Selective serotonin reuptake inhibitors Fluvoxamine Paroxetine Sertraline

A number of successful case reports, open trials and randomized controlled trials have been published with the selective serotonin reuptake inhibitors (SSRIs) fluoxetine, sertraline, paroxetine, and fluvoxamine in the treatment of adult PTSD (see reviews by Connor and Davidson, 1998 Hidalgo and Davidson, 2000). Two SSRIs, fertraline and paroxtine, have recently received FDA approval for treatment of PTSD in adults (Brady et ah, 2000 Marshal et al., 2001). Surprisingly, there are no reports of the use of SSRIs in pediatric... 

The first-line therapeutic options for PMDD include the selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine, fluvoxamine, sertraline, paroxetine, and citalopram. These agents can be given either continuously or only during the luteal phase of the menstrual cycle, i.e., initiated at the time of ovulation and discontinued on the first day of menses. 

Other Antidepressants. Antidepressant refinements for the next 30 years primarily consisted of the development of new TCAs. However, in 1988, a novel antidepressant class, the selective serotonin reuptake inhibitors (SSRIs), was introduced in the United States. The chief innovation of the SSRIs was that they afforded the comparable effectiveness of the TCAs with fewer side effects and minimal toxicity. The debut of the SSRIs coincided with the reworking of the nosology of the anxiety disorders in DSM-III and DSM-IV. As a result, the SSRIs have been studied extensively in each of the respective anxiety disorders and in many cases have obtained FDA approval for the treatment of one or more of these anxiety syndromes. The SSRIs currently available in the United States include citalopram (Celexa), escitalo-pram (Lexapro), fluoxetine (Prozac), fluvoxamine (Luvox), paroxetine (Paxil), and sertraline (Zoloft). 

The TCAs were once widely used to treat depression in brain-injured patients, but they have been replaced as first-line treatments by the so-called selective serotonin reuptake inhibitors (SSRIs) including citalopram (Celexa), fluoxetine (Prozac), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft), and, most recently. 

Selective serotonin reuptake inhibitors. Currently available selective serotonin reuptake inhibitors (SSRIs) include fluoxetine, paroxetine, sertraline, fluvoxamine, and citalopram. At present, expert opinion does not support the usefulness of these serotonergic compounds in the treatment of core ADHD symptoms (National Institute of Mental Health, 1996). Nevertheless, because of the high rates of comorbidity in ADHD, these compounds are frequently combined with effective anti-ADHD agents (see Combined Pharmacotherapy, below). Since many psychotropics are metabolized by the cytochrome P450 system (Nemeroff et ah, 1996), which in turn can be inhibited by the SSRIs, caution should be exercised when combining agents, such as the TCAs, with SSRIs. 

FIGURE 39.2 Treatment algorithm for pediatric obsessive-compulsive disorder (OCD). In adjusting cognitive behavior therapy (CBT), increase frequency or intensity, or alter the setting or format, e.g., have it be home based or day treatment. CMI, clomipramine DMI, desipramine NT, nortriptyline SSRI, selective serotonin reuptake inhibitor (fluoxetine, fluvoxamine, paroxetine, sertraline, citalopram). 

Selective serotonin reuptake inhibitors fluoxetine hydrochloride fluvoxamine maleate paroxetine hydrochloride sertraline hydrochloride... 

Although the efficacy of tricyclic antidepressants in the treatment of unipolar depression is beyond reproach, the side-effect profile of these agents makes them less desirable as first-line therapeutic agents. Introduction of selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine, paroxetine, sertraline, citalopram and fluvoxamine in the past decade has revolutionized the treatment of depression universally. The side-effect profile of SSRIs, such as nausea, diarrhea and sexual dysfunction, is considerably more benign than that of tricyclic drugs. Multiple controlled trials have proven the efficacy of SSRIs vs. placebo (Nemeroff, 1994). Recently, a number of SNRIs (serotonin and noradrenaline reuptake inhibitors) and so-called atypical antidepressants have been marketed that may have additional advantages over SSRIs, such as more rapid onset of action (venlafaxine. mirtazapine) and low sexual side-effect potential ( bupropion, nefazodone). Additionally, it appears that venlafaxine may be more efficacious in cases of treatment-refractory depression (Clerc et al., 1994 Fatemi et al., 1999). Finally, in a recent report (Thase et al., 2001),... 

The selective serotonin reuptake inhibitors (SSRIs) represent a chemically diverse class of agents that have as their primary action the inhibition of the serotonin transporter (SERT) (Figure 30-3). Fluoxetine was introduced in the United States in 1988 and quickly became one of the most commonly prescribed medications in medical practice. The development of fluoxetine emerged out of the search for chemicals that had high affinity for monoamine receptors but lacked the affinity for histamine, acetylcholine, and adrenoceptors that is seen with the tricyclic antidepressants (TCAs). There are currently six available SSRIs, and they are the most common antidepressants in clinical use. In addition to their use in major depression, SSRIs have indications in GAD, PTSD, OCD, panic disorder, PMDD, and bulimia. Fluoxetine, sertraline, and citalopram exist as isomers and are formulated in the racemic forms, whereas paroxetine and fluvoxamine are not optically active. Escitalopram is the S enantiomer of citalopram. As with all antidepressants,... 

Selective serotonin reuptake inhibitors (SSRIs) [P] Fluoxetine and paroxetine inhibit CYP2D6 and decrease metabolism of antidepressants metabolized by this enzyme (eg, desipramine). Citalopram, sertraline, and fluvoxamine are only weak inhibitors of CYP2D6, but fluvoxamine inhibits CYP1A2 and CYP3A4 and thus can inhibit the metabolism of antidepressants metabolized by these enzymes. 

Grimsley, S., 8c Jann, M. (1992). Paroxetine, sertraline, and fluvoxamine New selective serotonin reuptake inhibitors. Clinical Pharmacy, 11, 930—957. 

Selective serotonin reuptake inhibitors (SSRIs) A relatively new group of medicines that have been used successfully to treat emotional and behavioral problems such as depression, panic disorder, obsessive-compulsive disorder ((XID), bulimia, and posttraumatic stress disorder in adults. These medications are now being used to treat the same types of behavior in children. Some examples of SSRIs include Prozac (fluoxetine), Zoloft (sertraline), Luvox (fluvoxamine), and Paxil (paroxetine). 

Sertraline, at its usual effective dose of 50 mg/day, has been found to cause less pronounced modifications in plasma concentrations of tricyclic antidepressants (TCAs) as compared with other selective serotonin reuptake inhibitors (SSRIs) (mainly studies with fluoxetine, fluvoxamine, and paroxetine). However, since inhibition of the hepatic enzyme CYP2D6 is dose-dependent, significant increase in plasma concentration of TCAs may occur when higher doses of sertraline are administered. Acute liver damage possibly related to sertraline and venlafaxine ingestion has been reported. 

Selective serotonin reuptake inhibitors (SSRIs) are regarded as first-line treatment in social phobia. Fluvoxamine, paroxetine, and sertraline have been shown to be effective in double-blind placebo-controlled studies. - The irreversible monoamine oxidase inhibitor (MAOI) phenelzine shows robust results in terms of efficacy and has demonstrated (at least anecdotally), its efficacy in improving some of the cognitive aspects associated with SAD. However, phenelzine is usually less well tolerated than alternative treatments due to its associated dietary restrictions and adverse side-effect profile, including sedation and postural hypotension. Results with the reversible inhibitor of monoamine oxidase type A (RiMA) mociobemide are inconsistent. 

Selective serotonin reuptake inhibitors Fluoxetine Fluvoxamine Citalopram, paroxetine, sertraline... 

Fig. 22.21. Structures of the selective serotonin reuptake inhibitors (SSRIs) fluoxetine, fluvoxamine, paroxetine, sertraline, and escitalopram.

Several selective serotonin reuptake inhibitors (SSRIs), including escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline (Fig. 22.21), are effective as first-line treatment cf seme anxiety disorders, with the purported advantage that they lack the addictive preperties cf benzediazepines (135). Specifically, the SSRIs have been shown to be effective in obsessive-ccmpulsive diserder (139), panic disorder (140), and social phobia (141). The mechanism of action of these agents in anxiety may differ with their role in the treatment of depression however,... 

SSRIs (Selective serotonin reuptake inhibitors) Citalopram, Escitalopram, Femoxetine, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline... 

In a study on the effects of maca for sexual dysfunction induced by selective serotonin reuptake inhibitors (SSRI), patients who were stable on an SSRI (patients were taking escitalopram, citalopram, sertraline, venlafexine, fluoxetine, paroxetine, duloxetine, or fluvoxamine) were orally administered 1.5 or 3 g of maca daily for 12 weeks. No adverse effects of maca, including effects on SSRI efficacy, were reported, and patients in the high dose group had a modest improvement in depression (Dording et al. 2008). 

Citalopram, a new serotonin uptake inhibitor (20 to 60 mg) is an effective antidepressant. Together with fluoxetine, fluvoxamine, paroxetine, and sertraline, it belongs to the group of selective serotonin reuptake inhibiting (SSRI) antidepressants (see also Tables 5 through 7 and Figure 51). 

The older tricyclic agents show less than a ten-fold selectivity in inhibiting noradrenaline over that for 5-HT (e.g. desipramine, imipramine, nortriptyline) through amitryptyline. which shows virtually no selectivity, to trazodone, zimelidine and clomipramine, which are somewhat 5-HT selective. The newer Serotonin-Selective Reuptake Inhibitors (SSRIs) show a higher selectivity for inhibition of 5-HT reuptake in the brain, and have a different pharmacology. Examples clinically used include citalopram, fluoxetine, fluvoxamine, nefazodone, paroxetine, sertraline, trazodone and venlafaxine. Experimental agents include 6-nitroquipazine, alaproclate, litoxetine, indatraline and p-CIT. 

Sedatives or anticonvulsants (e.g., carbamazepine, oxcarbazepine, phenobarbital, and pheny-toin, but not valproate) that induce CYPs (see Chapter S) can enhance the metabolism of antipsychotic and many other agents (including anticoagulants and oral contraceptives), sometimes with significant clinical consequences. Conversely, selective serotonin (5-HT) reuptake inhibitors including fluvoxamine, fluoxetine, paroxetine, venlafaxine, sertraline, and nefazodone (see Chapter 17) compete for these enzymes and can elevate circulating levels of neuroleptics. 

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