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Pronunciation: SER-tra-leen HYE-droe-KLOR-ide
Class: Selective serotonin reuptake inhibitor
- Tablets 25 mg
- Tablets 50 mg
- Tablets 100 mg
- Solution, oral concentrate 20 mg/mL
Selectively blocks reuptake of serotonin, enhancing serotonergic function.
T max is 4.5 to 8.4 h postdose. Steady state should be achieved after approximately 1 wk of once-daily dosing. AUC was slightly increased when the tablet was given with food but C max was 25% greater; T max decreased from 8 h postdosing to 5.5 h. T max of the oral concentrate was prolonged from 5.9 to 7 h with food.
Sertraline is 98% protein bound.
Sertraline undergoes extensive first-pass metabolism. The principal initial metabolic pathway is N-demethylation. The liver is the primary site of metabolism.
Sertraline half-life is 26 h; half-life of metabolite is 62 to 104 h.
Special PopulationsRenal Function Impairment
Sertraline multiple-dose pharmacokinetics are unaffected by renal impairment.Hepatic Function Impairment
Liver function impairment can affect the elimination of sertraline. Give a lower, less frequent dose.Elderly
Plasma Cl 40% lower; steady state achieved after 2 to 3 wk.Children
Children metabolize sertraline with slightly greater efficacy than adults.
Indications and Usage
Treatment of major depressive disorder; treatment of obsessions and compulsions in patients with obsessive-compulsive disorder (OCD); treatment of panic disorder with or without agoraphobia; treatment of posttraumatic stress disorder (PTSD); treatment of premenstrual dysphoric disorder; treatment of social anxiety disorder (social phobia).
Cholestatic pruritus, hot flashes, nocturnal enuresis.
Hypersensitivity to any components; concomitant use in patients taking MAOIs or pimozide; oral concentrate is contraindicated with disulfiram because of the alcohol content in the oral concentrate.
Dosage and AdministrationMajor Depressive Disorder
PO 50 mg once daily (max, 200 mg/day). Dose changes should not occur at intervals of less than 1 wk.OCD
Adults and Children 13 to 17 yr of age
PO 50 mg once daily (max, 200 mg/day). Dose changes should not occur at intervals of less than 1 wk.Children 6 to 12 yr of age
PO 25 mg once daily (max, 200 mg/day). Dose changes should not occur at intervals of less than 1 wk.Panic Disorder, PTSD, and Social Anxiety Disorder
PO 25 mg once daily; the dosage should be increased to 50 mg once daily after 1 wk (max, 200 mg/day). Dose changes should not occur at intervals of less than 1 wk.Premenstrual Dysphoric Disorder
PO 50 mg/day, either daily throughout the menstrual cycle or limited to the luteal phase of the menstrual cycle. Patients not responding to 50 mg/day may benefit from increases (at 50 mg increments/menstrual cycle) up to 150 mg/day when dosing throughout the menstrual cycle, or 100 mg/day when dosing during the luteal phase of the menstrual cycle. If a 100 mg/day dosage has been established with luteal dosing, use a 50 mg/day titration step for 3 days at the beginning of each luteal phase dosing period.Hepatic Function Impairment
Give lower or less frequent dosage. Use with caution.Switching Patients To or From MAOIs
At least 14 days should elapse between discontinuation of an MAOI and initiation of therapy with sertraline and 14 days should be allowed after stopping sertraline before starting an MAOI.
- Oral concentrate must be diluted before use. Mix required amount of sertraline with 4 oz of water, ginger ale, lemon/lime soda, lemonade, or orange juice only. Administer immediately. Do not mix in advance.
Store at 59° to 86°F.
Drug Interactions5-HT 1 agonists (eg, naratriptan, rizatriptan, sumatriptan, zolmitriptan)
Weakness, hyperreflexia, and incoordination reported rarely.Alcohol, CNS depressants
May enhance CNS depressant effects. Alcohol use is not recommended.Carbamazepine
Sertraline plasma levels may be reduced, decreasing the pharmacologic effects.Cimetidine
Increased sertraline AUC (50%), C max (24%), and half-life (26%).Cisapride
Concurrent use reduced cisapride AUC and C max by approximately 35%.Clozapine
Elevated serum clozapine levels have occurred. Closely monitor patients during coadministration.Cyclosporine
Elevated cyclosporine levels may occur.Cyproheptadine
May decrease the pharmacologic effects of sertraline.Diazepam IV
Cl for diazepam decreased 32%.Disulfiram
Sertraline oral concentrate is contraindicated with disulfiram because of the oral concentrate's alcohol content.Drugs highly bound to plasma proteins (eg, warfarin, digitoxin)
May cause a shift in plasma concentrations resulting in adverse reactions.Drugs interfering with hemostasis (eg, aspirin, non-selective NSAIDs [eg, ibuprofen], warfarin)
Risk of bleeding may be increased.Drugs metabolized by CYP2D6 (eg, carvedilol, risperidone)
Plasma concentrations of these drugs may be elevated, increasing the pharmacologic effects and adverse reactions.Hydantoins (eg, phenytoin)
Plasma levels may be increased by sertraline, increasing the pharmacologic effects and adverse reactions.L-tryptophan
Concurrent use is not recommended.Lithium, macrolide antibiotics (eg, erythromycin), metoclopramide, sibutramine, sympathomimetics, tramadol, trazodone
Risk of serotonin syndrome may be increased.MAOIs, linezolid
May cause serious, even fatal reactions. Concomitant use is contraindicated. Discontinue MAOIs at least 14 days before starting sertraline; at least 14 days should be allowed after stopping sertraline before starting an MAOI.Pimozide
Increase in pimozide AUC and C max of about 40%; coadministration is contraindicated.St. John's wort
Sedative-hypnotic effects of sertraline may be increased. Avoid concurrent use.Tolbutamide
Sertraline significantly decreased the Cl of tolbutamide (16%).Tricyclic antidepressants (eg, amitriptyline)
Pharmacologic and toxic effects may be increased by sertraline; “serotonin syndrome” has been reported.Type 1C antiarrhythmics (eg, flecainide, propafenone)
Plasma levels may be increased. Monitor cardiac function.Zolpidem
Onset of action of zolpidem may be shortened and the effect increased.
Laboratory Test Interactions
None well documented.
Palpitations, chest pain (at least 1%); increased coagulation times, bradycardia, AV block, atrial arrhythmias, QT-interval prolongation, ventricular tachycardia (including torsades de pointes) (postmarketing).
Headache (25%); insomnia (21%); somnolence (13%); dizziness, fatigue (12%); malaise (9%); tremor (8%); decreased libido (6%); agitation, nervousness (5%); anxiety (4%); aggressive reaction, hyperkinesia (at least 2%); paresthesia (2%); asthenia, hypertonia, hypesthesia (at least 1%); extrapyramidal symptoms, NMS, oculogyric crisis, psychosis, serotonin syndrome (postmarketing).
Sweating (7%); rash (3%); photosensitivity, Stevens-Johnson syndrome, vasculitis (postmarketing).
Abnormal vision (3%); tinnitus (at least 1%); blindness, cataract, optic neuritis (postmarketing).
Nausea (25%); diarrhea (20%); dry mouth (14%); dyspepsia (8%); abdominal pain, anorexia, constipation (6%); vomiting (4%); increased appetite (at least 1%); pancreatitis (postmarketing).
Abnormal ejaculation (14%); sexual dysfunction, urinary incontinence (at least 2%); impotence (at least 1%); priapism; acute renal failure (postmarketing).
Purpura (at least 2%); agranulocytosis, aplastic anemia, leukopenia, lupus-like syndrome, pancytopenia, serum sickness, thrombocytopenia (postmarketing).
Elevated liver enzymes (1%); increased bilirubin, hepatomegaly, hepatitis, jaundice, liver failure (postmarketing).
Decrease in serum uric acid (7%); increased triglycerides (5%); increase in total cholesterol (3%).
Increased weight (at least 1%); hyperglycemia, hypothyroidism (postmarketing).
Epistaxis, sinusitis (at least 2%); rhinitis (at least 1%).
Pain (6%); fever, pain, weight loss (at least 2%); back pain, myalgia, yawning (at least 1%); anaphylaxis, angioedema, galactorrhea, hyperprolactinemia, pulmonary hypertension (postmarketing).
Antidepressants increase the risk of suicidal thinking and behavior (suicidality) in short-term studies in children, adolescents, and young adults with major depressive disorders and other psychiatric disorders. Closely observe all patients who are started on therapy for clinical worsening, suicidality, or unusual changes in behavior.
Ensure patient with depressive symptoms is screened to determine risk for bipolar disorder before initiating therapy with sertraline.
Category C . Consider tapering dosing in the third trimester.
Safety and efficacy not established, except in children 6 to 18 yr of age with OCD.
May be at greater risk of hyponatremia.
Use drug with caution. Lower or less frequent dosing schedule may be required.
Special Risk Patients
Use with caution in patients with diseases or conditions that could affect metabolism or hemodynamic responses.
Bleeding episodes have been reported in patients taking psychotropic drugs that interfere with serotonin reuptake.
Activation of mania/hypomania
Activation of mania/hypomania occurs infrequently in patients taking SSRIs.
Serious adverse reactions (eg, dysphoric mood, irritability, anxiety, emotional lability, insomnia, hypomania) may occur upon sertraline discontinuation, particularly when abrupt. A gradual reduction in dose is recommended.
Duration of therapy
Periodically reassess patients to determine the need for maintenance treatment.
Several cases of sertraline-induced hyponatremia have occurred.
The dropper dispenser supplied with the oral concentrate may contain dry natural rubber.
Use drug with caution in patients with history of seizures.
May cause a decrease in serum uric acid.
Weight loss has been reported.
Agitation, alopecia, bradycardia, bundle branch block, coma, convulsions, decreased libido, delirium, diarrhea, dizziness, ejaculation disorder, fatigue, hallucinations, hypertension, hypotension, insomnia, manic reaction, nausea, pancreatitis, QT-interval prolongation, serotonin syndrome, somnolence, stupor, syncope, tachycardia, tremor, vomiting.
- Advise patient to read patient information leaflet before starting therapy and with each refill.
- If patient is a child or adolescent, advise patient, family, or caregiver to read the Medication Guide About Using Antidepressants in Children and Teenagers before starting therapy and with each refill.
- Advise patient that medication usually is started at a low dose and then gradually increased until max benefit is obtained.
- Advise patient to take prescribed dose once daily in the morning or evening without regard to meals but to take with food if stomach upset occurs.
- Caution patient or caregiver that oral concentrate must be diluted before administration. Advise patient or caregiver to measure prescribed dose of oral concentrate using calibrated syringe and mix, immediately before use, with 4 oz (½ cup) of water, ginger ale, lemon/lime soda, lemonade or orange juice, and administer immediately after mixing. Caution patient or caregiver not to prepare ahead of time.
- Caution patient or caregiver not to dilute oral concentrate with any other liquid than those previously noted. Advise patient or caregiver that a slight haze may appear after mixing oral concentrate but that this is expected and is not a concern.
- Inform patient that it may take 1 to 4 wk to note improvement in symptoms and to continue with the prescribed therapy once improvement has been noted.
- Instruct patient to notify health care provider if symptoms do not appear to be getting better, or if they worsen, or if bothersome adverse reactions (eg, unusual sweating, headache, drowsiness, insomnia, nausea, diarrhea, nervousness, changes in sexual function) occur.
- Advise all patients, and family or caregiver of patient, to be alert for abnormal changes in mood or thinking and to immediately report any of the following to health care provider: anxiety; agitation; panic attacks; insomnia; irritability; hostility or aggressiveness; impulsivity; akathisia (psychomotor restlessness); suicidal thoughts or behavior. Advise families and caregivers of patients to observe for emergence on a day-to-day basis, because changes may be abrupt.
- Advise patient that if medication needs to be discontinued it will be slowly withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
- Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
- Advise patient to avoid alcoholic beverages and other depressants while taking sertraline.
- Advise patient that drug may impair judgment, thinking, or reflexes, and to use caution while driving or performing other activities requiring mental alertness until tolerance is determined.
- Instruct patient not to take any prescription or OTC drugs, including aspirin or NSAIDs (eg, ibuprofen), herbal preparations, or dietary supplements without consulting health care provider.
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