Amlodipine values

Julius S, Kjeldsen SE, Weber M, et al. Outcomes in hypertensive patients at high cardiovascular risk treated with regimens based on valsartan or amlodipine the VALUE randomised trial. Lancet 2004 363(9426) =2022-2231. 

Hypertension and type 2 diabetes mellitus are frequent co-morbid conditions resulting in a very high risk population. ARBs - losartan as compared to the beta-blocker atenolol in the LIFE Study [8], candesartan as compared to the control therapies in the SCOPE [16] and CHARM [33] Studies, valsartan as compared to amlodipine in the VALUE Study [34] have been found to have beneficial effects in preventing the development of type 2 diabetes mellitus. 

Julius S, Kjeldsen SE, Weber M et al. (2004). Outcomes in hypertensive patients at high cardiovascular risk, treated with regimens based on valsartan or amlodipine the VALUE randomized trail. Lancet 363 2022-2031 Kearney PM, Welton M, Reynolds K et al. (2005). Global burden of hypertension analysis of worldwide data Lancet 365 217-223 Keli S, Bloemberg B, Kromhout D (1992). Predictive value of repeated systolic blood pressure measurements for stroke risk. 

A 77-year-old man took amlodipine for 1 month and developed jaundice and raised aspartate transaminase, alanine transaminase, and bilirubin (9). A liver biopsy suggested a drug-induced hepatitis and the amlodipine was withdrawn. His symptoms and laboratory values normalized. Other drugs (metformin, fluindione, and omeprazole) were not withdrawn. 

Kass RS and Arena JP, Influence of pHo on calcium channel block by amlodipine, a charged dihydropyridine compound. Implications for location of the dihydropyridine receptor, /. Gen. Physiol, 93(6), 1109-1127 (1989). NB Although the pRg is repeatedly stated as 8.6, no experimental detail is given, nor any reference. The paper also claims an estimated pK value of <3.5 for nisoldipine (ref Hugenholtz PC and Meyer J (eds.), Nisoldipine, Springer-Verlag, Berlin, 3-348 (1987). 

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