Objectives: The aim was to investigate the effect of Huang-Lian-Jie-Du-Decoction (HLJDD) on the pharmacokinetic behaviour of verapamil in rats.
Methods: Rats orally received 3.33 g/kg of HLJDD extract for 14 days, and pharmacokinetics of verapamil was investigated after oral and intravenous verapamil. Norverapamil formation for assessing cytochrome P450 3A activity in hepatic and intestinal microsomes of the HLJDD-treated rats was investigated. The inhibitory effect of berberine on the formation of norverapamil in intestinal and hepatic microsomes was also evaluated.
Key Findings: HLJDD treatment increased the plasma concentration of verapamil and decreased the plasma concentration of norverapamil, resulting in a 24% increase in the AUC(0-480) of verapamil and a 25% reduction in the AUC(0-480) of norverapamil after oral administration. However, HLJDD did not alter the pharmacokinetic behaviour of verapamil after intravenous administration. Norverapamil formation showed biphasic kinetics in both intestinal and hepatic microsomes. HLJDD treatment significantly decreased the intrinsic clearance of verapamil in intestinal microsomes, but had no effect on the hepatic metabolism of verapamil. Berberine also inhibited norverapamil formation in both intestinal and hepatic microsomes; the extent of inhibition was larger in intestinal microsomes.
Conclusions: HLJDD displayed a route-dependent effect on the pharmacokinetics of verapamil in rats. HLJDD treatment increased the bioavailability of verapamil partly via inhibiting first-pass verapamil metabolism in the intestine.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1211/jpp.62.04.0005 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Curvilinear regression analysis and ranking of migraine treatment drugs using degree-based topological indices and the WASPAS method.
Comput Biol Med
January 2025
Department of Mathematics, COMSATS University Islamabad, Vehari Campus, 61100, Vehari, Pakistan. Electronic address:
Topological indices, derived from molecular graphs, provide valuable numerical descriptors for the comprehensive analysis of pharmaceuticals. These indices are pivotal in the physicochemical characterization and predictive assessment of various drugs. In this study, we calculate several degree-based topological indices for a range of migraine treatment medications, including aspirin, caffeine, eletriptan, ergotamine, sumatriptan, rizatriptan, verapamil, diclofenac, frovatriptan, and droperidol.
View Article and Find Full Text PDFA Longitudinal Exploration of -Related Hemiplegic Migraine in Children Using Electronic Medical Records.
Neurol Genet
February 2025
Division of Neurology, Children's Hospital of Philadelphia, PA.
Background And Objectives: Since the initial description of related hemiplegic migraine (HM), the phenotypic spectrum has expanded from mild episodes in neurotypical individuals to potentially life-threatening events frequently seen in individuals with developmental and epileptic encephalopathies. However, the overall longitudinal course throughout childhood remains unknown.
Methods: We analyzed HM and seizure history from electronic medical records in individuals with -related HM, delineating frequency and severity of events in monthly increments through a standardized approach.
Artemisinin-Quinidine Combination for Suppressing Ventricular Tachyarrhythmia in an Ex Vivo Model of Brugada Syndrome.
J Korean Med Sci
January 2025
Division of Cardiology, Department of Internal Medicine, Chonnam National University Medical School, Gwangju, Korea.
Background: The ionic mechanism underlying Brugada syndrome (BrS) arises from an imbalance in transient outward current flow between the epicardium and endocardium. Previous studies report that artemisinin, originally derived from a Chinese herb for antimalarial use, inhibits the Ito current in canines. In a prior study, we showed the antiarrhythmic effects of artemisinin in BrS wedge preparation models.
View Article and Find Full Text PDFEffects of antihypertensives with and without IL-6 lowering properties on long-term blood pressure control: The prospective HELIUS cohort.
Int J Cardiol Cardiovasc Risk Prev
March 2025
Department of Public and Occupational Health, Amsterdam Public health Research Institute, Amsterdam university Medical Center, University of Amsterdam, Amsterdam, the Netherlands.
Article Synopsis
- Chronic inflammation, particularly the role of interleukin-6 (IL-6), is being explored as a target for improving hypertension treatment.
- In a study involving 1,510 participants over six years, it was found that calcium channel blockers (CCBs) with IL-6-lowering properties (specifically amlodipine and barnidipine) resulted in better blood pressure control compared to other CCBs.
- No significant differences were seen in blood pressure control among other antihypertensive classes or across different ethnic groups, indicating a need for further research into IL-6's impact on hypertension management.
Determination of residual alkyl iodides and alkyl bromides as their corresponding alkyl chlorides in drug substances by headspace GC-FID.
Heliyon
December 2024
Curia Wisconsin, Inc. D/B/A Siegfried Acceleration Hub, 870 Badger Circle, Grafton, WI, 53024, United States.
Primary and secondary alkyl iodides and primary alkyl bromides were quickly and conveniently converted into their corresponding alkyl chlorides via S2 halide-halide substitution. The resultant alkyl chlorides simultaneously demonstrated increased volatility and stability paired with standard headspace GC-FID methodology. The derivatization was performed on both standard and sample alike and occurred during the headspace oven equilibration phase, eliminating the extra reaction step traditionally performed during many derivatization analyses.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!