SERTRALINE HCL
  • SERTRALINE HCL

  • (Generic for ZOLOFT)
  • QTY 30 • 100 MG • Tablet • Near 77381

SERTRALINE (SER tra leen) is used to treat depression. It may also be used to treat obsessive compulsive disorder, panic disorder, post-trauma stress, premenstrual dysphoric disorder (PMDD) or social anxiety.

SERTRALINE HCL Pediatric Monographs
  • General Administration Information
    For storage information, see the specific product information within the How Supplied section.

    Route-Specific Administration

    Oral Administration
    -May take without regard to meals in the morning or evening.
    Oral Liquid Formulations
    Oral solution:
    -Must be diluted before use.
    -Use the supplied calibrated dropper to measure the correct dose. The supplied calibrated dropper has 25 mg and 50 mg graduation marks only.
    -Mix the measured dose with 4 ounces (120 mL) of water, ginger ale, lemon-lime soda, lemonade, or orange juice ONLY.
    -After mixing, a slight haze may appear; this is normal.
    -Have the patient consume the dose immediately after mixing; do not prepare in advance.
    -The dropper contains dry natural rubber; use with caution in patients with latex sensitivity.

    The overall adverse reaction profile of sertraline during pediatric clinical trials (n = 281) was generally similar to that seen in adult studies.

    Gastrointestinal (GI) effects are among the most common adverse reactions to sertraline and are often associated with drug discontinuation. Nausea (26%), diarrhea/loose stools (20%), xerostomia (14%), dyspepsia (8%), constipation (6%), anorexia (7%), vomiting (4%), abdominal pain (5% or more), hematochezia (less than 2%), appetite stimulation (less than 2%), melena (less than 2%), and rectal hemorrhage (less than 2%) were reported in adult patients during premarketing evaluation. Anorexia was reported in at least 2% of pediatric patients and at a rate at least twice that of placebo during clinical trials. As with other SSRIs, decreased weight gain has been observed in children and adolescents receiving sertraline. Data are inadequate to determine whether the chronic use of SSRIs causes long-term growth inhibition, but height and weight should be monitored periodically throughout therapy. In a pooled analysis of two 10-week pediatric trials (n = 373), sertraline-treated patients lost approximately 1 kg, while those treated with placebo gained roughly 1 kg. Approximately 7% of children (ages 6 to 11 years) and 2% of adolescents (ages 12 to 17 years) had a weight loss more than 7% of body weight compared to 0% and 1%, respectively, of placebo-treated patients. For those who continued sertraline therapy in the 24-week open label extension study (n = 68), weight gain was similar to the expected using data from age-adjusted peers. The mechanism of growth inhibition in children may be due to the suppression of growth hormone secretion, which is known to occur in adults taking SSRIs.

    Nervous system effects are among the most common adverse reactions to sertraline and are often associated with drug discontinuation. Dizziness (12%), drowsiness/somnolence (11%), tremor (9%), insomnia (20%), and headache (more than 2%) were reported in adults during premarketing evaluation of sertraline. Ataxia, coma, convulsions, decreased alertness, hypoesthesia, lethargy, and psychomotor activity were reported in less than 2% of patients. The overall adverse reaction profile in pediatric clinical trials was generally similar to that seen in adult studies; however, hyperkinesis was reported in at least 2% of pediatric patients and at a rate at least twice that of the placebo group. Extrapyramidal symptoms including akathisia, dystonic reaction, and oculogyric crisis have been reported with postmarketing use; however, frequency and causality have not been established.

    Aggression and anxiety were reported in at least 2% of pediatric patients and at a rate at least twice that of placebo-treated patients during clinical trials. Agitation (8%) and nervousness were both reported in adult patients and have been associated with drug discontinuation. Teeth grinding (bruxism), confusion, euphoria, and hallucinations were reported in less than 2% of patients during premarketing evaluation. Psychosis, enuresis, and paroniria (abnormal dreams, nightmares) have been reported with postmarketing use; however, frequency and causality have not been established.

    Monitor all antidepressant-treated patients for any indication for worsening of depression or the condition being treated and the emergence of suicidal behaviors or suicidal ideation, especially during the initial few months of drug therapy and after dosage changes. In a pooled analysis of placebo-controlled trials of antidepressants (n = 4,500 pediatrics and 77,000 adults), there was an increased risk for suicidal thoughts and behaviors in patients 24 years of age and younger receiving an antidepressant versus placebo, with considerable variation in the risk of suicidality among drugs. The difference in the absolute risk of suicidal thoughts and behaviors across different indications was highest in those with major depression. No suicides occurred in any of the pediatric trials. Caregivers and/or patients should immediately notify the prescriber of changes in behavior or suicidal ideation. Antidepressants can precipitate mania in susceptible individuals. During initial clinical trials with sertraline, hypomania or mania occurred in about 0.4% of patients. Manic symptoms and suicidal ideation appear to be more prevalent in pediatric patients with or at high risk for bipolar disorder on antidepressants; monitor such patients closely. In a study of 52 pediatric and young adult patients (mean age: 15 years, range: 7 to 22 years) with bipolar disorder or subthreshold manic symptoms and exposure to antidepressants, 50% developed antidepressant-induced mania and 25.5% had new-onset suicidal ideation.

    Seizures were reported in less than 2% of patients during premarketing evaluation of sertraline. During a study of sertraline for obsessive-compulsive disorder, seizures occurred in roughly 0.2% (4/1,800) of patients; 3 of these patients were adolescents with a personal or family history of seizure disorder, none of whom were receiving anticonvulsant therapy. No seizures were reported among 3,000 patients during premarketing evaluation for major depressive disorder. Sertraline should be introduced cautiously in patients with a seizure disorder and promptly discontinued if seizures develop. Cerebrovascular spasm, including reversible cerebral vasoconstriction syndrome and Call-Fleming syndrome, have been reported during postmarketing use of sertraline; however, causality has not been established.

    Selective serotonin reuptake inhibitors (SSRIs), such as sertraline, may cause hyponatremia, which is frequently the result of the syndrome of inappropriate antidiuretic hormone secretion (SIADH). In some cases, serum sodium levels less than 110 mmol/L have been reported; however, the adverse effect appeared reversible upon discontinuation of the causative SSRI. Patients receiving diuretics or prone to dehydration, and those who are otherwise volume depleted (e.g., hypovolemia) appear to be at greatest risk. Hyponatremia may manifest as headache, difficulty concentrating, memory impairment, confusion, weakness, and unsteadiness which may result in falls. Severe manifestations include hallucinations, fainting, seizure, coma, respiratory arrest, and death. Symptomatic hyponatremia may require discontinuation of the SSRI, as well as implementation of the appropriate medical interventions.

    Combined clinical trial data indicate that palpitations were the most frequently reported cardiovascular effect in adult patients receiving sertraline compared to placebo (4% vs. 2%). Sinus tachycardia, vascular hemorrhage, hypertension, peripheral vasodilation, syncope, and hypercholesterolemia occurred in less than 2% of patients receiving sertraline during premarketing evaluation. During postmarketing use of the drug, the following cardiovascular or related effects have been reported, although the frequencies are unknown and causality to the drug has not been established: bradycardia, AV block, atrial arrhythmias, QT prolongation, ventricular tachycardia (including torsade de pointes), and vasculitis.

    Platelet dysfunction (i.e., impaired platelet aggregation) may occur during treatment with selective serotonin reuptake inhibitors (SSRIs) due to platelet serotonin depletion, possibly increasing the risk of a bleeding complication (e.g., GI bleeding, ecchymosis, epistaxis, hematoma, petechiae, hemorrhage). An increased risk of bleeding complications is possible in patients receiving antiplatelet or anticoagulant medications concurrently with sertraline. Epistaxis and purpura were reported in less than 2% of patients receiving sertraline during premarketing evaluation. Hematologic and lymphatic effects reported during postmarketing use include increased coagulation times (altered platelet function), agranulocytosis, aplastic anemia, pancytopenia, leukopenia, thrombocytopenia, lupus-like symptoms, and serum sickness.

    Combined clinical trial data indicate that hyperhidrosis (increased sweating) occurred in at least 5% of adult patients receiving sertraline and with an incidence twice that in placebo-treated patients (7% vs. 3%). Adverse dermatologic or hypersensitivity reactions observed during premarketing evaluation of sertraline and occurring in less than 2% of patients included alopecia, cold sweat, dermatitis (unspecified), bullous rash, pruritus, urticaria, anaphylaxis (anaphylactoid reactions), and erythematous, follicular, or maculopapular rash. During postmarketing use of the drug, the following effects have been reported, although the frequencies are unknown and causality to the drug has not been established: photosensitivity and other severe cutaneous disorders, and potentially fatal reactions including angioedema, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN). Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) has been reported during postmarketing use of sertraline according to the Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS). Manifestations of DRESS typically include pyrexia, rash, facial swelling, and/or lymph node involvement in conjunction with other organ system abnormalities including hepatitis, nephritis, hematologic abnormalities, myocarditis, or myositis. Eosinophilia is often present. Early manifestations of DRESS such as pyrexia and lymph node involvement may be present without evidence of a rash. Sertraline should be promptly discontinued and appropriate medical treatment should be initiated in patients presenting with a rash or symptoms indicative of DRESS in whom an unrelated etiology cannot be identified.

    Combined clinical trial data indicate that the most frequently reported ophthalmic effect in adult patients receiving sertraline compared to placebo was visual impairment (4%). Ophthalmic effects occurring in less than 2% of patients receiving sertraline during premarketing evaluation included mydriasis and blurred vision. Rare effects (less than 0.1%) include ocular hypertension (glaucoma or increased intraocular pressure). During postmarketing use, blindness, optic neuritis, and cataracts have been reported; however, the frequencies are unknown and causality to the drug has not been established. Otic effects occurring in less than 2% of patients receiving sertraline during premarketing evaluation included tinnitus.

    Elevated hepatic enzymes were reported in less than 2% of patients during premarketing evaluation of sertraline. Pancreatitis and severe liver events including hepatitis, jaundice (hyperbilirubinemia), and hepatic failure with some fatal outcomes have been reported during postmarketing use; however, the frequencies are unknown and causality to the drug has not been established.

    Musculoskeletal and connective tissue effects reported during premarketing evaluation of sertraline and occurring in less than 2% of adult patients included arthralgia and muscle spasms (muscle cramps), tightness, or twitching. Arthralgia and muscle spasms/twitching were reported in at least 2% of pediatric patients receiving sertraline at a rate of at least twice the placebo rate. Trismus and rhabdomyolysis have been reported with postmarketing use.

    Adverse respiratory and related effects reported during premarketing evaluation of sertraline and occurring in less than 2% of patients included bronchospasm and yawning. Pulmonary hypertension has been reported during postmarketing use; however, the frequency is unknown and causality to the drug has not been established.

    Combined clinical trial data indicate that fatigue (12%) was reported more frequently in adult patients receiving sertraline than placebo. Fatigue led to discontinuation in more than 2% of patients receiving sertraline and at twice the rate of placebo-treated patients. Fever has been reported in at least 2% of pediatric patients during clinical trials of sertraline. General disorders that were reported in less than 2% of adult patients receiving sertraline during premarketing evaluation included edema, gait disturbance, and fever. Malaise was reported in some adult clinical trials.

    Vaginal bleeding was reported in less than 2% of adult females during premarketing evaluation of sertraline. Dysmenorrhea has been reported with postmarketing use; however, frequency is unknown and causality has not been established.

    Priapism has been reported rarely with all of the SSRIs and was reported in < 2% of adult males in premarketing evaluation of sertraline. Because priapism is considered a medical emergency, discontinue sertraline if priapism develops and promptly initiate appropriate medical treatment.

    Adverse urinary system effects that were reported in less than 2% of patients receiving sertraline during premarketing evaluation included hematuria. Urinary incontinence was reported in at least 2% of pediatric patients and at a rate at least twice the placebo rate during clinical trials of sertraline. Acute renal failure (unspecified) and enuresis (nocturia or other involuntary urination) have been reported during postmarketing use; however, the frequencies are unknown and causality to the drug has not been established.

    During premarketing evaluation, endocrine effects including galactorrhea, diabetes mellitus, hypoglycemia, and hypothyroidism were reported in less than 2% of patients receiving sertraline. Endocrine effects that have been reported during postmarketing use of sertraline include hyperprolactinemia, gynecomastia, menstrual irregularity, and hyperglycemia; however, the frequencies are unknown and causality to the drug has not been established.

    Serotonin syndrome has been reported during postmarketing use of sertraline, although the frequency is unknown and causality has not been established. Serotonin syndrome has been reported during use of SSRIs alone, during concurrent use of other medications known to increase central or peripheral serotonin levels, or during SSRI overdose. Serotonin syndrome is a range of signs and symptoms that can rarely, in its most severe form, resemble neuroleptic malignant syndrome. Symptoms may include mental status changes (e.g., agitation, hallucinations, delirium, coma), gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea), autonomic instability (e.g., tachycardia, labile blood pressure, dizziness, diaphoresis, flushing, hyperthermia), neuromuscular symptoms (e.g., tremor, rigidity, myoclonus, hyperreflexia, incoordination), and/or seizures. Monitor all patients taking sertraline for the emergence of serotonin syndrome. If symptoms emerge, discontinue sertraline and any other serotonergic agent and initiate appropriate medical treatment.

    Selective serotonin reuptake inhibitors (SSRIs) should be used with caution in patients with osteopenia or risk factors for osteopenia. Epidemiological studies suggest an association between the use of SSRIs and bone fractures. Some data suggest that chronic treatment with SSRIs, such as sertraline, may be associated with reduced bone density.

    Discontinuation syndrome and drug withdrawal may occur after discontinuation of serotonergic antidepressants, such as sertraline, especially with abrupt discontinuation. Symptoms may include nausea, sweating, dysphoric mood, irritability, agitation, dizziness, sensory disturbances (paresthesia, electric shock sensation), tremor, anxiety, confusion, headache, lethargy, emotional lability, insomnia, and hypomania. Withdrawal symptoms usually begin 1 to 3 days after abrupt discontinuation of the SSRI and remit within 1 to 2 weeks. Gradual tapering is recommended during discontinuation of any SSRI to decrease or prevent the occurrence of withdrawal-like symptoms.

    A neonatal abstinence syndrome has been reported in infants exposed to serotonergic agents such as sertraline in utero, with features consistent with either a direct toxic effect of serotonergic agents (e.g., serotonin syndrome), or possibly a drug discontinuation syndrome. After birth, symptoms consistent with withdrawal (i.e., poor feeding, hypoglycemia, hypothermia, lethargy or irritability, vomiting) have been noted. Such complications can arise immediately upon delivery. Other symptoms have included respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, hypotonia, hypertonia, hyperreflexia, tremor, jitteriness, and constant crying. Serum concentrations of the serotonergic agent were measurable in the infants affected. Several other symptoms (bloody stools, necrotizing enterocolitis) may have been attributable to rebound platelet activation on withdrawal of the exposure to the SSRI. Neonatal symptoms generally improved over several days. A cohort study of 55 women revealed that 22% (12/55) of neonates exposed to an SSRI in the third trimester had complications requiring treatment or extended hospitalization compared with 6% in comparison groups. Complications included respiratory distress (n = 9), hypoglycemia (n = 2), and jaundice (n = 1). The incidence of prematurity in the third trimester SSRI group was significant at 20% vs. 3.7% of controls. Other potential adverse events have also been reported, including a potential association between maternal use of SSRIs in the third trimester and the development of persistent pulmonary hypertension of the newborn (PPHN). Some retrospective studies have not shown an increased risk of PPHN with SSRI exposure. The FDA has stated that an increased risk of PPHN from SSRI exposure cannot be determined due to conflicting data.

    Sertraline is contraindicated in patients with a hypersensitivity to sertraline or any of the formulation components.

    Avoid abrupt discontinuation of any SSRI if possible. Gradual reduction is recommended whenever possible to limit the occurrence of a discontinuation syndrome. The most frequent SSRI discontinuation reactions include dizziness, vertigo, nausea, vomiting, flu-like symptoms, sensory disturbances (e.g., paresthesias, electric shock sensation), sleep disturbances, irritability, anxiety, and/or agitation. Sweating, dysphoric mood, emotional lability, confusion, headache, tremor, lethargy, hypomania, tinnitus, and seizures may also occur. Discontinuation symptoms are more likely to occur after withdrawal of SSRIs with a short half-life (e.g., paroxetine, fluvoxamine).

    The risks or benefits of using sertraline during electroconvulsive therapy (ECT) have not been established in clinical studies. Some clinicians have reported that in rare instances the ECT-induced seizure was prolonged in the presence of an antidepressant.

    The safety and efficacy of sertraline have been established in the treatment of obsessive-compulsive disorder (OCD) in children and adolescents 6 to 17 years of age. Results from 2 placebo-controlled trials in pediatric patients less than 18 years of age were insufficient to support an indication for sertraline in treating pediatric major depressive disorder. In a pooled analysis of placebo-controlled trials of antidepressants (n = 4,500 pediatrics and 77,000 adults), there was an increased risk for suicidal thoughts and behaviors in patients 24 years of age and younger receiving an antidepressant versus placebo, with considerable variation in the risk of suicidality among drugs. The difference in absolute risk of suicidal thoughts and behaviors across different indications was highest in those with major depression. No suicides occurred in any of the pediatric trials. Data from a cohort of 36,842 children (age range of 6 to 18 years) suggested those who use multiple antidepressants have a higher risk of suicide behavior, most likely a result of increased severity of depression rather than drug effect. The need for an antidepressant in children or adolescents for any use must be weighed against the risk of suicidality; it is unknown if this risk extends to long-term use. All patients should be monitored for symptom worsening or suicidality, especially at treatment initiation or after dose changes. Caregivers and/or patients should immediately notify the prescriber of changes in behavior or suicidal ideation. A change to the treatment regimen or discontinuation of sertraline may be necessary in patients with emerging suicidality or worsening depression.

    Mania or hypomania can be precipitated in predisposed individuals during treatment with an antidepressant, including sertraline. Children with a family history of bipolar disorder, those who have a diagnosis of bipolar disorder, and those with subthreshold manic symptoms may be at increased risk for developing mania during treatment. In addition, patients with pre-existing bipolar disorder type I, compared to those with subsyndromal or type II bipolar disorder, and those with psychiatric comorbidities may be at increased risk for antidepressant-induced mania. Younger patients may be more likely to experience antidepressant-induced mania. Suicidal ideation appears to be more prevalent in children with or at high risk for bipolar disorder on antidepressants. In a study of 52 patients (mean age of 15 years, ranging from 7 to 22 years) with bipolar disorder or subthreshold manic symptoms, 25.5% had new-onset suicidal ideation within the first 3 months of antidepressant use. Progressive evaluation of youth at risk for bipolar disorder who were exposed to antidepressants (n = 21; age range of 9 to 20 years) suggested psychiatric adverse events such as irritability, aggression, impulsivity, and hyperactivity were more common in younger patients. A major depressive episode may be the initial presentation of bipolar disorder. Patients with depressive symptoms should be adequately screened to determine if they are at risk for bipolar disorder prior to initiating treatment. Such screening should include a detailed psychiatric history, including a family history of suicide, bipolar disorder, and depression. The response of patients with a previously established history of bipolar disorder should be closely monitored if therapy with an antidepressant is indicated.

    Sertraline should be used with caution in patients with a history of seizure disorder. Patients with a history of seizures were excluded from clinical studies with sertraline. Seizures have been reported rarely in patients taking SSRIs.

    Cases of QT prolongation and torsade de pointes (TdP) have been reported during the postmarketing use of sertraline; the reports primarily occurred in patients with associated risk factors for these events. Use sertraline with caution in patients with conditions that may increase the risk of QT prolongation including congenital long QT syndrome, cardiac arrhythmias, bradycardia, AV block, heart failure, stress-related cardiomyopathy, myocardial infarction, stroke, hypomagnesemia, hypokalemia, hypocalcemia, or in patients receiving medications known to prolong the QT interval or cause electrolyte imbalances. Females, patients with sleep deprivation, pheochromocytoma, sickle cell disease, hypothyroidism, hyperparathyroidism, hypothermia, systemic inflammation (e.g., human immunodeficiency virus (HIV) infection, fever, and some autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus (SLE), and celiac disease and patients undergoing apheresis procedures (e.g., plasmapheresis [plasma exchange], cytapheresis) may also be at increased risk for QT prolongation.

    Dosage adjustments of sertraline are recommended in patients with hepatic disease. In studies of patients with chronic mild hepatic disease, sertraline clearance was reduced. For patients with mild hepatic impairment (Child Pugh scores 5 or 6), the recommended initial dose and therapeutic range dosing is 50% of the normal daily dosage. The use of sertraline in patients with moderate (Child Pugh scores 7 to 9) or severe hepatic impairment (Child Pugh scores 10 to 15) is not recommended.

    Selective serotonin reuptake inhibitors (SSRIs) may cause hyponatremia, which is frequently the result of the syndrome of inappropriate antidiuretic hormone secretion (SIADH). In some cases, serum sodium levels less than 110 mmol/L have been reported; however, the adverse effect appeared reversible upon discontinuation of the causative SSRI. Patients receiving diuretics or prone to dehydration, and those who are otherwise volume depleted (e.g., hypovolemia) appear to be at greatest risk. Hyponatremia may manifest as headache, difficulty concentrating, memory impairment, confusion, weakness, and unsteadiness which may result in falls. Severe manifestations include hallucinations, syncope, seizure, coma, respiratory arrest, and death. Symptomatic hyponatremia may require discontinuation of sertraline, as well as implementation of the appropriate medical interventions.

    Decreased appetite and weight loss have been observed during administration of SSRIs. Therefore, caution is advisable when administering sertraline to patients with anorexia nervosa or other conditions where weight loss is undesirable.Monitoring of weight and growth in pediatric patients is desirable during treatment.

    Because sertraline may impair judgment, thinking, or motor skills, patients should use caution when engaging in activities requiring coordination and concentration (such as riding bicycles, driving, or operating machinery) until they are aware of the effects of sertraline on their cognition.

    Monitor patients taking an SSRI for signs and symptoms of bleeding. Platelet aggregation may be impaired by SSRIs due to platelet serotonin depletion, possibly increasing the risk of a bleeding complication (e.g., gastrointestinal bleeding, ecchymoses, epistaxis, hematomas, petechiae, hemorrhage). Concurrent use of aspirin, NSAIDs, anticoagulant therapy, thrombolytic therapy, or other medications that enhance bleeding potential may increase this risk. Patients taking sertraline should be instructed to promptly report any bleeding events to the practitioner.

    Caution is recommended when prescribing sertraline to patients with closed-angle glaucoma. The pupillary dilation that can occur with antidepressants may precipitate a closed-angle glaucoma attack in patients with anatomically narrow angles who do not have a patent iridectomy. An acute attack of closed-angle glaucoma is considered a medical emergency because the increased intraocular pressure is rapid and severe, and may quickly result in blindness if left untreated.

    Concomitant use of MAOI therapy with sertraline or within 14 days of stopping treatment with sertraline is contraindicated because of an increased risk of serotonin syndrome. The use of sertraline within 14 days of stopping MAOI therapy is also contraindicated. Starting sertraline in a patient who is being treated with linezolid or intravenous methylene blue, both of which inhibit monoamine oxidase, is also contraindicated because of an increased risk of serotonin syndrome. Starting sertraline in a patient being treated with an MAOI such as linezolid or methylene blue is also contraindicated; however, there may be circumstances when it is necessary to initiate treatment with a MAOI such as linezolid or methylene blue in a patient taking sertraline. If acceptable alternatives are not available and benefits are judged to outweigh the risks of serotonin syndrome, sertraline should be promptly discontinued before initiating treatment with the MAOI. Monitor the patient closely for symptoms of serotonin syndrome for 2 weeks or until 24 hours after the last dose of MAOI, whichever comes first. The development of a potentially life-threatening serotonin syndrome has been reported with the use of SSRIs such as sertraline alone, but particularly with concomitant use of other serotonergic drugs. If concomitant use of sertraline with certain other serotonergic drugs (i.e., triptans, tricyclic antidepressants, fentanyl, lithium, tramadol, buspirone, tryptophan, amphetamines, and St. John's Wort) is clinically warranted, be aware of a potential increased risk for serotonin syndrome, particularly during treatment initiation and dose increases. Treatment with sertraline and any concomitant serotonergic agents should be discontinued immediately if the above events occur and supportive symptomatic treatment should be initiated. Sertraline oral concentrate is contraindicated in patients receiving disulfiram due to the alcohol content of the sertraline concentrate.

    Neonates with in utero exposure to SSRIs late in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding upon delivery. Symptoms have included respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycemia, hypotonia, hypertonia, hyperreflexia, tremor, jitteriness, irritability, and constant crying. These features are consistent with either a direct toxic effect of SSRIs, a drug discontinuation syndrome, or serotonin syndrome. In addition, although available data are conflicting, some epidemiologic reports suggest an association between maternal use of SSRIs in late pregnancy and persistent pulmonary hypertension of the newborn (PPHN). Because PPHN is associated with significant morbidity and mortality, it is important that practitioners are aware of antidepressant exposure to avoid delays in diagnosis and treatment. In a meta-analysis of 7 studies, there was a small but significant association between SSRI exposure in late pregnancy and PPHN; effects were not significant for other variables examined (e.g., study design, congenital malformations, meconium aspiration). Effects of caesarian delivery, maternal body mass index, and preterm delivery were not assessed. PPHN occurs in approximately 1.9 of 1000 live births in the general population and is a relatively uncommon event; based on this analysis it is estimated that an average of 1 associated case of PPHN would result from 286 to 351 women being treated with an SSRI during late gestation. Increasing evidence suggests an association between antidepressant use during pregnancy and a subsequent diagnosis of autism spectrum disorder (ASD) in the offspring. In two separate population-based case-control studies, an approximate 2-fold increased risk of ASD was observed.

    The potential for growth inhibition in pediatric patients should be monitored during SSRI therapy. Monitor height and weight periodically while the patient is receiving sertraline. Data are inadequate to determine whether the chronic use of SSRIs causes long-term growth inhibition; however, decreased weight gain has been observed in children and adolescents receiving SSRIs. The mechanism of growth inhibition in children may be due to the suppression of growth hormone secretion, which is known to occur in adults taking SSRIs.

    Some reports suggest that a laboratory test interference of a false positive urine drug screen may occur for benzodiazepines in patients who have received sertraline. False-positive results may occur for several days following discontinuation of sertraline. Caution should be exercised when interpreting positive urine drug screens for these medications, and confirmation by alternative tests such as gas chromatography/mass spectrometry should be considered.

    Description: Sertraline is a selective serotonin reuptake inhibitor (SSRI) commonly indicated to treat obsessive-compulsive disorder (OCD) in pediatric patients 6 years and older. Several clinical guidelines, including the American Academy of Child and Adolescent Psychiatry (AACAP) practice parameter, describe a role for SSRIs in treating childhood depression. Because the available evidence provides the greatest support for the efficacy of fluoxetine, these guidelines recommend sertraline as an alternative to fluoxetine in patients with intolerance, potential drug interactions, lack of or poor response, and/or family resistance to fluoxetine. In addition, SSRIs are considered first-line therapy for childhood anxiety disorders requiring pharmacologic treatment, although few indications are FDA-approved, and long-term safety and efficacy data are limited. Sertraline is advantageous over some other SSRIs, such as paroxetine and fluoxetine, in that it has a lower potential for drug interactions involving CYP2D6 inhibition. Product labels for all antidepressants contain a warning related to an increased risk of suicidality in children and adolescents, particularly during initial treatment. Therefore, the necessity of pharmacologic therapy should be carefully considered in the pediatric population, taking into account the risks of pharmacologic treatment versus clinical need.

    For the treatment of obsessive-compulsive disorder (OCD):
    Oral dosage:
    Children 6 to 12 years: 25 mg PO once daily initially. Based on response and tolerability, may increase in increments of 25 to 50 mg/day at intervals of at least 1 week. The therapeutic range is 50 mg/day to 200 mg/day. Max: 200 mg/day. Maintenance treatment is generally needed. Periodically reassess the need for continued treatment.
    Adolescents: 50 mg PO once daily initially. Based on response and tolerability, may increase in increments of 25 to 50 mg/day at intervals of at least 1 week. The therapeutic range is 50 mg/day to 200 mg/day. Max: 200 mg/day. Maintenance treatment is generally needed. Periodically reassess the need for continued treatment.

    For the treatment of major depression*:
    Oral dosage:
    Children 6 to 11 years: 12.5 mg to 25 mg/day PO initially. Clinical guidelines recommend to start with a low dose and titrate gradually at 4-week intervals until clinical response is achieved ; some studies report titration in 25 mg to 50 mg/day increments as often as every 1 to 2 weeks. A dose of 50 mg/day PO is considered effective ; a mean final dose of 100 (+/- 53) mg/day PO, which was approximately 1.6 (+/- 0.7) mg/kg/day based on available weights, was reported in a retrospective review of 21 children (age range: 8 to 18 years). Max: 200 mg/day PO. Patients with minimal or no response after 8 weeks of treatment will likely need alternative treatment. Continuation of medication for 6 to 12 months after symptom remission is recommended. Periodically reassess the need for continued treatment.
    Children and Adolescents 12 to 17 years: 25 to 50 mg/day PO initially. Clinical guidelines recommend to start with a low dose and titrate gradually in 12.5 to 25 mg/day increments at 4-week intervals until clinical response is achieved ; some studies report titration in 25 mg to 50 mg/day increments as often as every 1 to 2 weeks. A dose of 50 mg/day PO is considered effective. A mean final dose of 110 (+/- 50) mg/day PO, which was approximately 2 (+/- 0.85) mg/kg/day, was reported in an open study of 13 hospitalized adolescents. In another analysis, the mean dosage range was approximately 121 to 134 mg/day PO. Max: 200 mg/day PO. Patients with minimal or no response after 8 weeks of treatment will likely need alternative treatment. Continuation of medication for 6 to 12 months after symptom remission is recommended. Periodically reassess the need for continued treatment.

    For the treatment of generalized anxiety disorder (GAD)*:
    Oral dosage:
    Children and Adolescents 7 to 17 years: 25 mg PO once daily, initially. After 1 week, increase the dose to 50 mg PO once daily. If necessary, increase at intervals of not less than 1 week. Max: 200 mg/day PO. Periodically reassess the need for continued treatment. Evaluation of the long-term safety and efficacy of sertraline in the treatment of childhood GAD is needed. One large placebo-controlled trial assessed 488 pediatric patients with a primary diagnosis of separation anxiety (1.4%), generalized anxiety disorder (GAD) (7.1%), social phobia (10%), or a combination of these anxiety disorders (81.5%). Nearly 81% of patients receiving cognitive behavior therapy (CBT) + sertraline were rated as very much or much improved compared to 54.9% of those receiving sertraline alone, 59.7% of those receiving CBT alone, and 23.7% of those receiving placebo. At the final visit (12 weeks), the mean dose of sertraline in the CBT-sertraline group was 133.7 mg/day and the mean dose in the sertraline group was 146 mg/day.

    For the treatment of social phobia (social anxiety disorder)*:
    Oral dosage:
    Children and Adolescents 7 to 17 years: 25 mg PO once daily, initially. After 1 week, increase the dose to 50 mg PO once daily. If necessary, increase at intervals of not less than 1 week. Max: 200 mg/day PO. One large placebo-controlled trial assessed 488 pediatric patients with a primary diagnosis of social phobia (10%), separation anxiety disorder (1.4%), generalized anxiety (7.1%), or a combination of these anxiety disorders (81.5%). Nearly 81% of patients receiving sertraline + cognitive behavior therapy (CBT) were rated as very much or much improved compared to 54.9% of those receiving sertraline alone, 59.7% of those receiving CBT alone, and 23.7% of those receiving placebo. At the final visit, the mean dose of sertraline in treated patients was 133.7 mg/day or 146 mg/day. Periodically reassess the need for ongoing maintenance treatment. Further study is needed to evaluate the long-term safety and efficacy of SSRIs in treating childhood anxiety disorders.

    For the treatment of separation anxiety disorder*:
    Oral dosage:
    Children and Adolescents 7 to 17 years: 25 mg PO once daily initially, then titrated no more often than once per week based upon response and tolerability. Max: 200 mg/day PO. Periodically reassess the need for continued treatment. Further study is needed to evaluate the long-term safety and efficacy of SSRIs in treating childhood anxiety disorders. One large placebo-controlled trial assessed 488 pediatric patients with a primary diagnosis of separation anxiety (1.4%), generalized anxiety (7.1%), social phobia (10%), or a combination of these anxiety disorders (81.5%). Nearly 81% of patients receiving cognitive behavior therapy (CBT) + sertraline were rated as very much or much improved compared to 54.9% of those receiving sertraline alone, 59.7% of those receiving CBT alone, and 23.7% of those receiving placebo. At the final visit, the mean dose of sertraline in the CBT-sertraline group was 133.7 mg/day and the mean dose in the sertraline group was 146 mg/day.

    For the treatment of panic disorder*:
    Oral dosage:
    Children and Adolescents 8 to 17 years: Published data are limited. A usual starting dose is 25 mg PO once daily with flexible dosing titration no more often than weekly, based upon response and tolerability. Max: 200 mg/day PO. Periodically reassess the need for continued treatment. Further evaluation of the long-term safety and efficacy of sertraline in the treatment of childhood panic disorder is needed. In a 6-month, open-label pilot study of 12 children and adolescents with panic disorder and some with comorbid mood or other anxiety disorders, 75% were classified as showing much to very much improvement at a median duration of 7.5 weeks of treatment with sertraline, fluoxetine, or paroxetine. Eleven patients showed some improvement, except 1 patient receiving fluoxetine who showed no change in symptomatology. The sertraline-treated patient received a dose of 125 mg/day PO during the acute treatment phase and 150 mg/day during the follow-up phase. A benzodiazepine was used in 67% of the patients while awaiting the clinical response to the SSRI.

    Maximum Dosage Limits:
    -Neonates
    Safety and efficacy have not been established.
    -Infants
    Safety and efficacy have not been established.
    -Children
    1 to 6 years: Safety and efficacy have not been established.
    6 to 12 years: 200 mg/day PO.
    -Adolescents
    200 mg/day PO.

    Patients with Hepatic Impairment Dosing
    Dosage adjustments are recommended if sertraline is administered to patients with hepatic impairment. For patients with mild hepatic impairment (Child Pugh scores 5 or 6), the recommended initial dose and therapeutic range dosing is 50% of the normal daily dosage. The use of sertraline in patients with moderate (Child Pugh scores 7 to 9) or severe hepatic impairment (Child Pugh scores 10 to 15) is not recommended.

    Patients with Renal Impairment Dosing
    No dosage adjustments are needed.

    Intermittent hemodialysis
    No dosage adjustments are needed. Sertraline is unlikely to be significantly removed by hemodialysis given its large volume of distribution.

    *non-FDA-approved indication

    Monograph content under development

    Mechanism of Action: The precise antidepressant effect of SSRIs is not fully understood, but involves selective serotonin reuptake blockade at the neuronal membrane, which enhances the actions of serotonin (5-HT). Initially, SSRIs increase availability of serotonin in the somatodendritic area through serotonin reuptake blockade at the serotonin transport pump. During long-term administration of SSRIs, serotonin autoreceptors are down-regulated and desensitized, allowing the neuron to increase serotonin release in the axon terminal synapses and increase its neuronal impulses. Because of the delay in therapeutic response to SSRIs, it is theorized that the change in the balance of serotonin receptors over time is an important mechanism of effect. The therapeutic action of SSRIs in treating anxiety disorders is thought to occur from potent central serotonin reuptake blockade although the exact mechanism is unknown. SSRIs have less sedative, anticholinergic, and cardiovascular effects than do tricyclic antidepressants due to dramatically decreased binding to histaminergic, muscarinic, and alpha-adrenergic receptors.

    Pharmacokinetics: Sertraline is administered orally. In young adults, steady-state concentrations are achieved after about 1 week. Sertraline appears to be highly protein-bound (98%), but it does not compete with warfarin or propranolol for binding sites, possibly because its presumed binding site is an alpha-1 acid glycoprotein and not albumin. Sertraline undergoes extensive first-pass metabolism. In vitro data suggest sertraline is a substrate of CYP2B6, CYP2C9, CYP2D6, CYP3A4, and CYP2C19. The primary metabolite is N-desmethylsertraline, which is substantially less active than sertraline. Both sertraline and N-desmethylsertraline undergo oxidative deamination and subsequent reduction, hydroxylation, and glucuronide conjugation. The average elimination half-life of sertraline is 26 hours. N-desmethylsertraline has an elimination half-life of 62 to 104 hours. Unchanged sertraline is not detected in the urine; however, 12% to 14% of unchanged sertraline is recovered in feces.

    Affected cytochrome P450 isoenzymes and drug transporters: CYP2D6
    Because sertraline is metabolized by various CYP450 isoenzymes, inhibition of one enzyme by another drug is not likely to significantly affect sertraline concentrations. Sertraline inhibits CYP2D6; it may be necessary to reduce the dosage of concomitantly administered drugs metabolized by CYP2D6. Sertraline appears to have little effect, if any, on the metabolic capacity of other CYP450 isoenzymes. Sertraline and N-desmethylsertraline have a high in vitro affinity for P-glycoprotein (P-gp); the clinical significance of this finding is unknown.


    -Route-Specific Pharmacokinetics
    Oral Route
    After oral administration of sertraline for 14 days, the peak concentration (Cmax) occurred between 4.5 to 8.4 hours after dosing. The single-dose bioavailability of the tablets is approximately equal to an equivalent dose of oral solution. Administration with food causes a small increase in Cmax and AUC. Steady-state concentrations are achieved after 1 week of once-daily dosing.


    -Special Populations
    Pediatrics
    Children and Adolescents
    Relative to adults, pediatric patients 6 to 17 years of age showed about 22% lower AUC and Cmax values when plasma concentrations were adjusted for weight. Half-life was similar to adults.

    Hepatic Impairment
    In adult patients with chronic mild liver impairment (n = 10; 8 with Child-Pugh scores of 5 to 6 and 2 with Child-Pugh scores of 7 to 8), sertraline clearance was reduced, resulting in about 3-fold greater exposure compared to those with no hepatic impairment. The exposure to desmethylsertraline was about 2-fold greater. There were no significant differences in plasma protein binding between the groups. The effects of sertraline in patients with moderate and severe hepatic impairment have not been studied.

    Renal Impairment
    Pharmacokinetic data indicate that renal elimination of sertraline is comparable between healthy volunteers and adult patients with mild to severe renal impairment, including those on dialysis.

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