Escitalopram - Uses, Dosage, Side Effects, Drug Warnings, and Precautions

Overview:

Escitalopram or Escitalopram Oxalate is the generic name of the prescription medicine Lexapro. It is available in the form of oral tablets and liquid forms. It is used to treat and manage the symptoms of depression in adults, teenagers, and children above 12 years of age. It is also used in the treatment of generalized anxiety disorder (GAD) in adults.

Escitalopram, an SSRI (selective serotonin reuptake inhibitor), is the S-enantiomer of racemic Citalopram and is used to treat anxiety and depression. Escitalopram is estimated to be 150 times more potent than Citalopram's R-enantiomer and is largely responsible for Citalopram's clinical activity. Escitalopram differs from other SSRIs by exerting an allosteric effect on its target; this may be the explanation behind its observed higher potency and quicker start than other SSRIs.

Escitalopram can cause suicidal tendencies and thoughts when used in children (above 12 years), teenagers, and young adults (24 years of age and below) to treat psychiatric disorders. Even in the initial days of Escitalopram or while your treating physician increases or decreases its doses in the middle of treatment for improved effects, it can make you suicidal (attempt, plan, or think about killing oneself) even if you are an adult above 24 years of age.

Discuss with your doctor the benefits and potential risks of getting you or your child treated with Escitalopram.

Drug Group:

Escitalopram is chiefly used to treat mental health disorders and belongs to the group of medications called antidepressants. Among the antidepressants, they belong to a class of drugs called selective serotonin reuptake inhibitors (SSRIs). All SSRI antidepressants work similarly to treat depression, anxiety disorders, and other psychological conditions. Other similar SSRI antidepressants are Citalopram, Sertraline, Fluoxetine, Paroxetine, Fluvoxamine, and Vilazodone.

What Is Escitalopram Used For?

Escitalopram is used to treat the following mental health disorders or psychological conditions:

• Major Depressive Disorder- Escitalopram is recommended for the acute and ongoing management of severe depressive disorder in adults and 12 to 17-year-old adolescents. A significant and prolonged depressive episode lasting for at least a period of two weeks is what is referred to as a major depressive episode. The existence of at least five of the following nine symptoms mentioned below concludes the presence of major depressive disorder:

  • Depressed mood.

  • Disinterest in routine tasks.

  • Considerable weight and/or hunger change.

  • Insomnia or hypersomnia.

  • Motor symptoms, agitation, or retardation.

  • Increased exhaustion, guilt, or worthlessness.

  • Sluggish thinking or attention deficit disorder.

  • Suicide attempt or suicidal thoughts.

  • Overwhelming anxiety.

• Generalized Anxiety Disorder- Generalized anxiety disorder or GAD in individuals is advised to be treated acutely with Escitalopram. Excessive worry and anxiety (apprehensive expectancy) that lasts for at least six months and is challenging to regulate are symptoms of generalized anxiety disorder. It must also be accompanied by at least three of the following signs or symptoms: irritability, muscle tension, sleep problems, a feeling of being on edge, restlessness, or being tired quickly.

Its off-label uses include:

• Obsessive-compulsive disorder (OCD).

• Insomnia.

• Vasomotor symptoms associated with menopause.

• Social anxiety disorder (SAD).

• Panic disorders with or without agoraphobia.

• Posttraumatic stress disorder (PTSD).

• Premenstrual dysphoric disorder.

Note: The safety and efficacy of Escitalopram are not known in children below 12 years of age and are contraindicated in the pediatric population. Also, SSRIs induce suicidal tendencies and thoughts in children, adolescents, and young adults. It can also switch your depression into mania. Seek medical assistance if you experience any worsening symptoms of your or your child’s condition.

Do not abruptly stop taking medicine without your physician’s consent. It can lead to withdrawal symptoms. If you feel like quitting the drug, talk to your doctor for alternative treatment or get your dose tapered gradually.

For Patients:

What Is Anxiety?

A sensation of worry, dread, and unease is known as anxiety. One can start to perspire, become agitated and anxious, and experience a rapid heartbeat. It can be a typical response to stress. One might have anxiety, for instance, when confronted with a challenging job, before attempting a test, or before making a crucial decision. It may enable you to manage. You might feel more energized or able to concentrate if you are anxious. But for some with anxiety disorders, the terror can be incapacitating and last for a long time.

What Is Depression?

Major depressive disorder, sometimes known as depression, is a serious medical condition that frequently affects people's feelings, thoughts, and behaviors. Thankfully, it is also curable. Sadness or a decline in interest in previous hobbies are symptoms of depression. It can impair the ability to perform at work and at home and cause a number of mental and physical issues.

What Are the Common Symptoms of Anxiety and Depression?

• Thoughts and social settings make an individual anxious.

• Having certain phobias.

• Rapid heartbeat.

• Restlessness.

• Dizziness.

• Shortness of breath.

• Feeling sad.

• A change in appetite.

• Loss of energy and fatigue.

• Difficulty in making decisions.

• Suicidal thoughts and

How Does Escitalopram Work?

Escitalopram is a selective serotonin reuptake inhibitor (SSRI) and is the most demanding of SSRIs. As their name suggests, they selectively inhibit serotonin’s reuptake, thereby increasing serotonin activity. The sodium-dependent serotonin transporter protein in the presynaptic neuron reuptakes serotonin from the synaptic cleft to the presynaptic neuron. Escitalopram binds to this sodium-dependent serotonin transporter protein, thereby preventing the reuptake of serotonin from the synaptic cleft, potentiating the effect of serotonin in the central nervous system.

Onset Of Action: Following the oral administration, 80% of Escitalopram reaches the circulation. It is almost completely absorbed. Nearly 8% of orally administered is excreted through the urine in its unchanged form, and 10% is passed through the urine in its metabolite form. Food does not affect Escitalopram’s absorbability, and peak levels of Escitalopram reach about 5 hours after its oral intake.

Habit-Forming: No habit-forming tendencies were observed in people taking Escitalopram. It does not cause addiction.

Expiry Date: Do not take Escitalopram or any other medicine past its expiry date. You can find one printed on the strip, back of the pack, or in the leaflet.

What is the Dosage of Escitalopram?

To treat mental health disorders, your treating doctor will typically start with 10 mg or minimal dosage based on your symptoms. After a week, your dosage might be increased to achieve beneficial effects. You will be periodically assessed by your doctor to monitor your symptom betterment and based on which your dosages will be adjusted to maintain the lowest possible effective dose. Escitalopram is available in oral tablets of strengths 5 mg, 10 mg, 20 mg, and 1mg/mL oral solution.

Escitalopram is suggested in children above 12 years of age only in case of major depressive disorders. Caregivers or parents of such adolescents must be watchful of their activities as Escitalopram can induce suicidal thoughts.

In older adults above 60 years of age, only 10 mg per day dosage is recommended. If you have any kidney or liver diseases, your dose will be adjusted accordingly.

If you plan to switch from antidepressants of monoamine oxidase inhibitors (MAOI) to Escitalopram or other medicines of the SSRI group, at least 14 days should elapse between stopping MAOI antidepressant and starting Escitalopram.

How to Use Escitalopram?

Escitalopram can be taken with or without food in the morning or evening as advised by your doctor. It is usually prescribed in a once-daily dosage only. Take it at the same time every day. Do not take it in larger or smaller quantities than prescribed. Continue taking Escitalopram even if you feel better. Do not abruptly stop taking it as it might cause withdrawal symptoms like irritability, sweating, confusion, headache, mood changes, agitation, tiredness, sleeping difficulties, etc.

Missed Dose:

If you forgot to take a dose of Escitalopram, take it as soon as you remember. If it is almost the time for the next dose, skip the missed dose and continue with the consecutive dose. Do not double up your next dose to compensate for the missed one.

What Are the Drug Warnings and Precautions?

1. Allergy - If you are allergic or hypersensitive to Escitalopram or Citalopram, do not take it.

2. Monoamine Oxidase Inhibitors (MAOIs) and Pimozide - Concomitant use in people taking MAOIs or Pimozide is contraindicated. If there is a need for a drug switch between MAOIs and Escitalopram (SSRIs), there should be a gap of at least 14 days between the last dose of MAOI and the first dose of SSRI and vice versa.

3. Suicidal Intentions - Suicidal intentions and ideations tend to occur during the initial months of treatment initiation or with dosage modifications (increase or decrease). Hence, close monitoring of the person taking antidepressants is necessary.

4. Drug Discontinuation - Escitalopram should not be abruptly stopped. Stopping so can lead to withdrawal symptoms. If you feel like your symptoms are worsening and feel like stopping them, consult your doctor. Your dosage will be tapered, and gradually you can stop it with your doctor’s consent.

5. Pregnancy - There are no adequate studies on the effects of Escitalopram in the growing fetus. Hence, if you are pregnant, you can only take Escitalopram if the potential benefits and risks are assessed.

6. Breastfeeding - Escitalopram is excreted in breast milk. Hence if you are a nursing mother, Escitalopram will be prescribed only if you clearly need it. Either you will have to discontinue breastfeeding temporarily, or your kid should be closely monitored for any adverse effects.

7. Kidney and Liver Impairment - Inform your doctor if you have any kidney or liver impairment. Your dosage will be adjusted. Use with caution.

8. Pediatric Use - Escitalopram is contraindicated in children below 12 years of age, and for teenagers of 12 to 18 years, Escitalopram is only used to treat major depressive disorders.

9. Seizures - If you have seizures, inform them in advance. Escitalopram should be used in caution in people with seizures. It can induce seizures in susceptible individuals.

10. Bleeding - Escitalopram can increase the risk of bleeding events like gastric bleeding, ecchymosis (a skin darkening brought on by bleeding beneath that is generally brought on by bruises), epistaxis (nose bleeding), hematomas (collection of blood outside the arteries), and serious bleeding conditions. Hence, concomitant use of Escitalopram with non-steroidal anti-inflammatory drugs (NSAIDs) or anticoagulants must be done cautiously.

11. Angle-Closure Glaucoma - If you have a history of glaucoma or have narrow angles without a patent iridectomy, Escitalopram can trigger glaucoma.

12. Serotonin Syndrome - Taking Escitalopram with serotonergic drugs like Tramadol, Lithium, Buspirone, Serotonin and norepinephrine reuptake inhibitors (SNRIs), MAOIs, Opioids, Cocaine, Ginseng, St.John’s Wort, etc., can raise the serotonin levels. Such extreme levels cause adverse health effects like agitation, nausea, headache, restlessness, vomiting, diarrhea, rapid heart rate, sweating, confusion, etc. If untreated it can lead to seizures, troubled breathing, coma, and eventually death.

What Are the Side Effects of Escitalopram?

The common side effects of Escitalopram include,

• Dry mouth.

• Nausea.

• Diarrhea.

• Constipation.

• Weight loss.

• Tiredness.

• Loss of appetite.

• Sexual dysfunction.

• Stomach pain.

• Heartburn.

• Drowsiness.

• Priapism.

Minor and common side effects subside with time or with drug discontinuation and do not cause any major health concerns.

Some of the serious side effects of Escitalopram include,

• Seizures.

• Hallucination.

• Bleeding.

• Altered moods (overexcitation).

• Loss of coordination.

• Allergic reactions.

• Fever.

• Itching.

• Rash.

• Decreased urine output.

• Rapid heartbeat.

• Confusion.

If you experience any of the above side effects or other adverse reaction not listed above and does not go away on its own, immediately call your doctor to seek medical assistance.

What Are the Interactions of Escitalopram?

Like with most drugs, Escitalopram also interacts with certain medications and disease conditions to create undesirable effects. However, this differs with people. The common interactions of Escitalopram are,

1. With Medicines:

• Ketoconazole.

• Monoamine oxidase inhibitors.

• Lithium.

• Digoxin.

• Sumatriptan.

• Linezolid.

• Cimetidine.

• Metoprolol.

• Pimozide.

• Theophylline.

• Warfarin.

• Carbamazepine.

• Anticoagulants.

• NSAIDs.

• Diuretics.

• Sulfonylureas.

• With Supplements:

• St.John’s Wort.

• Ginseng.

2. With Alcohol:

• Consuming alcohol along with Escitalopram increases the risk of its pronounced side effects like drowsiness and is not recommended.

3. With Disease:

• Seizures.
• Depression - Symptoms of depression can worsen at any time. Close monitoring is required.
• Heart problems (myocardial infarction and unstable heart disease).
• Bleeding disorders.

For Doctors:

Chemical Taxonomy of the Drug:

Pharmacodynamics:

Escitalopram is an SSRI (selective serotonin reuptake inhibitor) with little effect on dopamine neuronal or norepinephrine reuptake, according to animal experiments conducted in vitro and in vivo. Regarding the suppression of 5-HT reuptake and the inhibition of 5-HT neuronal firing rate, Escitalopram is at least 100 times more powerful than the R-enantiomer.

Alpha- and beta-adrenergic, histamine (H1-3), dopamine (D1-5), muscarinic (M1-5), and Benzodiazepine receptors are among the additional receptors for which Escitalopram has no or very little affinity. Additionally, Escitalopram has a poor affinity for or does not bind to a number of ion channels, such as the Na+, K+, Cl-, and Ca++ channels. It has been proposed that a number of anticholinergic, sedative, and cardiovascular adverse effects of other psychiatric medications are related to antagonizing histaminergic, muscarinic, and adrenergic receptors.

Pharmacokinetics:

Escitalopram undergoes primarily hepatic biotransformation, with a mean terminal half-life of about 27 to 32 hours. It takes about a week to reach a steady state of plasma concentrations with a once-daily dosage. Escitalopram was accumulating in young, healthy patients' plasma to the extent that it was 2.2 to 2.5 times more than the plasma concentrations seen after a single dosage at a steady state. Escitalopram oxalate is available in both tablet and oral solution dosage forms that are bioequivalent.

Mechanism of Action:

Escitalopram, the S-enantiomer of racemic Citalopram, is thought to work as an antidepressant by potentiating serotonergic activity in the central nervous system (CNS) by inhibiting serotonin reuptake by CNS (central nervous system) neurons. Similar to other selective serotonin reuptake inhibitors, Escitalopram increases serotonergic activity by interacting with the orthosteric, which is a primary binding site on the serotonin transporter (SERT), which is also the site where endogenous 5-HT binds. This interaction prevents serotonin from being re-uptaken into the presynaptic neuron. Escitalopram is regarded as an allosteric serotonin reuptake inhibitor because, like Paroxetine, it binds to a secondary allosteric location on the SERT molecule to more potently inhibit 5-HT reuptake. In comparison to other SSRIs, it has higher extracellular 5-HT levels, a quicker time to effect, and greater efficacy due to the combination of allosteric and orthosteric activity on SERT. Escitalopram's weak activity at a variety of off-target receptors, including muscarinic and histamine receptors, may help to explain some of its negative effects. Escitalopram has demonstrated low to no binding affinity at a number of additional receptors.

Metabolism and Elimination:

Following oral Escitalopram administrations, roughly eight percent and ten percent, respectively, of the medication is recovered in the urine as Escitalopram and S-desmethylcitalopram (S-DCT). Escitalopram has an oral clearance of 600 mL/min, with renal clearance accounting for about seven percent of it. The metabolites of Escitalopram are S-DCT and S-desmethylcitalopram (S-DDCT). Escitalopram, unmodified, makes up the majority of the plasma in humans. The plasma concentration of the Escitalopram metabolite S-DCT is roughly one-third that of Escitalopram in a steady state. In most patients, the level of S-DDCT was undetectable. Studies conducted in vitro reveal that Escitalopram is at least seven and 27 times more effective than S-DCT and S-DDCT, respectively, at inhibiting serotonin reuptake, indicating that Escitalopram's metabolites do not significantly contribute to the drug's antidepressant effects.

Non-clinical Toxicology:

Carcinogenesis:

For 18 and 24 months, respectively, the drug was ingested by mice and rats in a clinical research setting. In mice who were getting up to 240 mg/kg/day of the drug, there was no evidence of carcinogenicity. In rats getting 8 or 24 mg/kg/day of the drug, there was an increased incidence of small intestinal cancer. This result does not have a known no-effect dose. The unknown is how these findings apply to people.

Mutagenesis:

The drug was mutagenic in the absence of metabolic activation in the in vitro bacterial reverse mutation experiment in two of five bacterial strains. In both the presence and absence of metabolic activity, it was clastogenic for chromosomal abnormalities. In vitro tests showed that the drug was not mutagenic in a combination of in vitro and in vivo unscheduled DNA (deoxyribonucleic acid) synthesis assay in rat liver or the mammalian forward gene mutation assay in mouse lymphoma cells. In the in vitro chromosomal aberration experiment using human cells, it was not clastogenic.

Impairment in Fertility:

16 male and 24 female rats were given the drug orally at dosages of 32, 48, and 72 mg/kg/day before, during, and after mating and gestation. Mating was reduced at all levels, and fertility was reduced at doses below 32 mg/kg/day. The increased gestational length was achieved at 48 mg/kg/day.

Interactions With Other Drugs:

Escitalopram and Rasagiline together should not be used due to the possibility of serotonin syndrome. SSRIs, such as Escitalopram, impair platelet function; bleeding risk rises when used together with antiplatelet drugs. Low molecular weight Heparin (LWMH) administration increases the likelihood of bleeding. When Escitalopram is taken with NSAIDs, the risk of bleeding also rises. When taken with non-steroidal anti-inflammatory drugs (NSAIDs), SSRI (selective serotonin reuptake inhibitors) may raise the chance of UGIB (upper gastrointestinal bleeding).

According to a study, after an acute myocardial infarction, patients who received an SSRI together with Aspirin or dual antiplatelet treatment (DAPT) had a higher risk of bleeding.

When Escitalopram is used with medications like Amiodarone, which can lengthen QTc intervals, there is an increased risk of QT prolongation, especially in people with chronic kidney disease.

Dosage and Administration:

The dosage of this medication will vary depending on the patient. Observe the doctor's instructions or the label's instructions. Unless the doctor instructs the patient to, do not alter the dose if it differs from the recommended one. The potency of the medication determines how much of it one should take. Additionally, the medical condition for which the individual is utilizing the medication affects the number of doses they take per day, the interval between doses, and the duration of treatment.

For Pills or Solutions Used as Oral Dose Forms:

To Treat Depression:

Both adults and kids, for those who are 12 years old or above, must take 10 mg once daily, either in the morning or in the evening. If necessary, their doctor might change the dose. The dosage is typically no greater than 20 mg per day, though.

• Elderly Adults: 10 mg once daily, in the morning or the evening.

• Children Under the Age of 12: The doctor must determine the use and dosage.

In the Case of Generalized Anxiety Disorder:

• Adults - At the beginning, use 10 mg once a day, in the morning or the evening. If necessary, the doctor might change the dose. The dosage is typically no greater than 20 mg per day, though.

• Children - The doctor should determine the use and dosage.

Conclusion:

Never share Escitalopram or any medicine with anyone whose conditions appear similar to you. Avoid self-medication and do not start or stop taking any drug without a doctor’s consent.