Disease relevance of C07124

• These findings demonstrate the ability of doxazosin and terazosin (but not tamsulosin) to suppress prostate cancer cell growth in vitro and in vivo by inducing apoptosis without affecting cell proliferation [1].
• Tamsulosin. A review of its pharmacological properties and therapeutic potential in the management of symptomatic benign prostatic hyperplasia [2].
• The overall incidence of symptoms indicative of orthostasis was 1.4% with tamsulosin 0.4 or 0.8 mg/day treatment [3].
• alpha(1)-Adrenoceptor antagonists such as alfuzosin, doxazosin, tamsulosin and terazosin are first-line agents for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia (BPH), but are only second-line agents (doxazosin and terazosin only) for the treatment of arterial hypertension [4].
• CONCLUSION: Tamsulosin, an alpha1-adrenoceptor antagonist, has a well established place in the treatment of LUTS and has a tolerability profile similar to that of placebo (apart from a higher incidence of abnormal ejaculation, dizziness and rhinitis) [3].

Psychiatry related information on C07124

• Whereas tamsulosin is associated only with ejaculatory dysfunction, finasteride is additionally linked to decreased libido and impotence [5].
• Tamsulosin also significantly improved the mean total BSIA score and the mean Total Mental Health Rate [6].

High impact information on C07124

• CONCLUSION: These results suggest that although the alpha1-adrenergic receptor-blocking effect of tamsulosin on blood vessels is relatively small, it is clearly correlated with plasma drug concentration and a higher dose of the drug could cause systemic adverse effects [7].
• Tamsulosin concentrations in the aqueous humor and serum were analyzed [8].
• Tamsulosin concentrations varied between 0.1 and 1.0 ng/mL in the anterior chamber fluid [8].
• RESULTS: Each patient administered tamsulosin had a sluggish hypotonic iris, along with a tendency toward miosis and a tendency for prolapse of the iris into the phaco tunnel or into the side port during cataract surgery [8].
• CONCLUSIONS: Tamsulosin has selective alpha1A-adrenoreceptor antagonistic properties and obviously binds for a long period to the postsynaptic nerve endings of the iris dilator muscle, thus affecting iris dilatation and leading to complications in cataract surgery [8].

Chemical compound and disease context of C07124

• BACKGROUND: Terazosin and tamsulosin are drugs currently used in the treatment of benign prostatic hypertrophy (BPH) [9].
• PURPOSE: To evaluate the effectiveness of prophylactic tamsulosin (Flomax) in reducing the urinary symptoms in patients undergoing 125I prostate implantation (PI) for prostate adenocarcinoma [10].
• Treatment of the androgen-independent human prostate cancer cells PC-3 with doxazosin resulted in a strong caspase-3 activation within 24 h, whereas tamsulosin, a sulphonamide-based alpha 1-adrenoceptor antagonist, had no significant apoptotic effect against prostate cancer cells [11].
• Randomized trial of the efficacy of tamsulosin, nifedipine and phloroglucinol in medical expulsive therapy for distal ureteral calculi [12].
• There was no difference between tamsulosin and placebo or alfuzosin with regard to the occurrence of decreased libido or impotence [13].

Biological context of C07124

• In contrast, blood pressure is significantly reduced by alfuzosin compared with tamsulosin [2].
• Furthermore, blood pressure and heart rate are not significantly affected by tamsulosin in patients with symptomatic BPH [2].
• In the present study the pharmacokinetics and pharmacodynamics of tamsulosin were investigated in anesthetized male dogs [14].
• PURPOSE: We investigated the effect of the alpha-blockers alfuzosin, terazosin and tamsulosin on urodynamic parameters after 6 months of therapy [15].
• [3H]-silodosin binding sites also showed high affinity for silodosin and tamsulosin but low sensitivity to BMY 7378 (8-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-8-azaspiro(4.5)decane-7,9-dione) (Research Biochemicals International) in intact segments and in membrane preparations [16].

Anatomical context of C07124

• Tamsulosin: an update of its role in the management of lower urinary tract symptoms [3].
• Tamsulosin is the first subtype-selective (alpha IA) alpha 1 adrenoceptor antagonist with specificity for prostatic alpha 1 adrenoceptors (alpha 1A adrenoceptors are thought to be involved in prostatic smooth muscle contraction) to become available for the treatment of patients with symptomatic benign prostatic hyperplasia (BPH) [2].
• MATERIALS AND METHODS: A total of 60 consecutive symptomatic patients with stones located in the juxtavesical tract of the ureter were randomly divided into group 1--30 who received oral floroglucine-trimetossibenzene 3 times daily and group 2--30 who received 0.4 mg tamsulosin daily [17].
• PURPOSE: We evaluated the efficacy and safety of tamsulosin in patients with neurogenic lower urinary tract dysfunction secondary to suprasacral spinal cord lesions in a 4-week randomized controlled trial (RCT) followed by a 1-year, open label, long-term study [18].
• Improvement in bladder storage function by tamsulosin depends on suppression of C-fiber urethral afferent activity in rats [19].

Associations of C07124 with other chemical compounds

• In this model, Rec 15/2739 had greater selectivity than any other alpha-1 AR antagonist examined, including terazosin and tamsulosin [20].
• In addition to the weak antagonism of PHE-induced blood pressure responses, A-131701 also exhibited minimal effects on basal blood pressure in the dog, unlike terazosin, doxazosin or tamsulosin [21].
• After 4 weeks a pressure flow study was done and the effects of the alpha(1)-adrenoceptor antagonists KMD-3213 silodosin, tamsulosin and prazosin on urodynamics were compared [22].
• PURPOSE: We evaluate the effect of tolterodine combined with tamsulosin on quality of life in patients with bladder outlet obstruction and concomitant detrusor instability [23].
• Prophylactic tamsulosin (Flomax) in patients undergoing prostate 125I brachytherapy for prostate carcinoma: final report of a double-blind placebo-controlled randomized study [10].

Gene context of C07124

• 4. It is concluded that formation of tamsulosin metabolites, AM-1 and M-1, is catalysed by CYP3A4 whereas that of M-3 and M-4 is catalysed by CYP2D6 [24].
• Comparison of the affinities of these alpha-1-adrenoceptor antagonists at the cloned alpha-1a, alpha-1b and alpha-1d-adrenoceptor subtypes revealed that tamsulosin and 5-Me-urapidil showed selectivity for the alpha-1a subtype [25].
• We conclude that most tamsulosin metabolites are high potency antagonists at the alpha-1 adrenoceptors and retain the alpha-1A over the alpha-1B adrenoceptor selectivity of tamsulosin [26].
• 3. At the alpha 1B-adrenoceptor of the rat spleen and rabbit corpus cavernosum penis, tamsulosin again acted as a competitive antagonist but with a significantly lower affinity (pKB = 8.9-9.2) [27].
• The effects of tamsulosin, a high affinity antagonist at functional alpha 1A- and alpha 1D-adrenoceptor subtypes [27].

Analytical, diagnostic and therapeutic context of C07124

• Tamsulosin is available as a controlled release formulation suitable for once daily administration; dose titration is not required [2].
• Tamsulosin 0.4 and 0.8 mg/day in a modified-release formulation was significantly more effective than placebo in large (n >250) double-blind, randomised, multicentre, 12- to 13- week clinical trials in patients with LUTS [3].
• With the exception of a numberically greater incidence of abnormal ejaculation, dizziness and rhinitis, the incidence of adverse events with tamsulosin 0.4 mg/day was similar to that seen with placebo in randomised, double-blind studies [3].
• However, tamsulosin is unlikely to produce orthostatic hypotensive adverse effects or interfere with concomitant antihypertensive drug therapy [3].
• Moreover, 12, 18, and 24 h after the oral administration of KMD-3213, a dose-dependent inhibition of the IUP response was found, whereas the effect of tamsulosin disappeared at 18 h after the oral administration [28].

References