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Sertraline information from DrugsUpdate  

See Available Brands of Sertraline in India

P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *

Sertraline is primarily used to treat major depression in adult outpatients as well as obsessive–compulsive, panic, and social anxiety disorders in both adults and children.

Pharmacodynamics

The mechanism of action of Sertraline is presumed to be linked to its inhibition of CNS neuronal uptake of serotonin (5HT). Studies at clinically relevant doses in man have demonstrated that Sertraline blocks the uptake of serotonin into human platelets. In vitro studies in animals also suggest that Sertraline is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. In vitro studies have shown that Sertraline has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of Sertraline was found in animals to down regulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Sertraline does not inhibit monoamine oxidase.

Pharmacokinetics

Sertraline has a potent and selective inhibitory action on CNS neuronal reuptake of 5-HT resulting in increased 5-HT concentrations at the synaptic clefts, leading to sustained activity at the postsynaptic receptor sites and improvement of depression. Reduction of serotonin turnover (in brain) also contributes to its action. Its long half-life allows once daily admin.

Absorption

Absorbed slowly from the GI tract (oral); plasma concentrations peak 4.5-8.5 hours after oral admin.

Distribution
Body tissues (wide), enters breast milk. Protein-binding: 98%.

Metabolism
Extensive hepatic first-pass metabolism; demethylation to N-desmethylsertraline (inactive) then to glucuronide conjugates.

Excretion
Via urine and faeces (as metabolites); elimination half-life: about 26 hours.

Sertraline Indications / Sertraline Uses

Information Not Available

Sertraline Adverse Reactions / Sertraline Side Effects

Nausea, anorexia, dyspepsia, constipation, diarrhoea, dry mouth, flatulence, vomiting, ejaculation failure, increased sweating, somnolence, agitation, insomnia, headache, dizziness, fatigue, anxiety, nervousness, tremor, paraesthesia, decreased libido, rash, hot flushes, blurred vision.

Precautions

 A group of serious side effects, called serotonin syndrome, have resulted from the combination of antidepressants such as sertraline and members of another class of antidepressants known as monoamine oxidase (MAO) inhibitors. Serotonin syndrome usually consists of at least three of the following symptoms: diarrhea, fever, sweatiness, mood or behavior changes, overactive reflexes, fast heart rate, restlessness, shivering or shaking. Because of this, sertraline should never be taken in combination with MAO inhibitors. Patient taking any MAO inhibitors, for example Nardil (   phenelzine   sulfate) or Parmate (   tranylcypromine   sulfate), should stop the MAO inhibitor then wait at least 14 days before starting sertraline or any other antidepressant. The same holds true when discontinuing sertraline and starting an MAO inhibitor. Also, people should not take sertraline oral concentrate while using  disulfiram  (Antabuse). Sertraline should never be taken by people who are any other SSRI antidepressants.

Sertraline should be used with cautiously and with close physician supervision by people with a prior history of seizures , people who are at an increased risk of bleeding, and those for whom weight loss is undesirable. Sertraline may precipitate a shift to mania in patients with bipolar (formerly manic-depressive) disease.


Overdosage
Symptoms include nausea, vomiting and CNS excitation. May lead to death.

Special Precautions

History of hypomania and seizure disorders, hepatic and renal impairment, cardiac disease, recent MI, history of bleeding disorders, DM and angle-closure glaucoma. Discontinue treatment if seizures develop or if there is an increase in seizure frequency. Withdrawal should be gradual. Monitor for signs of clinical worsening, suicidality and unusual changes in behaviour especially during the initial treatment period or when there are dosage adjustments. Pregnancy and lactation.

Other Drug Interactions

May increase risk of delirium when used with antimuscarinics. Increased risk of extrapyramidal symptoms and neuroleptic malignant syndrome when used with aripiprazole. Serum levels may be reduced by carbamazepine. Concurrent use with dihydroergotamine or linezolid may lead to serotonin syndrome. May increase serum levels of lamotrigine and risk of toxicity. May increase serum levels of olanzapine, pimozide, risperidone, methadone, clozapine and amiodarone. Plasma levels may be increased by cimetidine and ritonavir. May increase the anticoagulant activity of warfarin and acenocoumarol.

Potentially Fatal: Concomitant admin with MAOIs can result in serious serotonin syndrome.

Other Interactions

Food Interaction
Co-admin with food increases peak plasma concentration of sertraline. Plasma levels are increased by grapefruit juice.

Dosage

Oral
Depression
Adult: Initially, 50 mg once daily, may increase in steps of 50 mg at weekly intervals. Max: 200 mg daily.
Child: For obsessive-compulsive disorder: 6-12 years: Initially, 25 mg once daily; 13-17 years: Initially, 50 mg once daily. May increase dose at intervals of at least 1 week, to a max of 200 mg/day. If somnolence is noted, give at bedtime.
Hepatic impairment: Dosage reduction may be required.

Oral

Obsessive compulsive disorder
Adult: Initially, 50 mg once daily, may increase in steps of 50 mg at weekly intervals. Max: 200 mg daily.
Child: For obsessive-compulsive disorder: 6-12 years: Initially, 25 mg once daily; 13-17 years: Initially, 50 mg once daily. May increase dose at intervals of at least 1 week, to a max of 200 mg/day. If somnolence is noted, give at bedtime.
Hepatic impairment: Dosage reduction may be required.

Oral
Panic disorder with or without agoraphobia
Adult: Initially, 25 mg daily, increased after 1 week to 50 mg daily. May increase in steps of 50 mg at weekly intervals. Max: 200 mg daily.
Hepatic impairment: Dosage reduction may be required.

Oral
Posttraumatic stress disorder
Adult: Initially, 25 mg daily, increased after 1 week to 50 mg daily. May increase in steps of 50 mg at weekly intervals. Max: 200 mg daily.
Hepatic impairment: Dosage reduction may be required.

Oral
Social anxiety disorder
Adult: Initially, 25 mg daily, increased after 1 week to 50 mg daily. May increase in steps of 50 mg at weekly intervals. Max: 200 mg daily.
Hepatic impairment: Dosage reduction may be required.

Oral
Premenstrual dysmorphic disorder
Adult: Initially, 50 mg daily. May be given throughout the menstrual cycle or only during the luteal phase. May increase by 50 mg each cycle if needed. Max: 150 mg daily for continuous dosing or 100 mg daily for luteal phase-only dosing. Patients who require 100 mg daily for luteal phase-only dosing should always start with 50 mg daily for the 1st 3 days of each luteal phase dosing period.
Hepatic impairment: Dosage reduction may be required.

Food(before/after)

May be taken with or without food.

List of Contraindications

Sertraline and Pregnancy

Caution when used during pregnancy

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Sertraline and Lactation

Caution when used during lactation

Sertraline and Children

Safety and effectiveness in pediatric patients with major depressive disorder have not been established.

Sertraline and Geriatic

No overall differences in the pattern of efficacy were observed in the geriatric clinical trial subjects relative to those reported in younger subjects.

Sertraline and Other Contraindications

Children <18 years. Poorly controlled epilepsy.

Storage

Oral
Store at 15-30°C

Lab interference

Oral
Store at 15-30°C

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