Pharmacological Profile

Among the various antidepressant agents that block the 5-HTT, sertraline is second only to paroxetine in potency for 5-HT reuptake blockade, as demonstrated in animal models (Hiemke and Hartter 2000; Owens et al. 2001; Richelson 1994). The selectivity of sertraline over norepinephrine follows that of escitalopram (Hiemke and Hartter 2000; Owens et al. 2001), although other work suggests greater selectivity for fluvoxamine than for sertraline (Richelson 1994). The relative selectivity for the 5-HTT, compared with the dopamine transporter (DAT), is lowest for sertraline (Owens et al. 2001).

Sertraline exhibits inhibitory activity on several cytochrome P450 (CYP) enzymes. The ability of the compound to slightly elevate dextromethorphan and desipramine supports modest inhibition of CYP2D6 (Hiemke and Hartter 2000; Ozdemir et al. 1998; Preskorn 1996). It has little appreciable inhibition of CYP1A2, even when used at higher doses (Ozdemir et al. 1998). A very mild elevation of CYP2C9/10 substrates has been found in several studies (Preskorn 1996). Sertraline has complex effects on the CYP3A3/4 enzyme system: it initially shows slight inhibition, but it also induces this system, albeit modestly, over time (Preskorn 1996).

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