Zoloft (Sertraline)

• Generic name: Sertraline
• Trade names: Zoloft, Lustral (UK)
• Pharmacologic category: Selective serotonin reuptake inhibitor
• FDA Approved: December 30, 1991
• Manufacturer: Pfizer Inc.
• Habit forming? No
• Pregnancy risk factor: C

What is Zoloft?

Zoloft is a potent representative of selective serotonin reuptake inhibitors (SSRIs). Sertraline strongly affects serotonin and weakly affects noradrenaline and dopamine. Imbalance of these chemical in the brain may cause several mental and mood disorders such as depression, panic or anxiety.

Zoloft is approved to treat depression, social anxiety disorder, posttraumatic stress disorder (PTSD), panic disorder, obsessive-compulsive disorder (OCD), and premenstrual dysphoric disorder (PMDD) in adults over age 18. It is also approved for OCD in children and adolescents age 6-17 years.

The most common side effects are nausea, dry mouth, fatigue, and decreased libido.

Withdrawal and discontinuation

You should not suddenly stop taking Sertraline because abrupt discontinuation can cause withdrawal symptoms. The most common withdrawal symptoms are dizziness, nausea, anxiety, headache, agitation, insomnia, increased sweating. These symptoms can be alleviated by gradual tapering off, usually over a period of weeks or months.

Pharmacological characteristics

• Elimination half-life: 25-26 hr.
• Metabolism: extensively metabolized by the liver; undergoes metabolism via N-demethylation to form the principal metabolite N-desmethylsertraline. In laboratory tubes, the conversion of sertraline to N-desmethylsertraline correlates more with CYP3A3/4 isoenzyme activity than with CYP2D6.
• Excretion: renal (40–45%) and fecal (40–45%).

Benefits

• Relatively low risk of weight gain [8]
• The only medication approved for the long-term treatment of PTSD
• Low potential for drug interactions, involving hepatic metabolism.
• Minimal anticholinergic side effects
• Well tolerated and effective for chronic depression [9]
• Sertraline is a good choice for elderly people because its elimination is not affected substantially by aging.

Unlabeled uses

• general anxiety disorder [1]
• bulimia nervosa [2]
• premature ejaculation [3]
• autistic disorders [6]
• fibromyalgia [4]
• bipolar depression [5]
• binge eating disorder (BED) [7]

Mechanism of action

Sertraline inhibits central nervous system neuronal re-uptake of serotonin, thus increasing the concentration of the serotonin and enhancing the neuronal transmission. The increased levels of serotonin are thought to improve the symptoms of depression.

Sertraline also appears to be a minor dopamine reuptake inhibitor.

Food appears to increase the bioavailability by about 40%.

References

• 1. Allgulander C, Dahl AA, Austin C, Morris PL, Sogaard JA, Fayyad R, Kutcher SP, Clary CM. Efficacy of sertraline in a 12-week trial for generalized anxiety disorder. Am J Psychiatry. 2004 Sep;161(9):1642-9 PubMed
• 2. Milano W, Petrella C, Sabatino C, Capasso A. Treatment of bulimia nervosa with sertraline: a randomized controlled trial. Adv Ther. 2004 Jul-Aug;21(4):232-7. PubMed
• 3. Mendels J, Camera A, Sikes C. Sertraline for premature ejaculation. J Clin Psychopharmacol. 1995 Oct;15(5):341-6. PubMed
• 4. Gonzalez-Viejo MA, Avellanet M, Hernandez-Morcuende MI. A comparative study of fibromyalgia treatment: ultrasonography and physiotherapy versus sertraline. Ann Readapt Med Phys. 2005 Nov;48(8):610-5. PubMed
• 5. Post RM, Altshuler LL, Leverich GS, Frye MA, Nolen WA, Kupka RW, Suppes T, McElroy S, Keck PE, Denicoff KD, Grunze H, Walden J, Kitchen CM, Mintz J. Mood switch in bipolar depression: comparison of adjunctive antidepressants. Br J Psychiatry. 2006 Aug;189:124-31. PubMed
• 6. Hellings JA, Kelley LA, Gabrielli WF, Kilgore E, Shah P. Sertraline response in adults with mental retardation and autistic disorder. J Clin Psychiatry. 1996 Aug;57(8):333-6. PubMed
• 7. McElroy SL, Casuto LS, Nelson EB, Lake KA, Soutullo CA, Keck PE Jr, Hudson JI. Placebo-controlled trial of sertraline in the treatment of binge eating disorder. Am J Psychiatry. 2000 Jun;157(6):1004-6. PubMed
• 8. Maina G, Albert U, Salvi V, Bogetto F. Obsessive-compulsive disorder: a prospective comparison between serotonin reuptake inhibitors. J Clin Psychiatry. 2004 Oct;65(10):1365-71. PubMed
• 9. Keller MB, Kocsis JH, Thase ME, Gelenberg AJ, Rush AJ, Koran L, Schatzberg A, Russell J, Hirschfeld R, Klein D, McCullough JP, Fawcett JA, Kornstein S, LaVange L, Harrison W. Maintenance phase efficacy of sertraline for chronic depression: a randomized controlled trial. JAMA. 1998 Nov 18;280(19):1665-72.

By HealthyStock Research Group, October 2009
Medical resources reviewed: August 2018