China
Africa
Explore chapters and articles related to this topic
Nonclassical Ion Channels in Depression
Published in Tian-Le Xu, Long-Jun Wu, Nonclassical Ion Channels in the Nervous System, 2021
Disruption of the Ih current in HCN113, HCN2, or TRIP8b18 -transgenic mice was also shown to affect anxiety-like behaviors. Moreover, researchers identified a manifest anxiogenic effect in mice via hairpin RNA silencing of hcn4, indicating that HCN4 plays an essential role in anxiety-like behaviors19. The chemogenetic inhibition of neurons in dorsal bed nucleus of the stria terminalis (BNST) imitates aspects of α-2A adrenergic receptor signaling. These receptors generate HCN-dependent excitatory actions and induce anxiety-like behaviors20, determined by the elevated zero maze (EZM) and open field (OF) tests. Two well-known Ih current potentiators, Gabapentin and lamotrigine (LTG), are used to treat different neurological disorders. Gabapentin is an effective treatment for anxiety, nightmares, and insomnia in individuals who have post-traumatic stress disorder (PTSD)21,22. Gabapentin is also used as an adjunctive treatment for the management of anxiety disorders, especially for social phobia and panic disorder23,24–25. Lamotrigine efficacy is limited to bipolar disorder treatment26.
Medications That May Be Useful in the Management of Patients with Chronic Intractable Pain
Published in Michael S. Margoles, Richard Weiner, Chronic PAIN, 2019
Gabapentin should be taken only as prescribed. Patients should be advised that gabapentin may cause dizziness, somnolence, and other symptoms and signs of central nervous system depression. Accordingly, patients should be advised to neither drive a car nor operate other complex machinery until they have gained sufficient experience on gabapentin to gauge whether or not it affects their mental or motor performance adversely (Facts and Comparisons, 1996).
Psychiatric Treatment Approaches for Pediatric Pain
Published in Andrea Kohn Maikovich-Fong, Handbook of Psychosocial Interventions for Chronic Pain, 2019
Gabapentin is the best-studied anticonvulsant used in management of adult chronic pain, revealing benefits for central and peripheral neuropathic pain, visceral hyperalgesia, autonomic dysfunction, and spasticity (Fornasari, 2017). Its mechanism of action primarily targets voltage-gated calcium channels to diminish excessive neuronal activity and excitatory neurotransmitter release. Occasionally used to target anxiety symptoms in youth, gabapentin is much more commonly used clinically in the management of chronic pain and partial seizures. Several case reports also have described benefits in children with reduction in pain behavior and improvement in sleep, but placebo-controlled trials are lacking (Correia, Soares, Azurara, & Palaré, 2017; Robinson & Malow, 2013). One recent RCT examined the efficacy of gabapentin compared to amitriptyline for CPRS and neuropathic pain in children (Brown et al., 2016). The medicines proved similar in efficacy for pain and sleep disruption, with no differences in adverse side effects.
Provider-directed analgesia for dental pain
Published in Expert Review of Clinical Pharmacology, 2023
Gabapentin was first approved by the FDA in 1993 as an antiepileptic, but also has proven efficacy in, for example, anxiety and mood disorders, fibromyalgia, neuropathic, and other types of pain [126]. A systematic Cochrane review published in 2010 reported that single-dose gabapentin (250 mg) was superior to placebo, in which significantly fewer participants suffering from postoperative dental pain required rescue medication within 6 hours compared to placebo [144]. With an NNT of 11, the authors concluded that gabapentin as a single agent may be of limited clinical value in the post-surgical setting, but does support its potential role as an adjunctive pain remedy [144]. Recent work by Quang et al. [145] support this postulation, in which patients treated with gabapentin combined with either acetaminophen or ibuprofen following dental extractions had significantly less failure rates than those receiving opioid combinations. Their work further emphasizes the role of gabapentin in potentially alleviating the opioid prescription burden [145].
Advances in molecular therapies for targeting pathophysiology in spinal cord injury
Published in Expert Opinion on Therapeutic Targets, 2023
Ha Neui Kim, Madeline R. McCrea, Shuxin Li
Some therapeutic strategies that target cellular and molecular pathophysiology have been moved to clinical trials for SCI patients, such as the use of the neuroprotective Na channel blocker riluzole, the cytokine G-CSF, and systemic hypothermia [5]. Other reagents aimed to promote axon regeneration are also under investigation in clinical trials for SCI, such as an anti-Nogo-A antibody (NG-101), a Nogo receptor antagonist [AXER-204 or NgR(310)ecto-Fc], and Elezanumab, a human anti-RGMa monoclonal antibody [5]. Early systemic treatments with gabapentinoid, an α2δ subunit Ca channel blocker, enhanced motor recovery in SCI patients [6]. Gabapentin is an FDA-approved drug used to treat regional seizures and neuropathic pain. Several clinical trials of SCI that target rewiring of spinal neuronal circuits are also ongoing, including transplants of adipose tissue-derived mesenchymal stem cells (MSCs) and neuro-spinal scaffolds, and implanting brain–spine interfaces. The recent clinical trials with transplanting human NSCs into patients with thoracic and cervical SCIs indicated a trend toward motor benefits [7]. This overall review is aimed to provide insight into preclinical therapeutic targets for SCI reported in recent years.
Recent advances in drug delivery to the central nervous system by inhalation
Published in Expert Opinion on Drug Delivery, 2022
Waiting Tai, Philip Chi Lip Kwok
Nonetheless, pulmonary delivery has fully demonstrated its ability to play a bigger role in administering drugs to the CNS. Therefore, more CNS-active drugs are expected to be delivered by inhalation in the future. Choosing suitable neurological drugs for inhalation should mainly be based on their PK profiles and indications. Drugs with unfavorable oral PK properties have great potential in pulmonary delivery as their absorption and bioavailability may be improved with less extensive metabolism. This allows the achievement of the same therapeutic effects with lower doses, and hence less adverse effects. Some drugs are intended to provide rapid relief. They may potentially benefit from inhalation to accelerate the onset of action as other routes of non-parenteral administrations are generally less efficient. A good example is oral gabapentin, which may benefit from pulmonary delivery. It is used to treat neuropathic pain so it should produce a fast onset of action. However, its oral form has a long tmax (3–4 hours), zero-order absorption kinetics, and a reduction in oral bioavailability from 60% at 900 mg to 33% at 3600 mg [132]. This suggests that oral delivery is unsuitable for gabapentin. Its PK profile may be improved if inhaled. However, one important point to note is that not all drugs should be inhaled as they may easily be abused by patients. These include fluoxetine for depression and amphetamine for attention deficit hyperactivity disorder. The purpose of changing the delivery route, doses, and even the aerosolization device should be considered carefully.