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)

Sedation may be a dose-limiting side-effect of opioid therapy in some cancer patients. This study was designed to evaluate further the use of the psychostimulant, methylphenidate, an agent that has been reported to counter-act opioid-induced sedation, in patients with cancer-related pain. Patients receiving a stable dose of an opioid for cancer-related pain were recruited for this randomized, double-blind, crossover clinical trial. In addition to their regular dose of narcotics, they received 5 days of methylphenidate followed by 5 days of placebo, or vice versa. Our data did not definitively demonstrate any statistically significant benefit for methylphenidate, but did suggest that this drug could mildly decrease narcotic-induced drowsiness and could increase night-time sleep. These data, in conjunction with other published data, suggest that methylphenidate can counteract narcotic-induced daytime sedation to a limited degree.
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PMID:A randomized, crossover evaluation of methylphenidate in cancer patients receiving strong narcotics. 753 1

We examined the plasma concentrations and resultant clinical effects produced by four different propofol bolus infusion regimens in 98 healthy males undergoing elective urologic procedures under regional anesthesia. Patients were randomly assigned to one of four propofol dosage groups. In Groups 1-4, loading doses of propofol equal to 0.2, 0.4, 0.5, or 0.7 mg/kg intravenously, respectively, were followed by fixed-rate propofol infusions of 0.5, 1, 2, or 4 mg.kg-1.h-1, respectively, during the regional block procedure. Sedation (sleepiness) was assessed independently by the patient and a blinded observer using 100-mm visual analog scales. Intraoperative amnesia was assessed using picture recall. Sedation scores increased in a dose-dependent fashion (13 +/- 19, 21 +/- 19, 45 +/- 28, and 73 +/- 26 mm at 30 min in Groups 1-4, respectively). Within a given dosage group, sedation scores were stable during the maintenance infusion period. Mean plasma propofol concentrations increased with higher propofol infusion rates (0.16 +/- 0.3, 0.18 +/- 0.1, 0.47 +/- 0.2, and 1.1 +/- 0.8 microgram/mL at 30 min in Groups 1-4, respectively). However, significant variability was observed among individual patient sedation scores and plasma propofol concentrations. Anxiety scores decreased in all four propofol infusion groups during the maintenance period. Hemodynamic variables and hemoglobin oxygen saturation values were similar in all four treatment groups. Recovery from propofol's central effects was rapid after discontinuation of the propofol infusion, and the incidence of side effects was low. Recall of intraoperative events was more commonly observed in the lower-dosage groups (86%, 96%, 58%, and 13% of patients in Groups 1-4, respectively).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Propofol infusion during regional anesthesia: sedative, amnestic, and anxiolytic properties. 763 71

A double-blind placebo-controlled cross-over trial was carried out to evaluate the efficacy and safety of the combined serotonin-dopamine antagonist risperidone in mentally retarded patients with persistent behavioural disturbances. After an observation period of 1 week, risperidone 4-12 mg or placebo was administered during 3 weeks as add-on treatment to the existing medication, followed by a 1-week single-blind placebo wash-out, and another 3 weeks of double-blind treatment with the cross-over medication. Thirty-seven patients participated in the trials; 30 completed the study. Risperidone was significantly superior to placebo in its effect on the Aberrant Behaviour Checklist and the Clinical Global Impression. The Extrapyramidal Symptom Rating Scale did not show any differences between risperidone and placebo. Two patients experienced hypotension at the start of the risperidone administration. Sedation and drowsiness were the most frequently reported treatment-emergent adverse events. The results of this trial warrant further investigation into the therapeutic assets of risperidone in this indication, as add-on therapy and as monotherapy.
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PMID:Risperidone as add-on therapy in behavioural disturbances in mental retardation: a double-blind placebo-controlled cross-over study. 768 29

The first central pharmacodynamic action of chlorpromazine to be described was sedation without narcosis. The antipsychotic action and extrapyramidal symptoms were observed later. Sedation can be separated into nonspecific sedation (drowsiness, somnolence) and specific sedation (psychomotor inhibition and psychic indifference). Both types are parts of the clinical profiles of classical neuroleptics. The sedative properties of neuroleptics may contribute to the overall efficacy in the treatment of psychotic patients, depending on the clinical situation. In most patients, however, sedation is only needed for a short period, or not at all. The drug induced sedation may adversely affect the patients' well-being and functional capabilities. The term neuroleptic-induced deficit syndrome (NIDS) has been coined to focus attention on the adverse mental effects of neuroleptics. NIDS still needs to be properly defined and to be differentiated from the deficit syndrome of schizophrenia and postpsychotic depression. Assessment methods are needed to establish the incidence and prevalence of NIDS, to evaluate the importance of NIDS in the overall treatment outcome in psychoses and to facilitate development of better antipsychotic agents.
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PMID:Neuroleptics and the neuroleptic-induced deficit syndrome. 791 56

Serotonin uptake inhibitors are generally considered activating antidepressants. To assess the 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 the pooled data from two fixed-dose studies 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 treatment-emergent phenomena (p < or = 0.05), but dose-effect relationships differed. Activation rates were relatively stable between 5 mg/day and 40 mg/day, but they increased at 60 mg/day. Sedation rates increased linearly up to 40 mg/day, and then were comparable at 40 mg/day and 60 mg/day. Discontinuations due to 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 at all doses. First occurrences of sedation also peaked early at all doses, but there may have been greater variability in first occurrences of sedation over time in patients receiving lower doses. The persistent occurrences of sedation may decline less over time than the persistent occurrences of activation.
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PMID:Fluoxetine: activating and sedating effects. 827 47

The sedative properties of astemizole-D and triprolidine-D were compared in a double-blind, placebo-controlled, repeated-measures design study comprising three experimental treatments, each with a duration of 2 days (n = 12). Sedation was assessed by continuous electroencephalographic measurement (C-EEG), intermittent performance testing and subjective measures. C-EEG monitoring revealed that triprolidine-D produced significantly more daytime sedation and drowsiness than either astemizole-D or placebo (p < 0.05). Intermittent performance testing did not reveal consistent psychomotor deficits. There were no differences from placebo; the only significant findings showed that astemizole-D improved tracking accuracy at T + 65 h (p < 0.05) compared to baseline. Also, when scores were summed across all time points, astemizole-D improved scores significantly in contrast to triprolidine-D for the total scores (p < 0.05). It is concluded that, in contrast to triprolidine-D, astemizole-D does not produce daytime drowsiness or sedation.
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PMID:Comparison of the effects of astemizole/pseudoephedrine and triprolidine/pseudoephedrine on CNS activity and psychomotor function. 873 11

Traditional centrally acting antihypertensives have been associated with a high incidence of adverse effects and are no longer recommended as first-line therapy. The newer imidazoline receptor agonists must overcome this reputation if they are to gain recognition as potential first-line agents for hypertension. Methyldopa, a centrally acting alpha(2)-agonist, is characterized by a number of serious adverse reactions that limit its use. Although unpredictable idiosyncratic or hypersensitivity reactions are uncommon, these include hepatitis, myocarditis, and hemolytic anaemia. Less serious problems such as abnormal liver function tests, positive Coombs test, drug-induced fever, and pancreatitis also occur. Central side effects include drowsiness, fatigue, lethargy, sedation, depression, psychotic reactions, nasal stuffiness, impotence, and exacerbation of Parkinsonism. In hypertensive men, methyldopa is less well tolerated than either captopril or propranolol, and up to 20% of patients discontinue therapy because of adverse effects. Clonidine acts primarily as an alpha(2)-agonist but also acts as an agonist at imidazoline receptors in the rostroventrolateral medulla. It is equipotent to most other antihypertensives but is considerably less well-tolerated in comparative trials. The principal adverse effects of clonidine are drowsiness, sedation, lethargy and dry mouth. Reserpine acts primarily by depleting central catecholamine neurotransmitter stores. It was very extensively used in early hypertension trials, but its central side effects of sedation, nasal stuffiness, and severe depression are now considered so undesirable that the drug is seldom prescribed. The imidazoline (I1) agonists moxonidine and rilmenidine act selectively and have very little central alpha(2)-agonist activity. In comparative studies against placebo and other reference antihypertensives, the only adverse effect consistently associated with these drugs was dry mouth (approximate placebo-corrected incidence 10%). Sedation was not pronounced. Withdrawal syndromes are complex pathophysiologic processes and occur with a variety of antihypertensive drugs. Cessation of therapy with clonidine and, to a lesser extent, methyldopa may result in a severe withdrawal syndrome characterized by restlessness, sweating, anxiety, tremor, palpitations, and headache. There may be a rapid rise in blood pressure, often with a true "rebound" to higher than pretreatment levels. Plasma and urinary catecholamine levels are increased, and fatalities have been reported. It is important to stress that such a syndrome has not been recorded, in animal or human studies, with either moxonidine or rilmenidine.
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PMID:Aspects of tolerability of centrally acting antihypertensive drugs. 887 99

Sedation is the principal side effect of first generation H1 antihistamines, and recent studies have suggested that this side effect should limit the clinical application of these drugs. The sedative effect also underlies the use of these first-generation drugs as nonprescriptive remedies for insomnia. In both cases, the potential for tolerance to the sedative effect of these drugs is an important issue for which there are few objective data. In the study reported here, 15 healthy men age 18 to 50 years received either diphenhydramine 50 mg or placebo twice a day for 4 days in a randomized, double-blind, crossover trial design. Dependent measures included objective and subjective assessments of sleepiness and computer-based tests of psychomotor performance. Both objective and subjective measures of sleepiness showed significantly higher levels on day 1 for diphenhydramine compared to placebo. By day 4, however, levels of sleepiness on diphenhydramine were indistinguishable from placebo. Similarly, diphenhydramine produced significant impairment of performance that was completely reversed by day 4. These data provide the first objective confirmation that tolerance develops to the sedative effect of a prototypical first-generation H1 antihistamine, diphenhydramine. On this dosing regimen, tolerance was complete by the end of 3 days of administration. While other antihistamines and dosing regimens may differ, these results suggest that tolerance to the sedation produced by these drugs develops with remarkable rapidity.
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PMID:Tolerance to daytime sedative effects of H1 antihistamines. 1235 76

Psychosis only rarely occurs in patients with untreated Parkinson's disease. Much more commonly, psychosis is induced by drug therapy for Parkinson's disease and is the strongest known risk factor for nursing home placement. Delusions are less frequent than hallucinations, but are more concerning as they are often paranoid in nature. Treatment begins with a search for correctable infectious, toxic, and metabolic aetiologies. If symptoms persist, anti-Parkinson's disease medications are slowly reduced. However, withdrawal of these drugs usually worsens parkinsonism and is often not tolerated. Certain atypical antipsychotics can be used to treat psychosis without compromising motor function. The choice of atypical antipsychotic is largely based on ease of use and adverse effect profile as most have comparable efficacy in improving psychosis. Currently, there are five marketed atypical drugs - clozapine, risperidone, olanzapine, quetiapine and ziprasidone. Ziprasidone is the only agent whose adverse effect profile has not been reported in Parkinson's disease. The most common adverse effects of clozapine in Parkinson's disease are sedation, orthostatic hypotension and sialorrhoea. Sedation is generally helpful since these patients are frequently awake at night and tend to have worse behavioural problems then. Clozapine does not induce deterioration of motor function, but it has the potential to cause agranulocytosis, which is idiosyncratic and not dose-related. In risperidone-treated Parkinson's disease patients, reported adverse effects include somnolence, sialorrhoea, dizziness, palpitations, constipation, delirium, fatigue, leg cramps, depression, urinary incontinence and hypotension. Although in some Parkinson's disease studies, risperidone has been well tolerated, others have shown that many patients are unable to tolerate the drug due to deterioration of motor function. While an initial study of olanzapine in Parkinson's disease psychosis showed the drug to be effective without deterioration of motor function, succeeding reports demonstrated a deleterious effect of the drug on motor functioning. The most common adverse effects of quetiapine in Parkinson's disease patients are sedation and orthostatic hypotension. There is a lack of double-blind trials; however, cumulative reports involving >200 Parkinson's disease patients strongly suggest that quetiapine is well tolerated and effective. Unlike clozapine, it does not improve tremor and may induce mild deterioration of motor function. Recently, cholinesterase inhibitors have been reported to alleviate psychosis in Parkinson's disease. Although ondansetron, an antiemetic with antiserotonergic properties, has been reported to relieve psychosis in Parkinson's disease, its prohibitive cost has prevented further study in this population. Electroconvulsive treatment is generally reserved for the patient with psychotic depression who is unable to tolerate any pharmacological therapy.
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PMID:Treatment of psychosis in Parkinson's disease: safety considerations. 1281 32

Diazepam rectal gel (Diastat) is the only medication approved by the US FDA for the management of selected, refractory patients with epilepsy, on stable regimens of antiepilepsy drugs, who require intermittent use of diazepam to control bouts of increased seizure activity. An analysis of the safety of diazepam rectal gel reveals that this formulation has certain advantages over intravenous diazepam administration: most notably a very low incidence of respiratory depression, low potential for abuse and the opportunity for out-of-hospital use by non-professional caregivers. Sedation is the most common adverse effect of rectal diazepam treatment, occurring in approximately one-quarter of patients, although drug-induced somnolence is difficult to distinguish from normal post-ictal sedation. Overdosage of diazepam rectal gel is rarely associated with serious clinical consequences, and overdoses of up to 330% of the maximum recommended dosage have been reported without any respiratory or cardiac depression. Under-administration may be a serious safety issue because of morbidity that may result if seizures are not terminated. Chronic administration may cause tachyphylaxis and should be avoided.
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PMID:Safety of Diastat, a rectal gel formulation of diazepam for acute seizure treatment. 1514 32


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