Fluoxetine nervous system

Serotonin mediates many central and peripheral physiological functions, including contraction of smooth muscle, vasoconstriction, food intake, sleep, pain perception, and memory, a consequence of it acting on several distinct receptor types. Although 5-HT may be metabolized by monoamine oxidase, platelets and neurons possess a high-affinity mechanism for reuptake of 5-HT. This mechanism may be inhibited by the widely prescribed antidepressant drugs termed selective serotonin re-uptake inhibitors (SSRl), e.g. fluoxetine (Prozac ), thereby increasing levels of 5-HT in the central nervous system. 

Sertraline is a recent antidepressant that is called a selective serotonin reuptake inhibitor (SSRI). It is chemically unrelated to the older tricyclic antidepressants (see Section 5.3). It works by preventing the movement of the neurohormone serotonin into nerve endings. It can help to improve mood and mental alertness, increase physical activity, and improve sleep patterns. It is prescribed for obsessive-compulsive disorder and obesity. It may offer some advantage over fluoxetine by exhibiting little central nervous system (CNS) action. It has less sedation and anxiety and is shorter acting. 

Hollander E, Schiffman E, Cohen B, et al Signs of central nervous system dysfunction in obsessive-compulsive disorder. Arch Gen Psychiatry 47 27-32, 1990b Hollander E, Mullen L, DeCaria CM, et al Obsessive compulsive disorder, depression, and fluoxetine. J Clin Psychiatry 52 418-422, 1991 Hollander E, De Caiia CM, Nitescu A, et al Serotonergic function in OCD. Arch Gen Psychiatry 49 21-28, 1992... 

FLUOXETINE, FLUVOXAMINE, PAROXETINE BZDs - ALPRAZOLAM, DIAZEPAM, MIDAZOLAM t in plasma concentrations of these BZDs. Likely t sedation and interference with psychomotor activity Alprazolam, diazepam and midazolam are subject to metabolism by CYP3A4. Fluvoxamine, fluoxetine and possibly paroxetine are inhibitors of CYP3A4 sertraline is a weak inhibitor. SSRIs are relatively weak compared with ketoconazole, which is possibly 100 times more potent as an inhibitor Warn patients about risks associated with activities that require alertness. Consider use of alternatives such as oxazepam, lorazepam and temazepam, which are metabolized by glucuronidation >- For signs and symptoms of CNS depression, see Clinical Features of Some Adverse Drug Interactions, Central nervous system depression... 

Selective serotonin reuptake inhibitors (SSRIs) inhibit the neuronal reuptake of serotonin in the central nervous system and have shown mixed efficacy in the treatment of autistic symptoms (Moore et al., 2004). A number of studies have shown reductions in repetitive behaviors, lethargy, inappropriate speech, and improvements in the ability to relate to others, cognition, language improvement with fluoxetine (DeLong et al., 1998 Fatemi et al., 1998 Peral et al., 1999), fluvoxamine (McDougle et al., 1996b), and sertraline (Steingard et al., 1997). However, other studies have shown a lack of response with fluvoxamine (Martin et al., 2003) and citalopram (Couturier and Nicolson, 2002). 

Fluoxetine has been found to cause selective central nervous system (CNS) neuronal uptake inhibition of serotonin. While fluoxetine may bind to adrenergic, muscarinic, and histaminic receptors, it has not been shown to have the profound effects on catecholamines that are common to tricyclic antidepressant overdose patients. 

MR-visible fluorinated compounds that can be measured in the human brain comprise a large number of psychiatric medications including most of the serotonin-specific reuptake inhibitors (SSRIs) such as fluoxetine (Prozac ) [1, 28, 41], as well as pharmaceuticals with mechanisms of action outside the central nervous system such as dexfenfluramine (fen-phen, a serotoninergic anorectic drug) [1, 31]. A recent review [1] covers the impact of MR spectroscopy in psychiatry. 

Fluoxetine (Prozac, Eli Lilly) Central nervous system GPCR... 

Casamenti et al. [1399] developed a method for screening 11 central nervous system drugs (phenobarbital, olanzapine, clozapine, risperidone, loxapine, haloperidol, imipramine, amitriptyline, fluoxetine, chlorpromazine, paroxetine) on a Cjg column (A = 230 nm) using a 20/11.7 water (0.4g tetramethylammonium perchlorate with 0.2 mL of 7% (m/m) HCIO4 to pH 2.8 with ammonia)/acetonitrile mobile phase. Keep in mind that perchlorates, when concentrated with some metals, are hazardous. Elution was complete in 35 min with good resolution for most compounds. Plots of the effects of mobile phase modifier level and percent acetonitrile on overall retention are presented. Linear ranges of 25-5000 ng/mL with detection limits of 10-250 ng/mL (analyte dependent) are reported. 

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