SERTRALINE HYDROCHLORIDE

SERTRALINE HYDROCHLORIDE
(ser'tra-leen)
Zoloft
Classifications: psychotherapeutic agent; antidepressant; selective serotonin reuptake inhibitor (ssri);
Therapeutic: antidepressant; ssri

Prototype: Fluoxetine
Pregnancy Category: C

Availability

25 mg, 50 mg, 100 mg tablets; 20 mg/mL liquid

Action

Potent inhibitor of serotonin (5-HT) reuptake in the brain. Chronic administration results in downregulation of norepinephrine, a reaction found with other effective antidepressants. Sertraline does not inhibit MAO.

Therapeutic Effect

Effective in controlling depression, obsessive-compulsive disorder, anxiety, and panic disorder.

Uses

Major depression, obsessive-compulsive disorder, panic disorder, social anxiety disorder, premenstrual dysphoric disorder, generalized anxiety, post-traumatic stress disorder.

Unlabeled Uses

Eating disorders, generalized anxiety disorder.

Contraindications

Patients taking MAO inhibitors or within 14 d of discontinuing MAO inhibitor; concurrent use of Antabuse; suicidal ideation, hyponatremia; mania or hypomania, pregnancy (category C); third trimester of pregnancy. Safety and effectiveness in children <6 y are not established.

Cautious Use

Seizure disorders, major affective disorders, bipolar disorder, history of suicide; liver dysfunction, renal impairment; abrupt discontinuation; anorexia nervosa, recent history of MI or unstable cardiac disease, dehydration; diabetes mellitus; older adults; ECT therapy, seizure disorder, seizures; lactation.

Route & Dosage

Depression, Anxiety
Adult: PO Begin with 50 mg/d, gradually increase every few weeks according to response (range: 50–200 mg)
Geriatric: PO Start with 25 mg/d

Premenstrual Dysphoric Disorder
Adult: PO Begin with 50 mg/d for first cycle, may titrate up to 150 mg/d

Obsessive-Compulsive Disorder
Adult: PO Begin with 50 mg/d, may titrate at weekly intervals up to 200 mg/d
Child (6–12 y): PO Begin with 25 mg/d, may increase by 50 mg/wk, as tolerated and needed, up to 200 mg/d

Administration

Oral
  • Give in the morning or evening.
  • Do not give concurrently with an MAO INHIBITOR or within 14 d of discontinuing an MAO INHIBITOR.
  • Dilute concentrate before use with 4 oz of water, ginger ale, lemon/lime soda, lemonade, or orange juice ONLY. Give immediately after mixing. Caution with latex sensitivity, as the dropper contains dry natural rubber.

Adverse Effects (≥1%)

CV: Palpitations, chest pain, hypertension, hypotension, edema, syncope, tachycardia. CNS: Agitation, insomnia, headache, dizziness, somnolence, fatigue, ataxia, incoordination, vertigo, abnormal dreams, aggressive behavior, delusions, hallucinations, emotional lability, paranoia, suicidal ideation, depersonalization. Endocrine: Gynecomastia, male sexual dysfunction. GI: Nausea, vomiting, diarrhea, constipation, indigestion, anorexia, flatulence, abdominal pain, dry mouth. Special Senses: Exophthalmos, blurred vision, dry eyes, diplopia, photophobia, tearing, conjunctivitis, mydriasis. Skin: Rash, urticaria, acne, alopecia. Respiratory: Rhinitis, pharyngitis, cough, dyspnea, bronchospasm. Body as a Whole: Myalgia, arthralgia, muscle weakness, bone fracture (older adults). Metabolic: Hyponatremia in older adults.

Diagnostic Test Interference

May cause asymptomatic elevations in liver function tests. Slight decrease in uric acid.

Interactions

Drug: maois (e.g., selegiline, phenelzine) should be stopped 14 d before sertraline is started because of serious problems with other serotonin reuptake inhibitors (shivering, nausea, diplopia, confusion, anxiety). Sertraline may increase levels and toxicity of diazepam, pimozide, tolbutamide. Use cautiously with other centrally acting CNS drugs; increase risk of ergotamine toxicity with dihydroergotamine, ergotamine. Concentrate interacts with disulfiram. Herbal: St. John's wort may cause serotonin syndrome (headache, dizziness, sweating, agitation). Food: Grapefruit juice (>1 qt/d) may increase plasma concentrations and adverse effects.

Pharmacokinetics

Absorption: Slowly from GI tract. Onset: 2–4 wk. Distribution: 99% protein bound; distribution into breast milk unknown. Metabolism: Extensive first-pass metabolism in liver to inactive metabolites. Elimination: 40–45% in urine, 40–45% in feces. Half-Life: 24 h.

Nursing Implications

Assessment & Drug Effects

  • Supervise patients at risk for suicide closely during initial therapy.
  • Monitor for worsening of depression or emergence of suicidal ideation.
  • Monitor older adults for fluid and sodium imbalances.
  • Monitor patients with a history of a seizure disorder closely.
  • Lab tests: Monitor PT and INR with patients receiving concurrent warfarin therapy.

Patient & Family Education

  • Report diarrhea, nausea, dyspepsia, insomnia, drowsiness, dizziness, or persistent headache to physician.
  • Report signs of bleeding promptly to physician when taking concomitant warfarin.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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