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At least 1,531 records · Page 85Linked to original sources
PubMed1975

Enzymatic transformation of morphine by hydroxysteroid dehydrogenase from Pseudomonas testosteroni.

Eznyme preparations from Pseudomonas testosteroni containing alpha- and beta- hydroxysteroid dehydrogenases catalyzed the oxidation of morphine and codeine by nicotinamide adenine dinucleotide. Morphine was converted in relatively low yield into 14-hydroxymorphinone probably via morphinone as an intermediate. Codeine was converted to codeinone and 14-hydroxycodeinone. Only the conversions at the 6-position were carred out by the hydroxysteroid dehydrogenase. Hydroxylation at the 14-position did occur spontaneously (or enzymatically with a contaminating enzyme) ater oxidation at the 6-position.

Androsterone↗
PubMed1988

Effect of inhaled and systemic opiates on responses to inhaled capsaicin in humans.

To determine the site of action of opiates in humans, we have studied the effect of systemic and inhaled opiates on cough and increase in respiratory resistance (Rrs) caused by inhaled capsaicin. In 13 subjects, a range of doses of capsaicin inhaled in single breaths given in random order produced a reproducible dose-cough response. Inhalation of a dose of capsaicin that caused fewer than two coughs increased Rrs by 28% (21-35, mean 95% confidence interval). Inhaled codeine (50 mg) and morphine (10 mg) did not alter the cough response. In contrast, both drugs increased base-line Rrs by 24% (16-44) and 13% (3-23), respectively, and significantly reduced the increase in Rrs after inhaled capsaicin (P less than 0.05). Oral codeine (60 mg) significantly (P less than 0.05) reduced the number of coughs at 1 and 2 h but did not alter base-line Rrs or its increase after capsaicin. Intravenous morphine (0.15 mg/kg) significantly reduced the sensitivity of the cough response (P less than 0.05), which was reversed by naloxone. However, there was no significant drug effect on either the base-line Rrs or its increase after capsaicin. Systemic dosing of opiates is therefore required to reduce the cough reflex, whereas inhaled opiates may reduce the increase in Rrs after inhaled capsaicin.

Administration, Inhalation↗
PubMed1999

Influence of central antitussive drugs on the cough motor pattern.

The present study was conducted to determine the effects of administration of centrally active antitussive drugs on the cough motor pattern. Electromyograms of diaphragm and rectus abdominis muscles were recorded in anesthetized, spontaneously breathing cats. Cough was produced by mechanical stimulation of the intrathoracic trachea. Centrally acting drugs administered included codeine, morphine, dextromethorphan, baclofen, CP-99,994, and SR-48,968. Intravertebral artery administration of all drugs reduced cough number (number of coughs per stimulus trial) and rectus abdominis burst amplitude in a dose-dependent manner. Codeine, dextromethorphan, CP-99,994, SR-48,968, and baclofen had no effect on cough cycle timing (CTtot) or diaphragm amplitude during cough, even at doses that inhibited cough number by 80-90%. Morphine lengthened CTtot and inhibited diaphragm amplitude during cough, but these effects were not dose dependent. Only CP-99,994 altered the eupneic respiratory pattern. Central antitussive drugs primarily suppress cough by inhibition of expiratory motor drive and cough number. CTtot and inspiratory motor drive are relatively insensitive to the effects of these drugs. CTtot can be controlled independently from cough number.

Animals↗
PubMed1983

Regulation of monooxygenation during development of chick embryo liver: role of cytochrome P-450 isozymes and NADPH.

The endoplasmic reticulum of the liver cell, supplied with molecular oxygen and NADPH, can monooxygenate a variety of lipid soluble compounds including steroids and many drugs. The essential enzymatic steps are carried out by cytochrome P-450 and NADPH cytochrome P-450 reductase. There are several molecular forms (isozymes) of cytochrome P-450 in liver, and it has been shown that their relative concentrations change during development and in response to phenobarbital. Because substrate specificities of the isozymes differ to some extent, changes in the isozyme pattern should alter the pattern of substrate utilization if the isozymes are controlling the rates of monooxygenation. We found that the rates of testosterone hydroxylation and the oxidative N-demethylations of benzphetamine, codeine, and ethylmorphine were equal in endoplasmic reticulum isolated from chick embryo liver on day 11 of egg incubation, and this equality was unaffected by age or phenobarbital. Thus, monooxygenation rates do not appear to be controlled by the isozymes of cytochrome P-450. A factor that might affect the pattern of steroid and drug utilization by endoplasmic reticulum may be the availability of reducing equivalents. Lowering the concentration of NADPH to one half-optimum values in our reaction mixtures (0.5 to 0.25 mM) diminished the monooxygenation rate of benzphetamine by 8%, of testosterone by 40%, and of codeine and ethylmorphine by 60%. These differential effects were independent of age and phenobarbital. Thus, the pattern of substrate utilization by the monooxygenase system in vivo is probably altered by changes in the tissue concentration of NADPH.

Animals↗
PubMed2003

In vivo pain relief effectiveness of an analgesic-anesthetic carrying biodegradable controlled release rod systems.

Pain is the most common and feared symptom for patients, especially those with cancer. Treatment of chronic pain with conventional ways of medication usually fails with increasing severity of the pain. New approaches enabling the prolonged provision of pain relievers are required. We designed a controlled release system of pain relievers, mainly for opioids (morphine, M, codeine, C, and hydromorphone, HM), and a local anesthetic (bupivacaine, BP) in the form of poly(L-lactide-co-glycolide) (PLGA) rods. The efficacy of these rods implanted alone or in combination in relieving chronic pain in rats caused by the ligation of the sciatic nerve of their right hind limbs was studied. The two most common tests for measuring analgesia, i.e. tail-flick tests, that show analgesia at sites other than the site of injury, were used to study the degree of systemic distribution of the drugs and paw-withdrawal tests were used to study the analgesia at the site of injury. Alleviation of this chronic and severe neuropathic pain could be obtained for about 3-4 days when rods for two drugs, 'dual drug' (analgesic-anesthetic), were used. This duration is decreased by half (2 days) with the single-drug rods. Also the dual-drug rods, though at half the dose of each single drug application, enhanced the degree of analgesia of the first day. These in vivo results are also consistent with the previous in vitro results as in the case with codeine which had a higher first-day analgesia than morphine, despite a lower potency due to the faster in vitro release rate. Similarly, slower release of hydromorphone from PLGA (85:15) rods resulted in less systemic analgesia than the more rapidly eroding PLGA (50:50) rods of the same drug.

Analgesics, Opioid↗
PubMed2006

The availability of web sites offering to sell opioid medications without prescriptions.

OBJECTIVE: This study was designed to determine the availability of web sites offering to sell opioid medications without prescriptions. METHOD: Forty-seven Internet searches were conducted with a variety of opioid medication terms, including "codeine," "no prescription Vicodin," and "OxyContin." Two independent raters examined the links generated in each search and resolved any coding disagreements. The resulting links were coded as "no prescription web sites" (NPWs) if they offered to sell opioid medications without prescriptions. RESULTS: In searches with terms such as "no prescription codeine" and "Vicodin," over 50% of the links obtained were coded as "NPWs." The proportion of links yielding NPWs was greater when the phrase "no prescription" was added to the opioid term. More than 300 opioid NPWs were identified and entered into a database. CONCLUSIONS: Three national drug-use monitoring studies have cited significant increases in prescription opioid use over the past 5 years, particularly among young people. The emergence of NPWs introduces a new vector for unregulated access to opioids. Research is needed to determine the effect of NPWs on prescription opioid use initiation, misuse, and dependence.

Acetaminophen↗
PubMed1985

Experience with a haemagglutination inhibition test for morphine detection in urine.

A commercially available haemagglutination inhibition (HI) test (Drug Test Opiates, Boehringer Biochemia Robin) for the detection of morphine in urine has been evaluated alongside a routine TLC method and a radioimmunoassay. TLC gave positive results for morphine, codeine or dihydrocodeine in 138 out of 300 samples from patients attending a drug dependence treatment unit. These were also positive according to the HI test, but a further 76 of the TLC negative samples also gave positive results with this technique. The TLC negative samples (162) were also analysed by RIA and positive results were obtained for 96 samples. Neither of the immunological tests could distinguish between morphine, codeine or dihydrocodeine, but no reactions with other abused drugs were observed.

Chromatography, Thin Layer↗
PubMedDate not supplied

Pulmonary microcrystalline cellulose deposition from intravenous injection of oral medication in a patient receiving parenteral nutrition.

A 50-year-old man who had been dependent on home parenteral nutrition (HPN) for 24 years presented with shortness of breath. A computed tomography scan of the lungs revealed a diffuse micronodular parenchymal infiltrate. On bronchoscopy, a crystalloid material was identified. This organic material was determined to be consistent with codeine. The patient had been injecting codeine into his intravenous catheter.

Analgesics, Opioid↗
PubMed1983

A double-blind trial of single-dose ciramadol for the treatment of post-episiotomy pain.

A randomized double-blind trial was carried out in 54 women to evaluate the effectiveness of ciramadol in a single (60 or 30 mg) oral dose regimen, compared with 60 mg codeine and placebo, in the treatment of post-episiotomy pain. Ciramadol gave a significantly better analgesic effect, at both 2 and 6 hours, and produced negligible side-effects. Codeine did less well than placebo in this study.

Amines↗
PubMed2003

Postoperative analgesia in children undergoing myringotomy and placement equalization tubes in ambulatory surgery.

UNLABELLED: We enrolled 120 children undergoing bilateral myringotomy and tube placement in this prospective, randomized, observer-blinded study. Patients were randomized into one of four groups: Group 1 (control) was plain acetaminophen 10 mg/kg orally, Group 2 was acetaminophen 10 mg/kg with 1 mg/kg of codeine orally, Group 3 was transnasal butorphanol 25 micro g/kg given immediately after the induction of anesthesia, and Group 4 was ketorolac 1 mg/kg given IM immediately after the induction of anesthesia. All children received oral midazolam (0.6 mg/kg) before surgery. A nurse blinded to the analgesic technique used assessed the child's behavior at the induction of anesthesia and in the postanesthesia care unit using a 4-point scale. Analgesic effectiveness was determined by assessing the child's pain at 5-min intervals using a modified 10-point objective pain scale. In the postanesthesia care unit, rescue pain medication was administered for an objective pain scale >or=4 or a behavior score >or=3. Our data suggest that IM ketorolac is a promising analgesic to be used in this surgical population. Time to first rescue analgesic was longest in the ketorolac group, and there was no associated postoperative vomiting or nausea. IM ketorolac given during surgery was the best analgesic regimen for these procedures. IMPLICATIONS: We compared four different analgesics in the management of pain after placement of pressure equalization tubes during myringotomy in children and demonstrated that ketorolac or butorphanol provided superior analgesia when compared with acetaminophen with codeine or plain acetaminophen. Children who received ketorolac versus butorphanol had less vomiting in the 24 h after surgery.

Acetaminophen↗
PubMed1993

Direct determination of opium alkaloid-bovine serum albumin conjugate by matrix-assisted laser desorption/ionization mass spectrometry.

Opium alkaloids (thebaine, codeine and morphine) have been conjugated with bovine serum albumin (BSA) to give individual antigen conjugates which are analyzed by matrix-assisted laser desorption/ionization (MALDI) mass spectrometry. It became clear that 9 molecules of thebaine were contained in a thebaine-BSA conjugate. Codeine and morphine contents in individual conjugates were determined to be 12 and 6 molecules, respectively.

Codeine↗
PubMed1984

Antitussive effect of RU-20201--central and peripheral actions.

The antitussive effect of the new compound 1, 2, 3, 4a, 9b-hexahydro-8, 9b-dimethyl-4-[3-(4-methyl-piperazine-1-yl) propionamide] dibenzofuran-3-one dihydrochloride (RU-20201) was investigated in dogs and guinea pigs, including its sites of action. The antitussive effect of RU-20201 was about 1/10 as potent as that of codeine phosphate in dogs with the puncture electrode-induced cough (PEC) method and about 1/12 and 1/4 as potent as that of codeine phosphate in guinea pigs with the PEC and chemical stimulation methods, respectively. When RU-20201 was administered in a dose range of 1 to 10 mg into the vertebral artery toward the brain in lightly anesthetized dogs, no antitussive effect was observed against the coughing elicited by electrical stimulation of the central cut end of the superior laryngeal nerve. However, a stimulative effect on respiration, especially on respiratory rate occurred. The peripheral effect of RU-20201 on the cough was investigated using the in situ upper trachea perfusion preparation which allows a direct drug administration to the local site around the tracheal mucosa, this site being electrically stimulated to induce coughing. A close i.a. infusion of RU-20201 in doses of 1 and 3 mg/min into the tracheal vascular bed for 5 min inhibited the cough response elicited by mucosal stimulation. The above findings suggest that RU-20201 has a significant antitussive activity, the site of action being probably, at least, at the cough receptor level.

Animals↗
PubMed2003

Severe hypokalaemia and weakness due to Nurofen misuse.

Nephrotoxicity from non-steroidal anti-inflammatory drugs (NSAID) is well recognized. We report a case of severe hypokalaemia and weakness due to renal tubular acidosis in a young woman who was taking 40-60 tablets per day of Nurofen Plus (ibuprofen 200 mg and codeine phosphate 12.8 mg). Proprietary brands of ibuprofen are freely available to the public and those containing codeine may be potentially subject to abuse. This case highlights the need to be aware of this potential and of the life-threatening electrolyte and acid-base disturbances that might be encountered with the widespread availability of these types of NSAID.

Acidosis, Renal Tubular↗
PubMed2001

Evaluation and application of liquid chromatographic columns coated with "intelligent" ligands. (III). Immobilized phospholipid column.

Immobilized enzyme columns have been developed for use as high-performance liquid chromatographic enzyme reactors. Enzyme reactors were prepared by immobilizing trypsin or cytochrome-c on phospholipid columns. Dynamic coating was employed to prepare the reactors by recycling a buffer solution containing trypsin or cytochrome-c through a phospholipid-coated column, on which the enzymes were immobilized by hydrophobic binding. The immobilized trypsin column displayed hydrolytic activity which catalyzed the hydrolysis of L-amino acid esters to amino acid. The immobilized cytochrome-c column exhibited oxidation activity which catalyzed N-demethylation of N,N-dimethylaniline, codeine, and dihydrocodeine in the presence of hydrogen peroxide as an oxygenating agent. The enzyme reaction proceeded rapidly in the column; both product and substrate could be separated and detected simultaneously. The immobilized enzyme columns could be readily regenerated using the original phospholipid column by repeating the dynamic coating. These immobilized enzyme columns could be utilized as enzyme reactors in the high-performance liquid chromatographic mode. Complete hydrolysis of amino acid ester was observed with the trypsin column. Demethylation of codeine and of dihydrocodeine were observed with the cytochrome-c column.

Aniline Compounds↗
PubMed1980

A psychic dependence study of cinepazide in rats.

I. V. self-administration of cinepazide by rats and the preference of the animals for this drug were studied; and the following were found: 1. I. V. self-administration of cinepazide to rats at dosages of 4, 15, 30, and 60 mg/kg/injection for 7 consecutive days resulted in no self-administration by the animals of the drug far beyond the operant level. 2. Rats undertook the self-administration of cocaine at 1 mg/kg/injection continuously, unlike that of saline or cinepazide. 3. Cross application of cinepazide at dosages of 4, 15, 30 and 60 mg/kg/injection to rats on i. v. self-administration of cocaine failed to substitute itself for the latter. These findings suggested that cinepazide was not a positive reinforcer. 4. Rats exhibited preference for morphine, codeine and pethidine but not for cinepazide. 5. The rats exhibiting preference for morphine also exhibited preference for codeine and pethidine in cross choice trials with these drugs but not for cinepazide in the cross choice trial with this drug. The findings in 4 and 5 suggested that rats showed no preference for cinepazide and that cinepazide failed to maintain the rats' preference for morphine.

Animals↗
PubMedDate not supplied

[Neocodion misuse: evolution between 1992 and 2002].

Neocodion, a codeine antitussive preparation (codeine camphosulfonate + Grindelia + sulfogaiacol) is known to be misused by opiate addicts. This study aimed to examine the evolution in Neocodion use between 1992 and 2002. Since 1992, three surveys (1992, 1997 and 2002) investigating Neocodion misuse were performed via several community networks of pharmacists. During the same time, data on Neocodion use were extracted from the French drug-dependence monitoring programme (OPPIDUM [Observation des Produits Psychotropes Illicites ou Détournés de leur Utilisation Médicamenteuse]). A marked and continuous decrease in Neocodion consumption was observed. The number of requests for Neocodion per pharmacy and per week largely decreased from 9.9 to 2.1 between 1992 and 2002. OPPIDUM data also showed a reduction in the rate of Neocodion consumption (from 8% in 1992 to 0.4% in 2002). Patients were older (30.4 years in 1992 and 33.7 years in 2002) and their socioeconomic conditions were better. Eighty-six percent of the subjects studied were poly-drug consumers. In fact, Neocodion was less sought after for opiate maintenance than for its psychoactive effects. Despite the reduction in the consumption of Neocodion, the changes observed in the consumption patterns for this medication suggest that vigilance is still required.

Adult↗
PubMed1978

Toxicologic assessments in acute heroin fatalities.

The recent improvements in analytic methods enable routine morphine detection in blood in microgram or nanogram quantities. It is now possible to assess acute death from heroin use by toxicologic analyses. A review of available data indicates a rapid distribution of morphine even in sudden fatalities, to the various organs of the body. Blood morphine levels in most acute heroin-involved deaths range from 0.1 to 1.0 microgram/ml, while morphine concentration in liver ranges from 0.1 to 10.0 microgram/gm. In rapid death, the blood to liver ratio is approximately 1:5. Blood and liver appear to be the specimens of choice in determining fatality due to heroin; however a distribution study that included other tissues such as brain, bile, and urine would afford a more meaningful evaluation in forensic investigation. The correlation of the survival periods of decedents to concentrations of morphine in tissues is discussed. Since morphine concentration decreases precipitously in antemortem blood immediately after administration of heroin, the assurance of detecting and determining morphine is greater in blood specimens from decedents who died within 1 hr after drug taking than from those who survived for a longer period. Blood levels of morphine also appear to be regulated by dosage. The role of ethanol and other drugs, including excipients in illicit heroin preparations, in acute narcotism is still poorly understood. Morphine is produced in the antemortem metabolism of codeine. A close evaluation of toxicologic data is necessary to determine whether the morphine detected, if a metabolite, is a conversion product of codeine, heroin, or both. In any event, the cause of death involving heroin is determined only after information from history and pathology, as well as toxicology, are carefully correlated.

Biotransformation↗
PubMed1992

Aberrant cutaneous weal and flare responses in chronic urticaria.

This study examined cutaneous mast cell behaviour in 14 patients with chronic urticaria but no dermographism and 11 healthy controls, by measuring cutaneous weal and flare reactions evoked in response to intradermal challenge injections of 0.1 ml isotonic saline, histamine (20 micrograms), codeine phosphate (10 micrograms) and compound 48/80 (10 micrograms). Five minutes after each injection, the area of the resulting weal and flare was calculated by computer-aided planimetry. The process was repeated at 15, 30 and 45 min following the injection. In patients, saline flares were significantly larger than those of the volunteers at 15, 30 and 45 min (p < 0.05). However, histamine and codeine flare areas were significantly smaller in the patients when compared to the controls at 15, 30 and 45 min (p < 0.05). Compound 48/80 produced smaller reactions in the patients without reaching statistical significance.

Adolescent↗