SER-tra-leen

Therapeutic Classification: antidepressants

Pharmacologic Classification: selective serotonin reuptake inhibitors ssris

• Major depressive disorder.
• Panic disorder.
• Obsessive-compulsive disorder (OCD).
• Post-traumatic stress disorder (PTSD).
• Social anxiety disorder (social phobia).
• Premenstrual dysphoric disorder.

Unlabeled Uses:

• Generalized anxiety disorder.

• Inhibits neuronal uptake of serotonin in the CNS, thus potentiating the activity of serotonin. Has little effect on norepinephrine or dopamine.

• Antidepressant action.
• Decreased incidence of panic attacks.
• Decreased obsessive and compulsive behavior.
• Decreased feelings of intense fear, helplessness, or horror.
• Decreased social anxiety.
• Decrease in premenstrual dysphoria.

Absorption: Appears to be well absorbed after oral administration.

Distribution: Extensively distributed throughout body tissues.

Protein Binding: 98%.

Metabolism/Excretion: Extensively metabolized by the liver; one metabolite has some antidepressant activity; 14% excreted unchanged in feces.

Half-life: 24 hr.

(antidepressant effect)

Contraindicated in:

• Hypersensitivity
• Concurrent use of MAO inhibitors or MAO inhibitor-like drugs (linezolid or methylene blue)
• Concurrent use of pimozide
• Oral concentrate contains alcohol; avoid in patients with known intolerance.

Use Cautiously in:

• Severe renal impairment
• Severe hepatic impairment
• History of mania
• History of suicide attempt
• Angle-closure glaucoma
• OB: Use during 3rd trimester may result in neonatal serotonin syndrome requiring prolonged hospitalization, respiratory and nutritional support. Use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Pedi: May ↑ risk of suicide attempt/ideation, especially during early treatment or dose adjustment; risk may be greater in children or adolescents
• Geri: Appears on Beers list. May worsen or cause syndrome of inappropriate antidiuretic hormone (SIADH) secretion and/or hyponatremia in older adults. Use with caution in older adults and closely monitor sodium concentrations when starting therapy or ↑ dose.

CV: chest pain, palpitations, QT interval prolongation, TORSADES DE POINTES.

Derm: ↑sweating, hot flashes, rash.

EENT: pharyngitis, rhinitis, tinnitus, visual abnormalities.

Endo: diabetes, SIADH.

F and E: ↑thirst, hyponatremia.

GI: diarrhea, dry mouth, nausea, abdominal pain, altered taste, anorexia, constipation, dyspepsia, flatulence, vomiting.

GU: ↓libido, delayed/absent orgasm, ejaculatory delay/failure, erectile dysfunction, menstrual disorders, urinary disorders, urinary frequency.

Hemat: BLEEDING.

Metab: ↑appetite.

MS: back pain, myalgia.

Neuro: dizziness, drowsiness, fatigue, headache, insomnia, tremor, agitation, anxiety, confusion, emotional lability, hypertonia, hypoesthesia, impaired concentration, manic reaction, nervousness, paresthesia, SUICIDAL THOUGHTS, twitching, weakness, yawning.
Misc: fever.

Drug-Drug:

• Serious, potentially fatal reactions (hyperthermia, rigidity, myoclonus, autonomic instability, with fluctuating vital signs and extreme agitation, which may proceed to delirium and coma) may occur with concurrent MAO inhibitors. MAO inhibitors should be stopped at least 14 days before sertraline therapy. Sertraline should be stopped at least 14 days before MAO inhibitor therapy.
• Concurrent use with MAO-inhibitor–like drugs, such as linezolid or methylene blue, may ↑ risk of serotonin syndrome; concurrent use contraindicated; do not start therapy in patients receiving linezolid or methylene blue; if linezolid or methylene blue need to be started in a patient receiving sertraline, immediately discontinue sertraline and monitor for signs/symptoms of serotonin syndrome for 2 wk or until 24 hr after last dose of linezolid or methylene blue, whichever comes first (may resume sertraline therapy 24 hr after last dose of linezolid or methylene blue).
• May ↑ pimozide levels and the risk of QT interval prolongation and ventricular arrhythmias; concurrent use contraindicated.
• Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SNRIs, fentanyl, lithium, buspirone, tramadol, meperidine, methadone, amphetamines, and triptans, ↑ risk of serotonin syndrome.
• May ↑ sensitivity to adrenergics and ↑ the risk of serotonin syndrome.
• Concurrent use with alcohol is not recommended.
• May ↑ levels/effects of warfarin, phenytoin, tricyclic antidepressants, some benzodiazepines (alprazolam), or clozapine.
• ↑risk of bleeding with NSAIDs, aspirin, clopidogrel, prasugrel, ticagrelor, dabigatran, apixaban, edoxaban, rivaroxaban, or warfarin.
• Cimetidine↑ blood levels and effects.
• Concurrent use of QT interval prolonging medications may ↑ risk of QT interval prolongation and torsades de pointes; avoid concurrent use.

Drug-Natural Products:

• ↑risk of serotonergic side effects including serotonin syndrome with St. John’s wort and SAMe.

Depression

• PO (Adults): 50 mg once daily in the morning or evening initially; after several wk may be ↑ at weekly intervals up to 200 mg/day, depending on response.

Obsessive Compulsive Disorder

• PO (Adults): 50 mg once daily in the morning or evening initially; after several wk, may be ↑ at weekly intervals up to 200 mg/day, depending on response.
• PO (Children 13–17 yr): 50 mg once daily.
• PO (Children 6–12 yr): 25 mg once daily.

Panic Disorder

• PO (Adults): 25 mg once daily initially, may ↑ after 1 wk to 50 mg once daily.

Post-Traumatic Stress Disorder

• PO (Adults): 25 mg once daily for 7 days, then ↑ to 50 mg once daily; may then be ↑ if needed at intervals of at least 7 days (range 50–200 mg once daily).

Social Anxiety Disorder

• PO (Adults): 25 mg once daily initially, then 50 mg once daily; may be ↑ at weekly intervals up to 200 mg/day.

Premenstrual Dysphoric Disorder

• PO (Adults): 50 mg/day initially either daily or daily during luteal phase of cycle. Daily dosing may be titrated upward in 50-mg increments at the beginning of a cycle. In luteal phase–only dosing a 50 mg/day titration step for 3 days at the beginning of each luteal phase dosing period should be used (range 50–150 mg/day).

(Generic available)

• Tablets: 25 mg; 50 mg; 100 mg;
• Capsules: 25 mg; 50 mg; 100 mg; 150 mg; 200 mg;
• Oral solution (concentrated) (contains 12% alcohol): 20 mg/mL;

• Assess for suicidal tendencies, especially during early therapy. Restrict amount of drug available to patient. Risk may be increased in children, adolescents, and adults 24 yr. After starting therapy, children, adolescents, and young adults should be seen by health care professional at least weekly for 4 wk, every 3 wk for next 4 wk, and on advice of health care professional thereafter.
• Monitor appetite and nutritional intake. Weigh weekly. Notify health care professional of continued weight loss. Adjust diet as tolerated to support nutritional status.
• Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyper-reflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs, triptans). If symptoms occur, discontinue sertraline.
• Assess sexual function before starting sertraline. Assess for changes in sexual function during treatment, including timing of onset; patient may not report.
• Depression: Monitor mood changes. Inform health care professional if patient demonstrates significant increase in anxiety, nervousness, or insomnia.
• Assess for suicidal tendencies, especially during early therapy. Restrict amount of drug available to patient.
• OCD: Assess patient for frequency of obsessive-compulsive behaviors. Note degree to which these thoughts and behaviors interfere with daily functioning.
• Panic Attacks: Assess frequency and severity of panic attacks.
• PTSD: Assess patient for feelings of fear, helplessness, and horror. Determine effect on social and occupational functioning.
• Social Anxiety Disorder: Assess patient for symptoms of social anxiety disorder (blushing, sweating, trembling, tachycardia during interactions with new people, people in authority, or groups) periodically during therapy.
• Premenstrual Dysphoric Disorder: Assess patient for symptoms of premenstrual dysphoric disorder (feeling angry, tense, or tired; crying easily, feeling sad or hopeless; arguing with family or friends for no reason; difficulty sleeping or paying attention; feeling out of control or unable to cope; having cramping, bloating, food craving, or breast tenderness) periodically during therapy.

• May cause false-positive urine screening tests for benzodiazepines.
  • May cause hyperglycemia and diabetes mellitus; monitor serum glucose if clinical symptoms occur.

• Do not confuse sertraline with cetirizine or Soriatane.
  • Periodically reassess dose and continued need for therapy.
• PO: Administer as a single dose in the morning or evening.
  • For oral concentrate, use dropper provided to remove oral concentrate and mix with 4 oz (1/2 cup) of water, ginger ale, lemon/lime soda, lemonade, or orange juice ONLY. Do not mix with other liquids. Take immediately after mixing. Do not mix in advance. Slight haze may appear after mixing; this is normal. Dropper dispenser contains dry natural rubber; advise patient with latex allergy.

• Instruct patient to take sertraline as directed. Take missed doses as soon as possible and return to regular dosing schedule. Do not double doses. Do not stop abruptly; may cause dysphoric mood, irritability, agitation, dizziness, sensory disturbances (paresthesias such as electric shock sensations), anxiety, confusion, headache, lethargy, emotional lability, insomnia, and hypomania.
• May cause drowsiness or dizziness. Caution patient to avoid driving and other activities requiring alertness until response to the drug is known.
• Advise patient, family, and caregivers to look for suicidality, especially during early therapy or dose changes. Notify health care professional immediately if thoughts about suicide or dying, attempts to commit suicide; new or worse depression or anxiety; agitation or restlessness; panic attacks; insomnia; new or worse irritability, aggressiveness, acting on dangerous impulses, mania, or other changes in mood or behavior or if symptoms of serotonin syndrome occur.
• Advise patient to avoid alcohol or other CNS depressant drugs during therapy and to consult with health care professional before taking other medications and to avoid alcohol or other CNS depressant drugs, including opioids, during therapy.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort or SAMe.
• Inform patient that frequent mouth rinses, good oral hygiene, and sugarless gum or candy may minimize dry mouth. If dry mouth persists for more than 2 wk, consult health care professional regarding use of saliva substitute.
• Advise patient to wear sunscreen and protective clothing to prevent photosensitivity reactions.
• Advise patient to notify health care professional if headache, weakness, nausea, anorexia, anxiety, or insomnia persists, or if bleeding (bruising, hematoma, epistaxis, petechiae) occurs.
• Inform patient that sertraline may cause symptoms of sexual dysfunction. In males, ejaculatory delay or failure, decreased libido, and erectile dysfunction may occur. In female patients, may result in decreased libido and delayed or absent orgasm. Advise patient to notify health care professional if symptoms occur.
• Advise females of reproductive potential to notify health care professional immediately if pregnancy is planned or suspected or if breastfeeding. If used during pregnancy, should be tapered during 3rd trimester to avoid neonatal serotonin syndrome. Use in the month before delivery may increase risk of postpartum hemorrhage. Monitor infants exposed to sertraline for excess sedation, restlessness, agitation, poor feeding, poor weight gain, respiratory distress; may ↑ risk of persistent pulmonary hypertension of the newborn. Inform patient of pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antidepressants during pregnancy. Register patients by calling the National Pregnancy Registry for Antidepressants at 1-866-961-2388 or visiting online at womensmentalhealth.org/research/pregnancyregistry/antidepressants.
• Emphasize the importance of follow-up exams to monitor progress. Encourage patient participation in psychotherapy to improve coping skills.

• Increased sense of well-being.
  • Renewed interest in surroundings. May require 1–4 wk of therapy to obtain antidepressant effects.
• Decrease in obsessive-compulsive behaviors.
• Decrease in frequency and severity of panic attacks.
• Decrease in symptoms of PTSD.
• Decrease in social anxiety disorder.
• Decrease in symptoms of premenstrual dysphoric disorder.

Zoloft