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)

Loxapine is a dibenzoxazepine, tricyclic compound recommended for the treatment of acute and chronic schizophrenia. In its therapeutic effectiveness and profile and incidence of side-effects, loxapine closely resembles the traditional antipsychotic agents. Although loxapine has tended to be less effective than some standard antipsychotic drugs in a few short-term (3 to 4 weeks) studies, it has been superior to a placebo and about as effective as chlorpromazine, haloperidol, trifluoperazine or thiothixene when evaluated after 4 to 12 weeks. Like the phenothiazine (e.g. chlorpromazine) and butyrophenone (e.g. haloperidol) antipsychotic agents, loxapine causes a high incidence of extrapyramidal reactions. Sedation occurs frequently, especially during early stages of treatment. Other, less common side-effects such as anticholinergic effects (dry mouth, blurred vision, etc.), hypotension, tachycardia and precipitation of epileptic seizures, which occur with the older antipsychotic drugs, have also been reported with loxapine.
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PMID:Loxapine: a review of its pharmacological properties and therapeutic efficacy as an antipsychotic agent. 2 67

Loratadine is a new selective peripheral histamine H1-receptor antagonist, that is orally effective, long-acting, and devoid of significant central and autonomic nervous system activity. Its safety and efficacy were evaluated in a 28-day study conducted in patients with chronic idiopathic urticaria. Patients were randomly assigned to one of three treatment groups (loratadine, 10 mg OD; terfenadine, 60 mg BID; or placebo). Evaluation of efficacy included weekly assessments of the individual disease signs and symptoms, the overall disease condition, and therapeutic response to treatment. Throughout the 28-day treatment period progressive improvement was observed in the loratadine and terfenadine treatment groups; however, at each evaluation, loratadine was significantly more effective than placebo (P less than .01) and clinically more effective than terfenadine in reducing disease signs and symptoms. Terfenadine was significantly more effective than placebo at day 7 and endpoint (last valid visit). The overall therapeutic response at the endpoint of treatment was rated as marked or complete relief of symptoms in 64%, 52%, and 25% of the patients in the loratadine, terfenadine, and placebo treatment groups, respectively. Loratadine was well tolerated and comparable to terfenadine and placebo in incidence of adverse experiences. Sedation was reported in one patient each in the terfenadine and placebo treatment groups and an anticholinergic side effect (dry mouth) in one terfenadine-treated patient. No sedative or anticholinergic side effects were observed in patients receiving loratadine. We concluded that loratadine, 10 mg, once daily is a safe and effective treatment for symptomatic relief of chronic idiopathic urticaria.
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PMID:Comparative effects of loratadine and terfenadine in the treatment of chronic idiopathic urticaria. 196 19

Two hundred sixty-four patients with moderate to severe seasonal allergic rhinitis were treated with loratadine 5 mg plus pseudoephedrine 120 mg twice a day or placebo in a 28-day multicenter study. Four nasal and four non-nasal symptoms were evaluated for efficacy. At the last evaluable visit, the active treatment group had significantly lower (P = .05) mean combined nasal and non-nasal symptom scores than the placebo group. Also, the physician's rating of overall therapeutic response was significantly better in the active-treatment group (P = .03). Dry mouth, insomnia, and nervousness were reported by a significantly greater proportion (P less than or equal to .04) in the active-treatment group. Sedation occurred in 7% of patients in each treatment group and 6% of patients in each group discontinued the study because of adverse experiences. Loratadine plus pseudoephedrine was safe and significantly more effective than placebo in relieving the symptoms of allergic rhinitis.
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PMID:Loratadine-pseudoephedrine combination versus placebo in patients with seasonal allergic rhinitis. 252 98

This phase I study determined the maximum tolerated dose of prochlorperazine when used as an antiemetic prior to cytotoxic chemotherapy. Initially, cohorts of three patients were given prochlorperazine at escalating doses of 0.2, 0.4, 0.6, 0.8, 1.0 and 1.2 mg/kg as an intravenous infusion over 20 min. The maximum tolerated dose was 1.2 mg/kg. The dose-limiting toxicity was hypotension which was reversed by a fluid load. The other major toxicities were extrapyramidal reactions which were dose related. All patients at the 1.2 mg/kg dose reported restlessness while five of six were restless and two of six at 1.0 mg/kg had muscle spasms. Two of seven patients reported restlessness at the 0.8 mg/kg level. Sedation and dry mouth were reported at all dose levels but were more common at higher doses. Prochlorperazine in plasma was assayed by high performance liquid chromatography with electrochemical detection and pharmacokinetics were determined for three patients at the 1.0 mg/kg dose level. The average terminal elimination half life was 7.6 +/- 0.4 h, plasma clearance 27 +/- 5 ml/min/kg and volume of distribution 17.7 +/- 4.5 l/kg. The dose of prochlorperazine recommended for further studies of antiemetic efficacy is 0.8 mg/kg intravenously.
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PMID:A dose finding study of prochlorperazine as an antiemetic for cancer chemotherapy. 259 37

The dose-effect and concentration-effect relations of rilmenidine, a new alpha 2 agonist, were evaluated for the hemodynamic and side-effect responses to single oral doses. Two studies were performed in a double-blind manner: study I in 8 healthy subjects and study II in 10 hypertensive patients. In the course of five 24-hour periods, each separated by at least 1 week, the following 5 treatments were administered in a random order: placebo, rilmenidine (0.5, 1, 2 and 3 mg). Blood pressure was measured with a Roche arteriosonde (study I) or a sphygmomanometer (study II). Sedation was measured using a visual analog scale. Dry mouth was assessed by measuring the salivary flow (study I) or by visual analog scale (study II). Plasma concentration of rilmenidine was assayed by gas chromatography linked with mass spectrometry. The antihypertensive and sedative effects (area under curve) were directly related to the dose and to the log of the plasma concentration of rilmenidine. In contrast to the 2- and 3-mg doses, rilmenidine (0.5 and 1 mg) did not induce orthostatic hypotension, a significant decrease in heart rate or a significant dryness of mouth. At doses of 0.5 and 1 mg, the effects of rilmenidine on sedation were not consistent in both studies: sedation was significant in study I but did not differ from placebo in study II. These studies show that rilmenidine, in common with other alpha 2 agonists, decreases blood pressure in a dose-dependent manner, in normotensive as well as in hypertensive subjects.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Dose and concentration-effect relations for rilmenidine. 289 61

A hyperkinetic heart syndrome has been diagnosed in 10 patients by clinical investigation and right-heart catheterization at rest and during exercise. Subsequently, the patients received 3 X 40 mg alinidine, and 2 X 40 mg propranolol and placebo, each for 2 weeks in a double-blind crossover study. Heart rate at rest (P less than 0.05) and during exercise (P less than 0.001) decreased significantly under alinidine and propranolol to the same extent (control, 83/170; alinidine, 68/146; propranolol, 73/139; placebo, 83/162 beats per min). Lower limb flow at rest and after exercise, measured by plethysmography, as well as left-ventricular fractional shortening and mean velocity of circumferential fiber shortening, measured by echocardiography, decreased insignificantly. Sedation and a dry mouth occurred in six patients under alinidine, while fatigue and cold hands and/or feet were reported by five patients under propranolol. Thus, alinidine may be used as an alternative to beta-blocking in the treatment of the hyperkinetic heart syndrome.
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PMID:[Treatment of hyperkinetic heart syndrome with alinidine and propranolol]. 356 Jul 88

The effects of oral guanfacine were examined in six patients with essential hypertension. Guanfacine caused a substantial fall in both lying and standing systolic and diastolic blood pressure. The fall in pressure was evident by 6 hr, maximal by 10 to 12 hr, and lasted as long as 36 hr. In four patients satisfactory blood pressure control throughout the day was achieved during inpatient administration with single daily doses of 2 to 4 mg in the evening. The other two patients required twice-daily dosing for optimal control of blood pressure. There was no evidence of tolerance to the hypotensive effect. Sedation and xerostomia were apparent after the first dose but did not limit dose titration. Guanfacine lowered lying and standing plasma norepinephrine; this continued on long-term dosing. Urinary catecholamines were reduced from 59.21 +/- 17.24 (mean +/- SEM) to 28.91 +/- 4.20 micrograms/24 hr after 7 days of treatment. The hemodynamic effects, side effects, and biochemical evidence of reduced sympathetic activity after guanfacine resembled the centrally acting antihypertensive clonidine, although guanfacine appeared to have a longer duration of action.
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PMID:Effects of single and multiple doses of guanfacine in essential hypertension. 700 28

Clonidine hydrochloride (Catapres), a potent antihypertensive agent, has been in clinical use since 1974 in the United States. Clonidine, an alpha-adrenergic receptor agonist, stimulates central alpha receptors in the depressor site of the vasomotor center of the medulla oblongata and hypothalamus, which diminishes efferent sympathetic tone to the heart, kidneys, and peripheral vasculature with a concomitant increase in vagal activity. Hemodynamic and renal effects include reduction in supine and erect blood pressure, heart rate, total peripheral resistance, plasma renin activity, and urinary aldosterone and catecholamine excretion, with little effect on resting cardiac output, response to exercise, and preservation of renal function. Clonidine alone produces a significant reduction in mean arterial pressure in all degrees of hypertension during acute and chronic administration, with little or no tendency toward tolerance or postural hypotension. Its antihypertensive potency is enhanced with the concomitant use of a diuretic or vasodilator, and it may be used in place of a beta blocker with equal efficacy in the diuretic plus vasodilator combination. Serious adverse effects are uncommon, with more than 93% of patients tolerating the drug well. Sedation and dry mouth, the most common adverse effects, are usually related to dose and duration and are minimized by gradually increasing the dose and by taking the major portion of the twice-daily schedule at bedtime. Clonidine may be safely given to patients with congestive heart failure, ischemic heart disease, obstructive lung disease, chronic renal insufficiency, and diabetes mellitus. Clonidine is one of the most versatile and effective agents presently available for the treatment of hypertension.
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PMID:Clonidine hydrochloride. 704 65

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

Eighteen women with severe premenstrual syndrome (PMS) (premenstrual dysphoric disorder, PMDD) were treated openly with paroxetine for 10 consecutive menstrual cycles. Dosage was flexible (5-30 mg/day); also, the patients were free to chose between continuous medication and medication in the luteal phase only. The rating of premenstrual irritability, depressed mood, increase in appetite, and anxiety/tension was markedly lower during treatment with paroxetine than before, and this reduction in symptomatology appeared unabated for the entire treatment period. Sedation, dry mouth, and nausea were common side-effects but declined during the course of the trial; in contrast, reduced libido and anorgasmia, which were reported by almost 50% of the participants, were not improved with time. The results indicate that the beneficial effects as well as the sexual side-effects of serotonin reuptake inhibitors persist unchanged for at least 10 consecutive cycles of treatment.
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PMID:A naturalistic study of paroxetine in premenstrual syndrome: efficacy and side-effects during ten cycles of treatment. 921 79


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