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At least 703 records · Page 39Linked to original sources
PubMed1994

Sulphotransferase-dependent dehydration of atropine and scopolamine in guinea pig.

1. Enzymatic dehydration of atropine and scopolamine was studied in guinea pig. 2. The incubation of these alkaloids with guinea pig liver cytosol in the absence of cofactors gave no dehydrated metabolite. However, when atropine and scopolamine were incubated with cytosol supplemented with ATP and sodium sulphate, dehydrated metabolites, apoatropine and aposcopolamine were formed. The formation of these metabolites was confirmed by gas chromatography-mass spectrometry. 3. The reaction required ATP as well as cytosol as the obligatory factors. Deletion of sodium sulphate from the reaction mixture also resulted in a decrease of the activities, although this treatment showed limited effect when the low concentration of atropine was used. Furthermore, dehydroepiandrosterone, an excellent substrate for hydroxysteroid-sulphotransferase, effectively inhibited the in vitro activity of atropine dehydration. 4. Administration of dehydroepiandrosterone to guinea pig followed by atropine treatment caused decreased urinary excretion of apoatropine. 5. These results strongly suggested that the dehydration of atropine and scopolamine takes place via the sulphate conjugate intermediates produced from the sulphotransferase-catalysed reaction. The present finding is the first example of the sulphotransferase-dependent dehydration of a drug, and its generality in drug metabolism is discussed.

Animals↗
PubMed1986

Transdermal scopolamine in the treatment of asthma: a preliminary report.

The use of atropine has emerged over the past few years as a treatment for asthma. Scopolamine is pharmacologically similar to atropine and, as such, was used in a study of nine patients as a bronchodilator. These nine patients had diverse types of lung diseases. Two patients were intolerant to the medication and were not able to participate in the study. The other seven patients had variable responses with significant improvement in baseline pulmonary function testing occurring in four patients. Five of the seven patients had symptomatic relief and are now employing transdermal scopolamine on a once-every-3-days basis for the treatment of their bronchoconstriction. Baseline testing was performed to indicate response to parasympatholytic medications. Transdermal scopolamine appears to be a safe and effective means of achieving bronchodilation in some patients with asthma.

Administration, Cutaneous↗
PubMed1974

A nonfatal case of intentional scopolamine poisoning.

Scopolamine, a drug not usually found in poisoning, was found to be the cause of toxicity in three persons. This paper stresses the need to confirm any unusual iodoplatinate spots that may occur in emergency drug screening. Gastric lavages appear to be the most useful source for recovering belladonna compounds as no scopolamine was found in the urine, either at admission or the day after. Atropine and scopolamine are easily separated from each other by TLC and GLC but homatropine separates poorly from atropine.

Chromatography, Thin Layer↗
PubMed1999

Cerebral blood flow responses to somatosensory stimulation are unaffected by scopolamine in unanesthetized rat.

Studies with positron-emission tomography have indicated that muscarinic acetylcholine receptors may be involved in the mechanism of enhancement of cerebral blood flow (CBF) by neuronal functional activation. We examined the effects of muscarinic receptor blockade by scopolamine on the local CBF responses to vibrissal stimulation in the whisker-to-barrel cortex sensory pathway in unanesthetized rats. Local CBF was measured by the quantitative autoradiographic [(14)C]iodoantipyrine method. Scopolamine (0.4 or 0.8 mg/kg) was injected i.v. 30 min before measurement of local CBF; control rats received equivalent volumes of physiological saline. Vibrissae on the left side of the face were stroked continuously throughout the 1-min period of measurement of CBF. Local CBF was determined bilaterally in four structures of the pathway, i.e., spinal and principal sensory trigeminal nuclei, ventral posteromedial thalamic nucleus, and barrel field of the sensory cortex, as well as in four representative structures unrelated to the pathway. The higher dose of scopolamine raised baseline CBF in the two trigeminal nuclei, but neither dose diminished the percentage of increases in local CBF because of vibrissal stimulation in any of the stations of the pathway. These results do not support involvement of muscarinic receptors in the mechanism of enhancement of local CBF by functional neuronal activation, at least not in the whisker-barrel cortex sensory pathway in the unanesthetized rat.

Animals↗
PubMed1999

Attenuation of scopolamine-induced deficits in navigational memory performance in rats by bis(7)-tacrine, a novel dimeric AChE inhibitor.

AIM: To study the effects of 1,7-N-heptylene-bis-9,9'-amino-1,2,3,4-tetrahydroacridine [bis(7)-tacrine], a novel dimeric acetylcholine-sterase inhibitor (AChEI) derived from 9-amino-1,2,3,4-tetrahydroaminoacridine (tacrine), on scopolamine-induced spatial memory impairment. METHODS: The effects of bis(7)-tacrine were investigated on the 5-d performance of young adult rats in the Morris water maze. The latency to find the platform in the water maze was measured to evaluate performance. Tacrine was used as a reference drug. RESULTS: Scopolamine (0.3 mg.kg-1, i.p.) resulted in an increase in latency period (> 100% increase) as compared with saline treated controls. Both bis(7)-tacrine and tacrine lessened the increased latency induced by scopolamine to the level of saline control group. The relative potency of bis(7)-tacrine (0.35 mumol.kg-1, i.g. or i.p.) to shorten the escape latency was 24 or 12 times of tacrine (8.52 mumol.kg-1 i.g., 4.26 mumol.kg-1 i.p.) following i.g. or i.p. administration, respectively. There appeared to be an inverse bell-shape dose-dependent effect for both compounds tested. CONCLUSION: Bis(7)-tacrine is a more potent and orally active AChEI than tacrine, and has potential for the palliative treatment of Alzheimer disease.

Animals↗
PubMed2000

The effects of scopolamine and cyclizine on visual-vestibular interaction in humans.

The aim of the present study was to investigate the effects of scopolamine (1.5 mg, transdermal patch) and cyclizine (50 mg tablet), at the doses usually used for the relief of motion sickness, on postural sway, optokinetic nystagmus (OKN) and circularvection (CV) in humans, using a within-subjects, double-blind, placebo-controlled design. Scopolamine and cyclizine were found to have no significant suppressive effect on these aspects of visual-vestibular interaction. Postural sway and CV were not significantly affected by either drug treatment; OKN SPV was significantly increased (p < 0.05), although OKN amplitude and frequency were unaffected. These results suggest that scopolamine and cyclizine, at doses used for the relief of motion sickness, may have minimal suppressive effects on these aspects of visual-vestibular interaction.

Administration, Cutaneous↗
PubMed2000

Effects of microdialyzed oxotremorine, carbachol, epibatidine, and scopolamine on intraspinal release of acetylcholine in the rat.

Intrathecally administered cholinergic agonists such as oxotremorine (muscarinic), carbachol (mixed nicotinic and muscarinic agonist), and epibatidine (nicotinic) have all been shown to reduce nociception in behavioral studies. Thus, there is substantial evidence for a role of acetylcholine (ACh) in the control of nociception in the spinal cord, but the mechanisms regulating ACh release are not known. The present study was initiated to establish a rat model to study which mechanisms are involved in the control of ACh release. Spinal microdialysis probes were inserted intraspinally at the C1-C5 spinal level in isoflurane-anesthetized rats. The probes were perfused with Ringer's solution containing 10 microM neostigmine to prevent degradation of ACh. Oxotremorine, carbachol, epibatidine, and scopolamine, dissolved in Ringer's solution, were administered intraspinally via dialysis and 30 microliter/10-min samples of dialysate were collected for HPLC analysis of ACh content. The release of ACh was found to be constant in the control (Ringer's only) situation during the experimental period of 150 min. Oxotremorine (100-1000 microM), carbachol (1 mM), and epibatidine (50-5000 microM) enhanced but scopolamine (50-200 nM) decreased the intraspinal release of ACh. Oxotremorine (ED(50) = 118 microM) and epibatidine (ED(50) = 175 microM) were found to produce a dose-dependent increase of ACh release. Cholinergic agonists caused an increase of intraspinal ACh and the antagonist scopolamine caused a decreased release of ACh. The data do not support an autoreceptor function of either nicotinic or muscarinic receptors in the spinal cord, contrary to what has been observed in the brain.

Acetylcholine↗
PubMed2000

Long-term effects of acute exposure to chlorphenvinphos on behavioural responsiveness to amphetamine and scopolamine in rats.

We investigated the effect of acute exposure to chlorphenvinphos (CVP) (2-chloro-1 (2,4-dichlorophenyl)-vinyl-diethyl-phosphate), an organophosphate anticholinesterase, on the amphetamine- and scopolamine-induced open-field locomotion in Wistar rats. CVP was administered at a single i.p. dose of 1.0 mg/kg (1/10 of LD50). In part of the rats cholinesterase (ChE) was determined. Three hours after CVP injection, the ChE activity decreased by about 27%. It returned to the preinjection level within 14 days after the exposure. In the behavioural part of the experiment, the animals were challenged with 1.0 mg/kg amphetamine or 0.75 mg/kg scopolamine three weeks after CVP exposure, i.e. after a period of time sufficient for cholinesterase recovery. It has been found that in the CVP-exposed rats, the behavioural responses to amphetamine or scopolamine challenge (the increase in locomotor activity) was significantly reduced compared to the controls. This suggests that acute exposure to CVP produced an increase in cholinergic activity which persisted long after ChE activity had returned to normal.

Amphetamine↗
PubMed2000

Huperzine A reverses scopolamine- and muscimol-induced memory deficits in chick.

AIM: To study the effects of huperzine A on disruption of spatial memory induced by scopolamine (a muscarinic antagonist) and muscimol (a GABAA agonist) in passive avoidance task. METHODS: One-trial passive avoidance task was used to investigate the effects of huperzine A. The avoidance rate was used to evaluate memory retention. RESULTS: Both scopolamine (100 ng) and muscimol (50 ng), injected intracranially 5 min before training, resulted in a decreased avoidance rate. Huperzine A (25 ng), injected intracranially 15 min before training, reversed memory deficits induced by scopolamine and muscimol at 30 min after training, and this reversal persisted at least 1 h. The improving effects of huperzine A exhibited a bell-shaped dose-response curve. CONCLUSION: Huperzine A improved the process of memory formation not only by acting as a highly potent and selective inhibitor of AChE, but also by antagonizing effects mediated through the GABAA receptor.

Alkaloids↗
PubMed1999

[The combined use of scopolamine, naltrexone and naloxone as a rapid, safe and effective detoxification treatment for heroin addicts].

OBJECTIVE: To evaluate the efficacy of a rapid detoxification schedule for heroin addicts by scopolamine combined with opiate receptor antagonists. METHODS: The life signs such as temperature, blood pressure, ECG, heart rate, respiratory rate and blood oxygen saturation were monitored during the process of rapid detoxification treatment. The naloxone challenge test, withdrawal symptoms scale and naltrexone maintenance were used to evaluate the efficacy of the rapid detoxification. RESULTS: The withdrawal symptoms of 84 heroin addicts induced by naltrexone and naloxone were controlled completely under scopolamine administration in the 6-8 hours treatment period, although the naloxone challenge test was able to induce slight and transient withdrawal symptoms in the second day, and all patients were transferred rapidly to naltrexone maintenance. During treatment, the temperature in 19 cases elevated, and all patients showed increased heart rate, blood pressure and respiratory rate. However, the blood oxygen saturation was still stable after oral-administration of naltrexone and continuous injection of naloxone during the detoxification. Blood test in gastric fluid was positive in 3 cases during the detoxification. The follow-up data showed that the average maintenance time of naltrexone was 2.6 months, and the percentage of drug free was 21% in 6 months after the detoxification in 84 cases. CONCLUSION: The combined use of scopolamine, naltrexone and naloxone is a rapid, safe and effective detoxification treatment protocol for heroin addicts.

Adult↗
PubMed2002

Effects of scopolamine and physostigmine on acquisition of morphine-treated rats in Morris water maze performance.

AIM: To investigate effects of morphine on acquisition process of rats a nd interactions of opioid and cholinergic systems by Morris water maze performance. METHODS: Morris water maze was used to measure the latency of rats with drug s treatment to find the covert platform. RESULTS: Chronic morphine administration (10 mg/kg) impaired the acquisition process of rats in Morris water maze task. Appreciable difference was identified with morphine 10 mg/k g group compared with morphine 3 mg/kg group. Co-administration of morphine (10 mg/kg) and scopolamine (3 mg/kg) aggravated acquisition impairment induced by morphine 1 0 mg/kg or scopolamine alone, though scopolamine itself induced no salient changes in acquisition capabilities of rats. In addition, physostigmine (0.1 mg/kg) could appreciably attenuate morphine-induced acquisition impairment. CONCLUSION: Morphine 10 mg/kg evidently impaired acquisition process of rats. There was a close relationship between the acquisition capabilities of morphine-treated rats and the functions of cholinergic system.

Animals↗
PubMed2002

Low dose transdermal scopolamine increases cardiac vagal tone in patients after acute myocardial infarction.

OBJECTIVE: To investigate whether transdermal scopolamine increased cardiac vagal activity in patients during the acute phase of myocardial infarction. METHODS: 30 patients with a first acute myocardial infarction and preserved sinus rhythm who were on no drug that could influence the sinus node were randomly assigned to either treatment group or placebo group. Measures of heart rate variability (HRV) in patients given drug or placebo were obtained by digital 24 hour Holter recording before and after treatment. Baroreflex sensitivity was performed using the phenylephrine method. RESULTS: No significant differences was found in the indices of the time domain and the frequency domain in both groups before treatment. Patients with transdermal scopolamine showed a significant increase in the standard deviation of normal RR intervals (SDNN), standard deviation of all five min mean normal RR intervals (SDANN), root mean square of differences of successive normal RR intervals (rMSSD), total power (TP, 0.000. - 0.40 Hz), low frequency peak (LF, 0.040 - 0.15 Hz), high frequency peak (HF, 0.15 - 0.40 Hz), and Baroreflex sensitivity after treatment (P < 0.05 - 0.01). These indices did not change in patients given placebo. CONCLUSION: Low doses of transdermal scopolamine safely increase cardiac parasympathetic activity and improve autonomic indices in patients with acute myocardial infarction.

Administration, Cutaneous↗
PubMed2003

[Kinetics of scopolamine bromide release from hydrogel with a filtering membrane].

The hydrated filtration membrane renders possible uniform hydration of hydroxypropylmethylcellulose hydrogel with subsequent uniform release of dissolved scopolamine bromide. Exponential dependence of the diffusion coefficient on the graded medium dimension of the pores of the testing membrane makes possible the estimation of the reactive fractal dimension DR by means of the modified exponent (3-DR). With increasing concentration of scopolamine bromide in xerogel (14.7 to 77.8 mg/cm3), DR decreases within a range of 2.814 to 2.704. A comparison with the structure of a suitable fractal (Menger sponge) leads to a conclusion about suitability of the use of membranes for the testing of concentrations of scopolamine bromide in xerogel, if DR > 2.727.

Chemical Phenomena↗
PubMed1992

Central anticholinergic syndrome in a pediatric patient following transdermal scopolamine patch placement.

A 9-year-old child was admitted to the hospital with congenital left ureteropelvic junction obstruction with massive left pyelocaliectasis and underwent dismembered pyeloplasty of the left kidney under general anesthesia without complications. Postoperatively, the child was placed on patient-controlled analgesia, with morphine as the drug of choice. The patient was discharged to the ward with adequate pain control and no complaints of nausea or vomiting. Once on the ward, a transdermal scopolamine patch was placed for nausea and vomiting. More than 24 hours after patch placement, the child experienced central anticholinergic syndrome (CAS) with hallucinations and incontinence. The scopolamine patch was promptly removed, and all symptoms of CAS rapidly ceased. A transdermal scopolamine patch should not be used in the pediatric population, and with extreme caution in the elderly. Treatment of CAS includes prompt removal of the patch, cleansing of the area, and possible physostigmine administration.

Administration, Cutaneous↗
PubMed2003

[Effects of treatment with redox agent, blood transfusion and scopolamine on 200 patients with severe chlorphenamidine poisoning].

OBJECTIVE: To verify the effects of treatment with blood transfusion and scopolamine on severe chlorphenamidine poisoning (SCP). METHODS: 400 patients with severe oral chlorphenamidine poisoning were randomly divided into two groups. 200 patients (Group I) were treated with the traditional combined therapy including gastrolavage, purgation and taking redox agent (methylene blue and vitamin C) while the other 200 patients (Group II) in addition to the above mentioned therapy, received blood transfusion and scopolamine injection. RESULTS: The cure rate of Group II was 99.5% and significantly higher than that of Group I (91.0%, P < 0.01). The average time of improving in health in Group II [(8.71 +/- 1.49) h] was obviously shorter than those in Group I [(10.65 +/- 1.72) h, P < 0.01]. Blood methemoglobin concentrations in Group II at 3, 7, 12, 24 h after admission [(43.58 +/- 2.69), (34.21 +/- 2.30), (20.60 +/- 4.03), (13.50 +/- 1.65) g/L respectively] were obviously lower than those in Group I [(54.42 +/- 12.79), (42.17 +/- 22.34), (30.66 +/- 17.67), (19.01 +/- 0.61) g/L respectively, P < 0.01]. CONCLUSION: Blood transfusion and scopolamine had distinctive therapeutic effect on SCP to makeup the deficiency of redox agent. Combination of three therapies may potentiate the detoxication for chlorphenamidine.

Adult↗
PubMed1992

Incidence of arterial oxygen desaturation in cardiac patients premedicated with intramuscular scopolamine and morphine.

The effect of a standard preoperative medication combination, morphine and scopolamine, on arterial oxyhemoglobin saturation was measured continuously in 29 patients scheduled for elective coronary artery bypass grafting procedures. On the morning of operation, both before and after administration of preoperative medication, each patient was monitored continuously with a pulse oximeter (SpO2). Patients received 0.05 to 0.11 mg/kg of morphine (mean = 6.0 +/- 2.1 mg) intramuscularly (IM) and 0.2 to 0.4 mg of scopolamine (mean = 0.30 +/- 0.07 mg) IM. The mean arterial blood oxyhemoglobin saturation decreased from 92.0 +/- 1.8% before preoperative medication to 89.0 +/- 3.8% (P greater than .001) after preoperative medication. Forty-five percent of the patients had SpO2 less than 90% for at least 2 minutes, and 21% below 85%. In conclusion, significant arterial oxyhemoglobin desaturation occurred in this group of cardiac surgical patients after preoperative medication with morphine and scopolamine. Prophylactic administration of oxygen with preoperative medication might reduce the incidence of hypoxemia in this group of patients at risk for myocardial ischemia.

Aged↗
PubMed2006

The influence of scopolamine and extreme temperatures on the lipid level in some mouse organs.

OBJECTIVES: The effect of scopolamine administration at dose 0,5 g/kg b.w. and high (+40 degrees C) and low (+4 degrees C) temperature on the level of triacyloglycerides, total lipids and cholesterol in the mouse liver, kidney and muscle of males and females. METHODS: The homogenates of the liver, kidney and muscle were taken for examination. The concentrations of triacyloglycerides, total lipids and cholesterol was estimated according to the Bio-La-Tests (Poland). RESULTS: The concentration of triacyloglycerides and total lipids in the liver, kidney and muscle increased of males and females after scopolamine injections and after exposure to high and low temperatures. CONCLUSION: Scopolamine may effect an increase in the rate of the lipid metabolism.

Adaptation, Physiological↗
PubMed2006

[Determination of scopolamine in the poisoning case by GC/MS].

OBJECTIVE: To separate and determine scopolamine from the food in a poisoning case by GC/MS. METHODS: The scopolamine was determined by GC/MS/El used CP5860(CP-sil8CB) column (30 mx 0.25 mmx 0.33 microm) with liquid- liquid extraction. RESULTS: The deny scopolamine was found in the case sample, and the chromatographic separation of the peaks is fine. CONCLUSION: The method is accurate and reliable.

Foodborne Diseases↗