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PubMed1980

[Covalent binding of codeine hydroxylation products to albumin and microsomal membranes].

It was shown that incubation of rat liver microsomes with [3H] codeine in the presence of 3 mM NADPH and 0.5% albumin is accompanied by covalent binding of codeine radioactive metabolites to albumin and microsomes. At low concentrations of the microsomal protein in the samples the number of metabolites bound to the membranes is greater than those bound to albumin. At increasing concentrations of the microsomal protein the binding occurs mainly at the expense of albumin. The animal induction with phenobarbital increases the number of bound metabolites. An injection of 3-methylcholantrene does not affect the degree of binding. All typical inhibitors of cytochrome P-450, i.e. SKF-525A, methyrapone, octylamine and CO, inhibit the binding. The data obtained suggest that the metabolites which bind to the macromolecules are generated by cytochrome P-450. It is assumed that the appearance in the blood of covalently bound albumin-hapten conjugates formed in the cytochrome P-450--hydroxylase system can induce the immune response. Hense, one more protective system of the organism becomes involved in the decontamination of low molecular weight compounds.

Albumins↗
PubMed1995

[Drug substitution treatment of heroin dependent patients with codeine preparations--treatment effects from the viewpoint of the physicians and patients].

The controversy caused by the debate on treatment and substitution strategies in drug addiction is unchanged. This is particularly true concerning the use of codein-based drugs in the substitution of heroin abusers. However, only a few studies on the effects of this old and widely used method of substitution have been carried out. This article presents one retrospective and prospective study on the effects of the codein-based substitution in heroin abusers (n = 416). With respect to the issues addressed by this study such as somatic and psychic health, social integration, delinquincy and consumption patterns, patients as well as clinicians report an improvement in general health and fewer of the problems usually associated with heroin abuse, similar to the results from substitution treatment elsewhere.

Adult↗
PubMed1984

Potential synthetic codeine substitutes: (-)-3-O-aryl-N-methylmorphinans.

A series of novel O-aryl-N-methylmorphinans (7-19) were synthesized by the Ullmann reaction from levorphanol (4) in our search for a synthetic codeine (2) substitute with reduced addition liability. The compounds were evaluated for antinociceptive potency and receptor binding affinity. Among these compounds, (-)-3-phenoxy-N-methylmorphinan (7) is an orally active analgesic comparable in potency to codeine (2), which exhibits decreased physical dependence liability and longer duration of action.

Animals↗
PubMed2006

The butterbur extract petasin has no effect on skin test reactivity induced by different stimuli: a randomized, double-blind crossover study using histamine, codeine, methacholine, and aeroallergen solutions.

BACKGROUND: Petasin (Ze 339) was recently introduced on the market as a potent herbal antiallergic drug for treatment of respiratory allergies such as hay fever. Few clinical studies have been performed so far addressing the clinical effectiveness of Ze 339. OBJECTIVE: To evaluate the antiallergic properties of Ze 339 using skin prick tests with different stimuli, such as codeine, histamine, methacholine, and a relevant inhalant allergen. METHODS: A randomized, double-blind, placebo-controlled study was performed in which Ze 339 was compared to acrivastine, a short-acting antihistamine, in 8 patients with respiratory allergy and in 10 nonatopic, healthy volunteers. Antiallergic activity of Ze 339 was determined by analyzing inhibitory potency in skin prick tests with codeine, histamine, methacholine, and an inhalant allergen. Wheal-and-flare reactions were assessed 90 minutes after a double dose of Ze 339, acrivastine, or placebo. An interval of at least 3 days was left between the skin tests. RESULTS: Acrivastine was identified as the only substance that significantly inhibited skin test reactivity to all solutions analyzed in all study subjects. In contrast, no significant inhibition could be demonstrated for Ze 339 with any test solution. Moreover, the results of Ze 339 did not differ significantly from placebo. CONCLUSIONS: In this study we found no antiallergic, particularly antihistaminic, effect of Ze 339 in skin tests using a variety of stimuli often used to evaluate immediate skin test reactivity. The mechanism by which Ze 339 is effective in the treatment of seasonal allergic rhinitis still needs to be elucidated.

Administration, Inhalation↗
PubMed2002

Partial filling micellar electrokinetic chromatography optimization studies of ibuprofen, codeine and degradation products, and coupling to mass spectrometry.

Studies have been performed to evaluate whether an on-line partial filling-micellar electrokinetic chromatography (PF-MEKC) system could be applied to a recently developed MEKC method for the separation of ibuprofen, codeine and one of the degradation products. Attempts to couple the PF-MEKC system to MS have also been performed. SDS concentration, micellar zone length and concentration of acetonitrile in the buffer were optimized using factorial design. When a small micelle zone was injected directly after the sample introduction, the results improved markedly. The MS parameters have not been optimized, but the studies show promising results for the use of PF-MEKC-mass spectrometry for identification of the degradation products.

Acetonitriles↗
PubMed2003

Partial filling-micellar electrokinetic chromatography optimization studies of ibuprofen, codeine and degradation products, and coupling to mass spectrometry: part II.

We describe the use of partial filling-micellar electrokinetic chromatography-mass spectrometry (PF-MEKC-MS) on the pharmaceutical ingredients ibuprofen and codeine phosphate as well as their degradation products and impurities. The study focuses on the change of the borate buffer to the volatile ammonium acetate and the optimization of critical MS parameters. The sensitivity of the method is also evaluated. The results are compared to an existing MEKC-UV method that is used for quantitative determination of the two main substances as well as for the analysis of the degradation products. It is concluded that the PF-MEKC-MS system is suitable for separation and identification.

Acetates↗
PubMedDate not supplied

Analgesic comparison of propiram fumarate with pentazocine, codeine, and placebo in postsurgical pain.

The safety and effectiveness of a single oral dose of 50 mg propiram fumarate as an analgesic was compared in a double-blind clinical trial trial against single doses of standard reference analgesics (50 mg pentazocine hydrochloride or 60 mg codeine sulfate) or placebo. Subjects were adult patients experiencing severe postsurgical pain. Mean pain scores and SPID scores showed all three active drugs to be favored (P less than 0.05) over placebo in patients with severe initial pain. The most common side effects seen were drowsiness, nausea, and dizziness. These were not severe enough to require treatment. Propiram fumarate (50 mg) was shown to be an effective and safe analgesic in the treatment of severe postsurgical pain.

Adolescent↗
PubMed1977

Binding of codeine, morphine, and methadone to human serum proteins.

The binding properties of codeine, morphine (as representative opium alkaloids), and methadone (a synthetic pharmacologically similar compound) were studied with selected human serum proteins. The methodology involved equilibrium and dynamic dialysis using 3H-and/or 14C-labeled compounds. For estimation of the percent binding with equilibrium dialysis, concentrations of the ligand used were approximately therapeutic blood levels and another concentration 30-60 times higher. The percent binding to whole human serum ranged from about 20% for morphine to almost 60% for methadone. Of the human serum proteins investigated, the highest percent binding was found with albumin, except for methadone for which it was beta-globulin III. The affinity for other serum proteins varied with the ligand. In studies with albumin using dynamic dialysis, the plots of nubar divided by free concentration versus nubar were similar for all three ligands studied and had positive slopes, unlike those reported for acidic compounds for which the slope is always negative. In studies of binding of one ligand in the presence of another, significant competition was demonstrated, suggesting that the same binding sites were involved.

Binding, Competitive↗
PubMed1977

Quantitative determinations of codeine phosphate, guaifenesin, pheniramine maleate, phenylpropanolamine hydrochloride, and pyrilamine maleate in an expectorant by high-pressure liquid chromatography.

The quantitative determinations of codeine phosphate, guaifenesin, pheniramine maleate, phenylpropanolamine hydrochloride, and pyrilamine maleate in a liquid dosage form are described. All active and inactive ingredients (sodium benzoate and FD&C Yellow No. 5 dye) can be separated with high-pressure liquid chromatography except the two antihistamines, pheniramine maleate and pyrilamine maleate. Pheniramine maleate is determined colorimetrically, and pyrilamine maleate is determined either by difference or spectrophotometrically. The methods are simple short, accurate, and precise. The standard deviations are reported.

Chromatography, High Pressure Liquid↗
PubMed1980

Simultaneous quantitation of acetaminophen, aspirin, caffeine, codeine phosphate, phenacetin, and salicylamide by high-pressure liquid chromatography.

A method for the simultaneous quantitation of acetaminophen, aspirin, caffeine, codeine phosphate, phenacetin, and salicylamide was developed. The method is based on reversed-phase high-pressure liquid chromatography with a mobile phase buffered with phosphate (pH 2.3). The procedure not only separated these six active ingredients but also salicylic acid, the major decomposition product of aspirin. The method gave excellent results for three commercial products and a synthetic mixture containing four active ingredients. Lowering the pH increased the retention time of some weak acids and decreased that of some weak bases. Only these changes in the retention times made the separation possible.

Acetaminophen↗
PubMed1994

Codeine-induced bronchoconstriction and putative bronchial opiate receptors in asthmatic subjects.

To determine whether a mu opiate agonist can constrict the human airways, the dose of codeine (C) or histamine (H) producing a 40% decrease (PD40) in specific airway conductance (SGAW) was measured in 17 asthmatic and 14 normal subjects. Then, the subjects were skin tested with C and H, and the effect of naloxone (N) and chlorpheniramine (CP) on PD40-C was assessed. In five asthmatic subjects responding to less than 5 mg (16.6 mumol) inhaled C, SGAW was also recorded after oral administration (30 mg) and pharyngeal spraying (5 mg) of C. PD40-C could be determined in 11 of the 17 asthmatics but in none of the normal subjects. This constrictor effect lasted less than 15 min, was unrelated to resting airway caliber, and required a relatively high bronchial sensitivity to H (PD40-H usually less than 0.2 mumol) and high doses of C (11.93 +/- 12.0 mumol). However, in C responders, PD40-C and PD40-H were unrelated. C-induced bronchoconstriction was blunted by N in a dose-dependent fashion and to a mild and inconsistent degree, by CP. Pharyngeal spraying or oral challenge with C failed to change SGAW. Skin sensitivity to H and C was similar in C-responders and non-responders. In conclusion, large doses of inhaled C constrict the airways of asthmatic subjects highly sensitive to H. This effect seems mediated through (mu?) opiate receptors located bronchially rather than centrally, pharyngeally or in the skin. In C-induced bronchoconstriction H liberation plays a contributory but minor role. Skin and bronchial sensitivity to C are unrelated.

Adolescent↗
PubMed1991

Genetic analysis of the interethnic difference between Chinese and Caucasians in the polymorphic metabolism of debrisoquine and codeine.

The Far Eastern and Caucasian populations are strikingly different with respect to the debrisoquine/sparteine hydroxylation polymorphism. The number of poor metabolizers, as defined for Caucasians, is very low among Chinese and Japanese. We investigated the molecular basis for this difference by analysis of the CYP2D6 gene in 115 Chinese subjects, combined with phenotypic classification of codeine and debrisoquine metabolism. A correlation between the rates of metabolism of these two drugs and genotype, as analyzed by RFLP using XbaI, was observed among the Chinese. A high frequency (37%) of alleles indicative of gene insertions (reflected by XbaI 44kb fragments) was recorded in the Chinese, but was not associated with the poor metabolizer phenotype, as it is in Caucasians. PCR amplification of part of the CYP2D6 gene with mutation specific primers for CYP2D6A (29A) and CYP2D6B (29B) allelic variants revealed that the XbaI 44kb fragment in Chinese apparently contains a functional CYP2D6 gene, in contrast to the situation among Caucasians. The results provide a molecular explanation of the interethnic difference in the metabolism of drugs affected by the debrisoquine hydroxylation polymorphism.

Adolescent↗
PubMed1980

[Determination of morphine and codeine in urine by high-pressure liquid chromatography (author's transl)].

A sensitive and specific method for the determination of morphine and codeine is described. The drugs are adsorbed from urine on Amberlite XAD-2 resin at pH 8.5 and eluted from it with organic solvent. After a clean up the residue is separated by high-pressure-liquid-chromatography on reversed phase column using 0.1 M NaH2PO4 in 25% CH3CN/H2O as mobile phase. The eluted drugs are detected by uv-absorption at 230 nm. The method is sensitive, specific and precise.

Chromatography, High Pressure Liquid↗
PubMed1993

Endogenous codeine and morphine are stored in specific brain neurons.

Codeine and morphine have been detected in mammalian brain by radioimmunoassay (RIA), and in brain and other tissues by gas-chromatography/mass-spectrometry (GCMS) in different laboratories. It has been also shown that rat liver can synthesize the skeleton of the morphine molecule, thus suggesting that this alkaloid, which is the prototype of mu-receptor agonists, plays a physiological role in brain. We report the presence of morphine-like immunoreactive compounds inside the cell body, fibers and terminals of neurons in different brain areas. Moreover, neurons localized in the same brain areas were capable of accumulating and storing [3H]morphine slowly infused intracerebroventricularly (i.c.v.) through an osmotic minipump.

Animals↗
PubMed1993

Characterization of morphine-specific monoclonal antibodies showing minimal cross-reactivity with codeine.

Six murine monoclonal antibodies against morphine were produced using N-(4-aminobutyl)normorphine as a hapten. Most of the antibodies obtained distinguished the substituents at the 3 and 6 positions of morphine. This property of the antibodies led to a reduction in cross-reactivity with codeine, morphine-3-glucuronide (M-3-G) and morphine-6-glucuronide (M-6-G) to negligible levels. However, one of the antibodies distinguished the substituent only at the 3 position of morphine, which cross-reacted with M-6-G, naloxone and naltrexone. In the competitive inhibition enzyme-linked immunosorbent assay, morphine was detected at concentrations as low as circa 100 pg/ml.

Animals↗
PubMedDate not supplied

Toxicological investigations of cases of death involving codeine and dihydrocodeine.

Drug levels in post-mortem specimens from 6 cases of poisoning involving codeine or dihydrocodeine have been determined using a direct extraction method followed by gas liquid chromatography. The relevant case histories are described. A preliminary qualitative investigation of dihydrocodeine metabolism has been described involving the analysis of urine samples by thin layer and gas chromatography.

Adult↗