Citalopram side effects profile

SSRIs are widely used for treatment of depression, as well as, for example, panic disorders and obsessive—compulsive disorder. These dmgs are well recognized as clinically effective antidepressants having an improved side-effect profile as compared to the TCAs and irreversible MAO inhibitors. Indeed, these dmgs lack the anticholinergic, cardiovascular, and sedative effects characteristic of TCAs. Their main adverse effects include nervousness /anxiety, nausea, diarrhea or constipation, insomnia, tremor, dizziness, headache, and sexual dysfunction. The most commonly prescribed SSRIs for depression are fluoxetine (31), fluvoxamine (32), sertraline (52), citalopram (53), and paroxetine (54). SSRIs together represent about one-fifth of total worldwide antidepressant unit sales. 

Antidepressants are used in the treatment of neuropathic pain and headache. They include the classic tricyclic compounds and are divided into nonselective nor-adrenaline/5-HT reuptake inhibitors (e.g., amitriptyline, imipramine, clomipramine, venlafaxine), preferential noradrenaline reuptake inhibitors (e.g., desipramine, nortriptyline) and selective 5-HT reuptake inhibitors (e.g., citalopram, paroxetine, fluoxetine). The reuptake block leads to a stimulation of endogenous monoaminer-gic pain inhibition in the spinal cord and brain. In addition, tricyclics have NMDA receptor antagonist, endogenous opioid enhancing, Na+ channel blocking, and K+ channel opening effects which can suppress peripheral and central sensitization. Block of cardiac ion channels by tricyclics can lead to life-threatening arrhythmias. The selective 5-HT transporter inhibitors have a different side effect profile and are safer in cases of overdose [3]. 

Both enantiomers and the racemate of l-(3,4-dichlorophenyl)-3-azabicyclo [3.1.0]hexane, 27a-c, have been reported to be in development. The racemate, DOV 216,303, inhibits the reuptake of NE, 5-HT and DA with IC50 values of 20, 14 and 78 nM, respectively [85]. DOV 216,303 is active in tests predictive of antidepressant activity, including the mouse FST (minimum effective dose = lOmg/kg), reversal of tetrabenazine-induced ptosis and locomotor depression. DOV 216,303 was also reported to be well tolerated in phase I clinical trials [85,86], In a phase II study designed to explore safety and tolerability in depressed individuals, patients received either DOV 216,303 (50 mg, b.i.d.) or citalopram (20 mg, b.i.d.) for two weeks [85]. It was found that the side effect profile was not remarkably different between the two treatment groups. In addition, time-dependent reductions in Hamilton Depression Scores (HAM-D) were similar for both groups. 

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),... 

Dencker SJ, Hopfner Petersen HE. Side effect profile of citalopram and reference antidepressants in depression. In Montgomery SA, editor. Citalopram—The New Antidepressant from Lundbeck Research. Amsterdam Excerpta Medica, 1989 31. 

The SSRIs (paroxetine, fluoxetine, sertraline, fluvoxamine, citalopram) and SNRI (ven-lafaxine) have an impressive side-effect profile, and this has contributed to their widespread use. Possible adverse effects include nausea, insomnia, and agitation, but these are generally manageable and diminish over time. More significant is the association of the SSRIs with sexual dysfunction, in both men and women. These effects are longer lasting, and can occur in up to 40% of patients (79). A withdrawal syndrome has also been observed with the SSRIs, characterized by dizziness, headache, and irritability upon abrupt discontinuation. This is much less serious than that observed with benzodiazepines. 

Compared with other classes of antidepressants, SRIs have a more favorable side-effect profile and better efficacy data. A review of randomized, controlled trials with SRIs for the treatment of PMDD reported that the agents were well tolerated and effective in treating physical as well as behavioral symptoms with either intermittent or continuous dosing. Citalopram, fluoxetine, paroxetine, sertraline, and venlafaxine all have been effective in PMDD placebo-controlled trials (60% to 90% efficacy rates with almost complete relief of symptoms). For fluvoxamine, there are mixed results because one controlled study reported that it had similar efficacy to placebo treatment in PMDD. Although antidepressants usually take... 

Since their introduction in the 1980s, selective serotonin reuptake inhibitors (SSRls) such as paroxetine, fluoxetine, and citalopram have enjoyed tremendous clinical and commercial success due to their improved safety profile when compared with first-generation tricyclic antidepressants like imipramine. Nevertheless, they still display several side effects including gastrointestinal distress, anxiety, insomnia, weight gain, and sexual dysfunction. Like other current antidepressants. 

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