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PubMed1991

Screening of Candida sp. for N-dealkylation of codeine.

A number of Candida species were selected in order to test their ability to N- or O-demethylate codeine. Complex media and chemically defined media used in our experiments. Transformation products were analysed by reversed phase HPLC and TLC methods. N- and O-demethylation of codeine was performed by C. tropicalis NCYC 997, NCYC 405, NCYC 470 and C. albicans LSHTM 3153. Transformation by C. tropicalis NCYC 997 had better results. N- and O-demethylation occurred in the chemically defined medium. Change in the colour of the transformation mixture, in cultures containing more than 5 mmol.l-1 codeine, was attributed to codeine N-oxide, but its presence was not confirmed by HPLC. N- and O-demethylation of codeine by Candida sp. was compared to that occurred in mammals.

Candida↗
PubMed1990

Evaluation of ketorolac, aspirin, and an acetaminophen-codeine combination in postoperative oral surgery pain.

One-hundred twenty-eight outpatients with postoperative pain after the surgical removal of impacted third molars were randomly assigned, on a double-blind basis, to receive oral doses of ketorolac tromethamine 10 mg, aspirin 650 mg, a combination of acetaminophen 600 mg plus codeine 60 mg, or placebo. Using a self-rating record, subjects rated their pain and its relief hourly for 6 hours after medicating. All active medications were significantly superior to placebo. The acetaminophen-codeine combination was significantly superior to aspirin for peak analgesia. Ketorolac was significantly superior to aspirin for every measure of total and peak analgesia, and significantly superior to acetaminophen-codeine for measures of total effect. The analgesic effect of ketorolac was significant by hour 1 and persisted for 6 hours. Repeat-dose data also suggested that ketorolac 10 mg was superior to aspirin 650 mg and acetaminophen-codeine on the day of surgery. Differences among the active medications were trivial for the postoperative days 1-6 analyses. The frequency of adverse effects was over 4 times greater for acetaminophen-codeine than for ketorolac or aspirin.

Acetaminophen↗
PubMed1990

A multiinstitutional evaluation of the analgesic efficacy and safety of ketorolac tromethamine, acetaminophen plus codeine, and placebo in cancer pain.

Seventy-five patients with moderate to severe cancer pain were randomly assigned in a double-blind fashion to receive first-dose ketorolac tromethamine 10 mg orally, acetaminophen 600 mg plus codeine 60 mg orally, or placebo, followed by subsequent doses of ketorolac or acetaminophen plus codeine four times daily for 7 days. Patient characteristics were similar among the treatment groups. The first-dose observation documented that both ketorolac and acetaminophen plus codeine produced an equivalent reduction in cancer pain and were superior to placebo as measured by pain intensity differences and pain relief. Multidose comparison documented a small but statistically significant advantage in mean daily pain relief favoring acetaminophen plus codeine, although there were no differences in mean daily ratings of overall effects for either study medication. Adverse symptoms were acceptable with both ketorolac and acetaminophen plus codeine. We conclude that ketorolac has significant analgesic activity in patients with cancer pain, although its precise role in the treatment regimen of these patients remains undefined.

Acetaminophen↗
PubMed1988

Effects of lidocaine, codeine and vadocaine hydrochloride on platelet aggregation in human platelet-rich plasma.

Lidocaine and vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl)propionanilide+ ++ hydrochloride, OR K-242-HCl; INN: vadocaine), which is structurally related to lidocaine, inhibited the second phases of human platelet aggregation induced by adenosine diphosphate (ADP, 10 mumol/l) or epinephrine (10 mumol/l) and partly aggregation induced by collagen (2.5 micrograms) at concentration relevant to local anesthetic action (0.1-1.0 mmol/l). Codeine was effective at slightly higher concentrations. The concomitant formation of thromboxane B2 (TXB2) was inhibited at similar concentrations. The aggregation induced by arachidonic acid (200 mumol/l) and the first phases of ADP (10 mumol/l)- or epinephrine (10 mumol/l)-induced aggregations were inhibited by all the compounds at the concentrations 1-10 mmol/l, codeine being the most potent inhibitor. The only exception was vadocaine, which inhibited the first phase of epinephrine-induced aggregation at concentrations greater than or equal to 0.25 mmol/l. Vadocaine may possess a2-adrenergic blocking activity. At low concentrations (less than or equal to 0.1 mmol/l), all the compounds stimulated/tended to stimulate the second phase of ADP-induced aggregation and concomitant formation of TXB2. They strongly stimulated TXB2 formation induced by exogenous arachidonic acid even at concentrations causing inhibition of aggregation. Codeine was the most and vadocaine the least potent in this respect. Lidocaine as well as vadocaine (0.1 mmol/l) and codeine (1.0 mmol/l) potentiated the antiaggregatory effect of dibutyryl-cyclic AMP (dB-cAMP) on the ADP-induced aggregation. Lidocaine (0.1 mmol/l) and codeine (1.0 mmol/l) similarly potentiated the effect of the adenylate cyclase stimulator prostaglandin E1 (PGE1).

Adenosine Diphosphate↗
PubMed1988

Gas chromatographic/mass spectrometric analysis of morphine and codeine in human urine of poppy seed eaters.

In this study, poppy seeds were examined for a natural constituent that might serve as a maker for the seeds' ingestion as opposed to opiate abuse. Thebaine was selected as possible marker, since it was found to be a component of all poppy seeds examined and was not a natural component of different heroin samples. During the course of this investigation, a new extraction and cleanup procedure was developed for the gas chromatographic/nitrogen phosphorus detection (GC/NPD) and gas chromatographic/mass spectrometric (GC/MS) analysis of morphine and codeine in urine. A linear response, over a concentration range of 25 to 600 ng/mL, was obtained for codeine and morphine (r = 0.9982 and 0.9947, respectively). The minimum detectable level (LOD) and limit of quantitation (LOQ) for morphine were 10 and 30 ng/mL, respectively; whereas LOD and LOQ for codeine were 2 and 8 ng/mL, respectively. The coefficients of variance (CV, n = 6) for morphine and codeine analyses at the 100-ng/mL level were 13.3 and 4.6%, respectively. This procedure was used for the analysis of urine samples from five poppy seed eaters who each ingested 200 g of poppy seed cake. Results indicated that significant amounts of morphine and codeine are excreted in urine and that in all subjects, at least at one point in time, the apparent morphine concentration as determined by radioimmunoassay (RIA) analysis exceeded the cutoff value (300 ng/mL) established for screening. Thebaine was not detected in urine specimens collected following poppy seeds ingestion and thus could not be used as a marker.

Chromatography, Gas↗
PubMed1988

Comparative studies on the dependence liability of morphine hydrochloride, codeine phosphate and two novel antitussive compounds vadocaine hydrochloride and N-(2',4'-dimethyl-6'-methoxyphenyl)-4-(diethylamine) butanamide hydrochloride in mice.

The effects of two novel antitussive compounds, vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl)propionanilide+ ++ hydrochloride, OR K-242-HCl; INN: vadocaine) and N-(2,4-dimethyl-6-methoxyphenyl)-4-(diethylamine)butanamide hydrochloride (OR K-269-HCl) on the suppression of withdrawal signs (hypothermia and weight loss) induced by repeated morphine administration were compared to those of acute morphine and codeine administrations. Moreover, spontaneous and precipitated withdrawal-induced hypothermia, weight loss and behavioural changes from repeated codeine, vadocaine and OR K-269-HCl administrations were studied. Acute administration of morphine clearly reversed the hypothermia and weight loss induced by spontaneous withdrawal from morphine. Codeine was not able to suppress the hypothermia and weight loss induced by morphine withdrawal. Acute injections of vadocaine and OR K-269-HCl did not alter these withdrawal signs either. Moreover, acute administration of codeine tended to prevent the weight loss induced by codeine withdrawal and caused behavioural changes. Spontaneous or precipitated withdrawal from repeated vadocaine or OR K-269-HCl administration caused neither hypothermia, weight loss nor behavioural changes. These results support the view that compounds vadocaine and OR K-269-HCl are free from morphine-like addictive properties.

Animals↗
PubMed1987

Chemical characterization and regulation of endogenous morphine and codeine in the rat.

Data on the tissue distribution of morphine and codeine in rat are presented. The concentration of these two opiate alkaloids seems to be distributed uniformly in the cortex, midbrain, pons/medulla and cerebellum. The spinal cord and the adrenal gland have high levels of morphine and codeine and the adrenal has more codeine than morphine. The major fraction of the alkaloids reside in a synaptosomal fraction and are present in tissues as the sulfate conjugate. The levels of morphine in the spinal cord and the urinary excretion of morphine are elevated in the arthritic rat model. We used extracted alkaloid samples from arthritic rats spinal cord for analysis by mass spectrometry and found molecular ions identical with morphine and codeine. The results are discussed in the light of possible physiological roles of endogenous morphine and codeine.

Animals↗
PubMed1986

Taste preference for cough syrups: a comparative study of three codeine-containing medications.

Unpleasant taste is a common feature of cough syrups, particularly those containing codeine. An antitussive compound of codeine sulfate and chlorpheniramine maleate was formulated in a coated drug-resin complex, which prevents release of the active ingredients until they reach the stomach and small intestine. Thus patients do not taste the bitterness of the codeine. A three-way crossover taste test was conducted in 175 volunteers who tasted each of three cough syrups in random sequence, rated the taste of each, and ranked their preferences. The cough syrups used in the study were the aforementioned formulation (CM), promethazine hydrochloride with codeine (PH), and iodinated glycerol with codeine phosphate (IG). Tastes were rated on a scale from +2 (very good) to -2 (very poor). Mean rating scores for each product were 0.97 for CM, 0.14 for PH, and -1.5 for IG. Pairwise comparisons showed statistically significant differences between CM and PH (P less than 0.01) and CM and IG (P less than 0.001) but no significant difference between PH and IG. CM was ranked as most liked by 115 respondents and as least liked by 27 respondents. Reasons cited for this preference were its sweet rather than medicinal taste and its smooth, thick consistency. Bitterness was a common reason for the lack of preference for PH and IG. CM thus was shown to have greater user acceptability than either of the other two cough syrups tested.

Antitussive Agents↗
PubMed1986

Effect of dextromethorphan on guinea pig ileal contractility in vitro: comparison with levomethorphan, loperamide and codeine.

Dextromethorphan (DM) was tested for its effect on the contractility of the guinea pig ileum in vitro. Comparisons were made with levomethorphan, levorphanol, codeine and loperamide. DM and codeine inhibited the contractions of the electrically stimulated ileum, with IC50 values of 15 and 8 microM, respectively. The inhibitory effect of DM, in contrast to codeine, was not blocked by the opiate antagonist naloxone. Pretreatment (8, 50 and 100 microM) with DM and its I-isomer levomethorphan reduced in a dose-dependent fashion both phasic and tonic contractions produced by maximally effective concentrations of carbachol and 80 mM KCl. Pretreatment (8, 50 and 100 microM) with codeine, dextrorphan or levorphanol, unlike DM, did not reduce carbachol or KCl-induced contractions. The concentration-response curves to calcium in K+ depolarized ileum were shifted to the right in a parallel manner suggesting competitive antagonism for DM (pA2 5.3), levomethorphan (pA2 5.3) and loperamide (pA2 6.6). Codeine and levorphanol (8, 50 and 100 microM) did not antagonize calcium-induced contractions. In two assays of calmodulin-dependent processes DM was inactive (IC50 greater than 1 mM), whereas trifluoperazine and calmidazolium (standard calmodulin antagonists) were active in the micromolar range. In summary, these data suggest that DM, through a nonopiate mechanism, antagonizes gut contractility possibly by "stabilizing" neuronal and/or muscle cell membranes.

Actins↗
PubMed1984

Dextromethorphan and codeine: comparison of plasma kinetics and antitussive effects.

Plasma kinetics of dextromethorphan (as dextrorphan ) and codeine were investigated after acute oral doses in 8 patients with pathological cough; after which the patients participated in an acute dose-response study of the antitussive effects of each drug administered as syrups. Maximum plasma codeine concentrations averaged 384 ng.ml-1 (s.d. +/- 78.3) occurring between 0.75 and 2h after ingestion of 60 mg codeine phosphate; in comparison mean peak plasma dextrorphan levels were 386 ng.ml-1 (s.d. +/- 107.2) and 388 ng.ml-1 (s.d. +/- 101.3) respectively, after administration of 60 mg dextromethorphan syrup and tablet formulations. Bioavailability of dextromethorphan tablets was comparable to syrup. No correlation emerged between instantaneous plasma concentrations of either dextrorphan or codeine and antitussive responses; however, peak antitussive effect was significantly related to log dose with both drugs. Antitussive effects of 30 mg codeine phosphate and 60 mg dextromethorphan hydrobromide did not differ significantly; both were superior to 30 mg dextromethorphan hydrobromide and placebo.

Administration, Oral↗
PubMedDate not supplied

Comparison of conorphone, a mixed agonist-antagonist analgesic, to codeine for postoperative dental pain.

The analgesic efficacy of two doses of conorphone (20 and 40 mg), a mixed agonist-antagonist analgesic, were compared to two doses of codeine for postoperative pain in the oral surgery model. Each subject received 2 of the 4 possible treatment at two separate sessions in an incomplete block, single crossover design. Both doses of conorphone and the 60 mg dose of codeine were superior to 30 mg of codeine for the various indices of analgesic activity. The 40 mg dose of conorphone resulted in a high incidence of side effects (25/30 subjects) such as drowsiness, dizziness, nausea and vomiting. The low dose of conorphone resulted in side effects similar to 60 mg of codeine with the exception of a greater incidence of drowsiness. These data suggest that while 40 mg of conorphone may not be well tolerated clinically, 20 mg of conorphone may be an alternative to 60 mg of codeine for postoperative pain.

Adolescent↗
PubMed1983

[Effects of codeine and morphine on the primary humoral immunity of the respiratory tract].

To investigate the effects of centrally acting antitussive drugs, codeine and morphine, on the humoral immunity in the respiratory tract, male guinea pigs were immunized either systemically (i.p.) or locally (intratracheally, i.t.) with sheep red blood cells (SRBC). The development of plaque-forming cells (PFC) was determined using the spleen (S-PFC) and tracheobronchial lymph node cells (T-PFC). (I) Number of S-PFC after i.p. immunization increased to the maximum on day 5. Peak number of S-PFC and T-PFC after i.t. immunization occurred on day 6. (II) i.p. immunization: The drugs were given i.p. for 5 days before or for 4 days after immunization. Morphine (5 mg/kg) given prior to the immunization decreased spleen cellularity. Pretreatments with codeine (15 mg/kg) and morphine (5 mg/kg) also markedly inhibited the number of S-PFC. These drugs given after the immunization hardly affected the number of S-PFC. (III) i.t. immunization: The drugs were given for 5 days before or after the immunization. Codeine (15 mg/kg) given prior to the immunization inhibited the number of S-PFC. Codeine (3, 15 mg/kg) and morphine (1, 5 mg/kg) given before and after the immunization markedly inhibited the number of T-PFC, dose-dependently. These results indicate that codeine and morphine affect the humoral immunity both locally in the respiratory tract and systemically, which cautions against an easygoing use in respiratory diseases.

Animals↗
PubMed1981

Propiram and codeine in episiotomy pain.

To evaluate relative efficacy, safety, and time course of analgesia, propiram fumarate (50 and 100 mg), a new narcotic agonist-antagonist, was compared with codeine sulfate (60 mg) and placebo in a clinical trial with a single peroral dose, parallel, stratified, randomized, and double-blind design involving 80 hospitalized postpartum women with medium or severe episiotomy pain. Using verbal subjective reports as index of response, patients rated pain intensity and side effects at periodic interviews for 6 h. Relative efficacy findings based on peak effects and summed pain-intensity differences suggested dose-dependent analgesia with propiram and also that 60 mg codeine lay between 50 mg propiram and placebo. Moreover, after 50 or 100 mg propiram, 8 of 20 patients reported greater than 50% reduction of initial pain compared with 7 of 20 after 60 mg codeine and 2 of 20 after placebo. After each of the propiram doses, distinct analgesia began within 1/2 h and reached peak effect between 1 h (p less than 0.02) and 2 h (p less than 0.05). After f60 mg codeine, onset was slower and peak later (4 h, p less than 0.05). All three active drugs continued to act until the 5th or 6th h. Drowsiness was the only statistically significant side effect reported after propiram. These results suggest that single 50 or 100 mg doses of propiram were effective in episiotomy pain, induced stronger analgesia than 60 mg codeine, and took effect more rapidly.

Analgesics↗
PubMed1980

[Plasma levels and renal excretion of [3H]-codeine phosphate in humans receiving tablets or depot capsules (author's transl)].

In two studies (a) a single 50 mg [3H]-codeine phosphate depot capsule (a special sustained-release form) and (b) two dosages of 25 mg [3H]-codeine phosphate tablets with a time lag of 4 h for the second administration were given to the same 4 healthy volunteers. In both studies plasma level and renal excretion of the radioactivity and plasma level of the specifically extracted unchanged drug were measured. The renal exretion was nearly complete within 48 h in both studies. The relative bioavailability of the [3H]-codeine phosphate released from the capsule and from the two tablets was shown to be the same comparing the areas under the plasma level curves. Assuming that the effective codeine plasma level is about 20 ng/ml a cough preventing period of at least 8 h after administration of a codeine depot capsule can be concluded from the given results.

Adult↗
PubMed1997

Differential brainstem Fos-like immunoreactivity after laryngeal-induced coughing and its reduction by codeine.

We used the expression of the immediate-early gene c-fos, a marker of neuronal activation, to localize brainstem neuronal populations functionally related to fictive cough (FC). In decerebrate, paralyzed, and ventilated cats, the level of Fos-like immunoreactivity (FLI) was examined in five groups of animals: (1) controls, sham-operated unstimulated animals; (2) coughing cats, including both animals in which FC was elicited by unilateral electrical stimulation of the superior laryngeal nerve (SLN) and (3) those in which FC was elicited by bilateral SLN stimulation; (4) stimulated-treated cats, in which bilateral SLN stimulation was applied after selective blockade of FC by codeine; and (5) codeine controls, sham-operated unstimulated cats subjected to administration of codeine. Fifteen brainstem structures were compared for numbers of labeled cells. Because codeine selectively blocks FC, brainstem nuclei activated specifically during FC were identified as regions showing increased FLI after FC and significant reductions in FLI after FC suppression by codeine in stimulated-treated cats. In coughing animals, we observed a selective immunoreactivity in the interstitial and ventrolateral subdivisions of the nucleus of the tractus solitarius, the medial part of the lateral tegmental field, the internal division of the lateral reticular nucleus, the nucleus retroambiguus, the para-ambigual region, the retrofacial nucleus, and the medial parabrachial nucleus. FLI in all these nuclei was significantly reduced in stimulated-treated cats. Our results are consistent with the involvement of neurons overlapping the main brainstem respiratory-related regions as well as the lateral tegmental field and the lateral reticular nucleus in the neural processing of laryngeal-induced FC.

Animals↗
PubMed1987

Symptomatic treatment of chronically recurring tension headache: a placebo-controlled, multicenter investigation of Fioricet and acetaminophen with codeine.

A double-blind, randomized, multicenter investigation was conducted to compare the efficacy and safety of Fioricet, acetaminophen with codeine, and placebo for the symptomatic treatment of tension headache. At the onset of a typical headache, the patients took two capsules of their assigned study medication and rated responses over the next four hours in three target symptoms areas: pain, emotional or psychic tension, and muscle contractions or stiffness in the head and neck. Physicians made global assessments of the same symptom responses and of adverse reactions for each patient. One hundred ninety-eight patients were evaluated. Both active analgesic preparations were more effective than placebo in relieving pain and muscle stiffness or contractions. Fioricet, but not acetaminophen with codeine, was significantly better than placebo in alleviating emotional or psychic tension; Fioricet was also significantly better than acetaminophen with codeine in relieving this symptom. Certain analyses suggested the possibility that Fioricet had a faster and more sustained analgesic effect than acetaminophen with codeine. By the end of the four-hour trial, significantly more patients achieved complete pain relief with Fioricet than with acetaminophen with codeine. The quality and quantity of adverse reactions did not differ significantly among the treatment groups. None was serious, and all abated without medical intervention.

Acetaminophen↗
PubMedDate not supplied

Rectal versus oral absorption of codeine phosphate in man.

Rectal absorption of codeine phosphate from various dosage forms was studied in man. The rectal dosage forms included aqueous solutions and fatty suppositories. A comparison was made with an orally administered solution. The plasma concentrations of codeine were measured by means of HPLC analysis after a single dose of 60 mg codeine phosphate in a cross-over study in 7 volunteers. Compared with oral dosing rectal absorption from an aqueous solution or a fatty suppository produced an almost identical plasma concentration profile with similar interindividual variations. Comparing the absorption rate characteristics it appeared that rectal absorption from an alkaline solution containing codeine phosphate proceeded significantly (P less than 0.05) more rapid than after oral dosing. No essential difference in bioavailability was observed between the various rectal and oral dosage forms.

Administration, Oral↗
PubMed1992

Acceptability and efficacy of two associations of paracetamol with a central analgesic (dextropropoxyphene or codeine): comparison in osteoarthritis.

A double-blind randomized parallel group trial was undertaken to compare the acceptability and efficacy of 2 forms of analgesic treatment, DI-Antalvic (Houde Laboratories, Puteaux, France) (30 mg dextropropoxyphene and 400 mg paracetamol per capsule) and Efferalgan-Codeine (UPSA Laboratories, Rueil Malmaison, France) (30 mg codeine and 500 mg paracetamol per tablet) prescribed for 1 week at doses of 6 capsules/day and 6 tablets/day, respectively, in 141 outpatients with active osteoarthritis of the knee or hip. The principal aim of the trial was concerned with acceptability, with efficacy as its secondary aim. The principal trial criterion was defined as overall assessment of acceptability by the patient at the end of the trial (success or failure) or by treatment dropouts because of an adverse effect (failure). Comparability of the groups was confirmed before any treatment regarding the physical characteristics of the patients, characteristics of osteoarthritis, and the initial level of pain and functional consequences of pain. Results show that the analgesic efficacy of the treatment was similar, but that the acceptability of Efferalgan-Codeine was significantly worse than that of DI-Antalvic: 53% failure with Efferalgan-Codeine versus 29% failure with DI-Antalvic (P = .005). Other trials of the same type would seem necessary (comparison of lower doses, other types of pain) before being able to generally extrapolate such findings.

Acetaminophen↗