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.

glycopyrrolate, glycopyrronium

an anticholinergic used to reduce gastric acid secretion and hypermotility.
References in periodicals archive ?
3M in collaboration and license revenue, which was primarily related to a portion of the $25M initial license payment received from Maruho pursuant to the exclusive license agreement entered into in September 2016 which granted Maruho the right to develop and commercialize glycopyrronium tosylate for the treatment of primary axillary hyperhidrosis in Japan.
In FLAME, 3,362 COPD patients who had at least one exacerbation in the preceding year were randomized to the LABA indacaterol (110 meg) plus the LAMA glycopyrronium (50 meg) once daily, or to the combination of the LABA salmeterol (50 mcg) and the ICS fluticasone (500 mcg) twice daily.
However, anticholinergic medicines unlicensed for hyperhidrosis--such as oxybutynin and glycopyrronium bromide--can also be prescribed if the doctor feels they might help .
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.
The company will be launching clinical trials for a new cardiology medication for premature newborn infants, and glycopyrronium a drug designed to combat sialorrhoea, or chronic pathological drooling in the first quarter.
Various treatment options available are topical applications like aluminium chloride, glutaraldehyde and glycopyrronium bromide, iontophoresis with tap water or anticholinergics, botulinum toxin injections, systemic anticholinergic drugs or sympathectomy.
One of the two ingredients in QVA149, glycopyrronium bromide, was approved in the EU in October 2012 as the Seebri Breezhaler, a once-daily maintenance dose of COPD.
Among the agents that are the most promising on this front, he said, are indacaterol plus glycopyrronium (QVA-149) and vilanterol plus GSK-573719.
These include Onbrez Inhalation Capsules 150 mcg (indacaterol maleate), which were launched in Japan on September 20, 2011, and, if approved, the investigational drugs NVA237 (glycopyrronium bromide) and QVA149 (fixed-dose combination of indacaterol maleate and glycopyrronium bromide), both of which are currently in Phase III development.
Hyoscine vs glycopyrronium for drying respiratory secretions in dying patients.