"Tocainide"

Tocainide An official website of the United States government Here's how you know Log inAccess keysNCBI HomepageMyNCBI HomepageMain ContentMain NavigationBookshelfSearch databaseBooksAll DatabasesAssemblyBiocollectionsBioProjectBioSampleBooksClinVarConserved DomainsdbGaPdbVarGeneGenomeGEO DataSetsGEO ProfilesGTRHomoloGeneIdentical Protein GroupsMedGenMeSHNLM and EffectsSummary of Use during LactationTocainide was removed from the market in the United States in 2003 because it can cause serious and potentially fatal hematological adverse effects. Limited data indicate that rather large amounts of tocainide are excreted into breastmilk. Because of the relative lack of data concerning breastfeeding during maternal tocainide therapy and is potential toxicity, tocainide

Increased sodium channel use-dependent inhibition by a new potent analogue of tocainide greatly enhances in vivo antimyotonic activity Although the sodium channel blocker, mexiletine, is the first choice drug in myotonia, some myotonic patients remain unsatisfied due to contraindications, lack of tolerability, or incomplete response. More therapeutic options are thus needed for myotonic patients , which require clinical trials based on solid preclinical data. In previous structure-activity relationship studies, we identified two newly-synthesized derivatives of tocainide, To040 and To042, with greatly enhanced potency and use-dependent behavior in inhibiting sodium currents in frog skeletal muscle fibers. The current study was performed to verify their potential as antimyotonic agents. Patch

. There are no other licensed treatments for myotonia in patients with non-dystrophic myotonia. It 6 has been approved in France for the symptomatic treatment of myotonic syndromes and has been used as an unlicensed medicine for the treatment of non-dystrophic myotonia in the UK for decades. Several medicines are also used off-label, including flecainide, phenytoin, procainamide, and tocainide. The EMA notes

used as an unlicensed medicine for the treatment of non-dystrophic myotonia in the UK for decades. Several medicines are also used off-label, including flecainide, phenytoin, procainamide, and tocainide. The EMA notes that these medicines cannot be recommended as treatment for myotonia, because of associated severe side effects.1, 2 The key study (MYOMEX) in patients with myotonia congenita

Searching for novel anti-myotonic agents: Pharmacophore requirement for use-dependent block of skeletal muscle sodium channels by N-benzylated cyclic derivatives of tocainide Drug screening on sodium currents of native myofibers by means of voltage-clamp recordings is predictive of pre-clinical anti-myotonic activity in vivo and ex vivo. By this approach we identified the N-benzylated beta -proline derivative of tocainide (To10) as the most potent use-dependent blocker of Nav1.4 so far. We tested novel analogs with modifications on the pharmacophore groups of To10. The substitution of the proline cycle with less planar piperidine or piperazine rings disclosed the importance of a two carbon atom distance and/or an additional nitrogen atom for potency. Structural changes on the xylididic

, Wegner or Goodpasture disease) - Often included with this group; however, predominant manifestation is vasculitis rather than fibrosis DPLDs related to drug exposure include the following: * * Cytotoxic agents (eg, bleomycin, busulfan, methotrexate) * * Antibiotics (eg, nitrofurantoin, sulfasalazine) * * Antiarrhythmics (eg, amiodarone, tocainide) * * Anti-inflammatory

results and improve the tolerance to treatment. Intravenous lidocaine can be used to treat acute pain, whereas botulinum toxin A might be used as refractory therapy. Proparacaine, dextromethorphan, and tocainide were generally reported to be inappropriate for treating TN.Additional outcome(s)most of the drugs reviewed in our article were inadequately studied. Thus, further studies are required

) 2. Class Ib: Shortens Action Potential duration 1. Lidocaine (Xylocaine) 2. Tocainide (Tonocard) 3. Mexiletine (Mexitil) 4. Phenytoin (Dilantin) 3. Class Ic: Slows conduction 1. Precautions 1. Increased proarrhythmia risk and risk of Sudden Cardiac Death 2. Avoid in structural heart disease, Coronary Artery Disease and Left Ventricular Hypertrophy 3. Must use

) 30 to 100 mg PO qhs 2. Doxepin (Sinequan) 50 to 75 mg PO qhs 3. Imipramine (Tofranil) 50 to 75 mg PO qhs 2. Systemic Anesthetics 1. Mexiletine (Mexitil) 200 mg PO q8 hours 2. Tocainide (Tonocard) 400 mg PO q8 hours 3. Other medications for refractory pain 1. Gabapentin (Neurontin) 300 mg PO tid

, small initial doses (10-100 μg boluses in adults) are preferable * * Vasopressin is not recommended * * Avoid calcium channel blockers and beta-blockers * * If ventricular arrhythmias develop, amiodarone is preferable In patients with cardiac toxicity, avoiding the use of lidocaine and related class IB antidysrhythmic agents (eg, mexiletine, tocainide) is crucial because they may worsen

] * * Sulfasalazine [2, 10, 12, 24] AntiarrhythmicsAntiarrhythmics include the following: * * Amiodarone [26] * * Disopyramide [10, 12] * * Procainamide [1, 2, 6, 10, 12, 27] * * Propafenone [10, 12] * * Tocainide [2] * * Quinidine [1, 2, 10, 12, 27] AntibioticsAntibiotics include the following: * * Amoxicillin + clavulanic acid [2, 19, 25] * * Cefepime [28] * * Ciprofloxacin [2, 19

, Wegner or Goodpasture disease) - Often included with this group; however, predominant manifestation is vasculitis rather than fibrosis DPLDs related to drug exposure include the following: * * Cytotoxic agents (eg, bleomycin, busulfan, methotrexate) * * Antibiotics (eg, nitrofurantoin, sulfasalazine) * * Antiarrhythmics (eg, amiodarone, tocainide) * * Anti-inflammatory

, codeine) * * Antidepressants - These drugs modulate sympathetic activity and provide analgesia (eg, amitriptyline) * * Anticonvulsants (eg, phenytoin) * * Membrane-stabilizing agents (eg, lidocaine, tocainide) * * Adrenergic compounds - Phentolamine (relief with intravenous [IV] phentolamine is pathognomic of sympathetically maintained pain [SMP], and patients with a positive response to IV

, codeine) * * Antidepressants - These drugs modulate sympathetic activity and provide analgesia (eg, amitriptyline) * * Anticonvulsants (eg, phenytoin) * * Membrane-stabilizing agents (eg, lidocaine, tocainide) * * Adrenergic compounds - Phentolamine (relief with intravenous [IV] phentolamine is pathognomic of sympathetically maintained pain [SMP], and patients with a positive response to IV

: * * If epinephrine is used, small initial doses (10-100 μg boluses in adults) are preferable * * Vasopressin is not recommended * * Avoid calcium channel blockers and beta-blockers * * If ventricular arrhythmias develop, amiodarone is preferable In patients with cardiac toxicity, avoiding the use of lidocaine and related class IB antidysrhythmic agents (eg, mexiletine, tocainide) is crucial because

, sulfasalazine) * * Antiarrhythmics (eg, amiodarone, tocainide) * * Anti-inflammatory medications (eg, gold, penicillamine) * * Illicit drugs (eg, crack cocaine, heroin) * * Sarcoidosis and other granulomatous diseases (eg, berylliosis) DPLDs related to other systemic illnesses include the following: * * Hepatitis C * * Inflammatory bowel disease

] * * Sulfasalazine [2, 10, 12, 24] AntiarrhythmicsAntiarrhythmics include the following: * * Amiodarone [26] * * Disopyramide [10, 12] * * Procainamide [1, 2, 6, 10, 12, 27] * * Propafenone [10, 12] * * Tocainide [2] * * Quinidine [1, 2, 10, 12, 27] AntibioticsAntibiotics include the following: * * Amoxicillin + clavulanic acid [2, 19, 25] * * Cefepime [28] * * Ciprofloxacin [2, 19