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Alpha Adrenergic Antagonist

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2501. Durability and cost-effectiveness of transurethral needle ablation of the prostate as an alternative to transurethral resection of the prostate when alpha-adrenergic antagonist therapy fails. (Abstract)

Durability and cost-effectiveness of transurethral needle ablation of the prostate as an alternative to transurethral resection of the prostate when alpha-adrenergic antagonist therapy fails. We analyzed the adverse event profile, long-term efficacy and cost-effectiveness of transurethral needle ablation of the prostate for lower urinary tract symptoms associated with benign prostatic hyperplasia as an alternative to transurethral resection of the prostate in men with symptoms uncontrolled (...) for anesthesia and now practice clean intermittent self-catheterization, 14 men (20%) reported improvement following resumption of treatment with an alpha-adrenergic antagonist after transurethral needle ablation of the prostate and 6 men (9%) have experienced deterioration in lower urinary tract symptoms with reduction in quality of life assessment (International Prostate Symptom Score 3 or greater) but have declined further intervention. There were 12 men (17%) who remained symptom-free up to 10 years

2007 Journal of Urology

2502. Primary bladder neck dysfunction in children and adolescents II: results of treatment with alpha-adrenergic antagonists. (Abstract)

Primary bladder neck dysfunction in children and adolescents II: results of treatment with alpha-adrenergic antagonists. Little has been reported on the occurrence of primary bladder neck dysfunction (PBND) in the pediatric patient, particularly as it relates to the use of alpha-blocker therapy, the mainstay of medical therapy in adults. Diagnosed on videourodynamics (VUDS), PBND is characterized by the constellation of prolonged opening time, incomplete bladder neck funneling, quiet pelvic (...) floor electromyogram (EMG) during voiding and abnormal pressure flow parameters. We report the VUDS findings in PBND and our experience with alpha-blocker therapy in the pediatric and adolescent population.A total of 34 symptomatic patients met all VUDS criteria for PBND, and alpha-blocker therapy was initiated in 26. All patients were monitored with serial noninvasive uroflow studies with pelvic floor EMG (uroflow/EMG) before and after initiation of alpha-blocker therapy. Objective clinical

2005 Journal of Urology

2503. Effects of alpha 1-adrenergic receptor subtype selective antagonists on lower urinary tract function in rats with bladder outlet obstruction. (Abstract)

Effects of alpha 1-adrenergic receptor subtype selective antagonists on lower urinary tract function in rats with bladder outlet obstruction. Antagonists of alpha 1-adrenergic receptors (alpha 1ARs) relieve obstructive and irritative symptoms in patients with bladder outlet obstruction. However, to our knowledge mechanisms underlying the relief of irritative symptoms remain unknown. Because bladder alpha 1dARs are up-regulated in some rats with bladder outlet obstruction, we investigated (...) the effect of the alpha 1aAR antagonist 5-methyl urapidil (5MU) vs the alpha 1a/alpha 1dAR antagonist tamsulosin on urinary frequency in obstructed rats.Baseline frequency was measured using a chronic micturition recording system and then obstruction (40 rats) or sham obstruction surgery (11 rats) was performed. After 6 weeks frequency was reassessed, followed by subcutaneous implantation of osmotic pumps to deliver 5MU, tamsulosin or vehicle for 1 week. Upon the completion of drug treatment urinary

2004 Journal of Urology

2504. Combined use of alpha-adrenergic and muscarinic antagonists for the treatment of voiding dysfunction. Full Text available with Trip Pro

Combined use of alpha-adrenergic and muscarinic antagonists for the treatment of voiding dysfunction. We provide an overview of the medical literature supporting the combined use of muscarinic and alpha-adrenergic antagonist therapy for the treatment of voiding dysfunction.The MEDLINE database (1966 to 2004) of the United States National Library of Medicine was searched for pertinent studies.Although the mechanism of action of alpha-adrenergic antagonist therapy for voiding dysfunction has (...) bladder contractions and there is evidence for an M2 component to the suprasacral control of voiding.Based on the physiology of alpha-adrenergic and muscarinic receptors the inhibition of each one would be expected to be more beneficial than that of either alone because they would work on 2 components of detrusor function. Patients who would likely benefit from this combination therapy are men with lower urinary tract symptoms, women with urgency/frequency syndrome (overactive bladder), patients

2005 Journal of Urology

2505. alpha(1)-Adrenergic receptor antagonists and the iris: new mechanistic insights into floppy iris syndrome. (Abstract)

alpha(1)-Adrenergic receptor antagonists and the iris: new mechanistic insights into floppy iris syndrome. Understanding the role of adrenergic receptors in iris biology has gained widespread interest due to the recently described intraoperative floppy iris syndrome sometimes encountered during cataract surgery. alpha(1)AR-mediated iris dilator smooth muscle contraction occurs via alpha(1a)ARs whereas alpha(1b)ARs mediate iris arteriolar contraction. Because alpha(1)AR antagonists are first (...) -line therapy for benign prostatic hyperplasia and lower urinary tract symptoms, more elderly patients requiring cataract surgery now receive these drugs. After reviewing intraoperative floppy iris syndrome, strengths/weaknesses of supporting data, and reviewing iris biology, a case is made that rather than being drug specific (alpha(1)AR antagonists), intraoperative floppy iris syndrome may represent the "tip of the iceberg." Relaxed iris dilator muscle resistant to adrenergic agonists should

2006 Survey of Ophthalmology

2506. Reserpine induces vascular alpha 2-adrenergic supersensitivity and platelet alpha 2-adrenoceptor up-regulation in dog. Full Text available with Trip Pro

Reserpine induces vascular alpha 2-adrenergic supersensitivity and platelet alpha 2-adrenoceptor up-regulation in dog. 1. The aim of the present study was to investigate the influence of catecholamine levels on the regulation of alpha 2-adrenoceptor sensitivity in dogs. 2. Blood pressure and heart rate values at rest, plasma catecholamine levels, platelet and adipocyte alpha 2-adrenoceptors as well as the alpha 2-mediated cardiovascular responses to clonidine (10 micrograms kg-1 i.v., after (...) % in systolic and diastolic blood pressures respectively) after reserpine treatment. This effect was suppressed by administration of RX-821002, a new specific alpha 2-adrenoceptor antagonist. 6. Reserpine treatment significantly increased platelet alpha 2-adrenoceptor number (identified with [3H]- yohimbine or [3H]-RX821002) with no change in Kd values. alpha 2-Adrenoceptor number remained unchanged in adipocytes (identified with [3H]-RX821002). 7. These results show that a 15 day treatment with reserpine

1990 British journal of pharmacology

2507. Alpha-adrenergic blockade in vasotonic angina: lack of efficacy of specific alpha 1-receptor blockade with prazosin. (Abstract)

Alpha-adrenergic blockade in vasotonic angina: lack of efficacy of specific alpha 1-receptor blockade with prazosin. To clarify the possible role of the alpha 1-adrenergic receptor in angina due to coronary artery spasm, a double-blind, randomized, placebo-controlled trial of the specific alpha 1-antagonist, prazosin, was performed. Six patients with vasotonic angina were studied, with efficacy measured by continuous electrocardiographic recording and the tabulation of chest pain (...) that coronary artery spasm is not primarily caused by an effect on or an abnormality of the coronary vascular alpha 1-receptor.

1983 Journal of the American College of Cardiology Controlled trial quality: uncertain

2508. [A cross-over study of ketanserin compared to placebo, beta-adrenergic blockader, diuretic and alpha 1-adrenergic blockader. Cooperative research in the USSR (the Cooperative Program to Study New Preparations in the Prevention of Arterial Hypertension). W (Abstract)

[A cross-over study of ketanserin compared to placebo, beta-adrenergic blockader, diuretic and alpha 1-adrenergic blockader. Cooperative research in the USSR (the Cooperative Program to Study New Preparations in the Prevention of Arterial Hypertension). W In 51 patients with stage II essential hypertension (mild and moderate arterial hypertension), a cross-over study was carried out to estimate the efficacy of the use of ketanserin (KS), an antagonist of serotonin receptors, as compared

1991 TerapevticheskiÄ­ arkhiv Controlled trial quality: uncertain

2509. Adrenergic transmission in the dog mesenteric vein and its modulation by alpha-adrenoceptor antagonists. Full Text available with Trip Pro

Adrenergic transmission in the dog mesenteric vein and its modulation by alpha-adrenoceptor antagonists. Adrenergic transmission was investigated in the dog mesenteric vein by recording electrical responses of single smooth muscle cells to perivascular nerve stimulation. Perivascular nerve stimulation generated an excitatory junction potential (e.j.p.) and a slow depolarization of the membrane. The amplitude of the e.j.p. was increased by increasing the stimulus intensity, and at high intensity (...) . The slow depolarization was generated by activation of alpha 2-adrenoceptors. Exogenously applied noradrenaline reduced the e.j.p. amplitude through activation of prejunctional alpha 2-adrenoceptors, but the reduction may not involve alpha-autoinhibitory mechanisms.

1984 British journal of pharmacology

2510. Effect of the alpha 2-adrenergic antagonist yohimbine on orthostatic tolerance. (Abstract)

Effect of the alpha 2-adrenergic antagonist yohimbine on orthostatic tolerance. We studied the effect of yohimbine, a drug that inhibits presynaptic alpha 2-adrenergic receptors and increases the neuronal release of norepinephrine from the central and sympathetic nervous systems, on tolerance to cardiovascular stress in 10 untrained, healthy subjects. Using radioligand binding of tritiated yohimbine to platelets, these subjects were found to have a normal complement of alpha 2-adrenergic

1990 Hypertension

2511. Effect of alpha-adrenergic blockers, ACE inhibitors, and calcium channel antagonists on renal function in hypertensive non-insulin-dependent diabetic patients. (Abstract)

Effect of alpha-adrenergic blockers, ACE inhibitors, and calcium channel antagonists on renal function in hypertensive non-insulin-dependent diabetic patients. In the present study we investigated the effect of a selective alpha 1-adrenergic blocker (doxazosin), an angiotensin-converting enzyme (ACE) inhibitor (captopril), and a calcium channel antagonist (nifedipine) on renal function in hypertensive non-insulin-dependent diabetic patients. 30 NIDD hypertensive patients (age = 50 +/- 3 years (...) ), and nifedipine (155 +/- 4/93 +/- 1) groups prior to the start of antihypertensive therapy and declined to 143 +/- 3/84 +/- 3 (doxazosin), 139 +/- 3/82 +/- 3 (captopril), and 141 +/- 3/84 +/- 1 (nifedipine) mm Hg (all p < 0.01 vs. pretreatment). In summary, both doxazosin and captopril treatment were associated with significant rises in GFR, while all three antihypertensive agents caused a significant decline in proteinuria. These results indicate that alpha-adrenergic blockers, ACE inhibitors, and calcium

1996 Nephron Controlled trial quality: uncertain

2512. Enhancement of morphine analgesia by the alpha 2-adrenergic antagonist yohimbine. (Abstract)

Enhancement of morphine analgesia by the alpha 2-adrenergic antagonist yohimbine. Although interactions between opioids and adrenergic agonists in the treatment of pain have been demonstrated in humans, the contribution of specific adrenergic receptors in this interaction remains to be clarified. In a double-blind, placebo-controlled study in male patients with postoperative dental pain, we investigated the effect of preoperative administration of the alpha 2-adrenergic antagonist, yohimbine (...) , on analgesia produced by postoperative intravenous morphine. Although yohimbine by itself did not affect the pain, the overall analgesic effect of morphine was significantly enhanced in the presence of yohimbine. This report is the first to demonstrate that an alpha 2-adrenergic antagonist enhances opiate analgesia in humans.

1995 Neuroscience Controlled trial quality: uncertain

2513. Buccal delivery of an alpha 2-adrenergic receptor antagonist, atipamezole, in humans. (Abstract)

Buccal delivery of an alpha 2-adrenergic receptor antagonist, atipamezole, in humans. To evaluate the pharmacokinetics, systemic effects and clinical applicability of buccally administered atipamezole in healthy volunteers.The study was carried out in two parts. In the first part, spray preparations of atipamezole hydrochloride in water/alcohol (50/50) solution were applied on buccal mucosa of six volunteers. Single doses of 5, 10, 20, and 40 mg atipamezole hydrochloride were administered

1995 Clinical pharmacology and therapeutics Controlled trial quality: uncertain

2514. Prokinetic effect of indoramin, an alpha-adrenergic antagonist, on human gall-bladder. (Abstract)

Prokinetic effect of indoramin, an alpha-adrenergic antagonist, on human gall-bladder. The effects of alpha- and beta-adrenergic agents on gall-bladder motility remain undefined.To determine the effects of alpha- and beta-antagonists on gall-bladder motility in healthy humans.In this single, blind, three-way crossover study, a slow-release formulation of propranolol 80 mg (beta-antagonist), indoramin 25 mg (post-synaptic alpha1-antagonist) and placebo were administered to 10 healthy volunteers (...) after the administration of propranolol was 17.49 +/- 2.37 mL and was not significantly different from placebo (16.50 +/- 2.78 mL). When the mean post-prandial gall-bladder volumes were compared, indoramin significantly enhanced post-prandial gall-bladder emptying compared to placebo (P < 0.001). There was no significant post-prandial volume difference between placebo and propranolol.Indoramin, an alpha-adrenergic antagonist, acts as a prokinetic agent, enhancing post-prandial gall-bladder emptying

2002 Alimentary pharmacology & therapeutics Controlled trial quality: uncertain

2515. [Platelet adrenergic alpha receptors in hypertensive subjects undergoing treatment with calcium antagonists]. (Abstract)

[Platelet adrenergic alpha receptors in hypertensive subjects undergoing treatment with calcium antagonists]. The effects of two different calcium-channel blocking agents on platelet alpha-2 adrenoceptors were studied in 18 mild to moderate hypertensive patients. The subjects were randomly assigned in a double blind fashion to treatment with either nifedipine 10 mg t.i.d. or tiapamil 300 b.i.d. for six weeks. Platelet alpha-2 receptors were studied before and following 6 weeks of treatment (...) using radioligand binding assay (3H Rauwolscine). Both agents induced a reduction in alpha-2 receptors, which reached statistical significance only for nifedipine. Such a reduction may contribute to the antihypertensive effect of calcium-channel blocking drugs.

1990 Bollettino della Società italiana di biologia sperimentale Controlled trial quality: uncertain

2516. Effects of alpha- and beta-adrenergic antagonists on plasma apolipoproteins and forearm blood flow in patients with mild hypertension. (Abstract)

Effects of alpha- and beta-adrenergic antagonists on plasma apolipoproteins and forearm blood flow in patients with mild hypertension. To study the mechanisms by which adrenergic antagonists affect blood pressure and plasma lipid levels, the effects of alpha-blockade with prazosin were compared with those of beta-blockade with propranolol in 23 normolipidemic, mildly hypertensive patients. Plasma lipoprotein composition, apolipoproteins, and some of the processes involved in lipid synthesis (...) of plasma lipoproteins, measurements were taken of forearm blood flow, forearm vascular resistance, and maximal forearm vasodilatory potential during reactive hyperemia. The adrenergic antagonists had no effect on these measurements, nor did they affect cellular cholesterol synthesis as measured by the activity of 3-hydroxy-3-methylglutaryl coenzyme A reductase in blood mononuclear cells. The results of this study demonstrate differing actions between alpha- and beta-adrenergic antagonism. Alpha

1989 The American journal of medicine Controlled trial quality: uncertain

2517. Effect on resting blood pressure and blood pressure homeostasis of short-term administration of the alpha 1-adrenergic receptor antagonist, trimazosin, in hypertension. (Abstract)

Effect on resting blood pressure and blood pressure homeostasis of short-term administration of the alpha 1-adrenergic receptor antagonist, trimazosin, in hypertension. The effects of trimazosin on blood pressure and cardiovascular homeostasis were studied in 12 subjects with untreated essential hypertension of mild or moderate degree. After a 3-day placebo period, the subjects were given trimazosin at the dose of 50, 100, or 200 mg twice daily (7 am and 7 pm) according to a randomized, double

1988 Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy Controlled trial quality: uncertain

2518. The inhibitory effect of a selective alpha 2-adrenergic receptor antagonist on moderate- to severe-type asthma. (Abstract)

The inhibitory effect of a selective alpha 2-adrenergic receptor antagonist on moderate- to severe-type asthma. Midaglizole (DG-5128), a novel selective alpha 2-adrenergic receptor antagonist, was administered to 17 patients with moderate to severe asthma in a single-dose, double-blind, randomized, crossover study. All patients also continued their regular treatment regimens. FEV1 increased significantly (p less than 0.05), and respiratory resistance decreased significantly (p less than 0.05 (...) ). Wheezing and dry rales on auscultation improved in patients receiving 200 mg of midaglizole, and their assessment of overall benefit was also significantly better (p less than 0.05). Blood pressure and heart rate were unaffected. However, plasma glucose levels fell slightly. This study demonstrated the bronchodilating effect of midaglizole in moderate to severe bronchial asthma. This selective alpha 2-adrenergic antagonist may prove to be a useful addition to current treatment regimens for asthma.

1989 The Journal of allergy and clinical immunology Controlled trial quality: uncertain

2519. Assessment of MK-467, a peripheral alpha 2-adrenergic receptor antagonist, with intravenous clonidine. (Abstract)

Assessment of MK-467, a peripheral alpha 2-adrenergic receptor antagonist, with intravenous clonidine. The activity of MK-467, a new peripherally acting alpha 2-antagonist, was assessed in volunteers by a randomized, double-blind, crossover design. One hour after administration of either 15 mg or 30 mg MK-467 or placebo, 200 micrograms clonidine was given intravenously and observations were made for a further 8 hours. Clonidine reduced plasma norepinephrine levels to 79% +/- 7 (...) than 0.05). Plasma insulin was suppressed by clonidine from 72 +/- 14 to 47 +/- 7 IU.L-1, an effect antagonised by both doses of MK-467 (p less than 0.05 in each case). MK-467 had no effect on clonidine-induced increased drowsiness, xerostomia, or increase in growth hormone secretion, which is consistent with it being a peripherally acting specific alpha 2-antagonist. The small effect of MK-467 on clonidine-induced changes in plasma glucose and insulin suggests that peripheral alpha 2-adrenergic

1991 Clinical pharmacology and therapeutics Controlled trial quality: uncertain

2520. A pharmacodynamic study of the alpha 2-adrenergic receptor antagonist ethoxyidazoxan in healthy volunteers. (Abstract)

A pharmacodynamic study of the alpha 2-adrenergic receptor antagonist ethoxyidazoxan in healthy volunteers. Ethoxyidazoxan, a potent and highly selective alpha 2-adrenergic receptor antagonist, was administered intravenously to six healthy male volunteers in a double-blind, placebo-controlled, dose-rising design. Doses of 6 micrograms/kg and 8 micrograms/kg infused intravenously over 30 minutes produced significant elevations of plasma norepinephrine and body temperature and inhibited

1994 Clinical pharmacology and therapeutics Controlled trial quality: uncertain

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