Benign Prostatic Hyperplasia – Prostate Cancer – Prostatitis

Posts Tagged ‘Tadalafil’

Phosphodiesterase 5 Inhibitors

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Overview PDE 5 inhibitors have traditionally been used to treat patients with ED; several compounds are already approved and marketed for that indication. Tadalafil (Eli Lilly cos's Cialis) is the first PDE 5 inhibitor under investigation for the treatment of benign prostatic hyperplasia. Tadalafil has great potential as a supplemental treatment for dynamic benign prostatic hyperplasia, a role that is not filled by any other drug. Mechanism Of Action Researchers propose that PDE 5 inhibitors have an effect on the contractibility of prostate smooth muscle. An examination of their effect on rapid ejaculation shows that these agents can improve the symptoms of benign prostatic hyperplasia by reducing the contractile response of prostatic and urethral tissues. A bovine model has demonstrated that decreased blood flow to the prostate causes localized muscle contraction; treatment with a PDE 5 inhibitor relaxed muscles in the ischemic tissues. Further research is required to fully understand the mechanism of action of PDE 5 inhibitors on the prostate gland. Tadalafil Icos's tadalafil is currently Read more [...]

Benign Prostatic Hyperplasia:Emerging Therapies

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The ultimate goal of treatment of benign prostatic hyperplasia and its associated comorbidities is to alleviate clinical symptoms that affect quality of life, eliminate the need for surgery, and prevent chronic and acute urinary retention. The challenge to drug developers is to create agents that have an acceptable onset of action, show a measurable level of efficacy, and induce no significant adverse events. The pipeline of agents in development for treatment of benign prostatic hyperplasia is relatively sparse. Most of the drugs currently under investigation are in early-stage development. Because benign prostatic hyperplasia is not a life-threatening disease, safety is a primary area of product improvement for new therapies. Physicians are not willing to accept drugs with frequent or significant side effects because benign prostatic hyperplasia is not life-threatening. Currently, the majority of pharmaceutical research for benign prostatic hyperplasia is focused on hormone therapy, as opposed to the established alpha-blocker and 5-alpha-reductase inhibitor (5-ARI) classes. The new gonadotropin Read more [...]

Drug Interactions in the Treatment of ED, LUTS and BPH: Clinically Relevant Drug­-Drug Interactions

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Clinically Relevant Drug­-Drug Interactions With the 5-Alpha-Reductase Inhibitors Neither dutasteride nor finasteride have any clinically significant pharmacodynamic or pharmacokinetic adverse drug interactions. Studies show that the 5-alpha-reductase inhibitors do not affect the CYP 450 enzyme system. However, agents that inhibit the CYP 450 3A4 may, in theory, interfere with metabolism of these medications. Therefore, until more data are available, cautious monitoring should follow the concurrent administration of a 5-alpha-reductase inhibitor with an agent known to alter the activity of the hepatic mixed function oxidase enzyme system. Pharmacodynamic Drug-Drug Interactions With PDE-5 Inhibitors Pharmacodynamic drug interactions leading to precipitous hypotension and MI are clinically relevant with PDE-5 inhibitors. All selective inhibitors of cyclic GMP-specific PDE-5 are prone to clinically significant pharmacodynamic interactions with agents that produce vasodilation. The concurrent use of nitrate preparations is a contraindication to treatment with selective inhibitors of cyclic GMP-specific Read more [...]

Drug Interactions in the Treatment of ED, LUTS and BPH: Clinically Significant Drug­-Drug Interaction

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The English-language medical literature, from 1986 to the present, was searched via the computer-based Medline system of the National Library of Medicine. The search focused on drug interaction data for the following agents: alfuzosin, doxazosin, dutasteride, finasteride, sildenafil, tamsulosin, tadalafil, terazosin, and vardenafil. Data were limited to information derived from studies of human subjects or actual patients and included premarketing and postmarketing observations. Articles reviewed included original studies, meta-analyses, and systematic reviews. Drug interactions were grouped into either pharmacodynamic interaction or pharmacokinetic interaction based on the mechanism. Pharmacodynamic Drug­-Drug Interactions With Selective Alpha-1-Adrenergic Receptor Blockers As a class, these agents potentiate hypotension when given concurrently with other antihypertensive agents. However, tamsulosin and alfuzosin do not cause a greater hypotensive effect when given concurrently with antihypertensive agents because tamsulosin and alfuzosin are highly selective for alpha-1-adrenergic receptors Read more [...]

Drug Interactions in the Treatment of ED, LUTS and BPH: Selective Cyclic GMP-Specific PDE-5 Inhibitors

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Pharmacodynamics PDE-5 inhibitors are indicated for the treatment of erectile dysfunction (ED). The physiological mechanism of penile erections involves the release of nitric oxide (NO) during sexual stimulation. Nnitric oxide activates guanylate cyclase to release copious amounts of cyclic guanosine monophosphate (GMP). Subsequently, nitric oxide and cyclic GMP cause the smooth muscle of the corpus cavernosum to relax, and as the corpus cavernosum fills with blood, the penis becomes erect. Unfortunately, the cause of erectile dysfunction in many patients is an imbalance between contraction and relaxation of the smooth muscle of the corpus cavernosum. Competitive inhibition of PDE-5 enzymes increases the intracellular stores of cyclic guanosine monophosphate and enhances the vasodilatory effects of nitric oxide. Subsequently, cyclic GMP relaxes corpus cavernosal smooth muscle cells and increases blood flow into cavernosal spaces. These changes enhance blood flow into the corpus cavernosum and increase intracavernosal pressure to produce a firm erection during sexual stimulation. Pharmacokinetics PDE-5 Read more [...]