Compounded Pain Formulations: What is the Evidence?

Pain syndromes are among the most widespread, costly, and debilitating of all neurological disorders. The number of patients living with chronic pain is expected to increase with the aging population and with the rise in obesity and diabetes across the nation. This type of pain is often insensitive to the traditional pain pharmacopeia or surgical intervention. Over the last 10 years the number of prescriptions that have been compounded by pharmacists has increased dramatically. There are a number of drugs in the area of pain management that have been formulated and compounded by pharmacists to treat conditions such as diabetic neuropathy, fibromyalgia, postherpetic neuralgia, joint pain, arthritis, and a variety of other conditions. A significant portion of these compounded analgesic preparations is made up of topical/transdermal dosage forms such as gels and creams. While the efficacy and doses of these drugs in systemic dosage forms have been widely established, little is known about the permeation and efficacy of these compounds from topical/transdermal gels. This review will provide an overview of chronic pain as a disease, the mechanisms of chronic pain, current treatment approaches to chronic pain, and a discussion of the drugs that are typically compounded into these topical formulations and studied in clinical trials.

Compounded pain formulations: what is the evidence?

Pain syndromes are among the most widespread, costly, and debilitating of all neurological disorders. The number of patients living with chronic pain is expected to increase with the aging population and with the rise in obesity and diabetes across the nation. This type of pain is often insensitive to the traditional pain pharmacopeia or surgical intervention. Over the last 10 years the number of prescriptions that have been compounded by pharmacists has increased dramatically. There are a number of drugs in the area of pain management that have been formulated and compounded by pharmacists to treat conditions such as diabetic neuropathy, fibromyalgia, postherpetic neuralgia, joint pain, arthritis, and a variety of other conditions. A significant portion of these compounded analgesic preparations is made up of topical/transdermal dosage forms such as gels and creams. While the efficacy and doses of these drugs in systemic dosage forms have been widely established, little is known about the permeation and efficacy of these compounds from topical/transdermal gels. This review will provide an overview of chronic pain as a disease, the mechanisms of chronic pain, current treatment approaches to chronic pain, and a discussion of the drugs that are typically compounded into these topical formulations and studied in clinical trials.

In vitro skin penetration and skin content of progesterone from various topical formulations.

Progesterone has been compounded by pharmacists over the last decade using a variety of different dosage forms including, suppositories, troches, solutions, capsules, nasal sprays, creams, ointments, and gels. In particular, the topical/transdermal route has become very popular among physicians, compounders, and patients. There are a few studies in the medical literature that address the transdermal permeation of progesterone from topically applied dosageforms. The results are typically controversial with some studies showing permeation and others showing little to no permeation. Coupled with the high saliva levels that are often seen in patients undergoing topical/transdermal treatment with progesterone and the accompanying lack of progesterone blood levels, the transdermal route of delivery for progesterone is controversial. In this study, we examined the transdermal penetration of progesterone from four different formulations and the skin retention of progesterone in porcine skin. Our results indicate that only minute quantities of progesterone transdermally penetrated through the porcine skin. However, there was significant partitioning of progesterone in the skin tissues. Consequently, these results suggest that the lymphatic circulation that exists in the skin may potentially account for the systemic delivery of topically applied progesterone that is often observed clinically.