Sertraline is an antidepressant in a group of drugs called selective serotonin reuptake inhibitors (SSRIs). Sertraline affects chemicals in the brain that may be unbalanced in people with depression, panic, anxiety, or obsessive-compulsive symptoms.
Sertraline is used to treat depression, obsessive-compulsive disorder, anxiety disorders (including panic disorder and social anxiety disorder), post-traumatic stress disorder (PTSD), and premenstrual dysphoric disorder (PMDD).
For the management of major depressive disorder (MDD), posttraumatic stress disorder (PTSD), obsessive-compulsive disorder (OCD), panic disorder (PD) with or without agoraphobia, premenstrual dysphoric disorder (PMDD), and social anxiety disorder (SAD)
It may be used for premature ejaculation and vascular headaches as off-label indications.
Sertraline, an antidepressant drug similar to citalopram, fluoxetine, and paroxetine, is of the selective serotonin reuptake inhibitor (SSRI) type. Sertraline has one active metabolite and, like the other SSRIs, have less sedative, anticholinergic, and cardiovascular effects than the tricyclic antidepressant drugs because it does not have clinically important anticholinergic, antihistamine, or adrenergic (alpha1, alpha2, beta) blocking activity.
In vitro, sertraline has no significant affinity for GABA, dopaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors. It mediates a weak inhibitory actions on the neuronal uptake of norepinephrine or dopamine and exhibits no inhibitory action on monoamine oxidase.
The pharmacological role of sigma receptors in the mechanism of action of sertraline is unclear.
The exact mechanism of action sertraline is not fully known, but the drug appears to selectively inhibit the reuptake of serotonin at the presynaptic membrane. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission.
It is suggested that these modifications are responsible for the antidepressant action observed during long term administration of antidepressants. It has also been hypothesized that obsessive-compulsive disorder is caused by the dysregulation of serotonin, as it is treated by sertraline, and the drug corrects this imbalance.
Metabolism: Extensively metabolized in the liver. Sertraline metabolism involves N-demethylation, N-hydroxylation, oxidative deamination, and glucuronidation of sertraline carbamic acid. Sertraline undergoes N-demethylation to form N-desmethylsertraline, which retains substantially less pharmacological activity than its parent compound.
Absorption: Following once-daily administration over the range of 50 to 200 mg for 14 days, mean peak plasma concentrations (Cmax) of sertraline occurred between 4.5 to 8.4 hours post-administration. The steady-state concentrations are reached after 1 week following once-daily administration, and approximately two-fold accumulation up to steady-state concentrations is observed. The single dose bioavailability of sertraline tablets is approximately equal to an equivalent dose of sertraline oral solution.
Route of elimination: Sertraline and its metabolites are excreted via both renal and fecal elimination.
Half life: The elimination half-life of sertraline is approximately 25-26 hours. The elimination half-life of desmethylsertraline is approximately 62-104 hours.
All medicines may cause side effects, but many people have no, or minor, side effects.Some medical conditions may interact with Sertraline.
Tell your doctor or pharmacist if you have any medical conditions.
The most common signs and symptoms associated with non-fatal sertraline overdosage were somnolence, vomiting, tachycardia, nausea, dizziness, agitation and tremor. No cases of fatal overdosage with only sertraline have been reported. Other important signs of overdose include bradycardia, bundle branch block, coma, convulsions, delirium, hallucinations, hypertension, hypotension, manic reaction, pancreatitis, QT-interval prolongation, Torsade de Pointes, serotonin syndrome, stupor, and syncope.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider.
