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At least 1,333 records · Page 74Linked to original sources
PubMed1983

[Experience with suprofen for acute and chronic pain in neurologic practice].

A single-dose, double-blind study included a total of 196 patients with neurologic pain. The subjects were subdivided into five groups and treated with alpha-methyl-4-(2-thienylcarbonyl) benzene acetic acid (suprofen, Suprol) 400 mg; suprofen 200 mg acetylsalicylic acid (ASA) 650 mg; ASA 650 plus codeine 60 mg; and placebo. The population was homogeneous as to age, sex, and body weight. About 95% of the patients rated the intensity of pain severe prior to treatment. The clinical effect was appreciated by investigator and patients after up to 6 h following administration of the single dose. It was demonstrated that the active substances all were significantly superior to placebo in all criteria tested. Statistical analysis of the parameters investigated revealed the following order of effectiveness of the test medications: Suprofen 400 and 200, respectively, = ASA 650 + codeine 60 greater than ASA 650 greater than placebo. The final overall patients appreciation of effectiveness showed good to very good results in 97.4% of the patients on suprofen 400; 65% of those on suprofen 200; 72.5% of those on ASA 650 + codeine 60; 13.5% of those on ASA 650; and 7.5% of those on placebo. During the treatment 26 patients experienced adverse reactions; of these, 18 subjects on ASA 650 + codeine 60 complained of fatigue or somnolence as the side effect experienced most frequently.

Acute Disease↗
PubMed1976

Unfavorable effect of atropine-diphenoxylate (Lomotil) therapy in lincomycin-caused diarrhea.

In this double-blind, randomized study, 200 normal subjects received a three-day course of one of five treatment regimens: lincomycin hydrochloride monohydrate injection (sterile solution, 300 mg/ml) with two tablets of either placebo, a mixture of atropine sulfate and diphenoxylate hydrochloride (Lomotil), an aspirin-phenacetin-caffeine (APC) combination or the latter with codeine, or an injection of saline with two placebo tablets. Gastrointestinal irritation was most prominent in subjects receiving lincomycin with atropine-diphenoxylate and lincomycin with APC plus codeine (P less than .05). Decreased intestinal motility from atropine-diphenoxylate or codeine may increase the contact time between the lincomycin (or its metabolites) or some developing toxic substances and the mucosal epithelium. The use of atropine-diphenoxylate or codeine in treating lincomycin-induced diarrhea may be questionable.

Administration, Oral↗
PubMed1978

Effect of benzopyranoperidine, a delta-9-THC congener, on pain.

In a double-blind, 5-way crossover designed study, single doses of placebo, 2 doses of codeine sulfate (60 and 120 mg), and 2 doses of benzopyranoperidine (2 and 4 mg) were administered orally to 35 patients who required analgesics for chronic pain due to malignancies. Benzopyranopyridine is an analogue of delta-9-tetrahydrocannabinol and was chosen on the basis of its sedative, hypnotic, and analgesic properties in animals. Pain relief scores indicated a degree of relief of clinical significance with 120 mg of codeine but no consistent difference between placebo and any other active agent. On the basis of the data, bezopyranoperidine (2 or 4 mg) is not as effective as codeine (120 mg or 60 mg) and not more effective than placebo in relieving pain due to cancer; indeed, pain perception appeared to be augmented by both doses.

Adult↗
PubMed2003

Application of capillary zone electrophoresis in the separation and determination of the principal gum opium alkaloids.

We describe the use of capillary zone electrophoresis (CZE) for the qualitative and quantitative determination of major alkaloids (i.e., thebaine, codeine, morphine, papavarine and narcotine) in gum opium involving the analysis of alkaloids without derivatization or purification. Three extractions with 2.5% w/v aqueous acetic acid quantitatively extracted major alkaloids. The separation was carried out by CZE using a 7:3 mixture of methanol and sodium acetate (100 mM, pH 3.1) at a potential of 15 kV, with UV detection at 224 nm. Spiking of pure reference alkaloid standards in the opium extract was used for peak identification. The influences of buffer composition, pH and voltage on the separation of alkaloids were studied. The detection limit of each alkaloid dissolved in methanol was found to be 850 ng/mL (morphine), 450 ng/mL (thebaine), 500 ng/mL (codeine), 550 ng/mL (papaverine), and 500 ng/mL (narcotine) at an injection pressure of 300 mbar (injection volume, 4 nL) with a signal-to-noise ratio of 3:1. The external standard method was used for the quantification of alkaloids. The calibration plot was based on linear regression analysis. The relative standard deviation (RSD) for peak area and migration time was in the range of 1.03-3.56% and 0.34-0.69%, respectively. Percentage compositions (g%) of opium alkaloids in five gum opium samples were found to be in the range of 14.45-15.95 (morphine), 2.0-3.45 (codeine), 1.32-2.73 (thebaine), 0.92-2.37 (papavarine), and 3.85-5.77 (narcotine). The method developed is suitable for the routine analysis of major gum opium alkaloids in samples of forensic importance.

Acetic Acid↗
PubMed1980

Clinical effects of parenteral narcotics in hospitalized medical patients.

Of 38,221 hospitalized medical patients monitored by a drug surveillance program, 1821 (4.8 per cent) received morphine, 504 (1.3 per cent) received codeine, 493 (1.3 per cent) received papaveretum, 115 (0.3 per cent) received hydromorphone, and 101 (0.3 per cent) received methadone parenterally. Hydromorphone had an unusually high adverse reaction rate (18 per cent); therefore, it probably should not be used since other equally effective strong analgesics are available. Adverse reactions occurred in 2 per cent of papaveretum recipients, in 4 per cent of methadone and codeine recipients, and in 6 per cent of morphine recipients. Gastrointestinal reactions (primarily nausea, vomiting, and constipation) were most common. Central nervous system disturbances (primarily respiratory depression, drowsiness, and confusion) were second most common. Adverse reactions occurred more often with higher doses of morphine and codeine; the dose-response relationship could not be evaluated for the other three drugs. Life-threatening adverse reactions were reported in 28 patients. Respiratory depression was the most common life-threatening reaction. Most patients with these reactions were seriously ill, and many received other drugs that may have contributed to the event.

Codeine↗
PubMed1978

Biosynthesis of morphine alkaloids in Papaver bracteatum Lindl.

Administration of 1-3H-N-methyl-14C-(+/-)-reticuline to Papaver bracteatum gave good incorporation of carbon-14 into thebaine and a decrease in the tritium to carbon-14 ratio indicative of racemization. The incorporation of carbon-14 and the extent of tritium loss were the same whether reticuline was administered to the intact plant or to isolated leaves. Carrier dilution with cold codeine, codeinone, and morphine showed only insignificant incorporation of radioactivity into codeine and none at all into codeinone and morphine. When codeinone was administered to the living plant, it was converted to codeine rapidly and efficiently, but no O-demethylation to morphine could be detected. The experimental data indicate that the biosynthesis of thebaine in P. bracteatum proceeds by the same pathway as in the opium poppy. The limiting step in the sequence is the demethylation of the enol ether group of thebaine to neopinone.

Codeine↗
PubMed1995

Schistosoma mansoni: the presence and potential use of opiate-like substances.

The present study demonstrates that morphine- and codeine-like molecules are present in Schistosoma mansoni following HPLC separation and identification with an appropriate commercially available antibody. Furthermore, the endogenous material, corresponding to morphine, mimics authentic morphine in its ability to induce immunocyte rounding and immobility, an action that is naloxone sensitive. The codeine-like material is not found at high concentrations compared to the morphine-like material, indicating, as in mammals and Mytilus edulis, the potential rapid conversion of codeine to morphine. Coincubation with human leukocytes increases the endogenous level of this material in adult worms, indicating the presence of a positive feedback loop. Last, EDTA, a chelator of divalent cations, has a strong stimulating effect in the synthesis of morphine-like material by the worm as noted by higher levels of this material in its presence. Taken together, the results suggest that this parasite may utilize this immune downregulating molecule in its effort to escape host immunosurveillance as well as in inhibiting an immune response directed against itself.

Analgesics, Opioid↗
PubMed1985

[Methodology and interpretation of morphiate detection in urine samples].

In TLC screenings of 335 urine samples taken because of suspicion of heroin consumption, positive evidence of morphine was found in about 50% of the cases, which was confirmed without exception by gas chromatography-mass spectrometry. In 66% of the positive cases, morphine and codeine were found; in about 31% only morphine was found, and the median value of 0.4 mg/l free morphine and 1.0 mg/l conjugated morphine was considerably lower than in the whole collection of samples. Comparison of the codeine/morphine quotients (Q), especially the free bases, proves that the groups of heroin/morphine or codeine consumers can be distinctly differentiated. The critical conditions of the conjugated bases worked out by Dutt et al. (1983) proved to be right. Using the equation Qf less than 0.5 square root c, a boundary condition for the free flare bases can also be developed, which is dependent on the sum of the codeine and morphine concentrations and which proves heroin/morphine consumption with 98% certainty.

Codeine↗
PubMed1980

The influence of 5-HT receptor blocking agents on the behavioral effects of analgesics in rats.

The influence of methergoline, methysergide, mianserine, cyproheptadine, and pizotifen on catalepsy induced by morphine, codeine, and fentanyl, and antinociception induced by these three drugs and by pentazocine was studied in rats. Methergoline dose-dependently reduced catalepsy induced by these three drugs. Methysergide abolished only morphine catalepsy, while mianserine significantly reduced the effect of morphine and codeine. Cyprohepatide and pizotifen did not modify the cataleptic effect of the three analgesics used. Antinociceptive action of morphine, codeine, fentanyl, and pentazocine, measured by the hot plate method, was not influenced or changed differentially by any serotonin receptor blocking compounds. One may conclude that catalepsy induced by morphine is, in general, antagonized by serotonin receptor blockade, but this does not concern all narcotic analgesics. In the antinociceptive effects of drugs used, the serotonergic influence seems to play a less important role than in catalepsy.

Analgesics↗
PubMed1980

Zinc tannate salts of heroin, LAAM and hydromorphone attenuate opiate withdrawal syndrome.

The effects of long-acting narcotic agonist preparations on the severe withdrawal syndrome following abrupt cessation of daily injections of codeine phosphate were studied in rats. Twelve hours after the last codeine injections, one injection of either a high or low dose of the zinc tannate salt of heroin, levo-alpha-acetylmethadol (LAAM) or hydromorphone in slow-release vehicle (SRV) was administered. Body weight, core temperature and hyperirritability scores (Teiger, 1974) were recorded every 6 h for the next 3 days. With the exception of the group that received the lower dose of heroin zinc tannate, all drug-treated groups lost significantly less weight than the SRV controls. All rats injected with either LAAM or hydromorphone zinc tannate exhibited prolonged marked hyperthermia, but the low, the high dose heroin groups and the SRV groups showed no significant differences in diurnal temperature patterns. Rats treated with the narcotic agonists were generally less irritable, as indicated by lower Teiger scores. These results indicate that a single injection of heroin, LAAM or hydromorphone zinc tannate can ameliorate the characteristic and intense signs of abstinence following withdrawal from codeine.

Animals↗
PubMed1983

Visual analogue scale and the analysis of analgesic action.

A double-blind randomized trial was carried out in 90 male patients suffering from pain after meniscectomy. The patients received a single dose of paracetamol 1000 mg plus codeine 60 mg, paracetamol 1000 mg, codeine 60 mg, or placebo. The tablets were taken when needed after surgery and the postoperative pain was recorded on a visual analogue scale. Over a period of 4 h the efficacy of the drugs was calculated in terms of pain intensity, pain intensity difference and percentage pain reduction. The greatest effect was obtained in patients taking the paracetamol plus codeine combination. Statistical analysis was carried out by use both of parametric and non-parametric procedures. The results suggest that pain reduction is a valuable measurement of analgesic efficacy and that non-parametric assumptions are preferable in the statistical analysis of analgesic activity.

Acetaminophen↗
PubMed1987

Limitations of indirect methods of estimating small bowel transit in man.

Experiments were carried out in healthy volunteers to explore the utility of a new [14C]lactulose breath test for measuring small intestinal transit time in man and to use this procedure to test whether two antidiarrheal agents, codeine and clonidine, alter small intestinal transit time during digestion of a liquid meal. In an initial validation study performed in 12 subjects (three studies in each subject), a liquid test meal containing 10 g [14C]lactulose was administered and the colonic entry time estimated from the time course of 14CO2 excretion in breath compared with that of H2 excretion. There was a fair correlation (r = 0.77; P less than 0.001) between results obtained by the two methods; both methods gave similar results, but 14CO2 output was delayed when compared to H2 output and was incomplete. The meal also contained xylose and [13C]glycine, permitting the duodenal entry time of the meal to be estimated by the appearance of xylose in blood and 13CO2 in breath, respectively. The same liquid meal was then used to examine the effect on small intestinal transit time (colonic entry time minus duodenal entry time) of codeine or clonidine. 99Tc-sulphur colloid was also added to the meal to permit a comparison of small intestinal transit estimated by imaging with that estimated by the 14CO2-lactulose breath test. 99Tc radioactivity appeared in the cecum (as assessed using gamma scintigraphy) about 2 hr before 14CO2 radioactivity appeared in breath; the correlation between transit time estimated by the two methods was moderate (r = 0.61; P less than 0.05). Based on the [14C]lactulose data, small intestinal transit time ranged from less than 1 to 3 hr for a liquid meal containing 10 g lactulose; within-subject variation (coefficient of variation 17%) was considerably less than between-subject variation (coefficient of variation 56%). Codeine increased the small intestinal transit time significantly (from 2.7 +/- 0.3 hr to 5.0 +/- 0.9 hr; mean +/- SE), whereas clonidine did not alter small intestinal transit time, as estimated by the colonic entry time minus duodenal entry time. Neither drug influenced duodenal entry time. These results suggest that the [14C]lactulose breath test, which has only moderate accuracy, may have occasional utility as a convenient, noninvasive method for estimating small intestinal transit time in man. However, this study also suggests that indirect methods of estimating small bowel transit in man have limitations, variability, and possibly may lack the desired sensitivity.

Antidiarrheals↗
PubMed1990

[Lidocaine aerosol following tonsillectomy in children].

Post-tonsillectomy analgesia was compared using ten per cent aerosol lidocaine or 1.5 mg.kg-1 intramuscular codeine. Thirty ASA physical status I or II children between two and ten years of age were assigned, in a random fashion, to one of two groups: Group A received codeine 1.5 mg.kg-1 intramuscularly, Group B received a total dose of 4 mg.kg-1 of ten per cent aerosol lidocaine on the tonsillar beds. For both groups, the treatment was administered at the end of the surgical procedure. The postoperative comfort state was assessed on a global scale using the following statement: (1) comfortable = 1, (2) agitation = 2, (3) uncontrollable = 3. Assessment of postoperative comfort was recorded after 20 min in the post-anaesthetic recovery room. Blood samples for lidocaine concentration estimation were obtained at 5, 7.5, 10, and 15 min after administration. Finally, the time of recovery was recorded. The immediate post-anaesthetic comfort observed with ten per cent aerosol lidocaine was statistically superior to that obtained with 1.5 mg.kg-1 intramuscular codeine. The maximal systemic lidocaine concentration which was 2.1 +/- 0.2 micrograms.ml-1 was well below the accepted toxic level of 5.3 micrograms.ml-1. The recovery room times were not statistically different between the two groups. In conclusion, 4 mg.kg-1 of ten per cent aerosol lidocaine applied directly on the tonsillar beds was shown a superior immediate post-tonsillectomy analgesic technique.

Aerosols↗
PubMed1993

Antitussive effect of SR 48968, a non-peptide tachykinin NK2 receptor antagonist.

The antitussive effects of SR 48968, a non-peptide tachykinin NK2 receptor antagonist, were investigated on citric acid-induced cough in the unanesthetized guinea-pig and compared with the effects of codeine. SR 48968 (0.01-0.3 mg/kg i.p.) inhibited in a dose-dependent manner the number of coughs induced by inhalation of an aqueous solution of citric acid with an ED50 of 0.1 mg/kg (0.17 mumol/kg). Under similar conditions, the codeine ED50 was 8 mg/kg (27 mumol/kg). Naloxone, an opioid receptor antagonist, abolished the effects of codeine but did not modify the effects of SR 48968. These data suggest that NK2 receptor stimulation might play an important role in the regulation of the cough reflex and that SR 48968 could be a potential antitussive agent.

Animals↗
PubMed1981

Behavioral effects of thebaine in the rhesus monkey.

Three experiments were conducted with rhesus monkeys to assess some behavioral effects of the opium alkaloid, thebaine, in relation to its dependence liability. The concurrent intramuscular administration of naloxone did not antagonize the rate-decreasing effects of thebaine on a fixed-ratio (FR) schedule of food-reinforced responding. Animals trained to self-administer codeine (0.3 mg/kg/inj) on an FR 30 schedule did not self-administer thebaine (0.003-1.0 mg/kg/inj) at rates comparable to these of codeine. Rates were minimally above those of saline at 0.3 mg/kg inj. Monkeys given 23 hrs/day continuous access to 1.0 mg/kg/inj thebaine did, however, self-administer the drug at rates significantly higher than those maintained by saline, but not as high as those supported by 2.0 mg/kg/inj codeine. Two animals self-administering thebaine did not show any signs of withdrawal when injected with 0.1-1.0 mg/kg of naloxone or when saline was substituted for thebaine. A third monkey showed a severe reaction leading to death following an injection of 1.0 mg/kg naloxone.

Animals↗
PubMed1990

Preferences for opioids by the weight pulling method in rats.

The preference for morphine and codeine was studied by means of the antagonistic conflict behavior between the positive drive of drug intake and the negative drive of weight pulling in rats. An apparatus was developed in which rats were compelled to pull the weight for the intake of drug-admixed food. The experiments began with the preadministration of the drug through the repetition of CFF schedule. The schedule consisted of one choice trial between the intake of normal food and drug-admixed food followed by two consecutive forced trials, in which the rats were forced to take the drug-admixed food only. In the test trial, the findings were that the rats which had already shown a drug seeking behavior toward morphine or codeine pulled weight to take each drug and that the reinforcing effects of these drugs on the drug seeking behavior depended on the treatment period of these drugs. The reinforcing effect of codeine was weaker than one of morphine. It is suggested that the reinforcing effects of these opioids can be evaluated quantitatively by the weight pulling method in rats.

Animals↗
PubMed1985

A modified cold stimulation technique for the evaluation of analgesic activity in human volunteers.

This report describes the effects of a modified cold pressure technique (MCP) on the dominant hand of 6 healthy right-handed volunteers, after single p.o. doses of codeine (60 mg), aspirin (1 g) and placebo in a cross-over, double-blind design. The method employed 9 serial tests on each study day, involving 5 consecutive 2 min periods of hand immersion in an equilibrating bath at constant temperature (37 degrees C), followed by a stimulating bath (0 degree C +/- 0.5) containing 15% ethylene glycol. For better control of peripheral circulatory temperature changes, a blood pressure cuff was inflated to 20 mm Hg below diastolic BP on the right upper arm, thereby preventing venous return from the lower arm during MCP stimulation. Although the test population was relatively small, the results showed a difference between aspirin, codeine and placebo. Codeine was statistically different from placebo (P less than 0.05). It is concluded that this modified technique offers a stable and sensitive method for the early assessment of analgesic activity.

Adolescent↗
PubMed1995

Lack of analgesic effect of 50 and 100 mg oral tramadol after orthopaedic surgery: a randomized, double-blind, placebo and standard active drug comparison.

Tramadol hydrochloride is a synthetic mu-opioid agonist with additional monoaminergic activity. Tramadol's analgesic effect has been equated with that of pethidine, with a more favourable side-effect profile. Tramadol has been the most-selling prescription analgesic in Germany for several years, and it is now available in many other European countries, but still there is a lack of adequately controlled clinical studies of its analgesic properties. The purpose of this study was to compare the analgesic efficacy of 50 and 100 mg oral tramadol with our standard analgesic for postoperative pain treatment, 1000 mg paracetamol + 60 mg codeine, and placebo. A single-dose, parallel group, double-blind design was used. One hundred forty-four patients were enrolled the day after total hip replacement if they had a pain intensity of 60 mm or more on a 0-100 mm visual analogue scale. Treatments were compared on the basis of pain intensity and derived variables (pain intensity difference, and summed pain intensity differences), the need of rescue medication, and a global evaluation. Serum concentrations confirmed rapid and good absorption comparable with that reported in healthy volunteers. The active drug control, paracetamol+codeine, was significantly superior to placebo for all efficacy variable (P = 0.0002-0.004), confirming good assay sensitivity. Paracetamol+codeine was also significantly superior to both 50 mg tramadol (P = 0.002-0.03) and 100 mg tramadol (P = 0.002-0.02). There was no difference between placebo and 50 and 100 mg tramadol for any of the efficacy variables.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetaminophen↗