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PubMed1983

Quantitative assessment of jumping behaviour of morphine-like analgesics in mice.

The withdrawal jumping behaviour under the influence of twelve narcotic analgesics was compared in order to estimate the degree of morphine-like physical dependence in mice. The vertical jumping was elicited by an intraperitoneal injection of nalorphine followed by seven subcutaneous administrations of each drug studied during two days. During the 30 min of the observation period, the number and the height of jumps as well as the distribution of jumps were recorded. The jumping rate of the mice due to the drugs was nearly dose-dependent. The mice injected with morphine or levorphanol exhibited a large number of high jumps mostly during the first 10 min, with a maximal incidence of jumping. Mice injected with drugs inducing a low or moderate degree of physical dependence such as codeine exhibited low and few jumps, a maximal incidence being observed with codeine, whereas the incidence with pentazocine and nalorphine amounted to only 20% or less. Levorphanol exhibited the lowest JD50 (median effective dose required to produce jumping) and the JD50 of morphine was about one-tenth that of codeine. The potential rank order of the drugs as to jumping activity roughly corresponded with that of their morphine-like physical dependence inducing effect in man. Of eighteen non-narcotic drugs tested, only apomorphine possessed a jumping activity. However, the jumping behaviour with apomorphine was dissimilar to that with morphine-like analgesics. From these results, it can be suggested that this method to observe the jumping behaviour is suitable to evaluate the degree and property of morphine-like physical dependence in mice.

Administration, Oral↗

PubMed1983

The effect of antihistaminics on cataleptogenic action of analgesics and haloperidol.

We investigated the effect of benzhydramine, thenalidine, mepyramine (H1 receptor antagonists) and cimetidine (H2 receptor antagonist) on cataleptogenic action of morphine, codeine, fentanyl, and haloperidol. Benzhydramine antagonized the catalepsy induced by analgesics (particularly by codeine). The antagonistic effect of thenalidine was weaker (but also very prominent for codeine catalepsy). Mepyramine did not affect the catalepsy induced by analgesics. All three H1 receptor antagonists attenuated the catalepsy induced by haloperidol. Cimetidine, injected intraventricularly, did not affect the catalepsy induced either by analgesics or by haloperidol. It is suggested that the antagonistic action of benzhydramine and thenalidine against analgesic catalepsy is related rather to their antiserotonin properties, while the anticataleptic activity of all three H1 receptor antagonists against haloperidol catalepsy is caused by their anticholinergic and antiserotonin properties.

Analgesics↗

PubMed1982

Impact of a drug bulletin on prescribing oral analgesics in a teaching hospital.

The impact of a drug bulletin on prescribing oral analgesics in a teaching hospital was studied. Using an abbreviated time-series design, prescriptions for oral analgesics for all inpatients were surveyed one, three, and five weeks before and one, three, five, and seven weeks after the distribution of one of the hospital's regular drug bulletins. This bulletin contained guidelines for the treatment of minor, moderate, and severe pain. The 493 patients included in the study were classified by drug category, pain severity, and timer period. The drug categories were: (1) propoxyphene, (2) aspirin or acetaminophen alone or with codeine 8 mg or less, and (3) codeine alone or in combination products with more than codeine 8 mg, or other oral narcotic drugs. Each patient's pain severity was determined by interviewing attendant nursing staff; the validity of this approach was confirmed by correlating nurse and physician perception of pain at one time point. Multivariate contingency table analysis revealed that the drug bulletin significantly (p less than or equal to 0.05) reduced the prescribing of propoxyphene hydrochloride across both the minor and moderate pain categories. An increased use of aspirin and acetaminophen was significant three weeks after the release of the drug bulletin. This effect, however, was not significant at other time points. Drug bulletins can be used to achieve a temporary change in physician prescribing patterns of oral analgesics. For a sustained effect, alternative strategies are needed.

Administration, Oral↗

PubMed1993

[Hypersensitivity reactions in patients with irritable colon syndrome].

In a group of 74 patients with irritable colon syndrome the studies were carried out evaluating the frequency of abnormal reactions after meal and positive skin reactions with extracts of inhalatory and alimentary substances, 0.1% histamine and 1% codeine. An assessment was also done of the correlation of skin reactions with the degree of irritability of the large bowel expressed as score. Abnormal reactions after meal were reported by 89% of the studied patients with irritable colon syndrome. All meals giving abnormal reactions after consumption may be the source of allergens and may trigger allergic reactions in predisposed persons, but many of them, in view of the contents of histamine, tyramine, and the ability of release or synthesis and release of mast cell mediators, may cause reactions of pseudoallergic mechanism. Intensity of skin reaction in the form of oedema and erythema after intracutaneously administered codeine varied between the studied groups. The highest intensity was found in patients with irritable colon syndrome (ICS) who had intermittent diarrhoeas. The intensity of oedematous skin reaction after codeine in patients with ICS was correlated with the degree of irritability of the large bowel evaluated by the accepted score. The obtained results may be an indirect evidence of the participation of pseudoallergic reaction in the pathological mechanism of ICS in certain patients.

Adolescent↗

PubMed1982

Diflunisal. A new oral analgesic with an unusually long duration of action.

The analgesic efficacy of single 500- and 1,000-mg doses of diflunisal (Dolobid), a new nonsteroidal anti-inflammatory analgesic, was compared in a double-blind study with that of acetaminophen, 600 mg, the combination of acetaminophen, 600 mg, with codeine phosphate, 60 mg, and placebo in 159 oral surgery outpatients. Using a self-rating record, patients rated their pain and its relief hourly for 12 hours after medication. Both doses of diflunisal were significantly more effective than acetaminophen alone and produced peak analgesia comparable to that of the acetaminophen-codeine combination. Diflunisal proved to have an unusually long duration of analgesic action. Acetaminophen and the combination were significantly superior to placebo through hours 2 and 5, respectively; both doses of diflunisal were significantly superior through the end of the 12-hour observation period. None of the active treatments produced more side effects than the placebo.

Acetaminophen↗

PubMed1981

Adverse effects of commonly ordered oral narcotics.

Approximately equianalgesic oral doses of codeine, an oxycodone compound resembling Percodan, and pentazocine were compared for adverse effects in a double-blind, randomized study of four doses of each drug given over two days to 247 postsurgical patients with pain. Placebo and parenteral morphine were also treated as negative and positive controls, respectively. Approximately 50 patients each received one of the five drugs. Codeine, pentazocine, and morphine had the same incidence of adverse effects (22 to 28 per cent). One capsule of oxycodone compound was the analgesic equivalent of 12.5 mg morphine with an adverse effect incidence of 4 per cent (placebo 8 per cent). Smoking made no difference in analgesic effect or adverse effects. Analgesics given in the evening intervening between the two days may have affected the analgesic performance of placebo.

Administration, Oral↗

PubMed2005

Surface-activated chemical ionization ion trap mass spectrometry in the analysis of drugs in dilute urine samples. Part II: analysis of morphine and other street drugs.

The new ionization method, called surface-activated chemical ionization (SACI), was employed for the analysis of fives drugs (morphine, codeine, 6-monoacetylmorphine (6-MAM), benzoylecgonine and cocaine) by ion trap mass spectrometry. The results so obtained have been compared with those achieved by using atmospheric pressure chemical ionization (APCI), no-discharge-APCI and electrospray ionization (ESI) clearly showing that SACI is the most sensible one mainly due to the high ionization efficiency and the lower chemical noise. The performance of SACI in terms of sensitivity and linearity was compared with the sensitivity and linearity obtained using APCI, no-discharge-APCI and ESI, showing that the new SACI approach gives rise to the best results. Then, SACI was used to analyze morphine, codeine, 6-MAM, benzoylecgonine and cocaine in urine samples. After the optimization of the instrumental parameters for a mixture of the standard compounds, eight urine samples were analyzed. They were strongly diluted (1 : 20 and 1 : 100) in order to prevent the chromatographic column damage due to the matrix composition. Furthermore, the diluted urine samples were directly analyzed, without pretreatment, through LC-MS and LC-MS/MS, and the obtained results are reported.

Cocaine↗

PubMed1993

Ion-pair reversed-phase liquid chromatographic identification and quantitation of papaverine congeners.

A reversed-phase ion-pair high-performance liquid chromatographic separation was developed for identification and quantitation of papaverine drug congeners, namely papaverine (1), moxaverine (2), drotaverine (3), and ethaverine (4) hydrochlorides. A synthetic reference mixture of the four congeners in the range 1-4 micrograms showed good separation. With a reference standard (codeine phosphate), the relative retention times to codeine were 1.356, 1.984, 2.46, and 2.91 (mean of six) for 1, 2, 3, and 4, respectively. Good linearity was obtained in the quantitation of 1 and 2 in the range 1-2 micrograms [correlation coefficient (r), 0.9978 and 0.9997, respectively] and 3 and 4 in the range 2-4 micrograms, (r, 0.9998 and 0.9991, respectively). Analysis of some commercial dosage forms containing one of these congeners showed good recovery with sufficient accuracy and precision. The method was sensitive and permitted the use of small sample sizes or unit doses.

Chromatography, High Pressure Liquid↗

PubMed2006

Use of gas chromatography/mass spectrometry with positive chemical ionization for the determination of opiates in human oral fluid.

An analytical method for the simultaneous determination of codeine, morphine and 6-acetylmorphine (6AM) in human oral fluid was developed. The method involves liquid-liquid extraction in Toxitubes A, derivatization with 99:1 (v/v) N,O-bis(trimethylsilyl)trifluoroacetamide (BSTFA)/trimethylchlorosilane (TMCS), and gas chromatography/mass spectrometry with positive chemical ionization (GC/PCI-MS) determination. The detector response was linear over the concentration range 30-500 ng/mL with coefficients of correlation higher than 0.99. The precision was acceptable with coefficients of variation less than 7.5%. The limits of detection achieved were 0.7 ng/mL for codeine, 2.0 ng/mL for morphine, and 0.6 ng/mL for 6AM. The method proposed was applied to 80 oral fluid samples from opiates users, 98% of which were positive for the three analytes. Human oral fluid is a suitable biological fluid for the determination of opiates by GC/PCI-MS.

Analgesics, Opioid↗

PubMed1997

Opioid effects on macrovascular dopamine release.

Both alkaloid opiates and met-enkephalin occur in vertebrate chromaffin cells, where they affect catecholamine (CA) secretion. Since the large blood vessels of the eel and the rat release dopamine (DA) from as yet unidentified source(s), we studied the impact of alkaloid opiates and met-enkephalin on the secretion of DA from three macrovessels of the American eel (Anguilla rostrata) in a perifusion system. Codeine, morphine, and met-enkephalin increased the release of DA from both the ventral aorta and the caudal vein. The antagonist naloxone stimulated DA release from the caudal vein, but had no impact on release from the ventral aorta. Only codeine had a significant effect on DA release from the posterior cardinal vein. These findings show that the DA release from the macrovessels is sensitive to opioid substances, and they suggest that the antagonistic effects between alkaloid opiate and opioid peptide, seen in other systems, are absent in large blood vessels. Furthermore, the "unorthodox" stimulatory effect of naloxone in the caudal vein raises the question of as yet unidentified receptor and/or effector systems.

Analgesics, Opioid↗

PubMed1990

Microbial degradation of the morphine alkaloids: identification of morphine as an intermediate in the metabolism of morphine by Pseudomonas putida M10.

A strain of Pseudomonas putida was isolated by selective enrichment with morphine that was capable of utilising morphine as a primary source of carbon and energy for growth. Experiments with whole cells showed that both morphine and codeine, but not thebaine, could be utilised. A novel NADP-dependent dehydrogenase, morphine dehydrogenase, was purified from crude cell extracts and was shown to be capable of oxidising morphine and codeine to morphinone and codeinone, respectively. This NADP-dependent morphine dehydrogenase was not observed in any other species of pseudomonads examined and was quite distinct from the beta-hydroxysteroid dehydrogenase found in Pseudomonas testosteroni, which had previously been shown to have activity against morphine.

Biodegradation, Environmental↗

PubMed1981

Comparison of opioid agonists in maintaining responding and in suppressing morphine withdrawal in rhesus monkeys.

Sixteen opioid agonists were studied for their capacity both to maintain responding previously reinforced by codeine and to suppress the withdrawal syndrome induced by morphine deprivation in rhesus monkeys. All compounds, which included examples from each of the major chemical families of opioids, maintained responding at rates above those maintained by saline. There were differences among the compounds in the maximal response rates maintained, and large differences in their potencies in maintaining responding. In morphine-dependent monkeys, the abstinence signs that developed 14 h after the last morphine dose were suppressed completely by all of the compounds except codeine. There was a strong positive correlation (r = 0.92) between the potency of a compound in maintaining drug-reinforced responding and the potency of the compound in suppressing the morphine withdrawal syndrome.

Animals↗

PubMed1992

Differences between jejunal myoelectric activity after a meal and during phase 2 of migrating motor complexes in healthy humans.

Using an intraluminal probe with six pairs of annular electrodes, the myoelectric activity of the proximal jejunum was recorded during 48-hr sessions in 16 healthy volunteers receiving evening and noon meals (1000 kcal) and breakfast (400 kcal). In 10 subjects receiving no drug, the characteristics of the migrating motor complexes (period, duration of each phase, velocity of propagation of phase 3, duration of the postprandial disruption) varied markedly between subjects but were relatively constant from the first to the second day of recording. Single spike bursts propagated at a rate of 2-5 cm/sec, clusters of 3-10 spike bursts propagated at a rate of 0.5-1 cm/sec, and similar clusters recurring repetitively each 1.5-2 min were observed after the meals and very rarely in the fasted state during phase 2 of nocturnal migrating motor complexes. In six subjects, oral administration of codeine (50 mg) 1 hr before a meal induced migrating motor complexes in the postprandial state, with characteristics similar to that observed in the fasted state except a longer duration of phase 2. Single spike bursts and isolated and repetitive clusters of spike bursts were observed during phase 2 of the codeine-induced migrating motor complexes and after meals preceded by placebo, but very rarely during the phase 2 of nocturnal (fasted state) migrating motor complexes. It is concluded that the patterns of jejunal contractions consisting of propagated single spike bursts and isolated or repetitive spike bursts characterize the postprandial state in healthy humans and are dependent upon digesta flow.

Adult↗

PubMed1977

Studies on the potency of various antitussive agents.

Several antitussive agents were assessed for their cough-suppressant activity. Cough responses were obtained by electrically stimulating the lower brainstem, in cats lightly anesthetized with sodium pentobarbital or in unanesthetized midcollicular decerebrate preparations. Cough sounds were recorded with the aid of a microphone. The cough reactive region was concentrated in an area dorsomedial to the trigeminal tract and nucleus. The potency of these antitussive agents (dextromethorphan, RO 21-4790-001, codeine, clonazepam, diazepam and caramiphen) were determined by studying their effect on the centrally induced cough responses. Each of these agents was administered in graded doses intravenously to determine the minimal effective doses for suppressing the cough responses. They are 0.57, 2.55, 1.71, 0.048, 0.28 and 3.18 mg/kg for the above listed drugs. The results indicate that clonazepam was found to be the most potent antitussive among these agents, the mean effective dose being about 1/35 of that of codeine. The antitussive potency of benzodiazepines is not well correlated with their muscle relaxant activity. For instance, clonazepam and diazepam have the same potency in depressing polysynaptic spinal reflexes, whereas the former is six times more potent than diazepam as an antitussive. This finding indicates that clonazepam has a high specificity as an antitussive.

Animals↗

PubMed1998

The effectiveness of clonidine as an analgesic in paediatric adenotonsillectomy.

PURPOSE: To compare the analgesic effects of preoperative oral clonidine with intraoperative intravenous fentanyl in children undergoing tonsillectomy or adenotonsillectomy. METHODS: This randomized, controlled, double-blind study of 36 ASA I-II children, age 7-12 yr undergoing adenotonsillectomy was conducted at a tertiary care paediatric teaching hospital. Either 4 micrograms.kg-1 clonidine po was given 60-90 min preoperatively or 3 micrograms.kg-1 fentanyl i.v. was given intraoperatively. Postoperatively visual analog pain scores (VAS) were recorded at rest and on swallowing every 10 min for the first 30 min and then every 15 min for two hours. Morphine 0.05 mg.kg-1 i.v. was given for VAS > or = 5. If > 3 doses were required, 1.5 mg.kg-1 codeine po and 20 mg.kg-1 acetaminophen po were given. Sedation and anxiety scores were recorded preoperatively. Haemodynamic changes, blood loss, recovery scores, and the incidence of vomiting, hypotension, and airway obstruction were recorded. RESULTS: Children who received clonidine had a higher incidence of preoperative sedation (63%) than those receiving fentanyl (6%). Preinduction mean arterial pressure was lower in the clonidine group but required no intervention. VAS scores were similar throughout the observation period. There was no difference either in the number of morphine or codeine rescue doses administered or in the incidence of side effects. CONCLUSION: Oral clonidine is an effective analgesic and sedative for children undergoing tonsillectomy or adenotonsillectomy.

Acetaminophen↗

PubMed1983

Review of the comparative analgesic efficacy of salicylates, acetaminophen, and pyrazolones.

Use of salicylates, acetaminophen, and pyrazolones has become increasingly complex, extending from the treatment of acute, mild pain to chronic, moderately severe pain. The intensity, rather than the nature, of the pain determines the efficacy of aspirin. A clinical dose-response relationship has been established, and time-effect curves indicate that the total threshold-raising effect depends on dosage frequency. Contrary to popular belief, aspirin and acetaminophen appear to be equipotent and equianalgesic for the relief of most pain. The combination of aspirin (650 mg) plus codeine (30 mg) is only slightly more effective than aspirin alone. The same holds true for acetaminophen (600 mg) plus codeine (60 mg); the efficacy of the combination is only slightly better than that of acetaminophen alone.

Acetaminophen↗

PubMed1986

Effects of glutathione and phenobarbital on the toxicity of codeinone.

The ability of sulfhydryl compounds to provide protection against the acute toxicity of codeinone, a toxic metabolite of codeine, was investigated in mice. Subcutaneous administration of codeinone produced a slight reduction in hepatic glutathione concentration. Pretreatment of the mice with glutathione or cysteine significantly increased the survival rate for mice given a lethal dose of codeinone (10 mg/kg). The lethality of codeine was lowered by naloxone, whereas that of codeinone was not blocked by naloxone. The strychnine-like convulsant action of codeinone could be prevented by phenobarbital pretreatment. Glutathione pretreatment reduced the amounts of radioactivity in tissues of mice injected with [N-methyl-3-H]codeinone. A possible explanation for these observations is that glutathione reacts in vivo with codeinone and plays a role as a scavenger of this compound. This assumption is supported by the observation that codeinone reacts non-enzymatically with glutathione under physiological conditions.

Animals↗

PubMed1975

Etonitazine-induced rigidity and its antagonism by centrally acting muscle relaxants.

Some narcotic drugs have been reported to produce increases in muscle tone in rats. In our laboratory we have found that etonitazine produces a 'lead-pipe' rigidity of the trunk and limb musculature. The reported studies were conducted to characterize etonitazine-induced rigidity more fully, to compare the degree of rigidity with that produced by morphine, codeine and methadone, and to assess the sensitivity of this rigidity to centrally acting muscle relaxants. Of the 4 narcotics tested, etonitazine was far more potent than methadone or morphine for producing rigidity; codeine did not produce peak rigidity comparable to the other 3 narcotics. Etonitazine-induced rigidity occurs at a supraspinal level since the effect was prevented by spinal transsection. Etonitazine-induced rigidity was prevented by the narcotic antagonists cyclazocine, pentazocine and naloxone but not by the serotonin depletor, p-chlorophenylalanine. Etonitazine-induced rigidity was antagonized by centrally acting muscle relaxants, including diazepam, methocarbamol, carisoprodol and zoxazolamine; in agreement with their relative clinical muscle relaxant potencies, diazepam is the most potent antagonist of etonitazine-induced rigidity.

Analgesics, Opioid↗