Schedule H

Oral

• Tablet: 3.75 mg

• Tablet: 7.5 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Insomnia (Short-term management only)

Parameter Details

Starting dose 3.75 mg orally at bedtime (recommended for elderly, hepatic impairment, or sensitive individuals)

Titration May increase to 7.5 mg if 3.75 mg inadequate; not to exceed 7.5 mg

Usual maintenance dose 7.5 mg orally once at bedtime

Maximum dose 7.5 mg per day

Duration Shortest duration possible; ideally ≤2 weeks, maximum 4 weeks including tapering period

Key notes Administer immediately before bedtime; rapid onset of action; do not re-dose during same night; ensure 7–8 hours available for sleep before next activity requiring alertness

Secondary Indications — Adults (Off-label, if any)

Pre-procedural night sedation — OFF-LABEL

Parameter Details

Indication Night-time anxiolysis before elective procedures

Dose 3.75–7.5 mg orally once on night before procedure

Duration Single dose only

Notes Specialist/anaesthesia practice only; not first-line; ensure no residual sedation affecting procedure consent

Evidence basis Occasional use in Indian anaesthesia protocols; limited formal evidence

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Not recommended for use in children and adolescents below 18 years of age.

Safety and efficacy data not established in paediatric population. No approved paediatric indication in India.

Secondary Indications — Paediatrics (Off-label, if any)

• Off-label paediatric use is discouraged

• Any use below 18 years requires specialist psychiatrist supervision with documented informed consent

• No established dosing guidelines available for Indian paediatric practice

Mild to moderate impairment No dose adjustment required

• Known hypersensitivity to zopiclone or any formulation excipient

• Severe hepatic impairment

• Obstructive sleep apnoea syndrome (untreated)

• Severe respiratory insufficiency or respiratory depression

• Myasthenia gravis

• Acute alcohol intoxication

• Concurrent use with high-dose opioids or multiple CNS depressants

• Elderly patients — increased risk of falls, confusion, next-day impairment

• Chronic obstructive pulmonary disease or mild respiratory compromise

• History of alcohol or substance abuse/dependence — potential for misuse

• Depression or history of psychiatric illness — may unmask or worsen suicidal ideation

• Use beyond 2–4 weeks — increased risk of tolerance, dependence, and rebound insomnia

• Patients with history of complex sleep behaviours (sleepwalking, sleep-eating)

• Concurrent use of other sedating medications

Aspect Details

Overall safety Not recommended; limited human safety data; animal studies suggest potential risk

Risk category Avoid unless absolutely necessary

When may be used Only if benefit clearly outweighs risk; short-term use; lowest effective dose; obstetric and psychiatric consultation advised

Preferred alternatives Non-pharmacological sleep hygiene measures first; if medication essential, consult specialist

What to monitor If used near term: monitor neonate for hypotonia, respiratory depression, withdrawal symptoms, poor feeding

Aspect Details

Compatibility Not recommended during breastfeeding

Drug levels in milk Low to moderate; approximately 50% of maternal plasma levels may appear in milk

Preferred alternatives Non-pharmacological interventions; if sedation essential, consult specialist

Recommendations If single dose essential, avoid breastfeeding for at least 8–12 hours after dose

Infant monitoring Monitor for sedation, lethargy, poor feeding, respiratory depression

Aspect Details

Starting dose 3.75 mg at bedtime (mandatory reduced starting dose)

Titration Avoid increasing to 7.5 mg unless absolutely necessary; reassess need frequently

Extra risks Increased sensitivity to CNS effects; higher risk of falls, fractures, next-day cognitive impairment, confusion, paradoxical reactions

Duration Use for shortest possible duration; frequent reassessment essential

Monitoring Assess for falls risk, cognitive function, and daytime sedation at each review

Drug/Class Interaction Recommendation

Alcohol Additive CNS depression; respiratory depression risk Avoid concurrent use

Opioid analgesics (morphine, tramadol, fentanyl) Profound sedation, respiratory depression, coma, death risk Avoid combination; if unavoidable, use lowest doses and monitor closely

Benzodiazepines Additive sedation and respiratory depression Avoid concurrent use

Strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir) Increased zopiclone plasma levels; enhanced and prolonged sedation Reduce zopiclone dose or avoid combination

Erythromycin, clarithromycin CYP3A4 inhibition; increased zopiclone levels Consider dose reduction; monitor for excessive sedation

Drug/Class Interaction Recommendation

CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, phenobarbital) Reduced zopiclone efficacy due to increased metabolism Monitor therapeutic effect; may need alternative hypnotic

SSRIs (fluoxetine, fluvoxamine, sertraline) Additive sedation; fluvoxamine inhibits CYP3A4 Monitor for excessive drowsiness

Antipsychotics Additive CNS depression Use cautiously; monitor for over-sedation

First-generation antihistamines (diphenhydramine, promethazine) Additive sedation Avoid concurrent use at night if possible

Antiepileptics (valproate, levetiracetam) Additive CNS depression Monitor for sedation

• Bitter or metallic taste (dysgeusia) — very common, characteristic of zopiclone

• Dry mouth

• Daytime drowsiness and residual sedation

• Dizziness

• Headache

• Fatigue

• Nausea

• Complex sleep-related behaviours — sleep-walking, sleep-driving, sleep-eating, sleep-related activities with amnesia; discontinue immediately if reported

• Dependence and withdrawal symptoms — rebound insomnia, anxiety, tremor, sweating with prolonged use or abrupt discontinuation

• Respiratory depression — particularly with overdose or combined CNS depressants; may require hospitalisation

• Paradoxical reactions — agitation, aggression, hallucinations, psychosis (more common in elderly)

• Suicidal ideation — particularly in patients with underlying depression; requires immediate psychiatric evaluation

• Anaphylaxis/angioedema — rare; discontinue immediately

Baseline (Before Initiation):

• Assess underlying cause of insomnia (psychiatric, medical, substance use)

• Mental status and mood assessment (screen for depression, suicidal ideation)

• Respiratory status evaluation

• History of substance abuse or dependence

• Current medication review for CNS depressant interactions

After Initiation:

• Review within 1–2 weeks of starting therapy

• Assess efficacy, adverse effects, daytime functioning

• Monitor for signs of dependence or dose escalation

Long-term:

• Reassess need for continued therapy every 2–4 weeks

• Avoid use beyond 4 weeks without documented reassessment

• Taper gradually if discontinuing after prolonged use

• Zolfresh (Sun Pharma)

• Zopicon (Intas)

• Hypnite (Consern Pharma)

• Zopitran (Ranbaxy/Sun)

• Zopiclone IP (various generic manufacturers)

3.75 mg tablet ₹2–₹6 per tablet

7.5 mg tablet ₹4–₹12 per tablet

• NLEM Status: Not included in NLEM

• Availability: Prescription only (Schedule H); available at private pharmacies

1. Short-term only: Limit use to 2–4 weeks maximum including taper; always address underlying cause of insomnia rather than prolonged pharmacotherapy

1. Elderly dosing: Always start at 3.75 mg in elderly patients — they are highly susceptible to falls, confusion, and next-day impairment

1. Metallic taste: Counsel patients about characteristic bitter/metallic taste — common and expected, not a reason to discontinue

1. Timing critical: Administer immediately before bed with 7–8 hours available for sleep; avoid re-dosing if patient wakes mid-night

1. Avoid with alcohol: Absolute contraindication to concurrent alcohol use due to synergistic respiratory depression — counsel explicitly

1. Taper when stopping: After more than 2 weeks of use, taper gradually to avoid rebound insomnia and withdrawal symptoms; do not stop abruptly

Zopiclone; insomnia; hypnotic; Z-drug; cyclopyrrolone; short-term-use; elderly-caution; dependence-risk; CNS-depressant; Schedule-H

RxIndia v1.0 — 10 Apr 2025

• CDSCO approved product information

• Indian Pharmacopoeia 2018

• API Textbook of Medicine, 11th Edition

• AIIMS Drug Formulary

• Goodman & Gilman's The Pharmacological Basis of Therapeutics, 13th Edition

• Indian psychiatric specialist practice protocols