Brand Name :
lunesta
Synonyms :
eszopiclone
Class :
Sedative
Dosage Forms & Strengths
Tablet
1mg
2mg
3mg
Initial dose: 1mg orally before bedtime
Maintenance dose: 1-3mg orally before bedtime
Maximum dose:3mg/kg
Dose Adjustments
The starting dose for those taking a CYP3A inhibitor should not exceed 1 mg. No dose adjustment is required for mild to moderate renal impairment, but those with severe hepatic impairment should start with 1 mg PO HS
Dosage adjustments may be necessary to avoid additive effects when eszopiclone is coadministered with another central nervous system (CNS) depressant
Safety and efficacy not established
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may enhance the serum concentration
may enhance the serum concentration
may enhance the serum concentration
may enhance the serum concentration
may enhance the serum concentration
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may enhance the serum concentration of CYP3A4 inhibitors
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
CYP3A strong enhancers of the small intestine may reduce the bioavailability of eszopiclone
it increases the effect of CNS depressants
it increases the effect of CNS depressants
CNS depressants increase the CNS depressing effect of paraldehyde
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
eszopiclone: they may diminish the serum concentration of CYP3A4 Inducers
eszopiclone: they may diminish the serum concentration of CYP3A4 Inducers
eszopiclone: they may diminish the serum concentration of CYP3A4 Inducers
eszopiclone: they may diminish the serum concentration of CYP3A4 Inducers
eszopiclone: they may diminish the serum concentration of CYP3A4 Inducers
the effect of eszopiclone is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of thalidomide
it increases the effect of CNS depressants
it increases the effect of CNS depressants
may increase the toxic effects
Mechanism of action
It is a nonbenzodiazepine hypnotic drug that acts as an agonist at the GABA-A receptor. Its mechanism of action enhances the effect of GABA, a neurotransmitter in the brain that promotes sleep, leading to a decrease in sleep latency and an improvement in sleep quality.
Spectrum
Its spectrum of activity is for the treatment of insomnia, particularly for difficulty falling and staying asleep
Frequency defined:
>10%
Unpleasant taste
headache
1-10%
Accidental injury
Dizziness
Dyspepsia
Neuralgia
Pruritis
Somnolence
UTI
Abnormal dreams
Diarrhea
Dry mouth
Nervousness
Pain
Rash
Unpleasant tase
<1%
Alopecia
Asthma
Cystitis
Fever
Hypertension
Hypercholesterolemia
Agitation
Angioedema
Anorexia
Dysphagia
Epistaxis
Hostility
Hypokalemia
Post-marketing reports
Complex sleep behaviors
dysosmia
Black box warning
It can cause complex sleep behaviors, including sleepwalking, sleep-driving, and performing other activities while not fully awake. These behaviors can result in severe injury or even death. If a patient experiences such behavior, it is essential to discontinue drug use immediately.
Contraindications
Hypersensitivity reactions
Caution
Pregnancy consideration: Insufficient data available
Lactation: Excretion of the drug in human breast milk is unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology
The exact mechanism by which eszopiclone interacts with GABA receptor complexes is unknown. However, it is thought to act at binding domains allosterically coupled to benzodiazepine receptors, leading to an enhancement of the effect of GABA, a neurotransmitter that promotes sleep. This results in a decrease in sleep latency and an improvement in the quality of sleep.
Pharmacodynamics
It is a nonbenzodiazepine hypnotic drug that acts as an agonist at the GABA-A receptor. Its pharmacodynamics involves enhancing the effect of GABA, a neurotransmitter in the brain that promotes sleep, leading to a decrease in sleep latency and an improvement in sleep quality. This is achieved by binding to specific sites on the GABA-A receptor, which leads to an increase in the affinity of GABA for the receptor and an enhancement of its inhibitory effect on the nervous system, resulting in sedation and improved sleep. The onset of action is typically within 30 minutes, and the duration of action is generally 6-8 hours.
Pharmacokinetics
Absorption: It is well absorbed after oral administration, with peak plasma concentrations reached in approximately 1-2 hours.
Distribution: It is widely distributed throughout the body. Its volume of distribution is approximately 0.9 L/kg
Metabolism: It is primarily metabolized by the liver, and its metabolites are primarily excreted in the urine
Elimination/Excretion: The elimination half-life of eszopiclone is approximately 6 hours. It is eliminated primarily through renal excretion, with less than 10% of the dose excreted unchanged in the urine.
Administration
It is a medication that is taken orally, usually at bedtime. The recommended dose is 1 to 2 mg. It is essential to take it precisely as a healthcare provider directed and not exceed the recommended dose.
Patient information leaflet
Generic Name: eszopiclone
Pronounced: [ e-ZOP-i-klone ]
Why do we use eszopiclone?
It treats insomnia (difficulty falling asleep or staying asleep). It works by affecting certain chemicals in the brain that may become unbalanced and cause sleep problems.