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)

Most alpha 2-adrenoceptor agonists developed so far will penetrate into the brain, thus causing central hypotensive activity, mediated by the stimulation of alpha 2 adrenoceptors in the region of the nucleus tractus solitarii, the vasomotor center and the nucleus of the vagus nerve. The central alpha 2 adrenoceptors are probably located at postjunctional (postsynaptic) sites. Their stimulation causes sympathoinhibition and thus a decrease in blood pressure and heart rate. The central hypotensive effect is the dominating activity of all alpha 2-adrenoceptor agonists developed so far, of which clonidine, guanfacine and alpha-methyl-DOPA (which is converted into alpha-methyl-noradrenaline) are the prototypes. Peripheral postsynaptic effects probably do not greatly contribute to the hypotensive activity of these drugs. Sedation, also mediated by central alpha 2 adrenoceptors is the major adverse reaction to these antihypertensive agents. More selective alpha 2-adrenoceptor agonists (B-HT 920, azepexole, UK 14,304) appear to display the same pattern of hypotensive and sedative activities as the nonselective compounds like clonidine. After the general survey on centrally acting alpha 2-adrenoceptor agonistic drugs, the pharmacologic profile of the new oxazoline derivative, rilmenidine, (S 3341) was compared with that of the classic compound, clonidine. In all current animal and in vitro models, rilmenidine was characterized as a clonidine-like, centrally acting antihypertensive drug. Thus, its central hypotensive activity proved mediated by the stimulation of central alpha 2 adrenoceptors. In radioligand binding studies, rilmenidine proved somewhat more selective for alpha 2 adrenoceptors, but this selectivity was not reflected by a clearly different pharmacologic profile of the drug.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacology of the alpha 2-adrenoceptor agonist rilmenidine. 289 60

Dyskinesias commonly appear during L-dihydroxyphenylalanine (L-DOPA) therapy of advanced Parkinson's disease (PD) and can occur in both dose-related and dose-independent patterns. Clozapine exerts a dose-related suppression of L-DOPA-induced dyskinesias by shifting the i.v. L-DOPA dose-response curve for production of dyskinesias without altering relief of parkinsonism. We report our outpatient experience with 13 patients on daily clozapine therapy (maximum dose 400 mg/day), followed for 3-21 months (median 10). Beneficial effects of clozapine, determined from twice-weekly diaries, included increased "on time" and decreased "off time" and time "on with dyskinesia." Improvements were statistically apparent by 75 mg/day and remained so through 200 mg/day. Sedation was a common problem, reflected by increased time "asleep" which was significant by 50 mg/day. Sedation was dose limiting in most patients. Orthostatic hypotension and sialorrhea were variably present. No patients had seizures, bone marrow toxicity, or detectable loss of efficacy of clozapine with chronic use. We conclude that clozapine is an effective agent for suppression of dyskinesias in PD with an effective daily dose for most patients of 100-200 mg/day.
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PMID:Suppression of dyskinesias in advanced Parkinson's disease: moderate daily clozapine doses provide long-term dyskinesia reduction. 796 7

Infants with congenital hyperinsulinism may require a positron emission tomography examination with 18F-labeled L-DOPA for the evaluation and planning of surgical interventions. To obtain optimal results it is important for the child to be in a stress-free situation because a stable glucose homoeostasis must be maintained by intravenous glucose infusion. The infant needs to lie calm over a long period of time to obtain optimal results. Sedation for this purpose can be achieved with a continuous infusion of propofol and should be carried out by an anesthesiologist. Additionally blood glucose measurements must be regularly carried out and the glucose infusion must be adjusted to prevent hypoglycemia.
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PMID:[Sedation of infants with congenital hyperinsulinism during PET CAT scanning. A case collection]. 1872 79