Drug information of Sertraline

Sertraline


Sertraline is an antidepressant in a group of drugs called selective serotonin reuptake inhibitors (SSRIs).
Sertraline affects chemicals in the brain that may become unbalanced and cause depression, panic, anxiety, or obsessive-compulsive symptoms. Sertraline is used to treat depression, obsessive-compulsive disorder, panic disorder, anxiety disorders, post-traumatic stress disorder (PTSD), and premenstrual dysphoric disorder (PMDD).

Mechanism of effect

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.

Pharmacodynamic

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 blocking activity.

Pharmacokinetics

The effects of food on the bioavailability of the sertraline tablet and oral concentrate were studied in subjects administered a single dose with and without food. For the tablet, AUC was slightly increased when drug was administered with food but the Cmax was 25% greater, while the time to reach peak plasma concentration (Tmax) decreased from 8 hours post-dosing to 5.5 hours.
For the oral concentrate, Tmax was slightly prolonged from 5.9 hours to 7.0 hours with food. 98% bound to serum proteins, principally to albumin and α1-acid glycoprotein.
Extensively metabolized in the liver. Sertraline undergoes extensive first pass metabolism. Sertraline has a plasma terminal elimination half-life of 62 to 104 hours.
Sertraline is extensively metabolized and excretion of unchanged drug in urine is a minor route of elimination.

Dosage

Usual Adult Dose for Depression Initial dose: 50 mg orally once a day. Increase dose by 50 mg increments no more often than weekly.
Maintenance Dose: Can increase once a week, to a maximum of 200 mg once a day.
Usual Adult Dose for Panic Disorder Initial dose: 25 mg orally once a day, after one week, the dose may be increased to 50 mg once a day. Increase dose by 50 mg increments no more often than weekly.
Maintenance dose: Can increase once a week, to a maximum of 200 mg once a day.

Alerts

1-Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior
2- Sertraline is not approved for use in treating bipolar depression.
3-The development of a potentially life-threatening serotonin syndrome has been reported with SNRIs and SSRIs, including Sertraline hydrochloride
4-The pupillary dilation that occurs following use of many antidepressant drugs including Sertraline hydrochloride may trigger an angle closure attack in a patient with anatomically narrow angles who does not have a patent iridectomy.
5-Significant weight loss may be an undesirable result of treatment with Sertraline for some patients.
6-Sertraline hydrochloride has not been evaluated in patients with a seizure disorder.

Points of recommendation

1-Instruct patients that discontinuation of duloxetine may be associated with symptoms such as dizziness, headache, nausea, diarrhea, paresthesia, irritability, vomiting, insomnia, anxiety, hyperhidrosis, and fatigue, and should be advised not to alter their dosing regimen, or stop taking duloxetine without consulting their physician.
2-SSRIs and SNRIs, including Sertraline hydrochloride, may increase the risk of bleeding events ranging from ecchymoses, hematomas, epistaxis, petechiae, and gastrointestinal hemorrhage to life-threatening hemorrhage. Concomitant use of aspirin, nonsteroidal anti-inflammatory drugs, warfarin, and other anticoagulants or other drugs known to affect platelet function may add to this risk.
3-Hyponatremia may occur as a result of treatment with SSRIs and SNRIs, including Sertraline hydrochloride tablets. In many cases, this hyponatremia appears to be the result of the syndrome of inappropriate antidiuretic hormone secretion (SIADH)

Pregnancy level

C


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