SERTRALINE

brands

Class

• Neuroscience-based Nomenclature: serotonin reuptake inhibitor (S-RI)
• SSRI (selective serotonin reuptake inhibitor); often classified as an antidepressant, but it is not just an antidepressant

SERTRALINE commonly prescribed for

(Bold for FDA approved)

How SERTRALINE works

• Boosts neurotransmitter serotonin

• Blocks serotonin reuptake pump (serotonin transporter)

• Desensitizes serotonin receptors, especially serotonin 1A receptors

• Presumably increases serotonergic neurotransmission

• Sertraline also has some ability to block dopamine reuptake pump (dopamine transporter), which could increase dopamine neurotransmission and contribute to its therapeutic actions

• Sertraline also binds at sigma 1 receptors

How long until SERTRALINE works

• Some patients may experience increased energy or activation early after initiation of treatment

• Onset of therapeutic actions is usually not immediate, but often delayed 2–4 weeks

• If it is not working within 6 or 8 weeks, it may require a dosage increase (off label) or it may not work at all

• May continue to work for many years to prevent relapse of symptoms

Notable Side Effects

• Sexual dysfunction (dose-dependent; men: delayed ejaculation, erectile dysfunction; men and women: decreased sexual desire, anorgasmia)

• Gastrointestinal (decreased appetite, nausea, diarrhea, constipation, dry mouth)

• Mostly CNS (insomnia but also sedation, agitation, tremors, headache, dizziness)

• Activation (short-term; patients with diagnosed or undiagnosed bipolar or psychotic disorders may be more vulnerable to CNS-activating actions of SSRIs)

• Sweating

• Bruising and rare bleeding

• Syndrome of inappropriate antidiuretic hormone secretion (SIADH)

Life Threatening Side Effects

• Rare seizures

• Rare hyponatremia (mostly in elderly patients and generally reversible on discontinuation of sertraline)

• Rare hypotension

• Rare induction of mania

• Rare activation of suicidal ideation and behavior (suicidality) (short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo beyond age 24)

weight gain

unusual

sedation

unusual

What to do about SERTRALINE side effects

• Wait

• Wait

• Wait

• If sertraline is activating, take in the morning to help reduce insomnia

• Reduce dose to 25 mg or even 12.5 mg until side effects abate, then increase dose as tolerated, usually to at least 50 mg/day

• In a few weeks, switch or add other drugs

usual dosage range

• 50–200 mg/day

• 25–100 mg/day (Japan)

Dosage Forms

• Tablet 25 mg scored, 50 mg scored, 100 mg

• Capsule 150 mg, 200 mg

• Oral solution 20 mg/mL

long term use

• Safe

habit forming

• No

Renal Impairment

• No dose adjustment necessary

• Not removed by hemodialysis

Hepatic Impairment

• Lower dose or give less frequently, perhaps by half

Cardiac Impairment

• Proven cardiovascular safety in depressed patients with recent myocardial infarction or angina

• Treating depression with SSRIs in patients with acute angina or following myocardial infarction may reduce cardiac events and improve survival as well as mood

• Should be used with caution in patients with risk factors for QTc prolongation

Elderly

• Some patients may tolerate lower doses and/or slower titration better

• Risk of SIADH with SSRIs is higher in the elderly

• Reduction in the risk of suicidality with antidepressants compared to placebo in adults age 65 and older

Children and Adolescents

• Carefully weigh the risks and benefits of pharmacological treatment against the risks and benefits of nontreatment with antidepressants and make sure to document this in the patient’s chart

• Monitor patients face-to-face regularly, particularly during the first several weeks of treatment

• Use with caution, observing for activation of known or unknown bipolar disorder and/ or suicidal ideation, and strongly consider informing parents or guardian of this risk so they can help observe child or adolescent patients

• Approved for use in OCD

• Ages 6–12: initial dose 25 mg/day

• Ages 13 and up: adult dosing

• Long-term effects, particularly on growth, have not been studied

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Not generally recommended for use during pregnancy, especially during first trimester

• Nonetheless, continuous treatment during pregnancy may be necessary and has not been proven to be harmful to the fetus

• At delivery there may be more bleeding in the mother and transient irritability or sedation in the newborn

• Must weigh the risk of treatment (first trimester fetal development, third trimester newborn delivery) to the child against the risk of no treatment (recurrence of depression, maternal health, infant bonding) to the mother and child

• For many patients, this may mean continuing treatment during pregnancy

• Exposure to serotonin reuptake inhibitors early in pregnancy may be associated with increased risk of septal heart defects (absolute risk is small)

• Use of serotonin reuptake inhibitors beyond the 20th week of pregnancy may be associated with increased risk of pulmonary hypertension in newborns, although this is not proven

• Exposure to serotonin reuptake inhibitors late in pregnancy may be associated with increased risk of gestational hypertension and preeclampsia

• Neonates exposed to SSRIs or SNRIs late in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding; reported symptoms are consistent with either a direct toxic effect of SSRIs and SNRIs or, possibly, a drug discontinuation syndrome, and include respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycemia, hypotonia, hypertonia, hyperreflexia, tremor, jitteriness, irritability, and constant crying

Breast Feeding

• Some drug is found in mother’s breast milk

• Trace amounts may be present in nursing children whose mothers are on sertraline

• Sertraline has shown efficacy in treating postpartum depression

• If child becomes irritable or sedated, breast feeding or drug may need to be discontinued

• Immediate postpartum period is a high-risk time for depression, especially in women who have had prior depressive episodes, so drug may need to be reinstituted late in the third trimester or shortly after childbirth to prevent a recurrence during the postpartum period

• Must weigh benefits of breast feeding with risks and benefits of antidepressant treatment versus non-treatment to both the infant and the mother

• For many patients, this may mean continuing treatment during breast feeding