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Essential Oils as Carrier Oils
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Romana Aichinger, Gerhard Buchbauer
The EOs such as basil oil, petit grain oil, and thyme oil are able to enhance the permeation of nitrendipine 10–12 times by altering the solubility properties and improving the partitioning of the drug within the SC. Nitrendipine, also known as lipophilic 1,4-dihydropyridine derivative calcium channel blocker, represents a potent vasodilator able to decrease blood pressure. Because of its high first-pass effect and the following low bioavailability when administered orally, a transdermal patch is a good alternative for nitrendipine medication, noting that transdermal drug delivery is always a good choice to treat chronic disorders that require long-term dosing. Due to its poor skin permeation activity, a penetration enhancer is needed to overcome the SC barrier. Basil oil, followed by petit grain oil and thyme oil, turned out to be the best penetration enhancer among the other essential oils as it exhibits the highest increase in relative activity value due to increased thermodynamic activity and solubility of nitrendipine in the SC. The only enhancer that shows better results in facilitating the permeation of nitrendipine is oleic acid, an unsaturated fatty acid that is more effective than other saturated fatty acids. The similar structure of the oleic acid to the SC enables the fast penetration through the barrier (Mittal et al., 2008).
Cellular Regulation of Myometrial Contractility and Essentials of Tocolytic therapy
Published in Gabor Huszar, The Physiology and Biochemistry of the Uterus in Pregnancy and Labor, 2020
Several authors have begun to elucidate the role of calcium channel blockers in uterine physiology. In animal experiments with nicardipine, Csapo et al.55 showed the retardation of labor in rats ovariectomized during pregnancy. In recent experiments we demonstrated a tocolytic effect on rats with another calcium channel blocker, nitrendipine.38 Two groups of rats were treated with nitrendipine, starting on days 20 and 21 of the pregnancy (term pregnancy in rats is 22 days). The mean delivery time (hours ± S.D., past 11 a.m. on day 22) in the untreated group was 9.7 ± 6.5, while the groups who received nitrendipine from days 20 and 21 had mean delivery times of 18.9 ±9.1 (p = 0.002) and 12.8 ± 5.7, respectively. Nitrendipine treatment did not appear to influence maternal or fetal outcomes. For example, the weights of the dams and pups or the number of offsprings per dam were not different in the three groups. In order to investigate the effect of calcium channel blockers on the endocrine factors of labor, we also measured serum P levels on days 20 and 22 (the period of “P withdrawal” preceding labor in rats) in the control and experimental groups. Nitrendipine had no effect on the pattern of P one withdrawal (Figure 8), which further indicates that the actions of calcium channel blockers affect the contractile state of the myometrial muscle cells, rather than to the endocrine events underlying the initiation of labor.33
The Post-Transplant Patient with Hypertension
Published in Giuseppe Mancia, Guido Grassi, Konstantinos P. Tsioufis, Anna F. Dominiczak, Enrico Agabiti Rosei, Manual of Hypertension of the European Society of Hypertension, 2019
Martin Hausberg, Karl Heinz Rahn
In the 1990s, calcium channel blockers were recognized as very effective drugs for the treatment of hypertension in renal transplant patients. They combine vasodilating with natriuretic properties, lower blood pressure substantially and counteract cyclosporine-induced hypoperfusion (56). Therefore, they can be expected to exert some nephroprotective action after renal transplantation. Rahn et al. (57) evaluated the effects of the calcium antagonist nitrendipine on graft function in renal transplant patients receiving cyclosporine during an observation period of 2 years. Indeed, they observed a protective effect of nitrendipine on graft function which was independent of the blood pressure lowering effect.
Nanoemulsion-based dosage forms for the transdermal drug delivery applications: A review of recent advances
Published in Expert Opinion on Drug Delivery, 2022
Ankita Roy, Kumar Nishchaya, Vineet Kumar Rai
Nitrendipine is a calcium channel blocker that helps manage the hypertensive condition. However, being a BCS Class II drug, it faces solubility and bioavailability issues. Several delivery approaches have shown limited utility in this regard. However, Sharma et al. in 2020 has exploited its transdermal delivery with the help of nanoemulgel. The nitrendipine nanoemulgel comprised of 1:1 ratio of Capmul MCM and Triacetin (oil phase), Kolliphor ELP (surfactant), and Transcutol HP (co-surfactant) and 1.5% w/w Carbopol 934P showed 4-fold higher dissolution rate and up to 2-fold higher permeation flux than drug solution [18]. Dixit et al. increased Carvedilol’s solubility and transdermal penetrability in 2008 by making its NE. It showed 4500-fold higher aqueous solubility and increased skin flux and permeability [67].
Blood pressure medication should be routinely dosed at bedtime. An internist’s critical appraisal of the editorial by Rainhold Kreutz et al. (2020). Blood pressure medication should not be routinely dosed at bedtime. We must disregard the data from the HYGIA project. Blood Pressure. 29 (3):135–136
Published in Chronobiology International, 2020
The value and safety of the nighttime administration of antihypertensive medications is strengthened by the findings of the Syst-Eur (Staessen et al. 1997) and HOPE (Yusuf et al. 2000) trials. In both of these trials, participants ingested the study medications in the evening. In the Syst-Eur trial, evening administration of nitrendipine reduced the total rate of stroke by 42% and rate of non-fatal stroke by 44%. In the active treatment group, all fatal and non-fatal cardiac endpoints, including sudden death, declined by 26%; non-fatal cardiac endpoints decreased by 33% and all fatal and non-fatal CVD endpoints by 31%.