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At least 703 records · Page 39Linked to original sources
PubMed1985

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

In a double-blind, single-dose study, the analgesic effect of a combined ibuprofen-codeine phosphate preparation was compared with those of zomepirac and placebo in 127 patients with moderate or severe postepisiotomy pain. Both the combination and zomepirac were significantly more effective than placebo for up to six hours, but the onset of action of the combination was more rapid than that of zomepirac. The study was notable for the virtual absence of side effects.

Adult↗
PubMed1985

Dose response to fenoprofen calcium using placebo and codeine as controls.

This paper evaluates the dose-response relationship of several doses of fenoprofen calcium, between 12.5 and 300 mg, and their relationship to 60 mg of codeine sulfate and placebo. Three separate parallel studies are included in this evaluation, including a total of 867 patients. The types of pain were cesarean section, episiotomy wound, uterine cramping, and general surgery. This paper shows that a significant increasing relationship exists between efficacy and dose of fenoprofen, suggesting that relatively larger doses of fenoprofen will achieve greater amounts of efficacy.

Cesarean Section↗
PubMedDate not supplied

Acute psychosis associated with codeine and acetaminophen: a case report.

A twenty-year-old white male subject without a history of psychiatric disorder developed hallucinations and paranoid symptoms following ingestion of 540 mg codeine over a period of 36 hr. The symptoms reached an intensity where hospitalization became necessary but no specific treatment was required. In less than 72 hr, the patient completely recovered from his symptoms and was subsequently discharged. In view of the available data on the neurochemical effects of opiates and non-narcotic analgesics, it was concluded that inhibition of prostaglandin biosynthesis or interference with its action might have caused the psychotic symptoms reported.

Acetaminophen↗
PubMedDate not supplied

Spectrophotometric analysis of mixtures of acetaminophen, salicylamide, and codeine phosphate in tablets.

A simple and accurate spectrophotometric procedure for the analysis of a mixture of acetaminophen, salicylamide, and codeine phosphate is described. Determination of the first 2 components depends on pH-induced differential spectral changes of their nitroso derivatives. The third component is assayed by the acid dye method. The proposed procedure was successfully applied to the analysis of laboratory-made and commercial tablets containing the ternary drug mixture.

Acetaminophen↗
PubMedDate not supplied

Studies of the metabolic N- and O-demethylation of [6-3H]codeine.

We have modified our radiometric assay for ethylmorphine N-demethylase to examine the metabolism of codeine. We find that the current assay gives excellent separation of metabolites with a zero time activity of 0.08%. The N- and O-demethylations are linear for up to 30 min with up to 1 mg/ml of microsomal protein. The pH profiles show slightly different maxima (N-demethylation, pH 8.0; O-demethylation, pH 7.8). The kinetic parameters for N-demethylation were markedly higher (Vmax = 5.6 nmol/min/mg protein; KM = 714 microM) than those for O-demethylase (Vmax = 0.75 nmol/min/mg protein; KM = 149 microM). These data suggest that the HCHO results primarily from the N-demethylase. Further, the differences in the kinetic parameters and the pH profile suggest that these two activities are catalyzed by different enzymatic systems.

Animals↗
PubMed1983

Ciramadol--a new synthetic analgesic. A double-blind comparison with oral codeine for postoperative pain relief.

One hundred and eighty patients (American Society of Anesthesiologists rating 1-2) received one of three oral analgesics--ciramadol (Wy. 15705) 20 mg, ciramadol 60 mg or codeine 60 mg--on a double-blind random basis for the relief of pain 24-48 hours after major general surgical, gynaecological or orthopaedic operations. All three analgesics proved equally effective and caused mild sedation only. No patient showed signs of clinical cardiorespiratory depression, and other side-effects were infrequent. Ciramadol may therefore prove a useful clinical alternative to conventional oral analgesics provided its lack of respiratory depressant properties and addiction potential in monkeys can be substantiated in humans.

Adolescent↗
PubMed1984

The pharmacokinetics of meprobamate following its oral and rectal administration as a series of combinations with diphenhydramine, acetylsalicylic acid, codeine and pentaerythritol tetranitrate.

Studies in human volunteers of the pharmacokinetics of the active drugs in the formulations Visano-mini (meprobamate and diphenhydramine HCl), DoloVisano (meprobamate, diphenhydramine HCl, acetylsalicylic acid and codeine phosphate) and VisanoCor (meprobamate, diphenhydramine HCl and pentaerythritol tetranitrate (PETN], have demonstrated systemic absorption of each of the drugs from all of the formulations. Bioequivalence of meprobamate is indicated despite the drug combinations involved. Some differences in diphenhydramine pharmacokinetics are, however, apparent. The bioavailability of meprobamate administered rectally to human volunteers as the marketed preparations DoloVisano Suppositories and Dolo-Visano Suppositories sine codeino, is similar to that observed following oral administration.

Administration, Oral↗
PubMed1980

"In vivo", effectivity of codeine sulfate on the meiotic chromosomes of Saccobranchus fossilis.

Codeine sulfate which is obtained from opium or made by methylating morphine has been found to induce a number of anomalies in the meiotic chromosomes of S. fossilis. Feulgen technique was undertaken for experimental studies. At high doses abnormal metaphases, agglutination, achromatic lesions, some breaks and chromosomal scattering were evident. However, the frequency of abnormal metaphases was high amongst the rearrangements. The susceptibility of meiotic metaphase during peak period of breeding is indicative of inhibition in the division activity.

Animals↗
PubMed1997

Abuse of codeine-containing cough syrups: a report from India.

AIM: To study the socio-demographic and clinical profile of patients seeking treatment for abuse of codeine-containing cough syrups (CCS). DESIGN: Observational; case series. SETTING: An addiction clinic in North India. PARTICIPANTS: Forty-six consecutive treatment-seeking patients of DSM-III-R-diagnosed dependence on CCS, from January 1994 to June 1995. MEASUREMENTS: Semi-structured interview schedule for patients and their family covering socio-demographic and clinical variables. FINDINGS: All patients were male. Many were young (mean age 27 years), with completed school education (85%) and from urban backgrounds (80%). The mean age of starting CCS use was 23 years. Initiated commonly through friends (89%) and often for curiosity (63%), 89% of the patients progressed to daily use of CCS in less than 6 months (54% in less than a month), and in quantities much higher than prescribed limits. Opioid-like withdrawal was reported by 92%. Concurrent use of other substances, psychiatric co-morbidity and HIV-related risk behaviour were present in 72%, 24% and 45%, respectively. Most of the patients reported a 'stimulant' effect of CCS ('alert', 96%; 'more active', 94%). CONCLUSIONS: The combination of an opioid and a sympathomimetic agent in the CCS may cause a special, distinct euphoretic effect. This effect, along with the low price, easy availability and 'pure' preparation of CCS, may be responsible for the rapidly rising popularity of the CCS as drugs of abuse in India.

Adolescent↗
PubMed1976

[Teratologic studies in rabbits and rats with the morphine derivative codeine (author's transl)].

Codeine was administered to rabbits and rats during the organogenetic phase (days 6--18 and 6--15, resp.) in oral doses of 5, 12.5 and 30 mg/kg and 10, 35 and 120 mg/kg, resp. The tests in rabbits yielded no indication of a teratogenic or embryolethal action of the substance under investigation. Even in the experiments on rats no teratogenicity could be realised. The highest dose of 120 mg/kg led to an increased mortality of rat embryos around the time of implantation. As this dose was toxic even to adult rats the described experiments give no indication of an increased risk during pregnancy.

Animals↗
PubMed1995

Ethylmorphine O-deethylation in isolated rat hepatocytes. Involvement of codeine O-demethylation enzyme systems.

The O-dealkylation of ethylmorphine (EM) and codeine (CD) to morphine (M) co-segregates with debrisoquine/sparteine genetic polymorphism in man. CD O-demethylation is catalysed by cytochrome P450 2D1 (CYP2D1) in rats. In the present study, the O-deethylation of EM was examined and compared with that of CD in suspensions of freshly-isolated hepatocytes prepared by a collagenase method from Wistar rats with and without CYP2D1 inhibitors. Isolated hepatocytes were also prepared from Dark Agouti (DA) rats deficient in CYP2D1, and were incubated with EM or CD. EM, CD and their metabolites were quantified by HPLC with UV detection. EM had a similar pattern of metabolism to that of CD in suspensions of hepatocytes from Wistar rats. Both EM and CD were O-dealkylated to form M plus morphine-3-glucuronide (M3G) and N-demethylated to form norethylmorphine (NEM) or norcodeine (NCD), respectively, which were further metabolized to normorphine (NM) and finally glucuronidated to normorphine-3-glucuronide (NM3G). As compared to hepatocytes from Wistar rats, DA rats were characterized by a markedly decreased formation (70 approximately 75% reduction) of M plus M3G from both EM and CD. Quinine, quinidine, propafenone and sparteine all inhibited EM O-deethylation as well as CD O-demethylation. Quinine was the most potent inhibitor of both these O-dealkylations (Ki = 0.2 microM for both EM and CD, respectively). Quinine as well as the other inhibitors inhibited both EM and CD O-dealkylation competitively and with small differences in Ki versus EM and CD, respectively. The metabolism of EM to M plus M3G and that of CD to M plus M3G was highly correlated when results from the various separate cell suspensions were plotted. In conclusion all findings indicated that the enzyme responsible for O-demethylation of CD, CYP2D1 was also responsible for the O-deethylation of EM to M.

Animals↗
PubMed1991

A clinical study on the use of codeine, oxycodone, dextropropoxyphene, buprenorphine, and pentazocine in cancer pain.

The authors report a prospective study on 944 cancer pain patients treated with one of the following opioids: codeine, oxycodone, dextropropoxyphene, buprenorphine, and pentazocine. Level of analgesia, duration of treatment, side effects, and drop out were evaluated for each drug. Twenty-four percent of the patients still benefitted from treatment at the fourth week of study, even if high drug dosages were not used. Pentazocine did not show an evident analgesic effect during the first 2 wk of treatment. The other opioids were found to be valid therapeutic instruments for chronic cancer pain control in a limited number of patients.

Adult↗
PubMedDate not supplied

Confirmation of marijuana, cocaine, morphine, codeine, amphetamine, methamphetamine, phencyclidine by GC/MS in urine following immunoassay screening.

Rapid, reliable, sensitive, qualitative, and quantitative methods using small urine volumes (0.2-0.5 mL) were developed primarily for confirmation of marijuana, cocaine, benzoylecgonine, ecgonine methyl ester, morphine, codeine, amphetamine, methamphetamine, and phencyclidine. Using capillary gas chromatography/mass spectrometry (GC/MS) and selected ion monitoring (SIM), mass spectra were obtained for each analyte. Samples were prepared by hydrolysis where applicable, organic solvent extraction, and derivatization where necessary. Confirmation was achieved by comparing abundance of major ions and retention time of the total ion current (TIC) of an analyte with those of the appropriate analytical standard. Quantitation was achieved and calibration curves derived by obtaining the molecular ion ratios of that analyte/internal standard (IS) over a concentration range of 10-300 ng/mL (0.16-4.0 ng total injected into GC/MS). The overall extraction efficiency for these analytes ranged from 53% to 96%. Statistically significant cut-off values (p less than 0.01) were obtained for each analyte. The slope, y-intercept, and coefficient of determination (r2) were calculated for each analyte. All of the GC/MS methods were extensively tested against urine samples determined positive or negative by immunoassay (IA) and are now used in our laboratory.

Amphetamine↗
PubMed1991

[Assessment of the intake of opiates (heroin, morphine, codeine and ethylmorphine) by the analysis of intermediate metabolites in the urine: which are the criteria to adopt?].

This report presents the different strategies for identifying heroin users. The criteria allowing a clear distinction between an abuse of heroin and a lawful consumption of opiates are deeply discussed. Reliable and sensitive analytical methods are now available for forensic opiate testing. The detection of 6-mono-acetylmorphine (MAM) indicates that heroin was administered within 24 hours or less of specimen collection. In the absence of MAM or after consumption of several opiates, the relative ratios of morphine, codeine and eventually ethylmorphine must be known in order to determine which opiate(s) was (were) taken. A total amount of opiates of less than 0.3 mg/l very often precludes any characterization of the ingested drug(s). Here we have to point out that forensic opiate testing should be done carefully. Interpretation of results requires more than detection of opiates or morphine alone, irrespective of the number of techniques used.

Forensic Medicine↗