib, erlotinib, nilotinib, imatinib, sildenafil, and vardenafil, have been reported to overcome ABCC10-mediated MDR. This review discusses some recent and clinically relevant aspects of the ABCC10 drug efflux transporter from the perspective of current chemotherapy, particularly its inhibition by tyrosine kinase inhibitors and phosphodiesterase type 5 inhibitors.


Subject(s)
Humans , Antineoplastic Agents , Benzamides , Benzylisoquinolines , Drug Resistance, Multiple , Drug Resistance, Neoplasm , Erlotinib Hydrochloride , Imatinib Mesylate , Imidazoles , Multidrug Resistance-Associated Proteins , Piperazines , Purines , Pyrimidines , Quinazolines , Sildenafil Citrate , Sulfonamides , Sulfones , Taxoids , Triazines , Vardenafil Dihydrochloride
5.
The World Journal of Men's Health ; : 18-27, 2014.
Article in English | WPRIM | ID: wpr-55353

ABSTRACT

Phosphodiesterase type 5 (PDE5) inhibitors are the most commonly used treatment for erectile dysfunction (ED). Since the launch of sildenafil, several drugs-including mirodenafil, sildenafil citrate (sildenafil), tadalafil, vardenafil HCL (vardenafil), udenafil, and avanafil-have become available. Mirodenafil is a newly developed pyrrolopyrimidinone compound, which is a potent, reversible, and selective oral PDE5 inhibitor. Mirodenafil was launched in Korea in 2007, and an orally disintegrating film of mirodenafil was developed in 2011 for benefitting patients having difficulty in swallowing tablets. This study aimed to review the pharmacokinetic characteristic profile of mirodenafil and report evidence on its efficacy in the case of ED. In addition, we reviewed randomized controlled studies of mirodenafil's daily administration and efficacy for lower urinary tract symptoms.


Subject(s)
Humans , Male , Citric Acid , Deglutition , Erectile Dysfunction , Korea , Lower Urinary Tract Symptoms , Phosphodiesterase 5 Inhibitors , Tablets , Treatment Outcome , Sildenafil Citrate , Tadalafil , Vardenafil Dihydrochloride
6.
National Journal of Andrology ; (12): 991-995, 2013.
Article in Chinese | WPRIM | ID: wpr-268017

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate phosphodiesterase type 5 (PDE5) inhibitors in the management of temporary penile erectile dysfunction (ED) in patients undergoing assisted reproductive technology (ART).</p><p><b>METHODS</b>This study included 75 male patients that experienced ejaculation failure due to temporary ED during ART treatment. We treated the patients with PDE5 inhibitors sildenafil, tadanafil and vardenafil, and then evaluated the hardness of penile erection using Erection Hardness Score (EHS) and analyzed the end-point efficacy.</p><p><b>RESULTS</b>Sildenafil was administered to 28 of the patients, tadanafil to 25, and vardenafil to 22. Of the total number of patients, 61 (81.3%) achieved effective erection, but no significant differences were observed in the rate of effectiveness among the sildenafil (24 cases, 85.7%), tadanafil (20 cases, 80.0%) and vardenafil (17 cases, 77.3%) groups (P > 0.05). After medication, 53 (70.7%) of the patients successfully ejaculated, but there were no remarkable differences in the success rate among the sildenafil (21 cases, 75.0%), tadanafil (17 cases, 68.0%) and vardenafil (15 cases, 68.2%) groups (P > 0.05). Of the 75 patients, 37 received the recommended initial dose and 38 the maximum recommended dose of PDE5 inhibitors, but no significant differences were found in the rate of successful sperm retrieval between the former (28 cases, 75.7%) and the latter group (25 cases, 65.8%) (P > 0.05). Mild adverse events, including transient flush and dizziness, occurred in 5 cases (6.7%).</p><p><b>CONCLUSION</b>PDE5 inhibitors can help temporary ED patients to achieve penile erection and ejaculation during ART treatment.</p>


Subject(s)
Humans , Male , Ejaculation , Erectile Dysfunction , Drug Therapy , Imidazoles , Therapeutic Uses , Phosphodiesterase 5 Inhibitors , Therapeutic Uses , Piperazines , Therapeutic Uses , Purines , Therapeutic Uses , Reproductive Techniques, Assisted , Sildenafil Citrate , Sulfonamides , Therapeutic Uses , Sulfones , Therapeutic Uses , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride
7.
The World Journal of Men's Health ; : 31-35, 2013.
Article in English | WPRIM | ID: wpr-186056

ABSTRACT

Currently, phosphodiesterase type 5 (PDE5) inhibitors are the initial treatment option for erectile dysfunction. The reported efficacy of PDE5 inhibitors is about 70%, although it is significantly lower in difficult-to-treat subpopulations. Treatment failures might be due to the severity of the underlying pathophysiology, improper use of medication, unrealistic patient expectations, difficult relationship dynamics, severe performance anxiety, and other psychological problems. Physicians must address these issues to identify true treatment failures attributable to the drugs. This article discusses factors that might affect the response to PDE5 inhibitors and develops a strategy to maximize the overall efficacy of PDE5 inhibitors in initial non-responders to PDE5 inhibitors.


Subject(s)
Humans , Male , Carbolines , Erectile Dysfunction , Imidazoles , Performance Anxiety , Phosphodiesterase 5 Inhibitors , Piperazines , Purines , Sulfones , Treatment Failure , Triazines , Sildenafil Citrate , Tadalafil , Vardenafil Dihydrochloride
8.
Journal of Neurogastroenterology and Motility ; : 399-405, 2012.
Article in English | WPRIM | ID: wpr-21434

ABSTRACT

BACKGROUND/AIMS: To evaluate the effects of the phosphodiesterase type 5 (PDE5) inhibitor vardenafil on esophageal function, including bolus transit, using multichannel intraluminal impedance and esophageal manometry (MII-EM). METHODS: Sixteen healthy volunteers (15 men) underwent an MII-EM study including 10 liquid swallows and 10 viscous swallows in a seated position after fasting. Then, each subject was asked to ingest 50 mL distilled water or 10 mg vardenafil dissolved in 50 mL water, in a double-blind manner. After 25 minutes, the MII-EM study was repeated. RESULTS: Eight men received vardenafil and eight subjects received water. Resting and residual lower esophageal sphincter pressures differed significantly only in the vardenafil group (from 18 +/- 6.7 to 6.6 +/- 5.3 mmHg, P < 0.001 and from 4.9 +/- 2.6 to 2.1 +/- 3.6 mmHg, P = 0.006, respectively). Mean distal esophageal amplitude decreased significantly only in the vardenafil group (from 86.7 +/- 41.6 to 34.0 +/- 38.0 mmHg, P < 0.05). Complete bolus transits of liquid and viscous meals decreased significantly only after vardenafil ingestion (from 80.2% +/- 13.8% to 49.4% +/- 27.9%, P < 0.05 and from 72.8% +/- 33.6% to 21.5% +/- 29.0%, P = 0.01, respectively). CONCLUSIONS: Vardenafil decreased esophageal bolus transit in the seated position, despite decreased lower esophageal sphincter pressure.


Subject(s)
Humans , Male , Eating , Electric Impedance , Esophageal Sphincter, Lower , Fasting , Imidazoles , Manometry , Meals , Piperazines , Sulfones , Swallows , Triazines , Water , Vardenafil Dihydrochloride
9.
National Journal of Andrology ; (12): 322-324, 2011.
Article in Chinese | WPRIM | ID: wpr-266168

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the impact of penile surgery on the erectile function of the patient and to evaluate the role of small-dose vardenafil in restoring the impaired penile erection.</p><p><b>METHODS</b>Sixty cases of penile cavernosum surgery were equally and randomly divided into a vardenafil and a control group, the former treated 5 - 7 days after surgery with 10 mg vardenafil every other day, while the latter given vitamin E at 100 mg once a day, both for 12 weeks. The penile erectile function of the patients was evaluated with the IIEF-5 questionnaire before surgery and at 3 and 6 months after vardenafil medication.</p><p><b>RESULTS</b>The mean IIEF-5 scores of the vardenafil group were 18.83 +/- 2.98 and 20.13 +/- 2.98 at 3 and 6 months after vardenafil medication, significantly higher than 14.21 +/- 3.62 before surgery (P > 0.05), while that of the control group was significantly decreased at 3 months as compared with the preoperative score (13.38 +/- 2.82 versus 15.80 +/- 3.02, P < 0.05). The vardenafil group showed the highest IIEF-5 score after surgery (P < 0.05).</p><p><b>CONCLUSION</b>Long-term administration of small-dose vardenafil after penile surgery helps to restore and maintain penile erectile function.</p>


Subject(s)
Adult , Humans , Male , Middle Aged , Erectile Dysfunction , Drug Therapy , Imidazoles , Therapeutic Uses , Penile Erection , Penis , General Surgery , Piperazines , Therapeutic Uses , Postoperative Period , Recovery of Function , Sulfones , Therapeutic Uses , Treatment Outcome , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride , Vasodilator Agents , Therapeutic Uses
10.
International Neurourology Journal ; : 216-221, 2011.
Article in English | WPRIM | ID: wpr-173980

ABSTRACT

PURPOSE: We analyzed the prescriptions of alpha-blockers and phosphodiesterase 5 inhibitors (PDE5Is) in the urology department as well as in other departments of the general hospital. METHODS: We investigated the frequency of prescription of alpha-blockers and PDE5Is from 3 general hospitals from January 1, 2007 to December 31, 2009. For alpha-blockers, data were collected from patients to whom alpha-blockers were prescribed from among patients recorded as having benign prostatic hyperplasia according to the 5th Korean Standard Classification of Diseases. For PDE5Is, data were collected from patients to whom PDE5Is were prescribed by the urology department and by other departments. Alpha-blockers were classified into tamsulosin, alfuzosin, doxazosin, and terazosin, whereas PDE5Is were classified into sildenafil, tadalafil, vardenafil, udenafil, and mirodenafil. RESULTS: Alpha-blockers were prescribed to 11,436 patients in total over 3 years, and the total frequency of prescriptions was 68,565. Among other departments, the nephrology department had the highest frequency of prescription of 3,225 (4.7%), followed by the cardiology (3,101, 4.5%), neurology (2,576, 3.8%), endocrinology (2,400, 3.5%), pulmonology (1,102, 1.6%), and family medicine (915, 1.3%) departments in order. PDE5Is were prescribed to 2,854 patients in total over 3 years, and the total frequency of prescriptions was 10,558. The prescription frequency from the urology department was 4,900 (46.4%). Among other departments, the endocrinology department showed the highest prescription frequency of 3,488 (33.0%), followed by the neurology (542, 5.1%), cardiology (467, 4.4%), and family medicine (407, 3.9%) departments in order. CONCLUSIONS: A high percentage of prescriptions of alpha-blockers and PDE5Is were from other departments. For more specialized medical care by urologists is required in the treatment of lower urinary tract symptoms and erectile dysfunction.


Subject(s)
Humans , Male , Adrenergic alpha-1 Receptor Antagonists , Carbolines , Cardiology , Cyclic Nucleotide Phosphodiesterases, Type 5 , Doxazosin , Endocrinology , Erectile Dysfunction , Hospitals, General , Imidazoles , Lower Urinary Tract Symptoms , Nephrology , Neurology , Phosphodiesterase 5 Inhibitors , Piperazines , Prazosin , Prescriptions , Prostatic Hyperplasia , Pulmonary Medicine , Purines , Pyrimidines , Quinazolines , Sildenafil Citrate , Sulfonamides , Sulfones , Tadalafil , Triazines , Urology , Vardenafil Dihydrochloride
11.
National Journal of Andrology ; (12): 1092-1096, 2011.
Article in Chinese | WPRIM | ID: wpr-239028

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate the efficacy and safety of long-term on-demand use of vardenafil in the treatment of erectile dysfunction (ED).</p><p><b>METHODS</b>We conducted a questionnaire investigation among 891 ED patients treated by on-demand use of oral vardenafil at 20 mg every 3 days from March 2007 to January 2010, covering the general information of the patients, their need for and attitudes towards the treatment, clinical efficacy and adverse events of the drug, and satisfaction of the patients and their partners after 12 weeks of treatment.</p><p><b>RESULTS</b>Treatment and follow-up were completed in 700 patients, of whom 504 (72%) achieved sufficient hardness and duration of penile erection and overall sexual satisfaction, 84 (12%) admitted to improvement of erectile hardness and duration but not adequate satisfaction, and the other 112 (16%) experienced no significant changes. Significant differences were found in IIEF-5 scores, Rigiscan test results and partners TSS scores before and after the treatment (P < 0.05). Most frequent adverse events included flushing (15%), dizziness and headache (10%), dyspepsia (3%), and nasal congestion (1%).</p><p><b>CONCLUSION</b>Long-term on-demand use of oral vardenafil, in addition to its safety and good tolerance, can effectively improve the erectile function of ED patients, their success rate of sexual intercourse, and overall quality of sexual life.</p>


Subject(s)
Adult , Humans , Male , Young Adult , Erectile Dysfunction , Drug Therapy , Follow-Up Studies , Imidazoles , Therapeutic Uses , Piperazines , Therapeutic Uses , Sulfones , Therapeutic Uses , Treatment Outcome , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride , Vasodilator Agents , Therapeutic Uses
12.
National Journal of Andrology ; (12): 572-575, 2010.
Article in Chinese | WPRIM | ID: wpr-252781

ABSTRACT

Sociopsychological factors play a critical role in the pathogenesis of erectile dysfunction (ED). An optimal therapeutic regimen is supposed to bring sociopsychological benefits to both the patients and their partners. Psychological and Interpersonal Relationship Scales (PAIRS) is an effective measure for evaluating the impact of ED on the psychological aspects and interpersonal relationship of the patients and their partners, as well as for predicting the satisfaction of ED patients with the treatment. PAIRS scores on the effects of phosphodiesterase type 5 inhibitors on ED show a significant decrease in sexual activity-related time concerns of the patients treated with tadalafil, as compared with those medicated with sildenafil or vardenafil. This also underlies the preference of the patients and their partners for tadalafil in clinical practice. The drug attribute associated with the decreased time concerns is the long and outstanding efficacy of tadalafil for up to 36 hours.


Subject(s)
Female , Humans , Male , Carbolines , Therapeutic Uses , Erectile Dysfunction , Drug Therapy , Psychology , Imidazoles , Therapeutic Uses , Interpersonal Relations , Phosphodiesterase Inhibitors , Therapeutic Uses , Piperazines , Therapeutic Uses , Purines , Therapeutic Uses , Sildenafil Citrate , Sulfones , Therapeutic Uses , Tadalafil , Time Factors , Treatment Outcome , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride
13.
National Journal of Andrology ; (12): 856-859, 2010.
Article in Chinese | WPRIM | ID: wpr-294986

ABSTRACT

<p><b>OBJECTIVE</b>To study the clinical efficacy of vardenafil on erectile dysfunction (ED) patients with kidney-yang deficiency, kidney-yin deficiency or liver-qi stasis.</p><p><b>METHODS</b>Based on the syndromes of Traditional Chinese Medicine, 124 ED patients were divided into Groups A (kidney-yang deficiency, n=44), B (kidney-yin deficiency, n=41) and C (liver-qi stasis, n = 39). All the patients were treated with vardenafil at 5 mg daily for 8 weeks, and the therapeutic effects were evaluated by comparing the scores on IIEF-5 and Erection Quality Scale (EQS) before and after the treatment.</p><p><b>RESULTS</b>After vardenafil treatment, the IIEF-5 and EQS scores of the ED patients were markedly increased, with statistically significant differences among the three groups (P < 0.01). The success rate of sexual intercourse was significantly improved in Groups A, B (P < 0.01) and C (P < 0.05). And the hardness of penile erection was enhanced by 81.82%, 73.17% and 43.59% respectively in the three groups of patients.</p><p><b>CONCLUSION</b>Vardenafil is more effective for ED patients with kidney-yang or kidney-yin deficiency than for those with liver-qi stasis.</p>


Subject(s)
Adult , Humans , Male , Middle Aged , Erectile Dysfunction , Drug Therapy , Imidazoles , Therapeutic Uses , Piperazines , Therapeutic Uses , Sulfones , Therapeutic Uses , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride , Vasodilator Agents , Therapeutic Uses , Yang Deficiency , Drug Therapy , Yin Deficiency , Drug Therapy
14.
International Neurourology Journal ; : 213-219, 2010.
Article in English | WPRIM | ID: wpr-174466

ABSTRACT

PURPOSE: Oxytocin is associated with the ability to form normal social attachments. c-Fos is an immediate early gene whose expression is used as a marker for stimulus-induced changes in neurons. The effect of phosphodiesterase-5 (PDE-5) inhibitors on oxytocin activation in the brain without sexual stimuli has not yet been reported. In the present study, we investigated the effects of vardenafil on oxytocin and c-Fos expression in the paraventricular nucleus (PVN) of conscious rats. METHODS: Male Sprague-Dawley rats weighing 300+/-10 g were divided into 6 groups (n=5 in each group): the control group, the 1-day-0.5 mg/kg, the 1-day-1 mg/kg, the 1-day-2 mg/kg, the 3-day-1 mg/kg, and the 7-day-1 mg/kg vardenafil administration group. The experiment was conducted without sexual stimulation. Vardenafil was orally administered. The animals in the control group received an equivalent amount of distilled water orally. The expression of oxytocin and c-Fos in the PVN was detected by immunohistochemistry. RESULTS: Oxytocin expression in the PVN was increased by 1 day administration of 2 mg/kg vardenafil, and this effect of vardenafil appeared in a duration-dependent manner. c-Fos in the oxytocin neurons of the PVN was increased by 1 day administration of 2 mg/kg vardenafil, and this effect of vardenafil also appeared in a duration-dependent manner. These results showed that vardenafil augments the expression of oxytocin with activation of oxytocin neurons in the PVN. CONCLUSIONS: In this study, we showed that the PDE-5 inhibitor, vardenafil directly enhances oxytocin expression and also activates oxytocin neurons in the PVN, which indicates that vardenafil may exert positive effects on affiliation behavior and social interaction.


Subject(s)
Animals , Humans , Male , Rats , Brain , Cyclic Nucleotide Phosphodiesterases, Type 5 , Imidazoles , Interpersonal Relations , Neurons , Oxytocin , Paraventricular Hypothalamic Nucleus , Piperazines , Rats, Sprague-Dawley , Sulfones , Triazines , Water , Vardenafil Dihydrochloride
15.
National Journal of Andrology ; (12): 1035-1038, 2009.
Article in Chinese | WPRIM | ID: wpr-252835

ABSTRACT

In recent years, more and more attention has been drawn to the role of phosphodiesterase 5 (PDE5) in penile erection. The cyclic nucleotide (cGMP) signaling pathway mediates the smooth-muscle relaxing effect of nitric oxide necessary for normal erectile function. Down-regulation of this pathway is the pathological pivot of many forms of erectile dysfunction (ED) and leads to the development of some chronic diseases. Therapeutic outcomes have shown that vardenafil is effective and safe in the treatment of ED associated with dyslipidemia, hypertension, depression, diabetes, radical retropubic prostatectomy, spinal cord injury, sildenafil failure, renal transplantation, chronic prostatitis and that accompanied by premature ejaculation. Vardenafil provides a reasonable therapeutic alternative for these refractory ED patients. In addition, vardenafil can prolong erectile duration of ED patients.


Subject(s)
Humans , Male , Cyclic Nucleotide Phosphodiesterases, Type 5 , Therapeutic Uses , Erectile Dysfunction , Drug Therapy , Imidazoles , Therapeutic Uses , Phosphodiesterase Inhibitors , Therapeutic Uses , Piperazines , Therapeutic Uses , Sulfones , Therapeutic Uses , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride , Vasodilator Agents , Therapeutic Uses
16.
Korean Journal of Andrology ; : 218-222, 2008.
Article in Korean | WPRIM | ID: wpr-152750

ABSTRACT

PURPOSE: After the market launch of multiple phosphodiesterase type 5 inhibitors (PDE5Is), a considerable amount of information has emerged regarding the efficacy and the time of initiation of these drugs. In clinical situations, however, many patients with erectile dysfunction (ED) have complained about the onset of erection occurring later than expected or desired. We therefore studied the time course for initiating an erection after usage of PDE5Is. MATERIALS AND METHODS: One hundred forty-one patients who were medicated with PDE5Is > 4 times in the most recent 3 months were included for study. The patients were divided into 3 groups: sildenafil (n=51), vardenafil (n=51), and tadalafil (n=39). The choice of PDE5I was made according to the patient's and/or doctor's preferences. Regardless of the type of drug selected, the patients were recommended to have sexual stimulation 15 minutes after taking the medication. RESULTS: The onset of action of the 3 drug groups were significantly different (sildenafil, 57.0+/-38.5 min; tadalafil, 79.5+/-50.6 min; and vardenafil, 44.4+/-26.6 min; p<0.05). Psychogenic causes of ED resulted in a shorter PDE5I onset of action than organic causes of ED. Other factors, such as body mass index and international index of erectile function erectile function domain score, were shown not to differ with respect to the onset of action of PED5Is. CONCLUSION: In clinical situations, patients need more time for the onset of erections after taking PDE5Is. For restoration of a healthy sexual life, patients needs more time to achieve an erection after taking PDE5Is.


Subject(s)
Humans , Male , Body Mass Index , Carbolines , Erectile Dysfunction , Imidazoles , Phosphodiesterase 5 Inhibitors , Piperazines , Purines , Sulfones , Triazines , Sildenafil Citrate , Tadalafil , Vardenafil Dihydrochloride
17.
Korean Journal of Andrology ; : 49-60, 2008.
Article in Korean | WPRIM | ID: wpr-192850

ABSTRACT

The phosphodiesterase type-5 inhibitors (PDE5-Is) sildenafil, vardenafil and tadalafil are widely used as first-line therapy for erectile dysfunction (ED). Since the approval of sildenafil in 1998, more than 40 million men worldwide have been successfully treated with PDE5-Is. Pharmacologically, the proven safety and high tolerance of PDE5-Is is an attractive tool to investigate further physiological functions of PDE5, for example the modulation of intracellular cyclic GMP (cGMP) pools. As cGMP is a key component of intracellular signaling this may provide novel therapeutic opportunities beyond ED even for indications in which chronic administration is necessary. The approval of sildenafil for the treatment of pulmonary hypertension in 2005 was a notable success in this area of research. A number of other potential new indications are currently in various phases of preclinical research and development. In recent years, extensive but very heterogeneous information has been published in this field. The aim of this review is to summarize existing preclinical and clinical knowledge and critically discuss the evidence to support potential future indications for PDE5 inhibitors.


Subject(s)
Humans , Male , Carbolines , Cyclic GMP , Cyclic Nucleotide Phosphodiesterases, Type 5 , Erectile Dysfunction , Hypertension, Pulmonary , Imidazoles , Piperazines , Purines , Sulfones , Triazines , Sildenafil Citrate , Tadalafil , Vardenafil Dihydrochloride
18.
Korean Journal of Urology ; : 641-646, 2008.
Article in Korean | WPRIM | ID: wpr-198667

ABSTRACT

PURPOSE: To clarify whether vardenafil can be used as a substitute for intracavernosal injection as a method of induction of penile erection, we compared the outcome of penile duplex Doppler ultrasonography using both methods in the same patient with erectile dysfunction. MATERIALS AND METHODS: A total of 23 patients underwent penile duplex ultrasonography twice with a one week interval between procedures. Twelve were randomly selected for intracavernosal injection first with prostaglandin E1(PGE1) 20microgram and the remaining 11 were initially treated with oral vardenafil 20mg 1 hour before the Doppler study and in addition had visual sexual stimulation using a head-mounted display during the study. The peak systolic velocity(PSV), end diastolic velocity(EDV) and the degree of maximum erectile response were measured and compared between the two groups. RESULTS: Measurements from the PGE1 treatment were not significantly different from those with the vardenafil treatment. The percentage of compatibility between the two methods with regard to hemodynamic diagnosis and pharmaceutical erectile response was as high as 83%(19 of 23) and 91%(21 of 23), respectively. Both methods were tolerable and safe without severe complications. However, in 4 patients where the diagnosis was uncertain, the injection method provided a more accurate interpretation of the penile vascular status with duplex ultrasonography. CONCLUSIONS: These results suggest that oral vardenafil can be used as an initial method for inducing penile erection when assessing erectile dysfunction with penile duplex Doppler ultrasonography in selected patients with erectile dysfunction.


Subject(s)
Humans , Male , Alprostadil , Erectile Dysfunction , Hemodynamics , Imidazoles , Penile Erection , Phosphodiesterase Inhibitors , Piperazines , Sulfones , Triazines , Ultrasonography, Doppler, Duplex , Vardenafil Dihydrochloride
19.
Asian Journal of Andrology ; (6): 495-502, 2008.
Article in English | WPRIM | ID: wpr-359934

ABSTRACT

<p><b>AIM</b>To evaluate the efficacy and tolerability of vardenafil, a phosphodiesterase type-5 (PDE-5) inhibitor, in men of Asian ethnicity with erectile dysfunction (ED).</p><p><b>METHODS</b>In this prospective, double-blind, multinational study, Asian men were randomized to receive vardenafil (10 mg) or placebo (4:1 ratio) for 12 weeks. The primary efficacy variables were the International Index of Erectile Function erectile function domain (IIEF-EF), and Sexual Encounter Profile (SEP) questions related to penetration and intercourse completion. Significant mean improvements were required in all three measures to show positive benefits of vardenafil treatment. Secondary efficacy variables included the Global Assessment Question (GAQ) on erection improvement.</p><p><b>RESULTS</b>Least-squares mean baseline IIEF-EF domain scores (vardenafil 14.6, placebo 13.4) were consistent with moderate ED. After 12 weeks, vardenafil treatment was associated with significant increases from the baseline in IIEF-EF domain scores compared with the placebo (22.4 vs. 14.3; P<0.001). Vardenafil was associated with significant improvements from baseline in least squares (LS) mean success rates for SEP-2 (vardenafil 82.2 vs. placebo 43.6; P<0.001) and SEP-3 (vardenafil 66.1 vs. placebo 24.0; P<0.001). Positive GAQ responses were reported by 81.8% of vardenafil recipients vs. 24.3% of placebo recipients. Adverse events were reported by 25.4% of the vardenafil group, the majority mild and transient.</p><p><b>CONCLUSION</b>Vardenafil (10 mg) is a highly effective and well-tolerated treatment for moderate ED in Asian men. These results add to the increasing amount of data demonstrating the safety and efficacy of vardenafil for the treatment of ED in a range of patient populations.</p>


Subject(s)
Adult , Aged , Humans , Male , Middle Aged , Double-Blind Method , Erectile Dysfunction , Drug Therapy , Imidazoles , Therapeutic Uses , Phosphodiesterase Inhibitors , Therapeutic Uses , Piperazines , Therapeutic Uses , Prospective Studies , Sulfones , Therapeutic Uses , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride
20.
National Journal of Andrology ; (12): 737-739, 2008.
Article in Chinese | WPRIM | ID: wpr-309802

ABSTRACT

<p><b>OBJECTIVE</b>To observe the efficacy and safety of vardenafil in the treatment of erectile dysfunction (ED) in aged men with diabetes mellitus (DM).</p><p><b>METHODS</b>One hundred outpatients with diagnosed ED (40 diabetic and 60 non-diabetic) received vardenafil at the initial dose of 20 mg and sustained dose of 10 mg once a week for 8 weeks, and their erectile functions were evaluated by IIEF and EQS.</p><p><b>RESULTS</b>The scores on IIEF and EQS in the diabetic ED group were 18.9 +/- 0.2 and 25.1 +/- 1.4 after the vardenafil treatment, significantly higher than 8.1 +/- 0.5 and 9.1 +/- 1.3 before the treatment (P < 0.01), and the non-diabetic group scored 21.1 +/- 0.2 and 34.2 +/- 1.2 on IIEF and EQS after the treatment, as compared with the statistically lower scores of 10.1 +/- 0.3 and 10.1 +/- 1.7 before it (P < 0.01). The total rate of effectiveness was 65% in the diabetic and 73.30% in the non-diabetic group, with statistical differences (P < 0. 05).</p><p><b>CONCLUSION</b>Vardenafil can significantly improve erectile function and is well tolerated in the aged males with diabetic ED.</p>


Subject(s)
Aged , Humans , Male , Middle Aged , Aging , Physiology , Diabetes Mellitus, Type 2 , Erectile Dysfunction , Drug Therapy , Imidazoles , Therapeutic Uses , Phosphodiesterase Inhibitors , Therapeutic Uses , Piperazines , Therapeutic Uses , Sulfones , Therapeutic Uses , Treatment Outcome , Triazines , Therapeutic Uses , Vardenafil Dihydrochloride
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