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Pharmacology of the Lower Urinary Tract
Published in Karl H. Pang, Nadir I. Osman, James W.F. Catto, Christopher R. Chapple, Basic Urological Sciences, 2021
Pedro Abreu-Mendes, João Silva, Francisco Cruz
Only two of the drugs are considered selective:Silodosin: alpha-1A.Naftopidil: moderate alpha-1D selectivity.
Complementary and Alternative Medicine in Older Adults
Published in K. Rao Poduri, Geriatric Rehabilitation, 2017
In 2007, a randomized multicenter clinical trial of over 900 BPH patients was conducted from September 2002 to December 2003 across seven therapeutic drug groups, including selective adrenoceptor antagonist (terazosin, doxazosin, tamsulosin, naftopidil), 5-alpha-reductase inhibitor (finasteride, epristeride), and natural product (cernilton, prepared from Secale cereale [rye] pollen). According to baseline, at average follow-up of 6 months, no difference in the International Prostate Symptom Score was noted across the therapeutic intervention groups. However, prostatic volume and transitional zone volume were significantly decreased in the 5-alpha-reductase inhibitor group, and more significant symptomatic improvements were noted in the cernilton, doxazosin, and naftopidil groups.190
Dementia and lower urinary tract dysfunction
Published in Jacques Corcos, David Ginsberg, Gilles Karsenty, Textbook of the Neurogenic Bladder, 2015
α1-Adrenergic antagonists such as prazosin, terazosin, doxazosin, alfuzosin, silodosin, etc. are effective in the symptomatic management of benign prostatic hypertrophy. However, adverse effects of α1-adrenergic blockers may limit their use in frail elderly patients such as those with orthostatic hypotension. The proximal urethra has an abundance of α1A–D adrenergic receptors. In contrast, the vascular wall has an abundance of α1B receptors, particularly in the elderly.104 Prazosin may block both α1B receptors in the vascular wall and α1A-D receptors in the proximal urethra. Selective α1A–D adrenergic blockers, such as tamsulosin hydrochloride and naftopidil, are the drugs of choice because they have fewer side effects.
Optimization of lipid materials in the formulation of S-carvedilol self-microemulsifying drug-delivery systems
Published in Drug Development and Industrial Pharmacy, 2020
Qi Zhang, Kunkun Guo, Xin Wang, Baolin Huang, Zimin Lin, Zheng Cai
S-CAR was provided by School of Pharmaceutical Sciences, Southern Medical University (Guangzhou, China). Naftopidil was purchased from National Institute for the Control of Pharmaceutical and Biological Products (Beijing, China). Peceol and Labrafil M1944CS were kind gift samples from Gattefosse (Lyon, France). Oleic acid 85%, olein, and α-tocopherol were purchased from Aladin (Shanghai, China). Soybean lecithin was purchased from Tywei Pharmaceutical Co., Ltd. (Shanghai, China). Hanks’ balanced salt solution (HBSS; powder form) was supplied from Sigma-Aldrich (St. Louis, MO). Methanol and acetonitrile were from Merck (Darmstadt, Germany). Tween 80 and ethanol were obtained from Sinopharm Chemical reagent (Shanghai, China). Deionized water (DDW) was provided by Milli-Q (Millipore, Bedford, MA). All other chemicals were of analytical grade or better.
Established and recent developments in the pharmacological management of urolithiasis: an overview of the current treatment armamentarium
Published in Expert Opinion on Pharmacotherapy, 2020
Mohamed Abou Chakra, Athanasios E. Dellis, Athanasios G. Papatsoris, Mohamad Moussa
Alpha-blockers tend to decrease intra-ureteral pressure and increase fluid passage which might increase stone passage. A meta-analysis of 32 Randomized clinical trials (RCTs (5864 patients) reported significantly higher stone-free rates in the alpha-blocker group compared to the standard therapy. Also, the number of pain episodes, the need for analgesic medication and hospitalization were less in the alpha-blocker group but with a higher rate of mild adverse effects [16]. Another meta-analysis of 11 RCTs (911 patients) reported a 44% higher likelihood of spontaneous stone passage with α-blockers compared with no treatment [17]. Tamsulosin has been the most studied alpha-blocker in the MET. When testing the alpha1-Adrenergic blockers classes, tamsulosin, terazosin and doxazosin showed similar efficacy on the spontaneous rate of stone passage [18]. Selective alpha1D-blocker naftopidil can significantly facilitate spontaneous passage of distal ureteral stones [19]. A meta-analysis of eight RCTs with a total of 1145 patients knowing to have ureteral stones investigated the efficacy of silodosin in MET has been demonstrated that silodosin provided a significantly higher expulsion rate (RR: 1.25; 95% CI, 1.13–1.37; P < 0.0001) than tamsulosin for distal ureteral stones [20].
Development and evaluation of rapidly dissolving buccal films of naftopidil: in vitro and in vivo evaluation
Published in Drug Development and Industrial Pharmacy, 2019
Heba I. Elagamy, Ebtessam A. Essa, Ahmed Nouh, Gamal M. El Maghraby
Naftopidil is a poor water soluble weakly basic drug with a pKa of 7.3 [5]. It is classified as a class IV drug according to the Biopharmaceutical Classification System due to its poor solubility and limited intestinal permeability. In addition, naftopidil has been shown to exhibit extensive presystemic metabolism. These factors are responsible for the reported low bioavailability (17%) after oral administration [6]. Accordingly, enhancing the dissolution rate and the membrane permeability can overcome the problems contributing to the poor bioavailability after oral administration. The benefits will become even greater if the delivery system can be delivered to a specific site which avoids the presystemic metabolism. Alternative strategies have been adopted to enhance dissolution and solubility of naftopidil. For example, authors employed solid dispersions with cyclodextrin to enhance the solubility and dissolution via inclusion complexation with rapidly disintegrating tablets being prepared as well [7,8].