The local anesthetic effect of memantine on infiltrative cutaneous analgesia in the rat

Yu Wen Chen, Chin Chen Chu, Yu Chung Chen, Jhi Joung Wang, Ching-Hsia Hung

Research output: Contribution to journalArticle

25 Citations (Scopus)

Abstract

Background: Memantine blocks N-methyl-D-aspartate receptors and the Na current, one principal mechanism of local anesthesia. Until now, no study mentioned that memantine had a local anesthetic effect, and therefore we investigated the local anesthetic effect of memantine. Methods: After blockade of cutaneous trunci muscle reflex with subcutaneous injections, we evaluated the cutaneous analgesic effect of memantine, lidocaine, and dizocilpine (MK-801) in rats. The dose-dependent response of memantine on cutaneous analgesia was compared with lidocaine and MK-801 in rats. The duration of action for each drug was evaluated and compared on an equipotent basis (20% effective dose [ED20], ED50, and ED80). Lidocaine, a frequently used local anesthetic, was used as control. Results: We demonstrated that memantine, lidocaine, and MK-801 produced dose-dependent local anesthetic effects as infiltrative cutaneous analgesia. The relative potency was MK-801 (10.4 [9.7-11.1]) > memantine (17.6 [15.2-20.4]) > lidocaine (25.9 [23.8-28.1 ]) (P < 0.01). On an equipotent basis, memantine showed longer duration than lidocaine (P = 0.012) and MK-801 (P = 0.008). Coadministration of memantine (13.3 μmol/kg) and MK-801 (1.3 μmol/kg) produced greater blockade and duration than memantine (13.3 μmol/kg) or MK-801 (1.3 μmol/kg) alone. Neither local injection of saline nor intraperitoneal administration of a large dose of memantine, lidocaine, or MK-801 produced cutaneous analgesia (data not shown). Conclusions: This study indicated that memantine is less potent than MK-801, and that memantine elicits longer analgesic duration than both lidocaine and MK-801. When combined with MK-801, memantine demonstrates a synergetic effect of cutaneous analgesia. We conclude that memantine produces better local analgesia than lidocaine and that N-methyl-D-aspartate receptors also contribute to the analgesic effect of memantine.

Original languageEnglish
Pages (from-to)191-195
Number of pages5
JournalAnesthesia and analgesia
Volume113
Issue number1
DOIs
Publication statusPublished - 2011 Jan 1

Fingerprint

Memantine
Local Anesthetics
Analgesia
Dizocilpine Maleate
Anesthetics
Skin
Lidocaine
Analgesics
N-Methyl-D-Aspartate Receptors

All Science Journal Classification (ASJC) codes

  • Anesthesiology and Pain Medicine

Cite this

Chen, Yu Wen ; Chu, Chin Chen ; Chen, Yu Chung ; Wang, Jhi Joung ; Hung, Ching-Hsia. / The local anesthetic effect of memantine on infiltrative cutaneous analgesia in the rat. In: Anesthesia and analgesia. 2011 ; Vol. 113, No. 1. pp. 191-195.
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abstract = "Background: Memantine blocks N-methyl-D-aspartate receptors and the Na current, one principal mechanism of local anesthesia. Until now, no study mentioned that memantine had a local anesthetic effect, and therefore we investigated the local anesthetic effect of memantine. Methods: After blockade of cutaneous trunci muscle reflex with subcutaneous injections, we evaluated the cutaneous analgesic effect of memantine, lidocaine, and dizocilpine (MK-801) in rats. The dose-dependent response of memantine on cutaneous analgesia was compared with lidocaine and MK-801 in rats. The duration of action for each drug was evaluated and compared on an equipotent basis (20{\%} effective dose [ED20], ED50, and ED80). Lidocaine, a frequently used local anesthetic, was used as control. Results: We demonstrated that memantine, lidocaine, and MK-801 produced dose-dependent local anesthetic effects as infiltrative cutaneous analgesia. The relative potency was MK-801 (10.4 [9.7-11.1]) > memantine (17.6 [15.2-20.4]) > lidocaine (25.9 [23.8-28.1 ]) (P < 0.01). On an equipotent basis, memantine showed longer duration than lidocaine (P = 0.012) and MK-801 (P = 0.008). Coadministration of memantine (13.3 μmol/kg) and MK-801 (1.3 μmol/kg) produced greater blockade and duration than memantine (13.3 μmol/kg) or MK-801 (1.3 μmol/kg) alone. Neither local injection of saline nor intraperitoneal administration of a large dose of memantine, lidocaine, or MK-801 produced cutaneous analgesia (data not shown). Conclusions: This study indicated that memantine is less potent than MK-801, and that memantine elicits longer analgesic duration than both lidocaine and MK-801. When combined with MK-801, memantine demonstrates a synergetic effect of cutaneous analgesia. We conclude that memantine produces better local analgesia than lidocaine and that N-methyl-D-aspartate receptors also contribute to the analgesic effect of memantine.",
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The local anesthetic effect of memantine on infiltrative cutaneous analgesia in the rat. / Chen, Yu Wen; Chu, Chin Chen; Chen, Yu Chung; Wang, Jhi Joung; Hung, Ching-Hsia.

In: Anesthesia and analgesia, Vol. 113, No. 1, 01.01.2011, p. 191-195.

Research output: Contribution to journalArticle

TY - JOUR

T1 - The local anesthetic effect of memantine on infiltrative cutaneous analgesia in the rat

AU - Chen, Yu Wen

AU - Chu, Chin Chen

AU - Chen, Yu Chung

AU - Wang, Jhi Joung

AU - Hung, Ching-Hsia

PY - 2011/1/1

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N2 - Background: Memantine blocks N-methyl-D-aspartate receptors and the Na current, one principal mechanism of local anesthesia. Until now, no study mentioned that memantine had a local anesthetic effect, and therefore we investigated the local anesthetic effect of memantine. Methods: After blockade of cutaneous trunci muscle reflex with subcutaneous injections, we evaluated the cutaneous analgesic effect of memantine, lidocaine, and dizocilpine (MK-801) in rats. The dose-dependent response of memantine on cutaneous analgesia was compared with lidocaine and MK-801 in rats. The duration of action for each drug was evaluated and compared on an equipotent basis (20% effective dose [ED20], ED50, and ED80). Lidocaine, a frequently used local anesthetic, was used as control. Results: We demonstrated that memantine, lidocaine, and MK-801 produced dose-dependent local anesthetic effects as infiltrative cutaneous analgesia. The relative potency was MK-801 (10.4 [9.7-11.1]) > memantine (17.6 [15.2-20.4]) > lidocaine (25.9 [23.8-28.1 ]) (P < 0.01). On an equipotent basis, memantine showed longer duration than lidocaine (P = 0.012) and MK-801 (P = 0.008). Coadministration of memantine (13.3 μmol/kg) and MK-801 (1.3 μmol/kg) produced greater blockade and duration than memantine (13.3 μmol/kg) or MK-801 (1.3 μmol/kg) alone. Neither local injection of saline nor intraperitoneal administration of a large dose of memantine, lidocaine, or MK-801 produced cutaneous analgesia (data not shown). Conclusions: This study indicated that memantine is less potent than MK-801, and that memantine elicits longer analgesic duration than both lidocaine and MK-801. When combined with MK-801, memantine demonstrates a synergetic effect of cutaneous analgesia. We conclude that memantine produces better local analgesia than lidocaine and that N-methyl-D-aspartate receptors also contribute to the analgesic effect of memantine.

AB - Background: Memantine blocks N-methyl-D-aspartate receptors and the Na current, one principal mechanism of local anesthesia. Until now, no study mentioned that memantine had a local anesthetic effect, and therefore we investigated the local anesthetic effect of memantine. Methods: After blockade of cutaneous trunci muscle reflex with subcutaneous injections, we evaluated the cutaneous analgesic effect of memantine, lidocaine, and dizocilpine (MK-801) in rats. The dose-dependent response of memantine on cutaneous analgesia was compared with lidocaine and MK-801 in rats. The duration of action for each drug was evaluated and compared on an equipotent basis (20% effective dose [ED20], ED50, and ED80). Lidocaine, a frequently used local anesthetic, was used as control. Results: We demonstrated that memantine, lidocaine, and MK-801 produced dose-dependent local anesthetic effects as infiltrative cutaneous analgesia. The relative potency was MK-801 (10.4 [9.7-11.1]) > memantine (17.6 [15.2-20.4]) > lidocaine (25.9 [23.8-28.1 ]) (P < 0.01). On an equipotent basis, memantine showed longer duration than lidocaine (P = 0.012) and MK-801 (P = 0.008). Coadministration of memantine (13.3 μmol/kg) and MK-801 (1.3 μmol/kg) produced greater blockade and duration than memantine (13.3 μmol/kg) or MK-801 (1.3 μmol/kg) alone. Neither local injection of saline nor intraperitoneal administration of a large dose of memantine, lidocaine, or MK-801 produced cutaneous analgesia (data not shown). Conclusions: This study indicated that memantine is less potent than MK-801, and that memantine elicits longer analgesic duration than both lidocaine and MK-801. When combined with MK-801, memantine demonstrates a synergetic effect of cutaneous analgesia. We conclude that memantine produces better local analgesia than lidocaine and that N-methyl-D-aspartate receptors also contribute to the analgesic effect of memantine.

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