sertraline (Rx)

Brand and Other Names:Zoloft
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Dosing & Uses

AdultPediatricGeriatric

Dosing Forms Strengths

tablet

  • 25mg
  • 50mg
  • 100mg

oral concentrate

  • 20mg/mL

Major Depressive Disorder

Initial: 50 mg PO qDay

May increase by 25 mg at 1-week intervals; not to exceed 200 mg qDay

Obsessive-Compulsive Disorder

Initial: 50 mg PO qDay

May increase by 25 mg at 1-week intervals; not to exceed 200 mg qDay

Panic Disorder, Posttraumatic Stress Disorder

Initial: 25 mg PO qDay

May increase by 25 mg at 1-week intervals; not to exceed 200 mg qDay

Social Anxiety Disorder

Initial: 25 mg PO qDay

May increase by 25 mg at 1-week intervals not to exceed 200 mg qDay

Premenstrual Dysphoric Disorder

Initial: 50 mg qDay 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 qDay when administered continuously or 100 mg qDay when administered during luteal phase only

Pruritus (Off-label)

25-100 mg daily for up to 5 years; 75-100 mg doses found to be most effective

Dosage Modifications

Renal impairment: Dose adjustment not necessary

Hepatic impairment

  • Mild (Child-Pugh 5-6): Decrease recommended starting dose and therapeutic dose by 50%
  • Moderate-to-severe (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

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg
  • 100mg

oral concentrate

  • 20mg/mL
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Obsessive-Compulsive Disorder

<6 years: Safety and efficacy not established

6-12 years: 25 mg PO qDay initially

12-17 years: 50 mg PO qDay initially

May increase by 50 mg qDay at 1-week intervals to no more than 200 mg qDay; give qHS if somnolence experienced

Dosage Modifications

Renal impairment: Dose adjustment not necessary

Hepatic impairment

  • Mild (Child-Pugh 5-6): Decrease recommended starting dose and therapeutic dose by 50%
  • Moderate-to-severe (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

The elderly are prone to SSRI/SNRI-induced hyponatremia; monitor closely

Major Depressive Disorder

25 mg PO qDay initially; may increase by 25 mg every 2-3 days; not to exceed 200 mg qDay

Alzheimer dementia related depression: Start at 12.5 mg/day and titrate every 1-2 weeks to response; not to exceed 150-200 mg

Dosage Modifications

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

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Interactions

Interaction Checker

and sertraline

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Diarrhea (13-24%)

            Nausea (13-30%)

            Headache (20-25%)

            Insomnia (12-28%)

            Ejaculation disorder (7-19%)

            Dizziness (6-17%)

            Dry mouth (6-16%)

            Fatigue (10-16%)

            Drowsiness (2-15%)

            1-10%

            Agitation (1-6%)

            Anorexia (5-10%)

            Anxiety (4%)

            Constipation (5-8%)

            Paresthesia (2%)

            Impotence (5-10%)

            Sweating (< 1%)

            Malaise (7-9%)

            Vomiting (4%)

            Pain (3-6%)

            Frequency Not Defined

            Asthenia

            Back pain

            Chest pain

            Hypoesthesia

            Increased appetite

            Myalgia

            Palpitations

            Rhinitis

            Tinnitus

            Weight gain

            Yawning

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            Warnings

            Black Box Warnings

            In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 years) taking antidepressants for major depressive disorders and other psychiatric illnesses

            This increase was not seen in patients over age 24 years; a slight decrease in suicidal thinking was seen in adults over age 65 years

            In children and young adults, risks must be weighed against the benefits of taking antidepressants

            Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during initial 1-2 months of therapy and dosage adjustments

            The patient’s family should communicate any abrupt changes in behavior to the healthcare provider

            Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy

            This drug is not approved for use in pediatric patients for major depressive disorder but it is approved for obsessive compulsive disorder in children >6 years

            Not approved for the treatment of bipolar depression

            Contraindications

            Hypersensitivity

            Do not use disulfiram concomitantly with oral solution due to alcohol in preparation

            Concomitant pimozide: Risk of long QT syndrome

            Coadministration with serotonergic drugs

            • Do not use MAOIs concomitantly or within 14 days before initiating sertraline or within 14 days after discontinuing sertraline
            • Reactions to concomitant administration with MAO inhibitors include tremor, myoclonus, diaphoresis, nausea, vomiting, flushing, dizziness, hyperthermia with features resembling neuroleptic malignant syndrome, seizures, rigidity, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes that include extreme agitation progressing to delirium and coma
            • Starting sertraline in a patient who is being treated with linezolid or IV methylene blue is contraindicated because of an increased risk of serotonin syndrome
            • If linezolid or IV methylene blue must be administered, discontinue SSRI immediately and monitor for CNS toxicity; may resume 24 hr after last linezolid or methylene blue dose, or after 2 weeks of monitoring (5 weeks for fluoxetine), whichever comes first

            Cautions

            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

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            Pregnancy & Lactation

            Pregnancy

            Pregnancy category: C

            Use late in the third trimester associated with complications in newborns and may require prolonged hospitalization, respiratory support, and tube feeding

            Persistent pulmonary hypertension of the newborn

            • Potential risk of persistent pulmonary hypertension of the newborn (PPHN) when used during pregnancy
            • Initial public health advisory in 2006 was based on a single published study; since then, there have been conflicting findings from new studies, making it unclear whether use of SSRIs during pregnancy can cause PPHN
            • FDA has reviewed the additional new study results and has concluded that, given the conflicting results from different studies, it is premature to reach any conclusion about a possible link between SSRI use in pregnancy and PPHN
            • FDA recommendation: FDA advises healthcare professionals not to alter their current clinical practice of treating depression during pregnancy and to report any adverse events to the FDA MedWatch program
            • A meta-analysis of 7 observational studies, found exposure to SSRIs in late pregnancy (ie, >20 weeks' gestation) more than doubled the risk of PPHN that could not be explained by other etiologies (eg, congenital malformations, meconium aspiration) (BMJ 2014;348:f6932)

            Lactation

            Distributed into milk; use caution (AAP states effect on nursing infants is unknown but may be of concern)

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Selective serotonin reuptake inhibitor; little or no affinity for alpha-adrenergic histamine or cholinergic receptor

            Absorption

            Bioavailability: Absorption increased by food

            Peak plasma time: 4.5-8.4 hr

            Distribution

            Protein bound: 98%

            Metabolism

            Metabolized by hepatic cytochrome P450 enzymes

            Metabolites: Minimal potency

            Elimination

            Half-life: 26 hr

            Dialyzable: No

            Excretion: Urine (12-14% unchanged); feces (40-45%)

            Pharmacogenomics

            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

            Genetic testing laboratories

            • Genotyping tests for CYP2D6 variants are commercially available through the following companies
            • Applied Biosystems (http://www.appliedbiosystems.com/)
            • GenPath Diagnostics (http://www.genpathdiagnostics.com/)
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            Administration

            Oral Administration

            May take with or without food

            Oral solution preparation

            • Must be diluted before administration
            • Measure dose with calibrated dropper supplied; dropper has 25 mg and 50 mg graduation marks only
            • Mix dose with 4 oz of water, ginger ale, lemon/lime soda, lemonade or orange juice only
            • A slight haze may appear, which is normal
            • Swallow dose immediately after mixing

            Discontinuing therapy

            • Abrupt discontinuation may result in adverse effects including nausea, sweating, dysphoric mood, irritability, agitation, dizziness, sensory disturbances (eg, paresthesia, tremor, anxiety, confusion, headache, lethargy, emotional lability, insomnia, hypomania, tinnitus, and seizures
            • Gradually taper dose over at least several weeks to limit possibilities of withdrawal symptoms and detection of re-emerging symptoms
            • Consider the half-life of antidepressant when tapering; those with a shorter half-life may require longer and more conservative dose reductions
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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            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.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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