Drugs online research references
Planta Med. 1995 Dec;61(6):493-6.
Relaxing activity of two linear diterpenes from Cystoseira brachycarpa var. balearica on the contractions of intestinal preparations.
Pieta FD, Breschi MC, Scatizzi R, Cinelli F.
Dipartimento di Scienze dell'Ambiente e del Territorio, Universita degli Studi di Pisa, Italy.
Eleganolone (1) and elegandiol (2), two linear diterpenes isolated from Cystoseira brachycarpa var. balearica, were tested on guinea-pig intestinal preparations. Both these compounds inhibited the contractile activities of acetylcholine (Ach) and histamine (Hist) on ileum musculature; the relative pIC50 values of eleganolone were found to be 4.60 +/- 0.03 and 4.84 +/- 0.20, respectively, while those of elegandiol were 4.71 +/- 0.18 and 5.18 +/- 0.01, respectively. Furthermore, 1 and 2 dose-dependently relaxed the same preparations precontracted with 300 microM BaCl2(pIC50 = 4.34 +/- 0.18 for 1 and pIC50 = 4.34 + 0.02 for 2) or with 60 mM KCl (pIC50 = 4.73 +/- 0.18 and 4.47 +/- 0.06, respectively). On colon smooth muscle, the diterpenes inhibited the spontaneous contractile tone and this effect was reversed by both methylene blue (3 x 10(-6) M) and haemoglobin (3 x 10(-6) M). Tetraethylammonium (TEA), furosemide, N omega-nitro-L-arginine methyl ester (L-NAME), indomethacin, alpha-chymotrypsin, and metoprolol were unable to block the eleganolone and elegandiol relaxing action on colonic musculature, but rather potentiated this response. On the contrary, the beta 2-blocker butoxamine partially inhibited the diterpenes activity. These results suggest that Cystoseira diterpenes act at a second messenger cyclase system rather than at a receptor level.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8824939&dopt=Abstract
J Cardiovasc Pharmacol. 1987;10 Suppl 2:S86-93.
Do beta-blockers alter lipids and what are the consequences?
Holtzman E, Rosenthal T, Goldbourt U, Segal P.
Department of Medicine, Chaim Sheba Medical Center, Tel Hashomer, Israel.
The unpredictable effect of antihypertensive therapy on coronary risk resulting from changes in lipid levels is an increasingly recognized problem. Different drugs have been shown to exert varying effects on lipids. This problem is particularly evident in young hypertensive patients who may be candidates for lifelong therapy. The effects of chlorthalidone and metoprolol on fasting plasma lipids and lipoprotein levels were compared in two similar nonrandomized groups of patients with mild hypertension. Chlorthalidone therapy was associated with an increase in serum cholesterol of 8.1% (17 mg/dl), mainly reflecting an increase in low-density lipoprotein (LDL) cholesterol. Serum triglycerides increased by 16% (20 mg/dl) and high-density lipoprotein (HDL) cholesterol levels decreased by 10% (3 mg/dl, not significant). Metoprolol therapy induced no changes in total, low, very low, or high-density lipoprotein. Serum triglyceride concentration increased by 22% (28 mg/dl). Application of the Israel Ischemic Heart Disease Study data to these findings indicates a slight decrease at most in the 5-year estimated probability of myocardial infarction in the chlorthalidone-treated group, whereas a clearly favorable influence on the calculated risk of coronary heart disease was observed for those treated with metoprolol. These data suggest that the different forms of therapy for mild hypertension carry varying degrees of significance in terms of risk of coronary heart disease, which should be considered when choosing medication.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2444826&dopt=Abstract
J Cardiovasc Pharmacol. 1987;10 Suppl 2:S86-92; discussion S93.
Do beta-blockers alter lipids and what are the consequences?
Holtzman E, Rosenthal T, Goldbourt U, Segal P.
Department of Medicine, Chaim Sheba Medical Center, Tel Hashomer, Israel.
The unpredictable effect of antihypertensive therapy on coronary risk resulting from changes in lipid levels is an increasingly recognized problem. Different drugs have been shown to exert varying effects on lipids. This problem is particularly evident in young hypertensive patients who may be candidates for lifelong therapy. The effects of chlorthalidone and metoprolol on fasting plasma lipids and lipoprotein levels were compared in two similar nonrandomized groups of patients with mild hypertension. Chlorthalidone therapy was associated with an increase in serum cholesterol of 8.1% (17 mg/dl), mainly reflecting an increase in low-density lipoprotein (LDL) cholesterol. Serum triglycerides increased by 16% (20 mg/dl) and high-density lipoprotein (HDL) cholesterol levels decreased by 10% (3 mg/dl, not significant). Metoprolol therapy induced no changes in total, low, very low, or high-density lipoprotein. Serum triglyceride concentration increased by 22% (28 mg/dl). Application of the Israel Ischemic Heart Disease Study data to these findings indicates a slight decrease at most in the 5-year estimated probability of myocardial infarction in the chlorthalidone-treated group, whereas a clearly favorable influence on the calculated risk of coronary heart disease was observed for those treated with metoprolol. These data suggest that the different forms of therapy for mild hypertension carry varying degrees of significance in terms of risk of coronary heart disease, which should be considered when choosing medication.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2481177&dopt=Abstract
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