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The new topicals – So much more than pain relief & pediatrics in the age of polypharmacy

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Christopher Juozaitis is Chief Clinical Officer AdhereRx Inc. and co-owner Howe Sound Pharmacy, Gibson’s BC

Why should pharmacists consider topical options more often?

We are all well aware of the limitations of oral medications - namely, that a well-functioning digestive system will destroy and metabolize most of the administered dose before it can be distributed to the target sites, and that at the same time some common medications can also cause some irritation and damage to the GI tract. In addition, we are seeing an increasing prevalence of GI-related disorders (IBS, leaky gut) that can significantly alter the absorption of medications. Topical alternatives can overcome these limitations and reduce inter-patient variability in pharmacokinetics, which ultimately provide better efficacy and fewer adverse effects.

How do the new transdermal delivery systems work?

Conventional topical medications are generally only employed for localized topical conditions, such as eczema or psoriasis, due to the effectiveness of the stratum corneum layer of our skin as a barrier to the outside world. Transdermal penetration could only occur with small, lipophilic molecules, and even then, most of the dose is lost prior to absorption. The new transdermal products utilize features such as reservoirs, chemical enhancers, and encapsulation systems - alone or in combination - to allow for even large, hydrophilic molecules (i.e., most medications) to penetrate into target tissues. Encapsulation in particular provides many advantages, as it protects the active molecule from degradation, can contain other molecules, may be formulated in layers to provide timed-release, and minimizes irritation to the surrounding tissues. These products can be formulated to specifically target subdermal tissues such as nerves and muscles for local effects, or to blood vessels for systemic effects.

What OTC products should pharmacies be looking to add to their shelves?

It is important to have an assortment of OTC analgesics, but don’t stop there. Rutin (from buckwheat) is anti-inflammatory that blocks five pain pathways, has rapid onset, and has minimal adverse effects. It is a safe and effective alternative to commonly used diclofenac, salicylate, and menthol products and is indicated for injuries, arthritis and other forms of muscle and joint pain. Encapsulated capsaicin is delivered more effectively to the nerve cells and does not cause the skin irritation associated with traditional capsaicin. It is effective for nerve pain from shingles, diabetic neuropathy, and sciatica, but patients should be advised to avoid occlusion as it does generate heat. Delivra, the company behind LivRelief has announced an interesting new OTC topical pain cream that blends both pain relievers into a single tube.  We discovered recently that the LivRelief line also offers the only OTC topicals we are aware of to treat varicose veins and for wound healing. An isolate of witch hazel bark that acts locally as the astringent. It can help reduce the appearance of varicose veins and edema when used consistently for several weeks (good for sandal season!). The wound healing cream uses a number of antioxidant botanical extracts that together stimulate fibrinogen and collagen growth, reduce inflammation, control bleeding, and reduce infection. It is a great alternative to antibiotics or steroids, and can be used on open wounds, bed sores, burns, ulcers, and scars.

Are there any new prescription transdermal products?

Some of the most exciting prescription transdermal products are available as compounds. Existing and emerging compounding suppliers offer an ever-expanding selection of bases - including those that utilize encapsulation technology - and active ingredients to create patient-specific products. Some interesting examples include topical meloxicam as an alternative to diclofenac, topical tadalafil for Reynaud’s disease, and topical metformin for diabetics who cannot tolerate the GI effects of oral therapy. In addition, the possibility of transdermal cannabinoids being available through pharmacies in the future should be considered. If your pharmacy doesn’t compound in-house, it is worthwhile to explore what your area’s compounding pharmacies can offer you and your patients.

How do I incorporate new topicals into my patient care plans?

Over-the-counter consults, prescription counselling, and medication reviews are excellent opportunities to educate patients on the benefits of topical alternatives. Start by identifying patients who are experiencing adverse effects or sub-therapeutic effects from oral therapies or conventional topicals, who have contraindications to available options, or who have GI-related disorders affecting oral absorption. Patients who prefer not to “take pills” or who have a long list of intolerances are often more open to using topical therapies, especially if the active ingredients are from natural sources. For example, a gabapentin or pregabalin prescription may lead to a recommendation for encapsulated capsaicin such as LivRelief Nerve Pain Cream, and a client who is allergic to NSAIDs may be interested in topical rutin (LivRelief Pain Cream). The literature tells us that some of the older topicals work for less than half of all patients, so having as many safe and effective options for your patients as possible is always good medicine.

Jennifer May, BSP, ACPR, RPh, INHC is a clinical pharmacist at Vancouver Coastal Health, and Christopher Juozaitis BSP, CGP, is Chief Clinical Officer AdhereRx Inc, co-owner Howe Sound Pharmacy, Gibson’s BC



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