16 Jun 10
By U Ndefo, G Erowele, R Ebiasah and W Green
Am J Health Syst Pharm.2010; 67: 351-360
The pharmacology, pharmacokinetics, efficacy, safety, dosage and administration, and place in therapy of clevidipine are reviewed.
Clevidipine is a new lipophilic, short-acting, third-generation dihydropyridine calcium channel blocker (CCB) approved for use in the management of acute hypertension when oral agents are not feasible. It exerts its hemodynamic effects through selective arterial vasodilation without effects on the venous circulation. Clevidipine has a half-life of approximately two minutes after i.v. administration, resulting in very rapid onset and offset of antihypertensive action. Unlike many current i.v. antihypertensive agents that are metabolized by the kidneys or liver, clevidipine is metabolized in the blood and tissues and does not accumulate in the body. Clevidipine does not appear to inhibit or induce cytochrome P-450 isoenzymes. Several Phase III clinical trials have reported the clinical efficacy and safety of clevidipine in patients with severe hypertension and in cardiac surgical patients with perioperative hypertension. The most frequent adverse events reported in clinical trials of clevidipine were headache, nausea, and vomiting. Risk of rebound hypertension, especially in patients not transitioned from clevidipine to oral antihypertensive therapy after prolonged infusions, should be monitored for at least eight hours after the drug is discontinued.
Clevidipine, a novel third-generation dihydropyridine CCB, has demonstrated efficacy and safety in patients with acute hypertension and preoperative, perioperative, and postoperative hypertension. While its short duration of action and short half-life are appropriate for use in acute settings, more information on its safety is needed to assess its appropriate use in therapy.
11 Jul 09
By G Mancia; M Bombelli; R Facchetti; F Madotto; F Quarti-Trevano; H Friz; G Grassi and R Sega
Hypertension, advanced publication
It is debated whether white-coat (WCHT) and masked hypertension (MHT) are at greater risk of developing a sustained hypertensive state (SHT). In 1412 subjects of the Pressioni Arteriose Monitorate e Loro Associazioni Study, we measured office blood pressure (BP), 24-hour ambulatory BP, and home BP. The condition of WCHT was identified as office BP >140/90 mm Hg and 24-hour BP mean <125/79 mm Hg or home BP <132/82 mm Hg. Corresponding values for MHT diagnosis were office BP <140/90 mm Hg, 24-hour BP 125/79 mm Hg, and home BP 132/82 mm Hg. SHT was identified when both office and 24-hour BP means or home BP were over threshold values and normotension was under the threshold value. Subjects were reassessed 10 years later to evaluate the BP status of the various conditions defined previously. At the first examination, 758 (54.1%), 225 (16.1%), 124 (8.9%), and 293 (20.9%) subjects were normotensive, WCHT, MHT, and SHT subjects, respectively. At the second examination, 136 normotensives (18.2%), 95 WCHT (42.6%), and 56 MHT (47.1%) subjects became SHT. As compared with normotensives, adjusting for age and sex, the risk of becoming SHT was significantly higher for WCHT and MHT subjects (odds ratio: 2.51 and 1.78, respectively; P<0.0001). Similar results were obtained when the definition of the various conditions was based on home BP. Independent contributors of worsening of hypertension status were not only baseline BP, but also, although to a lesser extent, metabolic variables and age. Subjects with WCHT and MHT are at increased risk of developing SHT. This may contribute to their prognosis that appears to be worse as compared with that of normotensive subjects.