Eszopiclone
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triazabicyclo[4.3.0]nona-1,3,5-trien-9-yl] 4-methylpiperazine-1-carboxylate
Brand/Trade Names of Drug
Lunesta®
Generic Name of Drug
Eszopiclone (es-zoe-PIK-lone)
Description
Eszopiclone is a rapid-acting hypnotic/sedative agent is a pyrrolopyrazine derivative in the cyclopyrrolate class and is approved for the short-term and long-term treatment of insomnia.[1] This medication is the S(+)-enantiomer of zopiclone (Imovane). Transient insomnia is known to affect between 25% and 35% of the population.[2] Medications in the cyclopyrrolate class act at gamma-aminobutyric acid (GABA) by binding to receptor sites near benzodiazepine type 1 receptors (BZ1; omega-1 receptors). Medications in the cyclopyrralate class are not considered to be part of the benzodiazepine class.[1] Eszopiclone was approved by the FDA in December 2004.[1] The patent for eszopiclone is held by Sepracor and expires on January 12, 2012.
Eszopiclone has been shown to safely and effectively help patients fall asleep and maintain sleep.[1] [3] During this trial patients showed no symptoms of rebound insomnia, tolerance, or next-day residual effects. A second trial was conducted in 2005 that also determined that patients had good tolerance with all available doses of eszopiclone.[4] The safety of long-term use (up to 6 months) was determined during a six month study performed in 2003.[5]
Mechanism of action
Eszopiclone is the S-isomer of the previously approved hypnotic medication, zopiclone (Imovane). The sedative properties of eszopiclone are thought to be due to the modulation of GABA(A) receptor subunits by the increased production of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter.[6] [7]
Gamma-aminobutyric acid-A (GABA(A)) macromolecular complexes are found on post-synaptic neurons and are typically composed of five subunits that surround a chloride channel (refer to diagram).[8] It is unknown as to the exact location that eszopiclone acts on the GABA(A) complex.[1]
Time Required for Therapeutic Response
- Initial: Immediate response expected (15-30 minutes; no data available to support exact time to action)[1]
- Maximum: 1 hour[1]
Pharmacokinetics
Insert the Pharmacokinetic data as separated into Absorption, Distribution, Metabolism, & Excretion. This section requires focus because the information must be in your own words and will likely come from multiple sources. Package inserts, the primary phase I and phase II trials (if available), and PK review articles will have this information available. Make sure to be as complete as possible. We want to have the most complete source for clinical reference in one place.
Absorption
Distribution
Metabolism
Excretion
Special Population Pharmacokinetics
- Renal insufficiency
- Hepatic insufficiency
- Hemodialysis
- Geriatric
- Pediatric
- Gender
Indications
FDA Approved Indications
FDA-Approved and Non-FDA Approved Indications. This section should have the primary clinical trials which led to the indication approval or validation of the non-approved indication cited. These studies are generally discussed heavily in the current package inserts.
- 1st Indication
- 2nd Indication, etc.
Non-FDA Approved Indications
- 1st Indication
- 2nd Indication, etc.
Dosage
- 1st Indication
- Starting Dose:
- Titration Schedule:
- Maintenance Dose:
- 2nd Indication
- Starting Dose:
- Titration Schedule:
- Maintenance Dose:
- Maximum Dosage Limits
- Adults:
- Elderly:
- Adolescents and children >=10 years:
- Children < 10 years:
- Dosage Adjustment
- Renal insufficiency:
- Hepatic insufficiency:
- Hemodialysis:
- Geriatric:
- Pediatric:
- Gender:
Administration
- Route:
- Method:
- Special considerations:
- Route:
- Method:
- Special considerations:
Monitoring Parameters
- Parameter 1
- Parameter 2
- etc
Contraindications/Precautions
Contraindications
- 1st
- 2nd
- etc
Precautions
- 1st
- 2nd
- etc
Pregnancy indications
- Pregnancy category: C
- Teratogenicity: Studies investigating the effects of eszopiclone on the fetus of pregnant rats revealed that the drug has not been shown to cause teratogenic effects. However, the administration of toxic doses to the rats resulted in developmental delay and reductions in fetal weight. During a second trial involving administration of eszopiclone to pregnant rats, doses were given that were not toxic to the pregnant females. This trial revealed effects such as an increase in post-implantation loss, decreased postnatal birth weights, decreased chance of survival, and increased pup startle response.
The use of eszopiclone during pregnancy is NOT recommended. Eszopiclone should only be used during pregnancy if the benefit of this drug exceeds the risks posed to the fetus.
Breast-feeding indications
- Secretion into breast milk:
Drug-Drug Interactions
| 4 | List drugs that increase effect/toxicity as follows: clofibrate[1]Image:Eszopiclone Drug Interactions.gif fenofibrate[1]Image:Eszopiclone Drug Interactions.gif | List drugs that decrease effect. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 3 | List drugs that increase effect/toxicity. | List drugs that decrease effect.
| 4 | List drugs that increase effect/toxicity as follows: clofibrate[1][9]
[edit] Overdosage MeasuresIn the event of a zolpidem overdose, patients should receive immediate gastric lavage (if appropriate), supportive care, and continuous monitoring of vital signs. All sedating drugs should be withdrawn until the patient is stable. Flumazenil administration may also be an effective method to reverse the central inhibitory effects and sedation caused by eszopiclone during an overdose. Additional medical interventions should be used if necessary. [edit] Product Information and DistributionReplace fields with correct information and delete this sentence.
Ex: Calcium carbonate [edit] Pharmacogenomic informationSearch pharmgkb.orgfor information on your drug and place an external link. Ex: Atorvastatin Pharmacogenomic Information [edit] Patient InformationCreate a bulleted list of the most important information to express to a patient during initial counseling. This should include specific administration instructions, OTC products to avoid, the most common side effects, rare side effects that should be reported to a physician, pregnancy and breast feeding precautions, and other drug specific precautions. Ex:
[edit] ReferencesReferences on Pubdrug.org should conform to ICMJE format. The easiest way to ensure correct formatting is to import all your references into endnote and then reference a blank page in word from where you can copy and paste the citation text into your wiki-citation. Instructions for Wiki-citations is on the following help page: Wiki Footnotes
[edit] PUBMED ReferencesList Pubmed references as links to the abstracts on Pubmed as per the example below. To import the citation from pubmed follow the instructions on Importing PubMed References [edit] Efficacy Trial Articles1. Krystal AD, Walsh JK, Laska E, et al. Sustained efficacy of eszopiclone over 6 months of nightly treatment: results of a randomized, double-blind, placebo-controlled study in adults with chronic insomnia. SLEEP. 2003;26:793-799. 2. Scharf M. Erman M. Rosenberg R. Seiden D. McCall WV. Amato D. Wessel TC. A 2-week efficacy and safety study of eszopiclone in elderly patients with primary insomnia. [Journal Article. Multicenter Study. Randomized Controlled Trial. Research Support, Non-U.S. Gov't Sleep. 28(6):720-7, 2005 Jun 1.] 3. Roth T. Walsh JK. Krystal A. Wessel T. Roehrs TA. An evaluation of the efficacy and safety of eszopiclone over 12 months in patients with chronic primary insomnia. [Journal Article. Randomized Controlled Trial. Research Support, Non-U.S. Gov't Sleep Medicine. 6(6):487-95, 2005 Nov.] 4. Zammit GK. McNabb LJ. Caron J. Amato DA. Roth T. Efficacy and safety of eszopiclone across 6-weeks of treatment for primary insomnia. [Clinical Trial. Journal Article. Multicenter Study. Randomized Controlled Trial. Research Support, Non-U.S. Gov't Current Medical Research & Opinion. 20(12):1979-91, 2004 Dec.] 5. Rosenberg R. Caron J. Roth T. Amato D. An assessment of the efficacy and safety of eszopiclone in the treatment of transient insomnia in healthy adults. [Clinical Trial. Journal Article. Randomized Controlled Trial. Research Support, Non-U.S. Gov't Sleep Medicine. 6(1):15-22, 2005 Jan.] [edit] Therapeutic Class Comparison Trial Articles1. Anonymous. Eszopiclone: esopiclone, estorra, S-zopiclone, zopiclone--Sepracor. [Review [19 refs] [Journal Article. Review] Drugs in R & D. 6(2):111-5, 2005.] 2. Paul MA. Gray G. MacLellan M. Pigeau RA. Sleep-inducing pharmaceuticals: a comparison of melatonin, zaleplon, zopiclone, and temazepam. [Clinical Trial. Comparative Study. Journal Article. Randomized Controlled Trial Aviation Space & Environmental Medicine. 75(6):512-9, 2004 Jun.] 3. Drover DR. Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives: zaleplon, zolpidem and zopiclone. [Review [113 refs] [Comparative Study. Journal Article. Review] Clinical Pharmacokinetics. 43(4):227-38, 2004.] 4. Terzano MG. Rossi M. Palomba V. Smerieri A. Parrino L. New drugs for insomnia: comparative tolerability of zopiclone, zolpidem and zaleplon. [Review [125 refs] [Comparative Study. Journal Article. Review] Drug Safety. 26(4):261-82, 2003.] [edit] Pharmacokinetics Articles1. Drover DR. Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives: zaleplon, zolpidem and zopiclone. [Review [113 refs] [Comparative Study. Journal Article. Review] Clinical Pharmacokinetics. 43(4):227-38, 2004.] 2. Halas CJ. Eszopiclone. [Journal Article American Journal of Health-System Pharmacy. 63(1):41-8, 2006 Jan 1.] [edit] Drug Interaction Articles1. Hesse LM. von Moltke LL. Greenblatt DJ. Clinically important drug interactions with zopiclone, zolpidem and zaleplon. [Review [122 refs] [Journal Article. Research Support, U.S. Gov't, Non-P.H.S.. Research Support, U.S. Gov't, P.H.S.. Review] CNS Drugs. 17(7):513-32, 2003.] 2. Tornio, A. Neuvonen, P. Backman, J. The CYP2C8 inhibitor gemfibrozil does not increase the plasma concentrations of zopiclone. European Journal of Clinical Pharmacology. 62(8):645-51. 2006 August. [edit] Images[edit] External LinksList external links to webpages as per example below:
Sepracor Inc.; Sepracor Information
NIH Insomnia Treatment Overview in Elderly Patients; NIH State-of-the-Science Conference Statement on Manifestations and Management of Chronic Insomnia in Adults
Lunesta Information; Lunesta Package Insert
American Sleep Association; National Sleep Foundation; National Institute of Health - Insomnia Overview
Lunesta & Sleep Driving; FDA & Sleep Driving Risks; New York Times Report - Sleep Driving |
