Psychotropics India


JF Draf
Full Prescribing Info
Sertraline hydrochloride.
Each film coated tablet contains: Sertraline (as hydrochloride) 50 mg.
Pharmacotherapeutic group: Selective serotonin reuptake inhibitors. ATC Code: N06AB06.
Pharmacology: Pharmacodynamics: Mechanism of action: Sertraline is a potent and specific inhibitor of neuronal serotonin (5-HT) uptake in vitro, which results in the potentiation of the effects of 5-HT in animals. It has only very weak effects on norepinephrine and dopamine neuronal reuptake. At clinical doses, sertraline blocks the uptake of serotonin into human platelets. It is devoid of stimulant, sedative or anticholinergic activity or cardiotoxicity in animals. In controlled studies in normal volunteers, Sertraline did not cause sedation and did not interfere with psychomotor performance. In accord with its selective inhibition of 5-HT uptake, Sertraline does not enhance catecholaminergic activity. Sertraline has no affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors. The chronic administration of Sertraline in animals was associated with down-regulation of brain norepinephrine receptors as observed with other clinically effective antidepressants and antiobsessional drugs.
Clinical efficacy and safety: Major Depressive Disorder: A study was conducted which involved depressed outpatients who had responded by the end of an initial 8-week open treatment phase on Sertraline 50-200 mg/day. These patients (n=295) were randomized to continuation for 44 weeks on double-blind Sertraline 50-200 mg/day or placebo. A statistically significantly lower relapse rate was observed for patients taking Sertraline compared to those on placebo. The mean dose for completers was 70 mg/day. The % of responders (defined as those patients that did not relapse) for Sertraline and placebo arms were 83.4% and 60.8%, respectively.
Post traumatic stress disorder (PTSD): Combined data from the 3 studies of PTSD in the general population found a lower response rate in males compared to females. The results in females are more robust and males were associated with other baseline variables (more substance abuse, longer duration, source of trauma etc) which are correlated with decreased effect.
Paediatric OCD: The safety and efficacy of Sertraline (50-200 mg/day) was examined in the treatment of non-depressed children (6-12 years old) and adolescent (13-17 years old) outpatients with obsessive compulsive disorder (OCD). Patients randomized to sertraline showed significantly greater improvement than those randomised to placebo on the Children's Yale-Brown Obsessive Compulsive Scale CY-BOCS (p=0.005) the NIMH Global Obsessive Compulsive Scale (p=0.019), and the CGI improvement (p=0.002) scales. In addition, a trend toward greater improvement in the sertraline group than the placebo group was also observed on the CGI Severity scale (p=0.089).
Paediatric population: No data is available for children under 6 years of age.
Pharmacokinetics: Sertraline is slowly absorbed from the gastrointestinal tract with peak plasma concentrations occurring about 4.5 to 8.4 hours after ingestion. It undergoes extensive first-pass metabolism in the liver. The main pathway is demethylation to inactive N-desmethylsertraline, a process that appears to involve multiple cytochrome P450 isoenzymes; further metabolism and glucuronide conjugation occurs. Sertraline is widely distributed throughout body tissues and is about 98% bound to plasma proteins. The plasma elimination half-life of sertraline is reported to be about 26 hours; steady-state concentrations are achieved after about one week with regular oral doses. Sertraline is excreted in about equal amounts in the urine and faeces, mainly as metabolites. Sertraline is distributed into breastmilk.
Sertraline is used in the treatment of depression, obsessive-compulsive disorder, panic disorder with or without agoraphobia, social anxiety disorder and post-traumatic stress disorder.
It is also given for the treatment of premenstrual dysphoric disorder.
Sertraline is not indicated for use in children and adolescents under the age of 18 years with Major Depressive Disorder.
Dosage/Direction for Use
It is given orally as sertraline hydrochloride as a single dose in the morning or evening. Doses are expressed in terms of the base; sertraline hydrochloride 56 mg is equivalent to about 50 mg of sertraline.
In the treatment of depression, the usual initial dose of sertraline is 50 mg daily increased, if necessary, in increments of 50 mg at intervals of at least a week to a maximum of 200 mg daily.
The usual initial dose of sertraline in obsessive-compulsive disorder is 50 mg daily. In the treatment of panic disorder with or without agoraphobia, social anxiety disorder, and post-traumatic stress disorder, the usual initial dose is 25 mg daily increased after one week to 50 mg daily. Thereafter, doses in all these disorders may be increased, if necessary, in increments of 50 mg at intervals of at least a week to a maximum of 200 mg daily.
Sertraline is also given for the treatment of obsessive-compulsive disorder in children and adolescents aged 6 years and over. In children aged 6 to 12 years the usual initial dose is 25 mg once daily; adolescents may be started on 50 mg once daily. Increases in doses, if necessary, are similar to those in adults; however, the lower body-weights of children should be considered in order to avoid excessive doses. In the treatment of premenstrual dysphoric disorder, sertraline is given in an initial dose of 50 mg daily either throughout the menstrual cycle or during the luteal phase only, as appropriate. Doses may be increased by 50 mg each menstrual cycle up to a maximum of 150 mg daily for continuous dosing or 100 mg daily when dosing during the luteal phase only. Those patients who require 100 mg daily during luteal phase-only dosing should initially be given 50 mg daily for the first 3 days of each luteal phase dosing period. Once the optimal therapeutic response is obtained dosage should be reduced to the lowest effective level for maintenance. Reduced doses are recommended in patient with hepatic impairment. Sertraline should be withdrawn gradually to reduce the risk of withdrawal symptoms.
No specific therapy is recommended and there are no specific antidotes to sertraline. Establish and maintain an airway, ensure adequate oxygenation and ventilation. Activated charcoal, which may used to sorbitol, may be as or more effective than emesis or lavage, and should be considered in treating overdose. Cardiac and vital signs monitoring is recommended along with general symptomatic and supportive measures. Due to the large volume of distribution of sertraline, forced diuresis, dialysis, haemoperfusion and exchange transfusion are unlikely to be of benefit.
Sertraline Tablets are contraindicated in patients with a known hypersensitivity to sertraline.
Sertraline should not be used in combination with Monoamine Oxidase Inhibitor (MAOI).
Cases of serious and sometimes fatal reactions have been reported in patients receiving an SSRI and have been combination with MAOI and patients who have recently discontinued an SSRI and have been started on a MAOI. Sertraline may be started on a MAOI. Sertraline may be started 14 days after discontinuing treatment with an irreversible MAOI and at least one day after discontinuing treatment with moclobemide. At least 14 days should elapse after discontinuing Sertraline treatment before starting a MAOI.
Symptoms of a drug interaction with a MAOI include: hyperthermia, rigidity, myoclonus, automatic instability with possible rapid fluctuations of vital signs, mental status changes that include confusion, irritability and extreme agitation progressing to delirium and coma.
Special Precautions
As for SSRI's in general. Menstrual irregularities and, rarely, erythema multiforme and pancreatitis have also been reported. Sertraline should be used with caution in patients with hepatic or renal impairment; reduced doses should be considered in patients with hepatic impairment.
Use In Pregnancy & Lactation
Pregnancy: Although animal study did not provide any evidence of teratogenicity, the safety of Sertraline during human pregnancy has not been established. Sertraline should only be used in pregnancy if the potential benefits of treatment to the mother outweigh the possible risk to the developing fetus.
Lactation: Sertraline is known to be excreted in breast milk. Its effects on the nursing infant have not been established. If treatment with Sertraline is considered necessary, discontinuation of breast feeding should be considered.
Adverse Reactions
In pediatric OCD patients, side-effects which occurred significantly are headache, insomnia, agitation, anorexia and tremor. Most were of mild to moderate severity.
The following adverse reactions of sertraline have been reported: Cardiovascular: Blood pressure disturbances including postural hypotension, tachycardia.
Eye disorder: Abnormal vision.
Gastro-intestinal: Vomiting, abdominal pain.
Nervous system: Amnesia, headache, drowsiness, movement disorders paraesthesia, hypoaesthesia, depressive symptoms, hallucinations, aggressive reaction, agitation, anxiety, psychosis, depersonalisation nervousness, panic reaction and signs and symptoms associated with serotonin syndrome which include fever, rigidity, confusion, agitation, diaphoresis, tachycardia hypertension and diarrhea.
Convulsions (Seizures): Sertraline should be discontinued in any patient who develops seizures.
Musculoskeletal: Arthralgia, myalgia.
Hepatic/pancreatic: Rarely, pancreatitis and serious liver events including hepatitis, jaundice and liver failure. Asymptomatic elevations in serum transaminsases (SGOT and SGPT) have been reported in association with sertraline administration (0.8-1.3%), with an increased risk associated with the 200 mg daily dose. The abnormalities usually occurred within the first 1-9 weeks of drug treatment and promptly diminished upon drug discontinuation.
Renal & urinary disorders: Urinary retention.
Reproductive: Hyperprolactinemia, galactorrhea, menstrual irregularities, anorgasmy.
Skin and allergic reactions: Rash (including rare reports of erythema multiforme, photosensitivity), angioedema, ecchymoses, pruritus and anaphylactoid reactions.
Metabolic: Rare cases of hyponatremia have been reported and appeared to be reversible when sertraline was discontinued.
Haematologic: There have been rare reports of altered platelet function and/or abnormal clinical laboratory results in patients taking sertraline.
General: Malaise.
Others: Withdrawal reactions have been reported with sertraline. Common symptoms include dizziness, paraesthesia, headache, anxiety and nausea. Abrupt discontinuation of treatment with Sertraline should be avoided. The majority of symptoms experience on withdrawal of sertraline are non-serious and self-limiting.
Drug Interactions
Monoamine oxidase inhibitors: See Contraindications.
Centrally active medication: SSRIs have the potential to interact with tricyclic antidepressants leading to an increase in plasma levels of the tricyclic antidepressant.
Pimozide: Increased pimozide levels have been demonstrated in a study of a single low dose pimozide (2 mg) with sertraline coadministration. These increased levels were not associated with any changes ECG.
Lithium and Tryptophan: Co-administration of sertraline with lithium resulted in an increase in tremor relative in to placebo, indicating a possible pharmacodynamic interaction. There have been other reports of enhanced effects when SSRIs have given with lithium tryptophan and therefore the concomitant use of SSRIs with these drugs should be undertaken with caution.
Serotonergic drugs: Serotonergic drugs, such as tramadol, sumatriptan or fenfluramine, should not be used concomitantly with sertraline, due to a possible enhancement of 5-HT associated effects.
Warfarin: Co-administration of sertraline (200 mg daily) with warfarin may results in a small but statistically significant increase in prothrombin time.
St. John's Wort: Concomitant use of the herbal remedy St. John's Wort (Hypericum perforatum) in patients receiving SSRIs should be avoided since there is a possibility of serotonergic potention
Co-administration with cimetidine caused a substantial decrease in sertraline clearance.
Store at a temperature not exceeding 30°C. Protect from light.
MIMS Class
ATC Classification
N06AB06 - sertraline ; Belongs to the class of selective serotonin reuptake inhibitors. Used in the management of depression.
Tab 100 mg x 50's, 100's. FC tab 50 mg (white, round, biconvex, plain on both sides) x 50's.
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