Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0027066 (myoclonus)
4,275 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Fluoxetine is a bicyclic antidepressant that is a specific and potent inhibitor of the presynaptic reuptake of serotonin. It has essentially no effect on the reuptake of norepinephrine or other neurotransmitters. Similarly, it has negligible binding affinity for neurotransmitter receptor sites. It is well absorbed after oral administration, with absolute bioavailability in dogs of approximately 72 +/- 27.6%. The mean Tmax is between 4 and 8 hours, and it is approximately 94% protein bound. After a single dose, the elimination half-life is 1-3 days. After long-term administration, the elimination half-life averages 4 days. Its pharmacokinetics appear nonlinear. It is metabolized to an active metabolite norfluoxetine, which is also specific for the inhibition of serotonin reuptake. Norfluoxetine's elimination half-life averaged 7 days after long-term administration. Little is known about potential drug interactions; however, fluoxetine appears to have minimal clinically relevant interactions. Fluoxetine is indicated in the treatment of major depression. Its efficacy is comparable to the tricyclics and it has a similar onset of action. Although doses as high as 80 mg/day have been used, the optimal dosage range appears to be 20-40 mg once daily. Fluoxetine has been used with success in obsessive-compulsive disorder and intention myoclonus, however, its use in these disorders remains investigational. The frequency of side effects is low and dose related; the most common effects are nausea, anxiety, insomnia, anorexia, diarrhea, nervousness, and headache. Eight reports of intentional overdose with fluoxetine alone resulted in no deaths and mild adverse effects. It will be marketed as 20-mg capsules under the brand name of Prozac. Although fluoxetine should be added to formularies, its use should be reserved for treatment of those who do not respond to or do not tolerate tricyclic agents.
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PMID:Fluoxetine: a serotonin-specific, second-generation antidepressant. 355 56

Some types of intention myoclonus respond to serotonin precursor therapy (e.g., L-5-hydroxytryptophan, L-5HTP). Fluoxetine, a specific serotonin (5HT) uptake blocker, was found to have no antimyoclonic effect when administered by itself to four patients with intention myoclonus. However, in two patients with intention myoclonus responsive to L-5HTP and carbidopa, fluoxetine reduced the required dose of L-5HTP to approximately one-third, with greater antimyoclonic activity, decreased side effects, and reduction in platelet 5HT and plasma 5-hydroxyindoleacetic acid and L-5HTP concentrations. These findings further support the hypothesis that some forms of intention myoclonus are caused by a deficiency of brain 5HT, and suggest that the addition of fluoxetine to L-5HTP and carbidopa may improve antimyoclonic therapy.
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PMID:Fluoxetine in the treatment of intention myoclonus. 618 99

There is a new, potentially fatal disorder that is infrequently reported. The apparent rareness may be because of a lack of recognition of the syndrome or its predisposing factors. Fluoxetine (Prozac, Dista Products Co, Division of Eli Lilly Co, Indianapolis, IN), sertraline (Zoloft, Roerig Division, Pfizer Inc, New York, NY), and paroxetine (Paxil, SmithKline Beecham Pharmaceuticals, Philadelphia, PA) belong to a new class of antidepressant medication: the serotonin reuptake-inhibitors (SRIs). The relative safety profile of the SRIs has led to their widespread use. However, a syndrome of excessive serotonergic activity, the "serotonin syndrome" (SS), has recently been recognized. It is characterized by changes in mental status, hypertension, restlessness, myoclonus, hyperreflexia, diaphoresis, shivering, and tremor. A high index of suspicion is required to make the diagnosis in these acutely ill patients. The most common agents implicated in SS are the monoamine oxidase inhibitors in combination with L-tryptophan or fluoxetine. A case of a patient with significant peripheral vascular disease who developed SS while taking paroxetine and an over-the-counter cold medicine is reported. There have been no prior reports of this interaction. Discontinuation of the offending agents, sedation, and supportive care are the mainstays of treatment. The interactions of serotonin with platelets and vascular endothelium are also discussed.
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PMID:The serotonin syndrome associated with paroxetine, an over-the-counter cold remedy, and vascular disease. 766 67

The antidepressant efficacy of fluoxetine in major depression has been briefly reviewed. A brief outline of dose selection, therapeutic onset, and pharmacokinetics of fluoxetine were made. The potential use of the drug in management of various psychiatric conditions has been examined. These include obsessive-compulsive disorder and related variances, anorexia nervosa, bulimia nervosa, Tourette's syndrome, and trichotillomania. The suggested use of fluoxetine in pain relief in certain diabetics, premenstrual syndrome, and migraine headache were assessed. The reports on the use of fluoxetine in panic disorders, paraphilias, and related conditions and in the management of substance abuse, alcoholism, and cocaine abuse, were summarized and elaborated upon. A composite of preliminary reports cited in literature pertinent to the potential of fluoxetine in treatment of abusing injurious behavior, dysthymic disorder, fibrositis, postanoxicaction myoclonus, pathologic jealously, personality disorder, pseudobulbar affect, and social phobia were also reviewed. Fluoxetine pharmacological profile may be extended to cover a relative wide range of application, provided future controlled studies confirm the preliminary data found in the literature.
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PMID:Fluoxetine: a spectrum of clinical applications and postulates of underlying mechanisms. 830 48