Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0600097 (Sedation)
 1,337 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Serotonin uptake inhibitors are generally considered activating antidepressants. To assess rates and temporal patterns of activation and sedation as well as dose-effect relationships, adverse event data were evaluated from a fixed-dose study comparing placebo and fluoxetine 5, 20, and 40 mg/day in the treatment of major depressive disorder (N = 363) and two fixed-dose studies pooled together comparing placebo and fluoxetine 20, 40, and 60 mg/day in the treatment of major depressive disorder (N = 746). The adverse events nervousness, anxiety, agitation, and insomnia were considered indicative of activation; somnolence and asthenia were considered indicative of sedation. Activation and sedation were both statistically significant (p less than or equal to 0.05) treatment-emergent phenomena, but dose-effect relationships differed. Activation rates were relatively stable between 5 and 40 mg/day, and then increased at 60 mg/day. Sedation rates increased linearly to 40 mg/day and then were comparable at 40 and 60 mg/day. Discontinuations for either phenomenon were uncommon. The temporal patterns of first occurrences and persistence of activation and sedation differed. First occurrences of activation peaked early and declined over time with all doses. First occurrences of sedation also peaked early with all doses, but there may have been greater variability in first occurrences of sedation over time with lower doses. Persistent occurrences of sedation may decline less over time than persistent occurrences of activation.
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PMID:Fluoxetine: activating and sedating effects at multiple fixed doses. 147 50

Heavy i.v. sedation is often used in upper GI endoscopy. Sedation, however, creates the need for recovery facilities and precludes patients from returning to their normal daily activities. This is undesirable, since endoscopy is routinely performed as an out-patient procedure. Also the cost for medication and recovery facilities militate against the indiscriminate use of i.v. sedative premedication. The present study was undertaken in an attempt to establish what proportion of patients can benefit from oral premedication, and whether such an administration route can eliminate some of the disadvantages associated with i.v. sedation. Four hundred out-patients were randomized to receive orally either triazolam, 0.125 mg, or placebo. Of the patients, 359 were evaluable; 177 received placebo and 182 triazolam. All major aspects of the procedure were covered using visual analogue scale questionnaires for the endoscopist and patient. There were no differences in endoscopic experience, or sex and age distribution between the groups. Triazolam reduced patient discomfort, 38.6 +/- 25.6 vs 44.8 +/- 30.1 (p = 0.0379). Recollection of post-endoscopy information was the same in both groups. One patient complained of drowsiness following the procedure. No patient needed to stay in hospital to complete recovery. Endoscopy quality was identical in the two groups. Oral premedication has the potential to be of significant value, may optimize the use of endoscopy resources, and does not impair patient activities post-endoscopy.
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PMID:Oral sedation for diagnostic upper endoscopy. 191 46

The effects of high-dose fluoxetine (median 80 mg/day), standard-dose imipramine (median 200 mg/day), and placebo were studied in 706 outpatients meeting DSM-III criteria for major depressive disorder. Baseline psychomotor activity of each patient was prospectively categorized as agitated, retarded, or neither. Rates of occurrence of total and significant (leading to discontinuation) activating adverse events (insomnia, agitation, anxiety, nervousness) and sedating events (somnolence, asthenia) were compared between treatments on an overall basis and within categories of baseline psychomotor activity. Additionally, these rates were compared across baseline psychomotor activity for each treatment. Efficacy was evaluated on an overall basis and with respect to baseline psychomotor activity. There was more total activation with fluoxetine than placebo (p = 0.008), but total activation with fluoxetine (28%) showed only a trend (p = 0.092) for being greater than with imipramine (21%). Discontinuations for activation with fluoxetine (5%) did not differ from imipramine (5%). Sedation and discontinuations for sedation with both fluoxetine and imipramine significantly exceeded placebo. The only drug-drug difference in discontinuations was for sedation where imipramine (11%) exceeded fluoxetine (5%; p = 0.008). Only for the occurrence of sedation with imipramine (47% among patients retarded at baseline) was there a significant association with baseline psychomotor activity (p = 0.021). Both fluoxetine and imipramine were superior to placebo and equal in efficacy in decreasing total Hamilton Rating Scale for Depression (HAM-D), the sleep disturbance HAM-D factor, and the anxiety/somatization HAM-D factor scores. These improvements were independent of baseline psychomotor activity.
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PMID:High-dose fluoxetine: efficacy and activating-sedating effects in agitated and retarded depression. 162 94

In 1988 an estimated 30 million Americans spent more than $500 million for single-entity antihistamines. Classic first-generation antihistamines, which are available without prescription, can cross the blood-brain barrier and have been reported to produce various central nervous system effects. Sedation, the most common adverse effect of these agents, occurs in 10% to 25% of antihistamine users. Drowsiness has been attributed to the blockade of central histaminergic receptors; antagonism of other brain receptors, such as serotonergic, cholinergic, and central alpha-adrenergic receptors, has also been proposed. The newer second-generation H1-receptor antagonists are typically large, lipophobic molecules with a charged side chain and are extensively bound to albumin. Consequently, these agents have difficulty entering the brain, and they appear no more likely to induce sedation than does placebo. The effects of antihistamines on psychomotor reflexes and driving, antihistamine-induced drowsiness, and interaction of antihistamines with alcohol and tranquilizers have been studied with numerous methodologies. The centrally acting first-generation agents commonly cause greater performance decrements as compared with the newer, nonsedating, second-generation antihistamines.
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PMID:Performance effects of antihistamines. 222 23

In this study, the possible effects of rilmenidine on vigilance are evaluated. Sedation is the most disturbing side effect of alpha 2-agonists, especially during the first weeks of treatment. The level of vigilance was first determined by assessing drowsiness using visual analogue scales and/or by several psychometric tests in four pharmacoclinical studies in healthy subjects or in hypertensive patients: three studies with single administration of rilmenidine (0.5 to 3.0 mg) and one study with repeated administration for three days. These studies were double-blind, Latin-square designed, and controlled versus placebo (in all studies) and versus clonidine (in three studies). Analysis of these results illustrated that after short-term and repeated administration: (1) the effects on vigilance observed with rilmenidine 1 mg did not differ statistically from data observed with placebo; and (2) sedative effects observed with clonidine were significantly greater than with rilmenidine, at equihypotensive doses. Daytime drowsiness was systematically assessed and graded by inciting questioning at each visit in five clinical studies. Ambulatory hypertensive patients were treated with rilmenidine (1 mg per day or 1 mg twice a day). These studies were controlled versus placebo (one study for two weeks, 120 patients; and one study for one month, 126 patients), hydrochlorothiazide (six weeks, 56 patients), clonidine (six weeks, 333 patients), and methyldopa (three months, 157 patients). The results showed that: (1) drowsiness observed with rilmenidine did not differ statistically from that observed with placebo or diuretic; and (2) drowsiness occurred less frequently with rilmenidine than with reference alpha 2-agonists at equihypotensive doses. In conclusion, these results confirm in current clinical use the dissociation already observed in laboratory animals between the antihypertensive effects and the sedative effects and may distinguish rilmenidine among alpha 2-agonists.
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PMID:Rilmenidine and vigilance. Review of clinical studies. 257 Dec 96

A total of 317 patients received loratadine, 10 mg once daily, terfenadine 60 mg twice daily, or placebo in a 14-day, double-blind, randomized study in seasonal allergic rhinitis. Four nasal and four nonnasal symptoms were evaluated. At the end point evaluation, mean total scores of combined nasal and nonnasal symptoms decreased from baseline (improved) 46%, 44%, and 35%, respectively, for loratadine, terfenadine, and placebo. The difference between loratadine and placebo treatment was significant (p = 0.03). Loratadine was particularly effective compared with placebo in relieving nasal discharge, sneezing, and itching/burning eyes. Therapeutic response to treatment was good or excellent in 66 (64%) of 103 loratadine-treated patients, 58 (56%) of 104 terfenadine-treated patients, and 48 (47%) of 102 placebo-treated patients. Adverse experiences reported during the study were usually mild or moderate and were not significantly different among the three treatment groups. Sedation (somnolence) was reported by 10 loratadine-treated patients, seven terfenadine-treated patients, and eight placebo-treated patients. Loratadine, 10 mg once daily, was comparable to terfenadine, 60 mg twice daily, and significantly superior to placebo in the symptomatic relief of seasonal allergic rhinitis.
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PMID:Efficacy and safety of loratadine (10 mg once daily), terfenadine (60 mg twice daily), and placebo in the treatment of seasonal allergic rhinitis. 257 17

Six fasting male subjects (20-32 years of age) received an oral tablet and an IV 1.0-mg dose of alprazolam in a crossover-design study. Alprazolam plasma concentration in multiple samples during 36 h after dosing was determined by electron-capture gas-liquid chromatography. Psychomotor performance tests, digit-symbol substitution (DSS), and perceptual speed (PS) were administered at 0, 1.25, 2.25, 5.0, and 12.5 h. Sedation was assessed by the subjects and by an observer using the Stanford Sleepiness Scale and a Nurse Rating Sedation Scale (NRSS), respectively. Mean kinetic parameters after IV and oral alprazolam were as follows: volume of distribution (Vd) 0.72 and 0.84 l/kg; elimination half-life (t1/2) 11.7 and 11.8 h; clearance (Cl) 0.74 and 0.89 ml/min/kg. There were no significant differences between IV and oral alprazolam in Vd, t1/2, or area under the curve. The mean fraction absorbed after oral administration was 0.92. Performance on PS and DSS tests was impaired at 1.25 and 2.5 h, but had returned to baseline at 5.0 h for both treatments. Onset of sedation was rapid after IV administration and the average time of peak sedation was 0.48 h. Sedation scores were significantly lower during hour 1 after oral administration than after IV, but were not significantly different at later times. Alprazolam is fully available after oral administration and kinetic parameters are not affected by route of administration. With the exception of rapidity of onset, the pharmacodynamic profiles of IV and oral alprazolam are very similar after a 1.0-mg dose.
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PMID:Pharmacokinetics and pharmacodynamics of alprazolam after oral and IV administration. 615 55

A short sleep portion in an otherwise routinely performed EEG evaluation is often highly informative. This is particularly true for epileptological conditions. Several paroxysmal discharges are demonstrable solely in sleep and/or drowsiness; these potentials remain undetected in a waking tracing. Hence the inclusion of a sleep portion may be crucial in the assessment of epileptic seizure disorders but tends to yield less information in non-epileptic conditions. Sedation (Chloral Hydrate) is recommended if sleep does not occur spontaneously.
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PMID:[Short sleep on the EEG--a source of otherwise overlooked EEG abnormalities]. 620 49

A study was undertaken to characterize the H1 receptor blockade, central nervous system depressant properties, and kinetic parameters of methapyrilene in man. Eight healthy subjects received, in random order at weekly intervals, placebo and methapyrilene 20 mg intravenously and 50 mg and 25 mg orally. Methapyrilene exhibited a moderate antihistaminic effect as measured by the reduction of histamine-provoked skin wheals. Sedation and drowsiness were detected only at the first sampling time (0.75 hr) after intravenous doses. The terminal plasma half-life ranged from 1.1 to 2.1 hr, apparent volume of distribution from 2.14 to 6.61 1/kg, and plasma clearance from 0.013 to 0.048 1/min/kg. Systemic bioavailability was low and showed large interindividual differences, ranging from 4% to 46%. Recovery of unchanged drug from the 24-hr urine was under 2% of the doses.
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PMID:Methapyrilene kinetics and dynamics. 747 21

Loratadine is a long-acting antihistamine agent, exhibiting partial selectivity for peripheral histamine H1-receptors. To date, loratadine has been evaluated in allergic rhinitis, urticaria and, to a limited extent, in asthma. In several large controlled comparative clinical studies, loratadine was superior to placebo, faster acting than astemizole and as effective as azatadine, cetirizine, chlorpheniramine (chlorphenamine), clemastine, hydroxyzine, mequitazine and terfenadine in patients with allergic rhinitis and chronic urticaria. The clinical effectiveness of loratadine in asthma is at present unclear. Loratadine is well tolerated. At dosages of 10 mg daily, commonly reported adverse events were somnolence, fatigue and headache. Sedation occurred less frequently with loratadine than with azatadine, cetirizine, chlorpheniramine, clemastine and mequitazine. Serious ventricular arrhythmias, as reported with some other second generation histamine H1-receptor antagonists, have not been observed with loratadine to date. Thus, loratadine, with its attributes of once daily administration, fast onset of action and essentially nonsedating properties, would appear to be an appropriate first-line agent for the treatment of allergic rhinitis or urticaria.
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PMID:Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. 752 33


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