Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.PropylaminesAnti-Arrhythmia Agents: Agents used for the treatment or prevention of cardiac arrhythmias. They may affect the polarization-repolarization phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibers. Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade, beta-adrenergic blockade, repolarization prolongation, or calcium channel blockade.Myotonia: Prolonged failure of muscle relaxation after contraction. This may occur after voluntary contractions, muscle percussion, or electrical stimulation of the muscle. Myotonia is a characteristic feature of MYOTONIC DISORDERS.Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.Sodium Channel Blockers: A class of drugs that act by inhibition of sodium influx through cell membranes. Blockade of sodium channels slows the rate and amplitude of initial rapid depolarization, reduces cell excitability, and reduces conduction velocity.Tocainide: An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.Voltage-Gated Sodium Channel Blockers: A class of drugs that inhibit the activation of VOLTAGE-GATED SODIUM CHANNELS.Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.Medigoxin: A semisynthetic digitalis glycoside with the general properties of DIGOXIN but more rapid onset of action. Its cardiotonic action is prolonged by its demethylation to DIGOXIN in the liver. It has been used in the treatment of congestive heart failure (HEART FAILURE).Sodium Channels: Ion channels that specifically allow the passage of SODIUM ions. A variety of specific sodium channel subtypes are involved in serving specialized functions such as neuronal signaling, CARDIAC MUSCLE contraction, and KIDNEY function.Myotonia Congenita: Inherited myotonic disorders with early childhood onset MYOTONIA. Muscular hypertrophy is common and myotonia may impair ambulation and other movements. It is classified as Thomsen (autosomal dominant) or Becker (autosomal recessive) generalized myotonia mainly based on the inheritance pattern. Becker type is also clinically more severe. An autosomal dominant variant with milder symptoms and later onset is known as myotonia levior. Mutations in the voltage-dependent skeletal muscle chloride channel are associated with the disorders.Long QT Syndrome: A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Myotonic Dystrophy: Neuromuscular disorder characterized by PROGRESSIVE MUSCULAR ATROPHY; MYOTONIA, and various multisystem atrophies. Mild INTELLECTUAL DISABILITY may also occur. Abnormal TRINUCLEOTIDE REPEAT EXPANSION in the 3' UNTRANSLATED REGIONS of DMPK PROTEIN gene is associated with Myotonic Dystrophy 1. DNA REPEAT EXPANSION of zinc finger protein-9 gene intron is associated with Myotonic Dystrophy 2.Paralyses, Familial Periodic: A heterogenous group of inherited disorders characterized by recurring attacks of rapidly progressive flaccid paralysis or myotonia. These conditions have in common a mutation of the gene encoding the alpha subunit of the sodium channel in skeletal muscle. They are frequently associated with fluctuations in serum potassium levels. Periodic paralysis may also occur as a non-familial process secondary to THYROTOXICOSIS and other conditions. (From Adams et al., Principles of Neurology, 6th ed, p1481)Protective Devices: Devices designed to provide personal protection against injury to individuals exposed to hazards in industry, sports, aviation, or daily activities.Universal Precautions: Prudent standard preventive measures to be taken by professional and other health personnel in contact with persons afflicted with a communicable disease, to avoid contracting the disease by contagion or infection. Precautions are especially applicable in the diagnosis and care of AIDS patients.Caffeine: A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.Alcohol Drinking: Behaviors associated with the ingesting of alcoholic beverages, including social drinking.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Drug Information Services: Services providing pharmaceutic and therapeutic drug information and consultation.Medical Assistance: Financing of medical care provided to public assistance recipients.Uncompensated Care: Medical services for which no payment is received. Uncompensated care includes charity care and bad debts.Beneficence: The state or quality of being kind, charitable, or beneficial. (from American Heritage Dictionary of the English Language, 4th ed). The ethical principle of BENEFICENCE requires producing net benefit over harm. (Bioethics Thesaurus)Copyright: It is a form of protection provided by law. In the United States this protection is granted to authors of original works of authorship, including literary, dramatic, musical, artistic, and certain other intellectual works. This protection is available to both published and unpublished works. (from Circular of the United States Copyright Office, 6/30/2008)Software: Sequential operating programs and data which instruct the functioning of a digital computer.Skin Neoplasms: Tumors or cancer of the SKIN.Skin: The outer covering of the body that protects it from the environment. It is composed of the DERMIS and the EPIDERMIS.Licensure: The legal authority or formal permission from authorities to carry on certain activities which by law or regulation require such permission. It may be applied to licensure of institutions as well as individuals.Moral Obligations: Duties that are based in ETHICS, rather than in law.Drug Overdose: Accidental or deliberate use of a medication or street drug in excess of normal dosage.Pregnancy: The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.Mutagenesis, Site-Directed: Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Ion Channel Gating: The opening and closing of ion channels due to a stimulus. The stimulus can be a change in membrane potential (voltage-gated), drugs or chemical transmitters (ligand-gated), or a mechanical deformation. Gating is thought to involve conformational changes of the ion channel which alters selective permeability.Models, Molecular: Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.NAV1.7 Voltage-Gated Sodium Channel: A voltage-gated sodium channel subtype found widely expressed in nociceptive primary sensory neurons. Defects in the SCN9A gene, which codes for the alpha subunit of this sodium channel, are associated with several pain sensation-related disorders.Cysteine: A thiol-containing non-essential amino acid that is oxidized to form CYSTINE.Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.Aza CompoundsWalesLidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)QuinolinesCounterfeit Drugs: Drugs manufactured and sold with the intent to misrepresent its origin, authenticity, chemical composition, and or efficacy. Counterfeit drugs may contain inappropriate quantities of ingredients not listed on the label or package. In order to further deceive the consumer, the packaging, container, or labeling, may be inaccurate, incorrect, or fake.Pharmaceutical Services, Online: Pharmacy services accessed via electronic means.Adrenergic beta-Antagonists: Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.Romano-Ward Syndrome: A form of long QT syndrome that is without congenital deafness. It is caused by mutation of the KCNQ1 gene which encodes a protein in the VOLTAGE-GATED POTASSIUM CHANNEL.NAV1.5 Voltage-Gated Sodium Channel: A voltage-gated sodium channel subtype that mediates the sodium ion PERMEABILITY of CARDIOMYOCYTES. Defects in the SCN5A gene, which codes for the alpha subunit of this sodium channel, are associated with a variety of CARDIAC DISEASES that result from loss of sodium channel function.

Electrophysiological effects of mexiletine in man. (1/150)

The electrophysiological effects of intravenous mexiletine in a dose of 200 to 250 mg given over 5 minutes, followed by continuous infusion of 60 to 90 mg per hour, were studied in 5 patients with normal conduction and in 20 patients with a variety of disturbances of impulse formation and conduction, by means of His bundle electrography, atrial pacing, and the extrastimulus method. In all but 2 patients the plasma level was above the lower therapeutic limit. Mexiletine had no consistent effects on sinus frequency and atrial refractoriness. The sinoatrial recovery time changed inconsistently in both directions; however, of the 5 patients in whom an increase was evident, 3 had sinus node dysfunction. In most patients mexiletine increased the AV nodal conduction time at paced atrial rates and shifted the Wenckebach point to a lower atrial rate. The effective refractory period of the AV node was not consistently influenced, while the functional refractory period increased in 12 out of 14 patients. The HV intervals increased by a mean of 11 ms in 8 patients and were unchanged in 17. Both the relative and effective refractory period of the His-Purkinje system increased after mexiletine. Non-cardiac side effects occurred in 7 out of 25 patients, and cardiac side effects, including one serious, in 2. The results indicate that mexiletine shares some electrophysiological properties with procainamide and quinidine, when given to patients with conduction defects, and that the drug should not be used in patients with pre-existing impairment of impulse formation or conduction. It has additional effects on AV nodal conduction which may be of value in the treatment of re-entrant tachycardias involving the AV node.  (+info)

Differential effects of lidocaine and mexiletine on relaxations to ATP-sensitive K+ channel openers in rat aortas. (2/150)

BACKGROUND: In cardiac myocytes, lidocaine reduces but mexiletine increases adenosine triphosphate (ATP)-sensitive K+ currents, suggesting that these class Ib antiarrhythmic drugs may differentially modify the activity of ATP-sensitive K+ channels. The effects of lidocaine and mexiletine on arterial relaxations induced by K+ channel openers have not been studied. Therefore, the current study was designed to evaluate whether lidocaine and mexiletine may produce changes in relaxations to the ATP-sensitive K+ channel openers cromakalim and pinacidil in isolated rat thoracic aortas. METHODS: Rings of rat thoracic aortas without endothelia were suspended for isometric force recording. Concentration-response curves were obtained in a cumulative fashion. During submaximal contractions to phenylephrine (3 x 10(-7) M), relaxations to cromakalim (10(-7) to 3 x 10(-5) M), pinacidil (10(-7) to 3 x 10(-5) M), or diltiazem (10(-7) to 3 x 10(-4) M) were obtained. Lidocaine (10(-5) to 3 x 10(-4) M), mexiletine (10(-5) to 10(-4) M) or glibenclamide (5 x 10(-6) M) was applied 15 min before addition of phenylephrine. RESULTS: During contractions to phenylephrine, cromakalim and pinacidil induced concentration-dependent relaxations. A selective ATP-sensitive K+ channel antagonist, glibenclamide (5 x 10(-6) M), abolished these relaxations, whereas it did not alter relaxations to a voltage-dependent Ca2+ channel inhibitor, diltiazem (10(-7) to 3 x 10(-4) M). Lidocaine (more than 10(-5) M) significantly reduced relaxations to cromakalim or pinacidil in a concentration-dependent fashion, whereas lidocaine (3 x 10(-4) M) did not affect relaxations to diltiazem. In contrast, mexiletine (more than 10(-5) M) significantly augmented relaxations to cromakalim or pinacidil. Glibenclamide (5 x 10(-6) M) abolished relaxations to cromakalim or pinacidil in arteries treated with mexiletine (10(-4) M). CONCLUSIONS: These results suggest that lidocaine impairs but mexiletine augments vasodilation mediated by ATP-sensitive K+ channels in smooth muscle cells.  (+info)

Inhibition of human liver cytochrome P-450 1A2 by the class IB antiarrhythmics mexiletine, lidocaine, and tocainide. (3/150)

Mexiletine, lidocaine, and tocainide are class IB antiarrhythmic drugs that are used for the treatment of ventricular arrhythmias and are known to inhibit drug metabolism. The objectives of this study were to characterize the inhibitory effects of mexiletine, lidocaine, and tocainide on cytochrome P-450 1A2 (CYP1A2) activity in human liver microsomes and to evaluate their relative inhibitory potencies by using a molecular model of this P-450 isozyme. The inhibitory effect of mexiletine, lidocaine, and tocainide on cytochrome CYP1A2 in human liver microsomes was examined with methoxyresorufin O-demethylase activity as an index of the catalytic activity of this P-450 isozyme. The kinetic inhibition types and Ki values were determined by Lineweaver-Burk plots and Dixon plots, respectively. Molecular modeling was used to assess the interaction of these agents with the CYP1A2 active site. Methoxyresorufin O-demethylase activity was inhibited 67 +/- 8%, 20 +/- 5%, and 7 +/- 4% by 2 mM mexiletine, lidocaine, and tocainide, respectively. Mexiletine and lidocaine exhibited competitive inhibition with Ki values of 0.28 +/- 0.12 mM and 1.54 +/- 0.74 mM, respectively, whereas the inhibition type of tocainide could not be determined because of its weak potency. A charge interaction between mexiletine and the Asp313 side chain in the CYP1A2 active site was found, and varying degrees of hydrogen bond formation between these three compounds and the CYP1A2 active site were observed. The in vitro inhibitory potencies in human liver microsomes (mexiletine > lidocaine > tocainide) are consistent with the structural interactions found in a molecular model of the active site of CYP1A2.  (+info)

BIIR 561 CL: a novel combined antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors and voltage-dependent sodium channels with anticonvulsive and neuroprotective properties. (4/150)

Antagonists of glutamate receptors of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) subtype, as well as of voltage-gated sodium channels, exhibit anticonvulsive and neuroprotective properties in vivo. One can postulate that a compound that combines both principles might be useful for the treatment of disorders of the central nervous system, like focal or global ischemia. Here, we present data on the effects of dimethyl-(2-[2-(3-phenyl-[1,2, 4]oxadiazol-5-yl)-phenoxy]ethyl)-amine hydrochloride (BIIR 561 CL) on neuronal AMPA receptors and voltage-dependent sodium channels. BIIR 561 CL inhibited AMPA receptor-mediated membrane currents in cultured cortical neurons with an IC50 value of 8.5 microM. The inhibition was noncompetitive. In a cortical wedge preparation, BIIR 561 CL reduced AMPA-induced depolarizations with an IC50 value of 10.8 microM. In addition to the effects on the glutamatergic system, BIIR 561 CL inhibited binding of radiolabeled batrachotoxin to rat brain synaptosomal membranes with a Ki value of 1.2 microM. The compound reduced sodium currents in voltage-clamped cortical neurons with an IC50 value of 5.2 microM and inhibited the veratridine-induced release of glutamate from rat brain slices with an IC50 value of 2.3 microM. Thus, BIIR 561 CL inhibited AMPA receptors and voltage-gated sodium channels in a variety of preparations. BIIR 561 CL suppressed tonic seizures in a maximum electroshock model in mice with an ED50 value of 2.8 mg/kg after s.c. administration. In a model of focal ischemia in mice, i.p. administration of 6 or 60 mg/kg BIIR 561 CL reduced the area of the infarcted cortical surface. These data show that BIIR 561 CL is a combined antagonist of AMPA receptors and voltage-gated sodium channels with promising anticonvulsive and neuroprotective properties.  (+info)

Differential interaction of R-mexiletine with the local anesthetic receptor site on brain and heart sodium channel alpha-subunits. (5/150)

Mexiletine is a class I antiarrhythmic drug with neuroprotective effects in models of brain ischemia attributable to inhibition of brain sodium channels. We compared effects of R-mexiletine on wild-type and mutant rat brain (rbIIA) and heart (rh1) sodium channel alpha-subunits transiently expressed in tsA-201 cells. R-mexiletine induced tonic and frequency-dependent block and bound with a 26-fold (brain) or 35-fold (heart) higher affinity to inactivated sodium channels. Affinities of both resting and inactivated channels for R-mexiletine block were approximately 2-fold higher for heart than for brain channels. Mutations in transmembrane segment IVS6 of heart (rhF1762A) and brain (rbF1764A and rbY1771A) channels, which reduce block by other local anesthetics, reduced high-affinity block of inactivated channels and frequency-dependent block of open channels by R-mexiletine and abolished the difference in affinity between brain and heart sodium channels. Unlike previous local anesthetics studied, the strongest effect was observed for mutation rbY1771A. Comparison of mutations of the homologous phenylalanine residue in brain and heart channels showed striking differences in the effects of the mutations. rbF1764A reduced drug block by slowing R-mexiletine binding to inactivated channels, whereas rhF1762A reduced block by increasing the rate of dissociation from inactivated and resting channels. Thus, rbF1764/rhF1762 is a critical determinant of affinity and tissue-specific differences in mexiletine block of brain and heart sodium channels, but its role in drug interaction differs in these two channel isoforms.  (+info)

Increased hindrance on the chiral carbon atom of mexiletine enhances the block of rat skeletal muscle Na+ channels in a model of myotonia induced by ATX. (6/150)

1 The antiarrhythmic drug mexiletine (Mex) is also used against myotonia. Searching for a more efficient drug, a new compound (Me5) was synthesized substituting the methyl group on the chiral carbon atom of Mex by an isopropyl group. Effects of Me5 on Na+ channels were compared to those of Mex in rat skeletal muscle fibres using the cell-attached patch clamp method. 2 Me5 (10 microM) reduced the maximal sodium current (INa) by 29.7+/-4.4 % (n=6) at a frequency of stimulation of 0.3 Hz and 65.7+/-4.4 % (n=6) at 1 Hz. At same concentration (10 microM), Mex was incapable of producing any effect (n=3). Me5 also shifted the steady-state inactivation curves by -7. 9+/-0.9 mV (n=6) at 0.3 Hz and -12.2+/-1.0 mV (n=6) at 1 Hz. 3 In the presence of sea anemone toxin II (ATX; 5 microM), INa decayed more slowly and no longer to zero, providing a model of sodium channel myotonia. The effects of Me5 on peak INa were similar whatever ATX was present or not. Interestingly, Me5 did not modify the INa decay time constant nor the steady-state INa to peak INa ratio. 4 Analysis of ATX-induced late Na+ channel activity shows that Me5 did not affect mean open times and single-channel conductance, thus excluding open channel block property. 5 These results indicate that increasing hindrance on the chiral atom of Mex increases drug potency on wild-type and ATX-induced noninactivating INa and that Me5 might improve the prophylaxis of myotonia.  (+info)

Antioxidant action of the antiarrhythmic drug mexiletine in brain membranes. (7/150)

Mexiletine is a class Ib antiarrhythmic drug used in the treatment of ventricular arrhythmias. The Na+ channel blocker mexiletine inhibits calcium influx in cells via decreasing reverse operation of the Na+-Ca2+ exchanger. Thus this drug is shown to protect the CNS white matter against anoxic/ischemic injury. The aim of our study was to investigate if this drug could act as an antioxidant drug as well. The antioxidant action of this drug was studied under different oxidant conditions in vitro, and thiobarbituric acid-reactive substances were measured to follow lipid peroxidation. Mexiletine inhibited iron-ascorbate-H2O2-induced lipid peroxidation in brain membranes, liver microsomes and phospholipid liposomes, being most effective in brain membranes. The inhibition was dose- and time-dependent. Mexiletine also inhibited copper-ascorbate-H2O2-induced lipid peroxidation but to a lesser extent. It is concluded that mexiletine has a dual effect toward oxidative injury in brain, both by inhibiting Na+-Ca2+ exchanger-dependent Ca2+ influx and by acting as an inhibitor of lipid peroxidation. However, as this drug is effective at millimolar concentrations, it should be considered less active than natural antioxidants that are effective at micromolar concentrations.  (+info)

Effect of oral mexiletine on the cough response to capsaicin and tartaric acid. (8/150)

BACKGROUND: The effect of the orally active local anaesthetic mexiletine on the cough response to two different tussive agents, a C-fibre ending stimulator capsaicin and a chemostimulant tartaric acid, was examined in normal subjects. METHODS: The cough threshold, defined as the lowest concentration of capsaicin (C(5)-CP) or tartaric acid (C(5)-TA) causing five or more coughs, and histamine induced bronchoconstriction were measured three hours after a single oral dose of 300 mg mexiletine or placebo in 14 normal subjects. RESULTS: Mexiletene in a mean (SE) serum concentration of 0.99 (0. 04) microg/ml significantly increased C(5)-TA from a geometric mean (SE) of 32.0 (1.27) mg/ml with placebo to 49.9 (1.34) mg/ml, but C(5)-CP did not differ significantly between treatment with mexiletine (12.2 (1.33) microM) and placebo (14.9 (1.23) microM). CONCLUSIONS: These results suggest that the cough response to capsaicin and tartaric acid may be mediated in part via different neural pathways.  (+info)

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Mexiletine is well absorbed (~90%) from the gastrointestinal tract. Unlike lidocaine, its first-pass metabolism is low. Peak blood levels are reached in two to three hours. In normal subjects, the plasma elimination half-life of mexiletine is approximately 10 to 12 hours. It is 50 to 60% bound to plasma protein, with a volume of distribution of 5 to 7 liters/kg. Mexiletine is mainly metabolized in the liver, the primary pathway being CYP2D6 metabolism, although it is also a substrate for CYP1A2. With involvement of CYP2D6, there can be either poor or extensive metabolizer phenotypes. Since approximately 90% of mexiletine hydrochloride is metabolized in the liver into inactive metabolites, pathological changes in the liver can restrict hepatic clearance of mexiletine hydrochloride and its metabolites. The metabolic degradation proceeds via various pathways including aromatic and aliphatic hydroxylation, dealkylation, deamination and N-oxidation. Several of the resulting metabolites are submitted ...
Mexiletine has several uses including the treatment of abnormal heart rhythms or arrhythmias, chronic pain, and myotonia. In general when treating arrhythmias, mexiletine is reserved for use in dangerous heart rhythm disturbances such as ventricular tachycardia.[2] It is of particular use when treating arrhythmias caused by long QT syndrome.[3] The LQT3 form of long QT syndrome is amenable to treatment with mexiletine as this form is caused by defective sodium channels that continue to release a sustained current rather than fully inactivating, however other forms of long QT syndrome can also be treated with this medication.[3] Mexiletine has been used to treat chronic pain and may also be used to treat muscle stiffness resulting from myotonic dystrophy (Steinerts disease) or nondystrophic myotonias such as myotonia congenita (Thomsen syndrome or Becker syndrome).[4][5] ...
Mexiletine - Get up-to-date information on Mexiletine side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about Mexiletine
Mexiletine (Mexiletine) drug information & product resources from MPR including dosage information, educational materials, & patient assistance.
Several studies (5,7) reported that LQT3 patients have an excessive risk of arrhythmic events as compared to LQT1, even with beta-blocker treatment. Using an experimental preparation of LQT3, Shimizu and Antzelevitch (16) speculated that beta-blockers may be proarrhythmic in LQT3 and the efficacy of these drugs in LQT3 remains undefined. For these reasons, alternative therapeutic strategies are needed to reduce the risk of life-threatening events in LQT3 patients.. The use of sodium-channel blockers to shorten QT interval in LQT3 therapy has been supported in recent clinical guidelines (Class IIb, Level of Evidence: C) (10) but, due to the lack of clinical data, no recommendation on the antiarrhythmic efficacy of mexiletine in LQT3 was provided.. We demonstrated here for the first time that, besides shortening the QT interval (4,8,9), long-term treatment with mexiletine reduced the occurrence of arrhythmic events in LQT3 patients. During matched-period observations of almost 3 years, both the ...
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Mexiletine is an orally active local anaesthetic agent which is structurally related to lidocaine. Mexiletine capsules are launched worldwide by Boehringer
This eMedTV Web page provides a comprehensive list of products that may cause drug interactions with mexiletine. It describes the complications that could occur when medications like Cerebyx, Prozac, or Wellbutrin are combined with mexiletine.
It is important to know if you need to avoid any Food, Herbs, Alcohol, Caffeine when taking Mexiletine. Drug interaction with any of these substances may enhance or decrease the effect of Mexiletine.
The main types of treatments are surgery and intralesional injection of sclerosant agents. Based on these calculations a model for the differentiation of class Ia and class Ib antiarrhythmic drugs could be side effects for sildenafil deduced. Pretreatment with edaravone can prevent development of cognitive impairment after CEA.. A statistical significance for this measure has been derived using Monte Carlo techniques. Improving the utilization of medical crisis teams (Condition C) at an urban tertiary care hospital. The benefits of off-pump techniques may be more apparent for patients at high risk for complications associated with cardiopulmonary bypass and sildenafil 20 mg aortic manipulation. Total fertilisation rates were significantly reduced in ICSI cycles than IVF but there were no damaged oocytes in IVF cycles regardless of the semen parameters. have been sildenafil 50 mg tablets facilitated by the fundamental problems of asymmetric information and insurance-induced moral hazard. ...
Analysis of Holter Recordings In all three observation periods (baseline and at every 8 and 12 h) the Holter PVC rates used to determine efficacy of the
... Mexitil is an anti-arrhythmic drug. It is used to treat seriously irregular heartbeats, such as persistent ventricular tachycardia.
In each of the five treatment periods, the subjects were dosed three times during the day [Johannesen et al, Clin Pharmacol Ther. 2016]. Dofetilide (Tikosyn, Pfizer, New York, NY) and mexiletine (Teva Pharmaceuticals USA, North Wales, PA) were administered orally immediately after meals, whereas lidocaine (B. Braun Medical, Bethlehem, PA), moxifloxacin and diltiazem were administered intravenously. Intravenous infusions were split into a 60-minute loading dose followed by a 30-minute maintenance dose.. The primary pharmacokinetic samples were taken at the start and end of each of the three maintenance doses during the day (morning, afternoon and evening), as these were expected to be associated with highest plasma concentrations of both the oral and intravenously administered drugs. Additional pharmacokinetic samples were taken at 30 and 120 minutes poststart of intravenous dosing during each of the three dosing periods during the day. There was one week between treatment periods.. During each ...
In each of the five treatment periods, the subjects were dosed three times during the day [Johannesen et al, Clin Pharmacol Ther. 2016]. Dofetilide (Tikosyn, Pfizer, New York, NY) and mexiletine (Teva Pharmaceuticals USA, North Wales, PA) were administered orally immediately after meals, whereas lidocaine (B. Braun Medical, Bethlehem, PA), moxifloxacin and diltiazem were administered intravenously. Intravenous infusions were split into a 60-minute loading dose followed by a 30-minute maintenance dose.. The primary pharmacokinetic samples were taken at the start and end of each of the three maintenance doses during the day (morning, afternoon and evening), as these were expected to be associated with highest plasma concentrations of both the oral and intravenously administered drugs. Additional pharmacokinetic samples were taken at 30 and 120 minutes poststart of intravenous dosing during each of the three dosing periods during the day. There was one week between treatment periods.. During each ...
Easy to read patient leaflet for Mexiletine. Includes indications, proper use, special instructions, precautions, and possible side effects.
... capsules are taken every 8 or 12 hours to help treat potentially dangerous heart rhythm problems. This eMedTV article presents more details on this antiarrhythmia drug, including specific uses, dosing instructions, side effects, and more.
Class Ib antiarrhythmic agents are sodium channel blockers. They have fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. Class Ib agents shorten the action potential duration and reduce refractoriness. These agents will decrease Vmax in partially depolarized cells with fast response action potentials. They either do not change the action potential duration, or they may decrease the action potential duration. Class Ib drugs tend to be more specific for voltage gated Na channels than Ia. Lidocaine in particular is highly frequency dependent, in that it has more activity with increasing heart rates. This is because lidocaine selectively blocks Na channels in their open and inactive states and has little binding capability in the resting state. Class Ib agents are indicated for the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation. Class Ib ...
Our results provide strong support for the hypothesis that an intrinsic defect underlies the LQT phenomenon through characterization of the molecular phenotypes of all three LQTS-linked defects in the primary sequence of the human cardiac Na+ channel. All the mutations result in the potentiation of a late persistent component of inward Na+ current, which would have the effect of delaying myocardial repolarization. The main evidence is that when expressed in a heterologous system, the mutant channels show elevated levels of residual inward current that persist during long test pulses at a time when normal Na+ currents have decayed to nearly zero. This late current was isolated from unrelated background currents by its sensitivity to the specific Na+ channel blockers, TTX and mexiletine. There are mixed reports of the value of mexiletine and other class Ib agents in LQTS patients of unknown genotype.35 36 37 38 Recently, however, mexiletine has been shown to markedly shorten QTc (from 0.54 to 0.45 ...
Mexitil is known as an anti-arrhythmic drug. It works by blocking certain electrical signals in the heart that can cause an irregular heartbeat. Treating an irregular heartbeat can decrease the risk for blood clots, and this effect can reduce your risk of heart attack or stroke. It is used to treat certain types of serious (possibly fatal) irregular heartbeat (such as persistent ventricular tachycardia). It is used to restore normal heart rhythm and maintain a regular, steady heartbeat ...
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Patients with irregular heartbeats, or arrhythmia, have few effective treatment options - available drugs are not always effective, and implanted defibrillators can be too aggressive.. Jonathan Silva, a biomedical engineer in the McKelvey School of Engineering at Washington University in St. Louis, has developed the first computational model that shows the molecular groundwork of a popular drugs effectiveness in a variety of ways. The findings are published in the Journal of the American College of Cardiology: Basic to Translational Science October 2019 issue. Current treatment for arrhythmia is the drug mexiletine, which is designed to block extra current that travels through the sodium channel in the heart that causes it to beat too fast or irregularly. However, the drug is not effective for every patient, though researchers are not clear why. Silvas new model provides some answers. What we found is that the drug doesnt work because part of the channel is getting in the way, said Silva, ...
TY - JOUR. T1 - Mexiletine usage in a chronic pain clinic. T2 - Indications, tolerability, and side effects. AU - Romman, Adam. AU - Salama-Hanna, Joseph. AU - Dwivedi, Samvid. PY - 2018/9/1. Y1 - 2018/9/1. N2 - Background: Background: Intravenous lidocaine has multiple applications in the management of acute and chronic pain. Mexiletine, an oral lidocaine analogue, has been used in a number of chronic pain conditions although its use is not well characterized. Objectives: To report our experience using mexiletine in a chronic pain population, specifically looking at tolerability, side effects, and EKG changes. Study Design: Retrospective, cohort study. Setting: Multiple pain clinic locations in an integrated multispecialty health system. Methods: All patients who had a mexiletine prescription between August 2015 and August 2016 were queried via the electronic medical record. Each chart was examined for demographics, QTc changes on EKG, length of use, and reasons for stoppage. Results:There were ...
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Ischemia-Related Subcellular Redistribution of Sodium Channels Enhances the Proarrhythmic Effect of Class I Antiarrhythmic Drugs: A Simulation Study. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Preliminary research finds that for patients with nondystrophic myotonias (NDMs), rare diseases that affect the skeletal muscle and cause functionally limiting stiffness and pain, use of the anti-arrhythmic medication mexiletine ...
Understanding Buy Lidocaine Online Uk Lidocaine medicated plasters are utilised to deal with pain due to post herpetic neuralgia. Lidocaine operates by stopping the sodium going into the nerve ending at the website of the pain. Lidocaine 5% Ointment might not be suitable or may want to get employed with caution if youre taking some medicines including those to take care of heart arrhythmias (such as tocainamide and mexiletine), or in case you are planning to use other regional anaesthetics for one more condition at the very same moment. The amount of the gel needed varies based on the correction to be achieved and the region to be treated. These gels can be bought at the local drugstore or grocery shop. Lyracaine Gel employs a advances Micro-Emulsion delivery procedure to guarantee fast, effective outcomes. Numbing spray is helpful for numbing legs and massive regions of the body in preparation for waxing. Its also among the ideal delay spray with respect to how soon before sex you may apply ...
Are there any other precautions or warnings for this medication?. Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.. Abnormal heart rhythms: Rufinamide can cause changes to the normal rhythm of the heart, including an irregular heartbeat called QT shortening. QT shortening is a serious condition that can cause fainting and life-threatening heart rhythm problems.. If you are at risk for heart rhythm problems or are taking medications that cause QT shortening (e.g., digoxin, mexiletine, phenytoin, magnesium sulfate), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. People who have or ...
Change in Placebo Corrected Change From Baseline QTc and J-Tpeakc Intervals on the ECG Measured in Milliseconds When Dofetilide is Administered With Mexiletine or Lidocaine Compared to When Dofetilide is Administered Alone at Evening Dose on Treatment ...
Browse many computed properties for this triclinic BiIr3(CO)9 compound, including formation energy from the elements, energy of decomposition into the set of most stable materials at this chemical composition, bulk crystalline density, and band gap. Also known as: Nonacarbonyltetrahedro-bismuthtriiridium. Cite this material using DOI 10.17188/1280736.
Bisphenol A (BPA) has attracted considerable public attention as it leaches from plastic used in food containers, is detectable in human fluids and recent epidemiologic studies link BPA exposure with diseases including cardiovascular disorders. As heart-toxicity may derive from modified cardiac electrophysiology, we investigated the interaction between BPA and hNav1.5, the predominant voltage-gated sodium channel subtype expressed in the human heart. Electrophysiology studies of heterologously-expressed hNav1.5 determined that BPA blocks the channel with a Kd of 25.4±1.3 µM. By comparing the effects of BPA and the local anesthetic mexiletine on wild type hNav1.5 and the F1760A mutant, we demonstrate that both compounds share an overlapping binding site. With a key binding determinant thus identified, an homology model of hNav1.5 was generated based on the recently-reported crystal structure of the bacterial voltage-gated sodium channel NavAb. Docking predictions position both ligands in a cavity
The side effect profile ofhas been well established. Anticholinergic symptoms are most common, but cardiac toxicity is of greatest concern. In particular, the negative inotropic activity and proarrhythmic potential of disopyramide limits its use in s
Previous studies have reported that enhanced antiarrhythmic effects occur when agents that prolong repolarization are combined with agents that block the sodium channels. The mechanism(s) of this interaction have not been elucidated. In this study, the interactions between the prolongation of action potential duration (APD) by a potassium channel blocker and the reduction in the maximal upstroke velocity of phase 0 of action potential (Vmax) by sodium channel blockers were investigated in guinea pig papillary muscle using conventional microelectrode techniques. Agents that produce selective electrophysiologic effects were chosen, including low concentrations of barium chloride (BaCl2), which selectively blocks the inwardly rectifying potassium current without effects on other repolarizing or depolarizing currents, O-demethyl-encainide (ODME), which blocks the activated sodium channel with slow onset/offset kinetics, and mexiletine, which preferentially blocks the inactivated sodium channel with ...
10.1055/b-0035-121513 18 Cardiac Arrhythmias 18.1 Antiarrhythmic Drugs 18.1.1 Basics Antiarrhythmic drugs play a central role in the treatment of cardiac arrhythmias in childhood. But their use must be weighed critically. There are numerous studies in adults showing that class I antiarrhythmic drugs do not reduce mortality, but even increase it in patients with ventricular tachycardia…
Lee et al. 5 % in children who were exposed to passive smoking [77]. Significant reductions in drug concentrations with smoking have been reported for caffeine, chlorpromazine, clozapine, flecainide, fluvoxamine, haloperidol, mexiletine, olanzapine, proprandol, and tacrine due to increased metabolism of these drugs. Smokers may therefore require higher doses than nonsmokers in order to achieve pharmacological responses [76]. Warfarin disposition in smokers is also different than nonsmokers. 8 in an 80-year-old man when he stopped smoking. Moreover, no immunoassay is commercially available for more recently approved drugs, also many other drugs require monitoring and for these drugs chromatographic techniques are the only choice. 13 History of Chromatographic Techniques Chromatographic techniques are separation techniques by physical means where a complex mixture can be resolved into individual components or components of interest without physically altering the components. The word ...
If you have a muscle cramp, stop your activity and try stretching and massaging the muscle. Heat will relax the muscle when the spasm begins, but ice may be helpful when the pain has improved.. If the muscle is still sore, nonsteroidal anti-inflammatory medicines can help with pain. If the muscle cramps are severe, your health care provider can prescribe other medicines.. The most common cause of muscle cramps during sports activity is not getting enough fluids. Often, drinking water will ease the cramping. However, water alone does not always help. Salt tablets or sports drinks, which also replenish lost minerals, can be helpful.. Other tips for relieving muscle cramps:. ...
... People are always susceptible to muscle cramps so we had our forum members detail causes, prevention, and game situations when cramps occur. Learn more!
Muscle cramps are involuntary contractions of one or more of your muscles. Discover what can cause muscle cramps and how you can prevent them.
Muscle cramps, especially in the legs, are a common experience for many when they first adopt a Zero Carb diet. It is one of the many unpleasant symptoms that can occur during the adaptation period, but sometimes they can continue for longer. There are a number of reasons that these muscle cramps occur, but the…
Muscle cramps are can be caused by overexertion, dehydration, magnesium or calcium deficiencies, a poor blood supply to the legs...
Treating muscle cramps requires a multi-tiered approach that includes lifestyle changes, dietary changes and nutritional supplements. Regulating the activity level and eating a balanced diet with plenty of water is important.
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The evaluation of molecules that have potentially bioactive significance is an expanding field, but current screening assays are expensive and time consuming. Mammalian cell-based assays require aseptic techniques, complex media and long generation times. This thesis reports on an assay that incorporates Tetrahymena phagocytic ingestion and flow cytometry to evaluate several potentially bioactive molecules. Several factors that influenced optimal and reproducible results were analyzed. Seven potentially bioactive molecules (serotonin, norepinephrine, dopamine, morphine, colchicine, mexiletine and procainamide) were evaluated to determine their effect on phagocytosis by Tetrahymena. Assay results indicated that the phagocytic rate was unaffected by serotonin, norepinephrine, dopamine, and morphine but inhibited by colchicine, mexiletine and procainamide. The analysis of the data indicated that acclimation time, temperature, cell concentration, and cell wash media affected assay consistency. This
Cetirizine HCl 10 mg. Cetirizine Hydrochloride (UNII. extended release Find patient medical information for cetirizine oral on WebMD including its uses, side.Clenbuterol HCL by Accordo RX is an oral preparation containing 0.04mg of the substance Clenbuterol per tablet. Clenbuterol HCL, as it is often called, is often.. Electrochemical Impedance Spectroscopy Analysis of 2-Mercaptobenzimidazole (2MBI) as Corrosion Inhibitor in HCl 1M.. Flomax In Women For Kidney Stones Tramadol No Prescription Free Shipping Bottom Of Head Hair Loss Tramadol For Infants Uses Of Zyrtec Cetirizine Hydrochloride.What is HCl + CaCo3 (what is the reaction?)?. and calcium chloride is used in many things, notably on roads to keep the dust down. Gladys · hace 1 mes. 0.soda to remove hydrogen chloride and dried before storage. The drying process is essential since traces of. used to measure the oxygen, typically in the range of.If liquid contents are to be used in hard gelatine. _____Selegiline hydrochloride 10.0 mgLiquid ...
Roselli, Mariagrazia, Cavalluzzi, Maria Maddalena, Bruno, Claudio, Lovece, Angelo, Carocci, Alessia, Franchini, Carlo, Habtemariam, Solomon and Lentini, Giovanni (2016) Synthesis and evaluation of berberine derivatives and analogues as potential anti-acetylcholinesterase and antioxidant agents. Phytochemistry Letters, 18. pp. 150-156. ISSN 1874-3900 (Print), 1876-7486 (Online) (doi:10.1016/j.phytol.2016.10.005) Roselli, Mariagrazia, Carocci, Alessia, Budriesi, Roberta, Micucci, Matteo, Toma, Maddalena, Di Cesare Mannelli, Lorenzo, Lovece, Angelo, Catalano, Alessia, Cavalluzzi, Maria Maddalena, Bruno, Claudio, De Palma, Annalisa, Contino, Marialessandra, Perrone, Maria Grazia, Colabufo, Nicola Antonio, Chiarini, Alberto, Franchini, Carlo, Ghelardini, Carla, Habtemariam, Solomon and Lentini, Giovanni (2016) Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues. European Journal of Medicinal Chemistry, 121. pp. 300-307. ISSN 0223-5234 ...
Subject is expected to take within 7 days prior to randomization and during the study: TCAs, mexiletine hydrochloride, lidoderm patch, tramadol, AEDs, dextromethorphan, opioids, capsaicin, nonsteroidal anti-inflammatory drugs, acetaminophen / paracetamol, skeletal muscle relaxants, benzodiazepines, alpha-2-agonists (e.g. clonidine), drugs indicated for sleep disturbance (e. g. zolpidem tartrate, zaleplon) and over-the-counter medications with centrally acting properties ...
Introduction: Class I antiarrhythmic drugs increase duration of the excitable gap (EG) during typical atrial flutter whereas intravenous class III drugs decrease the EG. The effect of chronic oral amiodarone therapy on the EG is unknown. Methods and Results: EG was prospectively determined by introducing a premature stimulus and analyzing the response pattern during typical atrial flutter in 30 patients without antiarrhythmic drugs and in 20 patients under chronic oral amiodarone therapy. EG was calculated by the difference between the longest coupling interval leading to resetting and the effective atrial refractory period (EARP). A fully EG was defined by the portion of EG where the response curve of the return cycles was flat. A partially EG was defined by the portion of EG where the return cycle increases while coupling interval decreases. A resetting response curve was constructed by plotting the duration of the return cycle against the value of the coupling interval. Cycle length (CL; 222 ...
The most common cause of muscle cramps during intense exercise is damage to the muscle fibers themselves. Doctors in South Africa studied triathletes and found that most of the time muscle cramps are not caused by dehydration, thyroid disease, mineral abnormalities (calcium, sodium, magnesium or potassium), blocked blood flow or nerve damage.
Causes of forearm muscle cramps - My wife has severe arm pain in bothnarms, and burning as well from her shoulders to her fingers. Also muscle cramps in both arms. Leg spasms. Help!? Herniated disc. This may be caused by a herniated disc in the cervical spine. She should see a spine specialist. An MRI may be appropriate.
Tonic and use-dependent effects of Gd3+ in different conditions, in which blocker potency is altered. Gray lines illustrate traces elicited in the presence of blocker scaled to the magnitude of control currents in the absence of blocker. (A) In 10 mM Ca2+, application of 0.2 μM Gd3+ reduced peak currents by about one half during the first pulse (I1, tonic block), but to a much greater extent at the second pulse (I2, use-dependent block). (B) With 10 mM Ba2+, both tonic and use-dependent block occurred at 25 nM Gd3+. (C) Although Ba2+ currents inactivated more rapidly in channels with the β3 subunit rather than with the β2a subunit (compare with B), tonic and use-dependent effects of Gd3+ were similar for both β subunits. (D) Exemplar Ca2+ currents through the EEQE mutant of the selectivity locus recorded with and without 2 μM Gd3+. (E) Dose-response curves for tonic effect of Gd3+ determined for different experimental conditions (indicated). Tonic block is described by relative magnitude of ...
... is a member of the sodium channel blocking class of antiepileptic drugs.[60] This may suppress the release of glutamate and aspartate, two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs,[62] but it could have additional actions since it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and is effective in the treatment of the depressed phase of bipolar disorder, whereas other sodium channel blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side-effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasises its unique properties.[63] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and ...
TCAs were the first medications that had dual mechanism of action. The mechanism of action of tricyclic secondary amine antidepressants is only partly understood. TCAs have dual inhibition effects on norepinephrine reuptake transporters and serotonin reuptake transporters. Increased norepinephrine and serotonin concentrations are obtained by inhibiting both of these transporter proteins. TCAs have substantially more affinity for norepinephrine reuptake proteins than the SSRIs. This is because of a formation of secondary amine TCA metabolites.[24][25] In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of norepinephrine in or near the synaptic clefts. Actions of imipramine-like tricyclic antidepressants have complex, secondary adaptions to their initial and sustained actions as inhibitors of norepinephrine transport and variable blockade of serotonin transport. Norepinephrine interacts with postsynaptic α and β adrenergic ...
... (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain.[1] It is not effective for absence or myoclonic seizures.[1] It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder.[3][1] Carbamazepine appears to work as well as phenytoin and valproate for focal and generalised seizures.[4] Common side effects include nausea and drowsiness.[1] Serious side effects may include skin rashes, decreased bone marrow function, suicidal thoughts, or confusion.[1] It should not be used in those with a history of bone marrow problems.[1] Use during pregnancy may cause harm to the baby; however, stopping the medication in pregnant women with seizures is not recommended.[1] Its use during breastfeeding is not recommended.[1] Care should be taken in those with either kidney or liver problems.[1] Carbamazepine was discovered in 1953 by Swiss chemist Walter ...
In Peru, the ancient Incas are believed to have used the leaves of the coca plant as a local anaesthetic in addition to its stimulant properties.[59] It was also used for slave payment and is thought to play a role in the subsequent destruction of Incas culture when Spaniards realized the effects of chewing the coca leaves and took advantage of it.[59] Cocaine was first used as a local anesthetic in 1884. The search for a less toxic and less addictive substitute led to the development of the aminoester local anesthetics stovaine in 1903 and procaine in 1904. Since then, several synthetic local anesthetic drugs have been developed and put into clinical use, notably lidocaine in 1943, bupivacaine in 1957, and prilocaine in 1959. The invention of clinical use of local anaesthesia is credited to the Vienna School which included Sigmund Freud (1856-1939), Carl Koller (1857-1944) and Leopold Konigstein (1850-1942). They introduced local anaesthesia, using cocaine, through 'self-experimation' on their ...
Diagnosis of pain conditions relies on the character of the pain with a sharp stabbing character and the presence of particular features such as mechanical allodynia and cold allodynia. Neuropathic pain also tends to affect defined dermatomes and there may be limits to the area of pain. For neuropathic pain, clinicians look for an underlying lesion to the nervous system or an inciting cause consistent with the development of neuropathic pain. The obvious presence of an underlying feature or cause is not always detectable, and response to treatment may be used as a surrogate particularly in cases where diagnosis of the underlying lesion leaves the patient in pain for a prolonged period of time. MRI may be helpful in the identification of underlying lesions, reversible causes or serious underlying conditions such as primary presentation of a tumor or multiple sclerosis. Quantitative sensory testing (QST), a system of detailed analysis of the somatosensory system, is frequently used in research ...
Longer nerve fibers are affected to a greater degree than shorter ones because nerve conduction velocity is slowed in proportion to a nerve's length. In this syndrome, decreased sensation and loss of reflexes occurs first in the toes on each foot, then extends upward. It is usually described as a glove-stocking distribution of numbness, sensory loss, dysesthesia and night time pain. The pain can feel like burning, pricking sensation, achy or dull. A pins and needles sensation is common. Loss of proprioception, the sense of where a limb is in space, is affected early. These patients cannot feel when they are stepping on a foreign body, like a splinter, or when they are developing a callus from an ill-fitting shoe. Consequently, they are at risk of developing ulcers and infections on the feet and legs, which can lead to amputation. Similarly, these patients can get multiple fractures of the knee, ankle or foot, and develop a Charcot joint. Loss of motor function results in dorsiflexion, ...
... has a potential for drug interactions; caution should be used in combining other medicines with it, including other antiepileptics and mood stabilizers.[12] Lower levels of carbamazepine are seen when administrated with phenobarbital, phenytoin, or primidone, which can result in breakthrough seizure activity. Carbamazepine, as a CYP450 inducer, may increase clearance of many drugs, decreasing their concentration in the blood to subtherapeutic levels and reducing their desired effects.[19] Drugs that are more rapidly metabolized with carbamazepine include warfarin, lamotrigine, phenytoin, theophylline, and valproic acid.[12] Drugs that decrease the metabolism of carbamazepine or otherwise increase its levels include erythromycin,[20] cimetidine, propoxyphene, and calcium channel blockers.[12] Carbamazepine also increases the metabolism of the hormones in birth control pills and can reduce their effectiveness, potentially leading to unexpected pregnancies.[12] As a drug that induces ...
... is a class of prescription drugs in India appearing as an appendix to the Drugs and Cosmetics Rules, 1945 introduced in 1945. These are drugs which cannot be purchased over the counter without the prescription of a qualified doctor.The manufacture and sale of all drugs are covered under the Drugs and Cosmetics Act and Rules. It is revised at times based on the advice of the Drugs Technical Advisory Board, part of the Central Drugs Standard Control Organization[1] in the Ministry of Health and Family Welfare. The most recent schedule H (2006) lists 536 drugs from abacavir to zuclopenthixol.[2] However, enforcement of Schedule H laws in India is lax, compared to the more restrictive Schedule X, for which a mandatory documentation trail must be maintained.[3] ...
IB組:阻斷快速性Na+通道(Lidocaine (Xylocaine®));(Mexiletine(Mexitil®));(Phenytoin(Diphenylhydantoin; Dilantin®)) ...
There is a strong body of evidence that the so-called sensitization of the central nervous system contributes to the emergence of allodynia. Sensitization refers to the increased response of neurons following repetitive stimulation. In addition to repeated activity, the increased levels of certain compounds lead to sensitization. The work of many researchers has led to the elucidation of pathways that can result in neuronal sensitization both in the thalamus and dorsal horns. Both pathways depend on the production of chemokines and other molecules important in the inflammatory response. An important molecule in the thalamus appears to be cysteine-cysteine chemokine ligand 21 (CCL21). The concentration of this chemokine is increased in the ventral posterolateral nucleus of the thalamus where secondary nociceptive neurons make connections with other neurons. The source of CCL21 is not exactly known, but two possibilities exist. First, it might be made in primary nociceptive neurons and transported ...
Medications within the tetracycline family, mexiletine, corticosteroids and nerve blocks are being studied. Occipital nerve ...
They include lidocaine, mexiletine and phenytoin. Class Ic greatly slow phase 0 depolarization in the ventricles (however ...
The medications mexiletine or carbamazepine are occasionally helpful. Pain if it occurs may be treated with tricyclic ...
Class Ib agents include lidocaine, mexiletine, tocainide, and phenytoin. Class Ic antiarrhythmic agents markedly depress the ...
It is also commonly known as 2,6-dimethylphenol (DMP). A known application of DMP is in the synthesis of Mexiletine. 2,6- ...
... and mexiletine. Cardiopulmonary bypass is used if symptoms are refractory to treatment with these drugs. Successful use of ...
Mexiletine, a sodium channel blocker: In LQT3, the sodium channel does not close properly. Mexiletine closes these channels and ... Theoretically, mexiletine could be useful for people with this form of LQTS, but the medication is currently under study for ...
Others, however, require treatment for their muscle stiffness and often find mexiletine to be helpful. Others have found ...
... and orientation-dependent effects of mexiletine and quinidine on conduction in the intact dog heart". Circulation. 75 (5): 1065 ...
... and mexiletine and other local anaesthetic analogues. ...
It has been demonstrated that sotalol alone, or a combination of mexiletine and atenolol, results in a reduction in the ... A number of medications have been used for this purpose, including atenolol, procainamide, sotalol, mexiletine, and amiodarone ...
This species is also able to stereoselectively biotransform rac-mexiletine into hydroxymethyl mexiletine (HMM) and p- ... ISBN 978-0-387-92206-5. "Stereoselective metabolism of rac-mexiletine by the fungus Cunninghamella echinulata yields the major ... trypticase soy medium or peptone broth at a pH of 8 yielded 0 μg/ml of breakdown products from the metabolism of rac-mexiletine ...
... and of mexiletine. Mutations of Nav1.7 have been linked to itching (pruritus), and genetic knockouts of Nav1.7 and an antibody ...
... mexiletine போன்றன பயன்படுத்தப்படும். ஆனால் நீண்டகால சிகிச்சை எதுவும் அறியப்பட்டிருக்கவில்லை. ...
In five of the cases, the lidocaine treatment was combined with mexiletine (Mexitil®), which is a class 1B anti-arrhythmic with ...
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Mexiletine: learn about side effects, dosage, special precautions, and more on MedlinePlus ... Mexiletine should be taken with food or an antacid to prevent stomach upset. Take mexiletine at around the same times every day ... Mexiletine controls arrhythmias but does not cure them. Continue to take mexiletine even if you feel well. Do not stop taking ... Mexiletine is used to treat certain types of ventricular arrhythmias (abnormal heart rhythms). Mexiletine is in a class of ...
"Mexiletine". www.drugbank.ca. Retrieved 2019-06-17.. *^ "Lupin announces launch of NaMuscla". www.biospectrumindia.com. ... Mexiletine is predominantly metabolised by the liver. The pharmacokinetics of mexiletine are preserved with even moderate to ... Mexiletine (INN) (sold under the trade names Mexitil and NaMuscla) is a drug used to treat abnormal heart rhythms, chronic pain ... Mexiletine is an oral analogue of lidocaine.[5] It is a class IB antiarrhythmic which prolongs the refractory period by ...
Prescriber Checkup » MEXILETINE HCL MEXILETINE HCL. Mexitil (mexiletine) is anti-arrhythmic medicine. It treats heart rate ...
Mexiletine is used to treat seriously irregular heartbeats. Mexiletine may also be used for purposes not listed in this ... Mexiletine affects the way that your heart beats. ... Mexiletine 150 mg-TEV. slide 1 of 3, Mexiletine 150 mg-TEV, ... What is mexiletine?. Mexiletine affects the way that your heart beats.. Mexiletine is used to treat seriously irregular ... What is the most important information I should know about mexiletine?. You should not use mexiletine if you have a serious ...
Easy to read patient leaflet for Mexiletine. Includes indications, proper use, special instructions, precautions, and possible ... What do I need to tell my doctor BEFORE I take Mexiletine?. *If you have an allergy to mexiletine or any other part of ... Take mexiletine with food or an antacid. *Keep taking this medicine as you have been told by your doctor or other health care ... What are some things I need to know or do while I take Mexiletine?. *Tell all of your health care providers that you take this ...
Find the most comprehensive real-world treatment information on Mexiletine at PatientsLikeMe. 24 patients with fibromyalgia, ... bipolar I disorder or psoriasis currently take Mexiletine. ... 4 patient evaluations for Mexiletine Sort by: Most recent * ... Showing 3 of 4 patient evaluations for Mexiletine Previous page 1 2 Next page ...
... *Formula: C15H21NO4 ... MEXILETINE, M (HO-) ISOMER 1, AC. *MEXILETINE, M(HO-) ISOMER 3 ...
Mexilitine is an anti-arrhythmic agent used to treat neuropathic pain. The drug has a low side-effect profile with gastritis as the predominant complaint. The following two cases suggest that mexilitine can potentially cause persistent ophthalmic cha
Drug: Mexiletine *Blisters of 10 capsules of 200 mg mexiletine hydrochloride.. *Patients will receive gradual dose of the ... Drug: Mexiletine *Blisters of 10 capsules of 200 mg mexiletine hydrochloride.. *Patients will receive gradual dose of the ... Mexiletine and Non Dystrophic Myotonias (MYOMEX). The safety and scientific validity of this study is the responsibility of the ... Mexiletine will be started at 200 mg / day (1 capsule to be taken at the beginning of the meal) and will be increased by 200mg ...
Caffeine when taking Mexiletine. Drug interaction with any of these substances may enhance or decrease the effect of Mexiletine ... Drug Name : Mexiletine. Mexiletine is used to treat irregular heart rhythms (arrhythmias) and maintain a normal heart rate. It ... How to Take the Medication - Mexiletine Mexiletine is available in the form of a capsule. You may take this 3 times in a day ... Mexiletine Interactions with Alcohol. Mexiletine alone can cause dizziness and lightheadedness. When you take it with alcohol, ...
Mexiletine in Sporadic Amyotrophic Lateral Sclerosis (Mexiletine-2). The safety and scientific validity of this study is the ... Active Comparator: Mexiletine, 300 milligrams Mexiletine, 300 milligrams by mouth per day for 4 weeks. ... Active Comparator: Mexiletine, 600 milligrams Mexiletine, 600 milligrams by mouth per day for 4 weeks. ... the participants will be taking either 300mg/day of mexiletine, 600mg/day of mexiletine, or placebo (non-active study drug). ...
Mexiletine:. Mexiletine is a medication closely related to lidocaine that can be taken by mouth (instead of being injected). ... Mexiletine stops the type of sodium currents that are thought to cause muscle cramps. Mexiletine is a relatively older ... Mexiletine for the Treatment of Muscle Cramps in ALS. The safety and scientific validity of this study is the responsibility of ... The purpose of this study is to determine if mexiletine is effective for the treatment of muscle cramps in Amyotrophic Lateral ...
A formulation for preparing Mexiletine Hydrochloride 10-mg/mL Oral Suspension. Includes ingredients, method of preparation, ... Mexiletine Hydrochloride 10-mg/mL Oral Suspension. Allen Loyd V Jr May/Jun 2006. 225. Buy. ... Related Keywords: mexiletine, ventricular arrhythmias, neuropathic pain, class Ib antiarrhythmic agent, heart disease, ... Abstract: A formulation for preparing Mexiletine Hydrochloride 10-mg/mL Oral Suspension. Includes ingredients, method of ...
Lidocaine and mexiletine are class 1B antiarrhythmic drugs that act on sodium channels. Lidocaine is also an important ... and mexiletine is commonly used for neuropathic pain and myotonia. Both intravenous lidocaine and mexiletine are increasingly ... This is a practical review of mexiletine in the treatment of refractory headache in a tertiary headache clinic. CrossRefPubMed ... Scott RM: Mexiletine and vascular headaches. N Z Med J 1981, 93:92-93.PubMedGoogle Scholar ...
Mexiletine) drug information & product resources from MPR including dosage information, educational materials, & patient ... Indications for Mexiletine:. Documented life-threatening ventricular arrhythmias.. Adult:. Take with food or antacid. Initially ...
Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator ... Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator. * ... Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator. ... enantiomer of the orally active drug mexiletine 5 (a fragment hit from X-ray crystallographic screening) was the chemical ...
Teva Pharmaceuticals USA might be nations only maker of mexiletine hydrochloride. Dog stuck in crate highlights rare risk of ... Mexiletine hydrochloride in 150-mg capsules came back on the market last week after spending six months on backorder, yet ... Mexiletine hydrochloride is back in 150-mg capsules 4/9/2010 *Supply lines hazy ... Licensed only for human use, the popularity of mexiletine hydrochloride has waned in recent years due to its known ...
Learn more about Mexiletine for heart rate control in dogs and cats. Learn more about CVCA and our excellent veterinary care. ... Mexiletine. What is Mexiletine?. Mexiletine is an oral medication belonging to a group of medications known as antiarrhythmics ... Mexiletine has less effect on overall heart rate and heart muscle strength in comparison to some of the other commonly used ... Potassium levels may need to be monitored, as Mexiletine is more effective in the face of normal blood potassium levels ...
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Hi I was hoping others who are on or have tried mexiletine could chime in with their experience. Apologies in advance for the ... mexiletine side effects please advise Hi I was hoping others who are on or have tried mexiletine could chime in with their ... Re: mexiletine side effects please advise Heres what I found on Mexiletine side effects:. Adverse Reactions. ,10%:. ... I was told there is a possible drug:drug interaction between amylyx and mexiletine and that they want me to start mexiletine at ...
Because both lidocaine and mexiletine are frequently used antiarrhythmic drugs during my ... 89 μm for mexiletine.ConclusionsBoth lidocaine and mexiletine reduced flavoprotein fluorescence induced by diazoxide in rat ... Lidocaine (10−3 to 10 mm) and mexiletine (10−3 to 10 mm) reduced oxidation of the mitochondrial matrix in a dose-dependent ... Lidocaine or mexiletine was applied after administration of diazoxide (25 μm), a selective mitochondrial KATP channel opener. ...
MEXILETINE (mex IL e teen) is an antiarrhythmic agent. This medicine is used to treat irregular heart rhythm and can slow rapid ... mexiletine (generic name). This medicine is used to treat irregular heart rhythm and can slow rapid heartbeats ... an unusual or allergic reaction to mexiletine, other medicines, foods, dyes, or preservatives ...
Get up-to-date information on Mexiletine side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about ... How was your experience with Mexiletine?. First, a little about yourself. Male Female ... Mexiletine comes in capsule form. It is usually taken 3 times daily, every 8 hours. Sometimes it must be taken twice daily, ... Take mexiletine with food or an antacid to prevent stomach upset. Common side effects include poor upset stomach, ...
Using a dose of 10 mg/kg/day over a 4-week period, mexiletine produced improvement in pain in 8 of the 9 patients. Mexiletine ... Our findings suggest that mexiletine may be a safe and effective agent in the management of thalamic pain and possibly other ... We present our results of a preliminary open label study using mexiletine, an orally active antiarrhythmic agent, in the ... Using a dose of 10 mg/kg/day over a 4-week period, mexiletine produced improvement in pain in 8 of the 9 patients. Mexiletine ...
  • I was told there is a possible drug:drug interaction between amylyx and mexiletine and that they want me to start mexiletine at just once per day (150mg) first for a few week while they monitor me, then they will let me try going up to twice a day (total=300mg) with continued monitoring. (alsforums.com)
  • We present our results of a preliminary open label study using mexiletine, an orally active antiarrhythmic agent, in the management of thalamic pain in 9 patients. (semanticscholar.org)
  • BACKGROUND AND PURPOSE: The non-selective sodium channel inhibitor mexiletine has been found to be effective in several animal models of chronic pain and has become popular in the clinical setting as an orally available alternative to lidocaine. (ox.ac.uk)
  • Mexiletine (mexiletene) and tocainide are analogues of ligno-caine with modified structures (to enable them to be adminis-tered orally for long periods). (brainkart.com)
  • Mexiletine is a primary amine similar to lignocaine, but orally active. (brainkart.com)
  • Mexiletine is rapidly and well absorbed (greater than 90%) when administered orally. (brainkart.com)
  • Talk to your doctor about the risks of taking mexiletine. (medlineplus.gov)
  • We compared state-dependent affinities of mexiletine for Nav1.2, Nav1.4 and Nav1.5, and examined the effects of mutations of S6 residues in Nav1.5 affecting local anesthetic binding on mexiletine block. (aspetjournals.org)
  • In the present report, we present evidence indicating that systemic mexiletine, a local anesthetic and antiarrhythmic agent, effectively relieves the allodynia-like symptoms at doses of 15 and 30 mg/kg in these rats without inducing major side effects. (muscimol.xyz)
  • Mexiletine has been used to treat chronic pain and may also be used to treat muscle stiffness resulting from myotonic dystrophy ( Steinert's disease ) or nondystrophic myotonias such as myotonia congenita (Thomsen syndrome or Becker syndrome). (wikipedia.org)
  • Mexiletine may also be of use in patients experiencing refractory pain and is also effective for treating muscle stiffness resulting from myotonic dystrophy (Steinert's disease) or nondystrophic myotonias such as myotonia congenita (Thomsen disease). (wikipedia.org)
  • Do not stop taking mexiletine without talking to your doctor. (medlineplus.gov)
  • If you suddenly stop taking mexiletine, your condition may become worse. (medlineplus.gov)
  • Do not skip doses, change your dosing schedule, or stop taking mexiletine without talking to your doctor. (cigna.com)
  • Your doctor will probably start you on an average dose of mexiletine and gradually increase or decrease your dose, not more than once every 2 to 3 days. (medlineplus.gov)
  • So I took my first dose of mexiletine this morning shortly after my morning amylyx and other AM meds. (alsforums.com)
  • Antiarrhythmic drugs, similar to mexiletine, have been reported to increase the risk of death or heart attack, especially in people who have had a heart attack within the past 2 years. (medlineplus.gov)
  • Extracellularly applied QX-314, a membrane-impermeant derivative of lidocaine, elicited significantly enhanced tonic block in S1710L similar to mexiletine. (aspetjournals.org)
  • Many other medications may also interact with mexiletine, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list. (medlineplus.gov)
  • Other drugs may interact with mexiletine, including prescription and over-the-counter medicines, vitamins, and herbal products. (cigna.com)
  • Capillary zone electrophoresis for separation and quantitative determination of mexiletine and its main phase I metabolites. (semanticscholar.org)
  • To validate these observations, we have exploited a naturally occurring cardiac Na + channel mutation, S1710L, located next to the putative selectivity filter residue of domain 4, and evaluated the pharmacological properties to mexiletine using whole-cell, patch-clamp recordings. (aspetjournals.org)
  • Objectives The aim of this study was to determine whether mexiletine prevents arrhythmic events (arrhythmic syncope, aborted cardiac arrest, or sudden cardiac death) in LQT3 patients. (onlinejacc.org)
  • In patients with normal conduction systems, mexiletine has a minimal effect on cardiac impulse generation and propagation. (rxdrugsinfo.com)
  • Mild depression of myocardial function, similar to that produced by lidocaine, has occasionally been observed following intravenous mexiletine therapy in patients with cardiac disease. (rxdrugsinfo.com)
  • Quantum Mechanics/Molecular Mechanics Modeling of Drug Metabolism: Mexiletine N-Hydroxylation by Cytochrome P450 1A2. (semanticscholar.org)
  • Stereoselective metabolism of rac-mexiletine by the fungus Cunninghamella echinulata yields the major human metabolites hydroxymethylmexiletine and p-hydroxymexiletine. (semanticscholar.org)
  • Mexiletine is mainly metabolized in the liver, the primary pathway being CYP2D6 metabolism, although it is also a substrate for CYP1A2. (rxdrugsinfo.com)
  • To precisely investigate the effect of CYP2D6*10B and CYP2D6*36 frequently found in Oriental populations on mexiletine metabolism in vitro, CYP2D6 proteins of wild-type (CYP2D6.1) and variants (CYP2D6.10 and CYP2D6.36) were heterologously expressed in yeast cells and their mexiletine p- and 2-methyl hydroxylation activities were determined. (elsevier.com)
  • These findings suggest that CYP2D6*36 has a more drastic impact on mexiletine metabolism than CYP2D6*10. (elsevier.com)
  • The safety profile of mexiletine is good, with the most frequent side effects being nausea or other abdominal symptoms. (clinicaltrials.gov)
  • Neuro is the site investigator for the amylyx trial she is the one advised me there might be a drug interaction with mexiletine but i was under the impression the interaction would have cardio side effects. (alsforums.com)
  • This is not a complete list of mexiletine side effects. (rxwiki.com)
  • Just like any medicine, mexiletine can cause side effects. (emedtv.com)
  • Click Mexiletine Side Effects to learn more, including potentially serious side effects you should report immediately to your healthcare provider. (emedtv.com)
  • It remains unclear why patients with monogenic pain disorders secondary to gain-of-function SCN9a mutations benefit from a low systemic concentration of mexiletine, which does not usually induce adverse neurological side effects. (ox.ac.uk)
  • Objectives: To report our experience using mexiletine in a chronic pain population, specifically looking at tolerability, side effects, and EKG changes. (utmb.edu)
  • Efficacy of oral mexiletine therapy at a 12-h dosage interval. (semanticscholar.org)
  • Take the prescribed amount of Mexiletine that your doctor has specifically written for you and do not change the frequency or duration of the treatment or size of dosage in any way. (healthery.com)
  • To provide a steady supply of Mexiletine to your system, thereby increasing the effectiveness on your heart rhythm, it is advised that you take the dosage at evenly spaced times during the day without missing any doses. (healthery.com)
  • In patients with normal heart function, mexiletine has a minimal effect on heart rhythm. (clinicaltrials.gov)
  • By maintaining a steady, regular heart rhythm, Mexiletine prevents this irregular rhythm that can eventually lead to blood clots, stroke or heart attack if left untreated. (healthery.com)
  • In this trial, the participants will be taking either 300mg/day of mexiletine, 600mg/day of mexiletine, or placebo (non-active study drug). (clinicaltrials.gov)
  • The study is a double-blinded, placebo controlled (i.e., the investigator and the participant does not know if the pills contain mexiletine or placebo), crossover (all subjects receive two weeks of mexiletine and two weeks of placebo) study. (clinicaltrials.gov)
  • Participants who filled out their diary will be randomly assigned to either mexiletine or placebo for their first two weeks. (clinicaltrials.gov)
  • The 5 treatment periods are 1) dofetilide alone, 2) mexiletine with and without dofetilide, 3) lidocaine with and without dofetilide, 4) moxifloxacin with and without diltiazem and 5) placebo. (mit.edu)
  • Mexiletine is used to treat seriously irregular heartbeats. (cigna.com)
  • Mexiletine works by inhibiting the electrical impulses that seem to be over-stimulating the heart, causing an irregular rhythm. (healthery.com)
  • Methods The endpoint of this retrospective cohort study, which studied consecutive LQT3 patients who were referred to our center and treated with mexiletine, was to evaluate the antiarrhythmic efficacy of mexiletine by comparing the number of arrhythmic events per patient and the annual rate of arrhythmic events during observation periods of equal duration before and after the beginning of therapy with mexiletine. (onlinejacc.org)
  • More research is needed regarding efficacy and dose titration for mexiletine in chronic pain. (utmb.edu)
  • Toxicity potential of oral lidocaine in a patient receiving mexiletine. (nextgenhacks.ml)
  • Mexiletine, an oral lidocaine analogue, has been used in a number of chronic pain conditions although its use is not well characterized. (utmb.edu)
  • Mexiletine has been shown also to be protective of neurons following spinal cord, head injury, and cerebral ischemia, largely by blocking excitotoxicity. (clinicaltrials.gov)
  • Mexiletine also has neuroprotective effects in the models of brain ischemia. (aspetjournals.org)