• They accomplish this through a number of mechanisms involving automaticity or ion channel dynamics, which in turn affect the propagation of the myocardial electrical impulse via change in conduction velocity or refractory period. (medscape.com)
  • To evaluate the Swarm screening system, we optimized a series of heterologous optogenetic spiking HEK293 cell assays for several voltage-gated sodium channel subtypes including Nav1.2, Nav1.5, and Nav1.7. (frontiersin.org)
  • Genetic etiology of PE is mutations on SCN9A , the encoding gene of a voltage-gated sodium channel subtype Nav1.7. (biomedcentral.com)
  • This review mainly focuses on PE and the causative gene SCN9A -- its mutations and their effects on Nav1.7 channels' electrophysiological properties. (biomedcentral.com)
  • The causative gene for PE, SCN9A , encodes a voltage-gated sodium channel (VGSC) subtype Nav1.7. (biomedcentral.com)
  • We also recapitulate utilization of current treatments and updates of novel Nav1.7-targeted agents, and propose an integrated perspective of a genotype-channelopathy-phenotype network underlying this intricate condition. (biomedcentral.com)
  • PE is exclusively caused by mutations in SCN9A , the encoding gene of sodium channel subtype Nav1.7 and can be sub-classified into familial (inherited erythromelalgia) and sporadic forms. (biomedcentral.com)
  • A 2013 review on treatment for neonatal seizures recommended intravenous lidocaine as a second-line treatment, if phenobarbital fails to stop seizures. (wikipedia.org)
  • Intravenous lidocaine infusions are also used to treat chronic pain and acute surgical pain as an opiate sparing technique. (wikipedia.org)
  • it is used intravenously for the treatment of ventricular arrhythmias (for acute myocardial infarction, digoxin poisoning, cardioversion, or cardiac catheterization) if amiodarone is not available or contraindicated. (wikipedia.org)
  • Once membrane depolarization is complete, the membrane becomes impermeable to sodium ions again, and the conductance of potassium ions into the cell increases. (medscape.com)
  • Antidysrhythmics alter the propagation and mechanisms of cardiac rhythms, making toxicity from these agents highly lethal. (medscape.com)
  • The mechanisms of cellular excitability and propagation of electrical signals in the cardiac muscle are very important functionally and pathologically. (bvsalud.org)
  • Finally, it seems appropriate to consider the "sodium channel syndrome" (mutations in the gene of the α subunit of the sodium channel, SCN5A gene) as a single clinical entity that may manifest in a wide range of phenotypes, to thus have a better insight on these cardiac syndromes and potential outcomes for their clinical treatment. (bvsalud.org)
  • Additionally, the patients receiving these drugs may have a lower dysrhythmic threshold resulting from underlying cardiac conditions as well as other comorbidities, making them more suscpetible to toxicity. (medscape.com)
  • See also Beta-Blocker Toxicity and Calcium Channel Blocker Toxicity , as those topics are not covered in this article. (medscape.com)
  • Serum drug concentrations are not likely to be helpful to the emergency physician treating a patient with acute antidysrhythmic drug toxicity, but concentrations of quinidine, lidocaine, and propafenone can be measured in the acute care setting. (medscape.com)
  • As a demonstration of the versatility of the Swarm, we also developed an assay measuring cardiac action potential and calcium waveform properties simultaneously under paced conditions using human induced pluripotent stem (iPS) cell-derived cardiomyocytes as an additional counter screen for cardiac toxicity. (frontiersin.org)
  • Once the potential reaches a threshold level of approximately -55 mV, a rapid influx of sodium ions ensues. (medscape.com)
  • Although the exact mechanism by which local anesthetics retard the influx of sodium ions into the cell is unknown, 2 theories have been proposed. (medscape.com)
  • To address this challenge, we developed the Swarm TM , a custom designed optical instrument for highly parallelized, multicolor measurements in excitable cells, simultaneously recording changes in voltage and calcium activities at high temporal resolution under optical stimulation. (frontiersin.org)
  • In addition, because the nerve membrane is permeable to potassium ions and impermeable to sodium ions, 95% of the ionic leak in excitable cells is caused by K + ions in the form of an outward flux, accounting for the negative resting potential. (medscape.com)
  • Cardiac action potential Action Potential Abrupt changes in the membrane potential that sweep along the cell membrane of excitable cells in response to excitation stimuli. (lecturio.com)
  • The efficacy profile of lidocaine as a local anaesthetic is characterized by a rapid onset of action and intermediate duration of efficacy. (wikipedia.org)
  • Local anesthetics have been undergoing development for centuries, and, as this article illustrates, research continues to provide surgeons with pharmacologic variety and to provide patients with anesthetic agents that have superior safety and efficacy profiles. (medscape.com)
  • An adhesive transdermal patch containing a 5% concentration of lidocaine in a hydrogel bandage, is approved by the US FDA for reducing nerve pain caused by shingles. (wikipedia.org)
  • The concentration gradients are maintained by the sodium/potassium ATP pump (in an energy-dependent process) that transports sodium ions out of the cell and potassium ions into the cell. (medscape.com)
  • When used for local anaesthesia or in nerve blocks, lidocaine typically begins working within several minutes and lasts for half an hour to three hours. (wikipedia.org)
  • beta-blockers Beta-blockers Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. (lecturio.com)
  • Adrenaline vasoconstricts arteries, reducing bleeding and also delaying the resorption of lidocaine, almost doubling the duration of anaesthesia. (wikipedia.org)
  • lidocaine, though, has the advantage of a rapid onset of action. (wikipedia.org)
  • The Swarm was able to record pseudo-action potentials stably across all 24 objectives and provided pharmacological characterization of diverse sodium channel blockers. (frontiersin.org)
  • As a local numbing agent, it is used for the treatment of premature ejaculation. (wikipedia.org)
  • From a physiological and pathophysiological point of view, the conformational states of the sodium channel during heart function constitute a significant aspect for the diagnosis and treatment of heart diseases. (bvsalud.org)
  • Most ADRs associated with lidocaine for anesthesia relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, and allergic reactions only rarely occur. (wikipedia.org)
  • Optogenetic assays provide a flexible, scalable, and information rich approach to probe compound effects for ion channel drug targets in both heterologous expression systems and associated disease relevant cell types. (frontiersin.org)
  • Lidocaine is an antiarrhythmic medication of the class Ib type. (wikipedia.org)
  • In 1943, an alternative class of anesthetics was discovered when Lofgren developed lidocaine. (medscape.com)
  • Heart relaxation also stands out as an active process, dependent on the energetic output and on specific ion and enzymatic actions, with the role of sodium channel being outstanding in the functional process. (bvsalud.org)
  • Late Sodium Current of the Heart: where Do We Stand and Where Are We Going? (unideb.hu)
  • Adverse drug reactions (ADRs) are rare when lidocaine is used as a local anesthetic and is administered correctly. (wikipedia.org)
  • Contraindications Contraindications A condition or factor associated with a recipient that makes the use of a drug, procedure, or physical agent improper or inadvisable. (lecturio.com)
  • Antidysrhythmic medications are widely used to treat or prevent abnormalities in cardiac rhythms. (medscape.com)
  • Lidocaine drops can be used on the eyes for short ophthalmic procedures. (wikipedia.org)
  • In 1884, Sigmund Freud and Karl Koller were the first to use it as an anesthetic agent during ophthalmologic procedures. (medscape.com)
  • Systemic exposure to excessive quantities of lidocaine mainly result in central nervous system (CNS) and cardiovascular effects - CNS effects usually occur at lower blood plasma concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations. (wikipedia.org)
  • The recently identified 2-pore domain potassium (K2P) channels are believed to be responsible for leak K + currents. (medscape.com)