The chemical name of lidocaine is n-diethylaminoacetyl-2,6-xylidine. N-(2,6-2 methylphenyl)-2-(diethylamino) acetamide hydrochloride monohydrate is commonly used. 99.9% Pure Lidocaine Powde is a local anesthetic with extensive applications. In addition to its chemical reaction properties, Lidocaine also has various physical properties, which are also very important and have a significant impact on the performance and effectiveness of Lidocaine in the preparation and application process. The solubility in water is relatively high, reaching 6g/L. However, in organic solvents such as ethanol, methanol, and acetone, Lidocaine has relatively poor solubility. This characteristic affects the solubility and stability of Lidocaine in different carriers, and also determines the appropriate solvent type selected during the preparation process of the formulation. It is a local anesthetic widely used to relieve pain during surgical procedures, dentistry, skin surgery, and other processes. In addition to being used as an anesthetic, Lidocaine has also been found to have a range of other medical and non medical uses.
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Morphological |
powder |
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Acidity coefficient (PKA) |
PKA 7.88 (H2O) (approximate) |
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Solubility ethanol |
4 mg / ml |
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Storage condition |
store at RT |
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Flash point |
9 ℃ |
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Color |
white to slightly yellow |
Lidocaine Powder COA
When using Lidocaine, we need to consider all its reaction properties, which will help us better understand and use it. The following is a detailed description of all reaction properties of Lidocaine:
99.9% Pure Lidocaine Powder belongs to amine compounds and therefore appears alkaline in solution. Lidocaine molecules contain two basic nitrogen atoms that can accept protons to form salts. In water, Lidocaine salts are easily soluble and have strong electrolysis properties. When Lidocaine combines with strong acids, it can form hydrochloride, which is a commonly used method for preparing Lidocaine anesthetics.
Lidocaine molecules contain resonance structures of methylene and benzene rings, and the charge transfer between them gives Lidocaine good reducibility. In the body, Lidocaine is often reduced to its metabolites such as monoethylglycinxlide (MEGX) and glycinxlide (GX). These metabolites have different pharmacological activities and can affect the bioavailability and efficacy of Lidocaine in vivo.
Lidocaine has good thermal stability. After several months of storage at room temperature, there will be no significant decomposition reaction. In high temperature and humidity environments, Lidocaine may decompose, leading to a decrease in its anesthetic effect. Therefore, we need to pay attention to maintaining good conditions when storing and using Lidocaine.
Allergic reactions to Lidocaine are a very rare phenomenon, but they cannot be completely ruled out. If any allergic symptoms occur, such as swelling, shortness of breath, rash, gastrointestinal discomfort, etc., Lidocaine should be immediately stopped and seek medical assistance.
Lidocaine undergoes metabolism and transformation in the body, with the most important metabolic pathways including N-demethylation and hydroxylation reactions in the liver. The conversion products MEGX and GX have different pharmacological activities and can be used as indicators for evaluating Lidocaine metabolism. The conversion effect has a significant impact on the efficacy and tolerance of Lidocaine.
Side effects
Lidocaine powder is widely used in clinical practice, but it may also cause a series of side effects, involving multiple aspects such as the nervous system, cardiovascular system, and allergic reactions. The following will introduce in detail its common side effects and treatment methods.
Neurological side effects
Common symptoms
Lidocaine may have an impact on the central nervous system, initially manifested as symptoms such as dizziness, drowsiness, tinnitus, numbness of the mouth and tongue, blurred vision, and slurred speech. As the dosage increases or the degree of poisoning deepens, severe symptoms such as restlessness, muscle twitching, loss of orientation, and even convulsions, respiratory depression, and coma may occur.
Occurrence mechanism
Lidocaine blocks nerve excitation and conduction by inhibiting the sodium ion channels in the nerve cell membrane. When drugs are taken in excess or accidentally enter the blood vessels, the inhibitory effect of the central nervous system intensifies, leading to the above symptoms.
Treatment method
For mild symptoms, you can rest and observe. Avoid driving or operating machinery.
For severe symptoms, the medication should be stopped immediately and anticonvulsant drugs (such as diazepam) and respiratory support treatment should be given.
When a seizure occurs, short-acting barbiturates or muscle relaxants can be administered intravenously.
Cardiovascular system side effects
Common symptoms
Lidocaine may cause arrhythmias such as bradycardia, hypotension, atrioventricular block and sinus arrest. When used in large doses, it may even lead to life-threatening conditions such as ventricular fibrillation and cardiac arrest.
Occurrence mechanism
Lidocaine has a direct inhibitory effect on myocardial cells and can reduce myocardial contractility and cardiac output. Meanwhile, the drug may relax the vascular smooth muscle, leading to a decrease in blood pressure.
Treatment method
Stop the medication immediately and closely monitor the electrocardiogram and blood pressure.
When there is bradycardia or atrioventricular block, atropine or isoproterenol can be given for treatment.
Severe arrhythmia requires the use of pacemakers or defibrillation.
When blood pressure drops, oxygen inhalation is needed, acidosis should be corrected, and blood pressure-raising drugs should be used.
Allergic Reactions
Common symptoms
Allergic reactions may manifest as rashes, itching, edema, angioedema, bronchospasm, breathing difficulties, laryngeal spasm, shock and urticaria, etc. When lidocaine is injected into the spinal cord or applied externally, it may even cause fatal bronchospasm or respiratory distress syndrome.
Occurrence mechanism
Lidocaine allergic reactions belong to type I hypersensitivity reactions and are mediated by IgE. Drugs or their metabolites, as haptens, combine with proteins in the body to form total antigens, stimulating the body to produce specific IgE antibodies. When exposed to the drug again, IgE binds to mast cells and basophils, releasing active mediators such as histamine, which leads to allergic symptoms.
Treatment method
Immediately discontinue the medication and provide anti-allergy treatment, such as using antihistamines like loratadine and cetirizine hydrochloride.
Severe allergic reactions require intravenous injection of glucocorticoids (such as dexamethasone) and epinephrine.
Keep the airway unobstructed. If necessary, perform tracheal intubation or tracheotomy.
Local Reactions
Common symptoms
When lidocaine is used externally, symptoms such as erythema, edema, burning sensation, itching, dermatitis, papules, blisters, bruising, peeling or petechiae may occur at the injection site. These symptoms are usually mild and short-lived and can naturally subside within a few minutes or hours.
Occurrence mechanism
Lidocaine is irritating to the local skin and mucous membranes and may trigger an inflammatory response. In addition, excessively high drug concentration or improper injection techniques may also aggravate local reactions.
Treatment method
Mild symptoms can be observed. Avoid scratching and hot compresses.
For severe symptoms, local cold compresses can be applied and antihistamine creams (such as hydrocortisone cream) can be used.
Improve the injection technique to reduce the irritation of the drug to the local tissue.
Other Side Effects
Symptoms of the digestive system
Lidocaine may cause symptoms such as nausea and vomiting, which may be related to the irritation of the gastrointestinal tract or the inhibition of the central nervous system by the drug.
Impact on vision and hearing
Long-term or excessive use of lidocaine may lead to side effects such as blurred vision and hearing loss.
Treatment method
Nausea and vomiting can be treated with antiemetic drugs (such as metoclopramide).
Blurred vision and hearing loss require prompt medical attention. If necessary, change to other medications.
The discovery of lidocaine is an important milestone in the field of anesthesiology, and its development process embodies the wisdom of scientists and the spirit of medical exploration.
Early exploration and chemical fundamentals
The discovery of lidocaine originated from the study of the chemical structure of the alkaloid gramine. When scientists were synthesizing the isomer of isogarmine, they found that it has a local anesthetic effect. This discovery prompted researchers to further synthesize similar compounds, and eventually lidocaine was successfully synthesized by Nils Lofgren and Bengt Lundqvist from Stockholm University in Sweden in 1943. Lofgreen was still a doctoral student at that time, while Lundquist verified its anesthetic effect through autologous injection, laying the foundation for subsequent research.
Patents and commercialization processes
After the synthesis of lidocaine, Lundquist suggested conducting pharmacological tests at the Karolinska Institute and subsequently transferring the patent rights to the Swedish pharmaceutical company Astra AB. The company launched lidocaine to the market under the trade name "Xylocaine" in 1948, marking its official entry into clinical application. In the same year, Lofgreen completed his doctoral dissertation "Lidocaine: A New Synthetic Drug", further promoting the academic recognition of the drug.
Clinical advantages and wide application
Lidocaine has rapidly become one of the preferred drugs for local anesthesia due to its rapid onset and long-lasting effect. It is applicable to various scenarios such as infiltration anesthesia, block anesthesia and surface anesthesia, and has relatively low toxicity and high safety. Since 1949, lidocaine has been widely promoted on a large scale. It has not only been widely used in surgical operations but also gradually expanded into the field of arrhythmia treatment. In 1963, lidocaine was used to treat ventricular arrhythmias caused by acute myocardial infarction and became an important drug for the prevention and treatment of rapid ventricular arrhythmias.
Scientific breakthroughs and continuous impact
The discovery of lidocaine is a model of the interdisciplinary research between chemistry and medicine. It not only solves the addiction problem of traditional anesthetics such as cocaine, but also enhances the anesthetic efficacy and safety through structural optimization. To date, lidocaine remains a core drug in the field of local anesthesia. Its derivatives and improved dosage forms (such as aerosols and gels) keep emerging, further expanding the scope of clinical applications.
Summary
From the accidental discovery of the isomer of luteinine to the synthesis and commercialization of lidocaine, this process reflects the contingency and inevitability of scientific exploration. The birth of lidocaine not only promoted the development of anesthesiology, but also provided important inspirations for subsequent drug research and development. Its status as a classic local anesthetic remains difficult to be completely replaced to this day.
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