Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product Concentrate, Oral: Zoloft: 20 mg/m L (60 m L [DSC]) [contains alcohol, usp, menthol]Generic: 20 mg/m L (60 m L)Tablet, Oral: Zoloft: 25 mg [scored; contains fd&c blue #1 aluminum lake, fd&c red #40 aluminum lake, fd&c yellow #10 aluminum lake, polysorbate 80]Zoloft: 50 mg [scored; contains fd&c blue #2 aluminum lake]Zoloft: 100 mg [scored; contains polysorbate 80]Generic: 25 mg, 50 mg, 100 mg Antidepressant with selective inhibitory effects on presynaptic serotonin (5-HT) reuptake and only very weak effects on norepinephrine and dopamine neuronal uptake. In vitro studies demonstrate no significant affinity for adrenergic, cholinergic, GABA, dopaminergic, histaminergic, serotonergic, or benzodiazepine receptors. Hepatic; may involve CYP2C19 and CYP2D6; extensive first pass metabolism; forms metabolite N-desmethylsertraline (APA [Gelenberg 2010]); Note: Children 6 to 17 years may metabolize sertraline slightly better than adults, as pediatric AUCs and peak concentrations were 22% lower than adults when adjusted for weight; however, lower doses are recommended for younger pediatric patients to avoid excessive drug levels) Urine (40% to 45% as metabolites); feces (40% to 45%; 12% to 14% as unchanged drug) Depression: The onset of action is within a week, however, individual response varies greatly and full response may not be seen until 8 to 12 weeks after initiation of treatment (APA [Gelenberg 2010]). Plasma: Sertraline: 4.5 to 8.4 hours Sertraline: Mean: 26 hours; N-desmethylsertraline: 62 to 104 hours Children 6 to 12 years: Mean: 26.2 hours (Alderman 1998)Children 13 to 17 years: Mean: 27.8 hours (Alderman 1998)Adults 18 to 45 years: Mean: 27.2 hours (Alderman 1998) 98% Sertraline clearance was reduced in patients with chronic mild liver impairment resulting in a 3-fold greater exposure. Plasma clearance 40% lower; steady state achieved after 2 to 3 weeks Children 6 to 17 years may metabolize sertraline slightly better than adults, as pediatric AUCs and peak concentrations were 22% lower than adults when adjusted for weight; however, lower doses are recommended for younger pediatric patients to avoid excessive drug levels) Major depressive disorder (unipolar): Treatment of unipolar major depressive disorder (MDD) in adults. Obsessive-compulsive disorder: Treatment of obsessions and compulsions in patients with obsessive-compulsive disorder (OCD). Initial: 50 mg q Day PO given continuously throughout menstrual cycle or given during luteal phase only May increase by 50 mg at the onset of each new menstrual cycle; no more than 150 mg q Day when administered continuously or 100 mg q Day when administered during luteal phase only 25 mg PO q Day initially; may increase by 25 mg every 2-3 days; not to exceed 200 mg q Day Alzheimer dementia related depression: Start at 12.5 mg/day and titrate every 1-2 weeks to response; not to exceed 150-200 mg Renal impairment: Dose adjustment not necessary Mild hepatic impairment (Child-Pugh 5-6): Decrease recommended starting dose and therapeutic dose by 50% Moderate-to-severe hepatic impairment (Child-Pugh 7-15): Not recommended; sertraline is extensively metabolized, and the effects in patients with moderate and severe hepatic impairment have not been studied Clinical worsening and suicide ideation may occur despite medication Use caution in patients with seizure disorders May worsen mania symptoms or precipitate mania in patients with bipolar disorder Increases risk of hyponatremia and impairment of cognitive/motor functions in the elderly Increases risk of bleeding in patients taking anticoagulants/antiplatelets concomitantly Risk of mydriasis; may trigger angle closure attack in patients with angle closure glaucoma with anatomically narrow angles without a patent iridectomy Pregnancy: Conflicting evidence regarding use of SSRIs during pregnancy and increased risk of persistent pulmonary hypertension of the newborn (see Pregnancy) In neonates exposed to SNRIs/SSRIs late in third trimester: Risk of complications such as feeding difficulties, irritability, and respiratory problems Avoid abrupt withdrawal Bone fractures reported with antidepressant therapy; consider the possibility if patient presents with bone pain, bruising, or point of tenderness Coadministration with other drugs that enhance the effects of serotonergic neurotransmission (eg, tryptophan, fenfluramine, fentanyl, 5-HT agonists, St. John’s Wort) should be undertaken with caution and avoided whenever possible due to the potential for pharmacodynamic interaction (see Contraindications) May cause false-positive urine immunoassay screening tests for benzodiazepines SSRIs and SNRIs are associated with development of SIADH; hyponatremia reported Several SSRIs (eg, fluoxetine, fluvoxamine, paroxetine, sertraline) are metabolized by CYP2D6 CYP2D6 is involved in the metabolism of approximately 20% of drugs in clinical use and displays large individual-to-individual variability in activity due to genetic polymorphisms More than 80 CYP2D6 variant alleles have been identified; however, 4 of the most prevalent alleles, CYP2D6*3, *4, *5, and *6, account for 93-97% of CYP2D6 poor metabolizers CYP2D6*4, the most common variant (~25% frequency in whites), causes a splicing defect; CYP2D6*3 (2.7% frequency) causes a frameshift mutation; and CYP3D6*5 (2.6%) is an entire deletion of the CYP2D6 gene; individuals homozygous for these alleles have no CYP2D6 activity The impact of CYP2D6 activity is further complicated in some SSRIs (eg, fluoxetine, fluvoxamine, paroxetine, sertraline) because in addition to being substrates for CYP2D6, they are also known to moderately inhibit CYP2D6 activity The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information. Zoloft and alcohol Propecia shampoo Sertraline is a widely used serotonin reuptake inhibitor that has been shown to. onset of action, a significant reduction in depression scores was apparent at 2. Early Onset of Selective Serotonin Reuptake Inhibitor Antidepressant Action. fluvoxamine or citalopram or escitalopram or sertraline or paroxetine and the key. The exact mechanism of action sertraline is not fully known, but the drug appears. while the time to reach peak plasma concentration Tmax decreased from 8. Sertraline is used for a number of conditions, including major depressive disorder (MDD), obsessive–compulsive disorder (OCD), body dysmorphic disorder (BDD), posttraumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD), panic disorder, and social anxiety disorder (SAD). The comparative efficacy of sertraline and TCAs for melancholic depression has not been studied. A 1998 review suggested that, due to its pharmacology, sertraline may be more efficacious than other SSRIs and equal to TCAs for the treatment of melancholic depression. A meta-analysis of 12 new-generation antidepressants showed that sertraline and escitalopram are the best in terms of efficacy and acceptability in the acute-phase treatment of adults with unipolar MDD. Sertraline used for the treatment of depression in elderly (older than 60) patients was superior to placebo and comparable to another SSRI fluoxetine, and TCAs amitriptyline, nortriptyline (Pamelor) and imipramine. Sertraline had much lower rates of adverse effects than these TCAs, with the exception of nausea, which occurred more frequently with sertraline. In addition, sertraline appeared to be more effective than fluoxetine or nortriptyline in the older-than-70 subgroup. placebo in elderly patients showed a statistically significant (that is, unlikely to occur by chance), but clinically very modest improvement in depression and no improvement in quality of life. A meta-analysis on SSRIs and SNRIs that look at partial response (defined as at least a 50% reduction in depression score from baseline) found that sertraline, paroxetine and duloxetine were better than placebo. Studies have shown that sertraline has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors. The chronic administration of sertraline was found in animals to down regulate brain norepinephrine receptors. The effect of sertraline on the QTc interval was evaluated in a randomized, double-blind, placebo- and positive-controlled three-period crossover thorough QTc study in 54 healthy adult subjects. At 2-fold the maximum recommended daily dose (~3-fold the steady-state exposure for sertraline and N-desmethylsertraline), the largest mean ΔΔQTc was 10 ms with upper bound of two-sided 90% confidence interval of 12 ms. The length of the QTc interval was also positively correlated with serum concentrations of sertraline and N- desmethylsertraline concentrations. These concentration-based analyses, however, indicated a lesser effect on QTc at maximally observed concentration than in the primary analysis ) of sertraline occurred between 4.5 to 8.4 hours post-dosing. The average terminal elimination half-life of plasma sertraline is about 26 hours. Consistent with the terminal elimination half-life, there is an approximately two-fold accumulation up to steady-state concentrations, which are achieved after one week of once-daily dosing. Sertraline onset of action Sertraline 50mg tablets - Summary of Product Characteristics. - eMC, Early Onset of Selective Serotonin Reuptake Inhibitor Antidepressant. Cytotec for miscarriage protocol Mechanism of Action. The effect of sertraline on the QTc interval was evaluated in a randomized, double-blind. mg for 14 days, mean peak plasma concentrations Cmax of sertraline occurred between 4.5 to 8.4 hours post-dosing. ZOLOFT® sertraline HCl Clinical Pharmacology Pfizer Medical.. Sertraline DB01104 - Sertraline - DrugBank. Zoloft Sertraline Hcl Side Effects, Interactions, Warning, Dosage.. Antidepressant action Sertraline probably acts by blocking the reuptake of. Cimetidine Increases sertraline bioavailability, peak plasma levels, and half-life. Mechanism of Action Sertraline has dopamine reuptake inhibition DRI and sigma 1 receptor binding in addition to serotonin reuptake inhibition. The DRI. The mechanism of action of sertraline is presumed to be linked to its inhibition of. 200 mg for 14 days, mean peak plasma concentrations Cmax of sertraline.