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1.
Drug Des Devel Ther ; 16: 2861-2884, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36051157

RESUMO

Use of α-androgenic receptor blockers remains a mainstay therapeutic approach for the treatment of urological diseases. Silodosin is recommended over other α-blockers for the treatment of lower urinary tract symptoms (LUTS) and benign prostate hyperplasia (BPH), due to its high α1A uroselectivity. Current research data suggest that silodosin is efficacious in the management of various urological diseases. Thus, we herein review the current evidence of silodosin related to its efficacy and tolerability and appraise the available literature that might ultimately aid in management of various urological conditions at routine clinical practice. Literature reveals that silodosin is beneficial in improving nocturia events related to LUTS/BPH. Silodosin exerts effect on relaxing muscles involved in detrusor obstruction, therefore prolonging the need for patients undergoing invasive surgery. Silodosin treatment, either as a monotherapy or combination, significantly improves International Prostate Symptom Score (IPSS) including both storage and voiding symptoms in patients with BPH/LUTS. Patients on other treatment therapies such as phosphodiesterase 5 inhibitors or other α-blockers are well managed with this drug. Steadily, silodosin has proved beneficial in the treatment of other urological disorders such as chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS), overactive bladder/acute urinary retention (AUR), premature ejaculation (PE), and prostate cancer post brachytherapy-induced progression. In patients with distal ureteral stones, silodosin treatment is beneficial in decreasing stone expulsion time without affecting stone expulsion rate or analgesic need. Moreover, there were significant improvements in intravaginal ejaculation latency time, quality of life scores, and decrease in PE profile among patients with PE. Silodosin has also demonstrated promising results in increasing the likelihood of successful trial without catheter in patients with AUR and those taking antihypertensive drugs. Reports from Phase II studies have shown promising role of silodosin in the treatment of CP/CPPS as well as facilitating ureteral stone passage. From the robust data in this review, further silodosin treatment strategies in the management of different urological conditions need to be focused on.


Assuntos
Sintomas do Trato Urinário Inferior , Hiperplasia Prostática , Doenças Urológicas , Agentes Urológicos , Antagonistas de Receptores Adrenérgicos alfa 1/efeitos adversos , Humanos , Indóis , Sintomas do Trato Urinário Inferior/induzido quimicamente , Sintomas do Trato Urinário Inferior/tratamento farmacológico , Masculino , Hiperplasia Prostática/tratamento farmacológico , Qualidade de Vida , Resultado do Tratamento , Doenças Urológicas/induzido quimicamente , Doenças Urológicas/tratamento farmacológico , Agentes Urológicos/efeitos adversos
2.
J Control Release ; 93(3): 293-300, 2003 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-14644579

RESUMO

Colon-specific drug delivery systems (CDDSs) can be used to improve the bioavailability of protein and peptide drugs through the oral route. A novel formulation for oral administration using coated calcium alginate gel beads-entrapped liposome and bee venom peptide as a model drug has been investigated for colon-specific drug delivery in vitro. Drug release studies under conditions mimicking stomach to colon transit have shown that the drug was protected from being released completely in the physiological environment of the stomach and small intestine. The release rate of bee venom from the coated calcium alginate gel beads-entrapped liposome was dependent on the concentration of calcium and sodium alginate, the amount of bee venom in the liposome, as well as the coating. Furthermore, a human gamma-scintigraphy technique was used in vivo to determine drug delivery more precisely. The colonic arrival time of the tablets was found to be 4-5 h. The results clearly demonstrated that the coated calcium alginate gel beads-entrapped liposome is a potential system for colon-specific drug delivery.


Assuntos
Alginatos/administração & dosagem , Venenos de Abelha/administração & dosagem , Colo/efeitos dos fármacos , Sistemas de Liberação de Medicamentos/métodos , Ácido Glucurônico/administração & dosagem , Ácidos Hexurônicos/administração & dosagem , Administração Oral , Adulto , Alginatos/química , Alginatos/farmacocinética , Venenos de Abelha/química , Venenos de Abelha/farmacocinética , Colo/metabolismo , Géis , Ácido Glucurônico/química , Ácido Glucurônico/farmacocinética , Ácidos Hexurônicos/química , Ácidos Hexurônicos/farmacocinética , Humanos , Lipossomos , Masculino , Microesferas
3.
J Pharm Pharmacol ; 55(10): 1359-63, 2003 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-14607017

RESUMO

A simple and reproducible enzyme-linked immunosorbent assay (ELISA) was developed to determine the concentration of bee venom in rat plasma. The intra- and inter-assay coefficients of variation for the ELISA were less then 3% between 0.1 and 1,000 ng mL(-1) venom, and the sensitivity of the detection was 0.1 ng mL(-1). Total recovery of the bee venom added to rat plasma was determined. Using this ELISA, serum levels of bee venom were easily determined. The rats were administered a single intravenous injection or oral dose of bee venom (1 mg kg(-1) of body weight). The bioavailability of the bee venom under the two administrations was compared using pharmacokinetic parameters. Results showed that intravenous administration of bee venom produced high plasma concentrations with a short half-life. The area under the curve for oral administration was 10 times lower than for intravenous administration. This loss of bee venom may be due to the degradation that occurs in the enzymatic and acidic environment of the gastrointestinal tract.


Assuntos
Venenos de Abelha/análise , Venenos de Abelha/farmacocinética , Ensaio de Imunoadsorção Enzimática/métodos , Administração Oral , Animais , Venenos de Abelha/administração & dosagem , Sistema Digestório/química , Meia-Vida , Infusões Intravenosas , Masculino , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes
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