Escitalopram is the active S-stereoisomer of the selective serotonin reuptake inhibitor (SSRI) citalopram with an antidepressant, anti-obsessive-compulsive and antibulimic properties. Escitalopram inhibits the reuptake of the neurotransmitter serotonin (5-HT) at the serotonin reuptake pump of the neuronal membrane of the presynaptic cell, thereby increasing levels of 5-HT within the synaptic cleft and enhancing the actions of serotonin on 5HT1A autoreceptors. Unlike other SSRIs, escitalopram appears to not only bind to a primary high-affinity site on the serotonin transporter protein but also to a secondary lower-affinity allosteric site that is considered to stabilize and prolong drug binding.
Escitalopram is an antidepressant which belongs to the ‘SSRI’ group (selective serotonin reuptake inhibitors). These medicines act on the serotonin system in the brain by increasing the serotonin level. Disturbances in the serotonin-system are considered an important factor in the development of depression
Mechanism of Action of Escitalopram
The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Escitalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs. Escitalopram has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of escitalopram was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of the major depressive disorder. Escitalopram does not inhibit monoamine oxidase.
Indications of Escitalopram
- Major Depressive Disorder
- Borderline Personality Disorder
- Depression
- Bipolar Disorder
- Fibromyalgia
- Anxiety and Stress
- Depression
- Bipolar Disorder
- Postpartum Depression
- Agitation
- Borderline Personality Disorder
- Generalized Anxiety Disorder
- Neuralgia
- Anorexia Nervosa (AN)
- Bulimia Nervosa (BN)
- Diabetic Neuropathies
- Major Depressive Disorder (MDD)
- Obsessive Compulsive Disorder (OCD)
- Panic Disorders
- Post-Traumatic Stress Disorder (PTSD)
- Premature Ejaculation
- Premenstrual Dysphoric Disorder
- Social Anxiety Disorder (SAD)
- Obsessive Compulsive Disorder
- Panic Disorder
- Irritable Bowel Syndrome
- Somatoform Pain Disorder
- Labeled indications include major depressive disorder (MDD) and generalized anxiety disorder (GAD). Unlabeled indications include treatment of mild dementia-associated agitation in nonpsychotic patients.
Contra-Indications of Escitalopram
- Syndrome of Inappropriate Antidiuretic Hormone Secretion
- Low amount of magnesium in the blood
- Low amount of sodium in the blood
- Low amount of potassium in the blood
- Increased risk of bleeding
- Behaving with Excessive Cheerfulness and Activity
- Mild Degree of Mania
- Manic-Depression
- Having Thoughts of Suicide
- Neuroleptic Malignant Syndrome
- Serotonin syndrome – adverse drug interaction
- Closed-angle glaucoma
- Heart attack within the last 30 days
- Very Rapid Heartbeat – Torsades de Pointes
- Prolonged QT interval on EKG
- Heart Disease
- Abnormal EKG with QT changes from Birth
- Liver problems
- Bleeding from Stomach
- Esophagus or Duodenum
- Severe renal impairment
- Seizures
- Risk of angle-closure glaucoma due to narrow-angle of the anterior chamber of the eye
Dosages of Escitalopram
Strengths
Tablet :5mg ,10mg, 20mg
Oral solution
- 5mg/5mL
Anxiety Disorder
- Initial dose: 10 mg orally once a day; increase if necessary after at least 1 week of treatment to 20 mg once a day
- Maintenance dose: 10 to 20 mg orally once a day
- Maximum dose: 20 mg orally once a day
Depression
- Initial dose: 10 mg orally once a day; increase if necessary after at least 1 week of treatment to 20 mg once a day
- Maintenance dose: 10 to 20 mg orally once a day
- Maximum dose: 20 mg orally once a day.
Pediatric Dose for Depression
12 years and older
- Initial dose: 10 mg orally once a day; increase if necessary after at least 3 weeks of treatment to 20 mg once a day
- Maintenance dose: 10 to 20 mg orally once a day
- Maximum dose: 20 mg orally once a day
Major Depressive Disorder
- 10 mg bit/Day; may increase to 20 mg/day after 1 week
Generalized Anxiety Disorder
- 10 mg bit/Day; may increase to 20 mg/day after 1 week; maintain at the lowest effective dose and assess the need of therapy periodically if extended therapy required
Obsessive-Compulsive Disorder (Off-label)
- 10 mg bit/Day; may increase to 20 mg/day after 1 week; maintain at the lowest effective dose and assess the need of therapy periodically if extended therapy required
Insomnia (Off-label)
- Secondary to Depression: 5-20 mg PO over 8 week period
- Secondary to panic disorder in women: 5-10 mg PO over 8 week period
Vasomotor Symptoms Associated with Menopause (Off-label)
- 10 mg bit/Day; may increase to 20 mg PO qDay after 4 weeks if symptoms not adequately controlled
Side Effects of Escitalopram
The most common
- Constipation
- decreased interest in sexual intercourse
- sleepiness or unusual drowsiness
- clumsiness or unsteadiness
- dizziness
- drowsiness
- dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
- a light-headed feeling, like you, might pass out;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- A headache.
- Skin rashes.
- Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Serious
- agitation
- anxiety
- behavioral changes, including aggressiveness, angry outbursts, bizarre behavior, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- sleepwalking
Drug Interactions of Escitalopram
Escitalopram may interact with following drugs, supplements & may change the efficacy of drugs
- general anesthetics
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- aripiprazole
- baclofen
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- bupropion
- celecoxib
- cilostazol
- clopidogrel
- cyclosporine
- diabetes medications (e.g., chlorpropamide, metformin, nateglinide, rosiglitazone)
- diltiazem
- estrogens (e.g., conjugated estrogen, )
- glucosamine
- heparin
- low molecular weight heparins
- mirtazapine
- monoamine oxidase inhibitors (MAOIs; e.g. rasagiline, selegiline, )
- multivitamins
- muscle relaxants
- nifedipine
- non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, naproxen)
- omega-3 fatty acids
- pentoxifylline
- propranolol
- quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
- rasagiline
- seizure medications ( phenobarbital, phenytoin, valproic acid, )
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
- tapentadol
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- thiazide diuretics (water pills; e.g., hydrochlorothiazide, )
- thyroid replacements (e.g., desiccated thyroid, levothyroxine)
- tizanidine
- tramadol
- tricyclic antidepressants (e.g., desipramine, nortriptyline)
- triptans (e.g., sumatriptan, rizatriptan)
This medication may interfere with certain medical/laboratory tests (including a brain scan for Parkinson’s disease), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
Pregnancy & Lactation of Escitalopram
FDA Pregnancy Category C
Pregnancy
If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.
Make sure your midwife and/or doctor know you are on Escitalopram. When taken during pregnancy, particularly in the last 3 months of pregnancy, medicines like Escitalopram may increase the risk of a serious condition in babies, called persistent pulmonary hypertension of the new born (PPHN), making the baby breathe faster and appear bluish. These symptoms usually begin during the first 24 hours after the baby is born. If this happens to your baby you should contact your midwife and/or doctor immediately.
If you take Escitalopram during the last 3 months of your pregnancy you should be aware that the following effects may be seen in your newborn baby: trouble with breathing, blue-ish skin, fits, body temperature changes, feeding difficulties, vomiting, low blood sugar, stiff or floppy muscles, vivid reflexes, tremor, jitteriness, irritability, lethargy, constant crying, sleepiness and sleeping difficulties. If your newborn baby has any of these symptoms, please contact your doctor immediately.
Lactation
Do not take Escitalopram if you are breastfeeding unless you and your doctor have discussed the risks and benefits involved.
Pregnant or breastfeeding women should take it only if the drug’s potential benefits outweigh its risks. It is safe for adults and for adolescents/teens 12 to 17 years old. Children younger than 12 should not take.
References
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