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At least 55 records · Page 3Linked to original sources
PubMed1999

Method for quantification of morphine and its 3- and 6- glucuronides, codeine, codeine glucuronide and 6-monoacetylmorphine in human blood by liquid chromatography-electrospray mass spectrometry for routine analysis in forensic toxicology.

Simultaneous determination of opiates and their glucuronides in body fluids has a great practical interest in the forensic assessment of heroin intoxication. A selective and sensitive method for quantification of morphine and its 3- and 6-glucuronides, codeine, codeine glucuronide and 6-monoacetylmorphine (6-MAM) based on liquid chromatography-electrospray ionisation mass spectrometry is described. The drugs were analysed in human autopsy whole blood after solid-phase extraction on a C8 cartridge. The separation was performed on an ODS column in acetonitrile (analysis time 15 min). For the quantitative analysis, deuterated analogues of each compound were used as internal standards. Selected-ion monitoring was applied where the molecular ion was chosen for quantification. The limits of quantification were 0.5 ng/ml for morphine and 6-MAM and 1 ng/ml for the 6-glucuronide of morphine, codeine-6-glucuronide and codeine and 5 ng/ml for the 3-glucuronide of morphine.

Calibration↗
PubMedDate not supplied

High-performance liquid chromatographic study of codeine, norcodeine, and morphine as indicators of codeine ingestion.

A simple quantitative method for determining codeine, norcodeine, and morphine in urine by high-performance liquid chromatography (HPLC) is described. Urine samples are hydrolyzed and extracted through differential pH extraction. The subsequent use of HPLC allowed separation and quantitation on a reverse phase system with ultraviolet detection. A comparison study of the concentrations of single and therapeutic doses of codeine in urine over a period of time showed that morphine, the major metabolite, increases in proportion to codeine, eventually surpasses the codeine level, and remains higher for the duration of time that the drugs are detectable.

Chromatography, High Pressure Liquid↗
PubMed1985

The relative bioavailability of paracetamol and codeine after oral administration of a combination of buclizine, paracetamol and codeine, with or without docusate, and of paracetamol alone in healthy volunteers.

A randomized, double-blind, crossover study was carried out in 10 healthy volunteers to investigate whether the inclusion of the wetting agent docusate sodium (10 mg) in a combined oral formulation ('Migraleve') with buclizine hydrochloride (6.25 mg), codeine phosphate (8 mg) and paracetamol (500 mg) had any effect on the bioavailability of the analgesics. On 3 occasions at weekly intervals, the subjects were given 2 tablets of the standard formulation, the combination without docusate or 500 mg paracetamol alone. Blood samples were taken before and at fixed times during the 4 hours after administration of each preparation for estimation of plasma concentrations of paracetamol, by gas-liquid chromatography, and of codeine, by radioimmunoassay. The results showed that there were no significant differences between the mean paracetamol concentrations achieved after administration of each of the 3 preparations at any of the time points. Peak paracetamol plasma concentrations were 11.25 +/- 1.74 micrograms/ml at 0.5 hours, 9.6 +/- 1.04 micrograms/ml at 0.75 hours, and 9.53 +/- 1.66 micrograms/ml at 0.5 hours, respectively, after the standard formulation, the combination without docusate, and paracetamol alone. Mean elimination half-lives for paracetamol were 2.83 +/- 0.51, 1.92 +/- 0.20 and 2.49 +/- 0.46 hours, respectively, and the differences were not significant. The difference between mean plasma concentrations of codeine after the two preparations including this analgesic bordered on significance at 3 hours and was significant at 4 hours, but the areas under the curve were not significantly different. Peak codeine plasma concentrations after the standard formulation were 42.1 +/- 9.4 ng/ml at 0.75 hours compared with 36.9 +/- 3.4 ng/ml at 1.5 hours after the combination without docusate.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetaminophen↗
PubMed1990

Species differences in metabolism of codeine: urinary excretion of codeine glucuronide, morphine-3-glucuronide and morphine-6-glucuronide in mice, rats, guinea pigs and rabbits.

1. Metabolites of codeine were determined by use of h.p.l.c. in urine of male mice, rats, guinea pigs and rabbits injected with 10 mg codeine/kg subcutaneously. 2. In 24 h urines of these species, unchanged codeine, codeine glucuronide, free morphine, and morphine-3-glucuronide were as follows: mice, 6.8, 1.6, 0.8 and 7.6% dose; rats, 1.6, 0.2, 4.3 and 23.9% dose; guinea pigs, 1.6, 39.8, 0.2 and 1.6% dose; rabbits, 2.2, 24.5, 1.3 and 17.9% dose. Urinary excretion of morphine-6-glucuronide was 0.7% dose in guinea pigs, 1.9% in rabbits, and not detectable in mice and rats. Norcodeine was found only in the urine of mice. 3. These results indicate that codeine is metabolized in all four species by glucuronidation and by oxidative N- and O-demethylation, but the quantitative excretions of metabolites were quite different in different species.

Animals↗
PubMed1985

A double-blind comparison of a new ibuprofen-codeine phosphate combination, codeine phosphate, and placebo in the relief of postepisiotomy pain.

In a double-blind single-dose study, the analgesic effect of a new ibuprofen-codeine phosphate combination was compared with those of codeine phosphate alone and placebo for the relief of moderate and severe postepisiotomy pain. In the 113 patients studied, combination therapy was superior to codeine phosphate alone and to placebo, the difference between the combination and codeine phosphate alone reaching statistical significance (P less than 0.05) after two hours. The few side effects reported were not of a serious nature.

Clinical Trials as Topic↗
PubMed1968

Codeine and its alternates for pain and cough relief. I. Codeine, exclusive of its antitussive action.

This report-the first of a series on codeine and its alternates for pain and cough relief-presents a detailed evaluation of experimental and clinical data concerning the analgesic action of codeine (the antitussive action will be assessed separately). The authors discuss the pharmacology of the drug, including side-effects and toxicity; effects on the respiratory, circulatory, digestive and urinary systems; tolerance, dependence and liability to abuse; metabolic effects; and mechanism of action.Though codeine is generally more toxic than morphine to animals on account of its convulsant action, it is less toxic to man, possibly because it produces less respiratory depression. Again, tolerance to its analgesic effects has been demonstrated in several animal species, but dependence in man is observed far less frequently than it is with morphine, and the abstinence syndrome is less intense. From their extensive review of the evidence available, the authors conclude that codeine is a good analgesic and that little risk to public health is likely to arise from its clinical use to relieve pain.

Analgesics↗
PubMed1979

Urinary excretion levels of morphine and codeine in subjects consuming medicinal preparations containing morphine or codeine and in drug abusers.

Urinary levels of morphine and codeine were studied in two groups of people: Group A--urine samples of 76 subjects receiving three different medicinal preparations containing morphine or codeine. Group B--urine samples of 67 drug abusers detected at urinary mass screening. Distinct differences in these levels were observed. In Group A, UPPER 99% Confidence limits of morphine concentrations of 2.56 microgram/ml, 2.40 microgram/ml and 2.29 microgram/ml were reached after consumption of prescribed doses of Syrup Phensedyl, Tablet Codeine Co and Kaolin et Morphine mixture respectively. In Group B, the LOWER 99% Confidence limit of morphine concentration was 3 microgram/ml. In contrast, the codeine levels obtained for both groups were similar. The clear separation of the ranges of morphine values for the two groups shows that the urinary morphine level forms a reliable index for the differentiation between these two groups.

Adolescent↗
PubMedDate not supplied

Analysis of the analgesic efficacy of acetaminophen 1000 mg, codeine phosphate 60 mg, and the combination of acetaminophen 1000 mg and codeine phosphate 60 mg in the relief of postoperative pain.

Patients who experienced pain after surgery were administered a single dose of 1 of 3 treatments: acetaminophen 1000 mg, codeine phosphate 60 mg, or a combination of these. Patients rated their pain intensity on ordinal and visual analog scales just prior to medication and at intervals thereafter for up to 5 hours. They also rated pain relief, pain half gone, and any adverse effects. Sum of pain intensity difference and total pain relief scores were analyzed using Dunnett's procedure. The drug combination was statistically superior to codeine as measured by SPID, TOTPAR, pain half gone, and time to remedication. The combination achieved better mean scores than acetaminophen on all efficacy measures, but was (marginally) statistically superior only in pain half gone. No appreciable differences in adverse effects were noted among the treatments. The difficulty of showing the analgesic efficacy of codeine in a single dose trial is discussed.

Acetaminophen↗
PubMedDate not supplied

Analgesic effect of an aspirin-codeine-butalbital-caffeine combination and an acetaminophen-codeine combination in postoperative oral surgery pain.

The efficacy of an aspirin-caffeine-codeine-butalbital combination was compared to an acetaminophen-codeine combination and placebo in outpatients who had moderate or severe pain after the surgical removal of impacted third molars. Using a self-rating record, patients rated their pain, relief, anxiety and relaxation hourly for up to 6 hours after medicating. Each active medication was significantly superior to placebo for measures of analgesia and relaxation. Although the butalbital-containing combination provided consistently greater analgesia, the differences between active medications were not statistically significant. The acetaminophen-codeine combination significantly reduced anxiety; however, the butalbital containing combination did not. The results of this study suggest that female patients may have greater efficacy than male patients. All adverse effects were transitory and consistent with the known pharmacologic profiles of the study medications or the backup analgesic.

Acetaminophen↗
PubMed1980

High-performance liquid chromatographic assay of codeine in acetaminophen with codeine dosage forms.

An accurate, rapid, and specific high-performance liquid chromatographic (HPLC) assay was developed for codeine in acetaminophen with codeine combination products. The internal standard (chlorpheniramine maleate), codeine, acetaminophen, and several other test compounds or impurities were well separated. A complete analysis took < 10 min. The relative standard deviations of the retention time, precision, and accuracy were 0.5, 0.4, and 0.5%, respectively. An excellent linear correlation was obtained between the HPLC and GLC methods.

Acetaminophen↗
PubMed1986

Enhanced stability of codeine sulfate: effect of pH, buffer, and temperature on the degradation of codeine in aqueous solution.

In the absence of strong buffer catalysts, the degradation of codeine sulfate (7,8-didehydro-4,5 alpha-epoxy-3-methoxy-17-methylmorphinan-6 alpha-ol sulfate) in aqueous solution is described by the expression kobs = kH+ [H+] + k0 + kHO-[HO-], where kH+ = (3.9 +/- 1.3) X 10(-8) M-1 X S-1, k0 = (2.7 +/- 0.5) X 10(-8) S-1, and kHO- = (5.1 +/- 1.0) X 10(-6) M-1 X S-1 at 80 degrees C. The activation energies associated with these rate constants are 27.7, 21.0, and 28.3 kcal X mol-1, respectively. In the absence of buffer catalysis, codeine sulfate is predicted to have a room temperature shelf life of approximately 44 years between pH 1 and 10, significantly longer than the 1.1 year shelf life of codeine phosphate reported earlier.

Buffers↗
PubMed2000

Urinary excretion of codeine and morphine following the administration of codeine-containing cold syrup.

The concentrations of codeine ([C]) and morphine ([M]) excreted in urine obtained from nine subjects at various time intervals after the ingestion of 10-40 mg of both simple and compound codeine doses three times per day for three days were determined by gas chromatography-mass spectrometry analysis. Four distinct [C]/[M] distribution patterns (phases) were observed: a, [C] > [M] from ingestion of first dose to 78-108 h after ingestion of the first dose (18-48 h after the ingestion of the last dose); b, [C] approximately [M] 78-90 h after ingestion of the first dose (18-30 h after ingestion of the last dose); c, [C] < [M] 78-102 h after ingestion of first dose (18-42 h after ingestion of the last dose); and d, [C] <0.05 microg/mL and [M] > 0.05 microg/mL 84-96 h after ingestion of the first dose (24-36 h after ingestion of the last dose with [M] ranging from 0.10 to 0.30 microg/mL) toward the terminal phase. No single individual exhibited all four [C]/[M] distribution characteristics during the entire excretion period and intervals monitored in this study. These data are of reference value for differentiating codeine and morphine/heroin ingestion.

Analgesics, Opioid↗
PubMedDate not supplied

The human urinary excretion pattern of morphine and codeine following the consumption of morphine, opium, codeine and heroin.

The urinary excretion patterns of morphine and codeine in a number of individuals following consumption of morphine-based narcotic drugs have been studied. From the data collected the relative amounts of codeine and morphine in urine specimens were compared and certain trends, consistencies and irregularities were revealed. To a certain extent, the ratio of the proportion of codeine to morphine excretion in urine may be used to determine the nature of the drugs consumed. This correlation is useful in the interpretation of the results of urine analysis which is the basis of effective control and rehabilitation of drug addiction.

Codeine↗
PubMed1978

[The behaviour of codeine and codeine-6-glucuronide in hydrolysis with hydrochloric acid (author's transl)].

The behaviour of codeine and codeine-6-glucuronide with hydrochloric acid has been investigated. Three methods of hydrolysis were selected; they are often used in routine identification of drugs in urine. With method I (12--13% HCl; 30 min at 100 degrees C) about 53% of codeine-6-glucuronide were not hydrolized. The corresponding values: with method II (20% HCl; 6 min heated azeotrope in open vessel) about 8% and with method III (nearly 5% HCl; 30 min at 100 degrees C) about 83%.

Chemical Phenomena↗
PubMed1983

[Analysis and the stability of codeine phosphate. 2: Stability of aqueous codeine phosphate solutions].

The degradation velocity of aqueous codeine phosphate solutions is of first order. The formation of the degradation products (isomerization products) depends upon temperature, light and pH value. At pH = 3.5, codeine phosphate solutions are relatively stable. Atmospheric oxygen exerts no effect. Of the complexing agents and antioxidants tested, only citric acid and thiourea seem to be capable of reducing the rate of degradation. Besides glass ampoules, plastic containers of low-density polyethylene proved to be suited for codeine phosphate solutions.

Antioxidants↗
PubMed1992

A multiple dose comparison of combinations of ibuprofen and codeine and paracetamol, codeine and caffeine after third molar surgery.

In a randomised, double-blind, double-dummy, multiple dose, crossover study in 30 patients we compared an ibuprofen/codeine combination (400 mg ibuprofen/25.6 mg codeine phosphate) with a paracetamol/codeine/caffeine combination (1 g paracetamol/16 mg codeine phosphate/60 mg caffeine) for pain relief over 6 days after two-stage bilateral lower third molar removal. The ibuprofen combination produced significantly greater analgesia than the paracetamol combination, both on single-dose analysis of the first and second days and on multiple-dose measures for days 1, 2, 3 and 4. The mean incidence of adverse effects over the 6 days was 20% for both combinations. This trial design (crossover with multiple dosing in outpatients) is a sensitive way of testing for analgesia, and is potentially more predictive of adverse effect problems than single-dose studies. It confirms that multiple dosing may show increased efficacy.

Acetaminophen↗
PubMed1975

Acute codeine overdose: correspondence between clinical course and codeine metabolism.

A patient presented with clinical features of drug overdose. Although heroin was suspected, codeine was identified by drug analysis. The clinical course was complicated by shock, respiratory arrest and laboratory evidence of acute hepatic insufficiency. An inital slow rate of codeine metaboism, possibly related to the hepatic damage, corresponded to prolonged respiratory depression.

Adult↗
PubMed1969

Codeine and its alternates for pain and cough relief. 3. The antitussive action of codeine--mechanism, methodology and evaluation.

This report-the third of a series on codeine and its alternates for pain and cough relief-presents a detailed review of the physiology and pathophysiology of cough, the methods for the experimental and clinical measurement of the antitussive action of drugs, possible mechanisms of action of antitussive agents, and includes a compilation of experimental results and clinical experience with codeine as an antitussive.

Animals↗