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At least 19 recordsLinked to original sources
PubMed1986

The effects of transdermal scopolamine and four dose levels of oral scopolamine (0.15, 0.3, 0.6, and 1.2 mg) upon psychological performance.

Four dose levels of oral scopolamine (0.15 mg, 0.3 mg, 0.6 mg, 1,2 mg), transdermal scopolamine, and placebo, were investigated for their effects upon a battery of psychological performance measures in normal subjects. Oral scopolamine produced significant linear dose-related decrements on tasks involving continuous attention, continuous performance, memory storage for new information, and on self-rated feelings of alertness and sociability. Transdermal scopolamine produced significant performance impairments on these same assessment measures. Resting heart rate levels were significantly reduced by all scopolamine conditions. Side effects (dry mouth, dizziness) were frequent following transdermal scopolamine and the higher oral dose conditions. The overall effects of the transdermal scopolamine patch were broadly equivalent to the effects of 0.8 mg oral scopolamine. This oral dose equivalence for transdermal scopolamine is higher than expected, and possible reasons for this are discussed.

Administration, Oral↗
PubMedDate not supplied

Increased cognitive sensitivity to scopolamine with age and a perspective on the scopolamine model.

18 older normal volunteers (mean age = 66.5 +/- 7.9 years) and 46 younger volunteers (mean age = 27.0 +/- 6.1 years) were administered the anticholinergic drug scopolamine (0.5 mg i.v.) followed by a battery of cognitive tests evaluating attention, learning and memory. The older subjects were significantly more impaired than the younger by scopolamine on some tests of learning and memory. This increased sensitivity of the older group to scopolamine is consistent with studies in animals and humans showing decreased cholinergic system function with age. The findings also indicate that age is an important variable to consider in using the scopolamine model of memory impairment. The cognitive impairment caused by scopolamine in younger subjects in this and prior studies is similar to some, but not all aspects of the impairment which occurs in normal aging. Scopolamine also caused impairments on digit span and word fluency tasks, which are not consistent with normal aging changes. In the older group of subjects, scopolamine produced aspects of the cognitive impairment which occurs in AD on tests of episodic memory and learning, vigilance-attention, category retrieval, digit span, and number of intrusions. Other areas of cognition that are of relevance to aging and AD such as psychomotor speed, praxis, concept formation and remote memory were not evaluated in this study. Some of these are being evaluated in ongoing studies, along with additional and more specific tests of retrieval from knowledge memory, implicit memory and attention. The scopolamine model has provided a fruitful pharmacologic starting point for the study of a number of cognitive operations. The idea of dissecting apart aspects of memory systems pharmacologically depends on the availability of neurochemically specific drugs and on the specificity and sensitivity of neuropsychological tests for distinct cognitive operations or domains. Further studies using such tools will aid not only in the understanding of the impairments which occur in aging and in AD, but also of the conceptualization of memory and other cognitive operations and ultimately the physiological mechanisms involved in memory and learning.

Acetylcholine↗
PubMed1992

Blockade of conditioned taste aversion by scopolamine and N-methyl scopolamine: associative conditioning, not amnesia.

The anticholinergic, scopolamine, consistently disrupts one-trial passive avoidance conditioning but the effects of such drugs on one-trial conditioned taste aversion (CTA) are variable and contradictory. In the present study, treatment of rats with scopolamine impaired the suppression of sucrose intake by post-ingestion administration of lithium chloride (LiCl) in a two-bottle choice test. A similar effect was obtained by using N-methyl scopolamine which penetrates the brain only to a limited degree on acute administration. The blockade of CTA could be prevented in three ways: (i) by exposing the rats to sucrose only on the training day, (ii) by pre-exposing the rats to both sucrose and scopolamine, and (iii) by using a less palatable sucrose/ascorbate mixture. The results demonstrate that the effect of scopolamine on taste aversion is not mediated by the central nervous system, and can be modified by altering the novelty and relative salience of the taste conditioned stimulus. These experiments suggest that conditioned associations between taste and LiCl, and scopolamine and LiCl may underlie the blockade of CTA by scopolamine.

Amnesia↗
PubMed1987

Characteristics of effects of repeated scopolamine administration on ambulatory activity in mice and methamphetamine sensitivity in the scopolamine-experienced mice: comparison among 6 strains.

Effects of scopolamine (0.5 mg/kg, s.c.) on ambulatory activity were investigated in 6 strains of mice (dd, ICR, BALB, C57BL, C3H and DBA). Scopolamine increased ambulatory activity, and the sensitivities were in the order of ICR greater than C3H greater than BALB greater than DBA greater than C57BL greater than dd. This was different from that produced by methamphetamine (2 mg/kg, s.c.) where the order was ICR greater than dd greater than DBA greater than C3H greater than C57BL greater than BALB. A tolerance to the ambulation-increasing effect of scopolamine was progressively produced in dd, ICR, C57BL and DBA strains, but not in BALB and C3H strains, when the drug was administered 5 times at intervals of 3-4 days. The repeated scopolamine treatment elicited a major enhancement of the sensitivity to the ambulation-increasing effect of methamphetamine (2 mg/kg, s.c.) in BALB and C3H strains and a minor enhancement in the C57BL strain, whereas dd, ICR and DBA strains did not exhibit a marked change in the sensitivity to methamphetamine even after the same treatment with scopolamine. These results suggest that the ambulation-increasing effect of scopolamine is different from that of methamphetamine and that the interaction between scopolamine and methamphetamine varies among different strains of mice.

Animals↗
PubMed2000

Different impact of carvedilol and transdermal scopolamine on cardiovascular performance of mild-moderate chronic heart failure patients: evidence of useful effects of scopolamine on tolerance to work load.

OBJECTIVES: To verify and compare the effects respectively exercised in chronic heart failure patients by transdermal, slow release scopolamine patch and by the beta and alfa adrenoreceptor blocker carvedilol upon the main indexes derived from maximal cardiopulmonary stress test, as well as from analysis of heart rate variability. METHODS: In each of 14 patients suffering from NYHA class II chronic heart failure, admitted to study, the maximal cardiopulmonary test and heart period power spectrum assessment were performed, firstly during usual therapy, then after 7 days of continuous adjunctive treatment with scopolamine patch, and, finally after 3 months of regular administration of oral carvedilol, added to the basal therapy. The need of time enough to the adaptation of the cardiovascular system against the carvedilol pharmacodynamics, together with the need of slow, progressive dose titration, caused that the onset of therapy with carvedilol was separated from assessment of its effects on ergometric and spectral parameters by an interval period of 3 months. RESULTS: During administration of low doses of scopolamine, the values of VO2max, exercise time and double product were respectively 24 +/- 5.3 ml/kg/min, 12 +/- 3 min and 23630 +/- 3760, and resulted significantly higher than basal (p < 0.05 in all cases) and carvedilol-related readings (p < 0.01 by comparisons with VO2max and double product; p < 0.05 by comparison with exercise time). Again during scopolamine, the total variance, LF and HF powers exhibited the values reported as follows: 1255 msec2 and, respectively, 430 and 250 msec2, thus exceeding significantly the basal levels (p < 0.05 from comparison with total power, p < 0.01 from comparisons with LF and HF bands) as well as the levels reached during adrenergic blockade with carvedilol (LF scopolamine vs LF carvedilol: p < 0.01; total power and HF scopolamine vs corrispective carvedilol values p < 0.05). Compared to the basal findings, the carvedilol induced a significant reduction in VO2max (p < 0.05), double product (p < 0.01), peack of heart rate (p < 0.05) and LF power (p < 0.05), and elicited no significant decreases in exercise time; similarly a weak, not significant surge was product by carvedilol in total and HF powers. CONCLUSIONS: Therefore, in patients with left ventricle asymptomatic dysfunction, the low doses of scopolamine potentiate simultaneously the spontaneous heart rare variability and cardiopulmonary maximal testing; whereas, the carvedilol acts upon LF oscillatory component only, the effects upon total variance and HF band being negligible; moreover, this drug depress the myocardial functional capability; in fact, the carvedilol has been demonstrated to produce a remarkable fall in VO2max, this significant reduction in O2 maximal uptake involving the poor rise in cardiac output during the effort or less effective O2 removal from capillary beds or both.

Administration, Cutaneous↗
PubMed1993

DAU 6215, a novel 5-HT3-receptor antagonist, selectively antagonizes scopolamine-induced deficit in a passive-avoidance task, but not scopolamine-induced hypermotility in rats.

This study examined the effects of DAU 6215, a selective 5-HT3-receptor antagonist, on either impairment of a passive-avoidance task or hypermotility, both caused by scopolamine in rats. In the first experiment, scopolamine (0.75 mg kg-1, i.p.) disrupted acquisition of a one-trial 'step through' passive-avoidance response. Pretreatment with DAU 6215 (1, 10, 30 and 100 micrograms kg-1, i.p.) antagonized this deficit induced by scopolamine, with a bell-shaped dose-response curve. Scopolamine (0.75 mg kg-1, i.p.) produced a significant increase in locomotor activity which was unaffected by pretreatment with DAU 6215 (10 and 30 micrograms kg-1, i.p.). The present results further support the suggestion that 5-HT3-receptor antagonists may prevent the memory disturbance caused by a reduction in central cholinergic function in the rat. The inefficacy shown by DAU 6215 on hyperactivity induced by scopolamine appears to rule out the possibility of a pharmacokinetic interference between DAU 6215 and scopolamine.

Animals↗
PubMed2001

Scopolamine nasal spray in motion sickness: a randomised, controlled, and crossover study for the comparison of two scopolamine nasal sprays with oral dimenhydrinate and placebo.

Scopolamine has been used successfully for treatment of motion sickness for almost a century and the nasal administration was first studied 50 years ago. However, there never appeared a nasal dosage form. Finally, after finding a stable and suitable formulation for scopolamine, a study to investigate efficacy, safety, and tolerability was conducted, with a randomised, double-blind, double-dummy, crossover, Latin square design including placebo control and a placebo/placebo control for internal validity at the German Air Force Institute of Aviation Medicine. To assess the efficacy of a new, stable and well-tolerated formulation of scopolamine nasal spray the reproducible induction of whole body vibrations by a rotating chair was chosen and a validated seasickness score (SKS). The reduction of SKS showed that scopolamine nasal spray at a concentration of 0.2% was statistically superior to both placebo and dimenhydrinate (P=0.003 and 0.004, respectively). There were no signs for a nasal or epipharyngeal irritation of the mucous membrane. Scopolamine nasal spray was found to be an effective and safe treatment in motion sickness, with a fast onset of action within 30 min after administration.

Administration, Inhalation↗
PubMed1985

[Transdermal scopolamine (TTS-scopolamine) for the prevention of postoperative nausea and vomiting].

Parenteral scopolamine lost its significance for premedication because of severe side effects, at least in German speaking countries. The drug is now available as a transdermal therapeutic system (TTS-Scopolamine) which provides constant low plasma concentrations for three days, high enough to act as an antiemetic but low enough to be free from severe side effects. In a double blind study against TTS-Placebo TTS-Scopolamine was investigated in 40 patients, undergoing minor gynecological surgery. The anaesthetic procedure was standardized with alfentanil, etomidate, N2O and, if needed, Ethrane, drugs which have a moderate to strong emetic action. The premedication consisted of Flurazepam (evening) and diazepam (morning). The dosages were standardized. TTS-scopolamine was statistically significantly superior to TTS-placebo with respect to the antiemetic action and the judgment by the anaesthetist. Intraoperative complications such as thoracic rigidity and bradycardia were more frequent in the placebo group. There were no severe side effects. TTS-scopolamine can be recommended as an antiemetic for premedication, especially when benzodiazepines are used for the relief of anxiety. It should be administered on the evening before and can be removed one or two days after surgery.

Administration, Topical↗
PubMed2005

Pharmacokinetics and pharmacodynamics in clinical use of scopolamine.

The alkaloid L-(-)-scopolamine [L-(-)-hyoscine] competitively inhibits muscarinic receptors for acetylcholine and acts as a nonselective muscarinic antagonist, producing both peripheral antimuscarinic properties and central sedative, antiemetic, and amnestic effects. The parasympatholytic scopolamine, structurally very similar to atropine (racemate of hyoscyamine), is used in conditions requiring decreased parasympathetic activity, primarily for its effect on the eye, gastrointestinal tract, heart, and salivary and bronchial secretion glands, and in special circumstances for a CNS action. Therefore, scopolamine is most suitable for premedication before anesthesia and for antiemetic effects. This alkaloid is the most effective single agent to prevent motion sickness. Scopolamine was the first drug to be made commercially available in a transdermal therapeutic system (TTS-patch) delivering alkaloid. Recently, pharmacokinetic data on scopolamine in different biozlogic matrices were obtained most efficiently using liquid chromatographic-tandem mass spectrometric (LC-MS/MS) or gas chromatography online coupled to mass spectrometry. Pharmacokinetic parameters are dependent on the dosage form (oral dose, tablets; parenteral application; IV infusion; SC and IM injection). Scopolamine has a limited bioavailability if orally administered. The maximum drug concentration occurs approximately 0.5 hours after oral administration. Because only 2.6% of nonmetabolized L-(-)-scopolamine is excreted in urine, a first-pass metabolism is suggested to occur after oral administration of scopolamine. Because of its short half-life in plasma and dose-dependent adverse effects (in particular hallucinations and the less serious reactions, eg, vertigo, dry mouth, drowsiness), the clinical use of scopolamine administered orally or parenterally is limited. To minimize the relatively high incidence of side effects, the transdermal dosage form has been developed. The commercially available TTS-patch contains a 1.5-mg drug reservoir and a priming dose (140 microg) to reach the steady-state concentration of scopolamine quickly. The patch releases 0.5 mg alkaloid over a period of 3 days (releasing rate 5 microg/h). Following the transdermal application of scopolamine, the plasma concentrations of the drug indicate major interindividual variations. Peak plasma concentrations (Cmax) of approximately 100 pg/mL (range 11-240 pg/mL) of the alkaloid are reached after about 8 hours and achieve steady state. During a period of 72 hours the plaster releases scopolamine, so constantly high plasma levels (concentration range 56-245 pg/mL) are obtained, followed by a plateau of urinary scopolamine excretion. Although scopolamine has been used in clinical practice for many years, data concerning its metabolism and the renal excretion in man are limited. After incubation with beta-glucuronidase and sulfatase, the recovery of scopolamine in human urine increased from 3% to approximately 30% of the drug dose (intravenously administered). According to these results from enzymatic hydrolysis of scopolamine metabolites, the glucuronide conjugation of scopolamine could be the relevant pathway in healthy volunteers. However, scopolamine metabolism in man has not been verified stringently. An elucidation of the chemical structures of the metabolites extracted from human urine is still lacking. Scopolamine has been shown to undergo an oxidative demethylation during incubation with CYP3A (cytochrome P-450 subfamily). To inhibit the CYP3A located in the intestinal mucosa, components of grapefruit juice are very suitable. When scopolamine was administered together with 150 mL grapefruit juice, the alkaloid concentrations continued to increase, resulting in an evident prolongation of tmax (59.5 +/- 25.0 minutes; P < 0.001). The AUC0-24h values of scopolamine were higher during the grapefruit juice period. They reached approximately 142% of the values associated with the control group (P < 0.005). Consequently, the related absolute bioavailabilities (range 6% to 37%) were significantly higher than the corresponding values of the drug orally administered together with water (range 3% to 27%). The effect of the alkaloid on quantitative electroencephalogram (qEEG) and cognitive performance correlated with pharmacokinetics was shown in studies with healthy volunteers. From pharmacokinetic-pharmacodynamic modeling techniques, a direct correlation between serum concentrations of scopolamine and changes in total power in alpha-frequency band (EEG) in healthy volunteers was provided. The alkaloid readily crosses the placenta. Therefore, scopolamine should be administered to pregnant women only under observation. The drug is compatible with nursing and is considered to be nonteratogenic. In conclusion, scopolamine is used for premedication in anesthesia and for the prevention of nausea and vomiting associated with motion sickness. Pharmacokinetics and pharmacodynamics of scopolamine depend on the dosage form. Effects on different cognitive functions have been extensively documented.

Humans↗
PubMed2004

Scopolamine for preventing and treating motion sickness.

BACKGROUND: Motion sickness - the discomfort experienced when perceived motion disturbs the organs of balance - may include symptoms such as nausea, vomiting, pallor, cold sweats, hypersalivation, hyperventilation and headaches. The control and prevention of these symptoms have included pharmacological, behavioural and complementary therapies. Although scopolamine has been used in the treatment and prevention of motion sickness for decades, there have been no systematic reviews of its effectiveness. OBJECTIVES: To assess the effectiveness of scopolamine versus no therapy, placebo, other drugs, behavioural and complementary therapy or two or more of the above therapies in combination for motion sickness in persons (both adults and children) without known vestibular, visual or central nervous system pathology. SEARCH STRATEGY: The Cochrane Ear, Nose and Throat Disorders Group Specialised Register, the Cochrane Central Register of Controlled Trials (The Cochrane Library, Issue 4, 2003), MEDLINE (OVID, 1966 to March Week 1 2004), EMBASE (1974 to 2004) CINAHL (Ovid, 1982 to March Week 1 2004) and reference lists of retrieved studies were searched for relevant studies. No language restrictions were applied. SELECTION CRITERIA: All parallel-arm, randomised controlled trials (RCTs) focusing on scopolamine versus no therapy, placebo, other drugs, behavioural and complementary therapy or two or more of the above therapies in combination were included. Outcomes relating to the prevention of onset or treatment of clinically-defined motion sickness, task ability and psychological tests, changes in physiological parameters and adverse effects were considered. DATA COLLECTION AND ANALYSIS: Data from the studies were extracted independently by two authors using standardised forms. Study quality was assessed. Dichotomous data were expressed as odds ratio (OR) and a pooled OR was calculated using the random effects model. MAIN RESULTS: Of 27 studies considered potentially relevant, 12 studies enrolling 901 subjects met the entry criteria. Scopolamine was administered via transdermal patches, tablets or capsules, oral solutions or intravenously. Scopolamine was compared against placebo, calcium channel antagonists, antihistamine, meth-scopolamine or a combination of scopolamine and ephedrine. Studies were generally small in size and of varying quality. Scopolamine was more effective than placebo in the prevention of symptoms. Comparisons between scopolamine and other agents were few and suggested that scopolamine was superior (versus meth-scopolamine) or equivalent (versus antihistamines) as a preventative agent. Evidence comparing scopolamine to cinnarizine or combinations of scopolamine and ephedrine is equivocal or minimal. Although sample sizes were small, scopolamine was no more likely to induce drowsiness, blurring of vision or dizziness compared to other agents. Dry mouth was more likely with scopolamine than with meth-scopolamine or cinnarizine. No studies were available relating to the therapeutic effectiveness of scopolamine in the management of established symptoms of motion sickness. REVIEWERS' CONCLUSIONS: The use of scopolamine versus placebo in preventing motion sickness has been shown to be effective. No conclusions can be made on the comparative effectiveness of scopolamine and other agents such as antihistamines and calcium channel antagonists. In addition, no randomised controlled trials were identified that examined the effectiveness of scopolamine in the treatment of established symptoms of motion sickness.

Humans↗