sertraline hydrochloride
Zoloft

Available forms
Available by prescription only
Oral concentrate: 20 mg/ml
Tablets (film-coated): 25 mg, 50 mg, 100 mg

Indications and dosages
 Post-traumatic stress disorder (PTSD) or panic disorder. Adults: Initially, 25 mg P.O. once daily. Increase to 50 mg P.O. daily after 1 week. If no improvement, dose may be increased up to a maximum of 200 mg P.O. daily. Maintain patient on lowest effective dosage.
 Depression, obsessive-compulsive disorder (OCD). Adults: Initially, 50 mg P.O. once daily. Adjust dose as needed and tolerated. Dosage adjustments should be made at intervals of no less than 1 week.
Children ages 13 to 17 (OCD only): Initially, 50 mg P.O. once daily. Increase at intervals no less than 1 week. Maximum, 200 mg daily.
Children ages 6 to 12 (OCD only): Initially, 25 mg P.O. once daily. Increase at intervals no less than 1 week. Maximum, 200 mg daily.
 Premenstrual dysphoric disorder. Adults: 50 to 150 mg P.O. daily.
 Premature ejaculation ◇. Adults: 25 to 50 mg P.O. daily or p.r.n.
≡ Dosage adjustment. For patients with hepatic impairment, use lower dose or less frequent delivery. Take particular care in patients with renal failure.

Pharmacodynamics
Antidepressant action: Sertraline probably acts by blocking the reuptake of serotonin (also known as 5-hydroxytryptamine [5-HT]) into presynaptic neurons in the CNS, prolonging the action of 5-HT.

Pharmacokinetics
Absorption: Well absorbed after oral administration; absorption rate and extent are enhanced when taken with food.
Distribution: In vitro studies indicate that drug is more than 98% protein-bound.
Metabolism: Metabolism is probably hepatic; drug undergoes significant first-pass metabolism. N-desmethylsertraline is substantially less active than the parent compound.
Excretion: Excreted mostly as metabolites in the urine and feces. Mean elimination half-life is 26 hours. Steady state levels are reached within 1 week of daily dosing in young, healthy patients.

Contraindications and precautions
Contraindicated in patients receiving MAO inhibitors. Use cautiously in patients at risk for suicide and in those with seizure disorders, major affective disorder, or diseases or conditions that affect metabolism or hemodynamic responses. Avoid using the oral concentrate dropper, which is made of rubber, if patient has a latex allergy.

Interactions
Drug-drug. Cimetidine: Increases sertraline bioavailability, peak plasma levels, and half-life. Monitor patient closely.
Diazepam, tolbutamide: Decreases clearance of these drugs. Monitor patient for increased drug effects.
Disulfiram: Oral concentrate contains alcohol that could cause a reaction. Avoid use together.
Drugs metabolized by P-450 (CYP) 2D6: May increase plasma levels of coadministered drugs. Use with caution.
MAO inhibitors: Causes serious mental status changes, hyperthermia, autonomic instability, rapid fluctuations of vital signs, delirium, coma, and death. Don’t give drug within 14 days of an MAO inhibitor.
Warfarin, other highly protein-bound drugs: May cause interactions, increasing plasma levels of sertraline or the other highly bound drug. Monitor patient closely.
Drug-herb. St. John’s wort: Increases risk of serotonin syndrome.Discourage use together.

Adverse reactions
CNS: headache, tremor, dizziness, insomnia, somnolence, paresthesia, hypoesthesia, fatigue, nervousness, anxiety, agitation, hypertonia, twitching, confusion.
CV: palpitations, chest pain, hot flashes.
GI: dry mouth, nausea, diarrhea, loose stools, dyspepsia, vomiting, constipation, thirst, flatulence, anorexia, abdominal pain, increased appetite.
GU: male sexual dysfunction, polyuria, nocturia, dysuria.
Musculoskeletal: myalgia.
Skin: rash, pruritus, diaphoresis.

Effects on lab test results
• May increase ALT, AST, serum cholesterol, and triglyceride levels. May decrease uric acid levels.

Overdose and treatment
Experience with sertraline overdose is limited.
 Treatment is supportive. Establish an airway and maintain adequate ventilation. Because recent studies question the value of forced emesis or lavage, consider the use of activated charcoal in sorbitol to bind drug in the GI tract. There’s no specific antidote for sertraline. Monitor vital signs closely. Because drug has a large volume of distribution, hemodialysis, peritoneal dialysis, or forced diuresis probably isn’t useful.

Special considerations
• Zoloft is safe and effective in preventing relapse of PTSD and in sustaining symptom improvement over 28 weeks (long-term use) in men and women.
• Drug may activate mania or hypomania in patients with cyclic disorders.
• Record mood changes and monitor patient for suicidal tendencies.
• Avoid using the oral concentrate dropper, which is made of rubber, in a patient with a latex allergy.
• Mix oral concentrate with 4 oz (120 ml) of water, ginger ale, or lemon-lime soda and give the dose right away.
Breast-feeding patients
• It isn’t known if drug appears in breast milk. Use cautiously in breast-feeding women.
Pediatric patients
• Safety and efficacy in children with depression or panic disorder haven’t been established.
Geriatric patients
• Plasma clearance of drug is slower in elderly patients. Studies indicate that it may take 2 to 3 weeks of daily dosing before steady state levels occur.
• Monitor patient closely for dose-related adverse effects. Elderly patients may be more likely than younger patients to develop hyponatremia and transient SIADH.

Patient education
• Tell patient to take drug once daily, either in the morning or evening, with or without food.
• Advise patient to avoid alcohol while taking drug and to call before taking OTC medications.
• Although problems haven’t been reported to date, advise patient to use caution when performing hazardous tasks that require alertness, such as driving and operating heavy machinery. Drugs that influence the CNS may impair judgment.
• Advise patient to mix the oral concentrate with 4 oz (120 ml) of water, ginger ale, or lemon-lime soda only and to take the dose right away.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use