eszopiclone

eszopiclone

Lunesta

Pharmacologic class: Nonbenzodiazepine

Therapeutic class: Hypnotic

Controlled substance schedule IV

Pregnancy risk category C

Action

Unclear. Effect may result from interaction with GABA-receptor complexes at binding domains near or allosterically coupled with benzodiazepine receptors.

Availability

Tablets: 1 mg, 2 mg, 3 mg

⊘Indications and dosages

➣ Insomnia

Nonelderly adults: 2 mg P.O. immediately before bedtime. Drug may be initiated at, or dosage may be increased to, 3 mg if indicated clinically. In patients also receiving potent CYP3A4 inhibitors, starting dosage shouldn't exceed 1 mg.

Elderly adults: 1 mg P.O. immediately before bedtime. Dosage may be increased to 2 mg if indicated clinically. If patient's chief complaint is difficulty staying asleep, recommended dosage is 2 mg P.O. immediately before bedtime.

Dosage adjustment

• Hepatic impairment
• Concomitant use of other CNS depressants

Contraindications

None

Precautions

Use cautiously in:
• hepatic impairment, respiratory compromise, depression
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).

Administration

• Don't give with or immediately after a heavy, high-fat meal because this may slow drug absorption and reduce efficacy.

Route	Onset	Peak	Duration
P.O.	Unknown	1 hr	6 hr

Adverse reactions

CNS: headache, anxiety, confusion, depression, dizziness, hallucinations, nervousness, abnormal dreams

CV: chest pain, peripheral edema

GI: nausea, vomiting, diarrhea, dyspepsia, cholelithiasis, dry mouth

GU: urinary tract infection, decreased libido, dysmenorrhea, gynecomastia (in males)

Respiratory: respiratory infection

Skin: rash, pruritus

Other: unpleasant taste, viral infection, neuralgia, facial edema, allergic reaction

Interactions

Drug-drug. CYP3A4 inhibitors (such as itraconazole, ketoconazole, ritonavir, troleandomycin): increased eszopiclone blood level

CYP3A4 inducers (such as rifampin): decreased eszopiclone blood level

Drug-food. Heavy, high-fat meal: slowed drug absorption and reduced efficacy

Drug-behaviors Alcohol use: additive effects on psychomotor performance

Patient monitoring

• Before starting therapy, evaluate patient to help eliminate physical or psychiatric causes of insomnia.
• Know that after rapid dosage decrease or abrupt drug withdrawal, patient may experience signs and symptoms similar to those associated with withdrawal from other CNS depressants.

Patient teaching

• Instruct patient not to take drug with or immediately after a heavy, high-fat meal.
• Advise patient to take drug immediately before bedtime; otherwise, short-term memory impairment, hallucinations, incoordination, dizziness, and light-headedness may occur.
• Caution patient not to engage in hazardous activities after taking drug.
• Tell patient drug may have some effect the next day; advise him to use extreme care when driving or performing other hazardous activities until drug effects are known.
• Caution patient not to take drug with other psychotropics, anticonvulsants, antihistamines, or other drugs that cause CNS depression.
• Advise patient not to take drug with alcohol.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, foods, and behaviors mentioned above.