The principal initial pathway of metabolism for sertraline is N-demethylation. N-desmethylsertraline has a plasma terminal elimination half-life of 62 to hours.
Both in vitro biochemical and in vivo pharmacological testing have shown N-desmethylsertraline to be substantially less active than sertraline. Both sertraline and N-desmethylsertraline undergo oxidative deamination and subsequent reduction, hydroxylation, and glucuronide conjugation. Unchanged sertraline was not detectable in the urine. Desmethylsertraline exhibits time-related, dose dependent increases in AUC hour , Cmax and Cmin, with about a 5- to 9-fold increase in these pharmacokinetic parameters between day 1 and day Steady-state, therefore, was achieved after 2 to 3 weeks in older patients.
The same study showed a decreased clearance of desmethylsertraline in older males, but not in older females [See Use in Specific Populations ]. The exposure to desmethylsertraline was approximately 2-fold greater in patients with mild hepatic impairment compared to age-matched volunteers with normal hepatic function. There were no significant differences in plasma protein binding observed between the two groups.
Renal Impairment Sertraline is extensively metabolized and excretion of unchanged drug in urine is a minor route of elimination. Thus sertraline multiple dose pharmacokinetics appear to be unaffected by renal impairment [See Use in Specific Populations ]. The drugs for which this potential interaction is of greatest concern are those metabolized primarily by CYP2D6 and that have a narrow therapeutic index e.
The extent to which this interaction is an important clinical problem depends on the extent of the inhibition of CYP2D6 by the antidepressant and the therapeutic index of the co-administered drug. How should I take Zoloft? When should Zoloft not be taken? What precautions should I follow when taking Zoloft? What special warning s should I be aware of when taking Zoloft? What are the side effects of Zoloft?
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Use of sertraline during the 3rd trimester of pregnancy may lead to adverse effects in the newborn. Use of sertraline by nursing mothers has not been adequately evaluated. What else should I know about Zoloft sertraline? What preparations of Zoloft sertraline are available? Sertraline should be stored at room temperature between 15 C and 30 C 59 F and 86 F. How does Zoloft sertraline work? April format for version difficulty. Underage dose mouth in the price name brand zoloft happy phone of the data may be generally direct as an all reductase combination lack insurance.
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