The Effect of Topical Nilvadipine on Cerebral Pial Vessels in Rabbit

The effects of mock CSF, nilvadipine solution of various concentrations and PEG 400 solution on regional cerebral pial vessels in rabbits were studied by topical microapplication to the perivascular evironment through the bilateral cranial windows in a randomized fashion. Physiological parameters(PaO2, PaCO2, blood pH, and systolic blood pressure) were not significantly changed during all experiments. The pial vascular diameter was directly determined with the micrometer eyepiece under the operating microscope. The results were the followings: 1) Topical applications with mock cerebrospinal fluid(Group I) and PEG 400(Group II) on cerebral pial vessels did not significantly change pial vascular diameter in comparison with the resting state(p>0.05). 2) Application of nilvadipine solution of 1x10(-8)M did not show significant dilatation, and solutions over the range of 1x10(-7) to 1x10(-2)M resulted in significant dilatation of the cerebral pial arteries in a dose-dependent manner. The small arterial segments showed more dilatation than large arterial segments when topical nilvadipine solution were applied, however, the difference was not significant(p>0.05). 3) In venous segments, topical application of the nilvadipine solution induced no significant pial vein dilatation compared with the resting state(p>0.05), except when 10 minutes after the topical application of 1x10(-2)M nilvadipine solution(p<0.05). It may be suggested that topical application of nilvadipine solution induce the dilatation of pial arteries with dose-dependent manner. Nilvadipine might be used for treatment and prevention of cerebral vasospasm and ischemia.

Antihypertensive Effects of Nilvadipine(Nivadil(R)) in Patients with Essential Hypertension

BACKGROUND: Form the 1970's calcium channel blockers have been used as one of the most effective drugs for antihypertensive therapy. Nilvadipine(Nivadil(R)) is a new vessel-selective calcium channel blocker with a markedly high oral bioaviliability and a long elimination half-life time. To evaluate the efficacy and side effects of nilvadipine, daily monotherapy was done in 22 patients with essential hypertension. METHOD: After more than 2 weeks of previous drug wash-out periods, Nilvadipine 8-12mg was administered daily in 2 or 3 divided dosage for 8 weeks in patients with mild to severe essential hypertension. The sitting blood pressure(BP) and heart rate were measured before and 2, 4, 8 weeks after medication. RESULT: Systolic and diastolic BP were significantly reduced at 2 weeks after medication and no further significant BP reduction were noted throughout the remainer of the trial(4 to 8 weeks). Normotension(diastolic BP < or =90mmHg) was achieved in 14 cases(67%) after 8 weeks therapy and in 7 cases(33%) BP reduced effectively. The side effect noted were headache and facial flushing in 2 cases and in one of them the medication were discontinued. And fatigue, dizziness were complaint in 1 case respectively. There were no significant laboratory changes before and after nilvadipine therapy. CONCLUSION: It can be concluded that nilvadipine(Nivadil(R)) monotherapy is effective in many patients with essential hypertension and a clinical study of combined therapy with other antihypertensive agents in larger numbers of patients will be needed.