Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Codeine”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 1,783 records · Page 99Linked to original sources
PubMed1982

Concerning the specificity of the hypothalamic opiate receptor responsible for food intake in the rat.

Direct application of small quantities of morphine (a mu-opiate receptor agonist) to the ventromedial hypothalamus (VMH) of rats can induce a stimulated food intake. Because this effect is only partly reduced by the opiate antagonist naloxone, given into the VMH, various other studies were undertaken to examine characteristics of the receptors at this site. The opiate agonist levorphanol but not its stereoisomer dextrorphan effectively increased feeding. Codeine, a weak opiate ligand, was also ineffective as were the kappa-opioid agonist ketocyclazocine and the sigma-opioid agonist phencyclidine. the hyperthermia which accompanies peripheral and central injections of morphine was not observed after hypothalamic application of a quantity of levorphanol sufficient to stimulate feeding. This leads us to propose that the opioid receptors in the VMH are: (1) stereoselective; (2) responsive to mu-, but not kappa- or sigma-agonists: and (3) different from the receptors that elicit hyperthermia.

Animals↗
PubMed1984

Induction of human cutaneous mast cell degranulation by opiates and endogenous opioid peptides: evidence for opiate and nonopiate receptor participation.

In order to examine the capacity of pharmacologically useful opiates to stimulate human mast cell secretion, subjects were skin tested with morphine, codeine, or meperidine hydrochloride. All three agents acted equipotently in eliciting positive immediate skin reactions from all subjects tested. Each agent demonstrated 10 mm of net whealing at 5 to 10 micrograms base (16.7 to 40.4 nmol) injected intradermally. The ability to elicit immediate skin test reactions with endogenous opioid peptides was examined with the use of dynorphin, [D-Ala, 2-D-Leu5] enkephalin, beta-endorphin, and morphiceptin . All four compounds induced wheal-and-flare reactions with the order of potency: dynorphin, greater than beta-endorphin, and greater than [D-Ala, 2-D-Leu5] enkephalin approximately equal to morphiceptin at dose ranges of 0.3 to 8.45 nmol. The inhibition of reactivity by hydroxyzine and the demonstration of mast cell degranulation by electron microscopy suggest that the immediate skin responses to opioid stimulation occur as a consequence of mast cell degranulation. Experiments with the opioid receptor antagonist, naloxone, suggest that both opioid and nonopioid receptors may be involved. These results imply that endogenous opioid peptides possibly may play a role in mast cell function and/or degradulation .

Codeine↗
PubMed1977

On the sensitivity of the tourniquet pain test.

Twenty-four chronic pain patients were given, on each of 4 successive days, oral doses of 60 mg morphine, 60 mg codeine, 600 mg aspirin and placebo, using a double-blind counterbalanced design. Two hours after ingestion, subjective pain estimates and tourniquet pain scores were obtained. Variability of the tourniquet pain scores was too great for differences in response to the analgesics to be significant. However, differences in pain estimates were also too small to discriminate among the drugs, and the lack of sensitivity may be a function of pain chronicity. The tourniquet techniques will continue to be useful until there is a purely objective measure of the severity of clinical pain.

Aspirin↗
PubMed1985

Substitution and primary dependence studies in animals.

The mixed agonist-antagonist analgesics buprenorphine, butorphanol, nalbuphine, pentazocine and picenadol were compared to the prototype mu and kappa agonists morphine and Mr 2033, respectively, in the following tests in rhesus monkeys: overt behavioral effects upon acute administration in drug-naive animals; discriminative stimulus properties in monkeys trained to respond to either etorphine or ethylketazocine; self-administration of the test agent relative to codeine; single dose suppression and precipitation in withdrawn and non-withdrawn morphine-dependent monkeys, respectively; and primary addiction studies in drug-naive animals. Whereas both buprenorphine and nalbuphine precipitate withdrawal in morphine-dependent monkeys, withdrawal following chronic administration of buprenorphine resulted in no observable signs of abstinence, while nalbuphine withdrawal was similar to that seen in morphine-dependent monkeys. Butorphanol, pentazocine and picenadol all produced mild dependence of the kappa-type; that is, natural withdrawal behavior similar to that seen following chronic Mr 2033 administration.

Animals↗
PubMed1986

Evaluation of tilidine for morphine-like subjective effects and euphoria.

Tilidine is an opioid analgesic that has been abused predominantly by the oral route. Studies of parenterally administered tilidine in animals did not clearly indicate a dependence potential of the morphine type. In this study we examined the abuse potential of orally and parenterally administered tilidine in humans. Both orally and intramuscularly given tilidine produced miosis and morphine-like subjective effects in non-dependent subjects. Oral tilidine was 1/8-1/10 as potent and intramuscular tilidine was 1/22 as potent as parenteral morphine in producing morphine-like subjective and miotic effects. Intramuscular tilidine suppressed and did not precipitate signs of abstinence in morphine-dependent subjects. However, intramuscularly given tilidine produced toxic effects not seen with morphine. Meperidine, codeine and d-propoxyphene produced morphine-like subjective and miotic effects, but also produced toxic effects at the highest doses tested. The results suggest that tilidine has a potential to be abused, that this potential is less than that of parenteral morphine and that tilidine is more likely to be abused orally than by the intramuscular route.

Administration, Oral↗
PubMed1995

Simultaneous determination of dihydrocodeine and dihydromorphine in serum by gas chromatography-tandem mass spectrometry.

A sensitive and specific method was developed for the determination of dihydrocodeine and its metabolite dihydromorphine in human serum using codeine and morphine as internal standards. Measurement is performed with GC-tandem MS after one simple extraction step and derivatization to the pentafluoropropionic esters. Sensitivity of the method is excellent and allows for the reproducible quantification of dihydrocodeine and dihydromorphine with limits of quantification of 2 ng/ml and 40 pg/ml serum, respectively. The method is therefore well suited for investigation of the pharmacokinetics and the metabolism of dihydrocodeine.

Codeine↗
PubMed1995

Reversed-phase high-performance liquid chromatography--photodiode-array analysis of alkaloid drugs of forensic interest.

A reversed-phase high-performance liquid chromatography-photodiode-array method for the analysis of 23 drugs of forensic interest is presented. The separation method development was based on mobile-phase optimisation, temperature control and use of three ODS stationary phases. Multiwavelength detection and quantitation was performed at 225, 232, 239, 254, 275 and 289 nm. Absorbance rationing proved to be very helpful for the identification of these drugs. Recognition of the analysed compounds was achieved by means of correlation of retention time and absorbance ratios. The method was directly applied to the analysis of illicit heroin and cocaine samples and to the analysis of pharmaceutical preparations containing codeine.

Alkaloids↗
PubMed1996

Applicability of various brands of mixed-phase extraction columns for opiate extraction from blood and serum.

Four commercially available types of mixed-phase solid-phase extraction (SPE) columns (Bond Elut Certify, Isolute Confirm HCX, Chromabond Drug and Bakerbond Narc-2) were examined in order to compare the extraction efficiencies and chromatographic purity of extracts. The absolute recovery of morphine, 6-monoacetylmorphine and codeine was examined in blood and serum (ten samples each at two concentration levels), using SPE columns of the same batch. GC-MS (ion trap) and HPLC with amperometric detection were used for quantitation. A distinct variability in extraction recovery was observed among the same batches of all brands of SPE columns. All extracts were chromatographically pure and no interfering peaks were observed, neither in GC-MS nor in HPLC examinations, but in some extracts large peaks of plasticizers were identified. The measurements of flow velocities of the same samples of blood or serum through the SPE columns of the same batch showed very large variability of random character. The morphometric analysis of particles was performed for two batches of each sort of SPE columns by means of an image analysing system. Symmetrical distribution of particle size was observed only in Chromabond MN Drug packing, while in other cartridges large fractions of fine particles and nonhomogenous distribution were found. Only in one case the morphometric findings were pretty concordant with the data available from the manufacturer; in two cases, observed data varied considerably from that expected, and in one case no information was available at all. The study showed generally that there was room for improvement in the quality of mixed-phase SPE columns.

Analgesics, Opioid↗
PubMedDate not supplied

Opiate levels in hair.

By means of radioimmunoassay-technique, hair samples of users, drug related fatalities, carcinoma patients receiving morphine and of experimental guinea pigs receiving codeine were investigated for opiates. The RIA-investigations require a minimum of material; our routine procedures need only 50 mg of hair. No correlation existed between administered doses of opiates and their concentrations in hair of both human and experimental animals. By sectioning the hair, the approximate period of drug use in man could be detected. However, these findings could not be confirmed by the animal experiments. The growth rate of the hair, diffusion and adhesion processes may influence the transport of drugs along the hair. External contaminations and washing procedures were shown to increase or diminish the drug concentration of the samples.

Animals↗
PubMedDate not supplied

Pholcodine interference in the immunoassay for opiates in urine.

The excretion in urine after single oral therapeutic doses of morphine derivatives was analysed with radioimmunoassay (RIA) and homogeneous enzyme immunoassay (EMIT) for opiates. In contrast to the rapid excretion of ethylmorphine and codeine, pholcodine showed positive results for opiates 2-6 weeks after intake when the urines were analysed with the RIA-method. When analysed with the EMIT-method, positive results were obtained for pholcodine for approximately 10 days. As pholcodine is a common component in cough mixtures, its prolonged excretion could represent a hazard in interpreting the results from drug analyses of urines.

Antitussive Agents↗
PubMed1993

Hair analysis as evidence in forensic cases.

Because hair analysis can be used for the determination of drug use months after drug consumption, hair analysis data can often act as important and even decisive evidence in the courtroom. More recently developed GC/MS methods offer excellent sensitivity and can make the distinction between chronic heroin and codeine use, which was not possible earlier with radioimmunoassay techniques. From more than a thousand hair analyses, the morphine/codeine ratios necessary to determine heroin use were set at 5:1 for low morphine concentrations (< 1 ng/mg hair) and 2:1 for concentrations above 1 ng/mg hair. The distinction can be further focused with the additional analysis of the metabolite monoacetylmorphine (MAM). As can be seen from several case examples, hair analysis cannot pinpoint an exact date of opiate use, but it can be used to validate or invalidate a subject's statement concerning his/her drug consumption. Interpretations should always be made cautiously. Ranges, means and medians are also listed for amphetamine, cocaine and cannabis and work is under way to draw similar safety guidelines for these drugs.

Codeine↗
PubMed1993

Rapid and highly selective GC/MS/MS detection of heroin and its metabolites in hair.

A direct treatment of methanol-washed hair with a silylating solution is proposed to extract heroin, O-6-monoacetylmorphine, morphine, acetylcodeine, and codeine, obtaining the simultaneous derivatization of the hydroxylated metabolites and reducing potential sample contamination. Analysis is performed by capillary gas chromatography-tandem mass spectrometry (GC/MS/MS) using multiple selected reaction monitoring. Owing to the selectivity and sensitivity of the GC/MS/MS analysis, and to the extremely simple treatment of the sample, the method fulfils the requirements of both clinical and forensic diagnosis of heroin use.

Codeine↗
PubMed1995

Hair and urine analysis: relative distribution of drugs and their metabolites.

This work studies the distribution of cocaine and heroin metabolites in hair and urine of living polidrug abusers. Cocaine, benzoylecgonine (BEG), ecgonine methyl ester (EME), morphine, codeine and 6-monoacetylmorphine (6-MAM) were simultaneously extracted and analyzed by GC/MS in SIM mode. The results obtained show a different distribution of heroin and cocaine metabolites in urine and hair. In urine, we generally find BEG and EME for cocaine abuse, and morphine for heroin abuse. In hair, we detect cocaine and MAM as major metabolites for cocaine and heroin abuse, respectively.

Cocaine↗
PubMed1989

Determination of opiates and other basic drugs by high-performance liquid chromatography with electrochemical detection.

A procedure is described for the extraction and determination of morphine (M), hydromorphone (HM), codeine (C) and metoclopramide (MCP) present in human plasma. The drugs are separated by reversed-phase liquid chromatography and detected amperometrically at a glassy carbon electrode. The method provides high sensitivity and selectivity and has been used successfully in bioavailability studies.

Biological Availability↗
PubMed1993

Effectiveness of levodropropizine against cigarette smoke-induced airway hyperreactivity: possible mechanism.

We verified the possible effect of the new antitussive drug levodropropizine on airway hyperreactivity and lung inflammation induced by cigarette smoke exposure in anaesthetized guinea-pigs. Levodropropizine, administered by aerosol at 25 mg/ml for 30 s completely prevented smoke induced airway hyperreactivity. The protective effect was early in onset (3 min) and lasted up to 30 min. The same dose of codeine, administered in the form of an aerosol, decreased the increase in airway responsiveness induced by smoke inhalation slightly but not significantly. In parallel with the functional results, levodropropizine also inhibited the recruitment of inflammatory cells triggered by smoke exposure within the airway lumen. When levodropropizine was administered i.v. to anaesthetized guinea-pigs, it reduced the bronchocontractile effect of capsaicin dose-dependently, whereas it was without effect against substance P-induced bronchoconstriction. These data demonstrate the ability of levodropropizine to counteract the hyperreactive phenomenon and the associated inflammatory event induced by cigarette smoke exposure, an effect which might depend on its capacity to modulate the activation of the peptidergic system.

Airway Resistance↗
PubMed2004

Amperometric detection of morphine at a Prussian blue-modified indium tin oxide electrode.

In this work, the electrocatalytic oxidation of morphine (MO) at an optically transparent indium tin oxide (ITO) electrode modified by an electrodeposited Prussian blue (PB) thin film is first demonstrated, and the amperometric detection of MO was then investigated. Experimental results showed that the thin film on the ITO surface, confined to the PB/Berlin green (BG) redox pair, can serve as an excellent mediator which facilitates electron transfer and considerably lowers the overpotential required, as compared to a bare ITO electrode. Thus, PB can be regarded as a promising artificial peroxidase for MO. The rate of such an electrocatalytic reaction is pH dependent with the highest value at pH 5. By potential-step excitation from 0.55 to 0.70 V, a linear calibration curve, displaying the relationship between steady-state currents and MO concentrations (ranging from 0.09 to 1.0 mM), was obtained. The detection sensitivity is about 16.8 microA/cm2 mM. Most importantly, the method described herein can readily discriminate MO analogs lacking the phenolic -OH group, such as codeine, and can thus benefit the specific recognition of MO.

Biosensing Techniques↗
PubMed2005

Derivatives of tramadol for increased duration of effect.

Tramadol is a centrally acting opioid analgesic structurally related to codeine and morphine. Analogs of tramadol with deuterium-for-hydrogen replacement at metabolically active sites were prepared and evaluated in vitro and in vivo.

Analgesics, Opioid↗
PubMed2004

Phrenic and iliohypogastric nerve discharges during tussigenic stimulation in paralyzed and decerebrate guinea pigs and rats.

Although effects of antitussive drugs have been examined in inbred small animals using a whole body plethysmography, neuronal mechanisms underlying the cough reflex are not fully understood. The present study analyzed the reflex discharge patterns of the phrenic (PN) and iliohypogastric nerves (IHN) evoked in decerebrate and paralyzed guinea pigs and rats. In guinea pigs, electrical stimulation of the superior laryngeal nerve, chemical stimulation with capsaicin and mechanical stimulation to the intratracheal mucosa equally produced a serial PN-IHN response. This response was characterized by an increased PN discharge and following spindle-shaped burst of the IHN. The evoked discharges overlapped for 20 ms. In rats, by contrast, mechanical stimulation was without effect while capsaicin and electrical stimulation produced two types of responses, both of which differed from that observed in guinea pigs. The first type consisted of an augmented burst of the IHN that was immediately followed by an increased PN discharge. The second type was a large spindle-shaped burst of the IHN that occurred 80 ms after the end of the preceding PN discharge. Codeine (3 mg/kg i.v.) depressed all types of responses evoked in guinea pigs and rats. The present study demonstrated that the fictive cough comparable with those induced in other experimental animals was produced consistently in guinea pigs, but not in rats. Therefore, guinea pigs are suitable for investigation of the neuronal mechanisms underlying the cough reflex and assessment of antitussive drugs.

Abdominal Muscles↗