Glycostom 0,2 mg/ml Solution for injection

In anaesthesia: GLYCOSTOM is indicated for use as a preoperative antimuscarinic to reduce salivary, tracheobronchial, and pharyngeal secretions, to reduce the volume and free acidity of gastric secretions; and to block cardiac vagal inhibitory reflexes during induction of anaesthesia and intubation. GLYCOSTOM protects 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 nondepolarizing muscle relaxants.

Posology

Adults: Preanaesthetic medicine: The recommended dose of GLYCOSTOM is 0,004 mg (0,02 ml) per kilogram of body mass by intramuscular injection, given 30 minutes to one hour prior to the anticipated time of induction of anaesthesia or at the time the preanaesthetic narcotic and/or sedative is administered. Intraoperative medicine: GLYCOSTOM may be used during surgery to counteract anaesthetic induced or vagal traction reflexes with the associated arrhythmias (e.g. bradycardia). It should be administered intravenously as single dose of 0,1 mg (0,5 ml) and repeated as needed, at intervals of 2 to 3 minutes. The usual attempts should be made to determine the etiology of the arrhythmia, and the surgical or anaesthetic manipulations necessary to correct parasympathetic imbalance should be performed. Reversal of neuromuscular blockade: The recommended dose of GLYCOSTOM is 0,2 mg (1,0 ml) for each 1,0 mg of neostigmine or 5,0 mg of pyridostigmine. 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.

Paediatric population: The recommended dosage range of GLYCOSTOM in children up to 12 years of age, is 0,004 mg to 0,008 mg (0,02 ml to 0,04 ml) intramuscularly per kilogram of body mass. For intraoperative use and for reversal of neuromuscular blockade, the paediatric dose is 0,2 mg (1,0 ml) GLYCOSTOM intravenously for each 1,0 mg of neostigmine or 5,0 mg of pyridostigmine.

Method of administration: GLYCOSTOM is for intravenous or intramuscular injection. For instructions on dilution of the medicine before administration, see section 6.6.

• Hypersensitivity to glycopyrronium bromide or to any of the excipients of GLYCOSTOM (see section 6.1).
• Angle-closure glaucoma.
• Myasthenia gravis (large doses of quaternary ammonium compounds can block the nicotinic receptors).
• Paralytic ileus.
• Pylorus stenosis.
• Prostatic enlargement.
• Combinations of cholinesterase inhibitors and antimuscarinics such as neostigmine plus GLYCOSTOM should be avoided in patients with extended QT intervals (see section 4.5).

Because GLYCOSTOM causes tachycardia, caution is advised in patients with glaucoma, asthma, hypertension, dysrhythmia, cardiac disorder and hyperthyroidism and it is recommended to measure the pulse rate if the patient report very fast or very slow heart rate. Should be used with caution to patients with increased temperature, as GLYCOSTOM inhibits sweating, and it is recommended to measure the temperature at regular time points. Should be used with caution to patients with renal insufficiency, prostatic hypertrophy, diarrhoea, ulcerative colitis, parkinsonism, and asthma. Patients diagnosed with one/some of the mentioned diseases should be informed to tell the doctor if specific symptoms arise.

Duration of effect of GLYCOSTOM may be prolonged in patients with renal impairment since glycopyrrolate is excreted mostly in urine as unchanged medicine (see section 5.2). Dose adjustment can be needed in patients with renal impairment. GLYCOSTOM contains less than 1 mmol (23 mg) sodium per ml, i.e., sodium free.

The intravenous administration of any anticholinergic in the presence of cyclopropane anaesthesia can result in ventricular dysrhythmias; therefore, caution should be observed if GLYCOSTOM must be used during cyclopropane anaesthesia. If the injection is given in small incremental doses of 0,1 mg or less, the likelihood of producing ventricular arrhythmias is reduced. There is an increased risk of antimuscarinic side effects in patients taking medicines with antimuscarinic effects such as MAOIs, amantadine, clozapine, tricyclic antidepressants and nefopam. The simultaneous use of two or more of these may increase the risk of side effects such as dry mouth, urinary retention, and constipation. Concurrent use can also lead to confusion in the elderly. Anticholinergic medicines can delay the absorption of other medicines given at the same time. The simultaneous use of anticholinergic medicines and digoxin tablets that dissolve slowly can lead to that digoxin levels will be higher in serum. Domperidone/Metoclopramide: counteracting effect on gastrointestinal activity. Ketoconazole: Reduced absorption of Ketoconazole. Levodopa: Absorption of levodopa may decrease. Memantine: The effect may be amplified during simultaneous use. Use with other medicines during anaesthesia: Glycopyrrolate as in GLYCOSTOM has been used clinically with at least the following medicines: a barbiturate (sodium thiopental), narcotic analgesics (morphine, alphaprodine hydrochloride, fentanyl), sedative/tranquiliser (droperidol, diazepam), gaseous anaesthetics (nitrous oxide), volatile liquid anaesthetics (diethyl ether, halothane, methoxyflurane, enflurane), parenterally-acting skeletal muscle relaxants (succinylcholine, gallamine, d-tubocurarine, pancuronium), cholinergic medicines (neostigmine, pyridostigmine) and other anticholinergics (atropine).

Pregnancy: There are no or limited amount of data from the use of glycopyrronium bromide in pregnant women. Animal studies are insufficient with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of GLYCOSTOM during pregnancy.

Breastfeeding: Glycopyrronium bromide is excreted in human milk, but at therapeutic doses of GLYCOSTOM no effects on the breastfed newborns/infants are anticipated.

Fertility: There are no data on how glycopyrronium bromide affects human fertility.

GLYCOSTOM is used in anaesthesia. Patients are not expected to drive or use machines under the influence of the medicine. Administration of GLYCOSTOM may cause drowsiness, visual disturbances and other effects that impair the ability to drive and use machines. These activities should not be performed until the patient is recovered from these undesirable effects.

a. Summary of the safety profile: Adverse reactions listed by System Organ Class. Frequencies are defined using the following convention: frequent; less frequent; frequency unknown (cannot be estimated from the available data).

b. Tabulated summary of adverse reactions:

Reporting of suspected adverse reactions: Reporting suspected adverse reactions after authorisation of the medicine is important. It allows continued monitoring of the benefit/risk balance of the medicine. Health care providers are requested to report any suspected adverse drug reactions to SAHPRA via the Med Safety APP (Medsafety X SAHPRA) and eReporting platform (who-umc.org) found on SAHPRA website.

Symptoms: Peripheral anticholinergic effects.

Treatment: To combat peripheral anticholinergic effects, a quaternary ammonium anticholinesterase such as neostigmine methyl sulphate may be given in a dose of 1,0 mg for each 1,0 mg of GLYCOSTOM known to have been administered.