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PubMed1992

Ibuprofen plus codeine, ibuprofen, and placebo in a single- and multidose cross-over comparison for coxarthrosis pain.

The analgesic efficacy of 200 mg ibuprofen plus 30 mg codeine, 200 mg ibuprofen and placebo was investigated in a new analgesic evaluation model using single- and repeated-dose administration. The study was a double-blind randomized cross-over investigation in 26 coxarthrosis patients with persistent pain. After a washout period of at least 2 days with paracetamol available as rescue analgesic, each of the 3 treatments was administered in a total of 6 doses during 24 h. The hourly pain intensity was recorded on a 100-mm visual analogue scale (VAS) for 8 h after the 1st and the 6th dose. The pretreatment VAS score was 31-37 mm. After the 1st dose the 8-h mean pain intensity values were 25, 27, and 26 mm after ibuprofen plus codeine, ibuprofen, and placebo, respectively. Following another 5 doses every 4 h the corresponding values were 10, 17 and 29 mm. Repeated administration of both active drugs reduced the pain intensity significantly. The analgesic efficacy of ibuprofen plus codeine was significantly superior to that of ibuprofen which was, in turn, superior to that of placebo. In conclusion, analgesic efficacy was better differentiated after repeated-dose than after single-dose administration. The present study design was able to differentiate between 200 mg ibuprofen plus 30 mg codeine and 200 mg ibuprofen alone in a relatively small number of patients.

Adult↗

PubMed1990

Dose-response inhibition of rat compound nerve action potential by dextropropoxyphene and codeine compared to morphine and cocaine in vitro.

1. The effects of dextropropoxyphene hydrochloride (dextropropoxyphene) codeine phosphate (codeine), morphine hydrochloride (morphine), and cocaine hydrochloride (cocaine) on the compound action potentials (cAP) of the rat phrenic nerve were studied in vitro. 2. Dextropropoxyphene, cocaine, codeine and morphine depressed the cAP in a reversible, dose-dependent way. After 60 min exposure to the drugs, dextropropoxyphene, inhibited the cAP between 0.025 and 0.5 mM, cocaine between 0.01 and 5 mM, codeine between 0.1 and 10 mM and morphine between 0.5 and 70 mM. The inhibition caused by 5 mM morphine could not be reversed by naloxone. 3. Dextropropoxyphene demonstrated the most potent cAP inhibition compared to the other drugs tested. The observed dose range for the inhibition of the cAP of rat phrenic nerve includes that observed after intoxications with dextropropoxyphene (0.004-0.06 mM) in the clinic. 4. For all other drugs tested the present observed dose ranges are much greater than the plasma concentrations previously reported after therapeutic use and intoxication.

Action Potentials↗

PubMed1988

Excessive grooming induced by the administration of codeine and morphine.

Previous studies have shown that peripheral injections of the codeinone RX 336-M can induce excessive grooming in rats in an age-dependent fashion. The present experiment demonstrates that codeine, itself, also induces excessive grooming but with apparent equal effectiveness at all ages tested. Because of the structural similarity between codeine and morphine, the effects of intraperitoneally administered morphine were examined as well. Morphine was found to produce a temporal course of excessive grooming quite different from that produced by codeine. Morphine did not affect grooming in the first half (30 min) of the observation period, but accentuated it, briefly, for the next 30-45 min. Intraventricular administration of codeine at doses of 0.3 or 1.0 microgram/3 microliter had no effect on grooming in animals previously shown to demonstrate excessive grooming in response to either dose.

Aging↗

PubMed1991

Hydrocodone versus codeine in acute musculoskeletal pain.

STUDY OBJECTIVES: To evaluate the efficacy and prevalence of side effects of hydrocodone versus codeine in acute pain syndromes. TYPE OF PARTICIPANTS/SETTING: Sixty-two consecutive adult emergency department patients 18 to 70 years old with acute musculoskeletal pain. Patients using other analgesics or having any contraindication to opioid therapy were excluded. In addition, 12 patients were excluded because of insufficient data or study dropout. DESIGN/INTERVENTIONS: In a randomized, double-blind prospective manner, patients received either 5 mg hydrocodone with 500 mg acetaminophen or 30 mg codeine with 500 mg acetaminophen to take on discharge from the ED and every four hours thereafter as needed for pain. MEASUREMENTS: Pain intensity was evaluated by a visual analog scale at zero, one, two, four, eight, 24, and 48 hours. Specific side effects were sought, along with the number of patients reporting inadequate analgesia. MAIN RESULTS: Data were obtained on 50 subjects (25 per group). Mean and median pain scores did not differ significantly at time zero (x vs y, 6.03 vs 5.99 and 6.8 vs 6.1, respectively) or subsequent intervals. Side effects were noted in eight hydrocodone/acetaminophen and 18 codeine/acetaminophen patients (P = .005). No significant differences in gastrointestinal side effects were reported; however, less nausea or vomiting was reported in the hydrocodone group (P = .23). Central nervous system side effects (sedation or lightheadedness) were reported in six hydrocodone/acetaminophen patients compared with 16 codeine/acetaminophen patients (P less than .005). In addition, no hydrocodone/acetaminophen patients reported inadequate analgesia compared with six codeine/acetaminophen patients (P less than .05). CONCLUSION: Although pain scores were not significantly different, hydrocodone may be a more effective analgesic than codeine in acute musculoskeletal pain, as demonstrated by significantly fewer treatment failures. Central nervous system side effects are less common with hydrocodone than with codeine.

Acetaminophen↗

PubMed1975

Synthesis of thebaine and oripavine from codeine and morphine.

A practical synthesis of thebaine and oripavine has been developed from codeine and morphine, respectively. Attempts to use a codeinone intermediate gave poor yields; however, methylation of the potassium salt of codeine to give codeine methyl ether followed by oxidation with gamma-MnO2 gave thebaine in 67% yield from codeine. Similarly, the potassium salt of the di-O-anion of morphine was selectively alkylated to give morphine 6-methyl ether (heterocodeine) in better than 90% yield. Hetercodeine was then acetylated and oxidized to oripavine 3-acetate which was hydrolyzed to give oripavine in 73% yield from morphine.

Codeine↗

PubMed1987

The additive analgesic efficacy of acetaminophen, 1000 mg, and codeine, 60 mg, in dental pain.

In a double-blind, randomized, single-dose trial the analgesic contribution of acetaminophen, 1000 mg, and codeine, 60 mg, was determined. The study was a 2 X 2 factorial experiment in which 120 patients suffering from pain as a result of oral surgery rated their pain intensity and pain relief for up to 5 hours after a single dose of one of: 1000 mg acetaminophen, 60 mg codeine, 1000 mg acetaminophen plus 60 mg codeine, or placebo. The factorial analysis showed that both 1000 mg acetaminophen and 60 mg codeine made a statistically significant (P less than 0.05) contribution to the analgesic effectiveness of the combination on all measures of efficacy (sum of pain intensity differences, largest pain intensity difference, total pain relief, largest pain relief, and time to remedication). The incidence of adverse effects did not appear to differ among the treatments, including placebo.

Acetaminophen↗

PubMed1988

Association of pain relief with drug side effects in postherpetic neuralgia: a single-dose study of clonidine, codeine, ibuprofen, and placebo.

In a randomized, double-blind crossover study, 40 patients with postherpetic neuralgia were given single oral doses of clonidine, 0.2 mg, codeine, 120 mg, ibuprofen, 800 mg, or inert placebo. Pain relief and side effects were recorded for 6 hours. Patients reported significantly more relief after clonidine than after the other three treatments. Codeine and ibuprofen were ineffective. Sedation, dizziness, and other side effects were more frequent after clonidine (74%) or codeine (69%) than after placebo (36%) or ibuprofen (28%). Reported pain relief was greater during trials in which side effects were present. A single, mild side effect was associated with as much additional pain relief as multiple, severe side effects. Clonidine's superiority to codeine, which had a similar incidence of side effects, argues for a specific analgesic effect. In addition, side effects may have contributed to clonidine analgesia, perhaps by suggesting to patients that they had received a potent drug.

Aged↗

PubMed1988

Analgesic effect of picenadol, codeine, and placebo in patients with postoperative pain.

A double-blind, parallel study was conducted to evaluate the analgesic effect and safety of a single 25 mg oral dose of picenadol, a centrally acting analgesic, and to compare it with a 60 mg dose of codeine and a placebo in patients with postoperative pain. Two sites using similar protocols enrolled a total of 178 inpatients with postoperative pain. Pain intensity, relief, and adverse experiences were then measured for up to 6 hours after administration of the test medications. Both picenadol and codeine were significantly more effective than placebo in reducing pain intensity (mean sum of pain intensity difference scores: picenadol 5.21, codeine 5.19, and placebo 2.82) and increasing total relief (mean total pain relief: picenadol 10.21, codeine 11.07, and placebo 6.96). Adverse experience profiles were similar among the three treatment groups.

Adult↗

PubMed1992

Opioid analgesics and the risk of hip fracture in the elderly: codeine and propoxyphene.

We studied the risk of hip fracture in elderly persons receiving prescriptions for two commonly prescribed opioid analgesics--codeine and propoxyphene. Using automated prescription and hospitalization data, we identified 4,500 residents of Saskatchewan, Canada, aged 65 or older, who sustained a hip fracture between 1977 and 1985, and 24,041 age- and sex-matched controls. Compared to nonusers, the relative risk (95% CI) of hip fracture in current users of codeine or propoxyphene was 1.6 (1.4-1.9). There was no difference between relative risks of fracture among current users of codeine [1.6 (1.3-1.9)] and propoxyphene [1.6 (1.2-2.2)]. In new users of these opioids, the relative risk of fracture was 2.2 (1.7-2.8), compared to 1.3 (1.0-1.6) in users who received at least one additional prescription for codeine or propoxyphene in the 90-day period prior to the index date. Concurrent users of these opioids and psychotropic drugs (sedatives, antidepressants, or antipsychotics) had a risk of fracture 2.6 (2.0-3.4) times that of nonusers of either drug class. Review of a sample of medical records for 701 cases suggested this finding was not due to confounding by body mass, ambulatory status, functional status, or dementia. Given the essential role of opioids in the management of pain in geriatric practice, further study is needed to determine the psychomotor effects of opioid analgesics in older adults.

Age Factors↗

PubMedDate not supplied

Comparison of derivatives for determination of codeine and morphine by gas chromatography/mass spectrometry.

Pentafluoropropionic anhydride (PFPA) and heptafluorobutyric anhydride (HFBA) derivatives of morphine and codeine demonstrated poor spectra due to low abundances of secondary and tertiary ions. Trifluoroacetamide (MBTFA) has been a widely used derivative; however, the internal standard, nalorphine, displayed very poor stability and this resulted in split peaks by gas chromatography making MBTFA unsuitable for quantitative methods. Quantitation of codeine and morphine using bis-trimethylsilyltrifluoroacetamide (BSTFA/1%TMS) revealed a significant gradual decrease (p less than 0.05) of peak area ratio (PAR) of codeine and morphine compared to the internal standard using selected ion monitoring (SIM). The acetic anhydride derivative showed no significant differences in the peak area ratios for codeine/IS over a period of 24 hours, although the coefficient of variation (CV) was higher for the acetyl derivative than for the TMS derivative of codeine. There was a significant difference associated with the acetyl derivative of morphine at 4 h post derivatization compared to the initial injection (p less than 0.05); however, the acetyl derivative was stable for 24 hours and had a CV of less than 10% at a cutoff of 300 ng/mL.

Acetamides↗

PubMedDate not supplied

Simultaneous identification and quantitation of codeine and morphine in urine by capillary gas chromatography and mass spectroscopy.

An analytical procedure for simultaneous determination of codeine and morphine in urine is described. The detection of codeine and morphine is based on liquid-liquid extraction and derivatization to the acetylated compounds. The acetylated codeine and morphine are separated by capillary gas chromatography and identified mass spectrometrically by selected ion monitoring (SIM). Quantitative determination was carried out by SIM using nalorphine as internal standard. Excellent linearity was obtained over a concentration range of 25 to 800 ng/mL. The overall recovery for codeine and morphine in the extraction was found to be 58% and 40%, respectively. The on-column sensitivity for both compounds was 2 ng at a peak-to-noise ratio of 5:1. The derivatives, acetylcodeine, diacetylmorphine, and diacetylnalorphine were stable at room temperature for 72 hr.

Codeine↗

PubMed1990

The effects of codeine on human aggressive responding.

Ten healthy male research subjects received placebo, 25, 50 and 75 mg/70 kg of codeine in a controlled laboratory setting. During each session subjects had two response options. The non-aggressive response option was maintained by points exchangeable for ten cents. The aggressive response option ostensibly subtracted a point from the subject's fictitious partner. Aggressive responding was engendered by point subtractions attributed to a fictitious partner. Codeine did not significantly alter the frequency of monetarily reinforced, nonaggressive, responding. Aggressive responding was significantly increased at the 50 mg/70 kg dose of codeine. The frequency of aggressive responses during the placebo sessions preceding administration of the first codeine dose were significantly and positively correlated with scores on the Buss-Durkee Hostility Scale. Aggressive responding increased for four of five subjects scoring below the median on the Buss-Durkee Hostility Scale at the 50 mg/70 kg dose; while administration of 50 mg/70 kg increased aggressive responding of one subject who scored above the median. Aggressive responding for both groups of subjects was unaffected by the 75 mg/70 kg dose.

Administration, Oral↗

PubMed1975

The effect of codeine phosphate on the absorption of ethyl alcohol.

The effect of syrup, B.P. and codeine phosphate syrup, B.P.C. on blood alcohol levels was determined in six normal subjects. 2 Treatment with syrup alone had little or no influence on the concentration of ethanol in blood. 3 In contrast, pretreatment with codeine phosphate syrup significantly reduced alcohol absorption, as assessed by the maximum blood levels achieved or the area subtended by the blood concentration-time curve. It is suggested that the diminished absorption of ethanol is related to the pharmacological action of codeine on the stomach. 4 It was considered that the concentration of ethanol in linctuses or syrups containing codeine was unlikely to have any significant effect on the central nervous system.

Codeine↗

PubMed1983

Effects of codeine on the respiratory responses to exercise in healthy subjects.

In six healthy subjects, respiration and the sensation of breathlessness were assessed during submaximal exercise and the subsequent recovery. The overall responses were expressed by the relationship of breathlessness to minute volume. Because of the high subjective component in the assessments, validation of the method in these particular subjects was an integral part of the study. The relationship of breathlessness to ventilation during identical periods of exercise was highly reproducible and sensitivity was demonstrated by an alteration in this relationship in the presence of an inspiratory resistance. Codeine at a dose of 60 mg by mouth was compared with placebo, each treatment being given on two occasions. The study was conducted in a double-blind fashion with randomization of the order of treatments. Codeine at this dose allowed higher levels of carbon dioxide to be tolerated during breath-holding; oxygen uptakes at rest and during exercise were unaffected. Ventilation and breathlessness at the end of exercise were each slightly but significantly reduced by codeine but the relationship between breathlessness and ventilation was not changed. Codeine did not prevent detection of an inspiratory resistance.

Adult↗

PubMed1989

Interindividual and interethnic differences in the demethylation and glucuronidation of codeine.

1. The 8 h urinary excretion of codeine and seven of its metabolites was compared in 149 healthy Swedish Caucasians and 133 healthy Chinese following a single oral dose of 25 mg codeine phosphate. 2. The total 8 h urinary recovery of drug-related material was 74 +/- 24% in the Caucasians and 60 +/- 14% in the Chinese (P less than 0.001). The excretion of unchanged codeine was significantly higher in the Chinese (7.2%) compared with the Caucasians (4.3%, P less than 0.001). 3. The Caucasians excreted significantly greater proportions of codeine-6-glucuronide (C6G) (62%) than the Chinese (44%) (P less than 0.001). The frequency distribution of the log metabolic ratio (MR) for glucuronidation (codeine/C6G) was shifted towards higher values in the Chinese population. Males in both groups and Chinese smokers had significantly lower glucuronidation MRs than females and non-smokers in the respective populations (P less than 0.001). 4. The frequency distribution of the MR for O-demethylation (codeine/morphine (M) + M-3 and M-6-glucuronide (M3G and M6G) + normorphine (NM) was highly skewed in the Caucasians, suggestive of a bimodal distribution. There was a 160-fold interindividual variation in this MR. A unimodal distribution of the log O-demethylation MR was observed in Chinese. The Caucasians excreted less M and more M6G than did the Chinese (P less than 0.001). 5. Significantly more norcodeine (NC) and less NC-glucuronide (NCG) were excreted in the Chinese compared with the Caucasians (P less than 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗

PubMed1984

Effects of cromolyn on codeine-induced histamine release in vivo.

Cromolyn has been shown to inhibit histamine release from mast cells induced by various stimuli in vitro. However, the local effects of cromolyn on codeine-induced wheal and flare skin reactions are not well understood. Intradermal injection of codeine induced prominent whealing in almost all humans. We studied the effect of local cromolyn injection on codeine-induced skin reactions, histamine release, and ultramicroscopic changes in mast cells in 10 volunteers. The finding in this study showed that injection of a 2% cromolyn solution before or together with the codeine injection does not affect the subsequent skin reactions, histamine release and ultramicroscopic changes of mast cells.

Codeine↗

PubMed1977

Simultaneous determination of codeine and morphine in biological samples by gas chromatography with electron capture detection.

A sensitive gas chromatographic method for the simultaneous determination of codeine and morphine in plasma and brain samples is described. The method involves solvent extraction of the compounds from plasma, derivatization with pentafluoropropionic anhydride and subsequent separation on a 3% OV-17 column. The quantification is performed with electron capture detection. The sensitivity of the method (0.75 ng of morphine and 7.5 ng of codeine in a sample) makes it especially useful for pharmacokinetic investigations. The method was successfully applied to determine the time course of codeine and its metabolite morphine after intravenous administration of codeine to the rat.

Animals↗

PubMed1972

Blood-brain barrier: penetration of morphine, codeine, heroin, and methadone after carotid injection.

Labeled morphine, codeine, heroin, or methadone was injected as a bolus into the common carotid artery of the rat, and the rat was decapitated 15 seconds later. The brain uptake of the drug was calculated by measurement of the brain content of the drug as a percentage of a labeled, highly diffusible reference substance simultaneously injected. The uptake of morphine was below measurability; the uptake of codeine was 24 percent; heroin, 68 percent; and methadone, 42 percent. Brain uptakes of morphine and codeine were also studied after intravenous injection and correlated well with uptakes after carotid injection; the uptake of codeine being nearly complete by 30 seconds. These studies indicate that brain uptake of certain of these drugs is very rapid and that uptake of heroin injected intravenously is probably limited by the regional flow of blood in the brain. The possible relation of this rapid penetration of the blood-brain barrier by heroin to its strongly addictive properties is discussed.

Animals↗