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PubMedDate not supplied

Effects of pentagastrin and oxyphenonium on the levels of serotonin and 5-hydroxyindoleacetic acid in different parts of the digestive tract, blood and brain of rats.

In the experiments of Wistar rats it was found that pentagastrin in a dose of 0.6 microgram/kg decreased the level of serotonin and increased that of 5-HIAA in the stomach wall, and in a dose of 3 micrograms/kg it had no effect on these parameters, while in a dose of 6 micrograms/kg it decreased only the serotonin level. Oxyphenonium 0.5 mg/kg increased only the 5-HIAA level in the stomach, and in a dose of 5 mg/kg it decreased also the level of serotonin, In the duodenum these substances remained unchanged after pentagastrin administration, but oxyphenonium 5 mg/kg caused a significant fall of serotonin and increase of 5-HIAA, which was associated with a decrease in the number of enterochromaffin cells. In the small intestine pentagastrin 0.6 micrograms/kg increased the serotonin level and decreased that of 5-HIAA, in a dose of 3 micrograms/kg it decreased only the 5-HIAA level, and in the 6 micrograms/kg dose it had no effect on the levels of these substances. Oxyphenonium increased only the intestinal 5-HIAA level but only when administered in a dose of 5 mg/kg. In the brain both higher doses of pentagastrin decreased the serotonin level, and all three doses raised significantly the 5-HIAA level. Oxyphenonium in the higher dose raised the brain serotonin level, but was without effect on the 5-HIAA level. The blood serotonin level was not changed by pentagastrin and oxyphenonium.

Animals↗
PubMed1988

Comparative study of the bronchodilating effects of (-)- and (+)-oxyphenonium bromide.

1. Racemic oxyphenonium bromide, its enantiomers and placebo were inhaled by eight adult patients with chronic airflow obstruction, in a four-way double-blind cross-over study. 2. Forced expiratory volume in one second (FEV1) and slow inspiratory vital capacity (VC) were measured during the first 6 h after inhalation. 3. (+)-Oxyphenonium was found to be the active enantiomer (eutomer), providing better bronchodilation than (+/-)-oxyphenonium. 4. The distomer, (-)-oxyphenonium, showed only a slight effect on FEV1 and VC as compared with placebo.

Adult↗
PubMed1984

Protective effect of oral oxyphenonium bromide, terbutaline and theophylline against the bronchial obstructive effects of inhaled histamine, acetylcholine and propranolol.

The protective effects of oxyphenonium bromide, terbutaline and theophylline were compared in 8 asthmatic patients by determination of the degree of non-specific airway reactivity after 1 week of oral treatment according to a fixed dose scheme in a double-blind random order: oxyphenonium bromide 3 X 10 mg; terbutaline 3 X 5 mg; theophylline 2 X 300 mg and placebo. Controlled, standardized inhalation provocation tests were carried out with histamine, acetylcholine and propranolol. The study was monitored by measuring blood concentrations of the 3 drugs, and their effect on the plasma cAMP concentration was also determined. Significant protection by oxyphenonium bromide against the bronchial obstructive effects of acetylcholine and propranolol was observed, but not against the effect of inhaled histamine. The other two drugs provided no significant protection against the inhaled agents. The absence of any protective effect of terbutaline and theophylline might have resulted from too low a blood concentration. The observed differences in protection could not be explained by changes in pulmonary function. The study suggests dissociation between the bronchodilating effect of a drug and its protective effect against inhaled substances.

Acetylcholine↗
PubMed1984

Development of a sensitive radioreceptor assay for oxyphenonium in plasma and urine.

A radioreceptor assay (RRA) for oxyphenonium has been developed. It is based on competition between [3H]dexetimide and oxyphenonium for binding to muscarinic receptors from calf striata. The RRA is optimized towards incubation medium and to extraction by ion pair formation with sodium picrate. At least 4 X 10(-10) M of oxyphenonium is necessary to permit a reliable assay. This corresponds to a detection limit of drug of 2 ng ml-1 urine. After extraction, drug at 100 pg ml-1 of plasma can be estimated using 4 ml samples. The method is applicable to monitoring the drug and to the determination of its pharmacokinetics after therapeutic dosing. Urine levels can also be monitored.

Animals↗
PubMed1989

Unequal disposition of enantiomers of the organic cation oxyphenonium in the rat isolated perfused liver.

This paper describes the results of pharmacokinetic experiments in the rat isolated perfused liver with enantiomers of oxyphenonium. The study was performed with the [14C]methyl labelled compounds. In this preparation both metabolism and biliary excretion were significantly different for the (+)- and the (-)-isomer. Hepatic uptake rate was similar, but total biliary excretion (including metabolites) of the (-)-isomer was only 55% compared with the excretion of the (+)-isomer. In line with these data, after 2 h only 30% of the dose of the (+)-isomer and over 50% of the dose of the (-)-isomer was still found in the liver, predominantly in the form of metabolites. The metabolic profile was investigated using ion pair TLC. At least two metabolites were detected in bile for both enantiomers. However, unchanged (-)-oxyphenonium persisted for longer in bile, indicating either a more rapid canalicular transport of the (+)-isomer and/or a more rapid metabolism of (+)-oxyphenonium to cholephilic metabolites.

Animals↗
PubMed1977

Determination of oxyphenonium bromide in plasma and urine by means of ion-pair extraction, derivatization and gas chromatography-electron-capture detection.

A sensitive and selective method for the determination of the quaternary ammonium compound oxyphenonium bromide (Antrenyl), a drug with strong anticholinergic properties, in human plasma and urine is described. The method is based on ion-pair extraction of the cation with perchlorate, a re-extraction according to ion-pair principles with tetrapentylammonium as the counter ion, hydrolysis to cyclohexylphenylglycolic acid, derivatization of this acid to its pentafluorobenzyl ester and determination of the ester by gas chromatography and electron-capture detection. Quantitation is possible down to 2 ng/ml of oxyphenonium bromide using 1 ml of plasma and down to 200 ng/ml using 0.1 ml of urine. The method described can also be applied to other anticholinergic drugs with an ester function.

Animals↗
PubMed1984

Radioreceptor assay for oxyphenonium.

The development of a radioreceptor assay for the quaternary anticholinergic drug, oxyphenonium, in plasma is reported. It is based on competition between this drug and 3H-dexetimide for binding to muscarinic receptors. After ion pair extraction and reextraction, the drug can be determined in plasma at concentrations down to a value of 100 pg/ml. This permits pharmacokinetic studies to be made after inhalation of oxyphenonium.

Animals↗
PubMed1997

Safety pharmacology of a combination of tinidazole and oxyphenonium bromide.

The effect of a combination of 150 mg tinidazole (CAS 19387-91-8) and 1 mg oxyphenonium bromide (CAS 50-10-2), referred to as the combination, was examined in various animal species to assess its safety. In mice and rats, the combination in the dose range 30-1000 mg/kg p.o. or 250 mg/kg i.p. did not produce behavioural or neurological changes, nor did it influence pentobarbital sleeping time, though, alcohol sleeping time was altered. In anaesthetised dogs, neither blood pressure, ECG, heart rate, respiration or gastrointestinal motility was affected after single intraduodenal administration of the combination 20 and 50 mg/kg or after chronic oral administration of 25 mg/kg daily for 15 days. In isolated organs, viz. perfused rabbit heart, guinea-pig ileum and rat ileum no significant changes were observed following various doses of the combination, compared to tinidazole and oxyphenonium bromide given alone in corresponding concentrations. In conclusion, the pharmacological profile of the aforementioned combination in the dosages employed in mice, rats, guinea-pigs, rabbits and dogs shows that it is safe and well tolerated.

Animals↗
PubMed2001

Stoichiometric and microenvironmental effects on hydrolysis of propantheline and oxyphenonium bromides in cyclodextrin solutions.

The effects of alpha-, beta-, and gamma-cyclodextrins (CDs) on the basic hydrolysis of propantheline bromide (PB) and oxyphenonium bromide (OB) are analyzed in terms of the stoichiometry and microenvironments of their complexes. The rate constant of each species is evaluated with binding constant data for the 1:1, 1:2, and 2:1 complexes. The dielectric constant of the binding site of PB is estimated from the ultraviolet maximum wavelength in reference with the ethanol-water and dioxane-water systems. The energy-optimized structures of some complexes of PB with beta- and gamma-CD are obtained by molecular mechanics. Because the ester linkage of PB in the 1:1 complex with alpha-CD and in the 2:1 complex with gamma-CD is located near hydroxyls of the CD rim, these complexes catalyze the hydrolysis of PB. In contrast, the hydrolysis is inhibited by the formation of the 1:1 and 1:2 complexes of beta-CD and the 1:1 complex of gamma-CD because the ester linkage of PB is rather deeply incorporated into the CD cavities for these complexes. All the CDs inhibit the hydrolysis of OB. The rate constant of the 1:1 complex of OB and CD is in the decreasing order alpha-CD > gamma-CD > beta-CD. This order is consistent with that of the local dielectric constants of the binding sites.

Binding Sites↗
PubMed1990

Synthesis of d-[11C]oxyphenonium iodide, a potential radioligand for in vivo visualization of human cholinergic muscarinic receptor-sites by positron emission tomography.

Carbon-11 labeled d-oxyphenonium iodide, a cholinergic antagonist is synthesized for in vivo visualization of muscarinic receptor-sites on airway tissue by positron emission tomography (PET). Methylation with [11C]CH3I of d-demethyloxyphenonium, followed by HPLC purification affords the desired radiopharmaceutical with a radiochemical yield of 66% (based on [11C]CH3I, and corrected for decay) and with a specific activity of 110-300 Ci/mmol. The biologically active labeled d-enantiomer is prepared within 40 min after EOB. Optical and chemical purity proved to be better than 99.9%. Radiochemical purity was determined to be higher than 99%.

Binding Sites↗
PubMed1991

The effect of oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux in children with vesicoureteral reflux and detrusor instability.

In a prospective study the effects of the anticholinergic drugs oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux were studied. Although anticholinergic properties are claimed of both drugs, only oxybutynin hydrochloride proved to decrease detrusor contractility and the degree of reflux, probably due to a direct spasmolytic effect on the detrusor. Therefore, in cases of reflux and detrusor instability treatment with oxybutynin hydrochloride is recommended.

Child↗
PubMed1999

Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions.

The UV absorbance and bitter taste of oxyphenonium bromide (OB), an antiacetylcholine drug, in cyclodextrin (CD) solutions are measured, and the local environment of the binding site and the reduction of the bitter taste intensity are quantitatively estimated from the UV data. The UV spectrum of OB is changed with the addition of alpha-, beta-, and gamma-CD, because the phenyl group of OB is included into the CD cavity. The maximum wavelength, lambda(max), senses environmental changes of OB best among several spectral characteristics. From comparison of lambda(max) between a CD solution and the reference ethanol-water and dioxane-water systems, the dielectric constant of the binding site is evaluated. This value leads us to estimate the microenvironment and structure of the binding site. The suppression of the bitter taste of 4 mM OB by CDs is in the increasing order alpha-CD < gamma-CD < beta-CD. The extent of this suppression can be quantitatively predicted from the UV absorbance by assuming that the free OB molecule alone exhibits the bitter taste, regardless of the kind and concentration of CD. Some implications and limitations of the present approach are discussed.

Cyclodextrins↗
PubMedDate not supplied

Solution structures of 1:1 complexes of oxyphenonium bromide with beta- and gamma-cyclodextrins.

The solution structures of complexes of oxyphenonium bromide (OB) with beta- and gamma-cyclodextrins (beta- and gamma-CDs, respectively) in deuterium oxide have been investigated by 500 MHz proton NMR spectroscopy and molecular mechanics calculations. The chemical shifts induced by complex formation provide the 1:1 binding constants and the chemical shift variations, DeltadeltaOB-CD, with complexation for the protons of OB and the CDs. The observed binding constants are very close to those obtained by other methods and are in the following order: beta-CD > gamma-CD > alpha-CD. Initial structures of the complexes are constructed on the basis of the ROESY spectra and the DeltadeltaOB-CD values and are optimized by molecular mechanics calculations. The intermolecular distances between the protons of OB and CD calculated for these structures are well-correlated with the observed ROESY intensities. The cyclohexyl group of OB penetrates deeply into a beta-CD cavity, and the phenyl group is close to the wide rim of the cavity. The phenyl and cyclohexyl groups of OB are both incorporated into a gamma-CD cavity. Furthermore, these structures of the complexes are consistent with the suppression of bitter taste and basic hydrolysis of OB by CDs and the polarity of binding sites of OB.

Kinetics↗
PubMed1990

[The atropine test in patients with stress incontinence and their treatment with a combination of diltiazem and oxyphenonium].

The authors applied the Atropine test in 28 patients with the motor type of urgent incontinence in an attempt to establish the prognosis of the success of treatment with parasymthatholytics. Atropine was administered in amounts of 0.01 mg/kg body weight by the i.m. route and after 30 mins. a urodynamic control examination was made. The assumption that a reduced frequency or amplitude of detrusor contractions will occur or that they will disappear in patients, where subsequent treatment with parasympatholytics will be successful, was not confirmed. The patients were subsequently treated by a combination of dilthiazem (Diacordin), 3 X 30 mg by the oral route per day and oxyphenonium (Oxyphenon dupl.) 2 X 10 mg by the oral route per day. After evaluation of the therapeutic results the group was divided into two sub-groups. The first one comprised patients where during the urodynamic check-up examination a drop of the intracystic pressure occurred after Atropine administration. The second group comprised patients where the drop of intracystic pressure did not occur. The therapeutic effect in these groups was evaluated separately. In the course of treatment there was a relatively high percentage of undesirable side-effects of the drugs in 43% of the patients. After the general evaluation of the therapeutic effect when the patients had no complaints or improved markedly in 70.4% there were no marked differences between the sub-groups.

Atropine↗