Zespra Cap(Escitalopram)20 Mg, 2×7’s-Potential Overview

Generic Information

• Brand Name: Zespra Cap
• Generic Name: Escitalopram
• Strength: 20 mg per capsule, pack of 14 (2×7’s)
• Pharmaceutical Class:
  • Class: Selective Serotonin Reuptake Inhibitor (SSRI)
  • Type: Antidepressant

Indications for Use

Escitalopram is primarily used for the treatment of mood disorders, including:

1. Major Depressive Disorder (MDD):
   • Treatment of moderate to severe depression in adults and adolescents (12 years and older).
2. Generalized Anxiety Disorder (GAD):
   • Treatment of excessive worry and anxiety.
3. Panic Disorder:
   • Treatment of panic attacks with or without agoraphobia.
4. Social Anxiety Disorder:
   • Management of symptoms of social phobia in adults and children aged 7 and above.

Common Side Effects

• Nausea
• Dry mouth
• Drowsiness or insomnia
• Increased sweating
• Fatigue
• Dizziness
• Sexual dysfunction (reduced libido, difficulty achieving orgasm)
• Weight gain or loss

Serious Side Effects (Less Common)

• Cardiovascular:
  • QT interval prolongation, which may lead to arrhythmias, including torsades de pointes.
• Neurological:
  • Serotonin syndrome (symptoms include confusion, hallucination, seizure, extreme changes in blood pressure, and fever).
• Hematologic:
  • Low blood sodium (hyponatremia), particularly in the elderly.
• Psychiatric:
  • Suicidal thoughts or behaviors, especially during the early stages of treatment.
• Hepatic:
  • Liver damage or dysfunction, with elevated liver enzymes.
• Allergic Reactions:
  • Rash, itching, swelling (especially of the face or throat), which may indicate an allergic reaction.

Dosage and Usage Instructions

1. For Depression and Anxiety (Adults):
   • Starting dose: 10 mg once daily.
   • Maintenance dose: 10 to 20 mg daily (depending on patient response).
2. For Panic Disorder (Adults):
   • Starting dose: 10 mg daily, increased to 20 mg if needed.
3. For Children (7-17 years) with Anxiety and Depression:
   • Starting dose: 10 mg daily.
   • Maximum dose: 20 mg daily.

Usage Instructions:

• Escitalopram can be taken with or without food.
• It should be taken at the same time each day to help remember.
• If you miss a dose, take it as soon as you remember, unless it’s almost time for the next dose. Do not take two doses at once.
• It may take 1-4 weeks to notice improvements in mood or anxiety.

Drug Interactions

• With Food:
  • No specific food interactions. It can be taken with or without food.
• With Other Medications:
  • Monoamine Oxidase Inhibitors (MAOIs): Serious, potentially life-threatening reactions can occur if taken with MAOIs. At least 14 days should be allowed between stopping MAOIs and starting escitalopram.
  • Other SSRIs/SNRIs: Increased risk of serotonin syndrome. Combining with other SSRIs or SNRIs is not recommended.
  • Anticoagulants (e.g., warfarin): Escitalopram may increase the risk of bleeding, especially when combined with anticoagulants or antiplatelet drugs.
  • CYP2C19 Inhibitors (e.g., omeprazole): Escitalopram is metabolized by CYP2C19. Inhibitors of this enzyme may increase escitalopram blood levels.
  • Tricyclic Antidepressants (TCAs) and Lithium: Increased risk of serotonin syndrome and side effects.
• Other Interactions:
  • Alcohol: Caution is advised when drinking alcohol while on escitalopram as it may increase sedation or dizziness.
  • St. John’s Wort: May reduce the effectiveness of escitalopram.

Regulatory Approval and Manufacturer

• Regulatory Approval:
  • Escitalopram is approved by the U.S. Food and Drug Administration (FDA) for the treatment of depression, anxiety, panic disorder, and social anxiety disorder. It is also approved by other regulatory agencies globally for similar indications.
• Manufacturer:
  • Manufactured by various pharmaceutical companies, depending on the region. It is marketed by major companies like Lundbeck and Forest Laboratories (now part of Allergan).

Pharmacist-Related Data

Drug Name and Chemical Details

• Generic Name: Escitalopram
• Chemical Formula: C20H21FN2O
• Molecular Weight: 324.4 g/mol

Pharmacodynamics

1. Mechanism of Action:
   • Escitalopram is a selective serotonin reuptake inhibitor (SSRI) that works by increasing the levels of serotonin (a neurotransmitter) in the brain. It does this by blocking the reuptake of serotonin into the presynaptic neuron, thus enhancing serotonin’s activity in the synaptic cleft.
   • This action helps alleviate symptoms of depression, anxiety, and other mood disorders.
2. Therapeutic Effects:
   • Escitalopram is used to treat depression, generalized anxiety disorder (GAD), panic disorder, and social anxiety disorder.
   • It helps improve mood, reduce anxiety, and increase the ability to enjoy daily activities by restoring the balance of serotonin in the brain.

Pharmacokinetics

1. Absorption:
   • Escitalopram is well absorbed following oral administration, with peak plasma concentrations occurring within 4-6 hours.
   • The bioavailability is approximately 80%, and it is not significantly affected by food intake.
2. Distribution:
   • Escitalopram is widely distributed throughout the body, with a volume of distribution of about 12 L/kg.
   • It is about 56% protein-bound in plasma.
3. Metabolism:
   • Escitalopram is primarily metabolized in the liver by the cytochrome P450 (CYP) enzyme system, primarily by CYP2C19, CYP3A4, and CYP2D6.
   • The major metabolite, S-demethylescitalopram, has weak pharmacological activity.
4. Excretion:
   • The drug and its metabolites are primarily excreted in the urine (about 8% unchanged) and to a lesser extent in the feces.
5. Half-Life:
   • The elimination half-life of escitalopram is approximately 27-32 hours, allowing for once-daily dosing.

Drug Interactions

1. With Food:
   • No known significant interactions with food, so escitalopram can be taken with or without food.
2. With Other Medications:
   • Monoamine Oxidase Inhibitors (MAOIs): Concurrent use is contraindicated due to the risk of serotonin syndrome. At least 14 days should elapse before switching between an MAOI and escitalopram.
   • CYP2C19 Inhibitors: Escitalopram’s metabolism may be slowed when taken with CYP2C19 inhibitors (e.g., omeprazole), leading to increased drug levels.
   • Anticoagulants: Increased risk of bleeding when combined with anticoagulants such as warfarin or aspirin.
3. Other Interactions:
   • Alcohol: Alcohol should be avoided or used cautiously, as it may increase sedative effects.
   • St. John’s Wort: Can lower the effectiveness of escitalopram.

Clinical Considerations

1. Pregnancy Category:
   • FDA Category C: Animal studies have shown adverse effects, and there are no well-controlled studies in pregnant women. Escitalopram should only be used during pregnancy if the potential benefits outweigh the risks.
2. Lactation:
   • Escitalopram is excreted in breast milk in small amounts. It should be used with caution during breastfeeding, and the infant should be monitored for potential adverse effects, including sedation and weight gain.
3. Pediatric Use:
   • The safety and efficacy of escitalopram for the treatment of major depressive disorder in children under 12 years have not been established. It is approved for use in children aged 12 and older for depression and anxiety disorders.
4. Geriatric Use:
   • In elderly patients, escitalopram should be started at lower doses due to the potential for decreased liver function and increased sensitivity to the drug. Regular monitoring is advised.
5. Other Considerations:
   • Caution should be exercised in patients with a history of seizures, as SSRIs can lower the seizure threshold.
   • Escitalopram should be used cautiously in patients with liver impairment, and dosage adjustments may be required.