Drugs online research references
Cardiovasc Drugs Ther. 1990 Aug;4(4):1135-43.
The initial hemodynamic response to newer antihypertensive agents at rest and during exercise: review of visacor, doxazosin, nisoldipine, tiapamil, perindoprilat, pinacidil, dilevalol, and carvedilol.
Omvik P, Lund-Johansen P.
Medical Department, Haukeland Hospital, Bergen, Norway.
Antihypertensive drugs may lower blood pressure through very different mechanisms, initially as well as during chronic use. This article is a review of the immediate hemodynamic changes induced by a beta blocker (visacor), an alpha-receptor blocker (doxazosin), two calcium antagonists (tiapamil and nisoldipine), an angiotensin-converting enzyme inhibitor (perindoprilat), two double-acting compounds (dilevalol and carvedilol), and placebo studied in 126 patients with mild to moderately severe essential hypertension. The patient populations of the different treatment groups were comparable. The invasive hemodynamic technique, including intraarterial blood pressure (BP) recording and measurements of cardiac output by cardiogreen, was the same in all studies. All antihypertensive compounds examined induced a rapid reduction in blood pressure both at rest and during exercise, while no significant changes occurred in the placebo group. This review shows the scope of hemodynamic responses, ranging from peripheral vasodilation to a reduction of heart rate and blood flow. Furthermore, different counterregulatory effects blunting the immediate BP reduction are demonstrated.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1964580&dopt=Abstract
Prostate. 1990;16(1):29-38.
Binding and functional properties of doxazosin in the human prostate adenoma and canine brain.
Lepor H, Baumann M, Shapiro E.
Department of Urology (Surgery), Medical College of Wisconsin, Milwaukee 53226.
The binding and functional properties of doxazosin were characterized in the canine brain and human prostate. 3H-Doxazosin binding sites were characterized in canine brain and human prostate homogenates using saturation experiments. The binding of 3H-doxazosin in the canine brain was consistently saturable and of high affinity. The mean equilibrium dissociation constant (Kd) and density (Bmax) of 3H-doxazosin binding sites in the canine brain were 0.19 nM and 2.17 fmol/mg wet wt, respectively. The binding of 3H-doxazosin in human prostate homogenates was not consistently linear owing to a relatively high proportion of nonspecific doxazosin binding sites. The mean Kd and Bmax of 3H-doxazosin binding sites in the prostate determined from the saturation experiments yielding linear Scatchard plots were 0.2 nM and 0.51 fmol/mg wet wt. The pharmacology of doxazosin binding sites was further characterized in the canine brain using competitive binding experiments. The rank order of IC50corr values for norepinephrine, clonidine, yohimbine, terazosin, and prazosin indicated that doxazosin binds selectively to alpha 1 and alpha 2 adrenergic binding sites. The relative affinity of unlabeled doxazosin for alpha 1 and alpha 2 binding sites in the human prostate was determined by displacing 125I-Heat or 3H-rauwolscine with varying concentrations of unlabeled doxazosin. The affinity of doxazosin for alpha 1 binding sites in the prostate adenoma was approximately 100-fold greater than its affinity for alpha 2 binding sites. The potency of doxazosin for inhibiting phenylephrine-induced contractions in the prostate indicated that prostate smooth muscle contraction is mediated by alpha 1 adrenoceptors.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1968249&dopt=Abstract
Am Heart J. 1990 Mar;119(3 Pt 2):748-53.
The cost-benefit approach to pricing new medicines: doxazosin versus beta-blocker treatment in Sweden.
Lindgren B.
Swedish Institute for Health Economics, Lund.
The economic evaluation of pharmaceuticals is becoming increasingly important. This article presents an illustrative example of how the cost-benefit approach can be used in the pricing of a new pharmaceutical product. Doxazosin, a new selective alpha 1-inhibitor used in the treatment of hypertension, is compared with the established beta-blocker, atenolol. Cost-effectiveness ratios are calculated for both, and from the analysis it emerges that doxazosin is the more cost-effective agent. This is largely the result of the favorable high-density lipoprotein/total cholesterol changes that doxazosin produces. Even when doxazosin is priced 30% higher than atenolol, doxazosin is more cost-effective. It is concluded that in the future economic evaluations will have significant impacts on research and development within the pharmaceutical industry. However, a number of issues still must be addressed, and economic evaluation should be subject to continuous review.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1968701&dopt=Abstract
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