Compounded transdermal medications have been shown to be effective in the treatment of neuropathic, musculoskeletal, arthritic, and postoperative pain, among other pain-related conditions, and they continue to be explored as a viable alternative option for the management of pain related to a variety of conditions.
Compounded transdermal medications effectively reduce pain symptoms while offering a decreased risk of adverse effects commonly associated with oral pain medication, and they may help decrease the risk of drug abuse and addiction.
Compounded transdermal preparations for pain management can provide healthcare providers with individualized and potentially more effective options for the treatment of both acute and chronic pain-related conditions1.
Utilizing transdermal compounds for pain management presents opportunities to customize regimens to meet the challenges of treating pain. Potential benefits include side effect minimization, combination of multiple active ingredients in a single formulation (thereby providing greater convenience and potentially better efficacy than single-ingredient products), application of the medication directly to the site of pain, easy titration to meet individual patient needs, lower systemic absorption, and improvement of patient adherence to treatment regimens1.
Potential benefits of transdermal compounded medication:
On many occasions, multiple medications can be combined into a single dose of a specially prepared compound that combines the medications into a single capsule or topical preparation, providing greater convenience for the patient2.
Lidocaine is a widely used antiarrhythmic and amide-type local anesthetic. As an anesthetic agent, it is available as an ointment, jelly, patch, or aerosol for topical use, as an oral solution, and as an injection. Lidocaine is classified as a class Ib antiarrhythmic. It may be considered for ventricular fibrillation (VF) and pulseless ventricular tachycardia (pVT) that is unresponsive to cardiopulmonary resuscitation (CPR), defibrillation, and vasopressor therapy3.
Mechanism of Action
Lidocaine's antiarrhythmic effects result from its ability to inhibit the influx of sodium through the "fast" channels of the myocardial cell membrane, thereby increasing the recovery period after repolarization. Lidocaine suppresses automaticity and decreases the effective refractory period and the action potential duration in the His-Purkinje system at concentrations that do not suppress automaticity at the SA node. The drug suppresses spontaneous depolarizations in the ventricles by inhibiting reentry mechanisms, and it appears to act preferentially on ischemic tissue. Lidocaine shortens the refractory period, unlike procainamide, which lengthens it. Also, lidocaine does not possess vagolytic properties4.
Ketoprofen is a pain reliever that is used to treat a variety of conditions. It also helps with arthritis pain, swelling, and stiffness. It functions by preventing the development of those natural substances that induce inflammation in your body. This influence aids in the reduction of swelling, suffering, and fever. Whether you're dealing with a long-term illness like arthritis5.
Benzocaine is used in application to accessible mucous membrane except the eyes. These products are used for topical anesthesia and mild pain control. Benzocaine is more likely than other local anesthetics to cause contact sensitization. The potential for sensitization increases with the duration of contact, and can be avoided with appropriate application technique. These products are not intended for prolonged application time or use6.
Mechanism of Action
Benzocaine is a local anesthetic that cause a reversible blockade of nerve conduction by decreasing nerve membrane permeability to sodium. This decreases the rate of membrane depolarization, thereby increasing the threshold for electrical excitability. The blockade affects all nerve fibers in the following sequence: autonomic, sensory, and motor, with effects diminishing in reverse order. Clinically, loss of function occurs as follows: pain, temperature, touch, proprioception, and skeletal muscle tone. Direct nerve membrane penetration is necessary for effective anesthesia, which is achieved by applying the anesthetic topically to the area to be anesthetized. While systemic absorption of local anesthetics can produce effects on the central nervous and cardiovascular systems, systemic absorption of benzocaine; lidocaine; tetracaine is expected to be minimal with appropriate use7.
1. Branvold A., Carvalho M., (2014) Pain Management Therapy: The Benefits of Compounded Transdermal Pain Medication. J Gen Practice 2: 188. doi:10.4172/2329-9126.1000188
2. Pain Management Compounding | Key Compounding Pharmacy. (n.d.). Key Compounding Pharmacy. https://www.keycompounding.com/pain-management-compounding
3. Link MS, Berkow LC, Kudenchuk PJ, et al. Part 7: Adult Advanced Cardiovascular Life Support: 2015 American Heart Association Guidelines Update for Cardiopulmonary Resuscitation and Emergency Cardiovascular Care. Circulation. 2015;132:S444-64.
4. Panchal AR, Berg KM, Kudenchuk PJ, et al. 2018 American Heart Association focused update on advanced cardiovascular life support use of antiarrhythmic drugs during and immediately after
5. Ketoprofen (2021, May 21). Healthline.https://www.healthline.com/health/ketoprofen-topical
6. Cetacaine Topical Anesthetic (benzocaine; lidocaine; tetracaine) package insert. Pennsauken, NJ: Cetylite Industries, Inc.; 2013 Apr.
7. Exactacain Topical Anesthetic Spray (benzocaine; lidocaine; tetracaine) package insert. Cumberland, RI: Onset Therapeutics; 2008 Sep.