Topical

• Peripheral tissue activity
• Systemic side effects less likely
• If analgesic, applied directly over painful site
• Insignificant serum levels

Transdermal

• Systemic activity
• Potential for adverse effects
• If analgesic, may be applied away from painful site
• Serum levels necessary for effect

Medications that relieve pain, reduce inflammation, and relax muscles can have side effects that are detrimental to athletic performance, such as drowsiness. However, when these medications are administered topically, the therapeutic benefit can be enhanced while significantly reducing the risk of adverse effects.

For example, research has shown that topically-applied ketoprofen provides a high local concentration of drug below the site of application but decreases systemic exposure and significantly reduces the risk of gastrointestinal upset or bleeding. When properly compounded into an appropriate base, tissue concentrations of ketoprofen were found to be 100-fold greater below the application site (knee) compared to systemic concentrations. Muscle relaxants can be similarly prepared to minimize the risk of drowsiness.

To avoid the risks of COX-2 inhibitors, our pharmacy can compound topically applied NSAIDs such as ibuprofen and ketoprofen. Topical NSAIDs have a safety profile which is superior to oral formulations. Topical NSAID administration offers the advantage of local, enhanced delivery to painful sites with a reduced incidence of systemic adverse effects.

Topical preparations can be customized to contain a combination of medications to meet the specific needs of each patient.

Topical NSAIDs for Acute & Chronic Pain

Topical non-steroidal anti-inflammatory drugs have a lower incidence of gastrointestinal adverse effects than the same drugs when they are taken orally. The low incidence of systemic adverse effects for topical NSAIDs probably results from the much lower plasma concentration from similar doses applied topically to those administered orally. Topical application of ibuprofen resulted in measurable tissue concentrations in deep tissue compartments, more than enough to inhibit inflammatory enzymes. Topical NSAIDs have not been associated with renal failure.

BMJ. 1995 Jul 1;311(6996):22-6

The following article concluded: “topical non-steroidal anti-inflammatory drugs are effective in relieving pain in acute and chronic conditions.”

BMJ 1998 Apr 4;316(7137):1059

The following article reports “the systemic concentrations of ketoprofen have also been found to be 100 fold lower compared to tissue concentrations below the application site in patients undergoing knee joint surgery. Topically applied ketoprofen thus provides high local concentration below the site of application but lower systemic exposure.”

Pharm Res. 1996 Jan;13(1):168-72

Analgesic gels and sprays can be compounded to reduce pain and bleeding secondary to lacerations. The search for a “topical anesthetic that affords painless, safe application, does not contain narcotics or controlled substances, and has a maximum safety with complete anesthesia” revealed that LAT gel (lidocaine, adrenaline, tetracaine) is superior to preparations containing cocaine for topical anesthesia in laceration repair. Epinephrine (adrenaline) in the gel helps to stop bleeding secondary to injury.

Iontophoresis facilitates delivery of medications into the tissues beneath the skin by electronic transport of ionized drugs in solution. Acetic acid iontophoresis is effective in the treatment of heel pain. Iontophoresis of dexamethasone for plantar fasciitis should be considered when more immediate results are needed. Iontophoresis has also been used to successfully treat plantar hyperhidrosis.

Phonophoresis is a technique that combines topical drug therapy with ultrasound to achieve therapeutic drug concentrations in muscle and other tissues beneath the skin. Ultrasound gels can be formulated to contain medications such as anti-inflammatories and/or anesthetics.

Pregame rubs can be compounded to contain substances such as emu oil and anti-spasmodic drugs. Emu oil is a moisturizer that can improve healing of injured skin.

Hemorrhoids are particularly problematic for catchers, coaches, and others who are regularly in a squatting position. Treatment often involves use of a novel dosage form known as the “rectal rocket,” a suppository that permits simultaneous internal and external application of anti-inflammatories, anesthetics, antibiotics, or other medications.

Hyperhidrosis Therapy

Excessive perspiration is a concern for many athletes, as well as members of dance teams and marching bands. Numerous topical treatment options exist.

Primary hyperhidrosis (excessive perspiration) is a physically and emotionally distressing condition which involves mainly the palms, soles, and axillae. Oral anticholinergic agents and beta-blockers may be effective for controlling or reducing profuse sweating, but also carry significant side effects. Topical therapies may be the most practical and most common treatment for hyperhidrosis, but many agents that have proven useful in clinical trials are not commercially available.

Placebo-controlled trials have shown that topically applied 20% aluminum chloride hexahydrate significantly reduces the symptoms of hyperhidrosis in 60%-100% of patients. Skin irritation can be minimized with 1% hydrocortisone cream or by compounding 20% aluminum chloride in a 4% salicylic acid gel base, instead of in anhydrous alcohol base (as is the commercial product Drysol®).

Luh and Blackwell of the Dept. of Internal Medicine, University of Texas Medical Branch at Galveston describe a healthy, active 27-year-old male resident physician who had excessive facial sweating with minimal exertion or stress. The sweating was especially pronounced on the forehead, nose, and upper lip. Daily topical application of a 0.5% glycopyrrolate solution to the face and forehead significantly reduced facial sweating after the first treatment, without any discomfort to the skin. No loss of efficacy was seen after multiple face washings. Facial hyperhidrosis recurred after withdrawal of the glycopyrrolate for 2 days, confirming its therapeutic effect. Two years later, he continues to use glycopyrrolate as needed.

Mayo Clin Proc 1986 Dec;61(12):951-6
South Med J 2002 Jul;95(7):756-8
Ann Pharmacother 1995 May;29(5):489-92
Intl J Pharm Comp 2001 Jan/Feb;5(1):28-9

The following list is just a few of the preparations that we can compound for sports medicine. All formulations are customized to meet the unique needs of each individual; therefore, we can consider the athlete’s lifestyle and environmental factors when formulating medications. Our compounding professionals can choose the best base to administer the active ingredients, or consult with the prescriber to determine the most appropriate route of administration to solve a specific problem.

• Clotrimazole in DMSO solution
• Cyclobenzaprine/Ketoprofen transdermal gel
• Dexamethasone iontophoresis solution
• Fluconazole/Ibuprofen topical gel
• Ketamine/Gabapentin transdermal gel
• Ketoprofen 10% topical gel
• LAT topical gel
• Lidocaine/Hydrocortisone “rectal rocket” suppository
• Nutritional Supplements
• Rehydration Drinks