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PubMed2000

Scopolamine inhibits cocaine-conditioned but not unconditioned stimulant effects in mice.

RATIONALE: In animal models, cocaine cues contribute to the development of conditioned responses to the psychomotor stimulating and rewarding effects of the drug. OBJECTIVES: In the present study we investigated the effect of scopolamine, known to impair learning and memory, on cocaine-induced conditioned and unconditioned responses in Swiss Webster mice. METHODS: In the first experiment, mice were treated with saline/saline, saline/cocaine (20 mg/kg), scopolamine (1.0 mg/kg)/cocaine, or scopolamine/saline for 5 days. The treatments were paired with the locomotor activity test cage twice, on days 1 and 5. This allowed to determine: (a) the induction and expression of place-dependent sensitization (PDS) to the psychomotor-stimulating effect of cocaine and (b) place-dependent hyperlocomotion (PDH; i.e., conditioning) as defined by the response to saline injection in the test cage. In the second experiment, all injections were delivered in animals' home cage in order to induce place-independent sensitization (PIS) to cocaine and to avoid the development of PDH. In the third experiment, the effect of scopolamine (1.0 mg/kg) on the acquisition of cocaine-induced conditioned place preference (CPP) was investigated. RESULTS: Data from the first experiment suggest that pretreatment with scopolamine had no specific effect on the induction and expression of cocaine-induced PIS. However, scopolamine blocked cocaine-induced PDH. Results from the second experiment confirmed that scopolamine had no effect on the induction of PIS to cocaine. Results from the third experiment showed that scopolamine completely blocked cocaine-induced CPP. CONCLUSIONS: The finding that scopolamine blocked the conditioned behaviors, PDH and CPP, that develop after exposure to cocaine supports the hypothesis that cocaine cue reactivity in the paradigms tested is associated with learning and memory.

Animals↗
PubMed1998

Effects of the potassium channel blockers, apamin and 4-aminopyridine, on scopolamine-induced deficits in the delayed matching to position task in rats: a comparison with the cholinesterase inhibitor E2020.

The effects of the muscarinic antagonists, scopolamine HBr and MeBr, a cholinesterase inhibitor, E2020, and K+ channel blockers, 4-aminopyridine (4-AP) and apamin, on the performance of rats in a delayed matching to position (DMTP) task were examined. The percentage of correct choices (choice accuracy), number of trials completed and intertrial intervals were measured. Discriminability and response bias were also calculated, using signal detection analysis. Scopolamine HBr (0.1 mg/kg), but not scopolamine MeBr (0.1 mg/kg), significantly and consistently reduced the choice accuracy and discriminability, but neither affected the other measurements. E2020 (0.03-1.0 mg/kg) had no effect on the baseline performance in the DMTP task, but at 1.0 mg/kg, it significantly attenuated the deficits in choice accuracy induced by scopolamine. 4-AP (0.001-0.1 mg/kg) had no effect on either baseline performance or deficits induced by scopolamine. Apamin (0.1-0.4 mg/kg) had no effect on choice accuracy and discriminability. Apamin also failed to attenuate the scopolamine-induced deficits. When administered in combination with scopolamine, apamin at 0.4 mg/kg significantly decreased the number of trials completed and increased the intertrial interval relative to that of the control group. Taken together, these results demonstrate that K+ channel blockers (4-AP and apamin), unlike a cholinesterase inhibitor (E2020), fail to reverse the scopolamine-induced deficits in the DMTP task.

4-Aminopyridine↗
PubMed1976

Scopolamine: effects on fear or defense responses in the rat.

In previous research scopolamine reduced fear or defense responses of rats to a cat, and removal of the rats' olfactory bulbs had the same effect. This suggested that scopolamine might have affected defense responses by blocking olfactory perception of the stimulus cat. The present experiments studied this possibility and explored further the effects of scopolamine on defense responses of the hooded rat. In Experiment 1 rats treated with scopolamine were found to be responsive to olfactory cues from a cat. When cat smell, but not a cat, was present in the apparatus, scopolamine-treated rats showed a large and significant suppression of food consumption. In Experiment 2 the effects of scopolamine on defense responses were shown to be generalizable to an inanimate stimulus, mechanical robot. Scopolamine caused significantly less freezing and avoidance and significantly shorter latencies to drink in the presence of the robot. One of the primary findings of the present research is that scopolamine has now been shown to reduce the defensive response of freezing in a variety of stimulus situations. This finding was thought to have important implications for the literature relating anticholinergic drugs and avoidance behavior.

Animals↗
PubMed1994

Repeated scopolamine injections sensitize rats to pilocarpine-induced vacuous jaw movements and enhance striatal muscarinic receptor binding.

This experiment was conducted to determine if repeated administration of the muscarinic antagonist scopolamine could increase pilocarpine-induced vacuous jaw movements and also enhance muscarinic receptor binding. Rats received daily injections of either scopolamine (0.5 mg/kg IP) or saline for 14 days. On day 15 rats received no injections of scopolamine, but did receive injections of pilocarpine (1.0, 2.0 or 4.0 mg/kg IP) or saline. After administration of pilocarpine or saline, all rats were observed for vacuous jaw movements and rearing behavior. The day after pilocarpine injections, rats were sacrificed and samples of tissue from the lateral neostriatum were removed to assess muscarinic receptor binding using 3H-QNB as the ligand. Analyses of the vacuous jaw movement data indicated that there was a significant dose-related increase in vacuous jaw movements induced by pilocarpine, and also that there was a significant enhancement of pilocarpine-induced vacuous jaw movements in rats pretreated with repeated scopolamine injections. There was not a significant scopolamine x pilocarpine interaction, suggesting that pretreatment with scopolamine produced an apparent parallel shift in the pilocarpine dose-response curve. Pilocarpine significantly suppressed rearing behavior, and scopolamine pretreatment significantly enhanced the suppression of rearing produced by pilocarpine. Analysis of the receptor binding data indicated that there was a significant increase in the number of muscarinic receptor sites (Bmax) in rats that received repeated scopolamine injections as compared to saline-treated rats.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1992

Cholinergic blockade with scopolamine in adult cats. Effects on the behaviors evoked by apomorphine and amphetamine.

1. The aim of this work is to analyse the role that the cholinergic system could play in the production of the behaviors evoked by apomorphine and amphetamine in adult cats. These two drugs were injected s.c. in separate sessions, before and after a s.c. administration of scopolamine which blocked the muscarinic receptors. The pre and post-scopolamine results of the behaviors produced by the two catecholaminergic drugs were compared using the non-parametric Wilcoxon signed rank test. 2. In a previous step a dose-response study of the behavioral effects of scopolamine, in doses of 0.05, 0.1, 0.4 and 0.8 mg/kg was carried out in ten cats. The Kruskal-Wallis and the non-parametric multiple comparison tests were employed. A dose-dependent decrease in motility (locomotion) and a dose-dependent increase in inappetence and pupillary dilation were found. 3. In thirteen cats which were injected with 2 mg/kg of apomorphine and 2.5 mg/kg of amphetamine the findings were: 1--apomorphine after scopolamine produced a decrease in the hypermotility, compared with the results observed with the former drug previous to scopolamine; 2--with amphetamine an increase in immobility and a decrease in indifference were observed. 4. The authors conclude that the decrease in motility recorded with apomorphine and amphetamine after scopolamine, could be attributed to the proper effect of scopolamine. No explanation could be found for the decrease in indifference found by injecting amphetamine after scopolamine. 5. Considering the antagonistic effect between the dopaminergic and the cholinergic systems and that the latter one has an arousal effect, we postulate that the behavioral indifference produced by apomorphine and amphetamine could be the result of a kind of blockade of the cholinergic system when the catecholaminergic system is activated through the administration of the two cited drugs.

Amphetamine↗
PubMed1994

Dopaminergic and muscarinic regulation of striatal enkephalin and substance P messenger RNAs following striatal dopamine denervation: effects of systemic and central administration of quinpirole and scopolamine.

Striatal dopamine depletion produces an increase in enkephalin and a decrease in substance P messenger RNAs. Subsequent systemic administration of either the D2 dopamine agonist, quinpirole, or the muscarinic antagonist, scopolamine, results in the reduction of the lesion-induced elevation in striatal enkephalin messenger RNA. These changes in enkephalin messenger RNA levels may be mediated solely within the striatum or through trans-synaptic circuits involving the striatum. To dissociate these possibilities, we have compared the effects of systemic and central administration of quinpirole and scopolamine on striatal enkephalin and substance P messenger RNAs using in situ hybridization histochemistry. Systemic administration of both quinpirole and scopolamine blocked the elevation of striatal enkephalin messenger RNA normally observed in 6-hydroxydopamine-lesioned rats. In addition, high doses of systemic scopolamine (25 and 50 mg/kg per day) prevented the lesion-induced decrease in striatal substance P messenger RNA levels. In order to determine whether the effects of these drugs are mediated directly within the striatum, central administration of quinpirole and scopolamine were compared. In contrast to systemic administration, intraventricular and intrastriatal infusion of quinpirole but not scopolamine prevented the lesion-induced change in striatal enkephalin messenger RNA. However, neither quinpirole nor scopolamine administered centrally affected the level of substance P messenger RNA in the striatum of 6-hydroxydopamine-induced lesioned animals. Together, these data suggest that changes in D2 receptor activation directly in the striatum are responsible for the effects of quinpirole on enkephalin messenger RNA. In contrast, the effect of systemic scopolamine on striatal enkephalin and substance P messenger RNAs may not be mediated within the striatum.

Animals↗
PubMed2005

Play behavior in rats pretreated with scopolamine: increased play solicitation by the non-injected partner.

Play behavior was assessed in juvenile rat pups following chronic administration of scopolamine (0.5 or 1.0 mg/kg, i.p.) to one partner in each dyad of rats. Scopolamine administration significantly reduced the number of pins and mean pin duration of both playmates in pairs where only one rat was injected with scopolamine (irrespective of dose). However, dorsal contacts were significantly increased in rats exposed to a play partner that had been injected with scopolamine, indicating an increase in play solicitation when the partner was rendered non-responsive with this drug. These effects were stable and consistent over the course of 15 days of repeated testing in the presence of scopolamine. In other words, normal animals did not extinguish play solicitation even after prolonged periods of non-reciprocity. Upon cessation of drug treatment, play behavior returned largely to normal in both animals. Overall locomotor activity levels were significantly reduced in pairs where one rat had been injected with scopolamine. Together, these data suggest that the effects of repeated scopolamine are acute in nature, and that disruption of normal play behavior following chronic scopolamine treatment does not produce long-term impairments in social play behavior beyond acute action of the drug.

Analysis of Variance↗
PubMed2001

Comparative effects of scopolamine and quinpirole on the striatal fos expression induced by stimulation of D(1) dopamine receptors in the rat.

Treatment of intact rats with the full D(1) dopamine agonist A-77636 induced Fos-like immunoreactivity in the medial and, to a lesser extent, the lateral portions of the striatum. Pretreatment with the muscarinic antagonist scopolamine hydrobromide (1.5-6 mg/kg) potentiated the response to A-77636 and eliminated the mediolateral staining gradient seen after A-77636 alone. Similar effects were not produced by scopolamine methylbromide, which fails to cross the blood-brain barrier, demonstrating that the actions of scopolamine were centrally mediated. The effects of scopolamine were further compared to those of the D(2)-like dopamine agonist quinpirole using a factorial design in which subjects were pretreated with either scopolamine, quinpirole, or a combination of the two drugs before receiving A-77636. Pretreatment with either scopolamine or quinpirole increased staining in the lateral striatum, but the combination of the two drugs was no more effective than was quinpirole alone. Pretreatment with quinpirole, but not scopolamine, resulted in a markedly "patchy" pattern of staining and actually suppressed staining in the region between patches in the medial striatum. These findings demonstrate that there are both differences and similarities between the effects of scopolamine and quinpirole on D(1) agonist-induced Fos expression and suggest that although inhibition of cholinergic neurons may be one of the mechanisms through which the effects of quinpirole are produced, other factors must also contribute.

Adamantane↗
PubMed1997

Effect of combinations of insulin, glucose and scopolamine on radial arm maze performance.

Previous research has shown that glucose is an effective agent in facilitating memory performance and in attenuating scopolamine-induced amnesia. Although insulin has not been shown to facilitate unimpaired memory, a previous study has demonstrated that insulin can also attenuate scopolamine-degraded memory. The present study was designed to determine how different combinations of insulin, glucose and scopolamine affect memory. It involved nine rats whose memory was assessed through performance in a win-shift radial arm maze task under different drug treatments. A 2 x 2 x 2 (insulin x glucose x scopolamine) within-subjects design with a 5-h drug test interval was employed. Scopolamine disrupted memory performance, and both glucose and insulin counteracted this disruption. Combining the glucose and insulin treatments did not increase their ability to attenuate scopolamine deficits but slightly decreased this effect. Glucose tended to enhance memory, even in the absence of scopolamine, whereas insulin had no effect on memory in the absence of scopolamine. Blood glucose levels were measured and did not indicate changes caused by drug treatments. The memory effects may have been due to the acetylcholine-agonist actions of glucose and insulin, an interpretation consistent with previous research findings.

Animals↗
PubMed1988

Scopolamine amnesia of passive avoidance: a deficit of information acquisition.

Despite its increasing use as an animal model of memory deficit in human dementia, relatively few studies have attempted to assess the memory processes involved in the anticholinergic-induced impairment of passive avoidance retention. In the present experiments, the influence of scopolamine administered prior to or immediately following training on 24-h retention of step-through passive avoidance was studied in NMRI mice. In low doses (0.3-3.0 mg/kg ip) pretraining administration (-5 min) of scopolamine induced a very strong amnesia. Post-training scopolamine induced a significant effect only at the highest dose tested (30 mg/kg). In a retention test of longer than normal duration (600 vs 180 s), which resulted in a more favorable comparison value in the control group, an intermediate post-training dose (10 mg/kg) induced a small effect which approached significance; a finding which may account for conflicting reports in the literature concerning the ability of scopolamine to induce a post-training deficit. The pretraining effect does not appear to have been solely the result of state-dependent learning; scopolamine (3 mg/kg) administered before both the training and test sessions induced a deficit of approximately the same magnitude as that found when administered before training or before testing only. The results indicate that scopolamine can induce a small post-trial effect, presumably through an influence on consolidation processes. The much larger effect of pretrial scopolamine, however, indicates a primary influence on processes related to information acquisition. Together with findings from the literature, the present experiments suggest that scopolamine-induced amnesia partially, but not completely, models the memory deficits of human dementia.

Animals↗
PubMed1997

Effects of low-dose transdermal scopolamine on autonomic cardiovascular control in healthy young subjects.

We studied how posture influences the effects of transdermal scopolamine on autonomic cardiovascular regulation in a randomized, double-blind, placebo-controlled crossover study of 10 healthy young volunteers. We recorded the electrocardiogram and auscultatory sphygmomanometric and continuous non-invasive finger arterial pressure (Finapres device) to obtain signals for the beat-by-beat R-R interval and systolic, mean and diastolic pressures. R-R interval and arterial pressure variabilities were characterized by power spectral analysis. Scopolamine increased the mean R-R intervals and reduced arterial pressure in both the supine and the standing positions, but did not affect blood pressure variability. Scopolamine increased the total variability of R-R interval and its mid- (0.07-0.15 Hz) and high- (0.15-0.40 Hz) frequency band power in the standing position during controlled breathing at 0.25 Hz. In the supine position, scopolamine did not affect R-R interval variability. In the deep breathing test, scopolamine increased the maximal expiratory-inspiratory R-R interval ratio. This study showed that low-dose scopolamine increases vagal cardiac inhibition in both supine and standing positions in healthy volunteers. However, scopolamine increases heart rate variability only in the standing position during partial vagal withdrawal. The study also demonstrates that transdermal scopolamine decreases blood pressure in healthy young subjects.

Administration, Cutaneous↗
PubMed1990

Transdermal scopolamine reduces nausea and vomiting after outpatient laparoscopy.

The authors evaluated the effect of transdermal scopolamine on the incidence of postoperative nausea, retching, and vomiting after outpatient laparoscopy in a double-blind, placebo-controlled study. A Band-Aid-like patch containing either scopolamine or placebo was placed behind the ear the night before surgery. Anesthesia was induced with fentanyl (0.5-2 micrograms/kg iv), thiopental (3-5 mg/kg iv), and succinylcholine (1-1.5 mg/kg iv) and maintained with isoflurane (0.2-2%) and nitrous oxide (60%) in oxygen. Scopolamine-treated patients had less nausea, retching, and vomiting compared with placebo-treated patients (P = 0.0029). Severe nausea and/or vomiting was present in 62% of the placebo group but only 37% of those getting the scopolamine patch. Repeated episodes of retching and vomiting were also less frequent in the scopolamine group compared with the placebo group (23% vs. 41%; P = 0.0213) as was the need for additional antiemetic therapy (13% vs. 32%; P = 0.0013). Patients in the scopolamine group were also discharged from the hospital sooner (4 +/- 1.3 vs. 4.5 +/- 1.5 h; P = 0.0487). Side effects were more frequent among those patients treated with the scopolamine patch (91% vs. 45%; P less than 0.05) but were not troublesome. The authors conclude that transdermal scopolamine is a safe and effective antiemetic for outpatients undergoing laparoscopy.

Administration, Cutaneous↗
PubMed1994

Scopolamine improves autonomic balance in advanced congestive heart failure.

BACKGROUND: Sympathetic hyperactivity and parasympathetic withdrawal in patients with congestive heart failure correlate closely with disease severity and overall survival. The modulating effects of drugs on the autonomic dysfunction may contribute to improve survival. Low-dose scopolamine has a vagomimetic effect in normal subjects and patients after acute myocardial infarction. We assessed whether transdermal scopolamine would increase vagal activity in patients with congestive heart failure. METHODS AND RESULTS: Heart rate variability was assessed at baseline, 24 hours after one patch of transdermal scopolamine, and 48 hours after scopolamine withdrawal in 21 patients with moderate to severe heart failure. Scopolamine increased both time- and frequency-domain parameters of heart rate variability. Specifically, the mean RR interval and its SD increased by 5.5% (P < .001) and 45% (P < .001), respectively. The change remained significant when corrected for mean heart rate with a 39% (P < .01) increase of the coefficient of variation. The absolute power of the high-frequency component was also significantly augmented. All the parameters returned to baseline after scopolamine withdrawal. Individual analysis showed that in the 7 patients in whom scopolamine did not increase mean RR interval, heart rate variability did not change. CONCLUSIONS: Transdermal scopolamine increases vagal activity as assessed by heart rate variability in patients with congestive heart failure. This autonomic modulation does not occur in all patients and can be predicted by RR interval changes. Whether such restoration of the autonomic balance might have beneficial effects in the long-term management of patients with congestive heart failure remains to be determined.

Administration, Cutaneous↗
PubMed1978

The involvement of catecholamine in scopolamine-induced locomotor activation and rotational behaviour in mice.

Scopolamine-induced locomotor activation was studied in comparison with the responses to apomorphine and methamphetamine in mice. The responses to scopolamine and methamphetamine were markedly depressed by the pretreatment with the catecholamine synthesis inhibitor, alpha-methyl-p-tyrosine, while the activation response to apomorphine was not affected. p-Chlorophenylalanine did not affect the response to scopolamine. Phenoxybenzamine reduced the responses to scopolamine and methamphetamine, but did not affect the apomorphine response. Propranolol did not affect the responses to the three agonists, scopolamine, apomorphine and methamphetamine. Antipsychotic drugs haloperidol and pimozide reduced the responses to the three agonists. Haloperidol was especially effective in this regard. These results suggest the involvement of catecholamine in the locomotor activation produced by scopolamine. In the rotational behaviour model which is sensitive to dopamine receptor stimulating agents, effects of the three agonists were studied. Scopolamine produced the ipsilateral rotation in mice with unilateral striatal 6-hydroxydopamine-induced lesions. Methamphetamine induced the ipsilateral rotation, while apomorphine produced the contralateral rotation. The rotations induced by three agaonists were suppressed by pimozide. The results indicate the participation of dopamine in the scopolamine-induced rotational behaviour in mice.

Animals↗
PubMed2006

Transdermal scopolamine for prevention of motion sickness : clinical pharmacokinetics and therapeutic applications.

A transdermal therapeutic system for scopolamine (TTS-S) was developed to counter the adverse effects and short duration of action that has restricted the usefulness of scopolamine when administered orally or parenterally. The plaster contains a reservoir of 1.5 mg of scopolamine programmed to deliver 0.5 mg over a 3-day period. A priming dose (140 microg) is incorporated into the adhesive layer to saturate certain binding sites within the skin and to accelerate the achievement of steady-state blood levels. The remainder is released at a constant rate of approximately 5 microg/hour. The protective plasma concentration of scopolamine is estimated to be 50 pg/mL. TTS-S attains that concentration after 6 hours; a steady state of about 100 pg/mL is achieved 8-12 hours after application. Yet 20-30% of subjects failed to attain the estimated protective concentration, and plasma concentrations measured in subjects who failed to respond to TTS-S were lower than in responders. These findings may explain some of the treatment failures. Overall, the product appears to be the approximate functional equivalent of a 72-hour slow intravenous infusion. A combination of transdermal and oral scopolamine (0.3 or 0.6 mg) was effective and well tolerated in producing desired plasma concentrations 1-hour post-treatment. TTS-S has proved to be significantly superior to placebo in reducing the incidence and severity of motion sickness by 60-80%. It was more effective than oral meclizine or cinnarizine, similar to oral scopolamine 0.6 mg or promethazine plus ephedrine, and the same as or superior to dimenhydrinate. The addition of ephedrine or the use of two patches did not improve its efficacy, but rather increased the rate of adverse effects. TTS-S was most effective against motion sickness 8-12 hours after application. Despite previous evidence to the contrary, a recent bioavailability study demonstrated similar intraindividual absorption and sustained clinical efficacy with long-term use of the drug. The adverse effects produced by TTS-S, although less frequent, are qualitatively typical of those reported for the oral and parenteral formulations of this agent. Dry mouth occurs in about 50-60% of subjects, drowsiness in up to 20%, and allergic contact dermatitis in 10%. Transient impairment of ocular accommodation has also been observed, in some cases possibly the result of finger-to-eye contamination. Low-dose pyridostigmine was found effective in preventing cycloplegia but not mydriasis. Adverse CNS effects, including toxic psychosis (mainly in elderly and paediatric patients), have been reported only occasionally, as have difficulty in urinating, headache, rashes and erythema. Adverse effects were not correlated with plasma scopolamine concentrations. TTS-S produced only about half the incidence of drowsiness caused by oral dimenhydrinate or cinnarizine, and a level of adverse effects similar to that found with oral meclizine. Performance is not affected by short-term use. Prolonged or repeated application may cause some impairment of memory storage for new information. However, sea studies revealed significantly less reports of a decrement in performance or drowsiness due to prevention of sea sickness. The recommended dosage is a single TTS-S patch applied to the postauricular area at least 6-8 hours before the anti-motion sickness effect is required. For faster protection, the patch may be applied 1 hour before the journey in combination with oral scopolamine (0.3 or 0.6 mg). After 72 hours, the patch should be removed and a new one applied behind the opposite ear. Its place in therapy is mainly on long journeys (6-12 hours or longer), to avoid repeated oral doses, or when oral therapy is ineffective or intolerable.

Administration, Cutaneous↗
PubMed2001

Scopolamine bioavailability in combined oral and transdermal delivery.

Transdermal therapeutic system scopolamine (TTS-S) is effective in preventing motion sickness for 72 h. However, by this route a prophylactic effect is obtained 6 to 8 h postapplication. By the oral route, scopolamine is effective within 0.5 h for a period of 6 h. To achieve safe as well as effective protection against seasickness during the first hours of a voyage until the TTS-S patch takes effect, the pharmacokinetics of scopolamine was investigated after patch application in combination with oral tablets, 0.6 mg, 0. 3 mg, or placebo. Subjects were 25 naval-crew volunteers, randomly divided into three groups: group 1 (n = 9), TTS-S patch + 0.6 mg of scopolamine per os (p.o.); group 2 (n = 8), TTS-S patch + 0.3 mg of scopolamine p.o.; and group 3 (n = 8), TTS-S patch + placebo tablet. Blood samples were collected before treatment and 0.5, 1, 1.5, 2.5, 3.5, 6, 8, and 22 h post-treatment, and were analyzed for scopolamine levels using radioreceptor assay. Significantly higher plasma scopolamine levels were found in group 1 at 0.5, 1, 1.5, and 2.5 h, and in group 2 at 1 and 1.5 h post-treatment, compared with group 3. Thereafter, plasma levels did not differ significantly between the groups. In all subjects of group 1 and seven subjects (88%) of group 2, therapeutic levels (>50 pg/ml) were measured during the first 2.5 h, compared with only two subjects (25%) of group 3 (P < 0.05). Heart rate, blood pressure, visual accommodation, performance test results, and subjective complaints of adverse effects did not differ significantly. The combination of transdermal and oral scopolamine (0.3 or 0.6 mg) provides the required plasma levels to prevent seasickness, starting as early as 0.5 h post-treatment, with no significant adverse effects.

Accommodation, Ocular↗
PubMed2006

[Effects of midazolam on muscarinic receptor of brain in healthy and scopolamine-treated rats].

OBJECTIVE: To investigate the recent and permanent effects of pretreatment with midazolam on muscarinic receptor of brain in healthy and scopolamine-treated rats. METHODS: (1) In recent effect group, thirty-eight male SD rats were randomly divided into 4 groups: control group (Con, n=9), midazolam group (Mid, n=9), scopolamine group (Sco, n=10), midazolam+scopolamine group (Mid+sco, n=10). On the 1st, 2nd, and 3rd days, Mid group and Mid+sco groups were treated with intraperitoneal injection of 50 mg/kg midazolam per day while Con group and Sco group were treated with intraperitoneal injection of the same voluminal physiological saline per day. On the 4th, 5th, and 6th days, Scopolamine 0.8 mg/kg intraperitoneal injection per day was administered in Sco group and Mid+sco group while same voluminal physiological saline was administered in Con group and Mid group. (2) In permanent effect group, thirty-six male SD rats were randomly divided into 4 groups: control group (Con, n=9), midazolam group (Mid, n=9), scopolamine group (Sco, n=9), midazolam+scopolamine group (Mid+sco, n=9). On the 1st, 2nd, and 3rd days, Mid group and Mid+sco group were treated with intraperitoneal injection of 50 mg/kg midazolam per day while Con group and Sco group were treated with intraperitoneal injection of the same voluminal physiological saline per day. On the 10th, 11th, and 12th days, Scopolamine 0.8 mg/kg intraperitoneal injection per day was administered in Sco group and Mid+sco group while the same voluminal physiological saline was administered in Con group and Mid group. (3)Then the rats was decapitated and the cerebra cortex and hippocampus were removed. The binding capacity of muscarinic receptor with [3H] QNB were determined. Bmax and Kd of muscarinic receptor in hippocampus were determined by Scatchard analysis in recent effect group. RESULTS: (1) In recent effect group: the binding capacity of muscarinic receptor in hippocampus was significantly higher in Con group than in Mid group, Sco group and Mid+sco group (P<0.01), which was also higher in Mid group than in Sco group (P<0.05) and Mid+sco group (P<0.01), higher in sco group than in Mid+sco group (P<0.01). Kd of muscarinic receptor in hippocampus in Sco group and Mid group were higher than in Con group and Mid+sco group (P<0.01). Bmax of muscarinic receptor in hippocampus was significantly higher in Con group than in Mid group (P<0.05), Sco group and Mid+sco group (P<0.01), which was also higher in Mid group than in Sco group and Mid+sco group (P<0.01), higher in sco group than in Mid+sco group (P<0.05). There was no significant difference of the binding capacity of muscarinic receptor in cortex. (2) In permanent effect group: the binding capacity of muscarinic receptor in hippocampus was significantly higher in Con group and Mid group than in Sco group and Mid+sco group (P<0.01). There was no significant difference of the binding capacity of muscarinic receptor in cortex. CONCLUSION: Pretreatment with intraperitoneal injection of 50 mg/kg midazolam for three days had no effect on muscarinic receptor of cortex, but could induce the binding capacity of muscarinic receptor with [3H] QNB and change the density and affinity of muscarinic receptor in hippocampus in healthy and scopolamine-treated rats, yet the changes were not permanent.

Animals↗
PubMed1991

Hyperbaric oxygen and scopolamine.

Scopolamine (Hyoscine), an anticholinergic compound is widely used for the prophylaxis and treatment of motion sickness and might be used with oxygen diving and hyperbaric oxygen therapy. We therefore decided to test the interaction of scopolamine with oxygen at high pressure. Thirty-six rats implanted with cortical EEG electrodes were injected subcutaneously with two doses of scopolamine (0.02 or 0.2 mg.kg-1), or the vehicle (saline), 30 min before exposure to 5 atm abs (0.5 MPa) oxygen. Electroencephalogram and heart rate were monitored continuously. Spectral analysis of the EEG was carried out, and the duration of the latent period before convulsions was determined. No significant difference was found in the duration of the latent period between the control rats receiving vehicle (saline) and rats injected with scopolamine (n = 12 for each group). Changes in background EEG activity and maximal dilation of the pupil were detected at both scopolamine doses. Heart rate significantly decreased at 0.02 mg.kg-1 and increased at the dose of 0.2 mg.kg-1 scopolamine. Our findings indicate that the duration of the latent period preceding hyperoxic seizures is not altered by scopolamine in rats; however, other side effects of the drug regarding visual and cardiovascular symptoms should be considered when scopolamine is used in combination with hyperbaric oxygen.

Animals↗