The present study investigated the effect of cocaine (COC) on cerebral circulation (CBF) and oxidative metabolism (CMRO2) in the newborn piglet and aimed to relate pharmacokinetics of cocaine to cerebrovascular effects. COC decreased CBF and CMRO2 from 75 to 64 and 4.27 to 3.91 ml/min/100 g, respectively, at 4 min with reduced flow to all brain regions (p < 0.05) which returned to baseline by 10 min. COC was rapidly metabolized with a t1/2 of 43 min and peak plasma concentration of 1,172 ng/ml. Norcocaine (NOR) appeared in plasma and CSF within 3 min of cocaine administration and remained elevated for the duration of the study along with COC in the CSF. These data show that the timing of the peak plasma COC level is associated with maximal decreased CBF. Further, the stable elevated level of COC and NOR in the CSF suggests that biotransformation does not occur in the brain. As a result, accumulation of these drugs may occur in the brain with successive COC use and affect the developing CNS in a deleterious manner.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1159/000457539 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
From Psychoactivity to Antimicrobial Agents: Multifaceted Applications of Synthetic Cathinones and Extracts.
Molecules
December 2024
Valladolid University Foundation, Valladolid University, Paseo de Belén, 11, 47011 Valladolid, Spain.
The emergence of new psychoactive substances (NPS) in the global drug market since the 2000s has posed major challenges for regulators and law enforcement agencies. Among these, synthetic cathinones have gained prominence due to their stimulant effects on the central nervous system, leading to widespread recreational use. These compounds, often marketed as alternatives to illicit stimulants such as amphetamines and cocaine, have been linked to numerous cases of intoxication, addiction and death.
View Article and Find Full Text PDFPost-mortem distribution of MDPHP in a fatal intoxication case.
J Anal Toxicol
November 2024
FT-LAB, Department of Health Science, University of Florence.
Article Synopsis
- - The study investigates the distribution of the synthetic cathinone MDPHP in post-mortem specimens of a 30-year-old man, highlighting high concentrations in urine and gastric content, suggesting potentially lethal levels.
- - Various toxicological analyses, including gas chromatography and liquid chromatography, were used to measure MDPHP and other substances, with no evidence of recent cocaine injection found.
- - Findings indicated that MDPHP levels were significantly higher compared to previously reported fatal cases, leading the researchers to conclude that the individual's death was likely due to MDPHP overdose.
Implementation of a community-based LC-UV drug checking service: promising preliminary findings on feasibility and validity.
Harm Reduct J
October 2024
Aix Marseille University, INSERM, IRD, SESSTIM, Economic and Social Sciences of Health and Medical Information Processing, Marseille, France.
Background: The increasing diversity of psychoactive substances on the unregulated drug market poses significant health, psychological, and social risks to people who use drugs (PWUD). To address these risks, various harm reduction (HR) policies have been implemented, including drug checking services (DCS). Many analytical methods are used for DCS.
View Article and Find Full Text PDFClassics in Chemical Neuroscience: Medetomidine.
ACS Chem Neurosci
November 2024
Warren Center for Neuroscience Drug Discovery and Department of Pharmacology, Vanderbilt University, Nashville, Tennessee 37232, United States.
Medetomidine is an FDA-approved α-adrenoreceptor (α-AR) agonist used as a veterinary sedative due to its analgesic, sedative, and anxiolytic properties. While it is marketed for veterinary use as a racemic mixture under the brand name Domitor, the pharmacologically active enantiomer, dexmedetomidine, is approved for sedation and analgesia in the hospital setting. Medetomidine has recently been detected in the illicit drug supply alongside fentanyl, xylazine, cocaine, and heroin, producing pronounced sedative effects that are not reversed by naloxone.
View Article and Find Full Text PDFPositive allosteric modulation of glutamate transporter reduces cocaine-induced locomotion and expression of cocaine conditioned place preference in rats.
Eur J Pharmacol
December 2024
Department of Pharmacology and Physiology, Drexel University College of Medicine, Philadelphia, PA, 191022, USA. Electronic address:
The glutamatergic system, located throughout the brain including the prefrontal cortex and nucleus accumbens, plays a critical role in reward and reinforcement processing, and mediates the psychotropic effects of addictive drugs such as cocaine. Glutamate transporters, including EAAT2/GLT-1, are responsible for removing glutamate from the synaptic cleft. Reduced expression of GLT-1 following chronic cocaine use and abstinence has been reported.
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!