Pharmacokinetics of terazosin

Sonders, Robert C.

doi:10.1016/0002-9343(86)90847-8

Cited by 72 publications

(40 citation statements)

References 6 publications

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“…Blockade of alpha-1 receptors provides a rational approach to the treatment of hypertension by inhibiting the binding of noradrenaline, thereby promoting smooth muscle cell relaxation, reduced vascular tone and decreased peripheral resistance [28]. Early tolerability issues, for example, due to postural hypotension associated with unfavourable pharmacokinetics of immediate-release drugs, have been largely overcome by the development of controlledrelease formulations, such as prazosin and doxazosin gastrointestinal therapeutic system (GITS) [29][30][31][32]. Such formulations have been designed to improve the drugs' pharmacokinetic profiles and to minimize side effects by slowing absorption and reducing fluctuations in plasma concentration [30].…”

Section: Mechanism Of Action Of Alpha-blockersmentioning

confidence: 99%

Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?

Chapman

Chen

Fujita

et al. 2010

Journal of Hypertension

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The role of alpha-1 adrenoceptor antagonists (alpha-blockers) in the management of hypertension continues to evolve. Recent data support their use as add-on therapy in uncontrolled hypertension when used in combination with all other major classes of antihypertensive drug and there is increasing evidence suggesting that they have modest but significant beneficial effects on lipid and glucose metabolism. The availability of extended-release formulations has contributed to an excellent tolerability profile. New data from an observational analysis of the Anglo-Scandinavian Cardiac Outcomes Trial (ASCOT) suggest that doxazosin gastrointestinal therapeutic system (GITS) used as a third-line antihypertensive agent lowered blood pressure and caused modest reductions in plasma lipids. Furthermore, use of doxazosin in ASCOT was not associated with an increased risk of heart failure, in contrast to the earlier finding of the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT). Overall, currently available data support the use of alpha-blockers as safe, well tolerated and effective add-on antihypertensive drugs, which have additional favourable metabolic effects.

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Section: Mechanism Of Action Of Alpha-blockersmentioning

confidence: 99%

Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?

Chapman

Chen

Fujita

et al. 2010

Journal of Hypertension

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“…Terazosin has an oral bioavailability of approximately 90 % which seems unaffected by age or the presence of congestive heart failure (88). The compound's plasma half-life is considerably longer than prazosin, at 10-12 h (88,89), and is similar in older patients (88).…”

Section: Once-daily Q U I N a Z O L I N E A-1 A D R E N O C E P T O Rmentioning

confidence: 99%

“…Terazosin's pharmacokinetics are unaffected by renal impairment (89) and both drugs seem to improve renal blood flow (89,93). The prolonged half-life and almost complete bioavailability of terazosin are presumably due to its much increased water solubility; the furan ring of prazosin is hydrogenated in terazosin, leading to a hydrophilicity some 25 times greater than the prototype (27,88). Although doxazosin is also found to have a longer half-life than prazosin, the benzodioxan moiety may not be as water-soluble as the tetrahydrofuran group in terazosin.…”

Section: Once-daily Q U I N a Z O L I N E A-1 A D R E N O C E P T O Rmentioning

confidence: 99%

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Alpha-1 Blockers. A New Generation of Antihypertensive Agents

Humphreys

Waite

1989

J Clin Pharm Ther

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SUMMARYAlpha-1 blockers have certain disadvantages over conventional and antihypertensive therapies in their haemodynamic profile and metabolic effects.This paper reviews the development of a-blockade, the therapeutic efficacy of prazosin, the prototype a-1 blocker, and the rationale for the oncedaily antihypertensive compounds, terazosin and doxazosin. These drugs offer a useful alternative to first-or second-line therapy in suitable hypertensive patients, particularly with their potentially beneficial effects on serum lipids.

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“…They are also used to treat hypertension via reduction of total peripheral resistance by selective postsynaptic ␣1 blockade [36,37]. The pharmacology of both drugs has been well characterized in human and animal models [38][39][40], and their safety profile has been characterized with acceptable side effects such as dizziness, headache, and hypotension [41,42]. The adverse effects have been mild or moderate.…”

Section: Introductionmentioning

confidence: 99%

Induction of apoptosis in the prostate by α1-adrenoceptor antagonists: A novel effect of “Old” drugs

Kyprianou

Jacobs²

2000

Curr Urol Rep

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Advances in our understanding of the integrated functions governing prostate cell proliferation and cell death imply that effective therapies for prostate neoplasia should not only be molecularly targeted, but should be customized to take into account the delicate balance of opposing growth influences. Evidence from studies on the dynamics of prostate growth in benign prostatic hyperplasia (BPH) and prostate cancer established that disruption of the molecular mechanisms that regulate apoptosis and cell proliferation among the stroma and epithelial cell populations may underlie the neoplastic development that characterizes the aging gland. Our own efforts have been focused on investigating whether a1-adrenoceptor antagonists clinically used for the relief of the obstructive symptoms associated with BPH affect prostate pathophysiology via mechanisms other than smooth muscle contraction. Such efforts led to the identification of a novel effect of two alpha1-adrenoceptor antagonists, doxazosin and terazosin. More recent in vitro experiments examined the potential anti-tumor action of three clinically used alpha1-adrenoceptor antagonists--doxazosin, terazosin and tamsulosin--against prostate cancer cell growth. These findings demonstrate the ability of doxazosin and terazosin, but not tamsulosin, to suppress prostate growth by inducing apoptosis among the epithelial cells in the benign and malignant prostate. Thus, evidence indicates that rather than just causing pure relaxation of the smooth muscle, certain alpha1-blockers can also affect the dynamics of prostate growth by changing the balance between prostate cell proliferation and apoptosis at the expense of the proliferative process.

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Pharmacokinetics of terazosin

Cited by 72 publications

References 6 publications

Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?

Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?

Alpha-1 Blockers. A New Generation of Antihypertensive Agents

Induction of apoptosis in the prostate by α1-adrenoceptor antagonists: A novel effect of “Old” drugs

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