Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Azelnidipine is a new dihydropyridine calcium channel antagonist with selectivity for L-type calcium channels that has recently been approved in Japan for the treatment of patients with hypertension. Results from clinical trials showed that, in 95 patients with mild-to-moderate hypertension, long-term treatment with azelnidipine effectively controls blood pressure (BP). The mean reduction from baseline in sitting systolic/diastolic BP after 1 year of treatment was 27.8/16.6 mm Hg. Among 172 patients with uncontrolled hypertension receiving non-calcium channel antagonist antihypertensive agents, the addition of azelnidipine therapy significantly reduced mean BP in a noncomparative, 1-year study (a reduction from 165.7/95.4 mm Hg at baseline to 138.2/79.9 mm Hg at study end). The antihypertensive efficacy of azelnidipine in patients with mild-to-moderate hypertension was shown to be similar to that of amlodipine or nitrendipine in randomised, double-blind studies. Azelnidipine and amlodipine controlled 24-hour BP to a similar extent. Azelnidipine is generally well tolerated; vasodilator adverse events such as as headache and hot facial flushes account for most of the adverse events. Its use is not associated with reflex tachycardia.
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PMID:Azelnidipine. 1463 80

Azelnidipine (Calblock) is a newly developed dihydropyridine-type calcium antagonist for the treatment of hypertension. In hypertensive animals, a single oral administration of azelnidipine caused a slowly developed and long-lasting hypotensive effect with a little reflex tachycardia. The extent of tachycardia was less with azelnidipine than with other agents of the same class. Long-term administrations of azelnidipine produced a stable antihypertensive effect with a slight decrease in heart rate. The hypotensive effect was preceded by an increase in plasma drug concentration and it persisted even after plasma drug concentration declined to very low levels. In the isolated arteries, the calcium blocking action developed gradually after treatment with azelnidipine and survived for a long period of time after the drug was removed from the bathing solution. These data suggest that the high affinity to vascular tissue contributes to the long-lasting hypotensive effects of this agent. The results from clinical studies in hypertensive patients indicated that once daily administration of azelnidipine achieved stable, 24-h control of blood pressure with no change or a slight decrease in heart rate. Clinical studies also showed a low incidence of adverse events such as headache, facial flush, dizziness, and palpitations. These characteristics make azelnidipine a new generation calcium antagonist that can be used for the treatment of hypertension.
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PMID:Pharmacological profiles and clinical effects of azelnidipine, a long-acting calcium channel blocker. 1463 8

The purpose of this study is to compare the effects and safety of azelnidipine and amlodipine in Chinese essential hypertensive patients. Patients were randomized to receive administration of azelnidipine 8-16 mg/day or amlodipine 2.5-5 mg/day for 8 weeks. The blood pressure and pulse rate were evaluated in an outpatient clinic and by ambulatory blood pressure monitoring. There were 220 patients enrolled to the study. The blood pressure in both groups was decreased significantly (P < 0.001). Compared with amlodipine, the patients received azelnidipine had better response in systolic blood pressure (SBP) and diastolic blood pressure (DBP) (P < 0.01). No significant changes of pulse rate were observed in either group. For the ambulatory blood pressure monitoring, both drugs had stable anti-hypertensive effects over 24 h. The trough/peak ratios of DBP for the azelnidipine and amlodipine groups were, respectively, 46% and 40%. Adverse events occurred at 7.3% and 10.0%, respectively in the azelnidipine and amlodipine groups (P = 0.485). Headache and dizziness were observed at an incidence of more than 1% in both groups. Once-daily administration of azelnidipine effectively controlled blood pressure and had a stable action over 24 h. Azelnidipine had good safety and compliance similar to amlodipine.
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PMID:Azelnidipine and amlodipine: a comparison of their effects and safety in a randomized double-blinded clinical trial in Chinese essential hypertensive patients. 2102 1