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CAS NO.73-78-9
USP(1-5)Metric TonUSP(5-10)Metric Ton
| Molecular Formula | C14H23ClN2O |
| Molar Mass | 270.8 |
| Melting Point | 80-82°C |
| Boling Point | 350.8°C at 760 mmHg |
| Flash Point | 166°C |
| Vapor Presure | 4.28E-05mmHg at 25°C |
| Storage Condition | Inert atmosphere,2-8°C |
| Physical and Chemical Properties | White Crystal, odorless, slightly bitter and Hemp taste. Very soluble in water, ethanol and organic solvents, but insoluble in ether. Aqueous solution in the case of acid, alkali does not decompose, repeated high-pressure sterilization rarely deterioration. |
| Use | Local anesthetics, antiarrhythmic drugs, for a variety of anesthesia and rapid ventricular arrhythmias |
| lidocaine hydrochloride was used as local anesthetic and antiarrhythmic drug. Clinically, it is mainly used for infiltration anesthesia, epidural anesthesia, surface anesthesia (including mucosal anesthesia during thoracoscopy or abdominal surgery) and nerve conduction block. It can also be used for ventricular premature beats and ventricular tachycardia after acute myocardial infarction. It can also be used for Digitalis poisoning, cardiac surgery and ventricular arrhythmia caused by cardiac catheterization. But it is usually not effective for supraventricular arrhythmias. lidocaine hydrochloride is an amide local anesthetic. After blood absorption or intravenous administration, the central nervous system has obvious excitation and inhibition of biphasic effect, and can be no precursor of excitation, low blood concentration, analgesia and drowsiness, the pain threshold increases; With the increase of dose, the effect or toxicity increases, and the blood concentration of the sub-toxic drug has anticonvulsant effect; When the blood concentration exceeds 5 μg · ml-1, convulsions can occur. Lidocaine hydrochloride in low dose, can promote the outflow of K in myocardial cells, reduce myocardial automaticity, and has the effect of anti ventricular arrhythmia; In the treatment of dose, the electrical activity of myocardial cells, atrioventricular conduction and myocardial contraction had no significant effect; Further increase in blood concentration, can cause heart conduction velocity slowed, atrioventricular block, inhibit myocardial contractility and cardiac output decreased. |
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| function and use | lidocaine hydrochloride has the characteristics of strong penetration, strong diffusion, fast onset, 2 times of anesthetic efficacy and procaine, and the toxicity was 1. The anesthetic effect can appear 5 minutes after administration, and the anesthetic effect can last for 1~1.5 hours, which is 50% longer than procaine. After absorption can inhibit the central nervous system, and can inhibit ventricular automaticity, shorten the refractory period, can be used to control ventricular tachycardia, ventricular premature beats, ventricular tachycardia and ventricular fibrillation and other arrhythmia symptoms. It is effective for cardiac disorders or cardiac arrhythmias caused by cardiac glycosides, but not for supraventricular tachycardia. This product is fast, short duration, oral invalid, often as intravenous administration. |
| indication | lidocaine hydrochloride is an intermediate amide local anesthetic. It is used as local anesthetic and antiarrhythmic drug. Mainly used for: (1) infiltration anesthesia, epidural anesthesia, surface anesthesia (including in thoracoscopy or abdominal surgery for mucosal anesthesia) and nerve conduction block. (2) to treat ventricular premature beat and ventricular tachycardia after acute myocardial infarction (AMI), and ventricular arrhythmia caused by digitalis poisoning, cardiac surgery and cardiac catheterization, but it is usually not effective for supraventricular arrhythmias. |
| usage and dosage | topical anesthesia with 2%~ 5% solution. Infiltration anesthesia with 0.25% ~ 0.5% solution. Conduction anesthesia with 2% hydrochloric acid solution, each injection point, horses, cattle 8~12 ml, sheep 3~4 ml. Epidural anesthesia 2% solution, horses, cattle 8~12 ml, dogs, cats, 0.22 per kilogram of body weight. Subcutaneous injection of 2% solution, the maximum amount, pigs, sheep 80 ml, horses, cattle 400 ml, dogs 25 ml, cats 8.5 ml. treatment of arrhythmia, intravenous injection: the initial dose of 2~4 mg per kilogram of body weight in dogs, followed by intravenous infusion of 25~75 micrograms per minute, the initial dose of 250~500 micrograms in cats, this was followed by an intravenous infusion of 20 micrograms per minute. |
| adverse reactions | the incidence of adverse reactions of lidocaine hydrochloride was about 6.3%. Most adverse reactions are dose-related. Adverse reactions are drowsiness, dizziness, dizziness, Nausea, Vomit, burnout, euphoria, confusion, muscle twitching, convulsions, blurred vision, confusion and Dyspnea, high dose can produce severe sinus bradycardia, cardiac arrest, severe atrioventricular block and decreased myocardial contractility, decreased blood pressure, etc. High concentration of lidocaine hydrochloride in blood can cause slow atrial conduction velocity, atrioventricular block (A-V-B), inhibition of myocardial contractility and decrease of cardiac output. A small number of allergic reactions such as erythema rash and vascular nerve edema. |
| drug interaction | (1) cimetidine and β-blockers can inhibit the hepatic metabolism of lidocaine, to increase its blood concentration, adverse reactions can occur in the heart and nervous system, should adjust the dose of lidocaine hydrochloride. (2) barbiturates can promote the metabolism of lidocaine hydrochloride, and the combination of the two drugs can cause bradycardia and sinus arrest. (3) combined with procainamide, can produce a transient delirium and hallucinations, but does not affect the blood concentration of the product. (4) isoproterenol can increase the total clearance rate of this product due to increased hepatic blood flow; Norepinephrine can decrease the total clearance rate of lidocaine hydrochloride due to reduced hepatic blood flow. (5) with the following drugs are incompatible: phenobarbital, thiopental sodium, sodium nitroprusside, mannitol, amphotericin B, ampicillin, sulfadiazine. |
| note | (1) those allergic to other local anesthetics may also be allergic to lidocaine hydrochloride. (2) the following conditions should be used with caution: Pregnancy, newborns, especially premature infants, decreased hepatic blood flow, liver and kidney dysfunction, congestive heart failure, severe myocardial damage, hypovolemia and Shock. (3) strictly control the concentration and the total amount of medication, excessive can cause convulsions and cardiac arrest; The metabolism in the body is slower than procaine, there is accumulation, can cause poisoning and convulsions. (4) the dosage should be adjusted according to the needs and tolerance of the elderly, and the dose should be halved in patients over 70 years old. (5) during anesthesia, it is necessary to prevent the blood vessel and local anesthetic poisoning. (6) the treatment of arrhythmia should pay attention to monitoring blood pressure, ECG, and with rescue equipment; Electrocardiogram P-R interval prolongation or QRS wave broadening, patients with other arrhythmias or previous arrhythmias should be discontinued immediately. (7) during anesthesia, the P-R interval of ECG was prolonged or the QRS wave was widened, and the patients with other arrhythmia or the original arrhythmia should be discontinued immediately. |
| Use | Local anesthetics, antiarrhythmic drugs, for all kinds of anesthesia and rapid ventricular arrhythmia |
CAS:
73-78-9
MF:
C14H23ClN2O
MW:
270.8
EINECS:
200-803-8
MDL No.:
MFCD00034865
Melting point:
80-82°C
storage temp.
Inert atmosphere,2-8°C
Water Solubility
Water : ≥ 36 mg/mL (132.94 mM)
InChI
InChI=1S/C14H22N2O.ClH/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4;/h7-9H,5-6,10H2,1-4H3,(H,15,17);1H
InChIKey
IYBQHJMYDGVZRY-UHFFFAOYSA-N
SMILES
C(NC1=C(C)C=CC=C1C)(=O)CN(CC)CC.[H]Cl
LogP
2.359 (est)