Use of amlodipine oral solution for the treatment of hypertension in children

Vossen, A.C. van der; Cransberg, Karlien; Winter, Brenda C M de; Schreuder, Michiel F.; Rooij-Kouwenhoven, Roos W G van; Vulto, Arnold G.; Hanff, Lidwien M.

doi:10.1007/s11096-020-01000-9

Cited by 4 publications

(6 citation statements)

References 10 publications

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“…Pleasingly, this reaction protocol could also be applied for the post-modification of biologically active molecules or drugs, which are highly valuable for the discovery of novel clinical candidate compounds. For example, amlodipine is a commonly used antihypertensive drug in clinical practice . In this transition metal-free CN–K catalytic system, the formylation of the primary amine could be achieved in 85% isolated yield without affecting any other functional groups (Table , 2i ), even though a bis-alkene substituted cyclic amine is also present in the molecule.…”

Section: Resultsmentioning

confidence: 99%

“…For example, amlodipine is a commonly used antihypertensive drug in clinical practice. 69 In this transition metal-free CN−K catalytic system, the formylation of the primary amine could be achieved in 85% isolated yield without affecting any other functional groups (Table 1, 2i), even though a bis-alkene substituted cyclic amine is also present in the molecule.…”

Section: Methodsmentioning

confidence: 99%

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Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO₂

et al. 2022

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As an effective approach toward sustainability and global carbon balance, the reductive conversion of CO2 into value-added chemicals is of considerable significance. Here, by simply calcining the mixture of NH4SCN and KCl in an air atmosphere, potassium dopants and negatively charged electron-rich centers are simultaneously introduced into carbon nitride materials via a metalation engineering strategy. The resultant metalized catalysts with deprotonated imide sites and doped potassium ions demonstrate much-enhanced activity for catalyzing CO2 reductive hydrosilylation with excellent conversion and >90% selectivity, whereas the pristine carbon nitride catalyst shows only negligible activity. Both experimental and theoretical results reveal the crucial role of the negatively charged electron-rich centers and potassium dopants in tailoring the energy band positions and electronic structure for the efficient donor–acceptor interaction and much increased driving force for CO2 reduction. The present work offers molecular-level insights into the boosted CO2 reduction activity via engineering the electronic structure of the metalized carbon nitride catalyst and reducing the energy offset between frontier molecular orbitals of CO2 and the catalyst, which can provide a conceptual guide for further development of efficient catalytic CO2 reduction systems.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO₂

et al. 2022

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“…For comparison with the observed trough concentration (C min ) in the paediatric population [ 72 ], virtual trials in the paediatric population matching the demographic of observed data were run at 3 doses daily for 21 days, with the median (0.15 mg/kg/day), 1st interquartile (0.10 mg/kg/day), and 3rd interquartile (0.22 mg/kg/day). Additionally, the virtual paediatric subjects administered with more than 5mg/day were filtered out following the maximum daily dose allowed, resulting in 99%, 85%, and 58% of the virtual subjects being included for verification for 0.10, 0.15, and 0.22 mg/kg/day doses, respectively.…”

Section: Methodsmentioning

confidence: 99%

“… Simulated steady-state trough concentration (C min ) of amlodipine multiple dose in the paediatric population. Solid red circles represent the observed trough concentration of amlodipine published by van der Vossen et al (2020) [ 72 ]. Coloured open circles represent predicted trough concentration for 3 doses: 0.15 mg/kg/day, 0.10 mg/kg/day, and 0.22 mg/kg/day.…”

Section: Figurementioning

confidence: 99%

“…Acceptance of the simulation in paediatric populations with and without obesity was based on the VPC alone because, based on our search, only sparse data on amlodipine concentrations were available in paediatric populations [72,73]. Simulated plasma concentrations that mimicked the study design and dosing range of both studies fell in the middle of the reported plasma concentration data precisely when simulations were performed based on the mean and median doses [72,73]. Additionally, the proportion of obese children in the simulated population was comparable to that reported by Flynn et al (2006) [73] (50.73-50.86% versus 43.2%).…”

Section: Step 3: Validation Of the Amlodipine Modelmentioning

confidence: 99%

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The Impact of Paediatric Obesity on Drug Pharmacokinetics: A Virtual Clinical Trials Case Study with Amlodipine

Burhanuddin,

Mohammed,

Badhan

2024

Pharmaceutics

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The incidence of paediatric obesity continues to rise worldwide and contributes to a range of diseases including cardiovascular disease. Obesity in children has been shown to impact upon the plasma concentrations of various compounds, including amlodipine. Nonetheless, information on the influence of obesity on amlodipine pharmacokinetics and the need for dose adjustment has not been studied previously. This study applied the physiologically based pharmacokinetic modelling and established a paediatric obesity population to assess the impact of obesity on amlodipine pharmacokinetics in children and explore the possible dose adjustments required to reach the same plasma concentration as non-obese paediatrics. The difference in predicted maximum concentration (Cmax) and area under the curve (AUC) were significant between children with and without obesity across the age group 2 to 18 years old when a fixed-dose regimen was used. On the contrary, a weight-based dose regimen showed no difference in Cmax between obese and non-obese from 2 to 9 years old. Thus, when a fixed-dose regimen is to be administered, a 1.25- to 1.5-fold increase in dose is required in obese children to achieve the same Cmax concentration as non-obese children, specifically for children aged 5 years and above.

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Pharmacological importance of novel spiro derivatives against human pathogenic fungi

Sharma

Saxena

et al. 2023

BIOMED KHIM

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Human mycoses have become a threat to health world-wide. Unfortunately there are only a limited number of antimycotic drugs in use. In the present study, antifungal activity of earlier synthesized spiro-1,4-dihydropyridines (1,4-DHPs) was investigated. The antifungal activity of spiro-1,4-DHPs compounds were screened against Aspergillus flavus, A. fumigatus, and Candida albicans by using Disc Diffusion and Modified Microdilution method. Among six spiro-1,4-DHPs compounds tested all of them showed stronger antifungal activity possibly through inhibiting the synthesis of chitin in cell wall against A. flavus, A. fumigatus, and C. albicans as compared to fluconazole, a standard antifungal drug. The combination of compounds showed that the synthesized compounds had synergistic, additive effects as compared to currently used drugs as an antifungal agent. These results indicated that these designed compounds were potential chitin synthase inhibitors and had excellent antimycotic activity for the treatment of fungal infections.

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Use of amlodipine oral solution for the treatment of hypertension in children

Cited by 4 publications

References 10 publications

Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO₂

Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO₂

The Impact of Paediatric Obesity on Drug Pharmacokinetics: A Virtual Clinical Trials Case Study with Amlodipine

Pharmacological importance of novel spiro derivatives against human pathogenic fungi

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Use of amlodipine oral solution for the treatment of hypertension in children

Cited by 4 publications

References 10 publications

Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO2

Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO2

The Impact of Paediatric Obesity on Drug Pharmacokinetics: A Virtual Clinical Trials Case Study with Amlodipine

Pharmacological importance of novel spiro derivatives against human pathogenic fungi

Contact Info

Product

Resources

About

Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO₂

Metalized Carbon Nitrides for Efficient Catalytic Functionalization of CO₂