Reference

Effects of amlodipine orotate on hypertension-related complications in spontaneously hypertensive rats

Effects of amlodipine orotate on hypertension-related complications in spontaneously hypertensive rats. Choi, Seul Min; Kim, Jee Eun; Ahn, Byoung Ok; Kwon, Jong Won ( Research Laboratories, Dong-A Pharmaceutical Company, Kyunggi-do, S. Korea). Arzneimittel Forschung, 56(1), 12-17 (English) 2006 Editio Cantor Verlag. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Hypertension is a common problem in elderly patients, which usually requires chronic therapy under various physiol. conditions including low gastric acidity (hypo- or anacidity). This study investigated a new salt type of amlodipine (CAS 88150-42-9) on blood pressure and hypertension-related complications in stroke-prone spontaneously hypertensive rats (SHR-SP). Amlodipine orotate was prepd. by reacting orotic acid and amlodipine to increase the dissoln. rate at higher gastric pH conditions. Twelve-week-old SHR-SP were randomly divided into five groups to receive either amlodipine orotate or amlodipine besylate (CAS 111470-99-6) at the doses of 3 and 10 mg/kg/day orally for four weeks. The age-matched normotensive Wistar Kyoto rats (WKY) served as the normal pos. control group. The systolic blood pressure was reduced in the amlodipine treated SHR-SP in a dose-dependent manner with a similar potency irresp. of the salt type. Both amlodipines also reduced the left ventricular hypertrophy at high doses and concn.-dependently inhibited the Ca2+-induced contraction with a similar potency. Furthermore, semi-quant. anal. of a cerebral injury revealed that the two salts of amlodipine reduced the stroke-related lesions to a similar degree. These results suggest that the amlodipine orotate is effective in terms of its effects on hypertension, cardiac hypertrophy and stroke-related cerebral damage in SHR-SP.

Major outcomes in high-risk hypertensive patients randomized to angiotensin-converting enzyme inhibitor or calcium channel blocker vs

Major outcomes in high-risk hypertensive patients randomized to angiotensin-converting enzyme inhibitor or calcium channel blocker vs. diuretic. The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attach Trial (ALLHAT). Furberg, Curt D.; Wright, Jackson T., Jr.; Davis, Barry R.; Cutler, Jeffrey A.; Alderman, Michael; Black, Henry; Cushman, William; Grimm, Richard; Haywood, L. Julian; Leenen, Frans; Oparil, Suzanne; Probstfield, Jeffrey; Whelton, Paul; Nwachuku, Chuke; Gordon, David; Proschan, Michael; Einhorn, Paula; Ford, Charles E.; Piller, Linda B.; Dunn, J. Kay; Goff, David; Pressel, Sara; Bettencourt, Judy; deLeon, Barbara; Simpson, Lara M.; Blanton, Joe; Geraci, Therese; Walsh, Sandra M.; Nelson, Christine; Rahman, Mahboob; Juratovac, Anne; Pospisil, Robert; Carroll, Lillian; Sullivan, Sheila; Russo, Jeanne; Barone, Gail; Christian, Rudy; Feldman, Sharon; Lucente, Tracy; Calhoun, David; Jenkins, Kim; McDowell, Peggy; Johnson, Janice; Kingry, Connie; Alzate, Juan; Margolis, Karen L.; Holland-Klemme, Leslie Ann; Jaeger, Brenda; Williamson, Jeffrey; Louis, Gail; Ragusa, Pamela; Williard, Angela; Ferguson, R. L. Sue; Tanner, Joanna; Eckfeldt, John; Crow, Richard; Pelosi, John (Case Western Reserve University, Cleveland, OH 11000, USA). JAMA, the Journal of the American Medical Association, 288(23), 2981-2997 (English) 2002 American Medical Association. CODEN: JAMAAP. ISSN: 0098-7484. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review and comments. Antihypertensive therapy is well established to reduce hypertension-related morbidity and mortality, but the optimal first-step therapy is unknown. The aim was to det. whether treatment with a calcium channel blocker or an angiotensin-converting enzyme inhibitor lowers the incidence of coronary heart disease (CHD) or other cardiovascular disease (CVD).events vs. treatment with a diuretic. The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT), a randomized, double-blind, active-controlled clin. trial conducted from Feb. 1994 through Mar. 2002. A total of 33357 participants aged 55 yr or older with hypertension and at least 1 other CHD risk factor from 623 North American centers. Participants were randomly assigned to receive chlorthalidone, 12.5 to 25 mg/d (n = 15255); amlodipine, 2.5 to 10 mg/d (n=9048); or lisinopril, 10 to 40 mg/d (n=9054) for planned follow-up of approx. 4 to 8 yr. The primary outcome was combined fatal CHD or non-fatal myocardial infarction, analyzed by intent-to-treat. Secondary outcomes were all-cause mortality, stroke, combined CHD (primary outcome, coronary revascularization, or angina with hospitalization), and combined CVD (combined CHD, stroke, treated angina without hospitalization, heart failure [HF], and peripheral arterial disease). Mean follow-up was 4.9 yr. The primary outcome occurred in 2956 participants, with no difference between treatments. Compared with chlorthalidone (6-yr rate, 11.5%), the relative risks (RRs) were 0.98 (95% Cl, 0.90-1.07) for amlodipine (6-yr rate, 11.3%) and 0.99 (95% Cl, 0.91-1.08) for lisinopril (6-yr rate, 11.4%). Likewise, all-cause mortality did not differ between groups. Five-year systolic blood pressures were significantly higher in the amlodipine (0.8 mm Hg, P = . 88150-42-9 and 77-36-1 are cas registry numbers of chemicals which are used as reagents here.03) and lisinopril (2 mm Hg, P < .001) groups compared with chlorthalidone, and 5-yr diastolic blood pressure was significantly lower with amlodipine (0.8 mm Hg, P < .001). For amlodipine vs. chlorthalidone, secondary outcomes were similar except for a higher 6-yr rate of HF with amlodipine (10.2% vs 7.7%; RR, 1.38; 95% Cl, 1.25-1.52). For lisinopril vs. chlorthalidone, lisinopril had higher 6-yr rates of combined CVD (33.3 % vs. 30.9%; RR, 1.10; 95% Cl, 1.05-1.16); stroke (6.3% vs. 5.6%; RR, 1.15; 95% Cl, 1.02-1.30); and HF (8.7% vs. 7.7%; RR, 1.19; 95% Cl, 1.07-1.31). Thiazide-type diuretics are superior in preventing 1 or more major forms of CVD and are less expensive. They should be preferred for first-step antihypertensive therapy. .