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Glycopyrrolate

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Glycopyrrolate chemical structure
Glycopyrrolate

3-(2-cyclopentyl-2-hydroxy-2-phenylacetoxy)-1,1-dimethylpyrrolidinium
IUPAC name
CAS number
596-51-0
ATC code

A03AB02

PubChem
3494
DrugBank
APRD01000
Chemical formula {{{chemical_formula}}}
Molecular weight 318.431 g/mol
Bioavailability {{{bioavailability}}}
Metabolism {{{metabolism}}}
Elimination half-life 0.6–1.2 hours
Excretion 85% renal, unknown amount in the bile
Pregnancy category B
Legal status {{{legal_status}}}
Routes of administration oral, IV

Glycopyrrolate is a medication of the muscarinic anticholinergic group. It does not cross the blood brain barrier and consequently has no to few central effects. It is a synthetic quaternary amine. It is available in oral and intravenous (i.v.) forms.

With counterion, it is known as glycopyrronium bromide.[1]

PharmacologyEdit

Glycopyrrolate blocks muscarinic receptors,[2] thus inhibiting cholinergic transmission.

Medical usesEdit

In anesthesia, glycopyrrolate injection can be used as a preoperative medication in order to reduce salivary, tracheobronchial, and pharyngeal secretions, as well as decreasing the acidity of gastric secretion. It is also used in conjunction with neostigmine, a neuromuscular blocking reversal agent, to prevent neostigmine's muscarinic effects such as bradycardia.

It is also used to reduce excessive saliva (sialorrhea).[3][4][5]

It decreases acid secretion in the stomach and so may be used for treating stomach ulcers, in combination with other medications.

Use in treating asthma[6][7] and COPD[8] has been described.

It has been used topically and orally to treat hyperhidrosis.[9][10]

Side effectsEdit

Since glycopyrrolate reduces the body's sweating ability, it can even cause fever and heat stroke in hot environments. Dry mouth, difficulty urinating, headaches, diarrhea and constipation are also observed side effects of the medication.

The medication also induces drowsiness or blurred visions, an effect exacerbated by the consumption of alcohol.

ReferencesEdit

  1. Bajaj V, Langtry JA (July 2007). Use of oral glycopyrronium bromide in hyperhidrosis. Br. J. Dermatol. 157 (1): 118–21.
  2. Haddad EB, Patel H, Keeling JE, Yacoub MH, Barnes PJ, Belvisi MG (May 1999). Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways. Br. J. Pharmacol. 127 (2): 413–20.
  3. Mier RJ, Bachrach SJ, Lakin RC, Barker T, Childs J, Moran M (December 2000). Treatment of sialorrhea with glycopyrrolate: A double-blind, dose-ranging study. Arch Pediatr Adolesc Med 154 (12): 1214–8.
  4. Tscheng DZ (November 2002). Sialorrhea - therapeutic drug options. Ann Pharmacother 36 (11): 1785–90.
  5. Olsen AK, Sjøgren P (October 1999). Oral glycopyrrolate alleviates drooling in a patient with tongue cancer. J Pain Symptom Manage 18 (4): 300–2.
  6. Hansel TT, Neighbour H, Erin EM, et al. (October 2005). Glycopyrrolate causes prolonged bronchoprotection and bronchodilatation in patients with asthma. Chest 128 (4): 1974–9.
  7. Gilman MJ, Meyer L, Carter J, Slovis C (November 1990). Comparison of aerosolized glycopyrrolate and metaproterenol in acute asthma. Chest 98 (5): 1095–8.
  8. Tzelepis G, Komanapolli S, Tyler D, Vega D, Fulambarker A (January 1996). Comparison of nebulized glycopyrrolate and metaproterenol in chronic obstructive pulmonary disease. Eur. Respir. J. 9 (1): 100–3.
  9. Kim WO, Kil HK, Yoon DM, Cho MJ (August 2003). Treatment of compensatory gustatory hyperhidrosis with topical glycopyrrolate. Yonsei Med. J. 44 (4): 579–82.
  10. Kim WO, Kil HK, Yoon KB, Yoon DM (May 2008). Topical glycopyrrolate for patients with facial hyperhidrosis. Br. J. Dermatol. 158 (5): 1094–7.


Template:Drugs for functional gastrointestinal disorders


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