Sedation

SSRls may induce sedation in some patients. Altering the time of administration (e.g., having the patient take the medication in the evening rather than the morning) is often not successful. 

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Biological Activities and Analogues. Somatostatin exerts some neurotropic actions, eg, as a tranquilizer and as a spontaneous motor activity depressor. It also lengthens barbiturate anesthesia time and induces sedation and hypothermia. These actions are consistent with the strong association between somatostatin and GABA in the primate cerebral cortex, 90—95% of somatostatin-positive ceHs also contain GABA (100). 

Benzodiazepines. Several BZs have anticonvulsant activity and ate used for the treatment of epilepsy producing their anticonvulsant actions via interactions with the GABA /BZ receptor complex to enhance inhibitory GABAergic transmission (1). The anticonvulsant actions of the BZs tend to tolerate upon chronic usage in six months, and BZs also lead to withdrawal symptomatology. Other side effects include sedation, ataxia, and cognitive impairment. 

Neuroleptic analgesia is so called because the combination of a major tranquilizer, a neuroleptic dmg, and a potent opiate produces an anesthetic state characterized by sedation, apathy, and mental detachment (see Psychopharmacological agents) (152). Iimovar [8067-59-2] a combination of droperidol [648-72-2], C22H22FN2O2, (19) and fentanyl (9) citrate, is used for procedures that do not require muscle relaxation. However, the onset of action is slow. 

Benzodiazepines, ie, the hiU BZR agonists, are prescribed for anxiety, insomnia, sedation, myorelaxation, and as anticonvulsants (97). Those benzodiazepines most commonly prescribed for the treatment of anxiety disorders are lorazepam (19), alprazolam (20), diazepam (21), bromazepam (22), chlorazepate (23), and oxazepam (24). These dmgs together represent about 70% of total... 

The pharmacological profile of buspirone in both animals and humans differs substantially from that of the ben2odia2epine anxiolytics. Buspirone lacks anticonvulsant, myorelaxant, and hypnotic effects. It also produces less sedation resulting in less psychomotor impairment in conjunction with... 

Sahcylamide [65-45-2] is prepared by the reaction of methyl sahcylate with ammonia. Sahcylamide has mild analgesic, antiinflammatory, and antipyretic properties. Sahcylamide is unlike other sahcylates in that it causes sedation and central nervous system depression. Sahcylamide is not hydroly2ed to sahcylate and its action depends on the entire molecule. Sahcylamide has been useful for protection against mil dew and fungus in a variety of soaps, salves, lotions, and oils. The May 1996 price was 8.00/kg (18). 

M,E oral oral 68 Glyceryl thioglycolate >25 <200 sedation, coma, dyspnea, piloerection Mercaptopropionic acid 96-400 21 24... 

The side effects or toxic effects that the calcium antagonists have in common are hypotension, facial flushing, headache, di22iness, weakness, sedation, skin rash, edema, constipation, and abdominal discomfort (nausea, vomiting, and epigastric pressure). 

Methyldopa is effective in mild, moderate, and severe hypertension but a thiazide-type diuretic is needed to overcome the fluid retaining side effect. Methyldopa has been shown to prevent and induce regression of ventricular hypertrophy in hypertensive patients. The principal side effects are sedation, drowsiness, nasal congestion, fluid retention, and in rare occasions, hemolytic anemia. 

When clonidine is withdrawn abmpdy, patients may experience a rebound hypertensive phenomenon, whereia blood pressure rises rapidly to a level higher than the predmg level. These patients may experience symptoms of headache, tachycardia, agitation, and nervousness. If rebound hypertension occurs, resumption of clonidine therapy or adrninistration of phentolamine reduces the blood pressure. For clonidine withdrawal, the dose should be reduced gradually over a two-week period. The principal side effects are sedation, dry mouth, drowsiaess, di22iQess, and fatigue. 

Guanfacine. Guanfaciae, used ia patients having mild to moderate hypertension, can lower blood pressure 50/25 mm Hg (systoHc/diastoHc) ia hypertensive patients. Side effects such as sedation, dry mouth, and asthenia are less as compared to those of guanaben2 and clonidine. Guanfaciae reduces blood cholesterol and triglyceride and does not cause glucose iatolerance. 

Rilmenidine. RiLmenidine is a central a2 adrenoceptor agonist and has been shown to be a potent centrally acting antihypertensive agent without the prominent side effect of sedation. 

In the search for new structures with antiinflammatory activities some 1-substituted 3-dimethylaminoalkoxy-lJ/-indazoles (704) have been synthesized and pharmacologically tested (66JMC38). Doses of 20-40 mg g i.p. produced sedation, muscle relaxation and motor incoordination, whereas doses of 80-100 mg kg produced depression. Toxicity was fairly constant in all series, varying from 120 to 150 mg kg i.p., with the exception of compounds possessing a nitro group or an amino group in the indazole nucleus, which provoked cyanosis. 

Boron enflames in contact with IF3 so do P, As and Sb. Molybdenum and W enflame when heated and the alkali metals react violently. KH and CaC2 become incandescent in hot IF3. However, reaction is more sedate with many other metals and non-metals, and compounds such as CaCOs and Ca3(P04)2 appear not to react with the liquid. 

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