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Sertraline

Serotonin Uptake Inhibitors
CATEGORIES

Serotonin Uptake Inhibitors, Antidepressive Agents


ALIASES

Oralin, Sertralin Actavis, Sertralin Alpharma, Sertralin Alternova, Sertralin Amendia, Sertralin Bluefish, Sertralin Copyfarm, Sertralin Hexal, Sertralin IVAX, Sertralin Krka, Sertralin Mylan, Sertralin Orion, Sertralin Paranova, Sertralin Ranbaxy, Sertralin STADA, Sertralin Sandoz, Sertralin Teva, Sertralin Winthrop, Sertralin ratiopharm, Sertraline Accord, Sertrone, Setaloft, Zoloft, Zoloft®


SUBSTANCES

sertraline, sertraline hydrochloride


ENVIRONMENTAL CONCERN: HIGH
Sertraline hydrochloride belongs to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Despite distinct structural differences between compounds in this class, SSRIs possess similar pharmacological activity. As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine reuptake and do not antagonize α- or β-adrenergic, dopamine D2 or histamine H1 receptors. During acute use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT1A and terminal autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to enhanced serotonergic neurotransmission. Side effects include dry mouth, nausea, dizziness, drowsiness, sexual dysfunction and headache (see Toxicity section below for a more detailed listing of side effects). Compared to other agents in this class, sertraline may cause greater diarrheal and male sexual dysfunction effects. Side effects generally occur within the first two weeks of therapy and are usually less severe and frequent than those observed with tricyclic antidepressants. Sertraline may be used to treat major depressive disorder, obsessive-compulsive disorder (OCD), panic disorder, post-traumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD) and social anxiety disorder (social phobia).

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HIGH
The T-value in the score for hazard refers to acute toxicity. Underlying data for P, B and T are from Fass.se, see below.

Levels of several SSRI/SNRI exceed the concentrations that have an influence on aquatic organisms, particularly invertebrates. However, studies with the very least effect concentrations have been questioned. Sertraline has been detected i wild fish in concentrations near therapeutic levels in human. 

Sertraline is included in the Stockholm County Council's table of pharmaceuticals with risk for negative environmental impact according to the environmental program 2017-2021. Sertraline has been detected in treated wastewater in Stockholm County in the last five years (2012-2016).

Is recommended in The Wise List. Environmental classification of pharmaceuticals is taken into consideration, sometimes with other environmental aspects, when selecting pharmaceuticals for the Wise List. When comparable pharmaceuticals are equivalent to medical effects, safety and pharmaceutical efficacy, environmental impact and price are considered.

Below is Hazard and Risk from Fass environmental information for Zoloft (sertraline) (downloaded 2011-04-08)


Hazard
Persistence: "9-32% sertralin kvar efter 45 dagar biologisk nedbrytning aktiv slam metod; Indirekt fotolys, halveringstid 4,6 dagar."

Bioaccumulation: "Log Kow vid pH 7 = 2,9; Beräknad Log D vid pH 7,0 = 2,39; Beräknad BCF = 10,4."

Acute toxicity: There are data for 3 trophic levels, lowest for algae (Green algae) 14 days EC50 0.056 mg/L.

Risk
PEC/PNEC is based on sales data in Sweden in year 2007. PEC/PNEC = 6.96 which gives the risk moderate.

No new environmental information for sertraline is published on Fass.se (2018-07-10). It is voluntary for manufacturers to provide information on the environmental impact on fass.se.

Suggestions on how to reduce the release of sertraline
Concrete proposals on how to work to reduce emissions of environmentally harmful pharmaceuticals on the list have been developed in close cooperation with the Stockholm Drug and Therapeutics Committee's expert advice. The action proposals were developed from an environmental perspective. The patient's best always goes first and several pharmaceuticals on the list are also included in the Wise List. However, for such pharmaceuticals, there may be measures that could reduce the environmental impact.

Concrete proposal for sertraline
• In the first place, non pharmacological treatment and/or measures (eg, CBT and physical activity) taken alone or in combination with pharmaceuticals for the treatment of depression. Avoid overconsumption of alcohol.
• Sertralin is recommended in the Wise List.
• Avoid randomized prescribing of SSRIs (for example, sertraline). Evaluate and reconsider the treatment with SSRIs. Can the pharmaceutical be de-prescribed?
• Starter pack is available within the reimbursement system.

Comparative assessment of environmental risk in the use of citalopram, escitalopram, sertraline, fluoxetine, venlafaxine, paroxetine and clomipramine in Sweden (Report Goodpoint 2018)
Overall, there is a risk profile for the studied antidepressants.

REFERENCES

  1. Fass.se för vårdpersonal
  2. Goodpoint. Prioritering av läkemedel med miljörisk inom SLL. Stockholm: Goodpoint; 2016. Rapport LS 2016–0634.
  3. Johnson DJ, Sanderson H, Brain RA, Wilson CJ, Solomon KR. Toxicity and hazard of selective serotonin reuptake inhibitor antidepressants fluoxetine, fluvoxamine, and sertraline to algae. Ecotoxicology and Environmental Safety. 2007;67:128–139.
  4. IVL Swedish Environmental Research Institute Ltd. Fick J, Lindberg RH, Kaj L, Brorström-Lundén E. Results from the Swedish National Screening Programme 2010. Subreport 3. Pharmaceuticals.
  5. IVL Swedish Environmental Research Institute Ltd Fick J, Lindberg RH, Fång J, Magnér J, Kaj L, Brorström-Lundén E. Screening 2014. Analysis of pharmaceuticals and hormones in samples from WWTPs and receiving waters. Rapport C 135.
  6. Fick J, Lindberg RH, Tysklind M, Larsson DG. Predicted critical environmental concentrations for 500 pharmaceuticals. Regul Toxicol Pharmacol. 2010;58:516-23.
  7. SLL. Sammanställning av läkemedelsprovtagningar - Bearbetning av regional försäljningsstatistik av läkemedel samt datamaterial från Stockholms läns landstings mätprogram för läkemedelssubstanser i vattenmiljö, 2012–2016.
  8. Stockholms läns landsting. Förteckning över miljöbelastande läkemedel med åtgärdsförslag framtagen inom ramen för SLL:s miljöprogram 2017–2021.
  9. Goodpoint. Jämförande bedömning av miljörisk vid användning av citalopram, escitalopram, sertralin, fluoxetin, venlafaxin, paroxetin och klomipramin. Stockholm: Goodpoint; 2018.
  10. Stockholms läns landsting. Kloka Listan 2018.