Evaluation of the Percutaneous Absorption of Ketamine HCl, Gabapentin, Clonidine HCl, and Baclofen, in Compounded Transdermal Pain Formulations, Using the Franz Finite Dose Model

Bassani, August S; Banov, Daniel

doi:10.1111/pme.12899

Cited by 20 publications

(10 citation statements)

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“…Choices include three of the most commonly used topical analgesics for chronic neuropathic pain: ketamine, clonidine, and gabapentin, with ketamine having the highest absorption rate. 15 Clonidine has been used as an adjuvant pain medication successfully in postoperative and chronic pain. As a relatively nonspecific a 2 -agonist, it acts to hyperpolarize nerve cell membranes, diminishing nociceptive function, and lowering circulating levels of catecholamines.…”

Section: Discussion: the Need To Recognize Topical Adjuvant Analgesicmentioning

confidence: 99%

“…Choices include three of the most commonly used topical analgesics for chronic neuropathic pain: ketamine, clonidine, and gabapentin, with ketamine having the highest absorption rate. 15 …”

Section: Discussion: the Need To Recognize Topical Adjuvant Analgesicmentioning

confidence: 99%

“…The coadministration with other adjuvants, such as clonidine and gabapentin, can provide a more robust response, and formulation in Lipoderm base increases transdermal penetration. 15 …”

Section: Incorporating Ketamine and Other Adjuvants Into The Who Laddmentioning

confidence: 99%

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Topical Ketamine with Other Adjuvants: Underutilized for Refractory Cancer Pain? A Case Series and Suggested Revision of the World Health Organization Stepladder for Cancer Pain

Winegarden

Carr

Bradshaw

2020

Journal of Palliative Medicine

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Background: Uncontrolled cancer pain is a significant problem in palliative medicine. Opioids are often firstline treatment that increase risks of analgesic tolerance and hyperalgesia. Topical ketamine with other adjuvant pain medications is an often-overlooked treatment, yet may be most effective in difficult-to-treat cancer pain. Objective: We report a case series of hospice patients with uncontrolled cancer pain who were suboptimally treated with opioids and nerve blocks, whose symptoms responded to topical ketamine with other adjuvants. We review the pronociceptive properties of opioids and how topical multimodal treatment of cancer pain can be more effective than standard opioids, other topical adjuvant medications, and nerve blocks. We discuss the shortcomings of the World Health Organization (WHO) stepladder for the treatment of cancer pain and suggest an adjuvant treatment algorithm, directing physicians to appropriate adjuvant pain agents based on pain type and distinct receptor actions. Design: This is a retrospective case series of patients who responded to topical multimodal pain treatment with implementation of findings into an addendum to the WHO stepladder. Subjects: Subjects were from a case series of community-based hospice patients with previously uncontrolled cancer pain. Measurement: Measurement was made by self-report of pain levels using the 10-point numeric pain rating scale. Results: Patients' pain was controlled with topical adjuvant medications with return to previously lost function and prevention of otherwise escalating opioid dosing. Conclusions: These patient cases reveal how ketamine-based topical treatment for cancer pain can be more effective than standard opioids, other topical adjuvant medications, and nerve blocks with no noted side effects and observed reduction in opioid consumption.

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Section: Discussion: the Need To Recognize Topical Adjuvant Analgesicmentioning

confidence: 99%

“…Choices include three of the most commonly used topical analgesics for chronic neuropathic pain: ketamine, clonidine, and gabapentin, with ketamine having the highest absorption rate. 15 …”

Section: Discussion: the Need To Recognize Topical Adjuvant Analgesicmentioning

confidence: 99%

See 1 more Smart Citation

Topical Ketamine with Other Adjuvants: Underutilized for Refractory Cancer Pain? A Case Series and Suggested Revision of the World Health Organization Stepladder for Cancer Pain

Winegarden

Carr

Bradshaw

2020

Journal of Palliative Medicine

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“…An in vitro study of human cadaver trunk skin revealed that clonidine can be successfully delivered transdermally for analgesic effects when incorporated into transdermal lipoderm compound bases. Furthermore, clonidine, approximately 1 hr after application on trunk skin, had a rapid penetration to peak flux and a secondary peak at approximately 40 hr (Bassani & Banov, ). Although the systemic delivery of clonidine has attenuated hyperalgesia in several pain models, the clinical use of clonidine is dose limited, because of its adverse side effects such as drowsiness, hypotension, and sedation.…”

Section: α2‐adrenoceptors As a Target For Neuropathic Pain Treatment;mentioning

confidence: 99%

Spinal α₂‐adrenoceptors and neuropathic pain modulation; therapeutic target

Bahari

Meftahi

2019

British J Pharmacology

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Neuropathic pain can arise from disease or damage to the nervous system. The most common symptoms of neuropathic pain include spontaneous pain, allodynia, and hyperalgesia. There is still limited knowledge about the factors that initiate and maintain neuropathic pain. However, ample evidence has proved the antinociceptive role of spinal α‐adrenoceptors following nerve injury. It is well‐documented that https://www.sciencedirect.com/topics/neuroscience/norepinephrine descending pathways from supraspinal loci exert an inhibitory influence on the spinal cord nociceptive neurons, mostly through the activation of spinal α2‐adrenoceptors. This, in turn, suppresses transmission of pain input and the hyperexcitability of spinal dorsal horn neurons. There is considerable evidence demonstrating that spinal application of α2‐adrenoceptor https://www.sciencedirect.com/topics/neuroscience/agonists leads to analgesic effects in animal models of neuropathic pain. Today, despite the recent rapid development of neuroscience and drug discovery, effective drugs with clear basic mechanisms have remained a mystery. Here, we give an overview of the cellular mechanisms through which brainstem adrenergic descending inhibitory processing can alter spinal pain transmission to the higher centres, and how these pathways change in neuropathic pain conditions focusing on the role of spinal α2‐adrenoceptors in the spinal dorsal horn. We then suggest that α2‐adrenoceptor agonist may be useful to treat neuropathic pain. Linked Articles This article is part of a themed section on Adrenoceptors—New Roles for Old Players. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.14/issuetoc

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“…Ketamine is usually combined with gabapentin, clonidine and baclofen, using either transdermal Lipoderm or Lipoderm ActiveMax. This technique can personalize treatment thus embettering focal pain control [233]. Also, topical ketamine cream, compounded in combination with other drugs (amitriptyline, baclofen, lidocaine, ketoprofen, clonidine, gabapentin, pregabalin), was reported by this group with excellent pain control in patients suffering from peripheral neuropathic pain [55].…”

Section: Topical (External) Use Of Ketaminementioning

confidence: 99%

Role and Advantageousness of Ketamine in Obese and Non-Obese Patients: Peri-Interventional Considerations

Amit

2018

JPT

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Obese and morbidly obese patients are a growing group of individuals that generates medical, social and economicproblems worldwide. They undergo various interventions that require anesthesia and/or analgesia. Despite theirhealthy look, these individuals are graded at high ASA physical status, mainly because of their impaired respiratoryand cardiovascular conditions, and the metabolic changes their body undergoes. Opioids are the default drugsfor perioperative analgesia. Nevertheless, their use has reached a frightening epidemic-like condition worldwide.Multimodal analgesia regimens have been recommended as a perioperative standard of care, particularly useful in theobese. These regimens employ combinations of opioids and non-opioid compounds that reciprocate each analgesicpotencies, thus providing superior pain relief at rest, movement, or on effort, while reducing opioid consumption andtheir concerned adverse effects. The most important perioperative IV adjuvant currently employed is ketamine thatsees resurgence among physicians from diverse medical specialties. After summarizing obese patients’ perioperativedrawbacks, this review will illustrate ketamine’s neuropharmacology, and will describe its therapeutic usefulness asan analgesic adjuvant. Since data regarding the use of the drug in obese patients is scarce, brief exemplifications ofits benefits in non-obese cohorts will be portrayed as well.

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Evaluation of the Percutaneous Absorption of Ketamine HCl, Gabapentin, Clonidine HCl, and Baclofen, in Compounded Transdermal Pain Formulations, Using the Franz Finite Dose Model

Cited by 20 publications

References 25 publications

Topical Ketamine with Other Adjuvants: Underutilized for Refractory Cancer Pain? A Case Series and Suggested Revision of the World Health Organization Stepladder for Cancer Pain

Topical Ketamine with Other Adjuvants: Underutilized for Refractory Cancer Pain? A Case Series and Suggested Revision of the World Health Organization Stepladder for Cancer Pain

Spinal α₂‐adrenoceptors and neuropathic pain modulation; therapeutic target

Role and Advantageousness of Ketamine in Obese and Non-Obese Patients: Peri-Interventional Considerations

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Evaluation of the Percutaneous Absorption of Ketamine HCl, Gabapentin, Clonidine HCl, and Baclofen, in Compounded Transdermal Pain Formulations, Using the Franz Finite Dose Model

Cited by 20 publications

References 25 publications

Topical Ketamine with Other Adjuvants: Underutilized for Refractory Cancer Pain? A Case Series and Suggested Revision of the World Health Organization Stepladder for Cancer Pain

Topical Ketamine with Other Adjuvants: Underutilized for Refractory Cancer Pain? A Case Series and Suggested Revision of the World Health Organization Stepladder for Cancer Pain

Spinal α2‐adrenoceptors and neuropathic pain modulation; therapeutic target

Role and Advantageousness of Ketamine in Obese and Non-Obese Patients: Peri-Interventional Considerations

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Product

Resources

About

Spinal α₂‐adrenoceptors and neuropathic pain modulation; therapeutic target