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Ketoprofen

Ketoprofen

Beyond Conventional NSAIDs: Transdermal Efficacy and Therapeutic Potential of Nepafenac in Comparison to Diclofenac Sodium

Date: 2.2025

​Oral non-steroidal anti-inflammatory drugs (NSAIDs) are associated with a multitude of treatment-limiting contraindications, conflicting comorbidities, drug-drug interactions, and bothersome systemic effects. Contrary to the widespread use and well-established efficacy of systemic NSAIDs, locally-acting NSAIDs are still an area of ongoing pharmacologic investigation. As of December 2024, diclofenac is the only FDA-approved NSAID for cutaneous use, despite the availability of other structurally-similar NSAIDs with comparable potencies, physicochemical properties, and pharmacokinetics. Nepafenac, a relatively new ophthalmic NSAID, has certain unique attributes which make it a promising candidate for transdermal formulations. (Read more...)

Does OTC Diclofenac Gel Meet Therapeutic Needs? A DoseResponse Review in Neuropathic & Inflammatory Pain Management

Date: 2.2025

​Diclofenac (VOLTAREN) was synthesized in 1973 and is the most widely prescribed NSAID worldwide. Subsequently, transdermal diclofenac sodium (TDS) emerged as a promising therapeutic option for localized pain management, offering a targeted approach with negligible plasma/systemic exposure. Through a comprehensive analysis of applicable pharmacokinetic and biopharmaceutic studies, this review aims to clarify the dose and formula optimization of TDS preparations. Our findings suggest that TDS 1.5- 2% may not only enhance local bioavailability and analgesic efficacy, but may also relieve neuropathic pain—a novel application for this drug class.  (Read more...)

Transdermal Ketamine: A Rising Star in Pain and Inflammation

Date: 12.2024

​Ketamine is a powerful dissociative anesthetic with a rich history in medicine due to its remarkably complex, dose-dependent pharmacology. Originally synthesized in 1962 as a safer and more effective alternative to phencyclidine (PCP), ketamine has expanded its clinical applications to include analgesia and
immunomodulation. Approximately 11–40% of adults in the United States report suffering from chronic pain, affecting more people than diabetes, heart disease, and cancer combined. Current therapies such as opioid agonists, non-steroidal anti-inflammatory drugs (NSAIDs), gabapentinoids, antidepressants, and topical anesthetic agents are first-line treatments for various pain conditions.  (Read more...)

"Applying" Pharmacokinetics: NSAID-Mediated Pain & Inflammation

Date: 11.2024

A comparative review of the cutaneous locomotion and PK parameters of diclofenac sodium vs ketoprofen.   (Read more...)

Efficacy of topical versus oral analgesic medication compared to a placebo in injured athletes: A systematic review with meta-analysis

Date: 06.2023

Athletes are injured frequently and often take analgesic medication. Moreover, athletes commonly use non-prescription topical and oral medications with little guidance. Despite wide use, relatively few studies exist on the efficacy of pain medication in injured athletes compared to a placebo.   (Read more...)

FDA says NSAIDS increase risk of heart attack

Date: 09.27.2021

The U.S. Food and Drug Administration (FDA) is strengthening an existing label warning that non-aspirin nonsteroidal anti-inflammatory drugs (NSAIDs) increase the chance of a heart attack or stroke. Nonsteroidal anti-inflammatory drugs (NSAIDs) are drugs with analgesic, anti-inflammatory, and antipyretic activity.   (Read more...)

New ACP Guidelines for Treatment of Acute Non Low Back Pain-Topical NSAIDs First-Line Therapy

Date: 08.31.2020

The American College of Physicians (ACP) and American Academy of Family Physicians (AAFP) recommend topical nonsteroidal anti-inflammatory agents (NSAIDs) as the first-line of therapy for non-low back pain. Physicians should encourage adults to use NSAIDs, particularly topical ones, to treat acute non-low back pain that stems from musculoskeletal injuries, according to the new guidelines.  (Read more...)

Cascade with GI Prostaglandin and Use of Topical NSAIDs vs Oral NSAIDs

Date: 08.28.2020

Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used for their anti-inflammatory, analgesic, and antipyretic effects. NSAIDs generally work by blocking the production of prostaglandins (PGs) through the inhibition of two cyclooxygenase enzymes. However, their use has been associated with potentially serious dose-dependent gastrointestinal (GI) complications such as upper GI bleeding. GI complications resulting from NSAID use are among the most common drug side effects in the United States, due to the widespread use of NSAIDs.  Topical products were developed to provide well tolerated, effective targeted therapies, based on the drug’s pharmacokinetics and penetration to the site of action.  (Read more...)

Topical Ketoprofen

Date: 02.11.2019

Ketoprofen, a nonsteroidal anti-inflammatory drug (NSAID), possesses analgesic, antipyretic and anti-inflammatory properties. Oral Ketoprofen is widely used in musculoskeletal pain and inflammation in muscles and joints, including arthritis pain, osteoarthritis, stiffness of the joints, soft tissue rheumatism, and sports injuries. Topical formulations of NSAIDs have analgesic effects similar to that of oral formulations, but are associated with less systemic exposure and, therefore, with fewer serious adverse events.  (Read more...)

Gabapentin

Gabapentin

Plasma concentration of oral gabapentin dose not increase proportionally with increase dosing

Date: 04.12.21

The gabapentinoids are often recommended as first-line treatments for the management of neuropathic
pain. The differing pharmacodynamic and pharmacokinetic profiles can have implications for clinical practice. Gabapentin, as an oral preparation, is absorbed in the small intestine by a combination of diffusion and facilitated transport. Oral bioavailability for gabapentin is between 30-60%. As the dose of gabapentin increases, the area under the plasma concentration–time curve (AUC) does not increase proportionally.   (Read more...)

Transdermal Gabapentin: The Route Less Traveled

Date: 10.13.2024

​A multimodal approach to optimize pharmacotherapy and improve safety outcomes in chronic neuropathy

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Why Gabapentin may become a Schedule V controlled substance

Date: 01.30.2020

Gabapentinoids (e.g. pregabalin and gabapentin) are widely used in neurology, psychiatry and primary healthcare but are increasingly being reported as possessing a potential for misuse. Gabapentin may be
abused for its euphoric and analgesic effects, or to substitute for or potentiate the effects of opioids or
methadone. Gabapentinoids are thought to possess GABA-mimetic properties whilst possibly presenting with direct/indirect effects on the dopaminergic 'reward' system.  (Read more...)

FDA warns about serious breathing problems associated with Gabapentinoids

Date: 01.14.2020

The U.S. Food and Drug Administration (FDA) is warning that serious breathing problems have been associated with gabapentinoids such as oral gabapentin and pregabalin when used with CNS depressants or in patients who have respiratory risk factors. These warnings are based on a review of several sources of data including case reports submitted to the FDA or published in the medical literature, observational studies, human trials and animal studies. Gabapentin and pregabalin are FDA-approved for a variety of conditions, including seizures, nerve pain, and restless legs syndrome.  (Read more...)

Topical Gabapentin use on CRPS

Date: 10.29.2019

Gabapentin is one of the most commonly prescribed pain medications for neuropathic pain in general, and specifically in Complex Regional Pain Syndrome (CRPS). Gabapentin is thought to work by modulating calcium channels at a specific alpha delta subunit. CRPS 1 is a disabling syndrome, in which a painful limb is accompanied by varying symptoms. Neuropathic pain is a prominent feature of CRPS I, and is often refractory to treatment. Topical delivery of gabapentin is desirable to treat peripheral neuropathic pain conditions while avoiding systemic side effects.  (Read more...)

Topical Gabapentin

Date: 10.09.2017

Topical Gabapentin is used for the treatment of chronic pain conditions including but not limited to postherpetic neuralgia (PHN), complex regional pain syndrome (CRPS) and vulvodynia (VVD). Multiple studies have already demonstrated the efficacy of oral gabapentin in treating chronic neuropathic pain. However, oral gabapentin is limited by dose-dependent toxicity which can cause systemic adverse effects.  (Read more...)

Naltrexone

Naltrexone

Naltrexone Utilization Along Its Dosing Spectrum - A Literature Review

Date: 2.2025

Naltrexone, a widely recognized opioid receptor antagonist, has been primarily used at standard doses of 50–100 mg daily to treat opioid and alcohol use disorders. Recent studies, however, reveal its versatility across a broader dosing spectrum. This review examines the therapeutic effects and safety profiles of naltrexone across three dosing strategies: standard doses for substance use disorders, low-dose naltrexone (LDN, 1–5 mg/day) for chronic pain and autoimmune diseases, and ultra-low-dose naltrexone (ULDN, microgram levels) as a complement to opioid therapy.  (Read more...)

Lidocaine

Focus: Addiction drug shows promise lifting long COVID brain fog, fatigue

Date: 10.18.2022

CHICAGO, Oct 18 (Reuters) - Lauren Nichols, a 34-year-old logistics expert for the U.S. Department of Transportation in Boston, has been suffering from impaired thinking and focus, fatigue, seizures, headache and pain since her COVID-19 infection in the spring of 2020. Last June, her doctor suggested low doses of naltrexone, a generic drug typically used to treat alcohol and opioid addiction. After more than two years of living in "a thick, foggy cloud," she said, "I can actually think clearly."   (Read more...)

Safety and efficacy of low dose naltrexone in a long covid cohort; an interventional pre-post study

Date: 10.24.2022

Up to 37.7% of patients experience symptoms beyond 12 weeks after infection with SARS-CoV-2. To date care for people with long covid has centred around multidisciplinary rehabilitation, self care and self pacing. LDN is safe in patients with PCS and may improve well-being and reduce symptomatology in this cohort. Randomised control trials are needed to further explore this.   (Read more...)

Low-Dose Naltrexone Could Treat Long COVID Symptoms

Date: 6.7.2023

Naltrexone is a drug approved by the Food and Drug Administration (FDA) to treat alcohol use disorder and opioid addiction. Low-dose naltrexone (LDN), usually at a fraction of the regular dose, has been used to treat fibromyalgia and multiple sclerosis.   (Read more...)

Lidocaine

The Case for Transdermal Lidocaine 7.5% in the Management of Localized Pain: A Biopharmaceutical Review

Date: 1.20.2025

Transdermal anesthesia is a cornerstone of pain management, offering localized analgesia with minimal systemic effects. Lidocaine, a widely utilized local anesthetic, achieves pain relief primarily through sodium channel blockade, with emerging evidence highlighting additional mechanisms such as modulation
of inflammatory mediators and nociceptive signaling. This review of the literature investigates Lidocaine 7.5% Cream as a potentially superior option compared to 4-5% lidocaine formulations and EMLA cream (lidocaine 2.5% and prilocaine 2.5%). With its higher concentration, Lidocaine 7.5% Cream may provide deeper, longer-lasting anesthesia while mitigating risks such as prilocaine-induced methemoglobinemia and delayed onset associated with EMLA Cream.  (Read more...)

Nalbuphine

Nalbuphine

Therapeutic Potential of Oral Nalbuphine for the Treatment of Chronic Pain: A Literature Review

Date: 2.2025

Typical opioids used for pain, including morphine, activate mu opioid receptors. Disadvantages of these drugs include their abuse potential, risk of respiratory depression, and the development of tolerance, dependance, and constipation. Nalbuphine is an injectable opioid agonist-antagonist analgesic with low abuse potential and a unique mechanism of action. Not only is its analgesic potency comparable to morphine within the typical dosing range, but it also has a low risk of clinically significant respiratory depression, and is generally considered much safer than morphine-like opioids.  (Read more...)

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