トカイニド 化学特性,用途語,生産方法
効能
抗不整脈薬, ナトリウムチャネル遮断薬
使用
Tocainide is used for suppressing symptoms of ventricular arrhythmia and tachycardia,
and for premature cardiac contractions.
定義
ChEBI: A monocarboxylic acid amide in which 2,6-dimethylphenylaniline and isobutyric acid have combined to form the amide bond; used as a local anaesthetic.
世界保健機関（WHO）
Tocainide, an antidysrhythmic agent, was introduced in 1981 for
the treatment of ventricular dysrhythmias. By 1984 its use was associated with
cases of agranulocytosis, aplastic anaemia and thrombocytopenia, some of which
were fatal. This led some regulatory authorities to restrict the indications for its
use. The major manufacturer has subsequently restricted its use on a worldwide
basis to the treatment of symptomatic ventricular dysrhythmias not responding to
other therapy, or when other therapy is contraindicated.
薬物動態学
The α-methyl group is believed to slow the rate of metabolism and, thereby, to
contribute to oral activity. The plasma half-life of tocainide is approximately 12 hours, and nearly
50% of the drug may be excreted unchanged in the urine. Adverse effects associated with tocainide
are like those observed with lidocaine—specifically, gastrointestinal disturbances and central
nervous system effects.
臨床応用
Tocainide (Tonocard) is an orally effective antiarrhythmic
agent with close structural similarities to lidocaine. Tocainide is indicated for the treatment of symptomatic
ventricular arrhythmias refractory to more conventional
therapy. Serious noncardiac adverse effects limit its use
to patients with life-threatening arrhythmias.
副作用
Light-headedness, dizziness, or nausea occurs in approximately
15% of patients, paresthesias and numbness
in 9%, and tremor in 8%.These adverse effects are
generally mild in intensity, transient, and dose related.
Overall, however, approximately 20% of patients prescribed
tocainide discontinue therapy because of such
effects. Serious immune-based side effects, such as pulmonary
fibrosis, have been reported, and blood
dyscrasias, such as agranulocytosis and thrombocytopenia,
may occur in up to 0.2% of patients.
薬物相互作用
When used with other class IB antiarrhythmic drugs, tocainide
toxicity may be increased without significant
gain in antiarrhythmic efficacy.
予防処置
Patients who are hypersensitive to tocainide or to local
anesthetics of the amide type should not be exposed to
tocainide.The presence of second- or third-degree heart
block in the absence of an artificial pacemaker also contraindicates
the use of tocainide.
トカイニド 上流と下流の製品情報
原材料
準備製品