1 ,2 Dantrolene has shown some efficacy for use in spasticity in debilitating conditions that hinders functionality, but there is little evidence exhibiting effectiveness for musculoskeletal conditions. Available in US: No, but the manufacturer is recruiting for Phase 3 STAR study under #NCT04671082 utilized in Europe since the 1960sĭantrolene is classified as an antispasmodic medication with the mechanism of action on the PNS by blocking the calcium channel of the sarcoplasmic reticulum to reduce the concentration of calcium and diminishing the potential for an actin-myosin interaction which could produce a muscle contraction.3 As a skeletal muscle relaxant with less CNS adverse effects than currently available in some analgesics, tolperisone may offer a more promising option for patients. 1 Unlike other skeletal muscle relaxants, tolperisone has been shown to exhibit less somnolence or cognitive adverse effects when used with for up to 14 days. 1 Tolperisone was shown to be more effective than placebo for patients with chronic low back pain and overall improvement with short term use over 21 days, but no reduction of muscle spasms or pain. Tolperisone is classified as an antispasmodic with the mechanism of action possessing lidocaine-like-activity by stabilizing nerve membranes of mono- and polysynaptic reflexes in the spinal cord by blocking in a dose-dependent manner. Potential targets: acute low back pain, neck pain, nocturnal leg cramps.Brand names: Norflex, Norgesic, Orphenesic Forte.In 2020, FDA granted a supplemental ANDA for a combination formulation of orphenadrine citrate with aspirin and caffeine in 2020. 1 Orphenadrine citrate is indicated for mild to moderate pain of acute MSK disorders and as an adjunct to rest, PT, and other measures for relief of discomfort associated with acute painful MSK conditions. However, given orphenadrine’s chemical nature, it consequently possesses anticholinergic activity and thus patients may experience dry mouth, blurry vision, constipation, urinary retention, and cognitive dysfunction. Orphenadrine citrate is classified as an antispasmodic with the mechanism of action being unclear, but is a derivative of diphenhydramine and its activity is believed to be related to its sedative effects. In four placebo-controlled trials, orphenadrine was found to be fairly effective in some musculoskeletal conditions (acute low back pain, neck pain, nocturnal leg cramps) as well as symptoms of pain intensity, stiffness, and functionality. Antispasmodics are used to reduce muscle spasms resulting from a painful condition whereas antispasticity medications are used to decrease spasticity that hinders functionality. Muscle relaxants can be divided into two main categories: antispasmodic and antispasticity medications. Skeletal muscle relaxants are a broad category of medications consisting of a wide spectrum of drugs with different indications and mechanisms of action. Here, we revisit the “land of lost analgesics” with the goal of refamiliarizing pain-treating clinicians – whether in specialty or primary care – with alternative treatment options. Not all pharmacologic treatment options are viable for every patient. Potential uses, clinical considerations, and US availability are noted for each. Here, we revisit this “land of lost analgesics” with the goal of refamiliarizing pain-treating clinicians – whether in specialty or primary care – with alternative treatment options that are worth consideration when initial first and second-line pain therapies have been optimized or are contraindicated. Over time, some pharmacologic options are withdrawn from the market by the manufacturer, forgotten, or underutilized due to a lack of clinician knowledge or familiarity. Not all pharmacologic treatment options are viable for every case due to patient-specific factors, compelling medical indications and comorbidities, drug interactions, and even pharmacogenetics. Clinicians are challenged and quite possibly hesitant with managing complex pain syndromes in individuals with medical comorbidities. The current opioid crisis in the US has significantly shifted the pendulum of opioid prescribing practices due to various restrictive guidelines, laws, regulations, and policies at both the federal and state level.
The management of pain – whether acute or chronic – is one of the most difficult medical conditions to treat and when treatment options are limited, the patient is the one left to suffer while the clinician bears the burden of trying to help the patient. Perhaps, older treatment modalities just need to be reconsidered. Pain-treating clinicians are constantly searching for medications that improve patient outcomes and/or that can minimize the use of opioids.
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