scholarly journals Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review

2021 ◽  
Vol 13 (1) ◽  
Author(s):  
Abhijit Nair ◽  
Subodh Kamtikar ◽  
Suresh Seelam

AbstractGabapentin and pregabalin, known as gabapentinoids, have been used effectively as a monotherapy or in combination with other agents for managing chronic neuropathic pain due to various etiologies. These drugs act via α2δ-1 and α2δ-2 subunits of voltage-gated calcium channels (VGCCs) non-selectively. Due to its non-selective action, a certain group of patients reports central nervous system adverse effects like dizziness, drowsiness, somnolence, and cerebellar ataxia.Mirogabalin besylate is an orally administered next-generation gabapentinoid approved for use in diabetic neuropathy and post-herpetic neuralgia. It binds selectively and with greater affinity to the α2δ-1 and α2δ-2 subunits of human VGCCs and thus has lesser central nervous system adverse events making it more tolerable. We reviewed all articles in various categories, published in reputed databases since 2014 where mirogabalin was used to treat chronic neuropathic pain. Case series and open-label studies have demonstrated the safety and efficacy of mirogabalin in cancer pain and lumbar spine disease. Pharmacokinetic/pharmacodynamic studies have cautioned using full dose in patients with renal/hepatic impairment and along with drugs that could lead to adverse effects like sedatives and opioids. Dose up to 30 mg/day when administered as a twice-daily divided dose has been tolerated quite well with adequate pain relief in diabetic neuropathy and post-herpetic neuralgia.Mirogabalin appears to be a safe gabapentinoid in diabetic neuropathy and post-herpetic neuralgia. Further studies need to be conducted to explore the role of mirogabalin in cancer pain, postoperative pain, and neuropathic pain due to various other etiologies.

2011 ◽  
Vol 64 (9-10) ◽  
pp. 443-447
Author(s):  
Milan Cvijanovic ◽  
Svetlana Simic ◽  
Sofija Banic-Horvat ◽  
Zita Jovin ◽  
Petar Slankamenac ◽  
...  

Introduction. Neuropathic pain, or pain associated with disease or injury to the peripheral or central nervous system, is a common symptom of a heterogeneous group of conditions, including diabetic neuropathy, trigeminal neuralgia, postherpetic neuralgia and spinal cord injury. Chronic neuropathic pain should not be thought of as a symptom. It should truly be thought of as a disease with a very complicated pathophysiology. Pathophysiology. The mechanisms involved in neuropathic pain are complex and involve both peripheral and central pathophysiologic phenomenon. The underlying dysfunction may involve deafferentation within the peripheral nervous system (e.g. neuropathy), deafferentation within the central nervous system (e.g. post-thalamic stroke) or an imbalance between the two (e.g. phantom limb pain). Clinical characteristics. Neuropathic pain is non-nociceptive, in contrast to acute nociceptive pain, and it can be described as ?burning?, ?electric?, ?tingling?, and ?shooting? in nature. Treatment. Rational polypharmacy is often necessary and actually it is almost always the rule. It would be an exception if a patient was completely satisfied with his treatment. Treatment goals should include understanding that our patients may need to be titrated and managed with more than one agent and one type of treatment. There should be the balance of safety, efficacy, and tolerability. Conclusion. There are many new agents and new applications of the existing agents being currently studied which will most certainly lead to even more improved ways of managing this very complicated set of disorders.


1993 ◽  
Vol 27 (6) ◽  
pp. 767-774 ◽  
Author(s):  
Kelly S. Lewis ◽  
Wade M. Mueller

OBJECTIVE: To evaluate the use of intrathecal baclofen for the treatment of muscle spasticity in patients with spinal cord injury. DATA SOURCES: A MEDLINE search was used to identify relevant and pertinent literature. Information was obtained from open-label clinical trials, abstracts, conference proceedings, and review articles. Index terms in the search included baclofen, spasticity, intrathecal drug infusion, spinal cord disease, and neurosurgery. DATA EXTRACTION: Studies were selected for review if they evaluated intrathecal baclofen in patients with spinal cord injury. Emphasis was placed on human studies published in the English language. Trials were reviewed by dosage regimen, therapeutic response, adverse effects, and complications. DATA SYNTHESIS: Thus far, intrathecal baclofen administration shows promise in the treatment of spasticity resulting from spinal cord trauma. Few complications and adverse effects have been reported. CONCLUSIONS: Muscle spasms and spasticity constitute a significant problem in spinal cord injuries, interfering with rehabilitation and leading to inconveniences and complications in these patients. Oral baclofen is the drug of choice for spasticity due to spinal cord trauma. It often is ineffective, however, because of the large dosages required to cross the blood-brain barrier and the subsequent appearance of central nervous system adverse effects. These adverse effects are not tolerated by many patients. Intrathecally administered baclofen has been approved by the Food and Drug Administration (FDA) for the treatment of spasticity in patients with spinal cord injury who are refractory to or cannot tolerate oral baclofen. It is intended for use only in implantable pumps approved by the FDA for the administration of baclofen into the intrathecal space. Intrathecal administration achieves high concentrations in the spinal cord with small dosages, thus reducing the incidence of central nervous system adverse effects. To date, approximately 350 patients with spinal cord injury have been treated with intrathecal baclofen. Reductions in spasticity have been demonstrated in both open-label and placebo-controlled trials. Patients also often make substantial gains in activities of daily living. Few adverse effects and complications have been reported. However, tolerance to the clinical effects of intrathecal baclofen has been reported. Further studies are needed to determine specific patient populations that may benefit most from intrathecal baclofen administration. Individual dosage ranges and follow-up care also need to be defined more completely. In addition, the question of whether tolerance detracts from long-term clinical benefits with intrathecal baclofen needs to be addressed.


2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Amir Aslam ◽  
Jaipaul Singh ◽  
Satyan Rajbhandari

The prevalence of diabetes is rising globally and, as a result, its associated complications are also rising. Painful diabetic neuropathy (PDN) is a well-known complication of diabetes and the most common cause of all neuropathic pain. About one-third of all diabetes patients suffer from PDN. It has a huge effect on a person’s daily life, both physically and mentally. Despite huge advances in diabetes and neurology, the exact mechanism of pain causation in PDN is still not clear. The origin of pain could be in the peripheral nerves of the central nervous system. In this review, we discuss various possible mechanisms of the pathogenesis of pain in PDN. We discuss the role of hyperglycaemia in altering the physiology of peripheral nerves. We also describe central mechanisms of pain.


CNS Spectrums ◽  
2005 ◽  
Vol 10 (4) ◽  
pp. 298-308 ◽  
Author(s):  
Walter Zieglgänsberger ◽  
Achim Berthele ◽  
Thomas R. Tölle

AbstractNeuropathic pain is defined as a chronic pain condition that occurs or persists after a primary lesion or dysfunction of the peripheral or central nervous system. Traumatic injury of peripheral nerves also increases the excitability of nociceptors in and around nerve trunks and involves components released from nerve terminals (neurogenic inflammation) and immunological and vascular components from cells resident within or recruited into the affected area. Action potentials generated in nociceptors and injured nerve fibers release excitatory neurotransmitters at their synaptic terminals such as L-glutamate and substance P and trigger cellular events in the central nervous system that extend over different time frames. Short-term alterations of neuronal excitability, reflected for example in rapid changes of neuronal discharge activity, are sensitive to conventional analgesics, and do not commonly involve alterations in activity-dependent gene expression. Novel compounds and new regimens for drug treatment to influence activity-dependent long-term changes in pain transducing and suppressive systems (pain matrix) are emerging.


2021 ◽  
Vol 429 ◽  
pp. 118840
Author(s):  
Silvio Piffer ◽  
Raffaella Tanel ◽  
Roberto Bortolotti ◽  
Umberto Rozzanigo ◽  
Bruno Giometto ◽  
...  

2021 ◽  
Author(s):  
Esther Benedetti ◽  
James Burnett ◽  
Meredith Degnan ◽  
Danielle Horne ◽  
Andres Missair ◽  
...  

The neuronal, chemical, and electrical transmission of pain is a complex and intricate subject that continues to be studied and expounded. This review discusses the relevant physiology and influential factors contributing to the experience and subjective variation in a variety of acute and chronic pain presentations. This review contains 4 figures, 4 tables, and 30 references Keywords: acute pain, chronic pain, somatic pain, neuropathic pain, visceral pain, nociception, pain perception, gender-related pain, cancer pain, spine pain


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