甲哌卡因通过与神经元细胞膜中特定的电压门控钠离子通道结合来抑制钠流入和膜去极化。这会导致神经冲动的启动和传导出现障碍，从而导致暂时的感觉丧失。与其他局部麻醉剂相比，该药物起效更快且持续时间适中[2]。甲哌卡因的作用时间中等，比普鲁卡因短，并且起效相当快（比普鲁卡因快）[3]。 S(-)-布比卡因对 TTX Na(+) 通道具有选择性，而甲哌卡因则对 Na(v)1.8 表现出优先使用依赖性阻断[4]。

Absorption, Distribution and Excretion
Local absorption: The systemic absorption rate of local anesthetics depends on the total dose and concentration administered, the route of administration, the vascular distribution at the site of administration, and the presence of adrenaline in the anesthetic solution. It is rapidly metabolized; only a small portion (5% to 10%) of the anesthetic is excreted unchanged in the urine. The liver is the primary site of metabolism, with over 50% of the administered dose excreted as metabolites in the bile. Metabolism/Metabolites It is rapidly metabolized; only a small portion (5% to 10%) of the anesthetic is excreted unchanged in the urine. The liver is the primary site of metabolism, with over 50% of the administered dose excreted as metabolites in the bile. It is rapidly metabolized; only a small portion (5% to 10%) of the anesthetic is excreted unchanged in the urine. The liver is the primary site of metabolism, with over 50% of the administered dose excreted as metabolites in the bile. Elimination route: It is rapidly metabolized; only a small portion (5% to 10%) of the anesthetic is excreted unchanged in the urine. The liver is the primary site of metabolism, with over 50% of the administered dose excreted as metabolites via bile. Half-life: The half-life of mepivacaine in adults is 1.9 to 3.2 hours, and in newborns it is 8.7 to 9 hours.

Toxicity Summary
Local anesthetics work by blocking the generation and conduction of nerve impulses. The mechanism may involve increasing the electrical excitation threshold of nerves, slowing the propagation speed of nerve impulses, and reducing the rate of rise of action potentials. Generally, the progression of anesthesia is related to the diameter, degree of myelination, and conduction velocity of the affected nerve fibers. Clinically, the order of loss of nerve function is as follows: pain sensation, temperature sensation, touch sensation, proprioception, and skeletal muscle tone. Pregnancy and Lactation Effects ◉ Overview of Use During Lactation There is currently no information regarding the use of mepivacaine during lactation. Given the low secretion of other local anesthetics in breast milk, a single use of mepivacaine during lactation is unlikely to have adverse effects on breastfed infants. However, especially in breastfeeding newborns or premature infants, other medications may be preferred. It has been reported that the use of mepivacaine as a local anesthetic during delivery may affect initial breastfeeding behavior in some infants, but it does not affect weight gain in the first 5 days postpartum. Although research on mepivacaine is limited, it appears that with good breastfeeding support, epidural anesthesia, whether or not combined with fentanyl or its derivatives, has little or no adverse effect on breastfeeding success. Labor analgesia may delay the onset of lactation. More research is needed to clarify the impact of mepivacaine use during labor on breastfeeding outcomes.
◉ Effects on breastfed infants
As of the revision date, no relevant published information was found.
◉ Effects on lactation and breast milk
A study comparing the effects of epidural analgesia with mepivacaine, bupivacaine, and lidocaine during normal labor found no difference in weight change among the three groups of breastfed infants in the first 5 days postpartum. Overall weight gain was within the normal range in all groups.
Of the six infants who received mepivacaine pudendal nerve block within one hour of delivery, four started breastfeeding later and had fewer initial milk volumes than 10 infants who did not receive anesthesia during labor. The long-term consequences of these differences have not been reported. A nationwide survey of women and their infants from late pregnancy to 12 months postpartum compared the duration of lactation stage II in mothers who received and did not receive analgesics during labor. Drug classes included: spinal or epidural anesthesia alone, spinal or epidural anesthesia in combination with other drugs, and other analgesics alone. Women receiving any class of drugs had approximately twice the risk of delayed lactation stage II (>72 hours) compared to women who did not receive labor analgesia. Protein Binding: Mepivacaine binds to plasma proteins at approximately 75%. Generally, the lower the plasma concentration of the drug, the higher the binding rate to plasma. Toxicity Data: In rhesus monkeys, the mean epileptogenic dose of mepivacaine was 18.8 mg/kg, and the mean arterial plasma concentration was 24.4 μg/mL. LD50: 23-35 mg/kg (intravenous injection, mice) (A308) LD50: 280 mg/kg (subcutaneous injection, mice) (A308)

[1]. ECMO for Cardiac Rescue after Accidental Intravenous Mepivacaine Application. Case Rep Pediatr. 2012;2012:491692.

[2]. mepivacaine hydrochloride.

[3]. Pharmacokinetics of the enantiomers of mepivacaine after intravenous administration of the racemate in volunteers. Anesth Analg, 1997. 84(1): p. 85-9.

[4]. Leffler, A., J. Reckzeh, and C. Nau, Block of sensory neuronal Na+ channels by the secreolytic ambroxol is associated with an interaction with local anesthetic binding sites. Eur J Pharmacol, 2010. 630(1-3): p. 19-28.

Mepivacaine is a piperidine carboxamide compound composed of an amide bond formed by the combination of N-methylpiperidinic acid and 2,6-dimethylaniline. It is a local amide anesthetic. Mepivacaine is both a local anesthetic and a drug allergen. It is a local anesthetic with a chemical structure related to bupivacaine but pharmacologically related to lidocaine. It is suitable for infiltration anesthesia, nerve blocks, and epidural anesthesia. Mepivacaine is only effective when used locally in large doses and therefore should not be used via this route. (Excerpt from JAMA Drug Evaluation, 1994, p. 168) Mepivacaine is an amide local anesthetic. The physiological action of mepivacaine is achieved through local anesthesia. Mepivacaine is an amide local anesthetic. At the injection site, mepivacaine binds to specific voltage-gated sodium ion channels on the neuronal cell membrane, inhibiting sodium ion influx and membrane depolarization. This leads to the blockage of nerve impulse initiation and conduction, resulting in reversible sensory loss. Compared to other local anesthetics, this drug has a faster onset of action and a moderate duration of action. Mepivacaine is a local anesthetic with a chemical structure related to bupivacaine but a pharmacological action related to lidocaine. It is suitable for infiltration anesthesia, nerve blocks, and epidural anesthesia. Mepivacaine is only effective when applied topically in large doses and should therefore not be used via this route. (From JAMA Drug Evaluation, 1994, p. 168) See also: Mepivacaine hydrochloride (salt form). Drug Indications This drug is used to produce local or regional analgesia and anesthesia through local infiltration, peripheral nerve block techniques, and central nervous system techniques including epidural and caudal blocks. FDA Label Mechanism of Action Local anesthetics work by blocking the generation and conduction of nerve impulses. The mechanism may involve increasing the electrical excitation threshold of the nerve, slowing the propagation of nerve impulses, and reducing the rate of rise of action potentials. Typically, the progression of anesthesia is related to the diameter, degree of myelination, and conduction velocity of the affected nerve fibers. Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone. Pharmacodynamics Mepivacaine is an amide-type local anesthetic. Mepivacaine has a rapid onset of action and a moderate duration of action; its brand names are carbocaine and polocaine. Mepivacaine is used for local infiltration and regional anesthesia. Systemic absorption of local anesthetics can affect the cardiovascular and central nervous systems. The blood concentrations achieved at normal therapeutic doses have minimal impact on cardiac conduction, excitability, refractory period, contractility, and peripheral vascular resistance.

C15H22N2O

246.35

246.173

96-88-8

(+)-Mepivacaine;24358-84-7;Mepivacaine hydrochloride;1722-62-9;Mepivacaine-d3;1346597-90-7

4062

White to off-white solid powder

1.077 g/cm3

383.062ºC at 760 mmHg

150.5ºC

185.47ºC

2.737

32.34

1

2

2

18

282

0

INWLQCZOYSRPNW-UHFFFAOYSA-N

InChI=1S/C15H22N2O/c1-11-7-6-8-12(2)14(11)16-15(18)13-9-4-5-10-17(13)3/h6-8,13H,4-5,9-10H2,1-3H3,(H,16,18)

N-(2,6-dimethylphenyl)-1-methylpiperidine-2-carboxamide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 33.33 mg/mL (135.30 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。