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PubMedDate not supplied

[The characteristics of the morphological changes to the parenchymatous organs in persons who used street narcotics].

Morphologic signs of narcomania in subjects using primitively prepared narcotics from opium-containing raw material are described. Sites of injections and inflammatory reactions in the parenchymatous organs are described. Special attention is paid to productive hypersensitive inflammation, which can serve as a sign confirming narcomania in subjects using poorly purified narcotic mixture. The authors classify the granulomas in such patients as toxic allergic granulomatosis.

Adolescent↗

PubMed1964

THE USE OF CHANGES IN CAPILLARY PERMEABILITY IN MICE TO DISTINGUISH BETWEEN NARCOTIC AND NONNARCOTIC ALALGESICS.

An extension of the "squirming test" is described which makes the method specific for nonnarcotic analgesics. The intraperitoneal injection of acetic acid causes squirming and an increase in capillary permeability that is measured by direct estimation of plasma-bound dye (Pontamine Sky Blue) which has leaked into the peritoneal cavity. Nonnarcotic analgesics inhibit squirming and leakage of dye. Values for the oral ED50s for both effects are given for a number of typical compounds. Narcotic analgesics, in doses that produce analgesia, inhibit squirming but do not significantly affect leakage of dye. Drugs that stimulate the central nervous system and also inhibit squirming have no significant effect on leakage of dye over the range of doses which inhibit squirming. Corticosteroids do not significantly inhibit either squirming or leakage of dye.

Acetates↗

PubMed1989

[Analysis of regional trends in narcotic studies between 1980 and 1986].

During the period of survey, the number of narcotic drug seizures by the law, especially cannabis resin, has increased considerably. The details on this development are presented. The following main analytical results were obtained: the median concentration of THC in cannabis resin has increased up to 8.6%, in cannabis plants the THC content has fluctuated between 1% and 3%. In the heroin samples since 1982, diamorphin has predominated in the base form; the diamorphin content had dropped to 32%, which is connected with a rise simultaneous in the concentration of noscapine (up to 9%). The concentration of cocaine hydrochloride had diminished at the end of the period to 62%; on the other hand, the amphetamine sulfate content increased to 69%. LSD trips used from 10 to 120 micrograms per trip. Methadone occurred mostly in the form of tablets containing 5 mg methadone hydrochloride.

Amphetamine↗

PubMed1981

Assessment of physical dependence-inducing capacity of narcotic agonists and antagonists in rats by intermittent infusion technique.

Narcotics and other drugs were injected into the rat once an hour for about 1 week. Morphine and codeine showed physical dependency with a maintenance dose as low as 9.6 mg/kg/day. Development of dependence was also recorded in rats treated with cyclazocine (9.6 mg/kg/day) and pentazocine (96 mg/kg/day), and suspected in the levallorphan-treated (9.6 mg/kg/day) rats. Dependence on pethidine, which is known to be difficult to detect by the usual method in rats, also developed in this experiment (96 mg/kg/day), but it was estimated to be of lesser degree than that of codeine. Dependence on allazocine (9.6 mg/kg/day) and aminopyrine (96 mg/kg/day) did not develop. Barbital dependence (96 mg/dg/day) was induced, but it was distinguished from morphine-like drugs by the naloxone precipitation test and by substitution experiments. Cross-dependence between morphine and dependence-inducing drugs was investigated. Withdrawal weight loss in the morphine-dependent rats was suppressed or attenuated by pentazocine, pethidine, and codeine. Withdrawal weight loss in the rats dependent on cyclazocine, pentazocine, pethidine, or codeine was suppressed by morphine. Intermittent infusion of pentazocine at longer intervals induced dependence not as severe as that induced by 1-h infusion.

Animals↗

PubMed1982

Interactions between narcotic agonists, partial agonists andd antagonists evaluated by punished an unpunished behavior in the rat.

The effects of morphine, ketocyclazocine, cyclazocine, and SKF-10,047 were tested alone and in conjunction with naltrexone or naloxone, in rats responding under a multiple fixed-interval 3-min schedule of food presentation. Under this paradigm, electric shock was delivered on a fixed-ratio schedule for responses occurring during alternate schedule components. All of the drugs (except naltrexone and naloxone) decreased average rates of responding maintained by the unpunished component in a dose-dependent manner. The rate-decreasing effects of morphine and ketocyclazocine were antagonized by naltrexone. The rate-decreasing effects of cyclazocine were only slightly reversed by the antagonists, while those effects of SKF-10,047 were not affected by naltrexone. In some animals, certain doses of SKF-10,047 increased unpunished responding. This rate-increasing effect was antagonized by naltrexone. Morphine, ketocyclazocine, cyclazocine, and SKF-10,047 increased responding that was suppressed by electric shock, and these increases were antagonized by naltrexone and naloxone. Thus, the antagonism of opiate effects by narcotic antagonists depends in part on the behavior being evaluated.

Animals↗

PubMed2006

Narcotic analgesics for acute migraine in the emergency room: are we meeting Headache Societies' guidelines?

We analysed 161 patients with acute migraine in our emergency room (ER) to identify the use of narcotic analgesics as first-line treatment. Twenty-four percent of patients were treated with opioid analgesics and 76% patients were treated with non-opioid analgesics. Pain was completely relieved in 100 (62%) patients, partially relieved in 50 (31%) patients and was not relieved in 11 (7%) patients at the time of discharge. Pain relief was not related to the use of opioids vs. non-opioids. The treatment of acute migraine in our ER is in line with the guidelines of the Headache Societies and needs further improvement.

Adolescent↗

PubMed1999

Double-blind, randomized study of nalmefene and naloxone in emergency department patients with suspected narcotic overdose.

STUDY OBJECTIVES: To compare the efficacy, safety, and withdrawal symptoms in emergency department patients with suspected narcotic overdose treated with nalmefene, an opioid antagonist with a 4- to 10-hour duration of action, with those treated with naloxone. METHODS: Adults in 9 centers who would otherwise receive naloxone for altered consciousness levels were randomly assigned to receive intravenous study drug (1 mg nalmefene, or 2 mg nalmefene or 2 mg naloxone, double-blinded) every 5 minutes as needed for up to 4 doses in a 4-hour study. Outcomes were 20-minute and 4-hour posttreatment changes in respiratory rates, Neurobehavioral Assessment Scale scores, Opioid Withdrawal Scale scores, and incidences of adverse events. RESULTS: Opioid positivity was recorded for 30 of 63 (1-mg nalmefene), 23 of 55 (2-mg nalmefene), and 24 of 58 (naloxone) cases, 75% of whom also had nonopioid central nervous system depressants. Most patients received only 1 dose of study drug. Similar, clinically meaningful improvements in respiratory rates and Neurobehavioral Assessment Scale scores were seen with all treatments. No statistical differences in efficacy or withdrawal outcomes were seen between treatment groups, and no significant overall time-treatment interactions occurred, in either the entire patient group or among opioid-positive cases (P >.21, all comparisons). Adverse events occurred in 30.9% (2 mg nalmefene), 15.9% (1 mg nalmefene), and 15.5% (naloxone) of patients (P >.08); none were associated with morbidity. CONCLUSION: In this study of patients with varied potential causes of altered consciousness, nalmefene (1 mg and 2 mg) and naloxone (2 mg) appeared to be efficacious, safe, and to yield similar clinical outcomes.

Adult↗

PubMed1981

Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.

The N-allyl and N-(cyclopropylmethyl) analogues of (-)-alpha-acetylmethadol and (-)-alpha-methadol have been synthesized and evaluated for opiate agonist and opiate antagonist activity. Both acetylmethadol analogues possessed weak analgesic activity in vivo tests for narcotic analgesia; the N-allyl analogue partially antagonized morphine-induced tail-flick analgesia. All four compounds possessed only opiate agonist-like activity as determined by in vitro studies measuring inhibition of [3H]naloxone binding to opiate receptors.

Animals↗

PubMed1975

Narcotic agonist and antagonist potencies of a homologous series of N-alkyl-norketobemidones measured by the guinea-pig ileum and mouse vas deferens methods.

The narcotic agonist and antagonist potencies of the series of N-alkyl-norketobemidones from norketobemidone to decylnorketo-bemidone have been determined. The values obtained in the electrically stimulated preparations of the guinea-pig ileum and the mouse vas deferens are closely correlated. The agonist potencies observed in the guinea-pig ileum agree well with those found in the mouse hot-plate test (Oh-ishi & May) and those obtained by determining the inhibition of naloxone binding in brain homogenates (Wilson, Rogers, Pert & Snyder). The antagonist potencies in the guinea-pig ileum and, to a lesser extent, those in the mouse vas deferens agree with the values obtained in the morphine-dependent monkey.

Animals↗

PubMed1977

The solution to narcotic addiction in the People's Republic of China.

The People's Republic of China dealt with addiction as a political problem, offering the new society hope, food, shelter, work, and land instead of opium. Addiction no longer had its appeal. Opium producing poppies were replaced by food corps. Large opium distributors were imprisoned. Addicts were "clean". A mass campaign against addiction mobilized the entire nation. Before Liberation in 1949, the Chinese Communist Party had kept opium out of their areas. However, it took until 1953 to rid China completely of opium. Twenty million Chinese outside the People's Republic of China continue to have serious narcotic addiction problems.

China↗

PubMed2005

Hospital security response to narcotics theft.

Diversion of narcotics by health professionals is increasing, the author says, and professional security can be helpful to Pharmacy and Nursing in conducting a successful investigation. However, Security must recognize the reluctance of other departments to prosecute offenders, and utilize a team approach to develop a working relationship with those departments.

Drug and Narcotic Control↗

PubMed1980

Pharmacological studies with an alkylating narcotic agonist, chloroxymorphamine, and antagonist, chlornaltrexamine.

The 6-bis(2)chloroethyl)amino derivatives of oxymorphone and naltrexone, chloroxymorphamine (COA) and chlornaltrexamine (CNA), respectively, produce an irreversible inhibition of [3H]naltrexone binding to mouse brain homogenates. Intracerebroventricular (i.c.v.) injection of COA (4 nmol/mouse) elicits analgesia which lasts 4 times longer than analgesia produced by equimolar and equieffective dose of oxymorphone. The analgesia induced by COA can be reversed and blocked by naloxone. Injections of both COA and CNA i.c.v. antagonize morphine-induced analgesia for 3 days. Similarly, when [3H]naltrexone binding is measured in brains from mice pretreated i.c.v. with COA or CNA, there is a significant decrease in total specific binding for 3 days after pretreatment. These data suggest that CNA and COA alkylate the opioid receptors to produce antagonist and agonist-antagonist effects, respectively. The implications of these findings are discussed with respect to their effect on our perception of the opioid receptor-narcotic agonist interaction and the mechanisms of tolerance and dependence.

Analgesics↗

PubMedDate not supplied

The technique of controlled delivery as a weapon in dealing with illicit traffic in narcotic drugs and psychotropic substances.

The technique of controlled delivery is used when a consignment of illicit drugs is detected and allowed to go forward under the control and surveillance of law enforcement officers in order to secure evidence against the organizers of such illicit drug traffic. This technique has been proved effective in some countries in identifying and bringing to justice principals, organizers and financiers of the illicit drug traffic. The controlled delivery technique is compatible with the requirements of the Single Convention on Narcotic Drugs, 1961, but its application depends on the particular legal and administrative provisions in the countries concerned. The technique merits wider use, and it does not involve any element of entrapment. It has been used most effectively when illicit drugs are discovered in unaccompanied freight consignments or in the post. Controlled deliveries involving a courier present special difficulties and should be treated with caution. In a controlled delivery, security of information is of paramount importance as is the appropriate knowledge and co-operation of the law enforcement authorities. Such co-operation is essential between the country in which the initial detection of drugs has occurred, transit countries and the country of final destination. A number of important detections have been made as a result of speedy international co-operation of this type between law enforcement authorities.

Crime↗

PubMedDate not supplied

The role of the South American Agreement on Narcotic Drugs and Psychotropic Substances in the fight against illicit drug trafficking.

The States Parties to the South American Agreement on Narcotic Drugs and Psychotropic Substances (ASEP), which entered into force on 26 March 1976, decided to co-ordinate measures to achieve close co-operation and the efficient exchange of information between States Parties to the Agreement in the fight against drug abuse and illicit drug traffic. To this end, ASEP organizes regional and international training courses, seminars and conferences on the subject of illicit drug trafficking; facilitates permanent exchange of information between the States Parties to the Agreement regarding drug law enforcement techniques and the methods resorted to by illicit traffickers; and maintains close technical co-operation with the International Criminal Police Organization (Interpol), the United Nations and other international agencies concerned with drug control. In addition, ASEP is involved in a number of activities that indirectly contribute to the suppression of illicit drug trafficking such as: the establishment of national drug control co-ordinating bodies; co-operation between States in the area of legislative measures conducive to drug control; and the operation of a computerized system designed to facilitate contacts between the various drug law enforcement agencies of the States Parties to ASEP.

Crime↗

PubMedDate not supplied

Forfeiture of narcotics-generated wealth in the United States of America pursuant to the Comprehensive Forfeiture Act of 1984.

Trafficking in illegal narcotics and dangerous drugs exists mainly because it yields immense profits and it can be eradicated only by depriving traffickers of their drug derived profits and economic power. With that in mind and to cope more effectively with the problem, the United States Congress recently enacted the Comprehensive Forfeiture Act of 1984, which revised and strengthened the existing laws and procedures. This Act is comprised of four parts. Part A amends the forfeiture proceedings of the Racketeer Influenced and Corrupt Organization (RICO) statute. Part B adds a new criminal forfeiture statute to the Comprehensive Drug Abuse Prevention and Control Act of 1970, which permits forfeiture in all drug felony cases. This newly created section of the Act also adopts other measures, a number of which are identical to those contained in part A of the RICO amendments. In addition, part B contains a civil forfeiture provision to reach land and buildings used to facilitate felonious drug offenses. Part C, inter alia, establishes a revolving fund for the use of the Department of Justice in enforcing forfeiture laws and amends existing provisions regarding the disposition of forfeited property. Part D sets up a Customs Forfeiture Fund.

Crime↗

PubMed1998

Pharmacokinetics of a non-narcotic analgesic, DA-5018, in rats.

The pharmacokinetics of a non-narcotic analgesic, DA-5018, were compared after single intravenous (i.v.), subcutaneous (s.c.), and oral administrations, and after multiple (seven consecutive days) s.c. administration to rats. After i.v. administration of DA-5018, 1, 2, and 5 mg kg-1, the pharmacokinetic parameters of DA-5018 were independent of the dose ranges studied. After oral administration of DA-5018, absorption of the drug from gastrointestinal (GI) tract was fast, but the extent of absolute bioavailability (F) was low; the values were 23.2, 23.0, and 27.3% for 2, 5, and 10 mg kg-1, respectively. After single s.c. administration of DA-5018, absorption of the drug from the injected site was fast and the extent of absorption was fairly good; the F values were 74.5 and 71.8% for 2 and 5 mg kg-1, respectively. The lower F values after oral administration of DA-5018 to rats could be due to degradation of the drug in rat GI tract and/or considerable first-pass effect. After i.v., oral, and s.c. administration of DA-5018, the drug had a strong affinity to the rat tissues studied as reflected in the greater-than-unity tissue to plasma ratio. After i.v., oral, and s.c. administration of the drug, the biliary and urinary excretion of unchanged DA-5018 were negligible. There was no significant difference in the pharmacokinetics or tissue distribution of DA-5018 between single and multiple s.c. administration of the drug, 5 mg kg-1, to rats, indicating that there could be no tissue accumulation of the drug after multiple s.c. administration of the drug to rats.

Administration, Oral↗

PubMed2001

Narcotic drug methohexital: synthesis by enantioselective catalysis.

The narcotic drug methohexital 1 contains two asymmetric carbon atoms and, thus, consists of four isomers, two diastereomeric pairs of enantiomers. The commercial drug is the so-called alpha-racemate, one pair of diastereomers only. A method was developed to prepare differently enriched mixtures of methohexital isomers without resorting to lengthy and expensive optical resolutions. A model reaction for the synthesis of methohexital is the palladium-catalyzed allylation of 1,5-dimethyl-barbituric acid 3, which is optimized and checked by molecular modeling. Catalysts with the best ligands are used in the allylation of the methohexital precursor 7, which contains the C(6) sidechain at the tetrahedral center of the barbiturate skeleton. The product stereochemistry was determined by the contribution of the enantioselective Pd catalysts and by the fact that the allylation is a kinetic resolution. The methohexital isomer mixtures obtained were evaluated with the corneal stimulus test of rats. Methohexital compositions were found, which are superior to the commercially used alpha-racemate (Brevimytal).

Anesthetics, Intravenous↗

PubMed1975

Biocompatible implants for the sustained zero-order release of narcotic antagonists.

Implantable, sustained release drug delivery devices offer benefits not obtained through oral ingestion or injection. These include delivery at a constant therapeutic rate, thus avoiding adverse intermittent and massive dose effects, as well as reliance upon patients taking their prescribed dosages. The drawbacks to their widespread acceptance have been their inability to maintain a zero-order release rate over an extended period of time and poor biocompatibility. Devices capable of satisfying these requirements have been developed and tested extensively for in vitro release of the narcotic antagonist cyclazocine. By using implant models prepared from Hydron, a hydrophilic polymer known to exhibit excellent tissue compatibility, we have found that the release rate could be precisely regulated by proper geometry, copolymer composition, concentration of ionogenic groups and cross-link density. Devices in such varied forms as capusles, barrier-film coated tablets and bulk polymerized rods have been tested in vitro for periods approaching 1 year.

Biocompatible Materials↗