백서에서 4가 암모늄 리도카인 유도체 QX-314의 급성 전신성 독성비교 (Comparative acute toxicity of quaternary ammonium lidocaine derivative QX-314 to lidocaine in mice)

서지정보

· 발행기관 : 대한마취통증의학회
· 수록지 정보 : Anesthesia and Pain Medicine / 4권 / 1호 / 5 ~ 10페이지
· 저자명 : 이상묵, 정규돈, 손윤숙, 유승준, 유건희, 이상훈, 조현숙

초록

Background: The current study examined the acute systemic
toxicity of QX-314 that there have been few research results for
this so far. In order to be useful as a drug, it must be shown to
have minimal toxicities. Hence, we compared the CNS and cardiac
toxicities of QX-314 to the conventional local anesthetic lidocaine.
Methods: Acute toxicity was evaluated by determining the
individual intravenous CD50 and LD50 of QX-314 and lidocaine.
There were four doses for each LD50 determination and 8 animals
per dose level. Animals were observed for several hours immediately
following drug administration and recorded overt effects and
fatalities. Both lidocaine and QX-314 were dissolved in saline.
Lidocaine and QX-314 were diluted to 1, 2, 4, 6 and 0.5, 1, 2, 4%,
respectively with saline and injected at the same volume to
minimized cardiovascular effect.
Results: The intravenous CD50 and LD50 were 12.7 and 14.1
mg/kg for QX-314 and 15.7 and 28.8 mg/kg for lidocaine. Electrocardiograms
showed intraventricular block (widened QRS complex)
at high doses of lidocaine compared to AV block (loss of QRS
complex) at high concentrations of QX-314. There are no evidence
that CNS toxicity led mouse to death.
Conclusions: QX-314 is about 1.5 times as toxic as lidocaine.
Although QX-314 may still be useful clinically as a long-lasting local
anesthetic, its safety relative to other available local anesthetics
must be considered.

영어초록

Background: The current study examined the acute systemic
toxicity of QX-314 that there have been few research results for
this so far. In order to be useful as a drug, it must be shown to
have minimal toxicities. Hence, we compared the CNS and cardiac
toxicities of QX-314 to the conventional local anesthetic lidocaine.
Methods: Acute toxicity was evaluated by determining the
individual intravenous CD50 and LD50 of QX-314 and lidocaine.
There were four doses for each LD50 determination and 8 animals
per dose level. Animals were observed for several hours immediately
following drug administration and recorded overt effects and
fatalities. Both lidocaine and QX-314 were dissolved in saline.
Lidocaine and QX-314 were diluted to 1, 2, 4, 6 and 0.5, 1, 2, 4%,
respectively with saline and injected at the same volume to
minimized cardiovascular effect.
Results: The intravenous CD50 and LD50 were 12.7 and 14.1
mg/kg for QX-314 and 15.7 and 28.8 mg/kg for lidocaine. Electrocardiograms
showed intraventricular block (widened QRS complex)
at high doses of lidocaine compared to AV block (loss of QRS
complex) at high concentrations of QX-314. There are no evidence
that CNS toxicity led mouse to death.
Conclusions: QX-314 is about 1.5 times as toxic as lidocaine.
Although QX-314 may still be useful clinically as a long-lasting local
anesthetic, its safety relative to other available local anesthetics
must be considered.

참고자료

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