Esketamine
Esketamine Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Esketamine is a brand name. Its generic name is Esketamine.
Esketamine
Esketamine is a novel psychotropic drug used in the treatment of mental health disorders, including depression, bipolar disorder, and schizophrenia. It is the S-enantiomer of ketamine, which has long been used as a rapid-acting anesthetic. Esketamine is also known by its trade name, Spravato, and has been approved by the FDA for use in patients with treatment-resistant depression and suicidal ideation.
Uses for Esketamine
Esketamine is primarily used to treat treatment-resistant depression (TRD). It is an alternative therapy for individuals who have failed to respond to traditional antidepressant medications, such as SSRIs and SNRIs. TRD is a moderate to severe form of depression that doesn’t respond to first or even second line treatments. A person who experiences a major depressive episode lasting more than 8-12 months without relief is often diagnosed with treatment-resistant depression.
Mechanism of Action
The exact mechanism of action of esketamine is not fully understood. It is thought to work by acting on certain glutamate receptors in the brain, increasing the level of the neurotransmitter glutamate which helps with communication throughout the brain. Unlike traditional antidepressants, ketamine-derived medications act quickly and reach peak potency in the first 24 hours of administration.
How Long Does It Take to Work?
The effects of esketamine can start to be felt shortly after administration, with some people experiencing improvements in mood and other symptoms in two to five hours. Improvements can continue to be seen after repeated doses and prolonged treatment.
Absorption
Esketamine is rapidly absorbed after intravenous administration; levels peak 30-45 minutes after administration. Esketamine nasal spray also has a rapid onset of action, usually within 10-30 minutes of administration.
Route of Elimination
Esketamine is rapidly eliminated from the body after administration; most of the drug is excreted in the urine as the acid metabolite esketamine-hydrochloride. The half-life of esketamine is approximately four hours.
Dosage
The recommended dose of esketamine is 56mg twice-weekly, administered as a 20-30 minute intravenous infusion over 10-15 minutes. The same dose is also available as a nasal spray, which is used once-weekly in addition to the twice-weekly intravenous infusion. The dose should be individualized to each patient.
Administration
Esketamine can be administered as an intravenous infusion or as a nasal spray. The intravenous infusion is administered as two 0.45ml/kg doses over 10-15 minutes, administered twice-weekly. The nasal spray is administered as a single 56mg dose once-weekly in addition to the twice-weekly intravenous infusion.
Side Effects
The most common side effects of esketamine are dizziness, drowsiness, sedation, nausea, increased blood pressure, blurred vision, vertigo, confusion, and altered taste. Long-term use can increase the risk of serious reactions such as liver damage.
Toxicity
Esketamine is a relatively safe drug when used as directed, but excessive doses can lead to adverse effects, including confusion, hallucinations, agitation, abnormal behavior, and seizure. Prolonged use can also lead to tolerance, physical and psychological dependence, and withdrawal syndrome.
Precautions
Esketamine should not be used in patients with a history of mania, psychoses, suicidal thoughts, or substance abuse. It should also not be administered to patients who are pregnant or breastfeeding, or those suffering from hepatic or renal impairment, seizure disorders, or other unstable medical conditions.
Interaction
Esketamine can interact with other medications, including MAOIs, SSRIs, SNRIs, antibiotics, anti-seizure medications, and anticholinergics. Patients should be monitored for possible interactions when taking esketamine concurrently with other medications.
Disease Interaction
Esketamine may have an effect on conditions such as hypertension, diabetes, renal or hepatic impairment, seizure disorders, or other unstable medical conditions. Patients should be monitored for possible interactions when taking esketamine concurrently with other disease-related medications.
Drug Interaction
Esketamine is known to interact with certain drugs, including MAOIs, SSRIs, SNRIs, antibiotics, anti-seizure medications, and anticholinergics. Patients should be monitored for possible interactions when taking esketamine concurrently with other medications.
Food Interactions
Esketamine should not be taken with food. Eating fatty foods can decrease the absorption of esketamine and make it less effective.
Pregnancy Use
Esketamine is classified as a “Pregnancy Category X” medication, meaning it must not be used during pregnancy. It is known to cross the placental barrier and has been linked to fetal abnormalities and adverse pregnancy outcomes. Women should avoid taking esketamine while pregnant or planning to become pregnant.
Lactation Use
Esketamine is excreted in human milk and should be avoided while breastfeeding.
Acute Overdose
Esketamine has a low risk of overdose but taking high doses can lead to an increased risk of serious reactions, including confusion, hallucinations, agitation, abnormal behavior, and seizure. Overdose should be treated with supportive care, including monitoring heart rate, breathing, and vital signs.
Contraindication
Esketamine is contraindicated in patients with a history of mania, psychoses, suicidal thoughts, or substance abuse. It should also not be administered to patients who are pregnant or breastfeeding, or those suffering from hepatic or renal impairment, seizure disorders, or other unstable medical conditions.
Use Direction
Esketamine should be used as directed by a healthcare professional, according to the patient’s medical history and individual needs. The optimal dose should be determined by a doctor or other healthcare provider. The most common dosage is 56mg administered as an intravenous infusion over 10-15 minutes, twice weekly for a total of two doses. The same dose is also available as a weekly nasal spray.
Storage Condition
Esketamine should be stored at room temperature (15-25°C), away from moisture, heat, and light. It should also be kept from freezing.
Volume of Distribution
Esketamine has a volume of distribution of approximately 0.4 L/kg.
Half Life
Esketamine has a half life of approximately four hours.
Clearance
Esketamine is cleared by the liver; its clearance rate is 56 mL/min.
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