What are NSAIDs?

oral NSAIDsNSAID is an abbreviation that stands for nonsteroidal anti-inflammatory drugs. They work by inhibiting the production of prostaglandins, which is responsible for promoting pain, inflammation, and fever in our bodies. People with joint conditions such as arthritis often take over the counter NSAIDs such as ibuprofen to relieve joint pain and inflammation.

Are NSAIDs safe?

Taking oral NSAIDs often can be harmful to your health. The FDA black box warning states that NSAIDs may cause an increased risk of heart attack, stroke, high blood pressure, gastric ulcers, and gastric bleeding. It should not be used during the 3rd trimester of pregnancy, pre-surgery, or with any anticoagulants due to risk of excessive bleeding. Fortunately, adverse effects of NSAIDs are based on dose. Taking higher doses will result in a higher overall risk. The recommended daily dose for ibuprofen, for example, is not to exceed 1,200 milligrams per day. Granting all this, it is recommended that NSAIDs are used at the lowest effective dose for the shortest amount of time.

The advantage of transdermal NSAIDs

anti-inflammatory creamTransdermal creams or gels can be used to deliver NSAIDs through the skin into underlying joints or tissues to relieve pain and inflammation. The advantage with the transdermal NSAIDs is that they are more effective in treating localized pain than oral NSAIDs. As stated earlier, the majority of people who take oral NSAIDs are battling localized pain such as joint pain from arthritis. With arthritis, soft tissues around a joint become inflamed, causing pain and stiffness in that area. Oral NSAIDs will temporarily help relieve the pain by reducing inflammation. But taking NSAIDs orally will disperse the drug throughout the entire body, which lessens its effectiveness for localized pain. The best route of administration to treat localized pain is transdermal because the drug target will be in the tissue right below the site of application.

Another advantage with transdermal NSAIDS is that they are less likely to cause side effects the way that oral NSAIDs can. When we take medication orally, it gets absorbed by our digestive system. This is where we see side effects such as gastric ulcers and gastric bleeding. The medication then travels to the liver and gets metabolized before it reaches systemic circulation (the rest of the body). This is where we see systemic side effects such as an increased risk of heart attack, stroke, and high blood pressure. Transdermal NSAIDs does not necessarily produce a significant systemic drug level, therefore is less likely to cause systemic side effects.

PLO or Lipoderm?

Transdermal NSAIDs can be compounded in 2 forms, either as a Pluronic Lecithin organogel (PLO) or as a Lipoderm cream. PLO tends to have a tacky feel and separates upon refrigeration but it is cheaper and contains only a few ingredients. Lipoderm has a smooth consistency and is stable at room temperature and under refrigeration. It is slightly more expensive than PLO and contains a lot more ingredients including wheat. People will have their own preference when it comes to choosing between PLO and Lipoderm. Those with gluten intolerance will likely choose PLO. People who prefer the smooth and creamy feel will choose Lipoderm. As for effectiveness, they are both on par when it comes to transdermal drug delivery.

Where can I get transdermal NSAIDs?

There are currently no over the counter transdermal NSAIDs available in the United States since it has yet to be approved by the FDA. But compounded transdermal NSAID can be prescribed by your doctor. The most common transdermal NSAIDs are ketoprofen, ibuprofen, and piroxicam. They can be compounded from 5% up to 20% in PLO or Lipoderm. They can even be combined with each other or with anesthetics such as ketamine or muscle relaxers such as cyclobenzaprine to further relieve pain. Ask your doctor about compounded transdermal NSAIDs for a safe and effective way to manage localized pain.

References

    • Drugs.com. (2015, June 25) Ibuprofen Uses, Dosage & Side Effects [Web]. Retrieved from http://www.drugbank.ca/drugs/DB01050
    • Drugbank. (2015, June 25) acetaminophen, ibuprofen, ketoprofen, morphine [web]. Retrieved from http://www.drugbank.ca
    • Fox, Shelley C. Pharmaceutics. London: Pharmaceutical Press, 2014. Print.
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