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PubMed2006

Codeine-binding RNA aptamers and rapid determination of their binding constants using a direct coupling surface plasmon resonance assay.

RNA aptamers that bind the opium alkaloid codeine were generated using an iterative in vitro selection process. The binding properties of these aptamers, including equilibrium and kinetic rate constants, were determined through a rapid, high-throughput approach using surface plasmon resonance (SPR) analysis to measure real-time binding. The approach involves direct coupling of the target small molecule onto a sensor chip without utilization of a carrier protein. Two highest binding aptamer sequences, FC5 and FC45 with K(d) values of 2.50 and 4.00 microM, respectively, were extensively studied. Corresponding mini-aptamers for FC5 and FC45 were subsequently identified through the described direct coupling Biacore assays. These assays were also employed to confirm the proposed secondary structures of the mini-aptamers. Both aptamers exhibit high specificity to codeine over morphine, which differs from codeine by a methyl group. Finally, the direct coupling method was demonstrated to eliminate potential non-specific interactions that may be associated with indirect coupling methods in which protein linkers are commonly employed. Therefore, in addition to presenting the first RNA aptamers to a subclass of benzylisoquinoline alkaloid molecules, this work highlights a method for characterizing small molecule aptamers that is more robust, precise, rapid and high-throughput than other commonly employed techniques.

Aptamers, Nucleotide↗

PubMed1989

A fatality involving secobarbital, nitrazepam, and codeine.

A fatal case involving the suicidal ingestion of secobarbital, nitrazepam, and codeine is presented. The drugs were quantified using gas chromatography for codeine and high-performance liquid chromatography for the two other drugs. The blood concentrations of secobarbital, nitrazepam, and codeine were found to be 11.48, 1.72, and 0.036 microgram/ml, respectively. Results are discussed in the light of the existing literature.

Adipose Tissue↗

PubMed1998

A comparison of the effects of intravenous tramadol, codeine, and morphine on gastric emptying in human volunteers.

UNLABELLED: We compared the effects of i.v. tramadol (1.25 mg/kg), codeine (1 mg/kg), morphine (0.125 mg/kg), and saline on gastric emptying in 10 healthy human volunteers using a double-blind, randomized, cross-over design. Subjects received one treatment at each of four sessions, 2 wk apart. Gastric emptying was studied using the paracetamol absorption test. There were significant differences when comparing all treatments for concentration-time data (P = 0.002), peak serum paracetamol concentrations (Cmax; P < 0.001), times at Cmax (Tmax; P = 0.003), and areas under the curves from Time 0 to 360 min (AUC(0-360); P = 0.049). Morphine profoundly inhibited gastric emptying. Tramadol had measurable but statistically insignificant inhibitory effects on gastric emptying compared with saline (mean +/- SEM: Cmax 22.4 +/- 2.2 vs 26.8 +/- 2.5 mg/L [P = 0.19], Tmax 33 +/- 5.4 vs 19.5 +/- 2.3 min [P = 0.054] for tramadol versus saline, respectively). Compared with morphine, the Cmax (P < 0.01), Tmax, and AUC(0-360) (P < 0.05) values for tramadol were significantly different. The Tmax value for codeine (63.3 +/- 11.7) was greater than that for tramadol (P = 0.034). We conclude that tramadol has a measurable but smaller inhibitory effect on gastric emptying compared with other opioids. IMPLICATIONS: We compared the effect of tramadol, an unconventional opioid painkiller, on stomach emptying with that of codeine and morphine in a human volunteer study. Tramadol had a measurable but smaller effect and may have clinical and economic advantages in acute pain management compared with conventional painkillers.

Acetaminophen↗

PubMed1986

Experimental pain induced by electrical and thermal stimulation of the skin in healthy man: sensitivity to 75 and 150 mg diclofenac sodium in comparison with 60 mg codeine and placebo.

Models with experimentally induced pain in healthy man might be useful for the screening for analgesic effects of new drugs. Experimental pain models have been shown to discriminate reliably between the effects of opioid analgesics and placebo but their sensitivity to nonsteroidal anti-inflammatory agents is disputed. This study investigated whether it would be possible by using electrically and thermally induced cutaneous pain to discriminate reliably the effects of single oral doses of 75 and 150 mg diclofenac sodium on the one hand and 60 mg codeine on the other from those of placebo. Forty-eight healthy subjects participated each in four experiments in which they received, in random double-blind fashion, each of the treatments. Every experiment comprised eight series of measurements, two before and six after drug administration, carried out at 30 min intervals. Diclofenac sodium produced significant dose-related increases of threshold and tolerance to electrically and threshold to thermally induced pain. Codeine 60 mg was significantly superior to placebo in all pain measures. Its analgesic effects were stronger than those of diclofenac 75 mg but weaker than those of diclofenac 150 mg. Neither 150 mg nor 75 mg diclofenac caused more side effects than placebo, whereas codeine 60 mg elicited a high frequency of side effects. No severe adverse effects occurred after any one treatment. The results suggest that both electrically and thermally induced cutaneous pain are well suited to evaluate analgesic effects not only of opioids but also of nonsteroidal anti-inflammatory drugs.

Acoustic Stimulation↗

PubMed1992

The influence of codeine, propantheline and metoclopramide on small bowel transit and theophylline absorption from a sustained-release formulation.

1. The effects of the anticholinergic agent, propantheline, the opiate, codeine, and the prokinetic agent, metoclopramide, on oral-caecal transit time and on the absorption of theophylline from a sustained-release formulation were examined in six healthy male volunteers. 2. A cross-over randomised sequence design was followed, allowing at least 2 weeks interval between studies. On each occasion 500 mg theophylline in a sustained-release formulation was taken simultaneously with 2 g sulphasalazine at zero time. On three of the four occasions one of the following treatments was given concurrently at -0.5 h, +3.5 h, and +7.5 h: 30 mg codeine phosphate, 30 mg propantheline bromide, or 10 mg metoclopramide monohydrochloride. 3. The appearance of sulphapyridine in the plasma was used to assess oral-caecal transit time and the mean fraction absorbed-time profile of theophylline was calculated from serial serum theophylline concentration measurements using the Wagner-Nelson method. 4. Codeine increased the mean (s.d.) oral-caecal time (h) significantly (5.14 +/- 0.94) compared with the control value (3.78 +/- 0.34). Propantheline inhibited peristaltic contractions to such an extent that the oral-caecal transit time in five of the volunteers was between 9 and 25 h, while sulphapyridine appeared in the 9 h serum sample of the sixth. Metoclopramide did not significantly alter the oral-caecal transit time. 5. Despite the observed changes in oral-caecal transit time the rate and extent of theophylline absorption was similar with all regimens.

Adult↗

PubMed1991

The effects of astemizole, cetirizine and loratadine on the time course of weal and flare reactions to histamine, codeine and antigen.

An open cross-over study was performed to assess the effects of astemizole, cetirizine and loratadine on weal and flare reactions to intradermal histamine, codeine and house dust mite antigen. Percentage inhibition of weal area, flare area and weal volume was greatest for cetirizine, then astemizole and smallest for loratadine. Wealing due to mast-cell degranulation with either codeine or antigen was less inhibited by all three antihistamines than that due to histamine itself. Time-course studies revealed similarities between wealing provoked by codeine and histamine but different characteristics to that induced by antigen.

Adult↗

PubMed1996

Additive analgesic effect of codeine and paracetamol can be detected in strong, but not moderate, pain after Caesarean section. Baseline pain-intensity is a determinant of assay-sensitivity in a postoperative analgesic trial.

BACKGROUND: A randomized, double-blind, placebo-controlled single oral dose study was done in order to examine whether codeine has an additive analgesic effect to that of paracetamol for moderate and strong postoperative pain after abdominal surgery. The maximum recommended single dose of paracetamol 1000 mg (Paracet) was compared with a combination of a submaximal dose of paracetamol 800 mg plus codeine 60 mg (Paralgin forte) and placebo for pain relief after Caesarean section in 125 patients. METHODS: Visual analogue pain intensity score (VAS 0-100 mm) and categorical pain relief score were recorded for 6 hours after the study drug intake. The main efficacy variables analyzed were: pain intensity difference and summed pain intensity differences during the first 3 and 6 h after study drug intake, total pain relief during the first 3 and 6 h, global evaluation score at the end of the observation period, and time to rescue analgesic. RESULTS: Because of protocol violations, 17 patients were excluded from the analysis of effects. Among the 108 patients included in the analysis of analgesic effect, 49 patients had moderate baseline pain (VAS between 40 and 60 mm on a 100 mm scale), and 59 patients had strong baseline pain (VAS more than 60 mm). In patients with strong baseline pain, statistically highly significant differences were documented in efficacy variables between the active drugs and placebo and between the two active drugs. However, in patients with moderate baseline pain, no differences were found between the study drugs in any of the analgesic efficacy variables. CONCLUSION: This study thus confirms that codeine has additive analgesic effect to paracetamol in pain after surgery. Our results show the importance of initial pain intensity in postoperative assessment of analgesic drugs. Assay-sensitivity and test power are increased by selecting patients with sufficiently high initial pain intensity and by comparing groups of patients with identical surgery and similar demographic variables.

Acetaminophen↗

PubMed1988

The effect of nedocromil sodium, sodium cromoglycate and codeine phosphate on citric acid-induced cough in dogs.

1. The effects of nedocromil sodium, sodium cromoglycate and codeine phosphate on citric acid-induced cough have been studied in conscious tracheostomised dogs. 2. Nedocromil sodium (approximately 15 mg given as an aerosol) and codeine phosphate (5 mg kg-1, i.v.) significantly increased the time to the first cough when dogs were challenged with citric acid aerosol. The mean number of coughs in the initial period of coughing fell after treatment of dogs with nedocromil sodium or with codeine phosphate, but this reduction in mean cough number was not statistically significant. 3. Neither sodium cromoglycate (approximately 15 mg given as an aerosol) nor saline had significant effect on a citric acid challenge. 4. It is concluded that nedocromil sodium, but not sodium cromoglycate, possesses an anti-tussive action that may result from inhibition of sensory nerve activity in the lung. Nedocromil sodium may prove useful in the treatment of unproductive cough in situations where the use of a centrally-acting antitussive is undesirable.

Animals↗

PubMed1979

Comparative metabolism of codeine in man, rat, dog, guinea-pig and rabbit: identification of four new metabolites.

The metabolism and excretion of codeine and its metabolites in untreated urine of man, rat, dog, guinea-pig and rabbit have been examined. Metabolites were identified by gas chromatography mass spectrometry operated in the chemical ionization mode (methane). Concentrations of codeine and metabolites were measured by selected ion monitoring. Both codeine and norcodeine were detected in the urine of all species but a new metabolite, hydrocodone, was found only in the urine from man, guinea-pig and dog. Additional metabolites (presumably resulting from the metabolism of hydrocodone) were also detected in man and guinea-pig. Overall recoveries of drug and metabolites from untreated urine were low for all species.

Adult↗

PubMed1983

Dextromethorphan and codeine: objective assessment of antitussive activity in patients with chronic cough.

Dextromethorphan, the most widely used cough suppressant in the U.S.A., was compared with codeine, the traditional European antitussive, in a double-blind, crossover trial using both an objective and subjective assessment of efficacy in sixteen patients with chronic, stable cough. Both preparations, at a dose of 20 mg, were similarly effective in reducing cough frequency. Dextromethorphan lowered cough intensity to a greater degree than codeine (p less than 0.0008) and was considered the better antitussive by the majority of patients (p less than 0.001). In view of its lack of side-effects, its safety even in overdose and its non-narcotic status, the increasing trend in Europe to use dextromethorphan as a substitute for codeine in the treatment of cough is to be welcomed.

Adult↗

PubMed2004

Radiotherapy plus either transdermal fentanyl or paracetamol and codeine for painful bone metastases: a randomised study of pain relief and quality of life.

OBJECTIVE: To compare the effects of providing analgesia with either transdermal fentanyl (TTS-fentanyl) or paracetamol and codeine (P/C) in addition to radiotherapy in patients with metastatic bone pain. METHODS: In a prospective study, 26 patients with radiologically confirmed bony metastases received radiotherapy (R/T). They were randomised to receive either 500 mg paracetamol and 30 mg codeine four times per day (P/C group), or transdermal fentanyl patches delivering 25 microg fentanyl/h (TTS-fentanyl group). Pain was assessed using visual analogue pain ratings (VAS) and the Greek Brief Pain Inventory (G-BPI) questionnaire administered before R/T and after 3 months. RESULTS: Data were available from 24 eligible patients. Use of TTS-fentanyl was associated with significantly superior pain relief. Mean VAS fell from 7.0 to 1.1 with TTS-fentanyl and from 8.3 to 4.3 with P/C, p< 0.01. The TTS-fentanyl group also showed significantly greater improvements of important G-BPI domains including global quality of life, pain, and physical, cognitive, and role functioning, than the P/C group (p< 0.01). Four patients receiving TTS-fentanyl and three receiving P/C reported severe nausea/vomiting. CONCLUSIONS: Transdermal fentanyl combined with R/T was more effective in reducing metastatic bone pain and resulted in greater improvements in quality of life than paracetamol and codeine.

Acetaminophen↗

PubMed1978

The analgesic and anti-inflammatory efficacy of diflunisal and codeine after removal of impacted third molars.

A double-blind, randomized trial was carried out in 90 patients to compare the analgesic and anti-inflammatory efficacy of 500 mg diflunisal twice daily with that of 25 mg codeine phosphate 4-times daily and placebo in relieving pain and swelling after surgical removal of impacted third molars. Diflunisal was found to be superior to codeine and placebo on the first post-operative day, but the difference in efficacy of the drugs had diminished by the third post-operative day. In the diflunisal group of 30 patients, 10 (33%) developed 'dry socket' or alveolitis sicca dolorosa. Only 2 patients in the codeine group and 1 patient in the placebo group developed this very painful condition. The possible explanation of 'dry socket' is discussed.

Adolescent↗

PubMed2004

The pupillary effects of intravenous morphine, codeine, and tramadol in volunteers.

Opioid analgesics have pharmacological effects in many organ systems, including the eye. Because the metabolites of morphine and codeine contribute to their overall pharmacological effect pupil diameter measurements were made over a 6-h period. We studied the pupillary effects of IV morphine (0.125 mg/kg), codeine (1 mg/kg), tramadol (1.25 mg/kg), or placebo (10 mL 0.9% w/v sodium chloride) in 10 healthy volunteers. Pupil diameter was measured every 30 min using a pupil densitometer. Comparisons of the change in pupil diameter for each drug were made using analysis of variance with repeated measures. No significant change in pupil diameter was observed after placebo. After IV morphine and codeine administration there was a 26% decrease in pupil diameter (P < 0.001). Over the course of the study period, pupil diameter gradually returned to baseline values. After administration of tramadol there were no significant changes in pupil diameter until 150 min after administration, after which there was a significant reduction for the remainder of the study period (P < 0.01). The changes in pupil diameter may be explained in part by the pharmacokinetic profiles of the opioids studied. Measurement of pupil diameter may have a place in monitoring the central effect of opioids.

Adult↗

PubMed1993

Effects of zolpidem, codeine phosphate and placebo on respiration. A double-blind, crossover study in volunteers.

The effects of zolpidem, codeine phosphate and placebo on respiration were evaluated in a double-blind, randomised, crossover study involving 12 healthy men. Single oral doses of zolpidem 10 or 20 mg, codeine phosphate 60 mg or placebo were administered in the morning. Each treatment was separated by a washout period of at least 72 h. Ventilatory responses to carbon dioxide and mouth occlusion pressure, measured 1 h before and at 1 and 3 h after doses, were not significantly affected by either zolpidem dose; however, codeine phosphate produced a small but significant respiratory suppressant effect at 3 h. Mean inspiratory flow was noninvasively assessed using respiratory inductive plethysmography 1 h predose and at 1 to 5 h postdose. No significant change in mean inspiratory flow was noted after zolpidem 10 mg. Two hours after administration of zolpidem 20 mg, mean inspiratory flow was significantly lower than after placebo, possibly related to some individuals falling asleep during data collection. All volunteers reported adverse events; the most common were slurred speech (in 1 after 10 mg and in 5 after 20 mg of zolpidem), dizziness (in 4 after both 10 mg and 20 mg of zolpidem) and diplopia/blurred vision (in 4 after 20 mg of zolpidem). Zolpidem appears to be well tolerated, with no respiratory suppression up to doses of 10 mg and minimal suppression of mean inspiratory drive at doses of 20 mg.

Adult↗

PubMedDate not supplied

Application of liquid chromatography to the simultaneous determination of acetylsalicylic acid, caffeine, codeine, paracetamol, pyridoxine, and thiamine in pharmaceutical preparations.

This paper describes a rapid reversed-phase liquid chromatographic method, with UV detection, for the simultaneous determination of acetylsalicylic acid, caffeine, codeine, paracetamol, pyridoxine, and thiamine in pharmaceutical preparations. A reversed-phase C18 Nucleosil column is used. The mobile phase consists of 2 successive eluants: water (5 min) and acetonitrile-water (75 + 25, v/v; 9 min), both adjusted to pH 2.1 with phosphoric acid. Before determination acetylsalicylic acid is completely converted to salicylic acid by alkaline hydrolysis. Salicylic acid, caffeine, paracetamol, pyridoxine, and thiamine are all detected at 285 nm, whereas codeine is detected at 240 nm. Calibration curves were linear for salicylic acid, caffeine, paracetamol, and pyridoxine in the range of 50-500 mg/L, and for codeine and thiamine in the range of 50-1000 mg/L. The method was applied to the analysis of 13 fortified commercial pharmaceutical preparations. Recoveries ranged from 92.6 to 105.5%, with relative standard deviations of 1.1-5.8%.

Acetaminophen↗

PubMedDate not supplied

From codeine to transdermal fentanyl for cancer pain control: a safety and efficacy clinical trial.

BACKGROUND: Fentanyl is a synthetic opioid, suitable for transdermal delivery, offering an interesting solution as a step 3 opioid in cancer pain treatment. The purpose of the study was to carefully investigate: 1) the feasibility of the direct conversion from codeine to TTS fentanyl, in patients already receiving codeine and requiring strong opioids for their analgesia; 2) the safety of 25 microg/hour incremental steps and at shorter than 72-hour intervals, if clinically required. PATIENTS AND METHODS: 130 patients were judged eligible for the study. All the patients were receiving 280-360 mg or more of codeine and required strong opioid for their analgesia. The study lasted 56 days. The initial dose was 25 microg/hour. TTS fentanyl for all patients. Data assessments were made on baseline, day 1, day 2, day 3, in the hospital and thereafter on days 7, 14, 21, 28, 42 and 56. After the patch application, all the patients were given an immediate release oral morphine (5 mg) every 4-6 hours for the first 12 hours and then if needed only as rescue doses. The patients remained in the hospital for the first three days of the study where follow-up (pain score, satisfaction, side effects etc.). was recorded by the palliative care team and by daily cards. RESULTS: The itnitial dose of fentanyl was 25 microg/hour while the mean dose on day 3 was 45.9 microg/hour. All the patients required upward titration of the study medication during follow-up visits. On day 56 the mean dose of fentanyl was 87.4 microg/hour. Mean pain intensity decreased from an initial 5.96 on the baseline to 0.83 on day 3. Karnofsky scale measurements between treatment phases revealed non-significant changes. The rate of overall satisfaction was quite high. Nine patients discontinued the study due to inadequate pain relief or side effects between day 7 and day 28, while five patients died between day 28 and day 56. Constipation, nausea and vomiting were the most common side effects. Skin reaction was relatively mild and acceptable during the study. CONCLUSION: Under controlled conditions, TTS fentanyl seems to be feasible for direct conversion from mild to strong opioids and additionally, 25 microg/hour incremental steps day by day can be made by palliative care specialists, if clinically required for cancer pain management.

Administration, Cutaneous↗

PubMed1975

Gas chromatographic/thin-layer chromatographic analysis of acetylated codeine and morphine in urine.

This procedure positively identifies codeine and morphine in urine. Urine samples are hydrolyzed and extracted with organic solvent, and the extracts are evaporated and acetylated. The presence of codeine and morphine is ascertained by gas chromatography (3% OV-25 and 3% Poly-A 103 columns) and confirmed by thin-layer chromatography (system: ethyl acetate/acetone/concd ammonium hydroxide, 100/10/4.5 by vol; reagent: iodoplatinate). As little as 0.5 mg each of codeine and morphine per liter, in free and conjugated forms, is detectable by this method.

Acetylation↗

PubMed2001

Ibuprofen versus acetaminophen with codeine for the relief of perineal pain after childbirth: a randomized controlled trial.

BACKGROUND: Pain from episiotomy or tearing of perineal tissues during childbirth is often poorly treated and may be severe. This randomized double-blind controlled trial was performed to compare the effectiveness, side effects and cost of, and patient preference for, 2 analgesics for the management of postpartum perineal pain. METHODS: A total of 237 women who gave birth vaginally with episiotomy or a third- or fourth-degree tear between August 1995 and November 1996 at a tertiary-level teaching and referral centre for obstetric care in Vancouver were randomly assigned to receive either ibuprofen (400 mg) (n = 127) or acetaminophen (600 mg) with codeine (60 mg) and caffeine (15 mg) (Tylenol No. 3) (n = 110), both given orally every 4 hours as necessary. Pain ratings were recorded before the first dose and at 1, 2, 3, 4, 12 and 24 hours after the first dose on a 10-cm visual analogue scale. Side effects and overall opinion were assessed at 24 hours. RESULTS: Ibuprofen and acetaminophen with codeine had similar analgesic properties in the first 24 hours post partum (mean pain rating 3.4 and 3.3, mean number of doses in 24 hours 3.4 and 3.3, and proportion of treatment failures 13.8% [16/116] and 16.0% [16/100] respectively). Significantly fewer subjects in the ibuprofen group than in the acetaminophen with codeine group experienced side effects (52.4% v. 71.7%) (p = 0.006). There were no significant differences in overall patient satisfaction between the 2 groups. The major determinant of pain intensity was forceps-assisted delivery. Overall, 78% of the treatment failures were in women with forceps-assisted deliveries. INTERPRETATION: Since the 2 analgesics were rated similarly, ibuprofen may be the preferred choice because it is less expensive and requires less nursing time to dispense. Further studies need to address improved analgesia for women with forceps-assisted deliveries.

Acetaminophen↗