Schedule H

Oral, Inhalation, Parenteral (IM/IV)

• Tablets (glycopyrronium bromide): 1 mg, 2 mg

• Solution for injection: 0.2 mg/mL (1 mL, 2 mL ampoules)

• Dry powder inhaler capsules: 50 mcg per capsule (for use with specific inhaler device)

Note: Transdermal formulation is NOT AVAILABLE in India.

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Chronic Obstructive Pulmonary Disease (COPD) — Maintenance Bronchodilation

(Long-Acting Muscarinic Antagonist — LAMA)

Inhalation Route:

Parameter Details

Starting dose 50 mcg inhaled once daily (one capsule via DPI device)

Titration Not applicable

Usual maintenance dose 50 mcg once daily

Maximum dose 50 mcg once daily

Clinical Notes:

• NOT for acute bronchospasm or rescue therapy

• Onset of action: 5–15 minutes; duration: approximately 24 hours

• May be combined with LABA (as LABA/LAMA) or ICS/LABA for GOLD Group B–D patients

• Capsules for inhalation only — must NOT be swallowed

• 2. Reduction of Salivary and Respiratory Secretions — Perioperative Use

• Parenteral Route (IM/IV):

Parameter Details

Starting dose 0.2 mg (200 mcg) IM or IV

Titration Not applicable

Usual maintenance dose 0.2 mg as single preoperative dose

Maximum dose 0.4 mg per dose; up to 0.6 mg/day in divided doses

Timing: Administer 30–60 minutes before induction (IM) or immediately before induction (IV)

Clinical Notes:

• Preferred antisialagogue with ketamine anaesthesia

• Produces less tachycardia compared to atropine

• Used in dental and ENT procedures requiring dry field

1. Reversal of Neuromuscular Blockade — Adjunct with Neostigmine

Parenteral Route (IV):

Parameter Details

Starting dose 0.2 mg (200 mcg) IV with neostigmine

Titration Not applicable

Usual maintenance dose 0.2 mg per reversal

Maximum dose 0.4 mg per dose

Clinical Notes:

• Administer IV slowly with neostigmine (typically 0.2 mg glycopyrronium per 1 mg neostigmine)

• Prevents muscarinic side effects of neostigmine (bradycardia, excessive secretions)

• Preferred over atropine due to more stable heart rate profile

1. Sialorrhoea (Pathological Hypersalivation)

(Neurological disorders: Parkinson's disease, motor neuron disease, cerebral palsy)

Oral Route:

Parameter Details

Starting dose 1 mg orally twice daily

Titration Increase by 1 mg per dose every 5–7 days based on response and tolerability

Usual maintenance dose 1–2 mg two to three times daily

Maximum dose 3 mg three times daily (9 mg/day)

Clinical Notes:

• Administer 1 hour before meals for optimal effect

• Clinical benefit typically seen within 1–2 weeks

• Monitor anticholinergic burden in patients on multiple medications

Secondary Indications — Adults Only (Off-label)

Indication Dose Duration Remarks

Hyperhidrosis — OFF-LABEL 1–2 mg orally at bedtime; may increase to 2 mg twice daily Long-term; reassess periodically Specialist only (Dermatologist); limited evidence; Indian dermatology practice

Peptic ulcer adjunct — OFF-LABEL 1–2 mg orally 2–3 times daily Short-term adjunctive use Rarely used; superseded by PPIs and H2 blockers; historical indication

PAEDIATRIC DOSING (Specialist Only)

Primary Indications

1. Sialorrhoea in Neurodisability

(Cerebral palsy, neurological impairment)

Oral Route:

Weight/Age Starting Dose Titration Usual Maintenance Maximum Dose

≥3 years, <40 kg 40 mcg/kg/day in 2–3 divided doses Increase by 40 mcg/kg/day every 5–7 days 40–100 mcg/kg/day in divided doses 100 mcg/kg/day (max 8 mg/day)

≥3 years, ≥40 kg 1 mg twice daily Increase by 1 mg per dose every 5–7 days 1–2 mg two to three times daily 3 mg three times daily

Monitoring:

• Constipation and bowel function

• Urinary retention symptoms

• Behavioural changes

• Dry mouth and dental hygiene

Note: Oral solution may require extemporaneous preparation as tablets are not ideal for weight-based dosing in young children.

1. Perioperative Antisialagogue

Parenteral Route (IM/IV):

Parameter Details

Starting dose 4–10 mcg/kg IM or IV

Titration Not applicable

Usual maintenance dose 4–10 mcg/kg as single preoperative dose

Maximum dose 200 mcg (0.2 mg) per dose

Timing: 30–60 minutes before anaesthesia (IM) or at induction (IV)

1. Reversal of Neuromuscular Blockade — Adjunct with Neostigmine

Parenteral Route (IV):

Parameter Details

Starting dose 10 mcg/kg IV (administered slowly with neostigmine)

Titration Not applicable

Usual maintenance dose 10 mcg/kg per reversal

Maximum dose 200 mcg (0.2 mg) per dose

Monitoring: Heart rate, secretions, signs of incomplete reversal

Secondary Indications — Paediatric (Off-label)

Not applicable — No established off-label paediatric indications with adequate evidence in Indian practice.

⚠️ Not recommended below 3 years of age for oral use except under specialist supervision (paediatric neurologist/gastroenterologist) in tertiary care settings with documented justification.

60 All routes No dose adjustment required

30–60 Oral Use with caution; consider reduced frequency (twice daily instead of thrice daily)

30–60 Inhaled No dose adjustment required

<30 Oral Reduce dose by 50% or increase dosing interval; monitor for anticholinergic toxicity

<30 Inhaled Use with caution; monitor for systemic effects

Haemodialysis All routes Limited data; use with caution; not significantly dialysable

Note: Glycopyrronium undergoes minimal hepatic metabolism; elimination is primarily renal.

• Hypersensitivity to glycopyrronium bromide or other anticholinergic agents

• Uncontrolled narrow-angle glaucoma (closed-angle glaucoma)

• Myasthenia gravis (may worsen muscle weakness)

• Paralytic ileus or intestinal obstruction

• Toxic megacolon

• Severe ulcerative colitis

• Urinary retention with complete bladder outlet obstruction

• Elderly patients — increased sensitivity to anticholinergic CNS and peripheral effects

• Bladder outflow obstruction or prostatic hypertrophy — risk of urinary retention

• Moderate to severe renal impairment (especially oral formulation)

• Pre-existing cognitive impairment — may exacerbate confusion or delirium

• Controlled narrow-angle glaucoma (under ophthalmology supervision)

• Tachyarrhythmias or unstable cardiovascular disease

• Autonomic neuropathy

• Severe constipation or history of faecal impaction

• Hot environmental conditions — risk of hyperthermia due to reduced sweating

• Concurrent use of other anticholinergic medications — cumulative burden

Parameter Details

Safety Category Limited human data; animal studies show no significant risk at therapeutic doses

Preferred alternatives For COPD: short-acting bronchodilators (salbutamol) preferred; for sialorrhoea: non-pharmacological measures

When to use Perioperative use acceptable if benefit outweighs risk; avoid long-term use during pregnancy

Monitoring Fetal growth if chronic use unavoidable; maternal anticholinergic effects

Parameter Details

Compatibility Likely compatible — quaternary ammonium compound with poor oral absorption

Drug levels in milk Expected to be low; poor infant oral bioavailability

Preferred alternatives Avoid chronic oral use if possible; inhaled route preferred for COPD

Infant monitoring Dry mouth, feeding difficulty, constipation, sedation, irritability

Parameter Recommendation

Starting dose 50% of usual adult oral dose (0.5–1 mg once or twice daily for sialorrhoea); inhaled: no adjustment

Titration Slower titration (every 7–10 days for oral)

Special considerations Increased sensitivity to anticholinergic effects — constipation, urinary retention, cognitive impairment, delirium, tachycardia

Additional risks Falls risk due to blurred vision and dizziness; heat intolerance; avoid in patients with dementia

Preferred route Inhaled route preferred over oral for COPD due to lower systemic anticholinergic burden

Drug Mechanism Clinical Effect Recommendation

Neostigmine, Pyridostigmine (cholinesterase inhibitors for myasthenia gravis) Pharmacological antagonism Reduced efficacy of cholinesterase inhibitors; worsening myasthenia Avoid combination (except for neuromuscular blockade reversal)

Potassium chloride (solid oral dosage forms) Reduced GI motility increases contact time Increased risk of GI ulceration Avoid combination; use liquid potassium if supplementation required

Other anticholinergics (atropine, tiotropium, oxybutynin, tricyclics) Additive antimuscarinic effects Enhanced toxicity — dry mouth, constipation, urinary retention, confusion, tachycardia Avoid duplication; if unavoidable, monitor closely

Clozapine Additive anticholinergic burden Risk of severe constipation, ileus, delirium Avoid combination; if essential, close monitoring mandatory

Drug Interaction Recommendation

Long-acting beta-agonists (LABAs) — formoterol, salmeterol, indacaterol Additive bronchodilation; generally beneficial Monitor for paradoxical bronchospasm

First-generation antihistamines (chlorpheniramine, diphenhydramine) Additive anticholinergic effects Use with caution; monitor for enhanced adverse effects

Tricyclic antidepressants (amitriptyline, imipramine) Additive anticholinergic effects Avoid combination if possible; monitor for toxicity

Opioids (morphine, tramadol) Additive constipation and urinary retention Monitor bowel function; consider prophylactic laxatives

Benzodiazepines, CNS depressants Additive sedation; increased delirium risk Use with caution, especially in elderly

Domperidone, Metoclopramide Opposing effects on GI motility Reduced efficacy of prokinetics; monitor GI symptoms

• Dry mouth (most common with oral/inhaled forms)

• Constipation

• Urinary hesitancy/retention

• Blurred vision

• Tachycardia (especially with parenteral administration)

• Nausea

• Cough and throat irritation (inhaled form)

• Headache

• Nasal dryness

• Acute angle-closure glaucoma — requires immediate ophthalmologic intervention; discontinue drug

• Acute urinary retention — may require catheterisation; discontinue drug

• Paralytic ileus — discontinue immediately; may require hospitalisation

• Severe delirium/acute confusional state — especially in elderly or paediatric patients; discontinue drug

• Anaphylaxis/severe hypersensitivity — rare; discontinue and manage appropriately

• Paradoxical bronchospasm (inhaled form) — discontinue; use rescue bronchodilator

Phase Parameters

Baseline Cognitive status (especially elderly/children); urinary function; intraocular pressure (if glaucoma risk factors); renal function; bowel habit history

After initiation Bowel function; urinary symptoms; mental status (elderly/paediatric); heart rate (parenteral use)

Inhaled form Pulmonary function periodically; symptom control assessment

Long-term oral use Cumulative anticholinergic burden assessment; cognitive function in elderly; constipation; dental health (dry mouth related)

Oral Tablets:

• Glycate® (Cipla)

• Cuvposa® (limited availability)

• Sialanar® (limited availability)

Injection:

• Glyco-P® (Neon)

• Pyrolate® (Samarth)

• Glycopyrrolate injection (generic — various manufacturers)

Dry Powder Inhaler (COPD):

• Seebri Breezhaler® (Novartis)

• Glyco® DPI (Sun Pharma)

Note: Not included in NLEM 2022; not NPPA price-controlled.

• COPD bronchodilation: Inhaled glycopyrronium (LAMA) has slower onset than short-acting ipratropium but provides 24-hour duration — suitable for maintenance, NOT rescue therapy

• Perioperative preference: Glycopyrronium causes less tachycardia than atropine — preferred antisialagogue for patients with cardiovascular concerns or when used with ketamine

• Anticholinergic burden: Avoid in elderly patients already on multiple anticholinergics — cumulative burden increases risk of confusion, falls, urinary retention, and constipation

• Paediatric sialorrhoea: Oral glycopyrronium is highly effective for drooling in children with neurodisability — start low and titrate slowly under specialist supervision

• Inhalation technique: Ensure proper inhaler technique training — capsules are for inhalation via specific device only and must NOT be swallowed

• Neostigmine reversal: When used with neostigmine for NMB reversal, administer slowly IV to avoid cardiac rhythm disturbances

glycopyrronium; LAMA; COPD; anticholinergic; antimuscarinic; sialorrhoea; perioperative; anaesthesia; neostigmine reversal; paediatric neurology; elderly-caution; renal-adjustment; Schedule H; India

RxIndia v1.0 — 10 Apr 2025

• CDSCO approved product information (glycopyrrolate tablets, injection, inhalation)

• Indian Pharmacopoeia 2022

• API Textbook of Medicine — COPD Management

• AIIMS Drug Formulary

• ICMR COPD Management Guidelines

• Indian Society of Anaesthesiologists protocols

• IAP Guidelines — Paediatric Neurodisability Management

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• Indian paediatric neurology specialist practice reports