glycopyrronium

glycopyrrolate (glycopyrronium (UK))

Robinul, Robinul Forte

Pharmacologic class: Anticholinergic

Therapeutic class: Antispasmodic, antimuscarinic, parasympatholytic

Pregnancy risk category B

Action

Inhibits action of acetylcholine on muscarinic receptors that mediate effects of parasympathetic postganglionic impulses. This inhibition relaxes cardiac smooth muscle, inhibits vagal reflexes, and decreases tracheal and bronchial secretions.

Availability

Injection: 0.2 mg/ml

Tablets: 1 mg, 2 mg

Indications and dosages

Adjunct in peptic ulcer disorders

Adults: 1 mg P.O. t.i.d. or 2 mg (Forte) two to three times daily, to a maximum of 8 mg/day; or 0.1 to 0.2 mg I.M. or I.V. three or four times daily

To diminish secretions and block cardiac vagal reflexes before surgery

Adults and children ages 2 and older: 0.0044 mg/kg I.M. 30 to 60 minutes before anesthesia

Children ages 1 month to 2 years: 0.0088 mg/kg I.M. 30 to 60 minutes before anesthesia

To diminish secretions and block cardiac vagal reflexes during surgery

Adults: 0.1 mg I.V. May repeat as needed at 2- to 3-minute intervals.

Children: 0.004 mg/kg I.V., not to exceed 0.1 mg as a single dose. May repeat at 2- to 3-minute intervals.

To diminish or block cholinergic effects caused by anticholinesterase

Adults and children: 0.2 mg I.V. for each 1 mg neostigmine or 5 mg pyridostigmine. May give I.V. undiluted or with dextrose injection by infusion.

Off-label uses

• Sweating

Contraindications

• Hypersensitivity to drug

• Arrhythmias

• Chronic obstructive pulmonary disease

• GI disease, infection, atony or ileus

• Myasthenia gravis

• Glaucoma

• Obstructive uropathy

• Severe prostatic hypertrophy

Precautions

Use cautiously in:

• cardiovascular disease, heart failure, hypertension, renal or hepatic disease, Down syndrome, hyperthyroidism, hiatal hernia, ulcerative colitis, mild to moderate prostatic hypertrophy, autonomic neuropathy, spasticity, suspected brain damage

• pregnant or breastfeeding patients.

Administration

• Give oral dose 30 to 60 minutes before meals.

• For I.V. injection, give either undiluted or diluted with dextrose 5% or 10% in water or saline solution. Give each 0.2 mg over 1 to 2 minutes.

Keep resuscitation equipment on hand to treat curare-like effects of overdose.

Adverse reactions

CNS: weakness, nervousness, insomnia, drowsiness, dizziness, headache, confusion, excitement

CV: palpitations, tachycardia

EENT: blurred vision, photophobia, mydriasis, increased intraocular pressure, cycloplegia

GI: nausea, vomiting, constipation, abdominal distention, epigastric distress, heartburn, gastroesophageal reflux, dry mouth, paralytic ileus

GU: urinary hesitancy or retention, lactation suppression, erectile dysfunction

Skin: urticaria, decreased sweating or anhidrosis

Other: loss of taste, fever, allergic reaction, irritation at I.M. injection site, anaphylaxis, malignant hyperthermia

Interactions

Drug-drug. Amantadine, antihistamines, antiparkinsonian drugs, disopyramide, glutethimide, meperidine, phenothiazines, procainamide, quinidine, tricyclic antidepressants: additive anticholinergic effects

Patient monitoring

Check for signs and symptoms of anaphylaxis and malignant hyperthermia.

• Monitor neurologic and cardiovascular status.

Assess for curare-like effects (neuromuscular blockade leading to muscle weakness and possible paralysis), which indicate overdose.

• Assess fluid intake and output. Have patient void before each dose to avoid urinary retention.

Patient teaching

• Advise patient to take oral dose 30 to 60 minutes before meals.

Tell patient to immediately report signs and symptoms of serious adverse effects, especially anaphylaxis.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, and alertness.

• Tell patient to minimize GI upset by eating frequent, small servings of food and drinking adequate fluids.

• Advise patient to report urinary hesitancy or retention.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.

References in periodicals archive ?
Other treatment options include Botox injections in the armpits and hands; the oral medication glycopyrronium; laser surgery; and microwave thermolysis, in which electromagnetic energy is used to stop sweat glands from functioning.
Tenders are invited for electronic auction among small businesses and socially oriented non-profit organizations for the right to conclude a contract for the supply of medicines (glycopyrronium bromide) to provide citizens eligible for state social assistance in moscow
The other reason to get serious about addressing primary axillary hyperhidrosis in pediatric patients is the recent approval of glycopyrronium tosylate as a topical therapy, Dr.
Vectura and its co-development partner Sosei Co Ltd licenced QVM149, which combines the drugs indacaterol acetate and glycopyrronium bromide, to Novartis in 2005.
The company's approved treatment, QBREXZA (glycopyrronium) cloth, is indicated for pediatric and adult patients (ages nine and older) with primary axillary hyperhidrosis (excessive underarm sweating).
Bronchodilators, which improve lung function, decrease hyperinflation, and improve exercise performance by decreasing airway smooth muscle tone, are the cornerstone of COPD treatment and include short- and long-acting [[beta].sub.2]-agonists (SABAs [eg, albuterol/salbutamol and levalbuterol] and LABAs [eg, formoterol, indacaterol, olodaterol, and salmeterol]), and shortand long-acting muscarinic antagonists (SAMAs [eg, ipratropium bromide] and LAMAs [eg, aclidinium, glycopyrronium bromide, umeclidinium, and tiotropium]).
These medications improve pulmonary function and reduce acute bronchial exacerbations with good safety.[7] Glycopyrronium bromide and aclidinium bromide are two represent LAMAs.
THE FOOD AND DRUG Administration has approved glycopyrronium tosylate, an anticholinergic for the topical treatment of primary axillary hyperhidrosis in adults and children aged 9 years and older.
Further PK evaluations have also been published for inhaled drugs such as glycopyrronium [61], a LAMA, and AZD5423, a nonsteroidal glucocorticoid receptor modulator [86].
Trimbow is the first 3-in-1 combination inhaler containing an inhaled corticosteroid (ICS) / long-acting [beta]2-agonist (LABA) / long-acting muscarinic antagonist (LAMA) containing beclometasone dipropionate (BDP; 87mcg), formoterol fumarate (FF, 5mcg) and glycopyrronium (GB, 9mcg), administered as a twice-daily fixed-dose in a pressurised metered-dose inhaler (pMDI) extrafine formulation.
However, anticholinergic medicines unlicensed for hyperhidrosis--such as oxybutynin and glycopyrronium bromide--can also be prescribed if the doctor feels they might help .Possible side effects of anticholinergics include a dry mouth, blurred vision, stomach cramps, constipation and difficulty passing urine.
Analysis of chronic obstructive pulmonary disease exacerbations with the dual bronchodilator QVA149 compared with glycopyrronium and tiotropium (SPARK): A randomised, double-blind, parallel-group study.