Pharmacokinetics, bioavailability, metabolism and acute and chronic antihypertensive effects of nitrendipine in patients with chronic renal failure and moderate to severe hypertension.

Mikus, Gerd; Mast, V.; Fischer, Christine; Machleidt, Christoph; Kuhlmann, Uwe; Eichelbaum, Michel

doi:10.1111/j.1365-2125.1991.tb05535.x

Cited by 13 publications

(3 citation statements)

References 23 publications

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“…For example, Cook et al (1990) found a significant correlation between log plasma nicardipine concentrations and change in diastolic blood pressure after intravenous administration of the drug, and similar data have been described for both nimodipine and nitrendipine (Gengo et al 1987;Mikus et al 1991). For example, Cook et al (1990) found a significant correlation between log plasma nicardipine concentrations and change in diastolic blood pressure after intravenous administration of the drug, and similar data have been described for both nimodipine and nitrendipine (Gengo et al 1987;Mikus et al 1991).…”

Section: Other Calcium Antagonistssupporting

confidence: 61%

Concentration-Effect Analysis of Antihypertensive Drug Response

Donnelly

Elliott

Meredith

1994

Clinical Pharmacokinetics

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Although individualised antihypertensive therapy is widely recommended, prospective methods for optimising treatment are hampered by the paucity of basic information about dose-plasma concentration-response relationships for commonly used drugs. Concentration-effect analysis has been applied to a number of therapeutic areas. With antihypertensive drugs this approach has clearly identified direct relationships between pharmacokinetic and pharmacodynamic profiles within individual patients. Thus, either a linear or nonlinear model can be used to quantify the antihypertensive drug response in terms of parameters that incorporate pharmacokinetic and pharmacodynamic information. Furthermore, these models take account of placebo effects and time-dependent changes in blood pressure and drug concentrations during a dosage interval. Concentration-effect analysis has been used to characterise the responses to a range of calcium antagonist drugs. These studies have demonstrated that these analyses are useful for optimising dosage schedules, identifying determinants of blood pressure response, and predicting steady-state profiles of blood pressure (including peak/trough effects) after administration of a single ('test') dose. This mode of analysis warrants early inclusion in the clinical development of any new antihypertensive agent, so that the familiar difficulties in identifying the optimum dosage range are avoided.

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Section: Other Calcium Antagonistssupporting

confidence: 61%

Concentration-Effect Analysis of Antihypertensive Drug Response

Donnelly

Elliott

Meredith

1994

Clinical Pharmacokinetics

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“…Widely used drugs, such as Ca" antagonists, provide an example for the necessity of enantioselective methods of determination. [2][3][4][5] With chiral stationary-phase high-performance liquid chromatography (CSP-HPLC) it is now possible to separate enantiomers of Ca2+ antogonists with the 1,4-dihydropyridine structure under mild conditions.69 However, the limit of quantification is such that when only 1 to 2 mg of these drugs of the class of 1,4-dihydropyridine compounds are given (especially after iv administration), serum concentrations can be measured only for 1-2 h, which is a too short a period of time to assess the kinetic parameters. GC/MS with detection in electron capture negative ion chemical ionization mode has the sensitivity required to obtain the values necessary for pharmacokinetic studies because concentrations as low as 20-30 pg/mL can be measured with 1,4-dihydropyridine compounds that possess a nitro-phenyl moiety, as is the case for nitrendipine and nimodipine.…”

mentioning

confidence: 99%

Simultaneous Assessment of the Intravenous and Oral Disposition of the Enantiomers of Racemic Nimodipine by Chiral Stationary- Phase High-Performance Liquid Chromatography and Gas Chromatography/Mass Spectroscopy Combined with a Stable Isotope Technique

Fischer

Schönberger

Mück

et al. 1993

Journal of Pharmaceutical Sciences

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“…So, a guideline developed by the American Association of Pharmaceutical Scientists in 1987 suggests that bioavailability tests of products in humans is necessary in the evaluation of controlled-release pharmaceutical dosage forms, unless the drug is highly toxic or the testee would be in danger during the test (Skelly et al, 1987). Until now, many pharmacokinetic studies relevant for nitrendipine in humans have been reported, which verified the safety and low toxicity of the drug in human beings (Baksi & Edwards, 1989;Lobo et al, 1987;Mikus et al, 1991). As a pilot study for future clinical trials, the pharmacokinetic behaviors of two types of self-manufactured controlled-release nitrendipine formulations were investigated in four healthy male volunteers in this paper.…”

Section: Introductionmentioning

confidence: 95%

In Vivo Evaluation of Two Novel Controlled-Release Nitrendipine Formulations

Yang

Cui

You

et al. 2005

Drug Development and Industrial Pharmacy

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The objective of this work is to assess two novel controlled-release nitrendipine formulations, i.e., sustained-release nitrendipine microspheres having solid dispersion structure and a novel pH-dependent gradient-release delivery system for nitrendipine in healthy male volunteers, which were prepared by current authors. Domestic commercial nitrendipine tablets and Baypress nitrendipine tablets were employed as reference formulations. In a randomized, single-dose, fasting-state, crossover study design with a 1-week washout period, each subject received a 40-mg nitrendipine formulation. Plasma samples were collected over a 25-hour period after oral administration and were analyzed by a validated method using high performance liquid chromatography with ultraviolet detection. Pharmacokinetic parameters were determined using a noncompartmental analysis. The results provided evidence that the time to maximum plasma concentration of two novel controlled-release nitrendipine formulations were statistically significant prolonged in comparison with that of Baypress nitrendipine tablets. The relative bioavailabilities of test formulations were intensively improved compared with the domestic nitrendipine tablets, while the ratio is in a range of 80-120% in comparison with Baypress nitrendipine tablets. It is concluded that the two types of controlled-release systems are feasible for improving the dissolution rate of nitrendipine and obtaining a long-acting in vivo as well.

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Pharmacokinetics, bioavailability, metabolism and acute and chronic antihypertensive effects of nitrendipine in patients with chronic renal failure and moderate to severe hypertension.

Cited by 13 publications

References 23 publications

Concentration-Effect Analysis of Antihypertensive Drug Response

Concentration-Effect Analysis of Antihypertensive Drug Response

Simultaneous Assessment of the Intravenous and Oral Disposition of the Enantiomers of Racemic Nimodipine by Chiral Stationary- Phase High-Performance Liquid Chromatography and Gas Chromatography/Mass Spectroscopy Combined with a Stable Isotope Technique

In Vivo Evaluation of Two Novel Controlled-Release Nitrendipine Formulations

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