Aurobindo Pharma


Full Prescribing Info
Sertraline hydrochloride.
Aurasert 50: Each film-coated tablet contains: Sertraline hyrdrochloride equivalent to sertraline 50mg.
Aurasert 100: Each film-coated tablet contains: Sertraline hydrochloride equivalent to sertraline 100mg.
Pharmacology: Pharmacodynamics: Setraline is a potent and selective inhibitor of neuronal serotonin (5-HT) reuptake. It has only a weak effect on Neuronal uptake of nor-epinephrine and dopamine. Setraline's inhibition of serotonin reuptake enhances serotonergic transmission.
In vitro studies have shown that sertraline has no significant affinity for adrenergic, muscarinic, cholinergic, gamma aminobutyric acid (GABA), dopaminergic, serotonergic (5HT1A, 5HT1B, 5HT2) histaminergic or benzodiazepine receptors.
Pharmacokinetics: The gastrointestinal absorption of setraline is slow but consistent. Sertraline undergoes extensive first-pass metabolism in the liver. The bioavailability is slightly increased if setraline is taken with food. Mean peak plasma concentrations of about 20-55 mcg/l occur between 4.5-8.4 hours after administration of a single 100mg dose. Sertraline is approximately 98% bound to plasma proteins. Both sertraline and its metabolites are extensively distributed into tissues. The metabolite n-desmethylsertraline exhibits only about 1/8 of its activity. It does not contribute to the antidepressant activity or toxicity of the parent compound. Both sertraline and its metabolite undergo oxidative deamination and subsequent reduction, hydroxylation and glucuronide conjugation. Only 0.2% of the unchanged drug is excreted through the kidneys. The elimination half-life of sertraline is 24 to 26 hours. The pharmacokinetics of sertraline in elderly patients is similar to younger adults.
Sertraline pharmacokinetics have been evaluated in a group of 61 pediatric patients (29 aged 6-12 years, 32 aged 13-17 years) with a DSM-III-R diagnosis of depression or obsessive-compulsive disorder. During 42 days of chronic sertraline dosing, sertraline was titrated upto 200mg/day and maintained at that dose for a minimum of 11 days. Relative to the adults, both the 6-12 year olds and 13-17 years old showed about 22% lower AUC (0-24 hours) and Cmax values when plasma concentration was adjusted for weight. These data suggest that paediatric patients metabolize sertraline with slightly greater efficiency in adults. Nevertheless, lower doses may be advisable for pediatric patients given their lower body weights, especially in very young patients, in order to avoid excessive plasma levels.
Aurasert is indicated for the treatment of symptoms of depressive illness including accompanying symptoms of anxiety. It is also indicated in preventing relapse of the initial episode of depression or recurrence of further depressive episodes including accompanying symptoms of anxiety.
Aurasert is indicated in the treatment of obsessions and compulsions in patients with obsessive compulsive disorder.
Aurasert is indicated for the treatment of panic disorder with or without agoraphobia.
Dosage/Direction for Use
Dosage for adults: Depression: Initially 50mg per day as a single daily dose. The dose may be increased after several weeks with increments of 50mg made at intervals of at least 1week, as needed and tolerated, upto a maximum dose of 200 mg once daily. In elderly individuals, a lower initiation dose (12.5 to 25mg) may be used.
Obsessive-compulsive disorder: Aurasert should be administered at a dose of 50mg. The daily dose may be increased if required at intervals of at least one week, up to 200mg.
Panic disorder: Aurasert treatment should be initiated with a dose of 25mg once daily. After one week, the dose should be increased to 50 mg once daily. Further increments may be made up to a dose of 200 mg/d.
Doses of 150 mg or more should not be used for periods exceeding 5 weeks.
Aurasert tablets should be administered once daily, either in the morning or evening.
Mode of adminisration: Aurasert tablets should be administered once daily, either in the morning or evening.
Signs & symptoms of over dosage with sertraline may include somnolence, nausea, vomiting, tachycardia, anxiety ECG changes and dilated pupils. There is no specific antidote for sertraline. Treatment of over dosage involves establishing and maintaining airway, oxygenation and ventilation. Activated charcoal may be used with sorbitol. Cardiac and vital signs monitoring is recommended along with general symptomatic & supportive measures.
Aurasert should not be used concomitantly to patients taking monoamine oxidase inhibitors, while switching from a MAOI to sertraline or vice-versa, a washout period of at least 14 days should elapse.
Aurasert is also contraindicated in patients with a previous history of hypersensitivity to sertraline.
Mutagenicity/carcinogenicity: Sertraline has no genotoxic effects with or without metabolic activation. Possibility of increase in follicular adenomas of the thyroid, unaccompanied by thyroid hyperplasia is higher if the dose exceeds 40mg/kg.
Suicidality in children and adolescents: Antidepressants increase the risk of suicidal thinking and behavior (suicidality) in children and adolescents with major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of an antidepressant in a child or adolescent for any clinical use must balance the risk of increased suicidality with the clinical need. Patients who are started on therapy should be observed closely for clinical worsening, suicidality or unusual changes in behavior. Families and caregivers should be advised to closely observe the patient and to communicate with the prescriber. A statement regarding whether the particular drug is approved for any pediatric indication(s) and, if so, which one(s).
Aurasert should not be used in combination with a MAOI, or within 14 days of discontinuing treatment with a MAOI.
As with other antidepressants, activation of mania/hypomania has been reported in a small proportion of patients.
Special Precautions
General: Sertraline should be used with caution in patients with hepatic impairment; in patients with cirrhosis of the liver, a lower dose or a lower frequency of dosing should be employed. Since sertraline is extensively metabolized in the liver, renal route is a minor route of elimination. Therefore, sertraline dosing does not have to be adjusted based on the degree of renal impairment. However, caution is advised in patients with severe renal impairment, until more data becomes available. Sertraline should be introduced with care in patients with seizure disorders. No clinical studies have been performed on the risks/benefits of combining sertraline therapy with electroconvulsive therapy. Careful supervision of depresses patients with suicidal tendencies is recommended especially during the early treatment phase.
Concomitant use of alcohol with Aurasert should be avoided.
Use in Children: The safety and efficacy of sertraline for the treatment of obsessive compulsive disorder has been demonstrated in a 12 week, multicenter, placebo-controlled study. The risks, if any that may be associated with sertraline's extended use in children adolescents with OCD have not been systematically assessed. Safety and effectiveness in pediatric patients below the age of 6 have not been established. Effectiveness of sertraline in pediatric patients with depression or panic disorder has not been established.
Use In Pregnancy & Lactation
Pregnancy: No teratogenic effects were demonstrated in rats and rabbits receiving 20 and 10 times the maximum daily human mg/kg dose, respectively. Adequate and well-controlled studies in humans have not been done. Aurasert should be used during pregnancy if clearly needed.
Lactation: There is no data available on the secretion of sertraline in breast milk, hence use in nursing mothers is not recommended.
Side Effects
Side effects reported with sertraline include nausea, diarrhea, vomiting, anorexia, abdominal cramps, tremor, anxiety, agitation, dizziness, nervousness, blurred vision, dryness of mouth and palpitations. Other side effects rarely reported with sertraline include fever, rash, weight loss, decreased sexual drive, delayed ejaculation, mania and insomnia.
Asymptomatic elevations in serum transaminases (SGOT and SGPT) have been reported infrequently (approximately 0.8%) in association with sertraline administration. The abnormalities usually occurred within the first 1 to 9 weeks of drug treatment and promptly diminished upon drug discontinuation.
Drug Interactions
Cases of serious, sometimes fatal, reactions have been reported in patients receiving sertraline, in combination with a monoamine oxidase inhibitor (MAOI). Symptoms of a drug interaction between an SSRI and a MAOI include: hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, mental status changes that include confusion, irritability, and extreme agitation progressing to delirium and coma. Some cases presented with features resembling neuroleptic malignant syndrome. Therefore, sertraline should not be used in combination with a MAOI or within 14 days of discontinuing treatment with a MAOI. Similarly, at least 14 days should be allowed after stopping sertraline before starting a MAOI (see also Contraindications).
Concurrent use of intravenous diazepam with sertraline may reduce the clearance and prolong the half-life diazepam.
Caution is recommended during concurrent use of digitoxin and warfarin with sertraline because of possible displacement of either medication from protein binding sites. This may lead to increase plasma concentrations and increased risk of adverse effects. Prothrombin time should be caredully monitored when sertraline therapy is initiated or stopped in patients taking warfarin. Drugs metabolized by cytochrome P450 2D6: sertraline inhibits the biochemical activity of the drug metabolizing isozyme P450 2D6 and, thus may increase the plasma concentration of co-administered drugs (which are metabolized by P450 2D6) such as tricyclic antidepressants and type IC antiarrhythmics, propafenone and flecainide: dose reduction may be required.
Nonetheless, it is recommended that plasma lithium levels be monitored following initiation of sertraline therapy with appropriate adjustments to the lithium dose.
Store at or below 30°C.
Shelf-Life: 36 months.
MIMS Class
ATC Classification
N06AB06 - sertraline ; Belongs to the class of selective serotonin reuptake inhibitors. Used in the management of depression.
FC tab 50 mg (white coloured, biconvex, capsule shaped, debossed with 'A' on one side and with a score line in between '8' and '1' on the other side) x 2 x 14's, 10 x 10's. 100 mg (white coloured, biconvex, capsule shaped debossed with 'A' on one side and '82' on the other side) x 2 x 14's, 10 x 10's.
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