Drugs online research references
J Hum Hypertens. 1990 Oct;4 Suppl 3:47-9.
Doxazosin in renal impairment.
Waller DG, Oliver RM.
Clinical Pharmacology Group, Southampton General Hospital, UK.
The pharmacokinetics of doxazosin given once daily are similar in patients both with normal and with impaired renal function and consequently doxazosin can be used effectively in both at similar doses. Renal blood flow is well preserved during long-term treatment but effects on glomerular filtration rates are less consistent and small reductions may occur. It is uncertain whether these reflect a reduction in perfusion pressure, progression of the underlying renal disease or a combination of the two. Postural hypotension may occur in some patients after an initial dose of 1 mg.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2148195&dopt=Abstract
Cardiologia. 1990 Nov;35(11):931-6.
[Doxazosin for the treatment of arterial hypertension]
[Article in Italian]
Mozzato MG, Semplicini A, Serena L, Valle R, Casolino P, Buzzaccarini F, Rubino N, Giusto M, Pessina AC.
Istituto di Clinica Medica I, Universita degli Studi, Padova.
Hypertension is often associated to other risk factors, such as abnormal lipid and carbohydrate metabolism, which should be considered for the choice of antihypertensive drug treatment. Doxazosin is a postsynaptic alpha-1 adrenoceptor blocker suitable for once a day treatment regime. It seems to induce fewer side effects than older drugs of the same class and it may improve lipid and carbohydrate profile, thereby reducing the risk of coronary artery disease. To verify its effects on blood pressure, serum lipids and glucose tolerance, doxazosin (1-8 mg od) was given for 8 weeks to 32 patients suffering from essential hypertension, of whom 16 had fasting serum cholesterol higher than 6 mmol/l and/or fasting serum triglycerides higher than 1.9 mmol/l. Sitting and standing blood pressure were significantly reduced (from 163 +/- 18/101 +/- 6 mmHg to 147 +/- 19/94 +/- 8, p less than 0.001 and from 162 +/- 18/107 +/- 9 to 145 +/- 18/95 +/- 8, p less than 0.001, respectively) at a mean daily dose of 5 mg. Normotension or a good hypotensive response was achieved in 60% of the patients. The daily dose which turned out to be effective in 50% of the patients was 7 mg. The drug treatment was well tolerated and orthostatic hypotension was never observed either on starting treatment or on increasing dosage. Blood lipids and glucose tolerance were not significantly affected. Doxazosin is therefore an effective antihypertensive agent suitable for use in patients with essential hypertension alone or combined with hyperlipidemia.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2151571&dopt=Abstract
Eur J Pharmacol. 1990 Jan 23;188(1):71-80.
Effect of detergent solubilization on the affinity of some quinazoline derivatives for the alpha 1-adrenoceptor.
Shreeve SM.
Department of Pharmacology, Vermont Center for Vascular Research, University of Vermont, Burlington 05405.
[3H]Prazosin bound to a single class of high-affinity sites in both bovine aortic and rat hepatic membranes. The absolute affinity values of displacing ligands (prazosin greater than doxazosin much greater than trimazosin greater than yohimbine) were the same for both tissues. After solubilization of the alpha 1-adrenoceptors with digitonin and 3-[(3-cholamidopropyl)-dimethylammonio]-1-propane sulfonate, an identical rank order potency was observed. However, solubilization significantly reduced ligand affinity. In both tissues the affinity of prazosin was reduced 10- to 13-fold, whereas the affinities of doxazosin, trimazosin and yohimbine were reduced two- to six-fold. There appeared to be no relationship between the lipophilicities of the ligands and the degree to which affinity is affected by solubilization. The results suggest that the reductions in affinity are the consequence of a conformational change in the alpha 1-adrenoceptor and appear to support the hypothesis that the alpha 1-adrenoceptor is so constructed that the spatial configuration of the binding site can change in response to an alteration in its microenvironment.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2155124&dopt=Abstract
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