Sertraline hydrochloride.
Each film-coated tablet contains Sertraline Hydrochloride equivalent to sertraline 50 mg.
Pharmacology: PHARMACODYNAMICS: Sertraline is a potent and selective inhibitor of neuronal serotonin (5-HT) reuptake 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 accord with its selective inhibition of 5-HT uptake, sertraline does not enhance catecholaminergic activity. Sertraline has little 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.
PHARMACOKINETICS: Sertraline exhibits dose proportional pharmacokinetics over the range of 50 to 200 mg. In man, following oral once-daily dosing over the range of 50 to 200 mg for 14 days, peak plasma concentrations (Cmax) of sertraline occur at about 4.5 to 8.4 hours post dosing. The mean half life of sertraline for young and elderly men and women ranges from 22-36 hours. Consistent with the terminal elimination half-life, there is an approximately two-fold accumulation up to steady state concentrations, which are achieved after 1 week of once daily dosing. Approximately 98% of the circulating drug is bound to plasma proteins. Animal studies indicate that sertraline has a large apparent volume of distribution. The pharmacokinetics of sertraline in pediatric OCD patients have been shown to be comparable with adults (although pediatric patients metabolize sertraline with slightly greater efficiency). However, lower doses may be advisable for pediatric patients, given their lower body weights (especially those patients 6-12 years), in order to avoid excessive plasma levels. Sertraline undergoes extensive first pass hepatic metabolism. The principal metabolite in plasma, N-desmethylsertraline, is substantially less active (about 20 times) than sertraline in vitro and there is no evidence of activity in in vivo models of depression. The half-life of N-desmethylsertraline is in the range of 62-104 hours. Sertraline and N-desmethylsertraline are both extensively metabolized in man and the resultant metabolites excreted in feces and urine in equal amounts. Only a small amount (<0.2%) of unchanged sertraline is excreted in the urine.
Sertraline is indicated for the treatment of depression, obsessive-compulsive disorder and panic disorder, with or without agoraphobia, post-traumatic disorder (PTSD), social phobia, premenstrual dysphoric disorder (PMDD).
Initial Treatment: Depression and obsessive-compulsive disorder: 50 mg once daily.
Panic Disorder, PTSD, social phobia: Treatment should be initiated with 25 mg once daily. After one week, the dose should be increased to 50 mg once daily.
Premenstrual Dysphoric Disorder (PMDD): Treatment should be initiated with 50 mg once daily, either daily throughout the menstrual cycle or limited to the luteal phase of menstrual cycle, depending on physician assessment.
Titration: Depression, OCD, Panic Disorder and PTSD: Patients not responding to a 50 mg dose may benefit from dose increases. Dose changes should be made at intervals of at least one week, up to a maximum of 200 mg/day. Changes in dose should not be made more frequently than once per week given the 24-hour elimination half life of sertraline. The onset of therapeutic effect may be seen within 7 days. However, longer periods are usually necessary to demonstrate therapeutic response, especially in OCD.
Premenstrual Dysphoric Disorder (PMDD): Patients not responding to a 50 mg dose may benefit from dose increases (at 50 mg increments/menstrual cycle) up to 150 mg/day when dosing daily throughout the menstrual cycle, or 100 mg/day when dosing during the luteal phase of the menstrual cycle. If a 100 mg/day dose has been established with luteal phase dosing, a 50 mg/day titration step for three days should be utilized at the beginning of each luteal phase dosing period.
Maintenance: Dosage during long-term therapy should be kept at the lowest effective level, with subsequent adjustment depending on therapeutic response.
Use in children: The safety and efficacy of sertraline has been established in pediatric OCD patients aged 6 to 17. The administration of sertraline to pediatric OCD patients (aged 13-17) should commence at 50 mg/day. Therapy for pediatric OCD patients (aged 6-12) should commence at 25 mg/day increasing to 50 mg/day after one week. Subsequent doses may be increased in case of lack of response in 50 mg/day increments, up to 200 mg/day, as needed. In a clinical trial in patients aged 6 to 17 years with depression or OCD, sertraline appeared to have a similar pharmacokinetic profile to that found in adults. However, the generally lower body weights of children compared to those of adults should be taken into consideration when increasing the dose from 50 mg.
Use in elderly: No special precautions are needed. The usual adult dose is recommended.
OVERDOSE AND TREATMENT: Symptoms of overdose include somnolence, nausea, vomiting, tachycardia, ECG changes, anxiety and dilated pupils. Treatment is primarily supportive and included monitoring and use of activated charcoal, gastric lavage or cathartics and hydration. Establish and maintain an airway, ensure adequate oxygenation and ventilation.
There are no specific antidotes for sertraline. Activated charcoal, which may be used with 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, force diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit.
1. Hypersensitive to sertraline.
2. Those taking concomitant monoamine oxidase inhibitors.
3. Those taking concomitant pimozide.
Monoamine oxidase inhibitors: Serious reactions such as confusion and irritability, chills, pyrexia and muscle rigidity have been reported in patients receiving sertraline in combination with a monoamine oxidase inhibitor (MAOI). Further, there have been reports of serious, sometimes fatal reactions including hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, mental status changes that include extreme agitation progressing to delirium and coma in patients receiving another SSRI in combination with a monoamine oxidase inhibitor (MAOI). Therefore, it is recommended that 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.
Other serotonergic drugs: Co-administration of sertraline with other drugs which enhance the effects of serotonergic neurotransmission, such as tryptophan or fenfluramine or 5-HT agonists, should be undertaken with caution and avoided whenever possible due to the potential for a pharmacodynamic interaction.
Switching from selective serotonin reuptake inhibitors (SSRIs), antidepressants or antiobsessional drugs: There is limited controlled experience regarding the optimal timing of switching from SSRIs, antidepressants or antiobsessional drugs to sertraline. Care and prudent medical judgment should be exercised when switching, particularly from long-acting agents such as fluoxetine. The duration of a washout period for switching from one SSRI to another has not been established.
Activation of mania/hypomania: As with other antidepressants, hypomania or mania have been reported to occur in approximately 0.4% of sertraline treated patients. Activation of mania/hypomania has also been reported in a small proportion of patients with major affective disorder treated with other marketed antidepressant and antiobsessional drugs. Use with caution in patients with a history of mania.
Seizures: Seizures are a potential risk with antidepressants and antiobsessional drugs. During the development program for OCD, four out of approximately 1800 patients exposed to sertraline experienced seizures (approximately 0.2%). Three of these patients were adolescents, two with a seizure disorder and one with a family history of seizure disorder, none of whom were receiving anti-convulsant medication. In all these cases, the relationship to sertraline therapy was uncertain. Since sertraline has not been evaluated in patients with a seizure disorder, it should be avoided in patients with unstable epilepsy; patients with controlled epilepsy should be carefully monitored. Sertraline should be discontinued in any patient who develop seizures.
Suicide: Since the possibility of a suicide attempt is inherent in depression and may persist until significant remission occurs, patients should be closely supervised during the early course of therapy.
Because of the well-established comorbidity between OCD and depression, panic disorder and depression, PTSD and depression, and social phobia and depression, the same precautions observed when treating patients with depression should be observed when treating patients with OCD, panic disorder, PTSD or social phobia.
Use in hepatic insufficiency: Sertraline is extensively metabolized by the liver. A multiple-dose pharmacokinetic study in subjects with mild, stable cirrhosis demonstrated a prolonged elimination half-life and approximately three-fold greater AUC and Cmax in comparison to normal subjects. There were no significant differences in plasma protein binding observed between the two groups. The use of sertraline in patients with hepatic disease should be approached with caution. A lower or less frequent dose should be used in patients with hepatic impairment.
Use in renal insufficiency: Sertraline is extensively metabolized. Excretion of unchanged drug in urine is a minor route of elimination. In studies of patients with mild to moderate renal impairment (creatinine clearance 30-60 ml/min) or moderate to severe renal impairment (creatinine clearance 10-29 ml/min), multiple-dose pharmacokinetic parameters (AUC0-24 or Cmax) were not significantly different compared with controls. Half-life were similar and there were no differences in plasma protein binding in all groups studied. This study indicates that, as expected from the low renal excretion of sertraline, sertraline dosing does not have to be adjusted based on the degree of renal impairment.
As there are no adequate and well-controlled studies of sertraline in pregnant women, this drug should be used during pregnancy only if clearly needed. It is not known whether, and if so in what amount, sertraline or its metabolites are excreted in human milk. Caution should be exercised when sertraline is administered to a nursing woman.
Gastrointestinal disorders: diarrhea, dry mouth, dyspepsia, nausea, abdominal pain, constipation, pancreatitis, vomiting.
Metabolism and nutrition disorders: anorexia, appetite increased, hyponatremia.
Nervous system disorders: dizziness, somnolence, tremor, coma, convulsions, headache, hypoesthesia, migraine, movement disorders.
Reproductive system and breast disorders: sexual dysfunction (principally ejaculatory delay in males), galactorrhea, gynecomastia, menstrual irregularities.
Skin and subcutaneous tissues disorders: increased sweating.
Blood and lymphatic system disorders: leucopenia, thrombocytopenia.
Cardiac disorders: palpitations, tachycardia.
Ear disorders: tinnitus.
Endocrine disorders: hyperprolactinemia, hypothyroidism, syndrome of inappropriate ADH secretion (SIADH).
Eye disorders: mydriasis, vision abnormal.
General disorders: asthenia, chest pain, edema peripheral, fever, malaise.
Musculoskeletal and connective tissue disorders: arthralgia, muscle cramps.
Psychiatric disorders: aggressive, agitation, anxiety, depression, euphoria, hallucination, libido decreased-female, libido decreased-male, paroniria, psychosis.
Renal and urinary disorders: urinary incontinence, urinary retention.
Vascular disorders: abnormal bleeding (such as epistaxis, gastrointestinal bleeding, hematuria), hot flushes, hypertension.
Other: symptoms following the discontinuation of sertraline have been reported and included agitation, anxiety, dizziness, headache, nausea, paresthesia.
Sertraline may increase the levels/effects of selected beta-blockers, bupropion, selected benzodiazepines, calcium channel blockers, cisapride, cyclosporine, dextromethorphan, ergot alkaloids, fluoxetine, paroxetine, phenytoin, risperidone, selegiline and sildenafil.
The levels/effects of sertraline may be increased by chlorpromazine, fluconazole, fluoxetine, fluvoxamine, gemfibrozil, isoniazid, miconazole, omeprazole, quinine and ticlopidine.
Combined use of sertraline and buspirone, nefazodone, serotonin agonists (such as sumatriptan), ritonavir, tramadol and venlafaxine may increase the risk of serotonin syndrome.
Concurrent lithium may increase risk of nephrotoxicity.
Risk of hyponatremia may increase with concurrent use of loop diuretics (bumetanide, furosemide, torsemide).
Co-administration of sertraline with warfarin results in small but significant increase in prothrombin time, prothrombin time should be carefully monitored in such cases.
Although sertraline did not potentiate the cognitive and psychomotor effects of alcohol in normal subjects, the concomitant use of this drug and alcohol in depressed patients is not recommended.
No interaction was observed with digoxin.
Concomitant use of sertraline and NSAIDs, aspirin, or other drug affecting coagulation has been associated with an increased risk of bleeding.
Sertraline may inhibit the metabolism of thioridazine or mesoridazine, resulting in increased plasma levels and increasing the risk of QTc interval prolongation. This may lead to serious ventricular arrhythmias.
The levels/effects of sertraline may be decreased by aminoglutethimide, carbamazepine, phenytoin, rifampin.
Store below 30°C. Protect from light.
N06AB06 - sertraline ; Belongs to the class of selective serotonin reuptake inhibitors. Used in the management of depression.
Serlin 50 FC tab 50 mg
3 × 10's
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