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Frontiers in Bioscience (Landmark... Jan 2022Aerosolised drugs have been approved for several diseases such as cystic fibrosis and diabetes. Moreover; there are already drugs for pulmonary hypertension in aerosol...
INTRODUCTION
Aerosolised drugs have been approved for several diseases such as cystic fibrosis and diabetes. Moreover; there are already drugs for pulmonary hypertension in aerosol form already on the market.
MATERIALS AND METHODS
Two drugs for pulmonary hypertension (Tadalafil and Macitentan) were milled and transformed from tablets to powder. Three different jet-nebulizers with seven different residual cups were combined. Moreover, we used 3 different ultrasound nebulizers with two different release methods.
RESULTS
The drug and residual cup designs produce alone or jointly different MMAD diameters. The three large (10 mls) residual cups with the jet-nebulisers produced the smallest aerosol droplets. Both ultrasound nebulisers are capable of producing optimal size aerosol droplets ≤5 μm mmad.
CONCLUSIONS
These two drugs can be easily administered as aerosol and an vivo clinical study will prove the safety for the airways.
Topics: Aerosols; Humans; Hypertension, Pulmonary; Particle Size; Pyrimidines; Sulfonamides; Tablets; Tadalafil
PubMed: 35090324
DOI: 10.31083/j.fbl2701019 -
Archives of Dermatological Research Mar 2022Vascular complication is one of the causes of skin flap healing failure. Sildenafil and tadalafil, a type-5 phosphodiesterase inhibitor, can improve flap viability,...
Vascular complication is one of the causes of skin flap healing failure. Sildenafil and tadalafil, a type-5 phosphodiesterase inhibitor, can improve flap viability, however, the action mechanisms involved in this process are still unclear. To assess the effects of orally administered sildenafil and tadalafil on the healing kinetics and skin flap viability, sixty-two Wistar rats were divided into three groups: control (n = 22), sildenafil (n = 20), and tadalafil (n = 20). The solutions were administered orally (dose: 10 mg/kg) immediately after the surgical procedure and then every 24 h. At postoperative days 7 and 14, the skin flap samples were collected, submitted to histological processing and evaluated under optical microscopy. In experimental groups (sildenafil and tadalafil), we found an increased vascularization (p < 0.05) on the 7th and 14th day associated with the ulcer size decrease on the 14th day, although it was not significant. There was a higher influx of neutrophils and a decrease of mononuclear population on the 7th day (p < 0.05). On the 14th day, these differences were observed only in the tadalafil group (p < 0.05). This study suggested positive results with the use of sildenafil and tadalafil as adjuvant drugs in skin flap viability.
Topics: Administration, Oral; Animals; Male; Models, Animal; Rats; Rats, Wistar; Sildenafil Citrate; Skin Neoplasms; Skin Transplantation; Surgical Flaps; Tadalafil; Vasodilator Agents; Wound Healing
PubMed: 33715076
DOI: 10.1007/s00403-021-02196-0 -
International Journal of Molecular... Apr 2022Tadalafil is a selective phosphodiesterase type-5 (PDE5) inhibitor that is approved for the treatment of men with erectile dysfunction (ED) and/or benign prostate... (Review)
Review
Tadalafil is a selective phosphodiesterase type-5 (PDE5) inhibitor that is approved for the treatment of men with erectile dysfunction (ED) and/or benign prostate hyperplasia (BPH) -associated symptoms. Besides its classical actions on PDE5 within the genitourinary tract, where the specific enzyme expression is maximal, it may exert different systemic effects. This is mainly due to the pleiotropic distribution of PDE5 enzyme throughout the human (and animal) body, where it can exert protective effects in different clinical conditions. Recently, it has been demonstrated that tadalafil may display novel actions on androgen receptor (AR) expression and activity and cytochrome P19a1 (Cyp19a1) and estrogen receptor β (ERβ) expression in different in vitro systems, such as adipose, bone and prostate cancer cells, where it can act as a selective modulator of steroid hormone production. This may determine novel potential mechanism(s) of control in pathophysiologic pathways. In this review, we summarize basic research and translational results applicable to the use of tadalafil in the treatment of obesity, bone loss and prostate cancer.
Topics: Animals; Carbolines; Cyclic Nucleotide Phosphodiesterases, Type 5; Erectile Dysfunction; Hormones; Humans; Male; Phosphodiesterase 5 Inhibitors; Prostate; Prostatic Hyperplasia; Prostatic Neoplasms; Steroids; Tadalafil; Treatment Outcome
PubMed: 35457011
DOI: 10.3390/ijms23084191 -
BMJ Clinical Evidence Jun 2011Erectile dysfunction may affect 30% to 50% of men aged 40 to 70 years, with age, smoking, and obesity being the main risk factors, although 20% of cases have... (Review)
Review
INTRODUCTION
Erectile dysfunction may affect 30% to 50% of men aged 40 to 70 years, with age, smoking, and obesity being the main risk factors, although 20% of cases have psychological causes.
METHODS AND OUTCOMES
We conducted a systematic review and aimed to answer the following clinical questions: What are the effects of phosphodiesterase inhibitors in men with erectile dysfunction of any cause? What are the effects of phosphodiesterase inhibitors on erectile dysfunction in men with diabetes, with cardiovascular disease, with spinal cord injury, and with prostate cancer or undergoing prostatectomy? What are the effects of drug treatments other than phosphodiesterase inhibitors in men with erectile dysfunction of any cause? What are the effects of devices, psychological/behavioural treatments, and alternative treatments in men with erectile dysfunction of any cause? We searched: Medline, Embase, The Cochrane Library, and other important databases up to August 2009 (Clinical Evidence reviews are updated periodically, please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA).
RESULTS
We found 81 systematic reviews, RCTs, or observational studies that met our inclusion criteria. We performed a GRADE evaluation of the quality of evidence for interventions.
CONCLUSIONS
In this systematic review we present information relating to the effectiveness and safety of the following interventions: alprostadil (intracavernosal, intraurethral, topical), cognitive behavioural therapy, ginseng, papaverine, papaverine plus phentolamine (bimix), papaverine plus phentolamine plus alprostadil (trimix), penile prostheses, phosphodiesterase inhibitors (sildenafil, tadalafil, vardenafil), psychosexual counselling, vacuum devices, and yohimbine.
Topics: Double-Blind Method; Erectile Dysfunction; Humans; Phosphodiesterase Inhibitors; Prostatectomy; Sildenafil Citrate; Tadalafil
PubMed: 21711956
DOI: No ID Found -
European Journal of Medical Research Jul 2022Chronic renal failure (CRF) is a progressive loss of renal function that lead to reduced sodium filtration and inappropriate suppression of tubular reabsorption that...
BACKGROUND
Chronic renal failure (CRF) is a progressive loss of renal function that lead to reduced sodium filtration and inappropriate suppression of tubular reabsorption that ultimately leads to volume expansion. The aim of this study was to study the efficacy of furosemide and tadalafil nanoforms compared to conventional forms against adenine-induced CRF rat-model.
METHODS
Addition of 0.75% adenine to the diet of rats for 4 weeks gained general acceptance as a model to study kidney damage as this intervention mimicked most of the structural and functional changes seen in human chronic kidney disease Urine analysis, histopathological changes and immunohistochemical expression of caspase-3 and interleukin-1 beta (IL-1β) in renal tissues were performed.
RESULTS
Our results showed that the combination of tadalafil and furosemide using conventional and nanoparticle formulations had better renoprotective effect than individual drugs. This was demonstrated by improvement of urinary, serum and renal tissue markers as indicative of organ damage. This was also reflected on the reduction of tubular expression of kidney injury molecule-1 (KIM-1) and neutrophil gelatinase-associated lipocalin (NGAL). Immunohistochemical studies showed that the deteriorated renal cellular changes indicated by increased expression of caspase-3 and IL-1β were greatly improved by the combined treatment particularly with the nanoforms.
CONCLUSIONS
The nanoforms of both furosemide and tadalafil had greater renopreventive effects compared with conventional forms against adenine-induced CRF in rats.
Topics: Adenine; Animals; Caspase 3; Furosemide; Humans; Kidney Failure, Chronic; Rats; Renal Insufficiency, Chronic; Tadalafil
PubMed: 35820963
DOI: 10.1186/s40001-022-00747-3 -
Investigative and Clinical Urology Jan 2022To investigate a therapeutic protocol for erectile dysfunction (ED) based on the combination of low-intensity extracorporeal shock wave therapy (Li-ESWT), tadalafil, and... (Randomized Controlled Trial)
Randomized Controlled Trial
Adjuvant daily therapy with L-arginine 2,500 mg and tadalafil 5 mg increases efficacy and duration of benefits of low-intensity extracorporeal shock wave therapy for erectile dysfunction: A prospective, randomized, single-blinded study with 1-year follow-up.
PURPOSE
To investigate a therapeutic protocol for erectile dysfunction (ED) based on the combination of low-intensity extracorporeal shock wave therapy (Li-ESWT), tadalafil, and L-arginine.
MATERIALS AND METHODS
Recruited patients completed the International Index of Erectile Function erectile function domain (IIEF-EF) and the Erection Hardness Score (EHS) questionnaires at baseline and were randomly assigned in two groups: A (treatment group) and B (control group). Men in both groups received six weekly applications of Li-ESWT. Group A was prescribed adjuvant oral therapy with tadalafil 5 mg and L-arginine 2,500 mg. Follow-up visits were scheduled 1, 6, and 12 months after the last Li-ESWT application. At each follow-up visit, the IIEF-EF and EHS questionnaires were administered again. The main outcome measures were the changes from baseline to every follow-up visit in IIEF-EF and EHS scores.
RESULTS
The mean IIEF-EF score in group A was 16.0±4.0, 24.8±3.4, 23.3±4.6, and 21.6±5.5 at baseline, 1, 6, and 12 months of follow-up, respectively, whereas in group B the mean IIEF-EF score was 16.5±4.1, 22.7±4.2, 21.5±4.5, and 19.5±4.9, respectively. We reported an increase in the mean EHS score in group A from 2.07±0.72 at baseline to 3.39±0.59, 3.17±0.67, and 2.98±0.72 at 1, 6, and 12 months, respectively, and in group B from 2.12±0.80 at baseline to 3.07±0.78 and 2.95±0.76 at 1 and 6 months, respectively.
CONCLUSIONS
Adjuvant daily therapy with L-arginine 2,500 mg and tadalafil 5 mg was safe and effective in increasing the efficacy and the duration of benefits of Li-ESWT.
Topics: Adult; Arginine; Combined Modality Therapy; Drug Administration Schedule; Erectile Dysfunction; Extracorporeal Shockwave Therapy; Follow-Up Studies; Humans; Male; Middle Aged; Phosphodiesterase 5 Inhibitors; Prospective Studies; Single-Blind Method; Tadalafil; Time Factors; Treatment Outcome
PubMed: 34983126
DOI: 10.4111/icu.20210317 -
Therapeutic Advances in Respiratory... Feb 2013The purpose of this review is to evaluate the use of tadalafil as monotherapy and in combination regimens for the treatment of pulmonary arterial hypertension (PAH). A... (Review)
Review
The purpose of this review is to evaluate the use of tadalafil as monotherapy and in combination regimens for the treatment of pulmonary arterial hypertension (PAH). A systematic English language search of the medical literature using PubMed was conducted between January 1960 and May 2012 using the search terms 'tadalafil', 'therapy', 'pulmonary (arterial) hypertension' and 'combination therapy'. Special emphasis was given to controlled clinical trials and case studies relevant for the use of tadalafil in PAH. The search revealed 113 relevant publications, 31 of which were clinical trials, 52 were reviews and 12 were case reports. Of these, 12 were clinical studies in human patients with PAH who were treated with tadalafil alone, and seven were clinical studies in human patients with PAH who were treated with tadalafil in combination with other agents. Only clinical studies in human patients were included. Exclusion criteria were monotherapy other than using tadalafil and any combination therapy that excluded tadalafil as part of the treatment regimen. Overall, 1353 human subjects were studied; 896 were treated with tadalafil alone while 457 subjects were treated with tadalafil in coadministration. Tadalafil appears to be an effective and a safe treatment option for patients with PAH. It improves clinical status, exercise capacity, hemodynamic parameters, compliance issues and quality of life and reduces the occurrence of clinical worsening. Tadalafil in combination therapy seems to be additive and synergistic in relaxing pulmonary vascular muscle cells but more clinical trials on human subjects are warranted.
Topics: Antihypertensive Agents; Arterial Pressure; Carbolines; Drug Therapy, Combination; Familial Primary Pulmonary Hypertension; Humans; Hypertension, Pulmonary; Phosphodiesterase 5 Inhibitors; Pulmonary Artery; Tadalafil; Treatment Outcome
PubMed: 23129569
DOI: 10.1177/1753465812463627 -
Alzheimer's & Dementia : the Journal of... Dec 2022There are few randomized clinical trials in vascular cognitive impairment (VCI). This trial tested the hypothesis that the PDE5 inhibitor tadalafil, a widely used... (Randomized Controlled Trial)
Randomized Controlled Trial
INTRODUCTION
There are few randomized clinical trials in vascular cognitive impairment (VCI). This trial tested the hypothesis that the PDE5 inhibitor tadalafil, a widely used vasodilator, increases cerebral blood flow (CBF) in older people with symptomatic small vessel disease, the main cause of VCI.
METHODS
In a double-blind, placebo-controlled, cross-over trial, participants received tadalafil (20 mg) and placebo on two visits ≥7 days apart (randomized to order of treatment). The primary endpoint, change in subcortical CBF, was measured by arterial spin labelling.
RESULTS
Tadalafil increased CBF non-significantly in all subcortical areas (N = 55, age: 66.8 (8.6) years) with greatest treatment effect within white matter hyperintensities (+9.8%, P = .0960). There were incidental treatment effects on systolic and diastolic blood pressure (-7.8, -4.9 mmHg; P < .001). No serious adverse events were observed.
DISCUSSION
This trial did not identify a significant treatment effect of single-administration tadalafil on subcortical CBF. To detect treatment effects may require different dosing regimens.
Topics: Humans; Aged; Tadalafil; Cognitive Dysfunction; Double-Blind Method
PubMed: 35135037
DOI: 10.1002/alz.12559 -
Archivio Italiano Di Urologia,... Feb 2023To compare the efficacy of Tamsulosin, Silodosin and Tadalafil as a medical expulsive therapy for treatment of distal ureteral calculi. (Comparative Study)
Comparative Study Randomized Controlled Trial
OBJECTIVE
To compare the efficacy of Tamsulosin, Silodosin and Tadalafil as a medical expulsive therapy for treatment of distal ureteral calculi.
PATIENTS AND METHODS
Over a period of 6 months (January 2022 to June 2022) this prospective randomized study was conducted on 170 patients with distal ureteric stone ≤ 10 mm. Patients were randomly divided into three groups. Patients in group A received Tamsulosin 0.4mg, in group B received Silodosin, and in group C receive Tadalafil 5 mg. Therapy was given for a maximum of 4 weeks. The rate and time of stone expulsion, the analgesic use, attacks of colic and hospital visits for pain, and adverse effects of drugs were recorded.
RESULTS
Among 170 patients who were enrolled in study, 20 were lost to follow-up (7, 8, 5 in group A, B, And C respective-ly). There was a significant higher stone passage rate in group C than group A and B (90% vs. 70% and 76% respectively; p-value = 0.043) and shorter expulsion time in group C (8.7 ± 3.3 days) vs. group A (12.5 ± 5.2 days) and group B (11.3 ± 4.2 days) with (p-value = 0.001)(highly statistically significant with p-value < 0.001) and increased amount of analgesics required in group A (225 ± 115.7 mg) and group B (163 ± 77.5 mg) when compared with group C (120 ± 55.3 mg).
CONCLUSION
Tadalafil is more effective than Tamsulosin and Silodosin in treatment of patients with distal ureteric stones ≤ 10 mm as regard stone expulsion rate, expulsion time with decreased number of colicky episodes and side effects.
Topics: Humans; Male; Female; Adult; Middle Aged; Prospective Studies; Tamsulosin; Ureteral Calculi; Tadalafil; Urological Agents; Indoles; Treatment Outcome
PubMed: 36924384
DOI: 10.4081/aiua.2023.10849 -
World Journal of Urology Aug 2022Men with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH), will have deterioration in the quality of life. Likewise, BPH can be... (Randomized Controlled Trial)
Randomized Controlled Trial
Prospective comparison of tadalafil 5 mg alone, silodosin 8 mg alone, and the combination of both in treatment of lower urinary tract symptoms related to benign prostatic hyperplasia.
BACKGROUND
Men with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH), will have deterioration in the quality of life. Likewise, BPH can be complicated by damage to bladder function, bladder stones formation, hematuria, and impaired kidney function. The goal of treatment is to avoid all those effects caused by BPH.
OBJECTIVE
To evaluate the efficacy of tadalafil alone, silodosin alone, and the combination of both in the treatment of LUTS associated with BPH.
PATIENTS AND METHODS
Patients in our department with BPH who had LUTS were assigned randomly to three groups: A (101 patients) received tadalafil, 5 mg; B (102 patients) received silodosin, 8 mg; and group C (105 patients) received the combination of tadalafil, 5 mg, and silodosin, 8 mg. For all participants, we asses changes in the maximum urinary flow rate (Qmax), International Prostate Symptom Score (IPSS), International Index of Erectile Function (IIEF) score, Post-voiding urine (PVR) and all results were recorded and analyzed with the (SPSS) and Microsoft Excel 2010.
RESULTS
Qmax, IPSS, PVR and IIEF score improved significantly more with the combination of tadalafil and silodosin than with either drug alone (p < 0.001). Three months after treatment, the mean Qmax values were 14.4 ml/sec in group A, 15.2 ml/sec in group B, and 15.8 ml/sec in group C; and the mean IPSSs were 17.6 in group A, 16.7 in group B, and 15.6 in group C (p < 0.001).
CONCLUSION
Tadalafil and silodosin are effective treatment options in men with BPH who have LUTS, but the combination of both is more effective and feasible in treating LUTS of BPH.
Topics: Erectile Dysfunction; Humans; Indoles; Lower Urinary Tract Symptoms; Male; Phosphodiesterase 5 Inhibitors; Prospective Studies; Prostatic Hyperplasia; Quality of Life; Tadalafil; Treatment Outcome
PubMed: 35773357
DOI: 10.1007/s00345-022-04071-7