Description
Glycopyrronium bromide or NVA 237 is a once-daily inhaled antimuscarinic bronchodilator newly approved by the European Commission for use in stable COPD. It is characterized by a quaternary ammonium structure, which reduces its oral bioavailability and, consequently, the systematic effects of any swallowed portion of the drug.
Animal studies suggest that there are fewer cardiovascular effects compared to tiotropium because of the higher affinity to M3 versus M2 muscarinic receptors. Human studies showed fast onset of action, sustained bronchodilatation for 24 h, reduced dynamic hyperinflation of the lungs, and improved exercise tolerance. Glycopyrronium bromide in COPD airways clinical trial series (GLOW1–3) are the major clinical trials studying the efficacy and safety of glycopyrronium[1].
Definition
ChEBI: (2R,3S)-glycopyrronium bromide is a glycopyrronium bromide that has (2R,3S)-configuration. The racemate, ritropirronium bromide, is used for treatment of chronic obstructive pulmonary disease. It is an enantiomer of a (2S,3R)-glycopyrronium bromide.
Side effects
The following reported adverse reactions are extensions of glycopyrronium bromide’s fundamentalpharmacological actions:
Cardiovascular: Tachycardia, ventricular fibrillation, bradycardia, palpitation and arrhythmia, hypertension, hypotension, cardiac arrest, heart block, prolonged QTc interval.
Dermatological: Flushing and inhibition of sweating. Severe allergic reactions or drug idiosyncrasies including urticaria and other dermal manifestations, pruritus, dry skin.
Gastrointestinal: Nausea, vomiting, dry mouth, constipation, taste alterations, including loss of taste.
Genitourinary: Urinary hesitancy and retention, impotence.
Ocular: Blurred vision due to mydriasis, cycloplegia, photophobia, increased ocular tension.
Nervous System: Inhibition of transmission at neuromuscular junction, headache, nervousness, drowsiness, dizziness, seizure, insomnia, some degree of mental confusion, especially in the elderly, hyperexcitability in children.
Pregnancy and perinatal: Suppression of lactation.
Respiratory System: Respiratory arrest.
General: Hyperpyrexia, bloated feeling, anaphylaxis/anaphylactoid reaction, hypersensitivity. Injection site reactions including pruritus, oedema, erythema, pain have been reported rarely.
