Esopam

ESOPAM 10: White, elliptical, biconvex, film coated tablet with scored on one side and plain on the other side.
Each film coated tablet contains Escitalopram oxalate 12.775 mg eq. to Escitalopram 10 mg.
ESOPAM 20: White, elliptical, biconvex, film coated tablet with engraved 20 on one side and plain on the other side.
Each film coated tablet contains Escitalopram oxalate 25.55 mg eq. to Escitalopram 20 mg.

Pharmacology: Pharmacodynamics: Escitalopram oxalate, a selective serotonin reuptake inhibitor (SSRI) and S-enantiomer of racemic citalopram, enhances serotonergic activity in the central nervous system (CNS) as a result of its inhibition of serotonin (5-HT) reuptake in CNS neurons. It possesses no or very low affinity for serotonergic (5-HT_1-7), alpha- and beta-adrenergic, dopamine (D_1-5), histamine (H_1-3), muscarinic (M_1-5), and benzodiazepine receptors as well as various ion channels including Na⁺, K⁺, Cl^-, and Ca²⁺ channels.
Pharmacokinetics: Absorption: Time to peak concentration: about 5 hours in adults, 2.9 hours in adolescents.
Effect of food: no effect.
Bioavailability: 80%.
Distribution: Protein binding: approximately 56% to plasma protein.
V_d: approximately 20 L/kg.
Metabolism: Hepatic via CYP3A4 and CYP2C19; N-demethylation.
Excretion: Renal: urine (8% as unchanged drug, 10% as S-DCT).
Hepatic impairment: decreased by 37%.
Mild to moderate renal impairment: decreased by 17%.
Severe renal impairment (CrCl <20 mL/minute): No information available.
Elimination Half Life: Adolescents: 19 hours.
Adults: 27 to 32 hours.
Elderly: increased by approximately 50% and doubled in patients with hepatic impairment.

Treatment of major depressive episodes.
Treatment of panic disorder with or without agoraphobia.
Treatment of social anxiety disorder (social phobia).
Treatment of generalized anxiety disorder.
Treatment of obsessive-compulsive disorder.

Adult: Major depressive episodes: Initial: 10 mg/day orally. The dose may increase to 20 mg/day depending on individual patient response.
Usually 2-4 weeks are necessary to obtain antidepressant response. After the symptoms resolve, treatment for at least 6 months is required for consolidation of the response.
Panic disorder with or without agoraphobia: Initial: 5 mg/day for the first week, then increase dose to 10 mg/day, may further increase to 20 mg/day based on response and tolerability.
Maximum effectiveness is reached after about 3 months. The treatment lasts several months.
Social anxiety disorder (social phobia): Initial: 10 mg/day orally. The dose may increase to 20 mg/day depending on individual patient response.
Usually 2-4 weeks are necessary to obtain symptom relief. Treatment for 3 months is recommended to consolidate response. Long-term treatment of responders for 6 months has been shown to prevent relapse and can be considered on an individual basis. Treatment benefits should be re-evaluated at regular intervals.
Generalized anxiety disorder: Initial: 10 mg/day orally. The dose may increase to 20 mg/day depending on individual patient response.
Treatment for 3 months is recommended to consolidate response. Long-term treatment of responders for 6 months has been shown to prevent relapse and can be considered on an individual basis. Treatment benefits should be re-evaluated at regular intervals.
Obsessive-compulsive disorder (OCD): Initial: 10 mg/day orally. The dose may increase to 20 mg/day depending on individual patient response.
Long-term treatment of patients responding to a 16-week open treatment phase has been studied for at least 24 weeks in patients receiving 10 or 20 mg/day. As OCD is a chronic disease, patients should be treated for a sufficient period to ensure that they are symptom free. This period may be several months or even longer.
Children and adolescents (<18 years): Escitalopram should not be used in the treatment of children and adolescents under the age of 18 years.
Elderly patients (≥65 years of age): Initial treatment with half the usually recommended dose and a lower maximum dose should be considered.
Renal impairment: Mild to moderate renal impairment: No adjustment necessary.
Severe renal impairment (CrCl <30 mL/minute): Use with caution.
Hepatic impairment: An initial dose of 5 mg/day for the first two weeks of the treatment is recommended. The dose may increase to 10 mg/day depending on individual patient response.
Poor metabolisers of CYP2C19: For patients who are known to be poor metabolisers with respect to CYP2C19, an initial dose of 5 mg daily during the first two weeks of treatment is recommended. Depending on individual patient response, the dose may be increased to 10 mg daily.
Discontinuation of therapy: Avoid abrupt discontinuation. Taper dose gradually over a period of at least one to two weeks in order to avoid possible discontinuations symptoms.
Administration: Administer once daily with or without food.

Many of the toxic effects are mediated by stimulation of the 5-HT₂ receptors causing excessive serotonin effect or serotonin syndrome. Serotonin toxicity may develop at therapeutic doses, particularly if another medication that increases CNS serotonin is used concomitantly.
Management of mild to moderate toxicity: Most patients require only supportive care. Control agitation and confusion with either benzodiazepines or serotonin antagonist such as cyproheptadine or chlorpromazine. Manage mild hypotension with IV fluids. Hypertension and tachycardia are generally mild and well tolerated, and do not require specific treatment.
Management of severe toxicity: Early intubation, neuromuscular paralysis, ventilation assistance, and aggressive cooling should be performed if the patient presents with respiratory depression, severe muscle rigidity, and severe hyperthermia. Adequate circulatory support with IV fluids and vasopressors (if needed) should be assured if patient presents with circulatory collapse.
Treat seizures with benzodiazepines; use barbiturates or propofol for recurrent seizures. Patients with wide-complex dysrhythmias should be treated with hypertonic sodium bicarbonate boluses. Although QTc interval prolongation is well described, torsade de pointes is rare. If torsade de pointes occurs, patients should be treated using standard interventions (magnesium sulfate 2 g IV, external or internal cardiac pacing). Because citalopram is lipid-soluble, consider intravenous lipid therapy for patients with ventricular dysrhythmias or hypotension who do not respond to other therapies.

Increased risk of serotonin syndrome with concomitant use with an MAOI, including linezolid or IV methylene blue, or use of escitalopram within 14 days of discontinuing an MAOI used to treat psychiatric disorders, or use of an MAOI used to treat psychiatric disorders within 14 days of discontinuing escitalopram.
Concomitant use of pimozide.
Hypersensitivity to citalopram, escitalopram, or any other component of the product.

Avoid use in older adults with a history of falls or fractures (unless safer alternatives are not available) as ataxia and impaired psychomotor performance may occur. Avoid concomitant use of 3 or more CNS-active agents in any combination due to increased risk of falls. Use caution if prescribed in older adults as SIADH or hyponatremia may occur or be exacerbated. Monitor sodium levels when starting or changing doses.
Use with caution in those with conditions or diseases that alter hemodynamic response.
Hyponatremia, usually the result of SIADH, has occurred, especially in volume-depleted and elderly patients or with concurrent diuretic therapy; discontinue if symptoms develop.
Use with caution in those with conditions or diseases that alter metabolism or hemodynamic responses.
Bleeding events (including life-threatening hemorrhages), have been reported with SSRIs and serotonin norepinephrine reuptake inhibitors; increased risk possible with concomitant use of NSAIDs, aspirin, warfarin, and other anticoagulants.
Dosage adjustment may be necessary in patients with hepatic impairment.
Convulsions have been reported with therapy; use with caution in patients with a history of seizure disorder.
Worsening of angle-closure glaucoma may occur in patients with anatomically narrow angle without a patent iridectomy.
Increased risk of suicidal thoughts and behaviors in pediatric patients and young adults (18 to 24 years old), especially in those with major depressive disorder. Monitoring recommended, especially during the initial few months of therapy and at dosage changes; consider changing therapy or discontinuation if occurs.
Antidepressant therapy may trigger a mixed/manic episode in patients with underlying bipolar disorder; screening recommended.
Life-threatening serotonin syndrome has been reported, often during concurrent use with other serotonergic drugs (ie, triptans, tricyclic antidepressants, fentanyl, lithium, tramadol, buspirone, amphetamines, tryptophan, St John's wort) or drugs than impair the metabolism of serotonin (ie, MAOIs, linezolid, methylene blue); monitoring recommended and discontinue if suspected.
Use with caution in patients with severe renal impairment.
Serious withdrawal symptoms upon abrupt discontinuation have been reported; monitoring and gradual withdrawal are recommended when possible.

Pregnancy: Escitalopram use later in the pregnancy may result in an increased risk for neonatal complications, including persistent pulmonary hypertension of the newborn, which may require prolonged hospitalization, respiratory support, and tube feeding. Weigh the potential benefits of drug treatment against potential risks before prescribing this drug during pregnancy.
Administer escitalopram during pregnancy only if the potential maternal benefit outweighs the potential fetal risk. The decision to treat a pregnant woman with escitalopram should be made on a case by case basis.
Lactation: Evidence and/or expert consensus has demonstrated harmful infant effects when used during breastfeeding. An alternative to this drug should be prescribed or patients should be advised to discontinue breastfeeding.

Common: Dermatologic: Diaphoresis (3% to 8%).
Gastrointestinal: Abdominal pain (2%), Constipation (3% to 6%), Diarrhea (6% to 14%), Indigestion (2% to 6%), Nausea (15% to 18%), Vomiting (up to 3%), Xerostomia (4% to 9%).
Neurologic: Dizziness (4% to 7%), Headache (24%), Insomnia (7% to 14%), Somnolence (4% to 13%).
Reproductive: Disorder of ejaculation (9% to 14%), Erectile dysfunction (3%), Orgasm incapacity (females, 2% to 6%), Reduced libido (3% to 7%).
Other: Fatigue (5% to 8%), Withdrawal symptom (56%).
Serious: Hematologic: Abnormal hemorrhage.
Psychiatric: Worsening depression, Suicidal thoughts, Suicide.
Other: Serotonin syndrome.

Avoid concomitant use of escitalopram with: Bromopride, Citalopram, Dapoxetine, Fexinidazole [INT], Linezolid, Methylene Blue, Monoamine Oxidase Inhibitors (Antidepressant), Pimozide, Rasagiline, Selegiline, Urokinase.
Escitalopram may increase the levels/effects of: Agents with Antiplatelet Properties, Anticoagulants, Antipsychotic Agents, Apixaban, Aripiprazole, Aspirin, Bemiparin, Blood Glucose Lowering Agents, Brexanolone, Cephalothin, Citalopram, Collagenase (Systemic), Dabigatran Etexilate, Deoxycholic Acid, Desmopressin, Domperidone, Doxepin-containing products, Duloxetine, Edoxaban, Enoxaparin, Gilteritinib, Haloperidol, Heparin, Ibritumomab Tiuxetan, Lofexidine, Methylene Blue, Monoamine Oxidase Inhibitors (Antidepressant), Nonsteroidal Anti-Inflammatory Agents (COX-2 selective), Nonsteroidal Anti-Inflammatory Agents (Nonselective), Obinutuzumab, Oxitriptan, Perhexiline, QT-prolonging Kinase inhibitors (Moderate Risk), QT-prolonging Miscellaneous Agents (Moderate Risk), QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk), Rasagiline, Rivaroxaban, Salicylates, Selective Serotonin Reuptake Inhibitors, Selegiline, Serotonergic Non-Opioids CNS Depressants, Serotonin/Norepinephrine Reuptake Inhibitors, Thiazide and Thiazide-Like Diuretics, Thrombolytic Agents, Tricyclic Antidepressants, Urokinase, Vitamin K Antagonists.
The levels/effects of Escitalopram may be increased by: Acalabrutinib, Alcohol (Ethyl), Almotriptan, Alosetron, Amphetamines, Antiemetics (5HT3 Antagonists), Antipsychotic Agents, Bromopride, Bupropion, Buspirone, Cimetidine, Citalopram, CNS Depressants, Cyclobenzaprine, Dapoxetine, Dexmethylphenidate-Methylphenidate, Dextromethorphan, Eletriptan, Ergot Derivatives, Fat Emulsion (Fish Oil Based), Fexinidazole [INT], Glucosamine, Herbs, Anticoagulant/Antiplatelet Properties), Ibrutinib, Inotersen, Lasmiditan, Limaprost, Linezolid, Lofexidine, Lorcaserin, Metaxalone, Metoclopramide, Metyrosine, Multivitamins/Fluoride (with ADE), Multivitamins/Minerals (with ADEK, Folate, Iron), Multivitamins/Minerals (with AE, No Iron), Nefazodone, Nonsteroidal Anti-Inflammatory Agents (Topical), Omega-3 Fatty Acids, Omeprazole, Ondansetron, Opioid Agonists, Pentamidine (systemic), Pentosan Polysulfate Sodium, Pentoxifylline, Pimozide, Prostacyclin Analogues, QT-prolonging Agents (Highest Risk), QT-prolonging Antipsychotics (Moderate Risk), QT-prolonging Class IC Antiarrhythmics (Moderate Risk), QT-Prolonging Quinolones Antibiotics (Moderate Risk), QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk), Ramosetron, Safinamide, Serotonergic Agents (High Risk Miscellaneous), Serotonergic Opioids (High Risk), Serotonin 5-HT1D Receptor Agonists (Triptans), St. John's Wort, Syrian Rue, Tipranavir, Tramadol, Tricyclic Antidepressants, Vitamin E (Systemic), Vortioxetine, Zanubrutinib.
Escitalopram may decrease the levels/effects of: Ioflupane I 123, Simeprevir, Thyroid Products.
The levels/effects of Escitalopram may be decreased by: Bosentan, CYP2C19 Inducers (Moderate), CYP2C19 Inducers (Strong), CYP3A4 Inducers (Moderate), CYP3A4 Inducers (Strong), Cyproheptadine, Dabrafenib, Deferasirox, Enzalutamide, Erdafitinib, Gilteritinib, Lorlatinib, Mitotane, Nonsteroidal Anti-Inflammatory Agents (COX-2 selective), Nonsteroidal Anti-Inflammatory Agents (Nonselective), Sarilumab, Siltuximab, St. John's Wort, Tocilizumab.

Store below 30°C.

Antidepressants

N06AB10 - escitalopram ; Belongs to the class of selective serotonin reuptake inhibitors. Used in the management of depression.

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