Kinetic and cardiovascular comparison of immediate-release isradipine and sustained-release isradipine among non-treatment-seeking, cocaine-dependent individuals

Johnson, Bankole A.; Javors, Martin A.; Lam, Y. W. Francis; Wells, Lynda T.; Tiouririne, Mohamed; Roache, John D.; Ait-Daoud, Nassima; Lawson, Kevin

doi:10.1016/j.pnpbp.2004.08.014

Cited by 19 publications

(31 citation statements)

References 11 publications

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“…Since a 90% CI for C max and AUCs ratios were ranging within the limits of the FDA (80-125%), it was determined that the two types of 5 mg SR isradipine formulations were considered to be bioequivalent. In previous reports, absorption of an orally administrated IR isradipine capsule in the fasting condition was rapid with 1.2-2.0 h of T max and 6.1-13.8 h of elimination half-life (T 1/2 ) [16][17][18]21]. SR isradipine capsules took about 3-4 times longer (6 h) for the T max compared to IR isradipine.…”

Section: Clinical Pharmacokinetic and Bioequivalence Study In Healthymentioning

confidence: 93%

“…Plasma concentrations of isradipine were in the standard curve range and remained above the LLOQ (10 pg/mL) for the entire sampling period except for one subject at 0.66 h, one subject at 1 h, one subject at 24 h, and one subject at 36 h after dosing. Even though the bioavailability of orally administered isradipine was characterized by considerable interindividual variation [16,19,21], the plasma profiles of the mean isradipine concentration versus time after oral administration of a single dose of both formulations in 24 subjects exhibited closely similar patterns. The mean estimated pharmacokinetic parameters derived from the plasma concentration profiles of isradipine are shown in Table 2 for the formulation effect in all tested parameters).…”

Section: Clinical Pharmacokinetic and Bioequivalence Study In Healthymentioning

confidence: 98%

“…The pharmacokinetics of isradipine have been reported following oral administration of immediate-release (IR) isradipine or sustained-release (SR) isradipine in healthy volunteers [16][17][18][19], cardiac patients [20], and cocaine-dependent individuals [21]. At an oral dose ranging between 2.4-20 mg, the pharmacokinetics of isradipine appeared to be linear [16,17].…”

Section: Introductionmentioning

confidence: 99%

“…At an oral dose ranging between 2.4-20 mg, the pharmacokinetics of isradipine appeared to be linear [16,17]. However, at doses needed to reduce blood pressure, the side effects associated with the vasodilatory activity were usually mild, transient, and welltolerated [7,19,21,22]. SR isradipine which has a significantly lower C max and extended T max compared to IR isradipine, exhibits a more favorable cardiovascular profile [18,21].…”

Section: Introductionmentioning

confidence: 99%

“…However these methods, possess disadvantages such as low sensitivity [6,19,26], long analytical run times [6,26], or pre-column derivatization processes [25]. The quantified data from the HPLC techniques coupled with UV detection (HPLC/UV) [21,27,28], and electrochemical detection (HPLC/ECD) [29] exhibit a LLOQ of almost 0.5 ng/ml. In addition, a spectrofluorometric method was recently published, but this method offered low sensitivity (16 ng/ml LLOQ) and needed derivatization to enhance the fluorescent intensity because isradipine itself yields little native fluorescence [30].…”

Section: Introductionmentioning

confidence: 99%

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Quantification of isradipine in human plasma using LC–MS/MS for pharmacokinetic and bioequivalence study

Park

Rhim

et al. 2009

Journal of Chromatography B

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Section: Clinical Pharmacokinetic and Bioequivalence Study In Healthymentioning

confidence: 93%

Section: Clinical Pharmacokinetic and Bioequivalence Study In Healthymentioning

confidence: 98%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Quantification of isradipine in human plasma using LC–MS/MS for pharmacokinetic and bioequivalence study

Park

Rhim

et al. 2009

Journal of Chromatography B

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Isradipine plasma pharmacokinetics and exposure–response in early Parkinson’s disease

Venuto

Yang

Javidnia

et al. 2021

Ann Clin Transl Neurol

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Objectives Isradipine is a dihydropyridine calcium channel inhibitor that has demonstrated concentration‐dependent neuroprotective effects in animal models of Parkinson’s disease (PD) but failed to show efficacy in a phase 3 clinical trial. The objectives of this study were to model the plasma pharmacokinetics of isradipine in study participants from the phase 3 trial; and, to investigate associations between drug exposure and longitudinal clinical outcome measures of PD progression. Methods Plasma samples from nearly all study participants randomized to immediate‐release isradipine 5‐mg twice daily (166 of 170) were collected for population pharmacokinetic modeling. Estimates of isradipine exposure included apparent oral clearance and area under the concentration‐time curve. Isradipine exposure parameters were tested for correlations with 36‐month changes in disease severity clinical assessment scores, and time‐to‐event analyses for initiation of antiparkinson therapy. Results Isradipine exposures did not correlate with the primary clinical outcome, changes in the antiparkinson therapy‐adjusted Unified Parkinson’s Disease Rating Scale parts I–III score over 36 months (Spearman rank correlation coefficient, rs: 0.09, P = 0.23). Cumulative levodopa equivalent dose at month 36 was weakly correlated with isradipine plasma clearance (rs: 0.18, P = 0.035). This correlation was sex dependent and significant in males, but not females. Those with higher isradipine exposure had decreased risk of needing antiparkinson treatment over 36 months compared with placebo (hazard ratio: 0.87, 95% CI: 0.78–0.98, P = 0.02). Interpretation In this clinical trial, higher isradipine plasma exposure did not affect clinical assessment measures of PD severity but modestly decreased cumulative levodopa equivalent dose and the time needed for antiparkinson treatment initiation. Trial Registration http://ClinicalTrials.gov NCT02168842.

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Pharmacokinetic properties of isradipine after single‐dose and multiple‐dose oral administration in Chinese volunteers: a randomized, open‐label, parallel‐group phase I study

Wang

Jin

Wang

et al. 2013

Biomedical Chromatography

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Isradipine could be used for the treatment of high blood pressure or Parkinsonism, yet the study on pharmacokinetics (PK) of isradipine is lacking in the Chinese population. The current study aims to assess the dose proportionality, pharmacokinetics and gender effect of isradipine following oral single and multiple doses in Chinese subjects. A randomized, open-label, parallel-group trial was conducted in 30 healthy Chinese volunteers. Subjects randomly received a single dose of 2.5, 5 or 10 mg, and multiple doses (2.5 mg) of isradipine. Blood samples were collected pre-dose (0 h) and 0.33, 0.67, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 h post-dose. Isradipine was rapidly absorbed with the time to maximum concentration <1.27 h for all dosage groups. The maximum concentrations were 2.46, 5.34, 10.93 and 3.32 ng/mL and area under the concentration-time curve from time zero to the last time point (AUClast ) were 7.05, 12.58, 24.68 and 5.31 ng/ml · h for the 2.5, 5 and 10 mg single-dose and 2.5 mg multiple-dose groups, respectively. The half-life ranged from 5.76 to 7.94 h. The maximum concentration and AUC were found to increase linearly and dose-dependently for isradipine. No statistical gender differences were found. These findings indicated that the pharmacokinetic parameters of isradipine in Chinese population were dose-proportional and predictable over a range of 2.5-10 mg isradipine oral doses.

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Kinetic and cardiovascular comparison of immediate-release isradipine and sustained-release isradipine among non-treatment-seeking, cocaine-dependent individuals

Cited by 19 publications

References 11 publications

Quantification of isradipine in human plasma using LC–MS/MS for pharmacokinetic and bioequivalence study

Quantification of isradipine in human plasma using LC–MS/MS for pharmacokinetic and bioequivalence study

Isradipine plasma pharmacokinetics and exposure–response in early Parkinson’s disease

Pharmacokinetic properties of isradipine after single‐dose and multiple‐dose oral administration in Chinese volunteers: a randomized, open‐label, parallel‐group phase I study

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