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At least 1,135 records · Page 63Linked to original sources
PubMed1983

[Transdermal scopolamine for postoperative vomiting: a new form of premedication?].

The author has used scopolamine-TTS, a fundamentally new therapeutic system, exclusively as anti-emetic premedication in 100 patients undergoing surgery with anaesthesia. Application is simple and non-invasive. The results are encouraging: in the first 12 hours after operation the antiemetic therapy had to be extended with i.V.-domperidone because of insufficient effect in only 9% of the patients. 24 hours later still 8% of the patients had slight nausea without vomiting. Slight side effects (delayed waking, accommodation disturbances, dry mouth) occurred in 3 to 30% of the patients. The transdermal therapeutic system opens basically new pharmacological and clinical perspectives.

Administration, Topical↗
PubMed1982

[Analysis and stability of atropine sulfate and scopolamine hydrobromide. 1. Qualitative detection of alkaloids in the presence of their decomposition products. 73. Contribution to the problem of the use of plastic receptacles for liquid pharmaceuticals].

The authors deal with the qualitative determination of tropane alkaloid salts (atropine sulphate and scopolamine hydrobromide) in aqueous solutions in the presence of their decomposition products using thin-layer chromatography. Aqueous solutions of these tropane alkaloid salts were tested for stability after storage in glass and polyethylene containers under various conditions (pH value, temperature, ultra-violet irradiation, oxidative effects). Besides tropine, apoatropine, alpha- and beta-belladonine, further decomposition products showing a basic reaction (and in part not yet identified) were detected. The stability of solid atropine sulphate was studied by means of differential thermal analysis and mass spectrometry.

Atropine↗
PubMed1980

Reduction of enflurane-induced spike activity by scopolamine.

The possibility of enflurane-induced spike activity being related to a cholinergic mechanism was investigated. Thirty mongrel dogs were anesthetized with an inspired enflurane concentration of 3.5 +/- 0.09% (mean +/- SD) to obtain a sustained EEG spike activity. Scopolamine, in 0.04 mg/kg to 0.4 mg/kg IV doses, significantly decreased the spike activity (p less than 0.05). We speculate that a central cholinergic muscarinic mechanism is at least partly responsible for the EEG spike activity produced by enflurane.

Action Potentials↗
PubMed1994

Stereotyped behavioral responses to an auditory stimulus in the course of repeated treatment with methamphetamine plus scopolamine and methamphetamine in rats.

The present experiment was designed to study the effects of an auditory stimulus with 300 Hz, 100 dB on gradual emergence of behavioral sensitization in the course of repeated administration of methamphetamine (MAP) in combination with scopolamine (SCOP) and MAP. Repeated intraperitoneal injection of MAP (4.0 mg/kg) plus SCOP (0.5 mg/kg) induced significantly progressive and enduring enhancement of stereotyped behavior, resulting in intense, focussed stereotypy intermingled with gnawing and licking compared to repeated MAP treatment. Vigorous stereotyped behavior induced by repeated MAP plus SCOP was progressively attenuated by the tone, resulting in attenuation of the development of behavioral sensitization. Conversely, the tone had no invariable effects on behavioral sensitization induced by repeated MAP treatment. The present findings indicate that repeated MAP plus SCOP treatment progressively induced attenuating effects of tone as low as 300 Hz on MAP plus SCOP-induced intense stereotypy and vigorous behavioral sensitization. These findings suggest that a reciprocal balance between dopaminergic and cholinergic inhibitory systems may be involved in producing behavioral sensitization, and in the attenuating effects of the tone on MAP plus SCOP-induced vigorous behavioral sensitization.

Acoustic Stimulation↗
PubMed1993

Teratogenic effects of a mixture of scopolamine and hyoscyamine in chick embryos.

The effect of a mixture of scopolamine and hyoscyamine (98:2) on developing chick embryos was investigated. The embryos were exposed at 2 stages of development to various doses of this mixture via yolk sac injection. This resulted in deaths at different stages of prenatal development, as well as various malformations and reduction deformities. These findings suggest that the studied mixture has a teratogenic effect when injected into the yolk sac of developing chick embryos.

Abnormalities, Drug-Induced↗
PubMed1993

Scopolamine impairs object exploration but not habituation in rats.

Memory of a novel object was examined in saline (Sal) and scopolamine (Scopo) treated rats (1.0 mg/kg). Scopo rats showed lower overall exploration time than Sal rats, resulting mainly from shorter durations per contact. In a second exposure to the same object, after 1 min or 20 min interval, both groups displayed marked decrease of exploration indicating between-session habituation. The shorter time spent by Scopo rats on investigation of an object during a single approach might be interpreted as a deficit in maintenance of attention. Nevertheless, Scopo rats were able to acquire sufficient information for the retention during 20 min interval, as indicated by habituation, which is an elementary index of memory.

Animals↗
PubMed1996

Scopolamine poisoning among heroin users--New York City, Newark, Philadelphia, and Baltimore, 1995 and 1996.

Heroin is mixed ("cut") frequently with other substances primarily to increase its weight for retail sale (e.g., mannitol and starch) and to add pharmacologic effects (e.g., dextromethorphan and lidocaine). During 1995 and 1996, health departments and poison-control centers in New York City (NYC); Newark, New Jersey; Philadelphia; and Baltimore reported at least 325 cases of drug overdoses requiring medical treatment in persons who had used "street drugs" sold as heroin that probably also contained scopolamine, an anticholinergic drug. This report summarizes the clinical and epidemiologic features of these cases, which represent a new type of drug overdose.

Baltimore↗
PubMed1996

Peripherally administered GM-CSF interferes with scopolamine-induced amnesia in mice: involvement of interleukin-1.

We studied the effects of granulocyte-macrophage colony stimulating factor (GM-CSF) on the classical behavioral test of scopolamine-induced amnesia for a passive avoidance response in the mouse. Pre-training intraperitoneal administration of this cytokine (1.25, 2.5, 5.0 or 10 micrograms/mouse) partially, although significantly, reduced the amnesic action of the muscarinic receptor antagonist. The peripheral administration of a specific interleukin-1 receptor antagonist (IL-1 ra, 50 micrograms/mouse i.p.) blocked the effect of GM-CSF. Our results suggest that GM-CSF is able to exert neuromodulatory actions and that it is involved (probably via IL-1) in the interactions between the immune system and the central nervous system.

Amnesia↗
PubMed1996

[Usefulness of pirenzepine in the study of the upper digestive tract and the large intestine with double contrast media: comparison with scopolamine methylbromide].

The purpose of the present study is to assess the importance of pirenzepine, a selective M1 antimuscarinic drug, as hypotonic agent for diagnostic double-contrast studies of the upper gastrointestinal tract and for double-contrast barium enema studies of the large bowel. Pirenzepine and scopolamine methylbromide (SMB) (Buscopan) were compared in a single blind randomized trial. One hundred-thirty consecutive patients were enrolled in the study. Seventy of them underwent double-contrast studies of the stomach and duodenum and sixty double-contrast barium enema studies of the large bowel. Visceral distension and painting of stomach, duodenal bulb and large bowel and global quality of the images were blindly evaluated by 4 independent observers by means of a numerical score (1 to 4). Quantitative analysis of bowel distension was done measuring the maximum diameter of the transverse colon before and after drug administration. No differences were found in the diagnostic performance between the two drugs in the study of the duodenal bulb (2.8 +/- 0.8 vs 2.9 +/- 0.7, p = NS) and of the large bowel (3.0 +/- 0.6 vs 3.1 +/- 0.6, p = NS). Under SMB, slightly but significantly better results were obtained in the stomach (3.0 +/- 0.6 vs 2.7 +/- 0.6, p = 0.01). However, large bowel distension was slightly but significantly improved with Pirenzepine (68 +/- 12 vs 65 +/- 8 mm, p = 0.02). Heart rate and rhythm during the study were recorded by ECG. SMB induced tachycardia in all patients while pirenzepine did not. Moreover, after SMB, 3 patients exhibited faintness, some patients complained of visual accommodation defects, dryness of the mouth and dizziness. Under pirenzepine, no side-effects were reported. To conclude, pirenzepine gives good results in double contrast studies, as good as SMB but with no adverse effects; thus, it could be proposed as the hypotonic agent of choice in upper gastrointestinal and large bowel examinations.

Adult↗
PubMed1997

[Clinical phase III study of cimetropium bromide (DA3177) on the pain with upper urinary calculus: a double-blind study in comparison with scopolamine butylbromide. DA3177 Study Group].

A double-blind study was conducted to evaluate the efficacy, safety and usefulness of cimetropium bromide (DA3177) in the patients with pain caused by upper urinary calculus at a daily dose of 75 mg t.i.d. (Group D, 97 patients) in comparison with scopolamine butylbromide at a daily dose of 60 mg t.i.d. (Group B, 101 patients). According to patient's impression, the rate of "moderately improved" or better was significantly higher in Group D (68.7%) than in Group B (53.5%; Wilcoxon 2 sample test: p = 0.0044). For pain, the rate of "moderately improved" or better was 69.1% in Group D and 60.4% in Group B. In global improvement, the rate of "moderately improved" or better was significantly higher in Group D (70.1%) than in Group B (61.4%; Wilcoxon 2 sample test: p = 0.0469). The rate of "no problem in safety" showed no significant difference between Group D (91.5%) and Group B (93.3%). Adverse reactions occurred in 8.5% in Group D and 6.7% in Group B. The major adverse reactions were "dry mouth", "abdominal distension", "constipation" and "nausea". The rate of "useful" or better was 68.7% in Group D, and 60.4% in Group B. In conclusion, DA3177 was confirmed to be a useful drug for patient with pain caused by upper urinary calculus.

Adult↗
PubMed1976

[Eosphagomanometric finding in man after intravenous administration of a new cholinolytic (pramiverine), atropine and scopolamine butylbromide].

The tone depressing effect on deglutition peristaltic processes in the esophagus by i.v. application of 4,4-diphenyl-N-isopropyl-cyclohexylamine hydrochloride (pramiverine, Sistalgin) (0.03 and 0.045 mg/kg body weight), atropine (0.5 mg) and hyoscine-N-butylbromide (scopolamine-butylbromide, SBB) (20 mg) was tested on trained subjects. During the first 30 min following the larger dose of pramiverine, the effect is not quite so pronounced as it is seen after the usual atropine dose; from the 30th to the 60th min, however, the tone depressing effect of pramiverine is superior to that of atropine, 1 h after application of pyramiverine the pressure amplitude is still reduced to 54.3% of the initial value, while after atropine the effect has returned to 70.9% of the initial value by this time. Neither atropine nor pramiverine were able to exert a tone depressing effect as pronounced as that of SSB. But 30 min after application of the effect of SBB was not statistically significant any longer and after 40 min it could not be measured at all. Following atropine and SBB, the side effect of tachycardia was correlated exactly to the main effect tested. Further side effects, such as dryness of mouth and disturbed accomodation, were most pronounced after atropine. With pramiverine at the effective doses of 0.03 and 0.045 mg/kg, the side effects were not appreciable; neither objective measuring nor subjective reports of the subjects indicated any conspicuous deviations.

Atropine↗
PubMed2000

Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site.

We have studied the interactions of five indolocarbazoles with N-[methyl-(3)H]scopolamine (NMS) and unlabeled acetylcholine at M(1)-M(4) muscarinic receptors, using equilibrium and nonequilibrium radioligand binding studies. The results are consistent with an allosteric model in which the primary and allosteric ligands bind simultaneously to the receptor and modify each other's affinities. The compounds were generally most active at M(1) receptors. [(3)H]NMS binding was enhanced by staurosporine, KT5720, and KT5823 at M(1) and M(2) receptors, and by K-252a at M(1) receptors. Gö 7874 reduced [(3)H]NMS affinity by up to threefold for all subtypes. A range of cooperative effects with acetylcholine was seen, and, at the M(1) receptor, KT5720 had a log affinity of 6.4 and enhanced acetylcholine affinity by 40%. The compounds inhibited the dissociation of [(3)H]NMS to different extents across the receptor subtypes, with the largest effects at M(1) receptors. In equilibrium binding studies the inhibitory potency of gallamine at M(1) receptors was not affected by KT5720, indicating that these agents bind to two distinct allosteric sites and have neutral cooperativity with each other. In contrast, gallamine and staurosporine had a negatively cooperative or competitive interaction at M(1) receptors. Similarly, the potency and relative effectiveness of KT5720 for inhibiting [(3)H]NMS dissociation from M(1) receptors were not affected by gallamine or brucine, but were affected in a complex manner by staurosporine. These results demonstrate that there are at least two distinct allosteric sites on the M(1) receptor, both of which can support positive cooperativity with acetylcholine.

Acetylcholine↗
PubMed1998

Induction of a transient dysexecutive syndrome in Parkinson's disease using a~subclinical dose of scopolamine.

Parkinson's Disease (PD) is often associated with a subcortico-frontal syndrome (SCFS) that is mainly characterized by executive dysfunctions. The complete biochemistry of these dysfunctions remain misunderstood although many studies have suggested a role of the dopaminergic lesions. However, cholinergic lesions in this disease may also account for the SCFS occurrence. The present study has assessed the effects of an acute subclinical dose of scopolamine in normal controls and in PD patients who were devoid of cognitive deficit. Results indicates that PD patients but not normal controls developed a transient SCFS for the duration of the drug action. In contrast to other populations with cholinergic depletions - such as Alzheimer's disease - cholinergic blockage in PD exacerbates specifically the dysexecutive syndrome without inducing amnesia or sedation. Such a discrepancy between these two neuropsychological profiles are discussed in terms of the specificity of the underlying cholinergic lesions.

Journal Article↗
PubMed2005

[Effect of esmolol on cardiovascular responses induced by scopolamine butylbromide].

BACKGROUND: Scopolamine butylbromide (hyoscine-N-butylbromide, HB) is an anticholinergic drug used as a smooth muscle relaxant, and is used even in some surgical procedures during general anesthesia. HB also causes an increase in heart rate as a side effect. The authors evaluated the efficacy of esmolol on hemodynamic changes induced by HB in major abdominal surgery under inhalation anesthesia. METHODS: Seventeen patients for major abdominal surgery were randomly assigned to control group (C group, n = 9) or to esmolol group (E group, n = 8). Anesthesia was induced with propofol and was maintained with isoflurane-nitrous oxide inhalation and intermittent administration of fentanyl and vecuronium. At the time of bowel anastomosis, 20 mg of HB was administrated as an antispasmodic. In E group, esmolol 0.6 mg x kg(-1) was administered immediately after HB administration. RESULTS: There were no differences in the patient background between the two groups. At 1 to 10 minutes after HB administration, heart rate increased significantly compared with that at pre-administration in C group, while there was no significant change in heart rate in E group. Heart rate in E group was significantly lower than that in C group at 2 and 3 minutes after HB administration. Blood pressure was not significantly changed in both groups during the observation period. CONCLUSIONS: The simultaneous administration of HB and esmolol was useful for heart rate control after HB administration.

Adrenergic beta-Antagonists↗