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At least 55 records · Page 3Linked to original sources
PubMed1989

Transdermal delivery of narcotic analgesics: comparative permeabilities of narcotic analgesics through human cadaver skin.

Relationships between the in vitro permeation rates of select narcotic analgesics through human skin and their physicochemical properties were investigated by following the permeation kinetics of six representative compounds in small diffusion cells. The relative permeability coefficients of three phenylpiperidine analogues, meperidine, fentanyl, and sufentanil, all measured on a single piece of skin, were 3.7 x 10(-3), 5.6 x 10(-3), and 1.2 x 10(-2) cm/hr, respectively. Using membranes from the same skin section, the permeability coefficients of three opioid alkaloids, morphine, codeine, and hydromorphone, were considerably lower, at 9.3 x 10(-6), 4.9 x 10(-5), and 1.4 x 10(-5) cm/hr, respectively. The high permeability coefficients of the former compounds are due to their highly lipophilic nature as reflected in high octanol/water partition coefficients and low solubility parameters. Generally, the permeability coefficients of the narcotics increase as the lipophilicity increases. When viewed in literature perspective, the data suggest that aqueous tissue control of transport is approached in the case of the phenylpiperidine analogues, all of which have Koctanol/water values greater than 40. Permeability coefficients of fentanyl and sufentanil were also determined as a function of pH over the pH range 7.4 to 9.4, in this instance with membranes prepared from additional samples of skin. The permeability coefficients of each drug varied less than threefold over the pH range, a behavior consistent with the highly hydrophobic natures of the compounds. The low permeability coefficients of morphine, codeine, and hydromorphone coupled with their low potencies make these drugs poor transdermal candidates. It appears that fentanyl and sufentanil can be successfully transdermally delivered.

Administration, Cutaneous↗
PubMed1983

Analgesic potencies of non-narcotic, narcotic and anesthetic drugs as determined by the bradykinin-induced biting-like responses in rats.

Aversive (nociceptive) biting-like responses induced by micro-application of bradykinin solution onto rat tooth pulp were dose-dependently suppressed by non-narcotic drugs such as baclofen and lidocaine as well as carbamazepine and phenytoin, which are employed for clinical treatment of trigeminal neuralgia. The potency order of these drugs on a molar basis is baclofen (4.20) greater than carbamazepine (1.00) greater than lidocaine (0.94) greater than phenytoin (0.19). Such responses were also inhibited by morphine, pentazocine and cyclazocine (potency ratio of the three general analgesics, 1.00:0.46:8.11), indomethacin (a non-narcotic and anti-inflammatory analgesic) and alpha-chloralose (an anesthetic). The latter drug produced an analgesic effect at doses much lower than those used for anesthesia. These findings suggest that our method is feasible for evaluating the activities of general and particular analgesic drugs in the trigeminal regions.

Analgesics↗
PubMed1978

Professionalization and narcotics: the medical and pharmaceutical professions and British narcotic use 1868-1926.

This paper analyses the influence of medical professional organization on the formation of attitudes and policies toward narcotics in England. Restrictions on sale were one corollary, and the extension of medical control helped delineate a hypodermic morphine problem and disease theories of 'inebriety'. In the period 1916-26 the Home Office attempted to impose a penal and non-professional policy. The 1926 Rolleston Report marked a compromise between medical professionalism and public policy.

Attitude of Health Personnel↗
PubMed2000

[Initial effects of the 1998 revised narcotic law in substitute drug treatment of narcotic dependent patients--results of a physician survey].

UNLABELLED: To study the consequences of the last revision of the German narcotics act (1998, which forbids prescribing codeines as substitutes), a survey was carried out several months after implementation with 639 physicians, who gave substitution treatment. It could be determined how far codeine patients were ready to change their substitute, how content physicians said their patients were after changing the substitute and which were the attitudes of physicians to the revision in question. RESULTS: The majority of patients (70%) who were formerly substituted by means of codeine accepted methadone as a substitute. After the method of substitution had been changed, 51% of patients had been classified as "very content" and 35% as "reasonably content". Especially those physicians who prescribed codeines in the past, unlike physicians who used methadone for substitution treatment only, criticised the revision in question and feared that many patients should be without medical care as a consequence of the new situation.

Attitude of Health Personnel↗
PubMedDate not supplied

Fetal outcome in narcotic-dependent women: the importance of the type of maternal narcotic used.

The records of 239 infants born to 228 women dependent on narcotic drugs were reviewed to determine if type of drug abused and adequacy of prenatal care would affect pregnancy and fetal outcome. Seventy-nine (33%) pregnancies occurred in women in supervised methadone maintenance, 78 (32%) in women on unsupervised methadone maintenance, 49 (21%) in women on street heroin, and 33 (14%) in women who were multiple drug users. Although the presence of withdrawal symptoms did not differ with respect to type of drug abused, the outcome was significantly better in those infants born to women on supervised methadone maintenance as compared to all other groups (p less than 0.001). There was no demonstrable relationship between the number of prenatal visits to the clinic and fetal outcome. A relationship could not be demonstrated between the maintenance dose during pregnancy and the presence of withdrawal symptoms in the infants born to women on supervised methadone maintenance. The findings of the study suggest that supervised methadone maintenance is compatible with an uneventful pregnancy and delivery. Neonatal complications, with the exception of withdrawal, do not appear to differ from that seen among infants born to nondrug dependent women.

Adult↗
PubMed1978

Differential effects of spinal cord lesions on narcotic and non-narcotic suppression of nociceptive reflexes: further evidence for the physiologic multiplicity of pain modulation.

These studies examined the effects of bilateral lesions of the dorsolateral funiculus (DLF) of the rat spinal cord on the inhibition of a nociceptive reflex produced either by a systemic injection of 4 mg/kg of morphine or by a 20 sec exposure to 1.0 mA of transcutaneous electric shock. Reflex inhibition was quantified and analgesia inferred by use of a modified version of the D'Amour-Smith tail-flick test. Lesions which included only the DLF reduced morphine-produced analgesia (MA) by 73% but had no effect on shock-produced analgesia (SA) observed in the same rats. Baseline tail-flick latencies of this group were not affected by the lesions. Control lesions restricted to the dorsal columns attenuated neither MA nor SA. Lesions which included both the dorsal columns and DLF did not affect SA and produced no greater reduction in MA than lesions of the DLF alone. Previous work indicates that both MA and SA result, at least in part, from supraspinal activity. The current data indicate that: (1) supraspinal modulation participating in two different types of analgesic induction involves separate descending spinal pathways and (2) the maximal expression of analgesia produced by administration of narcotics requires the integrity of a supraspinal neural system projecting in the DLF.

Animals↗
PubMed1990

[Narcotic abuse in Jylland. A study based on narcotics and deaths of addicts examined at the Institute of Forensic Medicine, University of Aarhus during the period 1981-1988. 2. Deaths among addicts].

A total of 229 deaths among drug addicts (194 men and 35 women) examined of the Institute of Forensic Medicine, University of Aarhus during the period 1981-1988 is described. In 178 deaths, the cause of death was poisoning with a drug or illegal narcotic. Alcohol was involved in nearly half of these deaths and was, in addition, the cause of death in 4% of the cases. Heroin or morphine were the causes of death in one third of the cases while detropropoxyphene, methadone and ketobemidone were responsible for approximately half of the deaths. Until 1986, dextropropoxyphene was the dominating drug whereas the number of methadone deaths was considerably greater in the latter half of the period investigated than in the first half. Amphetamine alone was rarely the cause of death but the drug was seen in an increasing number of deaths in recent years. Thus, amphetamine was found in one third of the deaths in 1988.

Adolescent↗
PubMed1981

Narcotics and diabetes. II. Streptozotocin-induced diabetes selectively alters the potency of certain narcotic analgesics. Mechanism of diabetes: morphine interaction.

The antinociceptive potencies of phenazocine and levorphanol were altered similarly to that of morphine in streptozotocin (STZ)-induced diabetic and transiently hyper- or hypoglycemic mice, but the potencies of methadone, propoxyphene and meperidine were not altered by changes in serum glucose levels. The acute, s.c. LD50 of morphine in STZ-induced diabetic mice was significantly lower than in the control mice, but the acute s.c. LD50 of methadone was not altered by STZ-induced diabetes. By using morphine as the prototype drug for subsequent experiments, it was demonstrated that the potency of naloxone in antagonizing the effects of morphine in te tail-flick test was not altered in diabetics. Levels of morphine in the brains of STZ-induced diabetic mice were not significantly different from control mice. The durations of action of morphine in STZ-induced diabetes and control mice were similar. We conclude that changes in serum glucose levels can selectively alter the potency of certain narcotic analgesics. The interaction between STZ-induced diabetes and morphine-induced antinociception does not appear to be due to differences in the absorption, distribution or elimination of morphine between diabetic and nondiabetic mice.

Analgesics, Opioid↗
PubMed1981

Pharmacology of narcotic analgesics in the horse: selective blockade of narcotic-induced locomotor activity.

The locomotor responses of horses given morphine and fentanyl were blocked or lessened by administration of naloxone or acepromazine. Naloxone given at the dosage of 0.015 mg/kg completely blocked the locomotor activity induced in horses given fentanyl (0.020 mg/kg of body weight). The locomotor stimulation produced by morphine given at the dosage of 2.4 mg/kg was reduced by 75% of naloxone (0.020 mg/kg). Acepromazine partially blocked the locomotor responses to fentanyl and morphine. This blockade activity reached its peak about 30 minutes after acepromazine was given (IV) and lasted more than 6 hours. Simultaneous administration of acepromazine and morphine was associated with substantial respiratory depression for more than 4 hours after administration of both drugs. In other experiments, fentanyl did not add to the partial locomotor response observed after large doses of pentazocine were given--this being consistent with the concept that pentazocine possesses both antagonist and agonist actions at the narcotic receptor. Furosemide and phenylbutazone, given at usually used clinical doses, had no effect on the locomotor response to fentanyl, indicating that the usual clinical dosages of neither drug exerted stimulant or depressant actions.

Acepromazine↗