Efficacy and positive benefit/risk of tamsulosin hydrochloride was not demonstrated in two studies conducted in patients 2 years to 16 years of age with elevated detrusor leak point pressure (,40 cm H2O) associated with known neurological disorder (e.g., spina bifida). Patients in both studies were treated on a weight-based mg/kg schema (0.025 mg, 0.05 mg, 0.1 mg, 0.2 mg, or 0.4 mg tamsulosin hydrochloride) for the reduction in detrusor leak point pressure below 40 cm H2O. In a randomized, double-blind, placebo-controlled, 14-week, pharmacokinetic, safety and efficacy study in 161 patients, no statistically significant difference in the proportion of responders was observed between groups receiving tamsulosin hydrochloride and placebo. In an open-label, 12-month safety study, 87 patients were treated with tamsulosin hydrochloride. The most frequently reported adverse events (≥5%) from the pooled data of both studies were urinary tract infection, vomiting, pyrexia, headache, nasopharyngitis, ...
Dutasteride: Following administration of a single 0.5 mg dose of a soft gelatin capsule, time to peak absolute bioavailability in 5 healthy subjects is approximately 60% (range: 40% to 94%). Tamsulosin: Absorption of tamsulosin is essentially complete (,90%) following oral administration of 0.4 mg tamsulosin hydrochloride capsules under fasting conditions. Tamsulosin exhibits linear kinetics following single and multiple dosing, with achievement of steady-state concentrations by the fifth day of once-daily dosing. Effect of Food Food does not affect the pharmacokinetics of dutasteride following administration of dutasteride and tamsulosin hydrochloride capsules. However, a mean 30% decrease in tamsulosin Cmax was observed when dutasteride and tamsulosin hydrochloride capsules was administered with food, similar to that seen when tamsulosin monotherapy was administered under fed versus fasting conditions. Distribution Dutasteride: Pharmacokinetic data following single and repeat oral doses show ...
This study will investigate the efficacy and safety of treatment with Dutasteride (0.5mg), administered once daily for one year in combination with Tamsulosin (0.4mg), administered once daily for 3 months, followed by counseling on flexible dosing of Tamsulosin on an as needed basis, on the improvement of symptoms and clinical outcome in men with moderate to severe symptomatic benign prostatic hyperplasia (BPH). At each scheduled visit (3, 6, and 9 months), the subject will be counseled on withdrawal of Tamsulosin.. A recently published, landmark study (MTOPS - Medical Therapy of Prostatic Symptoms), co-sponsored by the National Institute of Health and the National Institute of Diabetes, Digestive and Kidney Diseases (NIH-NIDDK), demonstrated that, in selected patients, combination therapy with Doxazosin and Finasteride provided additive symptomatic improvements, reduced the risk of acute urinary retention (AUR) and surgical intervention, and was a more effective treatment for reduction in the ...
The primary objective of the study is to demonstrate the superiority of SL77.0499-10 10mg once daily over placebo and the non-inferiority versus tamsulosin hydrochloride after 12 weeks treatment in terms of the efficacy in patients with lower urinary tract symptoms related to BPH.. The secondary objective is to assess the safety of SL77.0499-10 in patients with lower urinary tract symptoms related to BPH in comparison with placebo and tamsulosin hydrochloride. ...
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Astellas Pharma this morning said it has begun legal proceedings against several Spanish generics companies for infringing its patent for Omnic (tamsulosin hydrochloride), which is also available in the country under the brand name Urolosin, manufactured by partner Boehringer Ingelheim. - News - PharmaTimes
This project will determine if tamsulosin is useful in patients with a kidney stone. Tamsulosin is used for patients with an enlarged prostate gland, but it has...
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Chapter 10. Adrenoceptor Blockers. In: Trevor AJ, Katzung BG, Kruidering-Hall MM, Masters SB. Trevor A.J., Katzung B.G., Kruidering-Hall M.M., Masters S.B. Eds. Anthony J. Trevor, et al.eds. Katzung & Trevors Pharmacology: Examination & Board Review, 10e New York, NY: McGraw-Hill; 2013. http://accesspharmacy.mhmedical.com/content.aspx?bookid=514§ionid=41817522. Accessed December 10, 2017 ...
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Tamsulosin is a prescription medicine used to treat the medical condition known as benign prostatic hyperplasia (more commonly referred to as enlarged prostate), which affects males.
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Forray C; Bard JA; Wetzel JM; et al. (1994). „The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype.. Mol. Pharmacol. 45 (4): 703-8. PMID 8183249 ...
Alfuzosin, som er et racemat, er et oralt virkende quinazolinderivat, som selektivt blokerer postsynaptiske α1-receptorer. De kliniske symptomer ved benign prostatahypertrofi er ikke kun relateret til størrelsen af prostata, men også til sympatomimetiske nerveimpulser, da stimulation af de postsynaptiske α-receptorer øger spændingen i den glatte muskulatur i de nedre urinveje. Behandling med alfuzosin virker afslappende på muskulaturen i prostata og urethra og forbedrer dermed urinflowet. ...
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Terazosin should be taken in the form of capsules orally . The dosage can be two capsules per day, or one capsule per day before bedtime.. Your doctor may decide to gradually increase the initial prescription dosage.. ...
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Elworthy, T. R., Ford, A. P. D. W., Bantle, G. W., Morgans Jr., D. J., Ozer, R. S., Palmer, W. S., Repke, D. B., Romero, M., Sandoval, L., Sjogren, E. B., Talamas, F. X., Vazquez, A., et al. N-arylpiperazinyl-N-propylamino derivatives of heteroaryl amides as functional uroselective alpha(1)-adrenoceptor antagonists Journal of Medicinal Chemistry 1997 40:2674-2687 DOI:10.1021/jm970166j PMID:9276013 ...
The invention relates to processes for the preparation of alfuzosin or pharmaceutically acceptable salts thereof in high purity. More particularly, it relates to the preparation of pure crystalline a
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Background: Some α1-adrenoceptor antagonists possess anti-cancer actions that are independent of α1-adrenoceptors and the aim of these studies was to assess the relative cytotoxic potencies of α1-adrenoceptor antagonists and the mechanisms involved in these actions. Methods: PC-3 and LNCap human prostate cancer cells were exposed to α1-adrenoceptor antagonists (0.01-100μM) and cell survival assessed after 24-72hr. The levels of apoptosis, autophagy and stress related proteins were also determined. Results: The relative cytotoxic potency order was prazosin=doxazosin|terazosin=silodosin=alfuzosin|tamsulosin on both cell types, but LNCaP cells were significantly more sensitive to these effects than PC-3 cells. Prazosin and doxazosin increased levels of apoptotsis and autophagy in both cell lines, and activated EphA2 receptors in PC-3 cells. Autophagy contributed to survival of LNCaP, but promoted cell death in PC-3 cells. Treatment with prazosin (30μM) altered the expression of several cell stress
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After depletion of intracellular calcium stores sensitive to noradrenaline, a spontaneous increase in the resting tone (IRT) when incubated in Ca2+-containing solution was observed in isolated rat aorta, but not in tail artery. This IRT does not depend on agonist activation of α1-adrenoceptors but it is inhibited by prazosin. A close relationship was found between the inhibitory potencies of prazosin (pIC50 = 9.833), BMY 7378 (pIC50 = 8.924), and 5-methylurapidil (pIC50 = 7.883) against IRT and their affinities for cloned α1D-adrenoceptors. Chloroethylclonidine (100 μmol · l−1) did not inhibit the IRT. After depletion of internal calcium stores by noradrenaline in absence of the agonist, loading in Ca2+-containing solution also brings about an increase in the inositol phosphate (IP) levels in rat aorta (not seen in tail artery) that is inhibited by prazosin (1 μmol · l−1), BMY 7378 (10 μmol · l−1), and 5-methylurapidil (10 μmol · l−1), thus confirming the results obtained in ...
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Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.. The incidence of adverse reactions has been ascertained from 3 placebo-controlled clinical trials involving 1,608 men where daily doses of 10 and 15 mg alfuzosin were evaluated. In these 3 trials, 473 men received UROXATRAL (alfuzosin HCl) 10 mg extended-release tablets. In these trials, 4% of patients taking UROXATRAL (alfuzosin HCl) 10 mg extended-release tablets withdrew from the trial due to adverse reactions, compared with 3% in the placebo group.. Table 1 summarizes adverse reactions that occurred in ≥2% of patients receiving UROXATRAL, and at a higher incidence than that of the placebo group. In general, the adverse reactions seen in long-term use were similar in type and frequency to the events described below for ...
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