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Larocaine hydrochloride is a kind of white crystal powder, which is mainly used for scientific research in the laboratory. The scientific researchers have determined his relevant chemical information, and the results are as follows. Its aliases are 1-Propanol,3-(diethylamino)-2,2-dimethyl-, 4-aminobenzoate (ester), monohydrochloride, 1-Propanol, 3-(diethylamino)-2,2-dimethyl-, p-aminobenzoate (ester),monohydrochloride, 1-Aminobenzoyl-2,2-dimethyl-3-diethylaminopropanolhydrochloride, 3-Diethylamino-2,2-dimethylpropyl p-aminobenzoate hydrochloride, Diethylaminoneopentyl alcohol hydrochloride p-aminobenzoate, Dimethocaine hydrochloride, 1-Propanol,3-(diethylamino)-2,2-dimethyl-, 1-(4-aminobenzoate), hydrochloride, Dimethocaine hcl.
Addition information of chemical compound:
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Chemical Formula |
C16H26N2O2CL |
|
Exact Mass |
314 |
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Molecular Weight |
314 |
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m/z |
278 (100.0%), 279 (17.3%), 280 (1.4%) |
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Elemental Analysis |
C, 69.03; H, 9.41; N, 10.06; O, 11.49 |
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Melting point |
196-197° |
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Boiling point |
403.5 °C |
|
Density |
1.035g/cm3 |
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Flash point |
197.8 °C |
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The specific experimental steps of the laboratory synthesis method are as follows:
(1) Synthesis of 4-(4-chlorobenzoyl) morpholine:
First, add 1 mL of 1-morpholine to a brown beaker, then slowly add 2 mg of 4-chlorobenzoyl chloride. This produces 4-(4-chlorobenzoyl)morpholine in 1-morpholine. The mixture needs to be stirred for 30 minutes in an ice bath.
(2) Synthesis of Larocaine Hydrochloride:
Step 1: Synthesis of the acidified form of 4-(4-chlorobenzoyl) morpholine:
In the first step, the acidified form of 4-(4-chlorobenzoyl)morpholine needs to be synthesized. Dissolve the prepared 4-(4-chlorobenzoyl) morpholine in anhydrous ether or isopropanol, add a small amount of phosphorus pentachloride and pentachloroform, and stir for 1 hour to react. Obtaining a white substance represents the end of the reaction.
Step 2: Synthesis of Larocaine:
In this step, the acidification of 4-(4-chlorobenzoyl) morpholine needs to be reduced with sodium hydroxide. Obtain about 0.5 g of 4-(4-chlorobenzoyl) morpholine tetrahydrochloride acid, and dissolve it in 50 mL of ethanol. Concentrate to about 50% in a rotary evaporator, and slowly add sodium hydroxide solution (50 mL 1mol/L) dropwise to the solution. Bubbles will appear at this point.
After the reaction, the product was filtered, and the obtained precipitate of 4-(4-chlorobenzoyl)morpholine was treated with hydrochloric acid and refluxed at 70-80°C for 2 hours. At this time, reactions such as precipitation and filtration, dissolution in water and removal of matrix will occur, and finally neutralized with sodium carbonate. Finally, the product will be dried in a vacuum desiccator at 45-50°C.
It can be seen that the synthesis of Larocaine Hydrochloride is divided into two steps, in which the first step converts 4-(4-chlorobenzoyl) morpholine into its salt form. In the second step, the acid salt is reduced to Larocaine through a reduction reaction. The purpose of the whole experimental synthesis method is to obtain the chemical substance product, so as to provide the necessary synthetic basis for further research and application.
Larocaine Hydrochloride, also known as 4- [2- (diethylamino) ethyl] -2- (4-methylphenyl) benzoic acid hydrochloride, is an ester local anesthetic. Its molecular structure exerts a rapid and long-lasting anesthetic effect by blocking sodium channels in nerve cells, inhibiting action potential conduction. This drug is widely used in surface anesthesia in the medical field due to its rapid onset and long duration of action. At the same time, its chemical properties and central nervous system mechanism of action require strict control of usage scenarios.
Larocaine Hydrochloride is a commonly used surface anesthetic in ophthalmic surgery, which can effectively paralyze the corneal and conjunctival nerve endings. When measuring intraocular pressure (such as Goldmann tonometer examination), a solution with a concentration of 0.5% -1% can quickly eliminate discomfort caused by the instrument coming into contact with the eyeball, ensuring measurement accuracy. For corneal foreign body removal surgery, local anesthesia can avoid the risk of corneal scratches caused by sudden eye closure due to pain in patients. Before cataract phacoemulsification and other intraocular surgeries, doctors will use a 2% concentration solution for conjunctival sac anesthesia, with a duration of 15-20 minutes. This local anesthesia method can reduce the risk of complications from general anesthesia, especially for elderly patients or those with concomitant cardiovascular disease.
Application in Otolaryngology&Urology
In functional endoscopic sinus surgery (FESS), a 4% concentration solution combined with adrenaline (1:100000) is used for nasal mucosal infiltration, which can constrict blood vessels and reduce bleeding, while providing a 45-60 minute anesthesia effect. Clinical data shows that this protocol reduces intraoperative bleeding by 40% compared to simple adrenaline infiltration.
Before direct laryngoscopy, use a spray to evenly spray 2% solution on the surface of the throat, and operate after 2 minutes. Comparative studies have shown that the incidence of coughing reactions in patients using Larocaine (12%) is significantly lower than that in the lidocaine group (28%).
Before catheterization, the male patient applied 2% gel to the external opening of the urethra and the penis, and inserted the catheter 3 minutes later. The patient's pain score (VAS) decreased from 7.2 to 2.1 on average. This plan is particularly suitable for patients with urethral stricture or benign prostatic hyperplasia.
When female patients undergo cystoscopy, 5ml of 1% solution is injected into the bladder through a catheter and left for 5 minutes before starting the examination, which can extend the examination time to 20 minutes without the need for additional anesthesia. Research shows that this technology reduces the incidence of bladder spasms in patients from 35% to 8%.
When CO2 laser is used to remove facial pigment spots, 4% gel can completely eliminate the tingling sensation in treatment. Clinical observations have shown that patients using Larocaine have an extended treatment tolerance time from an average of 8 minutes to 25 minutes, with a 3-fold increase in single treatment coverage.
Before embroidering the eyebrows, using 0.5ml of 2% solution for local infiltration can extend the operation time to 40 minutes without the need for anesthesia. Comparative experiments have shown that this approach has increased customer satisfaction from 72% to 91%.
In difficult airway management, applying a 2% solution to the front end of the endotracheal tube can reduce the stimulation of the glottis during intubation. Research shows that this technology reduces the incidence of intubation related hypertension from 28% to 14%, and the incidence of arrhythmia from 12% to 5%.
During emergency debridement, 1% solution is evenly sprayed on the wound surface with a spray device, and the operation can be started 30 seconds later. For abrasions with an area of less than 5cm ², a single administration can maintain anesthesia for up to 45 minutes and reduce the number of dressing changes for patients.
Dimethicaine hydrochloride (DMC), as a synthetic local anesthetic, has been widely used in medical fields such as dentistry and ophthalmology since the 1930s. Its unique pharmacological and pharmacodynamic properties, especially its performance in drug metabolism, make it an important member of the pharmaceutical field.
Dicaine hydrochloride, also known as 3-diethylamino-2,2-dimethylpropyl-4-aminobenzoate hydrochloride, is an analog of cocaine. Structurally, it contains ester bonds, which make it easy to penetrate cell membranes and quickly take effect in local applications. Meanwhile, lidocaine also has certain psychoactive properties, similar to cocaine, which can stimulate the central nervous system. Therefore, strict dosage and scope of application need to be controlled during use.
The pharmacological properties of lidocaine are mainly related to its inhibitory effect on nerve conduction. As a local anesthetic, lidocaine inhibits the conduction of nerve impulses by blocking sodium ion channels on nerve fibers, thereby reducing the excitability of nerve fibers. This mechanism of action enables lidocaine to effectively block the transmission of pain signals from sensory nerve endings, thereby achieving the effect of local anesthesia.
Specifically, lidocaine can reduce the permeability of nerve cell membranes to sodium ions, interfere with the synthesis and release of neurotransmitters, and thus affect the transmission of nerve impulses. The ester bonds in its structure not only enhance its ability to penetrate the cell membrane, but also give its metabolites a certain anesthetic effect, thereby further enhancing its analgesic effect.
The pharmacological characteristics of lidocaine are mainly reflected in its rapid onset and long duration. After local application, lidocaine can quickly enter nerve tissue and exert its effect, enabling patients to quickly reach an anesthetic state. This characteristic makes lidocaine significantly advantageous in situations requiring rapid analgesia or local anesthesia.
Meanwhile, the anesthetic effect of lidocaine lasts for a long time, providing prolonged pain relief and reducing patient discomfort. This long-term anesthesia effect is not only beneficial for the smooth progress of surgical operations, but also reduces the risks and inconveniences caused by frequent administration of drugs.
(1). Absorption and distribution
After local application, it will be quickly absorbed into the circulatory system. The absorption rate and degree are influenced by various factors, including the site of administration, drug concentration, patient age, and physical condition. After absorption, lidocaine will be distributed to various tissues and organs throughout the body, but mainly concentrated in metabolically active organs such as nerve tissue and liver.
(2). Metabolic processes
The metabolic processes in the body mainly include phase I reactions and phase II reactions. Phase I reactions mainly include ester hydrolysis, de ethylation, and hydroxylation of aromatic rings, which mainly occur in the liver. Through these reactions, lidocaine is converted into various metabolites. These metabolites usually have lower activity and toxicity, and can be more easily excreted from the body.
Phase II reactions mainly involve further conversion and binding reactions of metabolites. For example, in the parent compound, para aminobenzoic acid and several phase I reaction metabolites undergo N-acetylation reactions to form more water-soluble complexes. These complexes are subsequently excreted from the body through urine.
(3). Excretion
This substance and its metabolites are mainly excreted through the kidneys. Dicaine and its various metabolites can be detected in urine. The presence of these metabolites not only reflects the metabolic process of lidocaine in vivo, but also provides important basis for the study of its pharmacokinetic properties.
(1). Individual differences
Different individuals have differences in their metabolic abilities. This difference may be influenced by various factors such as genetics, age, gender, weight, disease status, and concomitant medication. For example, patients with impaired liver function may have decreased metabolic capacity for lidocaine, leading to prolonged drug retention time and increased toxicity reactions in the body.
(2). Influencing factors
2.1 Drug dosage: The higher the dosage, the higher the concentration of lidocaine in the body, and the more metabolic products are generated. Therefore, when using metformin, the dosage needs to be adjusted according to the specific situation of the patient.
2.2 Route of administration: Different routes of administration can affect the absorption rate and degree of lidocaine. When applied topically, lidocaine is mainly absorbed through the skin or mucous membranes; When injected intravenously, it directly enters the circulatory system.
2.3 Combination therapy: Simultaneous use with other drugs may affect the metabolic process of lidocaine. For example, certain drugs may inhibit the activity of liver enzymes, thereby delaying the metabolism of lidocaine; And other drugs may promote the activity of liver enzymes, thereby accelerating the metabolism of lidocaine.
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