Sertraline hydrochloride
Sertraline hydrochloride (Zoloft)
Sertraline Hydrochloride
( SIR-trah-leen)
Pregnancy Category: C Zoloft (Rx)

Classification: Antidepressant

See Also: See also Selective Serotonin Reuptake Inhibitors.

Action/Kinetics: Steady-state plasma levels are usually reached after 1 week of once daily dosing but is increased to 2-3 weeks in older clients. Time to peak plasma levels: 4.5-8.4 hr. Peak plasma levels: 20-55 ng/mL. Time to reach steady state: 7 days. Terminal elimination t 1/2: 1-4 days (including active metabolite). Washout period is 7 days. Food decreases the time to reach peak plasma levels. Undergoes significant first-pass metabolism; significant (98%) binding to serum proteins. Excreted through the urine (40%-45%) and feces (40%-45%). Metabolized to N-desmethylsertraline, which has minimal antidepressant activity.

Uses: Treatment of depression with reduced psychomotor agitation, anxiety, and insomnia. Obsessive-compulsive disorders in adults and children as defined in DSM-IV. Treatment of panic disorder, with or without agoraphobia, as defined in DSM-IV.

Special Concerns: Use with caution in hepatic or renal dysfunction, and with seizure disorders. Plasma clearance may be lower in elderly clients. The possibility of a suicide attempt is possible in depression and may persist until significant remission occurs.

Side Effects: A large number of side effects is possible; listed are those side effects with a frequency of 0.1% or greater. GI: Nausea and diarrhea (common), dry mouth, constipation, dyspepsia, vomiting, flatulence, anorexia, abdominal pain, thirst, increased salivation, increased appetite, gastroenteritis, teeth-grinding, dysphagia, eructation, taste perversion or change. CV: Palpitations, hot flushes, edema, hypertension, hypotension, peripheral ischemia, postural hypotension or dizziness, syncope, tachycardia. CNS: Headache (common), insomnia (common), somnolence, agitation, nervousness, activation of mania/hypomania, seizures, anxiety, dizziness, tremor, fatigue, impaired concentration, yawning, paresthesia, hypoesthesia, twitching, hypertonia, confusion, ataxia or abnormal coordination, abnormal gait, hyperesthesia, hyperkinesia, abnormal dreams, aggressive reaction, amnesia, apathy, delusion, depersonalization, depression, aggravated depression, emotional lability, euphoria, hallucinations, neurosis, paranoid reaction, suicide ideation or attempt abnormal thinking, hypokinesia, migraine, nystagmus, vertigo. Dermatologic: Rash, acne, excessive sweating, alopecia, pruritus, cold and clammy skin, facial edema, erythematous rash, maculopapular rash, dry skin. Musculoskeletal: Myalgia, arthralgia, arthrosis, dystonia, muscle cramps or weakness. GU: Urinary frequency, micturition disorders, menstrual disorders, dysmenorrhea, dysuria, painful menstruation, intermenstrual bleeding, sexual dysfunction and decreased libido, nocturia, polyuria, dysuria, urinary incontinence. Respiratory: Rhinitis, pharyngitis, yawning, bronchospasm, coughing, dyspnea, epistaxis. Ophthalmologic: Blurred vision, abnormal vision, abnormal accommodation, conjunctivitis, diplopia, eye pain, xerophthalmia. Otic: Tinnitus, earache. Body as a whole: Asthenia, fever, chest pain, chills, back pain, weight loss or weight gain, generalized edema, malaise, flushing, hot flashes, rigors, lymphadenopathy, purpura.

Laboratory Test Alterations: AST or ALT, total cholesterol, triglycerides. Serum uric acid. Altered platelet function. Hyponatremia.

Overdose Management: Symptoms: Intensification of side effects. Treatment: Establish and maintain an airway, ensuring adequate oxygenation and ventilation. Activated charcoal, with or without sorbitol, may be as or more effective than emesis or lavage. Cardiac and VS should be monitored. Provide general supportive measures and symptomatic treatment. Since sertraline has a large volume of distribution, it is unlikely that dialysis, forced diuresis, hemoperfusion, or exchange transfusion will be beneficial.

Additional Drug Interactions Because sertraline is highly bound to plasma proteins, its use with other drugs that are also highly protein bound may lead to displacement, resulting in higher plasma levels of the drug and possibly increased side effects. Alcohol / Concurrent use is not recommended in depressed clients Benzodiazepines / Clearance of benzodiazepines metabolized by hepatic oxidation Cimetidine / Half-life and blood levels of sertraline Clozapine / Serum clozapine levels Diazepam / Plasma levels of desmethyldiazepam (significance not known) Erythromycin / Possiblity of "Serotonin Syndrome" Hydantoins / Possible hydantoin levels

How Supplied: Tablet: 25 mg, 50 mg, 100 mg

Dosage
?Tablets Depression.
Adults, initial: 50 mg once daily either in the morning or evening. Clients not responding to a 50-mg dose may benefit from doses up to a maximum of 200 mg/day.
Obsessive-compulsive disorder.
Adults: 50-200 mg/day. Children, 6 to 12 years: 25 mg once a day; adolescents, 13 to 17 years: 50 mg once a day. Those not responding may require doses up to a maximum of 200 mg/day.
Panic attacks.
Adults, initial: 25 mg/day for the first week; then, increase the dose to 50 mg once daily.

NOTE: Lower the dose or space dose frequency in those with hepatic or renal impairment.