Drugs online research references
Mol Pharmacol. 1987 Jan;31(1):97-102.
Comparison of the effect of eleven beta-adrenoceptor blocking drugs in perturbing lipid membrane: an ESR spectroscopy study.
Ondrias K, Stasko A, Jancinova V, Balgavy P.
The perturbation effect of the beta-adrenoceptor blocking drugs atenolol, propranolol, practolol, oxprenolol, doberol, pronethanol, metipranolol, alprenolol, Ko-1124, pindolol, and exaprolol on rat brain lipid membrane was investigated by ESR spectroscopy using the spin probe method. Using stearic acids spin labeled at the 5th, 12th, and 16th positions, it was found that lipophilic drugs disorder the membrane and their effect is about 5-10 times higher at the 16th carbon membrane depth than at the 5th depth. Exaprolol induced nonlamellar phases in the bovine brain lipid membrane as detected by 31P NMR spectroscopy. The relative potencies of the drugs at 10 mmol/liter concentration to disorder the lipid membrane at the 16th carbon depth were in the order: exaprolol greater than alprenolol approximately equal to propranolol greater than metipranolol approximately equal to doberol greater than control sample greater than pindolol approximately equal to practolol approximately equal to atenolol. This order qualitatively corresponds with some of their nonspecific biological membrane activities but is not related to their beta-adrenoceptor blocking potencies. The inequality of the membrane perturbation propensities of the drugs indicates that they perturb the lipid membrane in a structure-dependent manner, i.e., that each induces a specific rather than a nonspecific membrane perturbation.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2880287&dopt=Abstract
J Hypertens. 1988 Sep;6(9):711-7.
Sympathetic predominance in essential hypertension: a study employing spectral analysis of heart rate variability.
Guzzetti S, Piccaluga E, Casati R, Cerutti S, Lombardi F, Pagani M, Malliani A.
Istituto Ricerche Cardiovascolari, CNR, Milano, Italy.
In this study on 91 subjects we tested the hypothesis of an enhanced sympathetic activity in uncomplicated essential hypertension employing spectral analysis of heart rate variability. With this technique the tonic sympathetic and vagal activities and their changes are respectively assessed by the power of approximately 0.1 Hz (low frequency, LF) and approximately 0.25 Hz (respiratory linked, high frequency, HF) components of the spectrum of the beat by beat variability of RR interval. When comparing the 40 subjects with diastolic blood pressure consistently greater than 95 mmHg (hypertensives, Ht), with 35 age-matched controls (diastolic arterial pressure less than 90 mmHg, Nt), we observed that LF was greater and HF smaller in Ht as compared to Nt, thus suggesting an enhanced sympathetic activity and a reduce vagal activity in Ht. Additionally, passive tilt, which in Nt enhances LF [delta = 26 +/- 2 normalized units (nu)] and reduces HF (delta = -22 +/- 2, nu), produced smaller (P less than 0.05) changes in Ht (delta LF = 6.3 +/- 2.7 and delta HF = -7.5 +/- 2.3 nu). Furthermore, the values of LF at rest and the altered effects of tilt on LF and HF were significantly correlated with the degree of the hypertensive state. Chronic beta-adrenergic blockade (atenolol 100 mg once daily for 2 weeks, n = 13) reduced heart rate and blood pressure (from 162/103 to 136/88 mmHg) together with a significant diminution of LF and an increase of HF. Thus, spectral analysis of RR variability appears to be a convenient non-invasive technique to follow the progressive alterations in sympatho-vagal balance present in essential hypertension.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3183374&dopt=Abstract
Clin Ther. 1987;9(4):380-9.
Postmarketing survey of the effects of an atenolol/chlorthalidone combination in the treatment of hypertension.
Maxwell MH, Garrett BN, Saunders E, Schnaper H.
A large-scale postmarketing survey was conducted in the United States to evaluate the antihypertensive efficacy and safety of a combination of 50 mg of the long-acting cardioselective beta-blocker atenolol and 25 mg of the monosulfonamyl diuretic chlorthalidone. The program included 28,585 patients (of whom 26,892 provided sufficient information by questionnaire for an assessment of efficacy and race), and the participation of 7,009 primary-care physicians. After four weeks of treatment, patients had a mean reduction in systolic blood pressure of 21 mmHg and in diastolic blood pressure of 13 mmHg. The magnitude of these reductions did not differ appreciably with respect to age, sex, race, or previous therapy. Diastolic blood pressure was reduced by at least 11 mmHg in 55% of patients and systolic blood pressure was reduced by at least 16 mmHg in 59% of patients. Physicians' assessments indicated that 86% of patients achieved satisfactory control of blood pressure by the end of the study. The physicians' global assessment of the effectiveness of treatment indicated that the combination was better than previous therapy in 82% of patients; 91% of physicians planned to continue treatment with the fixed combination. There were no adverse experiences that had not been reported previously, and only dizziness exceeded an incidence of 1%. It was concluded that the fixed combination provides added blood pressure control and the convenience of a simplified once-daily regimen without added side effects, regardless of age, sex, race, or prior antihypertensive therapy.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3607820&dopt=Abstract
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