Glycopyrrolate and Oxybutynin are both anticholinergic medicines used to treat hyperhidrosis, a skin condition that causes excessive sweating. A patient must be actively managing their hyperhidrosis with a doctor in order to obtain these types of medications, as they are only available by prescription. Both Glycopyrrolate and Oxybutynin are most often used as oral medications to treat hyperhidrosis, although they can be given in other forms. Neither drug is specifically approved by the FDA for use in the treatment of hyperhidrosis, but they are commonly used off-label for this purpose.
Anticholinergics agents comprise a group of medications that work by affecting how the body is able to use the neurotransmitter acetylcholine. Specifically, anticholinergics interrupt acetylcholine from being used at muscarinic receptors throughout the body by binding with it. This action is called competitive inhibition. Muscarinic receptors are located throughout the autonomic nervous system, and spread out over the whole body, which is why anticholinergics are responsible for such widespread effects. The autonomic nervous system is the part of the nervous system that governs involuntary actions, like the movement of smooth muscle, breathing, heart rate, and many other functions. It is also responsible for regulating sweat production, which is why anticholinergic medications can be useful in the treatment of hyperhidrosis.
There are several types of anticholinergics, although most are not used in the treatment of hyperhidrosis. Glycopyrrolate and Oxybutynin are the two most common anticholinergic medications used to treat excessive sweating. Other types of anticholinergic medicines, like scopolamine and atropine, can cross the blood-brain barrier and cause more unwanted neurological side effects than glycopyrrolate. While there are other anticholinergics that can be used to treat hyperhidrosis, they are not available in the United States. The most studied anticholinergic agent, other than glycopyrrolate and oxybutynin, is called methantheline bromide, and it has had some promising results in Germany.
The Specifics of Each Medication
Glycopyrrolate (sold under the brand name Robinul) is one of the anticholinergics used most often in the treatment of hyperhidrosis, although this varies widely between doctors and studies. Patients are usually given glycopyrrolate in pill form and instructed to take 1 to 2 mg twice a day. If needed, patients can increase the dose by 1 mg per day at two-week intervals until the therapeutic dose is reached. The normal dosage range is usually between one and eight mgs per day. Many times patients are limited in the amount of glycopyrrolate they are able to take due to side effects that increase as the dose increases. There are several possible side effects, but the most common is dry mouth. This is because glycopyrrolate dries up bodily secretions, which is beneficial when attempting to reduce sweat production but can lead to aggravating side effects. Glycopyrrolate can also cause dry eyes, constipation, nausea and several other issues. Patients can drink more water, use mints, take eye-drops and increase fiber consumption to fight address side effects. Another limiting factor for the use of glycopyrrolate is its high cost.
The effectiveness of glycopyrrolate is often related to the dose a patient is able to handle. One study on the effectiveness of glycopyrrolate found that out of 19 patients 80% responded to treatment. However, one third of the patients had to stop treatment due to side effects. Other studies have found that the drug is effective in reducing sweating but that side effects often hinder treatment. Glycopyrrolate is often chosen as a second, or third line therapy for hyperhidrosis that causes excessive sweating of the palms, soles, and armpits. It is one of the first line treatments for craniofacial hyperhidrosis. Many times, using glycopyrrolate in conjunction with other therapies increases patient satisfaction.
Oxybutynin (brand name Ditropan) is the other most commonly used anticholinergic used in the treatment of hyperhidrosis. When being used orally to treat hyperhidrosis, oxybutynin is typically prescribed in 5 to 10 mg doses and taken daily. It can be used in amounts of 15 to 20 mgs a day if needed. It is also available as a topical gel, slow-release tablet, and as a transdermal patch. Oxybutynin has similar side effects when compared to glycopyrrolate. However, it is able to penetrate into the central nervous system (CNS) more easily so it can also have some added CNS side effects. These include dry mouth, constipation, somnolence, confusion and other potential effects. Oxybutynin is a relatively inexpensive drug so that can sometimes make it more accessible to patients.
Oxybutynin is found to be effective in treating the symptoms of hyperhidrosis but, like other anticholinergic drugs, it is limited by side effects. One study of 50 patients using oxybutynin to treat palmar and axillary hyperhidrosis found that 70% of patients reported improvements in those areas. Interestingly, 90% of the patients also reported improvement of plantar sweating. Side effects were noted as moderate to severe in 35% of the patients by the six week mark of the study. This indicates that oxybutynin is effective in reducing sweat production, but that, when used orally it can be limited by the side effects it can cause. Another study found that 60% of their patients showed improvement in their quality of life compared to only 27% in the placebo group, when low doses of oxybutynin were given. If patients can find relief at lower doses than this can mitigate the drawbacks caused by side effects.
Local Treatments that Use Glycopyrrolate and Oxybutynin
All oral medications for hyperhidrosis will cause systemic side effects throughout the body because of how they work. This can often make them less desirable treatment options. Sometimes, this is necessary, like in the case of a patient who has generalized all-over sweating instigated by a medication that causes hyperhidrosis as a side effect. However, both glycopyrrolate and oxybutynin are available in other forms that allow them to be used locally. Both drugs are available to be used in conjunction with an iontophoresis machine when being used to treat palmar and plantar hyperhidrosis. The electrical current from the iontophoresis machine aids the skin in absorbing the medications locally. Topical creams are available containing both medications but their effectiveness is currently unclear as the medications may have trouble penetrating the skin barrier in this form. A new product called Qbrexza uses glycopyrrolate on a medicated wipe that can be used once a day to prevent sweating.
Future Uses in the Treatment of Hyperhidrosis
There are various future treatments and research for hyperhidrosis that involve the use of both glycopyrrolate and oxybutynin. The most notable of these future treatments is the use of glycopyrrolate in a topical form which would be able to penetrate into eccrine glands. The cream would contain 1% or 2% glycopyrrolate. Oxybutynin is also being studied and potentially developed into a topical cream. Researchers are also looking into developing a glycopyrrolate pad to relieve sweating symptoms.
Recently, a product called Qbrexza (created by Dermira) was released and it uses Glycopyrronium Tosylate, a topical form of anticholinergic medication, on a wipe to reduce sweating. It is only marketed for underarm use, but it may have interesting implications for the future of hyperhidrosis treatment. For those who are interested in medicated antiperspirant wipes, but who don’t want to deal with prescription medications like Qbrexza, there are now over-the-counter antiperspirant wipes available from brands like Carpe.
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