SERTRALINE

B. In studies of radiolabeled sertraline, 40 to 45% of an administered dose is recovered in the feces in 9 days; 12 to 14% is excreted as unchanged sertraline (Prod Info Zoloft(R), 1992).

8.4.4 OTHER

A. BREAST MILK - It is unknown whether sertraline and its metabolites are excreted in breast milk (Prod Info Zoloft(R), 1992).

8.5 ELIMINATION HALF-LIFE

8.5.1 PARENT COMPOUND

A. GENERAL

1. The elimination half-life of sertraline is approximately 24 hours (Doogan & Caillard, 1988; Saletu et al, 1986).

8.5.2 METABOLITE

A. GENERAL

1. The elimination half-life of the metabolite desmethylsertraline ranges from 66 hours (Doogan & Caillard, 1988) to 80 hours (Saletu et al, 1986). According to the manufacturer, the elimination half-life of N-desmethylsertraline ranges from 62 to 104 hours (Prod Info Zoloft(R), 1992).

9.0 PHARMACOLOGY/TOXICOLOGY

9.1 PHARMACOLOGIC MECHANISM

A. The mechanism of action is thought to be associated with sertraline's ability to inhibit central nervous system neuronal uptake of serotonin (Jefferis, 1992).
B. Sertraline does not show significant affinity for adrenergic, cholinergic, GABA, dopaminergic, histaminergic, serotonergic, or benzodiazepine receptors when tested in vitro (Jefferis, 1992).

1. It has a greater selectivity for inhibiting 5-HT uptake relative to norepinephrine than any other drug in this class of therapeutic agents (Koe et al, 1983).

12.0 REFERENCES

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13.0 AUTHOR INFORMATION

13.1 CONTRIBUTOR(S) TO THIS DOCUMENT

A. Original publication: 08/92
B. Most recent revision: 11/00
C. List of contributors:

§ 1. Anthony Manoguerra, PharmD

§ 2. Katherine M Hurlbut, MD

§ 3. Lada Kokan, MD

§ 4. Barry H Rumack, MD

§ 5. POISINDEX(R) Editorial Staff

D. Specialty Board: PSYCHOACTIVE

Refer to the POISINDEX EDITORIAL BOARD section for more information. (MG0847)

End of Document