Sertraline

Products

Sertraline is commercially available as film-coated tablets and as an oral concentrate (Zoloft, generic). It was first released in the United States in 1991 and became a blockbuster. It was approved in many countries in 1993.

Structure and properties

Sertraline (C17H17Cl2N, Mr = 306.2 g/mol) is present in drugs as sertraline hydrochloride, a white crystalline powder that is sparingly soluble in water. It is a naphthaleneamine derivative.

Effects

Sertraline (ATC N06AB06) has antidepressant properties. The effects are due to selective reuptake of serotonin into presynaptic neurons. This increases the concentration of serotonin in the synaptic cleft. Sertraline also has an effect on dopamine reuptake (see also under dasotraline). The maximum effects usually occur within two to four weeks. Sertraline has a long half-life between 22 to 36 hours.

Indications

  • Depression
  • Obsessive-compulsive disorder
  • Panic disorders
  • Post-traumatic stress disorder
  • Social phobia
  • PMDD (Premenstrual dysphoric disorder, e.g., USA).

Dosage

According to the professional information. The dose is adjusted individually. The drug is taken once daily in the morning or evening due to the long half-life. The intake is independent of meals. Discontinuation should be gradual to avoid withdrawal symptoms.

Contraindications

  • Hypersensitivity
  • Combination with MAO inhibitors
  • Combination with pimozide
  • Unstable epilepsy
  • Severe hepatic insufficiency

Full precautions can be found in the drug label.

Interactions

Sertraline has a high potential for interaction. It is metabolized by CYP2D6 and CYP3A4 and is a weak inhibitor of these isoenzymes. Sertraline undergoes first-pass metabolism in the liver. The major metabolite -desmethylsertraline is much less active than the parent compound.

Adverse effects

The most common possible adverse effects include sleep disturbance, headache, dizziness, nausea, diarrhea, thin stools, dry mouth, male sexual dysfunction, and fatigue. Sertraline may cause serotonin syndrome when combined with serotonergic drugs. It may prolong the QT interval and increase the risk of suicide.