What is the mechanism of action of glycopyrrolate for treating hyperhidrosis?

From the Guidelines

Glycopyrrolate treats hyperhidrosis by blocking acetylcholine receptors in sweat glands, specifically targeting muscarinic receptors to prevent acetylcholine binding and subsequent sweat production. As an anticholinergic medication, glycopyrrolate disrupts the neural signal that stimulates sweat production, resulting in decreased sweating throughout the body 1. The mechanism of action involves the inhibition of acetylcholine receptors on eccrine sweat glands, which are responsible for regulating body temperature and producing sweat in response to heat, stress, or other stimuli.

Key Points

• Glycopyrrolate is an anticholinergic medication that targets muscarinic receptors in sweat glands
• The medication works systemically, affecting all sweat glands and making it useful for generalized hyperhidrosis
• Treatment can be continuous for chronic hyperhidrosis or used as needed for situational sweating
• Side effects may include dry mouth, blurred vision, urinary retention, and constipation due to its anticholinergic properties

Although the provided study 1 focuses on the respiratory management of patients with neuromuscular weakness, it mentions the use of anticholinergic agents, including glycopyrrolate, for treating sialorrhea, which is excessive salivation. The same mechanism of action that reduces salivation can also decrease sweat production, making glycopyrrolate a potential treatment for hyperhidrosis. However, the study does not provide specific guidance on the use of glycopyrrolate for hyperhidrosis, and the recommended doses are for sialorrhea treatment.

Clinical Considerations

• Glycopyrrolate may be prescribed at doses of 1-2 mg taken orally 2-3 times daily, with dosage adjusted based on response and side effects
• The medication's anticholinergic properties can cause side effects, and patients should be monitored for these effects
• Glycopyrrolate may be less targeted than topical treatments for localized sweating, but it can be effective for generalized hyperhidrosis that affects multiple body areas

From the FDA Drug Label

The FDA drug label does not answer the question.

From the Research

Mechanism of Action of Glycopyrrolate for Hyperhidrosis

The mechanism of action of glycopyrrolate for treating hyperhidrosis involves:

• Blocking the activation of acetylcholine receptors in peripheral sweat glands, thereby reducing sweat production 2
• Inhibiting the muscarinic acetylcholine receptor, which is the primary receptor responsible for sweat gland stimulation 3
• Having both local and systemic effects on perspiration, as evidenced by the increased efficacy of bilateral glycopyrrolate iontophoresis compared to unilateral treatment 4

Key Findings

• Glycopyrrolate has been shown to be effective in reducing sweat production in patients with hyperhidrosis, with studies demonstrating its efficacy in various formulations, including oral, topical, and iontophoresis 5, 6, 4, 2
• The drug's anticholinergic properties make it suitable for treating hyperhidrosis, with minimal penetration of the blood-brain barrier and lack of phototoxicity, genotoxicity, and carcinogenicity 3
• Glycopyrrolate's mechanism of action is primarily related to its ability to block muscarinic acetylcholine receptors, which are involved in the regulation of sweat gland activity 3

Clinical Implications

• Glycopyrrolate has been approved by the US FDA for the treatment of primary axillary hyperhidrosis, and has been shown to be a safe and effective treatment option for patients with this condition 2
• The drug's efficacy and safety profile make it a suitable treatment option for patients with hyperhidrosis, particularly those who have not responded to other treatments 5, 6, 4, 2, 3