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Cardiovascular Drugs during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Isradipine, a dihydropyridine calcium channel blocker, is used as an antihypertensive agent. Isradipine was not teratogenic in rats given several times the human dose (data from the manufacturer’s insert). The frequency of birth defects was not increased among 80 infants whose mothers took isradipine during the first trimester in the Swedish Birth Defects Registry (Kallen, 2019). Isradipine was evaluated for the treatment of hypertension in pregnancy and was effective for the treatment of non-proteinuric hypertension. No adverse fetal effects were mentioned in this report (Wide-Swensson et al., 1995).
Traditional systemic therapies and monitoring guidelines
Published in M. Alan Menter, Caitriona Ryan, Psoriasis, 2017
Maria Polina Konstantinou, Carle Paul
Hypertension develops in 2%–15% of patients. If hypertension develops, i.e., systolic blood pressure ≥160 mmHg and/or diastolic blood pressure ≥90 mmHg in two consecutive measurements, an antihypertensive therapy should be initiated or intensified. The use of calcium channel blockers is advised, i.e., isradipine or amlodipine. If blood pressure remains high, a dosage decrease of 25% is necessary.
Ion Channels and The Control of Uterine Contractility
Published in Robert E. Garfield, Thomas N. Tabb, Control of Uterine Contractility, 2019
Calcium channel current density, normalized by cell capacitance, significantly increases during gestation (Table 1). The average density of calcium channel current is maximal at day 18 of gestation (9.2 ± 1.1 μA/μF, n = 5) and remains elevated near term (7.3 ± 2.1 μA/μF, n = 8) at day 21 of gestation. The electrophysiological properties of calcium channels are not modified during gestation. Threshold for calcium channel current (about −40 mV), the voltage at the peak inward current (about +10 mV) and extrapolated reversal potential (about + 65 mV) are virtually identical in nonpregnant and pregnant rat myometrial cells between days 10 and 21 of gestation. Sensitivity of calcium current to ( + )isradipine is not affected during gestation as the concentration producing half inhibition at a holding potential of −80 mV is about 20 n M. These results differ from those of Inoue and Sperelakis,26 which show no change of calcium channel density during pregnancy. In order to confirm the increase in calcium channel density near term ( + )-[3H]isradipine specific binding is determined in intact strips of myometrium during gestation (Table 2). The dissociation constant KD is unchanged, whereas the maximal binding capacity Bmax increases from 21.2 ± 1.1 fM/mg wet weight at day 10 (n = 4) to 32.5 ± 0.5 fM/mg wet weight at day 18 of gestation (n = 4). These results suggest that the calcium channel protein may be synthesized and incorporated in a greater amount into myometrical cells near pregnancy. The mechanisms responsible for the increase in calcium channel density are not known. However, it can be postulated that changes in hormonal status or stretching of the cells caused by fetuses may act as signals for synthesis of calcium channel proteins.
A drift on liposomes to proliposomes: recent advances and promising approaches
Published in Journal of Liposome Research, 2022
Neha Dhiman, Jayrajsinh Sarvaiya, Poorti Mohindroo
Isradipine is a dihydropyridine calcium channel antagonist, used as an antihypertensive agent but its extensive first-pass metabolism limits its use (Anekonda and Quinn 2011, Ilijic et al.2011). Bobbala et al. formulated Isradipine PLs by film deposition carrier method, comprising HSPC and cholesterol (1:1), and spray-dried mannitol. The morphology of the formulation was studied using optical and scanning electron microscopy. The mean size of the vesicles was <700 nm and EE was measured between 89 and 97%, respectively. The Isradipine encompassing PLs disclosed an increased transport across the rat intestine, compared to a pure drug suspension. The research group added that the formulated Isradipine PLs improved the oral bioavailability of drug (2.4 times), compared to pure drug suspension along with desired intestinal permeability characteristics and can improve the low bioavailability issue related to the free drug (Bobbala and Veerareddy 2012).
Physicochemical, pharmacokinetic, and pharmacodynamic characterization of isradipine tablets for controlled release
Published in Pharmaceutical Development and Technology, 2021
D. Nagasamy Venkatesh, S. N. Meyyanathan, R. Shanmugam, S. S. Kamatham, J. R. Campos, J. Dias-Ferreira, E. Sanchez-Lopez, J. C. Cardoso, P. Severino, E. B. Souto
Isradipine is a well-known poorly water-soluble antihypertensive drug, commonly used in the treatment and management of hypertension. Its posology is usually 2.5 mg for immediate-release capsules, twice a day, because of its reduced water solubility (<10 µg/L at 37 °C) and therefore short plasma half-life (Hof and Rüegg 1988; Johnson et al. 2005; Ilijic et al. 2011; Tran et al. 2013). Sustained release (SR) solid dosage forms for oral administration may be effective to improve the therapeutic outcomes with drug molecules that exhibit a narrow therapeutic range and/or have a fast clearance from the blood (Venkatesh et al. 2020a, 2020b). Several categories of modified-release formulations for oral administration have been developed to improve the clinical outcomes of poorly water-soluble drugs and drugs with short half-lives, and also to increase patients’ compliance (Varum et al. 2010; Sahu et al. 2017). Modified-release formulations (e.g. controlled, sustained, delayed, and prolonged) aim at delivering drugs at a predetermined rate. These dosage forms are characterized by a release kinetics that keeps the drug concentration within its therapeutic window for a pre-determined time-frame (Yuen 2010; Goyanes et al. 2015). Besides the marketed 5 mg Dynacirc® capsules recommended for the treatment of hypertension (Schran et al. 1988), isradipine SR tablets have not yet been proposed for the treatment of left ventricular morphology function in systemic hypertension, or to minimize cardiovascular risk factors occurring in smoking cessation and type II diabetes mellitus (Staessen et al. 1988; Van Den Berg and Dehmer 1988; Grossman et al. 1991; Kumar et al. 2016). Its very limited water-solubility and short biological half-life, together with the need to increase patients’ compliance, especially in the management of hypertension, demand for new oral SR formulations for this drug. The novelty of this work is the development of a modified release tablet formulation that may reduce the number of doses required for the treatment of hypertension, thereby reducing the risk of overdose and associated adverse side effects.