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PubMed1988

Effects on mice locomotor activity of a narcotic-like principle from Psidium guajava leaves.

Studies were carried out on the suppression of both exploratory and spontaneous locomotor activities in the mouse by a non-polar fraction from a methanol extract of the dried leaves of Psidium guajava. Shortly after intraperitoneal administration of this fraction, typical narcotic-like effects were observed, including catalepsy, analgesia, Straub tail, shallow respiratory movements and exophthalmos. The dose for 90% suppression of exploratory activity was between 3.3 and 6.6 mg/kg intraperitoneally and the onset of action was 6-8 min. The duration of activity was dose-dependent and, for a dose of 13.2 mg/kg given intraperitoneally, it was found to be more than 6 h. Qualitatively similar results on exploratory activity were obtained when the extract was administered orally. Doses of 3.3-6.6 mg/kg i.p. depressed spontaneous locomotor activity and tunnel running was curtailed. Higher doses abolished the spontaneous locomotor reflex action. A flavonoid compound or compounds appear to account for the activity seen.

Animals↗
PubMed1991

Cost analysis of two implantable narcotic delivery systems.

This survey compares costs of two commonly utilized implantable narcotic delivery systems. The systems are classified into type-I (exteriorized system using the DuPen epidural catheter) and type-II (implanted system using the Synchromed pump). Costs were analyzed by reviewing actual patient hospital financial service records and Homecare vendor quotations. From the perspective of cost analysis alone, we conclude that savings accrue when patients requiring treatment beyond 3 months duration are managed with a type-II implanted system compared with a type-I system with an external pump.

Adult↗
PubMed1996

N-cubylmethyl substituted morphinoids as novel narcotic antagonists.

N-Cubylmethylnormorphine (1) and N-cubylmethylnoroxymorphone (2) have been synthesized and found to be more potent ligands at the mu and kappa opioid receptors than morphine and oxymorphone respectively. In the guinea-pig ileum preparation, compounds 1 and 2 were characterized as opioid mu antagonists (Ke = 68 and 16 nM, respectively). Compound 2 also showed effective kappa-antagonism (Ke = 22 nM). The narcotic antagonism activity of 1 has been confirmed by in vivo assays.

Analgesics, Opioid↗
PubMed2005

Surface enhanced Raman scattering for narcotic detection and applications to chemical biology.

Raman spectroscopy is rapidly finding favour for applications in the life science because of the ease with which it can be used to extract significant data from tissue and cells. However, the Raman effect is an inherently weak effect, which hinders the analysis of low concentration analytes. Raman sensitivity can be improved via the surface enhanced Raman scattering (SERS) effect. In SERS, Raman spectra are dramatically amplified when a molecule is adsorbed onto nano-roughened noble metal surfaces such as silver and gold. The degree of enhancement enables single-molecule detection, which offers the potential for the unambiguous identification of analytes at concentrations that are useful in both a forensic and a chemical biology context. Here we discuss some of the practical applications of SERS to both low-level narcotic detection, and how this can be applied to chemical biology.

Bacteria↗
PubMed2003

Interactions of the narcotic l-alpha-acetylmethadol with human cardiac K+ channels.

l-alpha-acetylmethadol is a long-acting narcotic analgesic that is used in the treatment of opiate addiction. However, the drug has been associated with cases of QT interval prolongation and ventricular arrhythmia. To understand the mechanism underlying these clinical findings, we examined the effects of l-alpha-acetylmethadol on the cloned human cardiac K(+) channels HERG (human ether-a-go-go-related gene), KvLQT1/minK and Kv4.3. Using patch clamp electrophysiology, we found that l-alpha-acetylmethadol inhibited HERG channel currents in a voltage-dependent manner displaying an IC(50) value of 3 microM. The major active metabolite of l-alpha-acetylmethadol, noracetylmethadol, inhibited HERG with an estimated IC(50) values of 12 microM. l-alpha-acetylmethadol had little or no effect on Kv4.3 or KvLQT1/minK K(+) channel currents at concentration up to 10 microM. We conclude that the proarrhythmic effects of l-alpha-acetylmethadol are due to specific blockade of the HERG cardiac K(+) channel and that its active metabolite noracetylmethadol may provide a safer alternative in the treatment of opiate addiction.

Animals↗
PubMed1985

Pharmacological effects of sedative-hypnotics, narcotic analgesics, and alcohol during sleep.

This article briefly reviews the well known effects of sedative-hypnotics, alcohol and narcotics on sleep. These drugs also have respiratory depressant effects, and the limited information about their effects on sleep-related breathing disturbances is reviewed. They exacerbate obstructive sleep apnea syndrome and have moderate to minimal effects on occasional apnea or hypopnea, but do not induce breathing disturbances de novo.

Adult↗
PubMed1987

Stimulants and narcotic drugs.

This article focuses on the use of stimulant and narcotic drugs, as well as lookalike preparations that are subject to abuse. There is a brief discussion of the pharmacology of these agents, demographic use patterns, and treatment modalities.

Adolescent↗
PubMed1992

Evaluation of cutaneous responses and lung function from exposure to opiate compounds among ethical narcotics-manufacturing workers.

We recently demonstrated morphine-6-hemisuccinate-human serum albumin conjugate (M-6-HS-HSA)-specific IgG in serum from ethic narcotics-manufacturing workers. In this article, we present results of epicutaneous tests to opiate compounds and lung-function studies in these same workers. Thirty-nine workers, exposed to opiates, were evaluated for possible work-related changes in lung function and were administered a questionnaire concerning opiate exposure and health history in February 1988. In December 1988, 33 employees with occupational exposure to opiates, six other workers (New Jersey referent) employed at the same factory with minimal exposure to opiate compounds, and 17 nonexposed individuals from Cincinnati, Ohio, were subjected to epicutaneous threshold testing with a panel of six opiate compounds and nine common aeroallergens. In opiate-exposed workers, significantly lower epicutaneous threshold concentrations were detected (compared to New Jersey referent and Cincinnati control subjects) for dihydrocodeine (p less than 0.01), hydrocodone (p less than 0.05), codeine (p less than 0.01), and morphine (p less than 0.05). Significant associates existed among epicutaneous threshold concentrations between the agents tested; that is, individuals with a positive morphine skin test would generally have a positive codeine skin test, etc. Atopic status (positive cutaneous test results to two or more of nine common aeroallergens) was not significantly associated (p greater than 0.05) with positive opiate skin sensitivity. Although the mean cross-shift decrements in FEV1 for all workers were nonsignificant, five opiate-exposed individuals demonstrated cross-shift decrements in FEV1 of greater than 10%. Daily maximum-minus-minimum changes in workweek PEFR (PEFRmax-min) were significantly reduced for Monday through Thursday (p less than 0.05) compared to PEFRmax-min changes during a nonwork, nonexposure 3-day weekend. Ten exposed workers demonstrated daily PEFRmax-min changes of greater than 20%, suggesting acute airway obstruction. Increased cutaneous reactivity to opiate compounds among opiate-exposed workers may reflect development of pharmacologic hyperresponsiveness to opiate compounds.

Adult↗
PubMed1986

Sites and mechanisms of basic narcotic receptor function based on current research.

Within the past decade, progress in opiate pharmacology has been phenomenal and has stimulated widespread interest. Several potent endogenous peptides with morphine-like activity were isolated and their structures were established. Opioid receptors in the brain were localized and characterized. Plausible hypotheses to explain the mechanism of action of the narcotic analgetics have been proposed. Antagonist-agonists that are potent analgesics with low addition liability were introduced for clinical application. Epidural administration of morphine and its surrogates to reduce side effects and prolong drug action is gaining increasing popularity. Extensive research is ongoing concerning the use of opioids in the treatment of shock and the mental states. Some of these advances will be discussed.

Animals↗
PubMedDate not supplied

Preclinical toxicity and teratogenicity studies with the narcotic antagonist analgesic drug TR5379M.

The narcotic antagonist TR5379M had po LD50 values of 365 and 750 mg/kg and iv LD50 values of 35.0 and 22.3 mg/kg in the mouse and rat, respectively. Subchronic (one month) po administration to rats at 40, 120, or 400 mg/kg/day and to cynomolgus monkeys at 20, 45, or 100 mg/kg/day showed the compound to be well tolerated at doses of 40 and 45 mg/kg, respectively. Deaths during the subchronic studies included one monkey following a single dose of 100 mg/kg and six rats following repeated doses of 400 mg/kg. Signs of toxicosis in rats included clonic convulsions (high-dose animals only) and mild dose-related salivation and hyperactivity. Signs of toxicosis in monkeys were limited to sporadic emesis and transiently decreased food consumption at all three dose levels. Emesis was not observed at doses of 20 or 45 mg/kg after the first week. Slightly increased weights (not significant at 40 mg/kg) for thyroid and adrenal glands occurred in male rats. Gross, microscopic, and clinical pathologic examinations revealed no treatment-related adverse effects at any dose level for either species. Administration of TR5379M to pregnant rats (20, 70, or 250 mg/kg/day on Days 6-15 of gestation) caused no teratogenicity or embryotoxicity and did not adversely affect any of the reproductive parameters examined. Dams given TR5379M at doses of 70 and 250 mg/kg salivated and had reduced weight gain. It was concluded from these studies that TR5379M has an adequate margin of safety to begin clinical investigations.

Abnormalities, Drug-Induced↗
PubMed2003

Narcotic drugs change the expression of cytochrome P450 2E1 and 2C6 and other activities of carcinogen-metabolizing enzymes in the liver of male mice.

Drug-metabolizing enzymes play a great role in the bioactivation and also detoxification of zenobiotics and carcinogens such as N-nitrosamines and polycyclic aromatic hydrocarbons (PAHs). Therefore, the present study was undertaken to investigate the effect of narcotic drugs such as cannabis (hashish) and diacetylmorphine (heroin) on the activity of N-nitrosodimethylamine N-demethylase I [NDMA-dI], arylhydrocarbon [benzo(a)pyerne] hydroxylase [AHH], cytochrome P450 (CYP), cytochrome b(5), NADPH-cytochrome c reductase, glutathione-S-transferase, and levels of glutathione and thiobarbituric acid-reactive substances (TBARS). In addition, the present study showed the influence of hashish and heroin after single (24 h) and repeated-dose treatments (4 consecutive days) on the expression of cytochrome P450 2E1 (CYP 2E1) and cytochrome P450 2C6 (CYP 2C6). The expression of CYP 2E1 was slightly induced after single-dose and markedly induced after repeated dose-treatments of mice with hashish (10 mg kg(-1) body weight). Contrarily, heroin markedly induced the expression of CYP 2C6 after single-dose and potentially reduced this expression after repeated-dose treatments. It is believed that N-nitrosamines are activated principally by CYP 2E1 and in support of this, the activity of NDMA-dI was found to be increased after single- and repeated-dose treatments of mice with hashish by 23 and 41%, respectively. In addition, single- and repeated-dose treatments of mice with hashish increased: (1) the total hepatic content of CYP by 112 and 206%, respectively; (2) AHH activity by 110 and 165%, respectively; (3) NADPH-cytochrome c reductase activity by 21 and 98%, respectively; (4) and glutathione level by 81 and 173%, respectively. Also, single-dose treatments of mice with heroin increased the total hepatic content of CYP, AHH, NADPH-cytochrome c reductase, and glutathione level by 126, 72, 39, 205%, respectively. However, repeated dose-treatments of mice with heroin did not change such activities except cytochrome c reductase activity increased by 20%. Interestingly, the level of free radicals, TBARS, was potentially decreased after single or repeated-dose treatments with either hashish or heroin. It is clear from this study that the effects of hashish are different from those of heroin on the above mentioned enzymes particularly after repeated dose treatments. It is concluded that hashish induced the expression of CYP 2E1 and other carcinogen-metabolizing enzymes activities, and this induction could potentiate the deleterious effects of N-nitrosamines and aromatic hydrocarbons, e.g. benzo(a)pyrene, upon the liver and probably other organs. Such alterations may also change the therapeutic actions of other drugs, which are primarily metabolized by the P450 system, when administered to peoples using hashish or heroin.

Animals↗
PubMed1997

Corneal reflex responses to mechanical and electrical stimuli in coma and narcotic analgesia in humans.

The corneal reflex, a bilateral eye-blink, can be elicited in humans either by mechanical or electrical corneal stimulation. Both in comatose patients and in normal subjects injected with the opiate fentanyl, the electrically-evoked corneal reflex was more suppressed than the mechanically-evoked reflex. We propose that the mechanical input yields a reflex more resistant to depression of the corticoreticular drive and to narcotic analgesia, because it exploits temporal summation at central synapses, whereas the electrical input exploits spatial summation.

Adult↗
PubMed1999

Sigmoidal admission rate-dependence of toluene narcotic potency in rats: comparison with nitrous oxide.

Aromatic solvents, such as toluene, can cause depression of the central nervous system functions in both solvent-exposed workers and abusers. The mechanism by which toluene produces its effects is generally thought to be similar to that produced by general anaesthetics, including inert gases and alcohols. However, whether lipophilic compounds indirectly influence activity by perturbing membrane lipids or bind directly to proteins remains a major question. In a recent study, the sigmoidal admission rate-dependence of inert gas anaesthetic potency has been suggested to possibly reflect a direct narcotic-protein interaction. Therefore, experiments have been carried out using seven input toluene flows of 0.5, 1, 2, 3, 4, 5 and 6 l/min. Our results indicate that as the rate of toluene delivery increased, the concentration of toluene required to produce anaesthetic effects increased. Although this was fitted relatively well with linear regression, this fitted better when using a sigmoidal model (r = 0.998 vs. r = 0.971, P < 0.01). In addition, comparison with previous data on nitrous oxide shows a striking similarity between plots (r = 0.991) which appears consistent with a similar site of action for both agents. We suggest that all classes of lipophilic agents could produce their inhibitory effects at similar 'non-specific' sites of action of finite size and limited occupancy.

Anesthetics, Inhalation↗
PubMed1997

Determination of a new non-narcotic analgesic, DA-5018, in plasma, urine and bile by high-performance liquid chromatography.

A high-performance liquid chromatographic method was developed for the determination of a new non-narcotic analgesic, DA-5018 (I), in rat plasma, urine and bile samples, using propranolol for plasma samples and protriptyline for urine and bile samples as internal standards. The method involved extraction followed by injection of 100 microliters of the aqueous layer onto a C18 reversed-phase column. The mobile phases were 5 mM methanesulfonic acid with 10 mM NaH2PO4 (pH 2.5)-acetonitrile, 70:30 (v/v) for plasma samples and 75:25 (v/v) for urine and bile samples. The flow-rates were 1.0 ml/min for plasma samples and 1.2 ml/min for urine and bile samples. The column effluent was monitored by a fluorescence detector with an excitation wavelength of 270 nm and an emission wavelength of 330 nm. The retention time for I was 4.8 min in plasma samples and 10.0 min in urine and bile samples. The detection limits for I in rat plasma, urine and bile were 20, 100 and 100 ng/ml, respectively. There was no interference from endogenous substances.

Analgesics, Non-Narcotic↗
PubMed1997

Distinguishing passive contamination from active cocaine consumption: assessing the occupational exposure of narcotics officers to cocaine.

Hair analysis has been used in probationary and parole populations to monitor for cocaine use, but only in very limited settings or circumstances. Its wider adoption has been limited by questions regarding the ability to distinguish environmental contamination of hair via casual contact from actual ingestion. To evaluate this capability we sought to identify persons routinely exposed to cocaine, who were not cocaine users. Undercover narcotics officers engaged in cocaine-centered enforcement activities and evidence room clerks who have no history of cocaine use were identified as an appropriate example population. Thirty-six active undercover officers and four evidence technicians were asked to voluntarily submit hair samples for analysis. Additionally two cocaine contaminated (aqueous soaked), three negative control samples, and hair from a self-reported crack smoker were also blindly submitted to the testing laboratory. The hair samples were washed and after washing, enzyme digested. The wash solutions and hair digest were each analyzed for the presence of cocaine. The results indicate that nearly every person had trace amounts of cocaine contamination in the wash fraction, and one person had cocaine present in their hair digest That person, when retested, was a negative. The laboratory correctly identified and characterized the contaminated, negative, and positive controls. The study concludes that the findings support the capability of hair analysis to distinguish cocaine use from exposure under normal field conditions. The study results indicate that cocaine-abstinent persons who are in chronic, casual environmental contact with cocaine are not likely to test hair positive for cocaine using the analysis protocols followed in this project. The study also indicates that passive microingestion of cocaine needs to be considered when examining persons who are in cocaine intensive environments.

Cocaine↗
PubMed1993

Narcotics and local anesthetics.

The recognition and alleviation of animal pain is a growing veterinary and public concern. Pain can be of an acute or chronic nature with different behavioral manifestations. Physiologically, pain is a dynamic and complex phenomenon that produces changes in the central and autonomic nervous systems as well as in the endocrine system. Horses and other animals appear to possess an endogenous pain-suppressing system involving the brainstem and spinal cord. This system can modulate pain perception and the responses to it. The recently discovered endogenous opioid peptides (endorphins and enkephalins) appear to play a role in this system, which is activated by stress. Opioids (narcotic analgesics) act to selectively depress pain-sensitive cells. Opioid analgesics may act via multiple opioid receptors. Each subclass of opioid receptor has a different pharmacologic profile. Classical opioids that act at mu (morphine) receptors typically produce analgesia, increased locomotor activity, cardiorespiratory stimulation, and a decrease in intestinal peristalsis in the horse. Opioids that act at kappa receptors produce analgesia, sedation, ataxia, and minimal autonomic effects in the horse. Owing to their lack of excitatory actions, the kappa opioids represent a potentially useful class of analgesics for use in equine species. Local anesthetics depress all excitable cells and can diminish sensory, motor, and muscular function. They do not act selectively on pain fibers, although pain is among the first sensations lost following a nerve block. Local anesthetic activity is enhanced by increased extraneuronal pH, nerve cooling, increased nervous activity, coadministration of a vasoconstrictor or hyaluronidase, delayed systemic absorption, prolonged drug metabolism, and by using agents with high lipid solubility. Procaine, lidocaine, and mepivacaine are among the most widely used and studied agents in horses. These agents and/or their metabolites can be readily detected in urine; in some cases, for prolonged periods.

Anesthetics, Local↗
PubMed1998

Comparative safety evaluation of non-narcotic analgesics.

Both spontaneous reports and single outcome studies may distort the overall safety evaluation of drugs. We identified epidemiologic studies, published from January 1970 to December 1995, that investigated the association of serious adverse effects with aspirin, diclofenac, acetaminophen, and dipyrone to determine and compare the excess mortality associated with short-term drug use. The estimated excess mortality due to community-acquired agranulocytosis, aplastic anemia, anaphylaxis, and serious upper gastrointestinal complications was 185 per 100 million for aspirin, 592 per 100 million for diclofenac, 20 per 100 million for acetaminophen, and 25 per 100 million for dipyrone. The estimates were largely influenced by the excess mortality associated with upper gastrointestinal complications. A relative risk estimate of 300 or more for the association of dipyrone with agranulocytosis would have been necessary for the excess mortality of dipyrone to be comparable to that of aspirin or diclofenac. Based on published epidemiologic evidence used to determine the excess mortality associated with short-term use of these four non-narcotic analgesics, the current regulatory ranking of the drugs appears inappropriate.

Acetaminophen↗
PubMed2002

QSAR study on narcotic mechanism of action and toxicity: a molecular connectivity approach to Vibrio fischeri toxicity testing.

Quantitative structure-activity relationships (QSARs) have been established based on narcotic mechanism of action and toxicity data to Vibrio fischeri using molecular connectivity indices. The results obtained suggest that both, the degree of branching and electronic characteristic of the compounds have dominant role in the exhibition of toxicity. The information obtained in the present study will be useful in designing more potent compounds.

Algorithms↗