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At least 199 records · Page 11Linked to original sources
PubMed1992

Increased urinary morphine, codeine and tetrahydropapaveroline in parkinsonian patient undergoing L-3,4-dihydroxyphenylalanine therapy: a possible biosynthetic pathway of morphine from L-3,4-dihydroxyphenylalanine in humans.

We have identified morphine and codeine in human urine by means of gas chromatography/mass spectrometry. Gas chromatography/mass spectrometry was also used to quantitate the two alkaloids and tetrahydropapaveroline (THP) in urine of both normal subjects and parkinsonian subjects receiving L-dopa therapy. The morphine, codeine and THP levels in healthy nondrinker controls were 2.93 +/- 0.23, 2.01 +/- 0.53 and 6.70 +/- 1.13 pmol/ml (mean +/- S.E.M.), respectively. In contrast, the urinary levels of codeine and THP in L-dopa-treated parkinsonian patients were significantly elevated to 62.20 +/- 17.54 and 31.04 +/- 15.69 pmol/ml, respectively. Some of the parkinsonian patients showed high urinary morphine levels. Morphine excretion was also enhanced in patients complaining of severe pain due to herpes zoster (24.60 +/- 9.51 pmol/ml) but not in patients with severe pain due to cerebral embolus. These alkaloid levels in the urine of abstinent alcoholics were very low. There were significant correlations among these three alkaloid levels in the urine. The results indicate that morphine and codeine are synthesized in the body from L-dopa and/or dopamine, via the THP-related pathway.

Adult↗
PubMed1991

[Pilot study of the metabolism of codeine to morphine and a possible modification by benzodiazepines].

After administration of high-dose codeine we found that in two cases 20-40% of the total morphine-equivalents in the 24-hour urine sample were free morphine. After another 24 hours the proportion of free morphine was up to 70% and after roughly 96 hours even went up to 96%. Although 10% of the administered codeine was eliminated as morphine. In contrast to the values reported in literature we found that even with codeine/morphine ratios greater than 0.5 and morphine concentrations of up to 2000 ng/ml urine one cannot naturally conclude that morphine/diamorphine has been consumed. The short half-life of codeine in serum was 2-4 hours, the final half-life was 9-11 hours. In urine we found a short half-life of 1-6 hours as well as a long half-life of 7-12 hours. When diazepam was administered simultaneously with codeine the expected half-life in serum was up to 1.5 times and in urine 2.5 times. The codeine/morphine ratios were hardly affected so far as evidence goes which they give of preceding drug-intake.

Biotransformation↗
PubMedDate not supplied

Effects of ephedrine and phenylpropanolamine on the antinociceptive effects of morphine and codeine in mice.

The effects of ephedrine and phenylpropanolamine on the antinociceptive activities of morphine and codeine were investigated. Both morphine and codeine exhibited dose-dependent antinociceptive activities in the tail flick test. Ephedrine (5, 10 and 20 mg/kg) and phenylpropanolamine (5, 10 and 20 mg/kg) showed no antinociceptive effect when administered alone. The antinociceptive effects of morphine were enhanced in mice pretreated with ephedrine or phenylpropanolamine. similarly, codeine antinociception was increased in mice pretreated with ephedrine or phenylpropanolamine. In all cases, the ED50 values and single dose comparisons were shifted in the same direction. These effects on the antinociceptive potencies of morphine and codeine were found to be dose-dependent, being statistically significant at the higher dose levels of ephedrine and phenylpropanolamine used in the present study.

Analgesics↗
PubMed1989

[Antitussive effects of Bakumondô-tô and codeine in bronchitic guinea-pigs].

Antitussive effects of Bakumondô-tô and codeine were examined in bronchitic guinea-pigs made by an exposure to SO2. Bakumondô-tô significantly depressed the cough reflex induced by mechanical and chemical stimulations in the bronchitic but not in the normal animals. Repeated administration of Bakumondô-tô significantly suppressed the increased spontaneous discharge of the superior laryngeal nerve in bronchitic animals. On the other hand, the antitussive action of codeine in bronchitic animals was significantly weaker than that in normal animals. Moreover, repeated administrations of codeine significantly potentiated the increased spontaneous discharge of the superior laryngeal nerve. The results suggest that Bakumondô-tô, unlike codeine, has a notable antitussive activity in bronchitic rather than in normal guinea-pigs.

Animals↗
PubMed1988

Antitussive action of the new anilide derivative vadocaine hydrochloride compared with codeine phosphate in four animal models.

Vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl) propionanilide hydrochloride, OR K-242-HCl; INN: vadocaine) is a novel antitussive compound structurally resembling local anaesthetics. Its antitussive profile was studied in several animal models. In guinea-pigs, vadocaine reduced by about 70% the cough episodes induced by sulphur dioxide or ammonia. The effective dose was 2.5 mg/kg p.o., and codeine phosphate was less effective. In cats, vadocaine (3 mg/kg i.v.) inhibited by about 80% for 10 min the cough reflex initiated by mechanical irritation of the trachea. When vadocaine was given via the vertebral artery, it was about 10 times more active than by the intravenous route. Codeine was 3 times as active as vadocaine by both routes. This result indicates an important central component in the antitussive action of vadocaine. In another cat model, 5 mg/kg of vadocaine was somewhat weaker than 1 mg/kg of codeine in inhibiting the cough caused by electrical stimulation of the laryngeal nerve (Domenjoz' method). In dogs, both oral and intravenous doses of 6 mg/kg of vadocaine and 2 mg/kg of codeine were approximately equiactive, inhibiting by 60-80% the cough induced by electrical stimulation of the trachea. Concentrations of vadocaine in serum were around 1 microgram/ml during oral administration. By both routes, the antitussive activity (inhibition of cough by 50% or more) lasted at least 2 h. Vadocaine caused local anaesthesia in the guinea-pig wheal preparation at concentrations of 0.25% and 0.5%, and on the guinea-pig cornea at 0.5%. Duration of anaesthesia was longer than that of lidocaine. Vadocaine did not affect the guinea-pig tracheal strip preparation.(ABSTRACT TRUNCATED AT 250 WORDS)

Anesthetics, Local↗
PubMed1987

Codeine-induced mast cell degranulation in human skin: effect of calcium channel blockers.

Codeine and other opiates can induce immediate type wheal and flare skin reactions. Calcium channel blockers including nifedipine have been shown to inhibit mast cell degranulation in different systems. The oral administration of nifedipine (10 mg) did not affect the size of codeine-induced skin reactions in ten normal volunteers. Mean wheal over flare sizes were 11.7 mm/29.2 mm before nifedipine and 11.5 mm/31.0 mm at peak nifedipine blood levels. Similar observations were made when codeine was injected locally with or without 20 micrograms nifedipine (12.1/29.2 mm and 13.2/29.2 mm, respectively). These data suggest that codeine-induced mast cell degranulation may be mediated by a calcium-independent mechanism. Alternatively, mast cells in the human skin may differ in their reactions to secretagogues when compared with basophils and mast cells from other human tissues or other species.

Adult↗
PubMed1986

[Relative bioavailability of paracetamol from tablets and suppositories as well as of paracetamol and codeine in a combination tablet].

Eight healthy male volunteers took part in this study to determine the relative bioavailability of Treuphadol oblong tablets (500 mg paracetamol), Treuphadol Plus oblong tablets (500 mg paracetamol, 30 mg codeine phosphate) and Treuphadol suppositories (750 mg paracetamol) against commercial tablets (500 mg paracetamol). Plasma levels of paracetamol and codeine, plus saliva levels of paracetamol for the two paracetamol only formulations, were determined by HPLC and the pharmacokinetic parameters established. The AUC data for paracetamol showed that all four preparations were bioequivalent. The saliva levels of paracetamol demonstrated a good correlation to the corresponding plasma levels. The pharmacokinetic data of codeine from the Treuphadol Plus tablet were compared with corresponding data from the literature. The bioequivalence of codeine when based on this comparison can also be assured.

Acetaminophen↗
PubMed1987

Concentrations of morphine and codeine in serum and urine after ingestion of poppy seeds.

We measured morphine and codeine in commercially available poppy seeds and in serum and urine samples from healthy adults who had ingested these poppy seeds. Four brands of black poppy seeds, examined by gas chromatography-mass spectroscopy (GC-MS) with deuterated internal standards, contained from 17 to 294 micrograms of morphine and 3 to 14 micrograms of codeine per gram of seeds. Morphine was detected by GC-MS in hydrolysates of serum as late as 24 h after ingestion, with a maximum mean concentration of 100 ng/mL (range 82-131) measured 2 h after the subjects ingested 25 g of seeds. Opiates were detectable (greater than 300 micrograms/L) in urine by enzyme-multiplied immunoassay (EMIT; Syva Co.) and by radioimmunoassay screening procedures for as long as 48 h after ingestion. The identity and quantities of morphine and codeine in poppy seed extracts and in hydrolysates of serum and urine were confirmed by GC-MS. Therefore a positive finding of morphine or codeine in blood and urine may sometimes be due to ingestion of poppy seeds.

Codeine↗
PubMed1977

Potentiation of antitussive effect of codeine by some 1-dimethoxyphenyl-3-alkylaminobutanols in guinea pigs.

Newly synthesized 1-(2',5'-dimethoxyphenyl)-1-n-butyl-3-diethylaminobutanol (compd. 4) and its analogs enhanced the antitussive effect of codeine and morphine as tested on the cough induced by mechanical stimulation of the trachea in guinea pigs. This effect was illustrated to be a potentiation on the Gaddum's diagram. The following parameters were affected little or to a small extent: 1. analgesic effect of codeine and morphine in guinea pigs and mice, 2. duration of anesthesia induced by hexobarbital in mice, 3. respiratory depression caused by codeine in guinea pigs, and 4. LD50 of codeine in guinea pigs and mice. Explorations of the mechanism of potentiating action suggested some peripheral mechanism, but the exact one remained to be elucidated.

Amino Alcohols↗
PubMed1983

Deaths related to propoxyphene or codeine or both.

Ninety-nine deaths involving propoxyphene or codeine or both were investigated through interviews with surviving relatives and associates. The criterion for admission to this study was the presence of propoxyphene or codeine in the body fluids or tissues, determined analytically. The codeine-related group included more ethnic minority persons, more histories of primary drug addiction, more users of street drugs, and more accidental deaths. In the propoxyphene-related group there were fewer histories of drug addiction and more persons with mental illness and more suicides. Most victims had considerable past experience with one or both of the drugs and other drugs as well. Propoxyphene was usually obtained by physician prescription. Codeine was often obtained illegally.

Adult↗
PubMed1980

Double-blind cross-over study comparing loperamide, codeine and diphenoxylate in the treatment of chronic diarrhea.

As no adequate comparison of these widely used drugs has been made, we have performed a double-blind cross-over trial in 30 individuals with chronic diarrhea. Each underwent three randomized treatment periods of 4 wk duration. Patients were instructed to increase the daily dose gradually until control was achieved or side effects became intolerable. Stool frequency, consistency, urgency, and incontinence were then compared when a stable dose was reached. Though 2.3 capsules (4.6 mg) of loperamide, 2.3 capsules (103.5 mg) of codeine and 2.5 capsulses (12.5 mg) of diphenoxylate all reduced stool frequency to the same extent, diphenoxylate was significantly less effective in producing a solid stool. Before treatment 95% of patients experienced urgency, sometimes associated with fecal incontinence, often as their major diability. Loperamide and codeine were more effective in relieving this than was diphenoxylate. Side effects, particularly central nervous effects, were greatest with diphenoxylate and least with loperamide. Approximately equal numbers discontinued each preparation; poor control and central-nervous-system side effects were the usual reasons for stopping diphenoxylate and codeine, and abdominal pain and constipation for stopping loperamide. We conclude that both loperamide and codeine phosphate are superior to diphenoxylate in the symptomatic treatment of chronic diarrhea.

Antidiarrheals↗
PubMed1976

A comparative study of the analgesic and respiratory effects of N-allylnorcodeine (nalodeine), nalorphine, codeine and morphine.

In this comparative study, the abdominal constriction test was used to determine analgesia in mice, and the body plethysmograph was used to study respiratory effects of nalodeine, nalorphine, naloxone, codeine, morphine and various agonist-antagonist combinations in rats. The analgesia dose-response curves for the surrogate pairs, nalodeine-nalorphine and codeine-morphine, were parallel but had significantly different slopes. Naloxone was a more potent antagonist of morphine and codeine than of nalorphine and nalodeine. In antagonizing morphine and codeine analgesia, naloxone was the most potent antagonist, nalorphine had a biphasic effect with decreasing activity at higher doses and nalodeine was not an antagonist. Moderate doses of nalorphrine depressed minute volume largely by their effect on tidal volume, but high doses stimulated respiratory rate and therefore had less effect on minute volume. Nalodeine depressed minute volume by depressing tidal volume, since all doses initially stimulated and then variably affected respiratory rate. Metabolic rate was not increased by either drug short of convulsant doses. Nalodeine depresses the ventilatory response to CO2 and weakly antagonizes the respiratory depressant actions of morphine.

Analgesics↗
PubMed1984

Analgesic efficacy after single and repeated doses of codeine and acetaminophen.

A double-blind randomized analgesic trial was carried out in patients suffering from pain after removal of a third molar tooth. In a two-dose regimen, 108 patients received either 60 mg codeine, 500 mg acetaminophen, or 1000 mg acetaminophen. On the day of surgery, the patients assessed their pain intensity hourly on a visual analog scale. The evaluation was carried out during the 10-hour period after first medication. The best pain reducing effects were achieved with 1000 mg acetaminophen. Both the category and position of each tooth were examined in relation to pain intensity; however, the statistical analysis did not reveal any significant correlation. In all treatment groups, the efficacy of the second dose was superior to that of the first, and the most pronounced difference was obtained in patients taking codeine, who increased their pain reduction from 20 to 60 per cent. Clinical comparisons including codeine may therefore be better carried out in a repeated-dose regimen.

Acetaminophen↗
PubMedDate not supplied

Double-blind parallel comparison of single oral doses of ketoprofen, codeine, and placebo in patients with moderate to severe dental pain.

Ketoprofen, 25, 50, and 100 mg, was compared with 90 mg codeine and placebo for relief of pain due to removal of impacted third molar teeth. Treatment was self-administered as a single oral dose under double-blind conditions in five parallel groups established by a random code in healthy young adults. Based on 129 patient evaluations of pain experience and pain relief, ketoprofen was shown to have a more rapid onset and longer duration of action than codeine. In the derived variables of SPID (Sum of Pain Intensity Differences) and TOPAR (Total Pain Relief), all three doses of ketoprofen, with no dose-related differences among them, were found to provide statistically superior analgesia to codeine and placebo. All five treatments were associated with some adverse reactions.

Adult↗
PubMedDate not supplied

A double-blind parallel comparison of ketoprofen, codeine, and placebo in patients with moderate to severe postpartum pain.

A total of 152 patients were treated at a single center in a single-dose, double-blind parallel study designed to compare the safety and efficacy of 25, 50, and 100 mg ketoprofen to 90 mg codeine and placebo in patients with moderate to severe postpartum pain (i.e., postepisiotomy, uterine cramping, or cesarean section pain). The analgesic responses to all three doses of ketoprofen and 90 mg codeine were superior to placebo and were not significantly different from each other. No dose-related response was observed with ketoprofen. The number of side effects was significantly greater (P = 0.001) among patients receiving codeine (six patients) than among those receiving ketoprofen (three patients).

Adult↗
PubMedDate not supplied

A double-blind comparison of orally administered ciramadol and codeine for relief of postoperative pain.

Ciramadol, a new analgesic with mixed narcotic agonist-antagonist actions, was compared with codeine and placebo in a double-blind study in 343 patients with postoperative pain. The patients received a single oral dose of either 30 or 60 mg of ciramadol, 60 mg of codeine, or placebo. As indicated by three efficacy measures (verbal and visual analog pain scores and pain relief scores), the three active treatments were superior to placebo in relieving pain, and 30 and 60 mg of ciramadol generally were equivalent and superior, respectively, to 60 mg of codeine. The group who took 60 mg of ciramadol had a significantly (P less than .05) lower cumulative remedication frequency than that for the other three groups and the highest proportion of satisfactory evaluations by patients and physicians. There was no statistically significant difference in the incidence of side effects (4% to 11%) among the treatment groups. Demonstrated safety and efficacy suggest a role for ciramadol in the treatment of postoperative pain.

Administration, Oral↗
PubMed1979

Solid-state acetylation of codeine phosphate by aspirin.

A nonsolvolytic (solid-state) acetylation of codeine phosphate in the presence of aspirin to yield acetylcodeine phosphate is reported. GLC assays for the simultaneous determination of aspirin and salicylic acid and codeine and acetylcodeine are described. The apparent heat of activation for codeine phosphate is estimated, and the possible reaction mechanisms are discussed.

Acetylation↗
PubMed1986

Negative reinforcing properties of naloxone in the non-dependent rhesus monkey: influence on reinforcing properties of codeine, tilidine, buprenorphine, and pentazocine.

Scheduled infusions of naloxone (1-100 micrograms/kg/inf.) and of buprenorphine (250 micrograms/kg/inf.) generated drug avoidance behavior in the non-dependent rhesus monkey under a continuous avoidance-escape paradigm. Pentazocine (1-100 micrograms/kg/inf.) codeine, (1-100 micrograms/kg/inf. and tilidine (1-250 micrograms/kg/inf.) were ineffective. Addition of varying doses of naloxone to scheduled infusions of codeine, tilidine, and pentazocine generated avoidance behavior not present with scheduled infusions of these opioids alone. The naloxone doses necessary for generation of avoidance behavior were low with the agonists codeine and tilidine, higher with the weak antagonist pentazocine, and highest with the strong antagonist buprenorphine. When monkeys were presented with the fixed tilidine-naloxone combination (100 + 8 parts) and pentazocine-naloxone combination (100 + 1 part) and the buprenorphine-naloxone combination (100 + 66 parts) presently in clinical use only the tilidine-naloxone combination generated drug avoidance behavior to an appreciable extent.

Animals↗