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Phosphodiesterase Inhibitor

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141. Off-Label Use of Phosphodiesterase Type 5 Inhibitor Erectile Dysfunction Medication to Enhance Sex Among Gay and Bisexual Men in Australia: Results From the FLUX Study. (PubMed)

Off-Label Use of Phosphodiesterase Type 5 Inhibitor Erectile Dysfunction Medication to Enhance Sex Among Gay and Bisexual Men in Australia: Results From the FLUX Study. Gay and bisexual men (GBM) use oral erectile dysfunction medications (EDMs) often with little evidence of medical indication necessitating their use.To investigate the prevalence, contexts, and motivations for oral EDM use and its relation to sexual risk behavior.A total of 2,250 Australian GBM completed an online survey (...) risky sexual behavior). Hammoud MA, Jin F, Lea T, et al. Off-Label Use of Phosphodiesterase Type 5 Inhibitor Erectile Dysfunction Medication to Enhance Sex Among Gay and Bisexual Men in Australia: Results From the FLUX Study. J Sex Med 2017;14:774-784.Copyright © 2017 International Society for Sexual Medicine. Published by Elsevier Inc. All rights reserved.

2017 Journal Of Sexual Medicine

142. Phosphodiesterase type 5 inhibitors and risk of melanoma: A meta-analysis. (PubMed)

Phosphodiesterase type 5 inhibitors and risk of melanoma: A meta-analysis. The association between phosphodiesterase type 5 (PDE5) inhibitors and melanoma risk is controversial.We quantify the association between use of PDE5 inhibitors and melanoma.We systematically searched PubMed, Embase, the Cochrane Central Register of Controlled Trials, Web of Science, and ClinicalTrials.gov for studies that were conducted up to July 13, 2016, and evaluated the association between PDE5 inhibitors and skin (...) cancer. Random effects meta-analyses were used to calculate the adjusted odds ratio (OR) with the 95% confidence interval (CI).Five observational studies were included. Compared with PDE5 inhibitor nonuse, PDE5 inhibitor use was slightly but significantly associated with an increased risk for development of melanoma (OR, 1.12; 95% CI, 1.03-1.21) and basal cell carcinoma (OR, 1.14; 95% CI, 1.09-1.19) but not squamous cell carcinoma. For melanoma risk, none of the prespecified factors (dose of PDE5

2017 Journal of the American Academy of Dermatology

143. Phosphodiesterase-5 Inhibitors Improve Clinical Outcomes, Exercise Capacity and Pulmonary Hemodynamics in Patients With Heart Failure With Reduced Left Ventricular Ejection Fraction: A Meta-Analysis. (Full text)

Phosphodiesterase-5 Inhibitors Improve Clinical Outcomes, Exercise Capacity and Pulmonary Hemodynamics in Patients With Heart Failure With Reduced Left Ventricular Ejection Fraction: A Meta-Analysis. Several studies have compared the use of phosphodiesterase-5 (PDE5) inhibitors sildenafil or udenafil with the placebo in patients suffering from pulmonary hypertension (PH) due to left chronic heart failure (CHF), corresponding to group 2 (PH due to left heart disease) of the PH classification (...) (according to 2015 ESC/ERS guidelines for the diagnosis and treatment of PH). The results of the use of PDE5 inhibitors in the PH due to left heart disease were inconsistent and heterogeneous. Therefore, we carried out a meta-analysis to assess the effect of PDE5 inhibitors in this clinical setting, i.e., patients with left CHF.A systematic search was conducted using the PubMed and Embase electronic archives. Studies had to be prospective randomized controlled trials (RCTs). In each of the RCTs admitted

2017 Journal of clinical medicine research

144. The phosphodiesterase 4 inhibitor apremilast inhibits Th1 but promotes Th17 responses induced by 6-sulfo LacNAc (slan) dendritic cells. (PubMed)

The phosphodiesterase 4 inhibitor apremilast inhibits Th1 but promotes Th17 responses induced by 6-sulfo LacNAc (slan) dendritic cells. The phosphodiesterase 4 (PDE4) inhibitor apremilast increases cellular cAMP levels and has proven effective in the treatment of psoriasis and psoriasis arthritis. We recently described 6-sulfo LacNAc dendritic cells (slanDCs) as immature DCs in blood and as a subset of inflammatory dermal DCs in psoriasis with a pronounced capacity to produce proinflammatory (...) cytokines and to program Th17/Th1 T cell responses.The aim of this study was to investigate possible immune regulatory effects of the PDE4 inhibitor apremilast on slanDCs.In vitro studies were performed analyzing the effects of apremilast on the proinflammatory function of slanDCs and their capacity to induce Th1/Th17-biased T cell responses.Increasing cAMP levels in slanDCs by PDE4 inhibition strongly reduced production of IL-12 and TNF-α. In line with these findings, co-culture experiments

2017 Journal of dermatological science

145. Relation of phosphodiesterase type 5 inhibitors and malignant melanoma: a meta-analysis and systematic review. (Full text)

Relation of phosphodiesterase type 5 inhibitors and malignant melanoma: a meta-analysis and systematic review. Data on the association between using PDE5 inhibitors and malignant melanoma are conflicting. To estimate the relation of using PDE5 inhibitors with risk of malignant melanoma, Medline (Ovid) and Embase (Ovid) databases were searched up to February 2017, and a random effects model was used to calculate the summary risk estimates. Five observational studies were included. Five studies (...) reports encompassed a total of 15,979 melanoma cases occurring among 1, 188,414 participants. The pooled multivariable-adjusted RR of melanoma in patients with using PDE5 inhibitors was 1.12 (95% CI: 1.03-1.21, I2 = 0.48). Findings from this systematic review support that PDE5 inhibitor use is associated with increased risk of melanoma in ED patients, the result remains inclusive and warrants further study in the future.

2017 Oncotarget

146. Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of <i>Ilex pubescens</i> Hook. et Arn. Using a Combination of Ultrafiltration and LC-MS. (Full text)

Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC-MS. The cyclic nucleotide phosphodiesterase (PDE) plays an important role in regulating the levels of second messenger molecules cAMP and cGMP. Various PDE inhibitors have been successfully developed into drugs for targeted diseases. In addition, PDE inhibitors can also be found in different foods and natural medicines. In this study (...) , ultrafiltration liquid chromatography-diode-array detector-electrospray ionization-ion-trap-time-of-flight-mass spectrometry (ultrafiltration LC-DAD-ESI-IT-TOF-MS) was applied to screen PDE inhibitors from the roots of Ilex pubescens Hook. et Arn. As a result, 11 major compounds were identified in I. pubescens roots, with nine compounds as potential PDE inhibitors, among which five were further confirmed to be active against PDEI and PDE5A dose-dependently in vitro, with ilexsaponin A1 and ilexsaponin B2

2017 Evidence-based Complementary and Alternative Medicine (eCAM)

147. 2-Year animal carcinogenicity results for crisaborole, a novel phosphodiesterase 4 inhibitor for atopic dermatitis. (PubMed)

2-Year animal carcinogenicity results for crisaborole, a novel phosphodiesterase 4 inhibitor for atopic dermatitis. Crisaborole is a novel, topical nonsteroidal, anti-inflammatory, phosphodiesterase 4 (PDE4) inhibitor for the treatment of mild to moderate atopic dermatitis.As part of a nonclinical safety testing program, these 2-year studies tested the carcinogenic potential of crisaborole.Crisaborole ointment, 2%, 5%, or 7%, was applied once daily topically to mice, and crisaborole

2017 Journal of dermatological science

148. The Effect of Oral Phosphodiesterase-5 Inhibitors on Sperm Parameters: a Meta-Analysis and Systematic Review. (PubMed)

The Effect of Oral Phosphodiesterase-5 Inhibitors on Sperm Parameters: a Meta-Analysis and Systematic Review.

2017 Urology

149. Selective phosphodiesterase-2A inhibitor alleviates radicular inflammation and mechanical allodynia in non-compressive lumbar disc herniation rats. (PubMed)

Selective phosphodiesterase-2A inhibitor alleviates radicular inflammation and mechanical allodynia in non-compressive lumbar disc herniation rats. Phosphodiesterase inhibitors possess anti-inflammatory properties. In addition, some studies report that phosphodiesterase 2A (PDE2A) are highly expressed in the dorsal horn of the spinal cord. The present study aimed to investigate whether intrathecal administration of Bay 60-7550, a specific PDE2A inhibitor, could alleviate mechanical allodynia (...) factor α (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6), cyclic adenosine monophosphate (cAMP), and cyclic guanosine monophosphate (cGMP) expressions were measured by ELISA. Furthermore, PDE2A mRNA and protein expressions in spinal cord were measured by Real-Time PCR and Western blot.Intrathecal administration of the PDE2A inhibitor Bay 60-7550, significantly attenuated mechanical allodynia, down-regulated spinal TNF-α, IL-1β and IL-6 over-expressions, increased the expression of spinal cAMP

2017 European Spine Journal

150. Efficacy and safety of short- and long-term, regular and on-demand regimens of phosphodiesterase type 5 inhibitors in treating erectile dysfunction after nerve-sparing radical prostatectomy: a systematic review and meta-analysis. (Full text)

Efficacy and safety of short- and long-term, regular and on-demand regimens of phosphodiesterase type 5 inhibitors in treating erectile dysfunction after nerve-sparing radical prostatectomy: a systematic review and meta-analysis. We performed a meta-analysis to evaluate the efficacy and safety of short-term (≤6 months) and long-term (>6 months), regular (OaD) and on-demand (PRN) regimens of phosphodiesterase type 5 inhibitors (PDE5-Is) in treating erectile dysfunction (ED) after nerve-sparing

2017 Clinical interventions in aging

151. Efficacy of phosphodiesterase type 5 inhibitors for the treatment of distal ureteral calculi: A systematic review and meta-analysis. (Full text)

Efficacy of phosphodiesterase type 5 inhibitors for the treatment of distal ureteral calculi: A systematic review and meta-analysis. To determine the efficacy of phosphodiesterase type 5 inhibitors (PDE5i) as medical expulsive therapy (MET) for the treatment of distal ureteral calculi.A search strategy was conducted in the MEDLINE, CENTRAL, and Embase databases. Searches were also conducted in other databases and unpublished literature. Clinical trials were included without language

2017 Investigative and clinical urology

152. Prospective Case-Crossover Study Investigating the Possible Association Between Nonarteritic Anterior Ischemic Optic Neuropathy (NAION) and Phosphodiesterase Type 5 Inhibitor (PDE5i) Exposure. (PubMed)

Prospective Case-Crossover Study Investigating the Possible Association Between Nonarteritic Anterior Ischemic Optic Neuropathy (NAION) and Phosphodiesterase Type 5 Inhibitor (PDE5i) Exposure. To evaluate the association between intermittent phosphodiesterase type 5 inhibitor (PDE5i) exposure and risk of acute nonarteritic anterior ischemic optic neuropathy (NAION) using a case-crossover design.Male adults with suspected NAION were enrolled at 41 US ophthalmology sites from 2010 to 2015

2017 Urology

153. The effect of phosphodiesterase-5 inhibitors on cerebral blood flow in humans: A systematic review. (PubMed)

The effect of phosphodiesterase-5 inhibitors on cerebral blood flow in humans: A systematic review. Agents that augment cerebral blood flow (CBF) could be potential treatments for vascular cognitive impairment. Phosphodiesterase-5 inhibitors are vasodilating drugs established in the treatment of erectile dysfunction (ED) and pulmonary hypertension. We reviewed published data on the effects of phosphodiesterase-5 inhibitors on CBF in adult humans. A systematic review according to PRISMA (...) by phosphodiesterase-5 inhibitors, but cerebrovascular regulation was improved in ED, pulmonary hypertension, diabetes, Becker's and a group of healthy volunteers. This evidence suggests that phosphodiesterase-5 inhibitors improve responsiveness of the cerebral vasculature, particularly in disease states associated with an impaired endothelial dilatory response. This supports the potential therapeutic use of phosphodiesterase-5 inhibitors in vascular cognitive impairment where CBF is reduced. Further studies

2017 Journal of Cerebral Blood Flow and Metabolism

154. Phosphodiesterase 4 (PDE4) Inhibitors. (PubMed)

Phosphodiesterase 4 (PDE4) Inhibitors. Historically, drugs available for treating atopic dermatitis (AD) have been limited to topical corticosteroids and topical calcineurin inhibitors, with systemic immunosuppressants and phototherapy reserved for severe AD. Despite their efficacy and infrequent adverse events, phobia about the use of topical steroids and calcineurin inhibitors has limited their use. More targeted options with fewer systemic and cutaneous side effects are needed for treating (...) AD. Phosphodiesterase 4 (PDE4) is involved in the regulation of proinflammatory cytokines via the degradation of cyclic adenosine monophosphate. PDE4 activity is increased in the inflammatory cells of patients with AD, leading to increased production of proinflammatory cytokines and chemokines. Targeting PDE4 reduces the production of these proinflammatory mediators in AD. Both topical and oral PDE4 inhibitors have a favorable safety profile. Crisaborole 2% ointment, a topical PDE4, is now US

2017 Journal of American Academy of Dermatology

155. The isozyme selective phosphodiesterase-4 inhibitor, ABI-4, attenuates the effects of lipopolysaccharide in human cells and rodent models of peripheral and CNS inflammation. (PubMed)

The isozyme selective phosphodiesterase-4 inhibitor, ABI-4, attenuates the effects of lipopolysaccharide in human cells and rodent models of peripheral and CNS inflammation. Inhibitors of phosphodiesterase-4 (PDE4) have been approved for the treatment of inflammatory disorders, but are associated with dose-limiting nausea and vomiting. These side effects are hypothesized to be mediated by inhibition of the PDE4D isozyme. Here we demonstrate the anti-inflammatory effects of the novel brain (...) penetrant PDE4D-sparing PDE4 inhibitor, ABI-4. ABI-4 was a potent (EC50∼14nM) inhibitor of lipopolysaccharide (LPS) induced TNF-α release from mouse microglia and human PBMCs. ABI-4 (0.32mg/kg) blocked LPS-induced release of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in blood and brain of mice. In a rat model of endotoxin induced uveitis, ABI-4 (0.03-0.3mg/kg) demonstrated steroid-like efficacy in preventing leucocyte infiltration of the aqueous humor when administered 4h after LPS. LPS (0.32mg/kg

2017 Brain, behavior, and immunity

156. Apremilast, an oral phosphodiesterase 4 inhibitor, in the treatment of Japanese patients with moderate to severe plaque psoriasis: Efficacy, safety and tolerability results from a phase 2b randomized controlled trial. (Full text)

Apremilast, an oral phosphodiesterase 4 inhibitor, in the treatment of Japanese patients with moderate to severe plaque psoriasis: Efficacy, safety and tolerability results from a phase 2b randomized controlled trial. Apremilast, an oral, small-molecule phosphodiesterase 4 inhibitor, works intracellularly within immune cells to regulate inflammatory mediators. This phase 2b randomized, placebo-controlled study evaluated efficacy and safety of apremilast among Japanese patients with moderate

2017 The Journal of dermatology Controlled trial quality: uncertain

157. Phosphodiesterase Type 5 Inhibitors and the Risk of Melanoma Skin Cancer (PubMed)

Phosphodiesterase Type 5 Inhibitors and the Risk of Melanoma Skin Cancer The association between phosphodiesterase type 5 inhibitors (PDE5-Is), drugs used in the treatment of erectile dysfunction (ED), and melanoma skin cancer is controversial.To assess whether the use of PDE5-Is is associated with an increased risk of melanoma skin cancer.Using the UK Clinical Practice Research Datalink, we assembled a cohort of men newly diagnosed with ED between 1998 and 2014 and followed until 2015. PDE5-I (...) with basal and squamous cell carcinoma, with an unclear association with numbers of prescriptions and pills received.The use of PDE5-Is was not associated with an overall increased risk of melanoma skin cancer. The increased risks observed in the highest prescription and pill categories require further validation.In this study, the use of phosphodiesterase type 5 inhibitors was not associated with an increased risk of melanoma skin cancer.Copyright © 2016. Published by Elsevier B.V.

2016 EvidenceUpdates

158. Apremilast, an oral phosphodiesterase 4 inhibitor, in patients with psoriatic arthritis and current skin involvement: a phase III, randomised, controlled trial (PALACE 3) (Full text)

Apremilast, an oral phosphodiesterase 4 inhibitor, in patients with psoriatic arthritis and current skin involvement: a phase III, randomised, controlled trial (PALACE 3) To evaluate apremilast treatment in patients with active psoriatic arthritis, including current skin involvement, despite prior therapy with conventional disease-modifying antirheumatic drugs and/or biologic agents.Patients (N=505) were randomised (1:1:1) to placebo, apremilast 20 mg twice daily, or apremilast 30 mg twice

2016 EvidenceUpdates Controlled trial quality: uncertain

159. Phosphodiesterase-4 Inhibitor

Phosphodiesterase-4 Inhibitor Phosphodiesterase-4 Inhibitor Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Phosphodiesterase-4 (...) Inhibitor Phosphodiesterase-4 Inhibitor Aka: Phosphodiesterase-4 Inhibitor , Roflumilast , Daliresp From Related Chapters II. Mechanism Phosphodiesterase-4 Inhibitor increases lung, intracellular cAMP III. Indications Severe, refractory with frequent exacerbations IV. Dosing Roflumilast 500 mcg orally daily ($250/month) V. Adverse Effects Gastrointestinal (common, intolerable in 5%) Weight loss (may be >10%) Other common symptoms Psychiatric (3%) Depression Anxiety VI. Drug Interactions Cytochrome P450

2018 FP Notebook

160. Phosphodiesterase Inhibitor

Phosphodiesterase Inhibitor Phosphodiesterase Inhibitor Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Phosphodiesterase Inhibitor (...) Phosphodiesterase Inhibitor Aka: Phosphodiesterase Inhibitor , Phosphodiesterase 5 Inhibitor , PDE5 Inhibitor , Avanafil , Stendra II. Preparations All agents are very expensive (except generic which costs $1/pill) ( ) Vardenafil ( , Staxyn) ( ) Avanafil (Stendra) Released in 2014 with similar activity as (onset in 30 minutes and duration for 5 hours) Similar s as for Vardenafil ( , Staxyn) III. Indications Psychogenic Neurogenic Vasculogenic IV. Contraindications Absolute Contraindications Men using nitrates

2018 FP Notebook

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