Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The efficacy and safety of nisoldipine CC and lisinopril were compared in 278 patients with mild to moderate systemic hypertension in a double-blind, placebo run-in trial. Patients were randomized to nisoldipine CC or lisinopril for 8 weeks to achieve a trough sitting diastolic blood pressure (BP) < or = 90 mmHg. Responders were maintained on their optimal dose for a further 8 weeks. Nonresponders were switched to combination therapy and treated for 8 weeks. Twenty-four-hour ambulatory BP monitoring (ABPM) was carried out during placebo and monotherapy. The responder rate of 73.8% with nisoldipine CC after 8 weeks was greater than 56.1% with lisinopril (p = 0.007). The responder rate with combination therapy was 61%. ABPM showed that both nisoldipine CC and lisinopril produced constant blood pressure lowering effects over the 24-hour period and maintained circadian rhythm. Adverse effects were more frequent with nisoldipine CC (headache and peripheral edema) than with lisinopril (cough) monotherapy. Nisoldipine CC monotherapy was at least as effective as lisinopril monotherapy in the management of mild to moderate hypertension. Both agents were well tolerated. Combination therapy with nisoldipine CC and lisinopril was effective and well tolerated in patients with blood pressure not controlled by monotherapy alone.
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PMID:Nisoldipine CC and lisinopril alone or in combination for treatment of mild to moderate systemic hypertension. Canadian Nisoldipine CC Hypertension Trial Group. 935 63

This study compared the efficacy and tolerability of nisoldipine coat core (CC) 10-40 mg o.d. and hydrochlorothiazide (HCTZ) 25-50 mg o.d. Patients with mild-to-moderate essential hypertension received either nisoldipine CC 10 mg o.d. or HCTZ 25 mg o.d. Treatment was titrated at two-weekly intervals as necessary. The primary efficacy endpoint was a defined reduction in diastolic blood pressure (DBP). Response rates were similar for both the nisoldipine CC- and HCTZ-treated groups (74% and 70%, respectively). Secondary efficacy endpoints were reductions in both diastolic and systolic blood pressures (SBP). At treatment endpoint, the change from baseline in SBP was 16.2 mmHg for the nisoldipine CC group and 14.9 mmHg for the HCTZ group. Both drugs were well tolerated, and adverse events were generally minor and typical of these antihypertensive agents. Drug-related adverse events were greater in the nisoldipine CC- than the HCTZ-treated patients (50% and 37%, respectively). Nisoldipine CC was shown to demonstrate antihypertensive efficacy similar to HCTZ in the treatment of mild-to-moderate hypertension.
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PMID:Comparative efficacy and tolerability of nisoldipine coat core and hydrochlorothiazide in mild-to-moderate hypertension. 948 83

Nisoldipine coat-core (nisoldipine CC), an extended-release once-daily formulation, is an effective treatment for mild-to-moderate hypertension, providing sustained blood pressure control over the 24-hour dosing interval. Nisoldipine CC is highly vascular selective. It causes neither reflex tachycardia nor symptomatic bradycardia; it lacks significant negative inotropy at therapeutic doses; and it does not affect circadian variation in blood pressure or heart rate. Data suggest that the lack of reflex sympathetic activation in response to the blood pressure-lowering effect of nisoldipine CC is due to the smooth onset of action of nisoldipine CC, causing resetting of the baroflex. The neutral heart rate profile of nisoldipine CC confers potential therapeutic advantages over several other calcium channel blockers, in particular, the short-acting agents, in the treatment of hypertension.
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PMID:Nisoldipine coat-core and heart rate response during treatment of hypertension. 1034 70

Nisoldipine, a second-generation dihydropyridine calcium antagonist, is a racemate compound used in the treatment of hypertension and coronary heart disease. This study presents an enantioselective HPLC-GC-MS method for the analysis of nisoldipine in human plasma and establishes confidence limits for its application to pharmacokinetic studies. Plasma samples were basified and extracted with toluene. The enantiomers were resolved on a Chiralcel OD-H column using hexane-ethanol (97.5:2.5, v/v) and the (+)- and (-)-fractions were collected separately with the diode array detector switched off. For the quantification of the nisoldipine enantiomers a GC-MS with an Ultra 1 Hewlett-Packard column was used with the detector operated in the single-ion monitoring mode with electron-impact ionization (m/z 371.35 and 270.20 for nisoldipine and m/z 360.00 for the internal standard, nitrendipine). The method proved to be suitable for pharmacokinetic studies based on the low quantification limit (0.05 ng/ml for each enantiomer) and the broad linear range (0.05-50.0 ng/ml for each enantiomer). Low coefficients of variation (<15%) were demonstrated for both within-day and between-day assays. No interference from drugs associated with nisoldipine treatment was observed. The enantioselective pilot study on the kinetic disposition of nisoldipine administered in the racemic form to a hypertensive patient using a multiple dose regimen revealed the accumulation of the (+)-enantiomer with an AUC(0-24) (+)/(-) ratio of approximately 8. Both enantiomers were quantified in plasma at a time interval of 24 h. This HPLC-GC-MS method is reliable, selective and sensitive enough to be used in clinical pharmacokinetic studies on the enantioselective disposition of nisoldipine in humans.
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PMID:Enantioselective assay of nisoldipine in human plasma by chiral high-performance liquid chromatography combined with gas chromatographic-mass spectrometry: applications to pharmacokinetics. 1158 62

Nisoldipine coat-core (CC), a 1,4-dihydropyridine calcium antagonist, is indicated for the treatment of hypertension and may be used alone or in combination with other antihypertensive agents. The CC technology allows for extended delivery of the drug and once-daily dosing. Nisoldipine CC tablets are absorbed across the entire gastrointestinal tract, including the colon. Eighty percent of the total dose is in the slow-release outer coat, while the core has immediate-release characteristics suitable for absorption in the distal gastrointestinal tract. Numerous double-blind, randomized studies of this agent have been done in patients with hypertension. The use of nisoldipine CC reduced both clinic and ambulatory blood pressure to a similar degree when compared with angiotensin-converting enzyme (ACE) inhibitors, beta-blockers, and the calcium antagonists amlodipine and felodipine. The drug has also been studied in hypertensive African Americans and demonstrated equivalent efficacy to amlodipine. Tolerability of the drug is good, with the most common side effect of edema at a rate similar to other dihydropyridine calcium antagonists. Thus, results of more than a decade of clinical trial data support the use of nisoldipine CC as once-daily therapy for the treatment of hypertension.
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PMID:Pharmacologic agents in the management of hypertension--nisoldipine coat-core. 1739 68

Nisoldipine is used for the treatment of hypertension and angina pectoris. However, it has very low bioavailabil-ty, which is attributed to extensive pre-systemic metabolism. In addition, nisol-ipine is highly potent (used at a low dose). Taking into consideration the fact that transdermal delivery avoids the pre-systemic metabolism and is only suit-ble for potent drugs, nisoldipine can be considered as an excellent candidate for transdermal delivery. Accordingly, the purpose of this study was to optimize nisoldipine transdermal delivery. That was achieved initially by investigating the effect of vehicles on skin penetration. The tested vehicles were ranked with respect to transdermal flux of nisoldipine as isopropyl myristate > oleic acid > propylene glycol > water > polyethylene glycol 400. A combination of oleic acid with propylene glycol was synergistic with a ratio of 1:2 w/w being the best. These results were taken further to develop microemulsion systems using either oleic acid or isopropyl myristate as the oil phase. Both cases employed polyoxy-thylene sorbitan monooleate as a surfactant with propylene glycol being uti-ized as a cosurfactant in the case of oleic acid and ethanol in the case of isopropyl myristate. The developed microemulsions produced significant enhancement in nisoldipine transdermal delivery with the flux being even greater than that obtained from the corresponding pure vehicles. This achieve-ent was recorded in optimum microemulsion formulations which contained a cosurfactant. The study provided stepwise optimization of a vehicle for trans-ermal delivery of nisoldipine.
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PMID:Transdermal Delivery of Nisoldipine: Refinement of Vehicles. 2668 95


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