sertraline

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:

May ↑ risk of suicide attempt/ideation especially during early treatment or dose adjustment; this risk appears to be greater in adolescents or children;
Severe renal impairment;
Severe hepatic impairment;
History of mania;
Angle-closure glaucoma;
OB: Use during 3rd trimester may result in neonatal serotonin syndrome requiring prolonged hospitalization and respiratory and nutritional support. Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Children <6 yr (safety and effectiveness not established);
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.

Adv. Reactions/Side Effects ⬆ ⬇

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/BEHAVIORS, twitching, weakness, yawning

Misc: fever

Interactions ⬆ ⬇

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 MAO inhibitors. MAO inhibitors should be stopped ≥14 days before sertraline therapy. Sertraline should be stopped ≥14 days before MAO inhibitor therapy.
MAO-inhibitor-like drugs, including 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 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, may ↑ risk of serotonin syndrome.
May ↑ sensitivity to adrenergics and ↑ the risk of serotonin syndrome.
Concurrent use with alcohol is not recommended.
May ↑ levels and risk of toxicity 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 may ↑ levels and risk of toxicity.
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.

Availability ⬆ ⬇

(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

Route/Dosage ⬆ ⬇

Depression

PO (Adults ): 50 mg once daily in the morning or evening initially; after several weeks, may ↑ 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 weeks, may ↑ 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 ↑ to 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).

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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

Therapeutic effects:

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.

Classifications ⬆ ⬇

Therapeutic Classification: antidepressants

Pharmacologic Classification: selective serotonin reuptake inhibitors ssris

Pharmacokinetics ⬆ ⬇

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.

Time/Action Profile ⬆ ⬇

(antidepressant effect)

ROUTE	ONSET	PEAK	DURATION
PO	within 2–4 wk	unknown	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct to take 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.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications, especially St. John's wort or SAMe.
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 provider 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 occur.
Advise patient and caregivers to immediately notify health care provider if signs/symptoms of serotonin syndrome occur.
Advise patient to avoid alcohol or other CNS depressant drugs during therapy and to consult with health care provider before taking other medications and to avoid alcohol or other CNS depressant drugs, including opioids, during therapy.
Inform patient that frequent mouth rinses, good oral hygiene, and sugarless gum or candy may minimize dry mouth. If dry mouth persists for >2 wk, consult health care provider regarding use of saliva substitute.
Advise patient to wear sunscreen and protective clothing to prevent photosensitivity reactions.
Advise patient to notify health care provider 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 men, ejaculatory delay or failure, ↓ libido, and erectile dysfunction may occur. In women, may result in ↓ libido and delayed or absent orgasm. Advise patient to notify health care provider if symptoms occur.
Emphasize the importance of follow-up exams to monitor progress. Encourage patient participation in psychotherapy to improve coping skills.
Rep: Advise women of reproductive potential to notify health care provider 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 ↑ risk of postpartum hemorrhage. Monitor infants exposed to sertraline for excess sedation, restlessness, agitation, poor feeding, poor weight gain, or 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 online at https://womensmentalhealth.org/research/pregnancyregistry/antidepressants.

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Indications ⬇

Contraind./Precautions ⬆ ⬇