Drugs online research references
Am J Med. 1986 May 23;80(5B):94-9.
Influence of renal insufficiency on the pharmacokinetics and pharmacodynamics of terazosin.
Jungers P, Ganeval D, Pertuiset N, Chauveau P.
Renal insufficiency was not shown to affect the pharmacokinetics of terazosin in fifteen patients receiving oral terazosin (1 mg once daily) for two weeks. Five patients had normal renal function (creatinine clearance 80 ml per minute or more), five had moderate renal insufficiency (creatinine clearance 30 to 79 ml per minute), and five had severe renal insufficiency (creatinine clearance 10 to 29 ml per minute). Urine and blood samples were collected, and blood pressure and pulse rate were determined on days one and 15 of the study. Renal insufficiency had no significant effect on the absorption lag time, rate of absorption, rate of elimination in the urine, volume of distribution, or plasma clearance of terazosin. The plasma half-life of terazosin in patients with normal renal function was 10.0 hours, compared with 8.4 hours in patients with moderate renal insufficiency and 9.8 hours in the group with severe renal insufficiency. There was also no apparent relationship between renal insufficiency and the maximum change in blood pressure or pulse rate. Renal excretion was found to play a minor role in the elimination of terazosin, and this explains the lack of a relationship between renal insufficiency and the pharmacodynamics of terazosin. After the administration of terazosin on day 1 of the study, 1.6 +/- 0.3 percent and 5.1 +/- 1.4 percent of the total dose was excreted in the urine of patients with severe renal insufficiency and normal renal function, respectively. Adverse experiences were reported by four patients and caused one patient to withdraw from the study. Symptoms reported included gastralgia, headache, dizziness, malaise, weakness, and palpitations. The results of this study indicate that terazosin may be safely administered to patients with renal insufficiency without altering the usual dosing regimen.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2872815&dopt=Abstract
Cardiology. 1986;73(3):164-74.
Clinical pharmacology and therapeutic role of prazosin and related alpha-adrenoceptor antagonists.
Reid JL, Vincent J.
Prazosin is a quinazoline derivative, which lowers blood pressure by selective alpha-1-receptor antagonism. It has been found that, for similar decreases in blood pressure, prazosin causes less reflex tachycardia than non-selective alpha blockers or direct vasodilators, and that it is as efficacious as other conventional antihypertensive agents (alpha-methyldopa, hydralazine, beta blockers, etc.) in controlling severe hypertension. Prazosin causes a dose-related decrease in blood pressure in humans; twice-daily dosing is sufficient for 24-hour blood pressure control. Prazosin in combination with other drugs has also been shown to control blood pressure effectively, and it has been associated with relatively few side effects. Other agents with selective alpha-1-receptor-blocking activity are under investigation: these include doxazosin, trimazosin, terazosin, and alfuzosin.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2872958&dopt=Abstract
Am J Med Sci. 1986 Sep;292(3):128-35.
The hemodynamic and clinical responses to terazosin, a new alpha blocking agent, in congestive heart failure.
Leier CV, Patterson SE, Huss P, Parrish D, Unverferth DV.
To determine the hemodynamic effects of a new alpha 1 blocker, terazosin, in congestive heart failure, six patients with this condition underwent hemodynamic testing (at rest and during exercise) before and after dosing. Doses of 2, 5, and 10 mg were examined in sequence over 3 days to define dose-response characteristics. Terazosin, in these doses, decreased pulmonary and systemic vascular resistances and right atrial and pulmonary capillary wedge pressures. Terazosin increased stroke volume and cardiac output, presumably through afterload-reduction, without altering heart rate. These aforementioned responses were apparent both at rest and during exercise. While a direct relationship existed between dose and plasma concentration, a similar relationship was not observed for dose (or plasma concentration) and hemodynamic response; no differences were noted between the hemodynamic responses to the three doses. Improvement in hemodynamics persisted and the clinical status and exercise capacity improved in the four patients chronically treated (over 2 months) with terazosin. Treating the heightened tone of the sympathetic nervous system in congestive heart failure with the alpha 1 blocker, terazosin, may be of benefit to some patients afflicted with this disorder.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2875651&dopt=Abstract
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