CHAPTER 32 TOPICEUTICALS Brad Galer, MD OVERVIEW 1. What is the history of topicals (topiceuticals) as analgesics? Evidence shows that since the dawn of man humans have been grinding plants and herbs into poultices and liniments to treat ailments such as inflammation, itch, and pain. Ancient cultures from around the world, including Egyptians, Chinese, Romans, Indians, and Native Americans, have utilized plants in their environment to formulate externally applied analgesics. Topical formulations of plant-derived natural products that have been used for centuries and are still used today as analgesics include camphor, capsaicin, and menthol. 2. How is a topiceutical medication different from a transdermal drug? Medications formulated as either a topical (topiceutical) or a transdermal preparation must be delivered across the skin, the body’s largest organ, which is designed to keep out foreign substances (including medications). These types of medications differ in what happens to the medication once it penetrates (absorbs) through the skin. Transdermal preparations are formulated to deliver medication across the skin and into the bloodstream; the bloodstream carries the medication throughout the body for a body-wide or systemic effect. Basically, with transdermal drug systems, the body is exposed to medication as if a tablet were swallowed and dissolved in the stomach. These kinds of patches can be applied to any skin area (according to the product instructions) because the medication will eventually find the bloodstream for delivery to the targeted area in the body. An example is the Durogesic patch (Janssen Pharmaceutica, Titusville, N.J.). A topical patch must be placed directly over the painful area. Medication in a topiceutical does not reach the bloodstream in an amount to produce any meaningful effect. Rather, topical medications penetrate the skin and remain in the upper layers of the skin to produce local effects when used according to the package instructions. Care must be taken when applying topical medications because application of excessive amounts for extended periods of time over a larger area can promote increased medication penetration and result in amounts in the bloodstream that cause side effects. Once the medication crosses the skin, it is where it needs to be and works on tissues (muscles, ligaments, tendons, nerves) that lie directly underneath the skin application area. Examples of topiceuticals include Bengay spa cream (Pfizer, N.Y.), Lidoderm patch (Endo Pharmaceuticals, Chadds Ford, Pa.), and EMLA cream (AstraZeneca, Wilmington, Del.). Delivering medications directly to the tissues directly under the skin application area can be an advantage. Topiceuticals can be safely added to an existing pain treatment plan without worry about drug-drug interactions with other body-wide (systemic) analgesics. Because it is not uncommon for pain patients to require several pain medications, the flexibility to add topiceuticals to the mix is helpful. The risk of unwanted body-wide side effects is also significantly reduced. 3. What are the various topical formulations available for the treatment of pain? Topical formulations to treat pain can be obtained as both prescription and nonprescription(e.g., over-the-counter) drugs. Prescription topical pain relievers include creams and skin patches. Skin patches vary in appearance from a soft, felt, white rectangular patch to a pink, flesh-colored, oval patch that heats up when exposed to air. Over-the-counter (OTC) medications include creams, ointments, lotions, rub-on sticks, gels, sprays, and patches. 4. What are the advantages and disadvantages of using topical medications? There are numerous advantages associated with delivering medication across the skin with little body-wide activity. Patients are able to place the medication directly at the location where it is needed. This reduces the level to which the entire body is exposed to the medication. Low body-wide exposure leads to reduced body-wide side effects and low risk for drug-drug interactions. Topical products are generally easy to use and begin to work relatively quickly. They are widely available in a number of different dosage formulations both by prescription and over the counter at the pharmacy. These dosage formulations do not require the use of needles and therefore are nonpainful when applied. Topiceuticals offer an alternative for patients who fear needles and who are unable to swallow tablets and capsules (e.g., patients with mouth sores, children, or older persons). Some skin patches can be cut to fit exactly over the painful skin area. 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CHAPTER 32 TOPICEUTICALS Brad Galer, MD OVERVIEW 1. What is the history of topicals (topiceuticals) as analgesics? Evidence shows that since the dawn of man humans have been grinding plants and herbs into poultices and liniments to treat ailments such as inflammation, itch, and pain. Ancient cultures from around the world, including Egyptians, Chinese, Romans, Indians, and Native Americans, have utilized plants in their environment to formulate externally applied analgesics. Topical formulations of plant-derived natural products that have been used for centuries and are still used today as analgesics include camphor, capsaicin, and menthol. 2. How is a topiceutical medication different from a transdermal drug? Medications formulated as either a topical (topiceutical) or a transdermal preparation must be delivered across the skin, the body’s largest organ, which is designed to keep out foreign substances (including medications). These types of medications differ in what happens to the medication once it penetrates (absorbs) through the skin. Transdermal preparations are formulated to deliver medication across the skin and into the bloodstream; the bloodstream carries the medication throughout the body for a body-wide or systemic effect. Basically, with transdermal drug systems, the body is exposed to medication as if a tablet were swallowed and dissolved in the stomach. These kinds of patches can be applied to any skin area (according to the product instructions) because the medication will eventually find the bloodstream for delivery to the targeted area in the body. An example is the Durogesic patch (Janssen Pharmaceutica, Titusville, N.J.). A topical patch must be placed directly over the painful area. Medication in a topiceutical does not reach the bloodstream in an amount to produce any meaningful effect. Rather, topical medications penetrate the skin and remain in the upper layers of the skin to produce local effects when used according to the package instructions. Care must be taken when applying topical medications because application of excessive amounts for extended periods of time over a larger area can promote increased medication penetration and result in amounts in the bloodstream that cause side effects. Once the medication crosses the skin, it is where it needs to be and works on tissues (muscles, ligaments, tendons, nerves) that lie directly underneath the skin application area. Examples of topiceuticals include Bengay spa cream (Pfizer, N.Y.), Lidoderm patch (Endo Pharmaceuticals, Chadds Ford, Pa.), and EMLA cream (AstraZeneca, Wilmington, Del.). Delivering medications directly to the tissues directly under the skin application area can be an advantage. Topiceuticals can be safely added to an existing pain treatment plan without worry about drug-drug interactions with other body-wide (systemic) analgesics. Because it is not uncommon for pain patients to require several pain medications, the flexibility to add topiceuticals to the mix is helpful. The risk of unwanted body-wide side effects is also significantly reduced. 3. What are the various topical formulations available for the treatment of pain? Topical formulations to treat pain can be obtained as both prescription and nonprescription(e.g., over-the-counter) drugs. Prescription topical pain relievers include creams and skin patches. Skin patches vary in appearance from a soft, felt, white rectangular patch to a pink, flesh-colored, oval patch that heats up when exposed to air. Over-the-counter (OTC) medications include creams, ointments, lotions, rub-on sticks, gels, sprays, and patches. 4. What are the advantages and disadvantages of using topical medications? There are numerous advantages associated with delivering medication across the skin with little body-wide activity. Patients are able to place the medication directly at the location where it is needed. This reduces the level to which the entire body is exposed to the medication. Low body-wide exposure leads to reduced body-wide side effects and low risk for drug-drug interactions. Topical products are generally easy to use and begin to work relatively quickly. They are widely available in a number of different dosage formulations both by prescription and over the counter at the pharmacy. These dosage formulations do not require the use of needles and therefore are nonpainful when applied. Topiceuticals offer an alternative for patients who fear needles and who are unable to swallow tablets and capsules (e.g., patients with mouth sores, children, or older persons). Some skin patches can be cut to fit exactly over the painful skin area. Disadvantages Only gold members can continue reading. Log In or Register to continue Share this:Click to share on Twitter (Opens in new window)Click to share on Facebook (Opens in new window) Related Related posts: Neuroimaging in the Patient with Pain Pharmacologic Management Tension-Type Headache Neuropathic Pain Cancer Pain Syndromes Temporary Neural Blockade Stay updated, free articles. Join our Telegram channel Join Tags: Pain Management Secrets Jun 14, 2016 | Posted by admin in PAIN MEDICINE | Comments Off on Topiceuticals Full access? Get Clinical Tree
