メピバカイン 化学特性,用途語,生産方法
使用
Local anesthetic.
一般的な説明
Mepivacaine hydrochloride is available in 1% to 3% solutionsand is indicated for infiltration anesthesia, dental procedures,peripheral nerve block, or epidural block. The onset of anesthesiais rapid, ranging from about 3 to 20 minutes for sensoryblock. Mepivacaine is rapidly metabolized in the liver with50% of the administered dose excreted into the bile asmetabolites. The metabolites are reabsorbed in the intestineand excreted in the kidney with only a small percentage foundin the feces. Less than 5% to 10% of the administered dose isfound unchanged in the urine. The primary metabolic productsare the N-demethylated metabolite and the 3 and 4 phenolicmetabolites excreted as their glucuronide conjugates.
臨床応用
Mepivacaine hydrochloride [N-(2, 6-dimethylphenyl)-1-methyl 2-piperidinecarboxamide
monohydrochloride] is an amino amide-type local anesthetic agent widely used to provide
regional analgesia and anesthesia by local infiltration, peripheral nerve block, and epidural and
caudal blocks. The pharmacological and toxicological profile of mepivacaine is quite similar to
that of lidocaine, except that mepivacaine has a slightly longer duration of action and lacks the
vasodilator activity of lidocaine. For this reason, it serves as an alternate choice for lidocaine
when addition of epinephrine is not recommended in patients with hypertensive vascular disease.
代謝
Mepivacaine undergoes extensive hepatic metabolism catalyzed by CYP1A2, with only a small
percentage of the administered dosage (<10%) being excreted unchanged in the urine. The major
metabolic biotransformations of mepivacaine are N-dealkylation (to give the N-demethylated
compound 2′,6′-pipecoloxylidide) and aromatic hydroxylations. These metabolites are excreted as
their corresponding glucuronides.
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