Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Sertraline is a selective inhibitor of central serotonin reuptake. Thus, it enhances serotoninergic transmission--a property which appears to explain its antidepressant activity. Its elimination half-life (approximately 26 hours) makes it suitable for once daily administration. Although clinical experience with sertraline is limited, it appears to possess antidepressant efficacy similar to that of amitriptyline and dothiepin, marginally better than imipramine, and significantly better than placebo. Additionally, sertraline is the only antidepressant licensed in the UK for the prevention of recurrence of depression, and preliminary findings suggest that the drug may also be effective in the treatment of obsessive-compulsive disorder. Sertraline and other serotonin reuptake inhibitors possess tolerability advantages over tricyclic antidepressants. Sertraline has minimal anticholinergic activity, is essentially devoid of cardiovascular effects, has a wide therapeutic index and may be administered to elderly patients or those with underlying cardiovascular disorders. However, as with other serotonin reuptake inhibitors, sertraline has been associated with gastrointestinal disturbances (nausea, diarrhoea/loose stools) and male sexual dysfunction (primarily ejaculatory disturbance), although each of these effects is usually mild and transient, decreasing in frequency with continued treatment. As a drug class, serotonin reuptake inhibitors such as sertraline appear to provide significant advantages compared with the more established antidepressant agents, particularly in terms of tolerability. Although much broader clinical experience is required before sertraline's full therapeutic potential can be realised, if future studies confirm the encouraging initial findings, sertraline will undoubtedly become an important option in the treatment of depression.
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PMID:Sertraline. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depression and obsessive-compulsive disorder. 128 Oct 75

The pharmacology and pharmacokinetics, adverse effects, drug interactions, efficacy, and dosage and administration of the new selective serotonin reuptake inhibitors paroxetine, sertraline, and fluvoxamine are reviewed. Paroxetine, sertraline, and fluvoxamine all have large volumes of distribution and are highly bound to plasma proteins. In contrast to fluoxetine, these three drugs possess shorter elimination half-lives of approximately one day and are metabolized to clinically inactive compounds. Nausea was the most commonly reported adverse effect for all three agents. Other reported adverse effects are headache, sedation, dry mouth, insomnia, sexual dysfunction, and constipation. Because of their favorable pharmacokinetic profiles, paroxetine, sertraline, and fluvoxaetine are less likely than fluoxamine to interact with other drugs. Paroxetine has been found to be superior to placebo and equivalent to amitriptyline, imipramine, clomipramine, and doxepin in treatment of depression. Sertraline has been found to be superior to placebo and equivalent to amitriptyline in treatment of depression. Fluvoxamine has been found to be superior to placebo and equivalent to imipramine, clomipramine, desipramine, mianserin, and maprotiline in the treatment of depression. Fluvoxamine and sertraline have been shown to be superior to placebo in the treatment of obsessive-compulsive disorder. Clinical experience has demonstrated all three drugs to be effective in treatment of depression. They may be especially useful in elderly patients, in those who cannot tolerate alternative treatments, and in those who do not respond to adequate trials of other antidepressant therapies.
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PMID:Paroxetine, sertraline, and fluvoxamine: new selective serotonin reuptake inhibitors. 146 19

Sertraline hydrochloride is a new naphthylamino compound that specifically blocks neuronal reuptake of serotonin. It is currently available in the United Kingdom and under review in the US. Sertraline follows first-order kinetics, with a plasma elimination half-life of 24-26 hours. It is highly bound to plasma proteins and has a large volume of distribution. Multicenter studies conducted by the manufacturer have shown sertraline to be efficacious in the treatment of depression and obsessive-compulsive disorder. The daily dose will range from 50 to 200 mg/d for the treatment of depression. The adverse-effect profile differs greatly from the tricyclic antidepressants, but is similar to that of fluoxetine. The most prominent adverse effects are gastrointestinal (nausea, diarrhea/loose stools, dyspepsia).
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PMID:Sertraline: a new specific serotonin reuptake blocker. 194 75

Two hundred forty-one elderly depressed patients entered the 8-week, double-blind phase of this parallel-group, multicenter study; 161 patients were randomized to receive sertraline (50-200 mg/day) and 80 were randomized to receive amitriptyline (50-150 mg/day). Among evaluable patients, there were no statistically significant differences between treatments in any of the primary efficacy variables: change in total Hamilton Rating Scale for Depression (HAM-D) score (17 items), percentage change in HAM-D score, change in HAM-D Item 1, change in Clinical Global Impressions (CGI) Severity score, change in the Depression Factor of the 56-item Hopkins Symptom Checklist, and the CGI Improvement score at the last visit. Similar results were obtained using data from all patients (intention-to-treat analysis), except that amitriptyline was superior in HAM-D Total score (p = .044). The two drugs produced a similar degree of response: on the basis of the HAM-D criterion, 69.4% of sertraline patients and 62.5% of amitriptyline patients responded, and, on the basis of CGI criterion, 79.5% of sertraline and 73.4% of amitriptyline patients responded. Twenty-eight percent of the sertraline patients withdrew from the study because of a treatment-related side effect and 2.5% (4) because of a laboratory abnormality. In comparison, 35% of the amitriptyline patients withdrew because of treatment-related side effects. Sertraline was associated with a statistically lower frequency of somnolence, dry mouth, constipation, ataxia, and pain and a higher frequency of nausea, anorexia, diarrhea/loose stools, and insomnia; thus, anticholinergic effects were less common and gastrointestinal effects were more common with sertraline than with amitriptyline.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Double-blind, multicenter comparison of sertraline and amitriptyline in elderly depressed patients. 225 79

The authors review preclinical data; clinical pharmacology data; and efficacy data of sertraline, a novel serotonin uptake inhibitor. Both in vitro and in vivo, sertraline is a potent and specific serotonin uptake inhibitor (possessing up to 10 times the activity of similar agents). Chronic dosing produces down-regulation of beta-adrenergic receptors. In man, sertraline inhibits platelet serotonin uptake and is devoid of obvious cardiac effects. The plasma half-life of sertraline is 25 hours. Studies on psychomotor performance show little or no effect at doses up to 100 mg, whereas 200 and 400 mg appear to possess some sedating action. Sertraline exhibits acute antidepressant effects in the dose range 50 to 200 mg/day; in addition, in the same dose range it prevents recurrence of depression. Its side-effect profile is similar to that of drugs of the same class (dry mouth, nausea, and diarrhea being the most prominent); it lacks the obvious anticholinergic and sedating effects of amitriptyline.
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PMID:Sertraline: a new antidepressant. 284 21

A double-blind, placebo-controlled, crossover study in 12 subjects (greater than or equal to 50 years) compared the effects of single oral doses of sertraline (100 mg) and amitriptyline (50 mg) with placebo as assessed by psychomotor function testing. Unlike sertraline and placebo, amitriptyline increased tracking error severity and impaired digit/symbol substitution. Sertraline slightly improved flicker frequency recognition. Both active drugs caused subjective drowsiness, although amitriptyline's effect was greater and of longer duration. Both drugs impaired subjectively assessed performance. Sertraline caused nausea, and amitriptyline, dry mouth; sertraline tended to increase supine systolic blood pressure. The authors conclude that sertraline has a considerably less detrimental effect on psychomotor performance and may have a slight activating effect not found with amitriptyline.
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PMID:Acute effects of sertraline, amitriptyline, and placebo on the psychomotor performance of healthy subjects over 50 years of age. 304 13

Sertraline is a highly specific, potent inhibitor of serotonin reuptake. It exerts no clinically significant effects on norepinephrine and dopamine uptake and possess negligible binding affinity for histaminergic, muscarinic, dopaminergic, and adrenergic receptors. Its pharmacologic profile permits once-daily dosing while allowing plasma drug levels to equilibrate within 1 week. In multicenter, double-blind trials, sertraline proved superior to placebo and comparable to amitriptyline in ameliorating acute depression. Moreover, the drug has been shown to be effective in preventing relapses of the index episode and recurrence of further episodes over the long term. Sertraline has not been associated with sedating or anticholinergic effects, psychomotor impairment, or cardiovascular toxicity. Its principal side effects are generally transient and include mild-to-moderate nausea or diarrhea and sexual dysfunction (ejaculatory delay) in males. The safety margin of sertraline is wider than that of the tricyclic antidepressants. This serotonin reuptake inhibitor shows promise as an important therapeutic and prophylactic alternative in the pharmacologic management of depression.
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PMID:The role of sertraline in the management of depression. 785 36

Sertraline is a selective serotonin reuptake inhibitor (SSRI) for which marketing approval has been obtained recently in Germany. The results of several double-blind, placebo-controlled studies have demonstrated that sertraline has a clear antidepressive effect. However these studies have been conducted in outpatient populations. In the context of this multicenter study, a total of 160 inpatients were treated with sertraline 50-150 mg or amitriptyline 75-225 mg over a period of 6 weeks in a double-blind fashion. Sixty-two patients in the sertraline and 59 patients in the amitriptyline group were evaluated for efficacy in the according-to-protocol (ATP) population; 80 sertraline and 75 amitriptyline patients were evaluated for safety in the Intention-to-treat population (ITT). No statistically significant differences were detected between the two groups in the efficacy analysis performed on the basis of the Hamilton Depression Scale (HAM-D) total score and Clinical Global Impression (CGI). Due to its sedating properties, amitriptyline was found to be significantly more effective with regard to the HAM-D factor "sleep disturbance". The safety analysis, which was based on the CGI, the global assessment at the end of study and a score for somatic adverse events (FSUCL) revealed statistically significant advantages of sertraline over amitriptyline. Amitriptyline was associated with more autonomic and circulatory side effects, while epigastric complaints occurred more often with sertraline. The incidence of nausea - a typical SSRI side effect - was the same in both groups.
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PMID:Double-blind, multicenter comparative study of sertraline and amitriptyline in hospitalized patients with major depression. 983 48

Sertraline (SRT) has been shown to be an effective antidepressant in extensive clinical trial programs but data on plasma concentrations regarding clinical outcome and tolerability are lacking. Twenty-one out-patients of both sexes, with mean age of 50.23 years (S.D. = 17.37), affected by major depressive disorder, recurrent (Diagnostic and Statistical Manual of Mental Disorder--IV, DSM-IV), were treated with 25-150 mg of SRT once a day (mean=66.26 mg, S.D.=30.50) for 30 days. Clinical evaluation was assessed at baseline (T0), after 15 days (T15), and then after 30 days (T30). Plasma samples for SRT level determination were collected at T30. Brief Psychiatric Rating Scale (BPRS), Hamilton Rating Scale for Depression (HRS-D), and Hamilton Rating Scale for Anxiety (HRS-A) showed a significant improvement during the study (P<.01 vs. T0). The most commonly reported side effects were nausea (19%), cephalalgia (9.5%), dry mouth (9.5%), decreased libido (9.5%), tremor (4.7%), and tachycardia (4.7%). SRT plasma levels ranged from 2.82 to 112.20 ng/ml (mean=40.42 ng/ml, S.D.=26.93). No correlation between SRT plasma levels and clinical improvement or side effects were observed. Drug plasma level determination does not seem be strictly necessary from a clinical point of view but further research seems advisable in patients at risk like elderly and during long-term studies.
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PMID:Clinical outcome and tolerability of sertraline in major depression: a study with plasma levels. 1199 14

(1) The choice of treatment for children with obsessive-compulsive disorder is difficult. Behaviour therapy and antidepressants have not been assessed adequately in this setting, and their efficacy seems limited. Clomipramine was the first antidepressant to show a degree of efficacy. (2) Sertraline is the first drug to be licensed in France for children aged from 6 to 17 years with obsessive-compulsive disorder. (3) According to our literature search, the evaluation file on sertraline in this indication mainly contains data from a double-blind placebo-controlled trial involving 187 children. After 3 months of treatment, sertraline was significantly more effective than placebo, although most children remained symptomatic. Direct comparison is lacking, but sertraline seems as effective as clomipramine. (4) However, 13% of children receiving sertraline left this trial because of adverse events (3% on placebo; p = 0.02). The short-term safety profile of sertraline in children is the same as in adults, i.e. mainly nausea, agitation, headache, insomnia and tremor. (5) We have no data on the effects of prolonged sertraline therapy in children, particularly on neuropsychological development. (6) The first-line treatment of obsessive-compulsive disorder is behaviour therapy. Sertraline, like clomipramine, is an option when behaviour therapy fails or is unfeasible. The choice between sertraline and clomipramine should be discussed case by case, according to their safety profiles; however, we have more experience with clomipramine, which should therefore be preferred over sertraline.
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PMID:Sertraline: new indication. May help children with obsessive-compulsive disorder. 1206 39


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