普洛卡因在 37 °C (43.8 mM) 下对转化成纤维细胞 (LM 细胞) 质膜 Na,K-ATP 酶的抑制作用比在 25 °C (28.2 mM) 下的作用更大 [2]。

Absorption, Distribution and Excretion
Prilocaine is metabolized in both the liver and the kidney and excreted via the kidney.
/CONCERNING/ HYDROLYSIS OF AMIDE BOND OF PRILOCAINE... PLASMA CONCN OF R-(-)-ENANTIOMER WERE FOUND TO BE LOWER THAN THOSE OF THE S-(+)-ENANTIOMER AFTER IV ADMIN TO CAT. IN VITRO STUDIES USING LIVER PREPN FROM VARIOUS MAMMALS CONFIRMED THE R-(-)-ISOMER TO BE HYDROLYZED @ MUCH HIGHER RATES THAN THE S-(+) FORM...
THERE IS...MORE RAPID PRODN OF METHEMOGLOBINEMIA BY D-(-) FORM, CAUSED PRESUMABLY BY HIGHER BLOOD LEVELS OF HYDROLYSIS PRODUCT, O-TOLUIDINE.
PRILOCAINE FETAL/MATERNAL CONCN RATIO: 1.0 /FROM TABLE/
PRILOCAINE DOSE 0.2 G IV GAVE BLOOD CONCN 0.26 MG% @ 0.3 HR & 0.14 MG% @ 0.17 HR; DOSE 0.4 G IV GAVE BLOOD CONCN 0.15 MG% @ 0.12 HR & 0.08 MG% @ 0.33 HR; DOSE 0.4 G EPIDURAL BLOCK GAVE BLOOD CONCN 0.26 MG% @ 0.25 HR (PEAK); DOSE 0.4 G INTERCOSTAL BLOCK GAVE BLOOD CONCN 0.40 MG% @ 0.25 HR. /FROM TABLE/

---

Metabolism / Metabolites
The amide-linked local anesthetics are, in general, degraded by the hepatic endoplasmic reticulum, the initial reactions involving N-dealkylation and subsequent hydrolysis. However, with prilocaine, the initial step is hydrolytic, forming o-toluidine metabolites that can cause methemoglobinemia.
BIOTRANSFORMATION OF PRILOCAINE...IN RATS GAVE O-TOLUIDINE & N-PROPYLALANINE.

---

Biological Half-Life
MEPIVACAINE-HCL (I-HCL) & PRILOCAINE-HCL (II-HCL) WERE INFUSED IV 250 MG INTO HEALTHY VOLUNTEERS. T/2 FOR I WAS GENERALLY LONGER THAN II; TOTAL BODY CLEARANCE II CONSISTENTLY GREATER THAN I. II CLEARANCE EXCEEDED NORMAL HEPATIC BLOOD FLOW: EXTRA-HEPATIC METAB SITE IS POSTULATED.

Interactions
...MOUSE TRIALS INDICATE INCR TOXICITY WHEN COMBINED WITH TETRACAINE.
...PRILOCAINE...REPORTED TO INTERACT WITH SUCCINYLCHOLINE /RESULTING IN INCR IN INTENSITY & DURATION OF SUCCINYLCHOLINE-INDUCED NEUROMUSCULAR BLOCKADE & RESP DEPRESSION; OTHER DEPOLARIZING MUSCLE RELAXANTS (EG DECAMETHONIUM) & NONDEPOLARIZING MUSCLE RELAXANTS (EG GALLAMINE TRIETHIODIDE & PANCURONIUM) MAY BEHAVE SIMILARLY/.
.../PRILOCAINE/ PRODUCED A SLIGHT INCR IN INTENSITY OF NEUROMUSCULAR BLOCKADE /OF ALCURONIUM CHLORIDE/. ...MARKED DECR IN TIDAL VOL, INDICATING RESP DEPRESSION, WAS OBSERVED...
EPINEPHRINE PROLONGS THE EFFECT /OF PRILOCAINE/. /PRILOCAINE HCL/
For more Interactions (Complete) data for PRILOCAINE (15 total), please visit the HSDB record page.

[1]. Neurotoxic effects of local anesthetics on the mouse neuroblastoma NB2a cell line. Biotech Histochem. 2015 Apr;90(3):216-22.

[2]. Effects of local anaesthetics on the activity of the Na,K-ATPase of canine renal medulla. Pharmacol Res. 2000 Jan;41(1):1-7.

Prilocaine is an amino acid amide in which N-propyl-DL-alanine and 2-methylaniline have combined to form the amide bond; used as a local anaesthetic. It has a role as a local anaesthetic and an anticonvulsant. It is an amino acid amide and a monocarboxylic acid amide.
A local anesthetic that is similar pharmacologically to lidocaine. Currently, it is used most often for infiltration anesthesia in dentistry. (From AMA Drug Evaluations Annual, 1992, p165)
Prilocaine is an Amide Local Anesthetic. The physiologic effect of prilocaine is by means of Local Anesthesia.
Prilocaine is a toluidine derivative and intermediate-acting amino amide with local anesthetic property. Prilocaine stabilizes the neuronal membrane by preferential binding to and inhibiting depolarization of the voltage-gated sodium channel. This results in a decrease in membrane permeability and subsequent inhibition of the ionic sodium influx required for the initiation and conduction of impulses.
A local anesthetic that is similar pharmacologically to LIDOCAINE. Currently, it is used most often for infiltration anesthesia in dentistry.
See also: Prilocaine Hydrochloride (has salt form) ... View More ...

---

Drug Indication
Used as a local anaesthetic and is often used in dentistry.

---

Mechanism of Action
Prilocaine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.
... BLOCK CONDUCTION IN NERVE PERHAPS BY COMPETING WITH CA @ SOME SITE THAT CONTROLS PERMEABILITY OF MEMBRANE ... CA IS ALSO INVOLVED IN ACTION OF LOCAL ANESTHETICS ON SMOOTH MUSCLE ... & ON ADRENAL MEDULLA ... /LOCAL ANESTHETICS/
... PREVENT THE GENERATION & THE CONDUCTION OF THE NERVE IMPULSE. THEIR PRIMARY SITE OF ACTION IS THE CELL MEMBRANE. ... BLOCK CONDUCTION BY DECREASING OR PREVENTING THE LARGE TRANSIENT INCREASE IN THE PERMEABILITY OF EXCITABLE MEMBRANES TO NA+ THAT NORMALLY IS PRODUCED BY A SLIGHT DEPOLARIZATION OF THE MEMBRANE. /LOCAL ANESTHETICS/
AS ANESTHETIC ACTION PROGRESSIVELY DEVELOPS IN A NERVE, THRESHOLD FOR ELECTRICAL EXCITABILITY INCR & SAFETY FACTOR FOR CONDUCTION DECR; WHEN THIS ACTION IS SUFFICIENTLY WELL-DEVELOPED, BLOCK OF CONDUCTION IS PRODUCED. /LOCAL ANESTHETICS/
.../2 POSSIBILITIES:/ ACHIEVE BLOCK BY INCR SURFACE PRESSURE OF LIPID LAYER THAT CONSTITUTES NERVE MEMBRANE...CLOSING PORES THROUGH WHICH IONS MOVE. ... /OR:/ AFFECT PERMEABILITY BY INCR DEGREE OF DISORDER OF MEMBRANE. /LOCAL ANESTHETICS/

---

Therapeutic Uses
Anesthetics, Local
AN AGENT CHEMICALLY SIMILAR TO LIDOCAINE & MEPIVACAINE USED FOR LOCAL & REGIONAL-BLOCK ANESTHESIA. IN ONSET OF ACTION & EFFECTIVENESS 1-3% SOLN... EQUIVALENT TO LIDOCAINE & MEPIVACAINE IN 1%-2% CONCN. ITS DURATION OF ACTION IS INTERMEDIATE TO SHORTER-ACTING LIDOCAINE & LONGER-ACTING MEPIVACAINE. /PRILOCAINE HCL/
PRILOCAINE HYDROCHLORIDE ... HAS BEEN EMPLOYED ... FOR SPINAL ANESTHESIA. /PRILOCAINE HCL/
... ACT ON ANY PART OF THE NERVOUS SYSTEM & ON EVERY TYPE OF NERVE FIBER. /LOCAL ANESTHETICS/
For more Therapeutic Uses (Complete) data for PRILOCAINE (10 total), please visit the HSDB record page.

---

Drug Warnings
AS WITH OTHER LOCAL ANESTHETICS, PRILOCAINE HCL IS CONTRAINDICATED IN PRESENCE OF SHOCK, SEVERE CARDIOVASCULAR DISEASE, OR HEART BLOCK. /PRILOCAINE HCL/
... SHOULD NOT BE ADMIN TO PT WITH IDIOPATHIC OR CONGENITAL METHEMOGLOBINEMIA, ANEMIA, OR CARDIAC OR VENTILATORY FAILURE WITH HYPOXIA; IT SHOULD BE USED WITH CAUTION FOR CONTINUOUS EPIDURAL ANESTHESIA SINCE THE METHEMOGLOBINEMIC EFFECT OF INDIVIDUAL DOSES IS ADDITIVE. /PRILOCAINE HCL/
IN PRESENCE OF HEMORRHAGE, SYMPATHETIC BLOCK PRODUCED BY EPIDURAL ANESTHESIA BECOMES EXTREMELY SIGNIFICANT & MAY RESULT IN RAPID & DELETERIOUS CIRCULATORY CHANGES. /LOCAL ANESTHETICS/
TWO OUTSTANDING DANGERS /OF CAUDAL ANESTHESIA/ ARE (1) INTRODUCING NEEDLE INTO VENOUS PLEXUS LINING SACRAL CANAL, WITH RESULTANT INTRAVASCULAR INJECTION OF DRUG, & (2) PENETRATING DURA, WITH DEVELOPMENT OF HIGH LEVEL OF SPINAL ANESTHESIA. /LOCAL ANESTHETICS/
For more Drug Warnings (Complete) data for PRILOCAINE (16 total), please visit the HSDB record page.

---

Pharmacodynamics
Prilocaine binds to the intracellular surface of sodium channels which blocks the subsequent influx of sodium into the cell. Action potential propagation and never function is, therefore, prevented. This block is reversible and when the drug diffuses away from the cell, sodium channel function is restored and nerve propagation returns.

C13H20N2O

220.32

220.157

721-50-6

Prilocaine hydrochloride;1786-81-8;Prilocaine acetate

4906

White to off-white solid powder

1.0±0.1 g/cm3

361.6±25.0 °C at 760 mmHg

37-38ºC

134.3±23.3 °C

0.0±0.8 mmHg at 25°C

1.543

1.74

41.13

2

2

5

16

218

0

MVFGUOIZUNYYSO-UHFFFAOYSA-N

InChI=1S/C13H20N2O/c1-4-9-14-11(3)13(16)15-12-8-6-5-7-10(12)2/h5-8,11,14H,4,9H2,1-3H3,(H,15,16)

N-(2-methylphenyl)-2-(propylamino)propanamide

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 : ~100 mg/mL (~453.91 mM)
H2O : ~2.5 mg/mL (~11.35 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (11.35 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

---

配方 2 中的溶解度: ≥ 2.5 mg/mL (11.35 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

---

View More

配方 3 中的溶解度: ≥ 2.5 mg/mL (11.35 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

---

配方 4 中的溶解度: 50 mg/mL (226.95 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

---

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。