Glycopyrrolate

Registered South African indications:

• Indicated for use as a pre-operative antimuscarinic to:
  - Reduce salivary, tracheobronchial and pharyngeal secretions to reduce the volume and free acidity of gastric secretions
  - To block cardiac vagal inhibitory reflexes during induction of anaesthesia and intubation
  - Protect against the peripheral muscarinic effects (e.g. bradycardia and excessive secretions) of cholinergic medicines such as neostigmine and pyridostigmine given to reverse the neuromuscular blockade due to nondepolarising muscle relaxants

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

Caution in the following patient groups

• Pregnancy
• Breastfeeding
• Renal impairment 
• Hepatic impairment 
• Elderly

Tachycardia

• Extreme caution is advised in patients with existing tachycardia, thyrotoxicosis, coronary artery disease, cardiac dysrhythmias, hypertension, congestive heart failure, and cardiac insufficiency

Inhibition of sweating

• Patients with increased temperature (especially children) should be observed closely as glycopyrrolate inhibits sweating

Prostatic hypertrophy, paralytic ileus, pyloric stenosis, and closed-angle glaucoma

• Caution is advised when glycopyrrolate is used in patients with these conditions

Ventricular dysrhythmias

• Anticholinergic medicines like glycopyrrolate can cause ventricular dysrhythmias, especially during inhalation anaesthesia in association with halogenated hydrocarbons. Caution should be observed if used during halogenated anaesthesia
• Administering in small incremental doses of 0.1mg or less reduces the likelihood of ventricular dysrhythmias.

Myasthenia gravis

• Quaternary ammonium compounds in large doses can block end plate nicotinic receptors, which should be considered before using glycopyrrolate in patients with myasthenia gravis

Renal elimination in uraemia

• The renal elimination of glycopyrrolate is considerably prolonged in patients with uraemia. Glycopyrrolate should be used with caution in these patients

Effects on ability to drive and use machines

• Adverse reactions such as dizziness, mental confusion, and blurred vision have been reported. Patients should not drive, use machinery, or perform tasks requiring concentration until they are certain that glycopyrrolate does not adversely affect their ability to do so

Forms avail. in SA and covered in this monograph: inj

Indicated for use as a pre-operative antimuscarinic to:
- Reduce salivary, tracheobronchial and pharyngeal secretions to reduce the volume and free acidity of gastric secretions
- To block cardiac vagal inhibitory reflexes during induction of anaesthesia and intubation
- Protect against the peripheral muscarinic effects (e.g. bradycardia and excessive secretions) of cholinergic medicines such as neostigmine and pyridostigmine given to reverse the neuromuscular blockade due to nondepolarising muscle relaxants

Pre-anaesthetic medication

• IM: 0.004mg (0.02ml)/kg of body mass, given 30 min. to 1hr prior to the anticipated time of induction of anaesthesia or at the time the preanaesthetic narcotic and/or sedative is administered

Intra-operative medication (may be used during surgery to counteract anaesthetic induced or vagal traction reflexes with the associated dysrhythmias (e.g. bradycardia))

• IV: 0.1mg (0.5ml), as a single dose; Repeat as needed, at intervals of 2-3 min; The usual attempts should be made to determine the aetiology of the dysrhythmia, and the surgical or anaesthetic manipulations necessary to correct parasympathetic imbalance should be performed

Reversal of neuromuscular blockade

• IV: 0.2mg(1.0ml) for each 1.0mg of neostigmine or 5.0mg of pyridostigmine; In order to minimise the appearance of cardiac side effects, these substances may be administered simultaneously by intravenous injection and may be mixed in the same syringe

Glycopyrrolate may be administered intramuscularly, intravenously or subcutaneously, without dilution

Compatibility with other medicines:
Chemical compatibility – Glycopyrrolate is chemically compatible for mixing and injection with the following: 5% and 10% glucose in water or saline; meperidine injection; morphine sulphate; fentanyl plus droperidol injection; hydroxyzine injection Glycopyrrolate may be administered via the tubing of a running infusion of physiological saline or lactated Ringer’s solution

Paed. forms avail. in SA and covered in this monograph: inj

Indicated for use as a pre-operative antimuscarinic to:
- Reduce salivary, tracheobronchial and pharyngeal secretions to reduce the volume and free acidity of gastric secretions
- To block cardiac vagal inhibitory reflexes during induction of anaesthesia and intubation
- Protect against the peripheral muscarinic effects (e.g. bradycardia and excessive secretions) of cholinergic medicines such as neostigmine and pyridostigmine given to reverse the neuromuscular blockade due to nondepolarising muscle relaxants

Recommended dosage range

• Up to 12 years: IM: 0.004-0.008mg (0.02-0.04ml)/kg of body mass

Intraoperative use and for reversal of neuromuscular blockade

• IV: 0.2mg (1.0ml) for each 1.0mg of neostigmine or 5.0mg of pyridostigmine

Glycopyrrolate may be administered intramuscularly, intravenously or subcutaneously, without dilution

Compatibility with other medicines:
Chemical compatibility – Glycopyrrolate is chemically compatible for mixing and injection with the following: 5% and 10% glucose in water or saline; meperidine injection; morphine sulphate; fentanyl plus droperidol injection; hydroxyzine injection Glycopyrrolate may be administered via the tubing of a running infusion of physiological saline or lactated Ringer’s solution

Pregnancy

• Caution
• There is no data from the use of glycopyrronium bromide injection in pregnant women. Animal studies for glycopyrronium bromide are insufficient with respect to reproductive toxicity. Use of glycopyrronium bromide Injection is not recommended during pregnancy

Breastfeeding

• Caution; not recommended
• It is unknown whether glycopyrronium is excreted in human milk. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from glycopyrronium bromide injection therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman

Renal Impairment

• Caution; no dose adjustment recommended
  eGFR <30 ml/min: Use only if the potential benefit outweighs the risk

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• Caution; dose adjustment recommended
  Initial: 20μg/kg, in 3 divided doses; Titrate by 20μg/kg at intervals of 5-7 days, as tolerated
  Dosage should not exceed 100μg/kg (in divided doses) daily; Do not exceed 3mg/dose

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Confusion
• Dizziness

Cardiovascular Disorders

• Transient bradycardia
• Tachycardia
• Palpitations
• Arrhythmias
• Flushing

Respiratory Disorders

• Reduced bronchial secretions

Gastrointestinal Disorders

• Constipation
• Dry mouth
• Nausea and vomiting

Genitourinary Disorders

• Difficulty in micturition
• Urinary urgency

Skin and Subcutaneous Tissue Disorders

• Dry skin
• Inhibition of sweating 

Sensory Disorders

• Dilation of pupils
• Loss of accomodation
• Photophobia
• Closed-angle glaucoma

• Halogenated anaesthetics 
• Anticholinergic agents
• Corticosteroids
• Digoxin
• Ritodrine
• Antimuscarinic agents
• Domperidone
• Metoclopramide
• Ketoconazole
• Levodopa
• Memantine
• Nitrates
• Parasympathomimetics

• Heart rate

Glycopyrrolate is a competitive muscarinic antagonist that diminishes the risk of vagal inhibition of the heart and reduces salivary and bronchial secretions.

Injection (per ml) 0.2mg

• Robinul (Pharmacare) originator