Tocainide

Therapeutic Function Antiarrhythmic Chemical Name 2-Amino-2, 6 -propionoxylidide Common Name — 

Chemical Abstracts Registry No. 41708-72-0 Trade Name Manufacturer 

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Tocainide. Tocainide is a po active primary amine analogue of lidocaine. It consists of the (3)-(—) and the more active (R)-(+) enantiomers. 

Tocainide is rapidly and well absorbed from the GI tract and undergoes very fitde hepatic first-pass metabolism. Unlike lidocaine which is - 30% bioavailable, tocainide s availability approaches 100% of the administered dose. Eood delays absorption and decreases plasma levels but does not affect bio availability. Less than 10% of the dmg is bound to plasma proteins. Therapeutic plasma concentrations are 3—9 jig/mL. Toxic plasma levels are >10 fig/mL. Peak plasma concentrations are achieved in 0.5—2 h. About 30—40% of tocainide is metabolized in the fiver by deamination and glucuronidation to inactive metabolites. The metabolism is stereoselective and the steady-state plasma concentration of the (3)-(—) enantiomer is about four times that of the (R)-(+) enantiomer. About 50% of the tocainide dose is efirninated by the kidneys unchanged, and the rest is efirninated as metabolites. The elimination half-life of tocainide is about 15 h, and is prolonged in patients with renal disease (1,2,23). 

Some rare toxic effects that may result from tocainide therapy are a lupus-fike syndrome, skin rash, pulmonary complications, and hematologic abnormalities, eg, agranulocytosis (1,2,24). 

Many local anesthetics have a selective depressant action on heart muscle when given system cally. This is useful in t.reatment of cardiac arrhythmias, and a 1 idocaine-1 ike drug with this kind of action is tocainide (2). ... 

Quingestanol acetate Stanzolol Tegafur Tiopronin Tocainide Vindesine Xipamid 2oxazo lamina Ammonium acetate Cyclopentamine HCl Ammonium carbonate Aminosalicylic acid Phenytoin... 

I b With shortening of action potential Lidocaine, Mexiletine, Tocainide, Phenytoin, Aprindine... 

ADM INI STERI NG TOCAIN IDE AN D M EXILETIN E Tocainide and mexiletine are administered at 8-hour intervals and with food (or an antacid) to prevent gastrointestinal upset. In addition, administering tocainide with food may offer some protection gainst toxicity because the absoq> tion rate is slowed in the presence of food. 

These drug s are contraindicated in those with a known hypersensitivity to any component of the preparation. The topical anesthetics are used cautiously in patients receiving Class I antiarrhytiimic drug s such as tocainide and mexiletine because the toxic effects are additive and potentially synergistic. 

C7H4Br20 563-76-8) see Prilocaine Propyramazine bromide Tiopronin Tocainide... 

C)jHi)N 87-62-7) see Bupivacaine Etidocaine LicIocaine Lidoflazine Mepivacaine Pilsicainide Pyrrocaine Ropivacaine hydrochloride Tocainide Xipamide... 

Tobi 65 Tobradex 82 Tobramycin 65, 82 Tobrex 65 Tocainide 65 Tofianil 41 Tolcapone 65 ToleSn 65 Tolmetin 65 Tonocard 65 Topamax 66 Topiramate 66 Toprol XL 48 Toradd 43 Tornalate 18 Torsemide 66... 

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. 

Tirofiban Tizanidine Tobramycin Tocainide Tolbutamide Tolcapone Tolmetin Tolnaftate Tolonium chloride Tolterodine tartrate Topiramate Tramadol Trandolapril Tranexamic acid Tranylcypromine... 

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