Propafenone Mexiletine

A2 Fluvoxamine Ciprofloxacin, mexiletine, propafenone, zileuton Acyclovir, cimetidine, famotidine, norfloxacin, verapamil... 

MEXILETINE PROPAFENONE t serum levels of mexiletine Propafenone inhibits CYP2D6-mediated metabolism of mexiletine no case reports of adverse clinical effects but is potential for proarrhythmias Monitor ECG closely... 

IMATINIB 1. ANTIARRHYTHMICS -flecainide, mexiletine, propafenone 2. ANTIDEPRESSANTS - fluoxetine, paroxetine, TCAs, trazodone, venlafaxine 3. ANTIPSYCHOTICS -clozapine, haloperidol, perphenazine, risperidone, thioridazine 4. BETA-BLOCKERS - metoprolol, propanolol, timolol 5. DONEPEZIL 6. METHAMPHETAMINE Imatinib may cause t plasma concentrations of these drugs, with a risk of toxic effects Inhibition of CYP2D6-mediated metabolism of these drugs Watch for early features of toxicity of these drugs... 

Hepatic metabolism plays a significant role in the elimination of each of the antiarrhythmics reviewed here. In fact, for propafenone, verapamil, and mexiletine, metabolism accounts for more than 90% of the elimination. Additionally, the biotransformations of mexiletine, propafenone, encainide, and flecainide cosegregate with polymorphic debrisoquine hydroxylation. 

Mexiletine is also metabolised by CYP2D6 (e.g. see Mexiletine + Propafenone , p.269). In an in vitro study using human liver microsomes, paroxetine, fluoxetine, and sertraline extensively inhibited the metabolism of mexiletine. Using a model to prediet in vivo interactions, it was suggested that both fluoxetine and paroxetine may interact with mexiletine to a clinically relevant extent, whereas sertraline is less likely to interact. ... 

In addition, the US manufacturer also recommends caution if tizanidine is given with other inhibitors of CYP1A2, of which they mention amio-darone, mexiletine, propafenone, cimetidine and ticlopidine. For a list of clinically important CYP1A2 inhibitors, see Table 1.2 , (p.4). 

Are there contraindications to concomitant drug use For instance, tizanidine is contraindicated in patients with concomitant use of CYP450 1A2 inhibitors such as fluvoxamine, amiodarone, mexiletine, propafenone, cimetidine, fluoroquinolones (ciprofloxacin, norfloxacin), rofecoxib, oral contraceptives, and ticlopidine [27]. 

Antiarrhythmics representative of these categories include Class lA— quinidine, procainamide, ajmaline, dis-opyramide, propafenone Class IB—lido-caine, mexiletine, tocainide, as well as phenytoin Qass 1C—flecainide. 

Drugs that may affect mexiletine include aluminum-magnesium hydroxide, atropine, narcotics, cimetidine, fluvoxamine, hydantoins, metoclopramide, propafenone, rifampin, urinary acidifiers, and urinary alkalinizers. 

Inhibitors codeine, encainide, flecainide, fluoxetine, haloperidol, hydrocodone, 4-methoxy-amphetamine, metoprolol, mexiletine, oxycodone, paroxetine, propafenone, propoxyphene, risperidone, selegiline (deprenyl), thioridazine, most tricyclic antidepressants, timolol Fluoxetine, haloperidol, paroxetine, quinidine... 

Mexiletine Procainamide Propafenone Quinidine Tocainide Sotalol... 

Other drugs imipramine mexiletine procainamide propafenone quinidine... 

ANAESTHETICS - LOCAL AMIODARONE, DISOPYRAMIDE, FLECAINIDE, MEXILETINE, PROCAINAMIDE, PROPAFENONE Risk of 1 BP Additive myocardial depression Particular care should be taken to avoid inadvertent intravenous administration during bupivacaine infiltration monitor PR, BP and ECG during epidural administration of bupivacaine... 

CIMETIDINE, RANITIDINE ANTIARRHYTHMICS-AMIODARONE, FLECAINIDE, MEXILETINE, PROCAINAMIDE, PROPAFENONE Likely t plasma concentrations of these antiarrhythmics and risk of adverse effects Cimetidine inhibits CYP2D6-mediated metabolism of flecainide, mexiletine, procainamide and propafenone. Ranitidine is a much weaker CYP2D6 inhibitor. Cimetidine is a potent inhibitor of organic cation transport in the kidney, and the elimination of procainamide is impaired Monitor PR and BP at least weekly until stable. Warn patients to report symptoms of hypotension (lightheadedness, dizziness on standing, etc.). Consider alternative acid suppression therapy... 

Labbe L, O Hara G, Lefebvre M, Lessard E, Gilbert M, Adedoyin A, Champagne J, Hamelin B, Turgeon J. Pharmacokinetic and pharmacodynamic interaction between mexiletine and propafenone in human beings. Clin Pharmacol Ther 2000 68(l) 44-57. 

Na+ Anticonvulsant drugs Class I antiarrhythmics Diuretic drugs Local anesthetic drugs Carbamazepine, phenytoin, valproic acid lA Disopyramide, procainamide, quinidine IB Lidocaine, mexiletine, phenytoin, tocainide IC Encainide, flecainide, propafenone Amiloride Bupivacaine, cocaine, lidocaine, mepivacaine, tetracaine... 

Extracted acetazolamide, amitriptyline, chlordiazepoxide, chlorpromazine, desipramine, dextromethorphan, diphenhydramine, doxepin, encainide, fentanyl, flecainide, fluoxetine, flurazepam, haloperidol, hydroxyethylflurazepam, ibuprofen, imipramine, lidocaine, ma-protiline, methadone, methaqualone, mexiletine, norchlorimipramine, nordoxepin, norfluoxetine, nordiazepam, nortriptyline, norverapamil, pentazocine, promazine, propafenone, propoxyphene, propranolol, protriptyline, quinidine, temazepam, trazodone, tri-mipramine, verapamil... 

Noninterfering mexiletine, captopril, dipyridamole, disopyramide, procainamide, propafenone, quinidine, sulfamethoxazole, trimethoprim, verapamil... 

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