Search results for "Narcotic"
showing 10 items of 106 documents
Diffusion of naltrexone across reconstituted human oral epithelium and histomorphological features
2006
Abstract In transbuccal absorption a major limitation could be the low permeability of the mucosa which implies low drug bioavailability. The ability of naltrexone hydrochloride (NLX) to penetrate a resembling histologically human buccal mucosa was assessed and the occurrence of any histomorphological changes observed. We used reconstituted human oral (RHO) non-keratinised epithelium as mucosal section and a Transwell diffusion cells system as bicompartmental model. Buccal permeation was expressed in terms of drug flux ( J s ) and permeability coefficients ( K p ). Data were collected using both artificial and natural human saliva. The main finding was that RHO does not restrain NLX permeat…
Bioavailability in vivo of naltrexone following transbuccal administration by an electronically-controlled intraoral device: a trial on pigs.
2010
Naltrexone (NLX), an opioid antagonist, is widely used in the treatment of opiate addiction, alcoholism and smoking cessation. Its current peroral administration induces various adverse side effects and has limited efficacy since bioavailability and patient compliance are poor. The development of a long-acting drug delivery system of NLX may overcome the current drawbacks and help in the improvement of treatment of addiction. The primary endpoints of this study were: a) to compare the NLX bioavailability and pharmacokinetics after delivering a single transbuccal dose, released by a prototype of intraoral device, versus an intravenous (I.V.) bolus of the same drug dose; b) to verify the func…
Release of naltrexone on buccal mucosa: Permeation studies, histological aspects and matrix system design
2007
Transbuccal drug delivery has got several well-known advantages especially with respect to peroral way. Since a major limitation in buccal drug delivery could be the low permeability of the epithelium, the aptitude of NLX to penetrate the mucosal barrier was assessed. Ex vivo permeation across porcine buccal mucosa 800 microm thick was investigated using Franz type diffusion cells and compared with in vitro data previously obtained by reconstituted human oral epithelium 100 microm thick. Both fluxes (Js) and permeability coefficients (K(p)) are in accordance, using either buffer solution simulating saliva or natural human saliva. Permeation was evaluated also in presence of chemical enhance…
The role of the hospital pharmacy in the storage and supply of antidotes
2013
Cases of poisoning have been analyzed with the aim of estimating both the incidence and the seriousness of such xenobiotic effects, the major determinant agents, and the related antidotes used in hospital departments. From 2009 to November 2012, a survey of the availability of antidotes in the emergency room services was carried out in all hospital pharmacies under the Palermo Health Authority: Policlinico Paolo Giaccone, ARNAS Civico di Cristina Benefratelli, Azienda Ospedaliera Ospedali Riuniti Villa Sofia-Cervello. Figures show that the majority of poisoning events were caused by the use/abuse of drugs, especially psychopharmaceuticals, alcohol and narcotic substances. This overdose of m…
Direct ELISA kits as a sensitive and selective screening method for abstinence control in urine.
2011
In 2009 cutoff values of assessment criteria to testify abstinence control in order to estimate driving ability were standardized in Germany. The cutoff values are lower than required in existing guidelines like SAMHSA and there is critical discussion about detection of low concentrations by using immunoassay, especially concerning amphetamines in urine (50 ng/ml). In this study Direct ELISA kits were tested for their applicability to identify the absence of amphetamines, cannabinoids, opiates, cocaine, methadone and benzodiazepines in urine. Results were confirmed by LC/MS or GC/MS analyses. Sensitivity, specificity, predictive values (positive as well as negative) and overall misclassific…
Influence of sample preparation on analytical results: drug analysis [GC/MS] on hair snippets versus hair powder using various extraction methods
1997
The comparison of aqueous extraction methods and hair extraction by organic solvents performed on hair powder as well as on hair snippets of the same sample revealed different qualities of the procedures. Qualitative and quantitative results by the same derivatization step and GC/MS detection demonstrated, that the risk of missing a drug substance is higher using hair snippets than after drug extraction on pulverised hair. Drug recovery for opiates, cocaine and benzoylecgonine from hair was found to be best in aqueous solvents or in methanol extracts. The results are discussed under the aspects of solid-phase extraction, the hair sample representing an inhomogenous material. The localisatio…
On cosmetically treated hair — aspects and pitfalls of interpretation
1997
Popular hair cosmetic treatments like bleaching or permanent waving were found to affect the stability of incorporated drugs and to cause alterations of the fibers at an ultrastructural level. This may result in a partial or complete loss of drug substances, depending on the particular drug molecule and on its concentration prior to the cosmetic treatment. Moreover, from literature, there is some evidence that drug molecules are not only incorporated into the growing fiber by passive diffusion from blood into the matrix cells and melanocytes, but that the substances enter the hair also via perspiration such as sweat and sebum. Since permed and bleached hair shows an enhanced sorption capaci…
Opioid switching from and to tapentadol extended release in cancer patients: conversion ratio with other opioids
2013
Objectives: The aim of this exploratory study was to assess the conversion ratios between tapentadol and other opioids in patients requiring an opioid switching. Methods: A prospective study was carried out in a convenience sample of consecutive patients admitted to an acute palliative care unit and a home care unit for a period of 1 year. Patients who were switched from/to tapentadol were selected. The initial ratio between tapentadol and other opioids, expressed as oral morphine equivalents was 1:3.3. The subsequent doses were flexible and were changed to fit the patients’ needs. Pain intensity and distress score were recorded until opioid doses were stable. In all, 37 patients were exami…
Cross-reinstatement by cocaine and amphetamine of morphine-induced place preference in mice
2005
The cross-reinstatement by psychostimulants of a conditioned place preference (CPP) induced by morphine was evaluated in mice. In Experiment 1, we examined the effects of a single dose of cocaine and amphetamine on a previously extinguished morphine CPP. After acquisition of CPP induced by morphine (40 mg/kg), animals underwent daily extinction sessions of 15 min duration until the CPP was extinguished. Subsequently, animals received a non-contingent injection of cocaine (25 mg/kg) or amphetamine (4 mg/kg), which produced the reinstatement of the extinguished morphine-induced CPP. In Experiment 2, we evaluated the reinstating effects of several priming doses of cocaine (Experiment 2A) or am…
Intracellular glutathione in human hepatocytes incubated with S-adenosyl-L-methionine and GSH-depleting drugs
1991
Abstract The present study was undertaken to investigate (a) whether S- adenosyl- L -methionine (SAMe) added to culture medium can increase intracellular glutathione (GSH) levels in human hepatocytes and (b) whether SAMe can prevent the GSH depletion found in human hepatocytes incubated with GSH-depleting drugs (paracetamol, opiates, ethanol). Incubation of hepatocytes with increasing concentrations of SAMe resulted in a dose-dependent elevation of intracellular GSH content, which reached its maximum (35% increase) at 30 μM after 20 h. SAMe, as the only sulfur source in the medium, was efficient in repleting GSH-depleted hepatocytes following treatment with diethyl maleate. Incubation of hu…