Clinical advantages of lipophilic dihydropyridines.
Lipophilic dihydropyridines have many theoretical and practical clinical advantages owing to their long permanence at the cell membrane. They have a greater chance of smoothly and permanently reducing blood pressure over 24 h than other dihydropyridines, a feature that may have positive prognostic implications since 24-h blood pressure is more closely related to the end-organ damage of hypertension. They may avoid the sympathetic activation consequent to an excessive early-dose hypotension, which is responsible for an increase in 24-h blood-pressure variability and reflex tachycardia, two phenomena that may worsen the prognosis of hypertensive patients. A further advantage which has been shown in experimental and clinical settings is the possibility of reducing the extension and progression of atherogenic lesions in blood vessels, which are responsible for cardiovascular complications in hypertension. Some of these features have been shown by the novel lipophilic dihydropyridine lercanidipine. In particular, clinical studies have shown that (i) this drug is effective in homogeneously reducing blood pressure over 24 h, (ii) its antihypertensive effect is similar to that of some common antihypertensive drugs, and (iii) the rate of adverse events experienced with lercanidipine is no greater than that observed with other antihypertensive drugs, with special reference to non-lipophilic calcium antagonists. In particular, studies performed so far have shown that lercanidipine does not exert a dangerous reflex tachycardia.
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Cattedra di Medicina Interna, Ospedale San Gerardo Monza, Università di Milano, Italy.
Omboni
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Zanchetti
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D000293:Adolescent; D000328:Adult; D000368:Aged; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000627:therapeutic use*; D018660:Blood Pressure Monitoring, Ambulatory; D002121:Calcium Channel Blockers / Q000009:adverse effects / Q000627:therapeutic use*; D004095:Dihydropyridines / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D008875:Middle Aged; D016032:Randomized Controlled Trials as Topic; D013610:Tachycardia / Q000139:chemically induced
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; C060343:lercanidipine