Procaine CAS:59-46-1

    Procaine is a local anesthetic drug of the amino ester group. It is used primarily to reduce the pain of intramuscular injection of penicillin, and it is also used in dentistry. Owing to the ubiquity of the trade name Novocain, in some regions procaine is referred to generically as novocaine. It acts mainly as a sodium channel blocker. Today it is used therapeutically in some countries due to its sympatholytic, anti-inflammatory, perfusion enhancing, and mood enhancing effects.

    Procaine was first synthesized in 1905, shortly after amylocaine. It was created by the German chemist Alfred Einhorn who gave the chemical the trade name Novocaine, from the Latin nov- (meaning new) and -caine, a common ending for alkaloids used as anesthetics. It was introduced into medical use by surgeon Heinrich Braun. Prior to the discovery of amylocaine and procaine, cocaine was the most commonly used local anesthetic. Einhorn wished his new discovery to be used for amputations, but surgeons preferred general anesthetic. Dentists, however, found it very useful.

    Procaine hydrochloride acts on peripheral nerves to produce conduction blocking effects. It relies on concentration gradients to penetrate the nerve cell membrane in a diffuse manner, blocking sodium ion channels on the inside, raising the excitation threshold of nerve cells and losing excitability and conductivity. Information Delivery blocked. Procaine hydrochloride has a stronger effect on sensory nerves than motor nerves, and on small fibers than large fibers. Procaine hydrochloride also has antiarrhythmic, anticonvulsant, anti-inflammatory and coronary artery dilation effects.

    It is less toxic and is one of the commonly used local anesthetics. This drug is a short-acting ester local anesthetic with low lipophilicity and weak penetration into mucous membranes. Generally not used for topical anesthesia, local injection is often used for infiltration anesthesia, conduction anesthesia, subarachnoid anesthesia and epidural anesthesia. It takes effect 1-3 minutes after injection and can last for 30-45 minutes.

    The maintenance time can be extended by 20% after adding epinephrine. Procaine can be hydrolyzed by esterase in plasma and converted into para-aminobenzoic acid (PABA) and diethylaminoethanol. The former can resist the antibacterial effect of sulfa drugs, so it should be avoided to be used together with sulfa drugs. Procaine can also be used for local sealing of injured areas. Overdose may cause central nervous system and cardiovascular reactions. Sometimes it can cause allergic reactions, so a skin allergy test should be done before taking the medicine, but those with negative skin tests can still have allergic reactions. Those who are allergic to this drug can use chloroprocaine and lidocaine instead.

    Procaine hydrochloride is mainly hydrolyzed by the liver into p-aminobenzoic acid and diethylamine in the body. The former is combined with glycine and excreted in the urine, and the latter is acetylated or methylated and excreted in the urine. The elimination half-life of procaine hydrochloride is 1.5 to 2 hours, which is affected by hepatic blood flow, liver function and plasma cholinesterase activity.

    Procaine hydrochloride is mainly used for infiltration anesthesia, catheter block and spinal topical anesthesia. Aqueous solutions with a commonly used concentration of 0.25% to 1% can be added with vasoconstrictors such as epinephrine to extend the local action time. Procaine hydrochloride can also be used as an adjuvant treatment for cardiac arrhythmias, status epilepticus, and acute myocardial infarction.

    Combining procaine hydrochloride with other local anesthetics can enhance or prolong the local anesthetic effect, but also increases the risk of toxic reactions. Combining procaine hydrochloride with antiarrhythmic drugs, beta-blockers, calcium channel blockers, digoxin, etc. can increase the cardioinhibitory effect. The combined use of procaine hydrochloride with anticonvulsants, barbiturates, chlorpromazine, etc. can increase the central nervous system depressant effect. Concomitant use of procaine hydrochloride with epinephrine may prolong local action but also increase the risk of arrhythmias. Combining procaine hydrochloride with reducing agents such as sodium thiosulfate can accelerate its hydrolysis failure.

    Local injection: The concentration of the injection is mostly 0.25%-0.5%, and the dosage depends on the needs of the condition, but it should not exceed 1.5g per hour. If the anesthesia time is short, a small amount of epinephrine (1; 1) can be added to prolong the effect. Dental anesthesia sometimes uses a solution concentration of 2% to 4%.
    Precautions
    1. When high concentrations are accidentally injected into blood vessels, it can cause restlessness, floating sensation, dizziness, confusion, perioral sensory abnormalities, tinnitus, and tremors of the face and distal limbs; subsequently, tonic-clonic convulsions may occur. When the plasma concentration is very high, it can inhibit breathing and cause respiratory arrest and
coma.

    2. Excessive dosage may cause nausea, sweating, pulse rate, difficulty breathing, facial flushing, delirium, excitement, and convulsions. Convulsions can be rescued by intravenous injection of amobarbital.
    3. During spinal anesthesia, blood pressure often drops, which can be prevented by intramuscular injection of 15 to 20 mg of ephedrine before anesthesia.
    4. Anaphylactic shock sometimes occurs, so the patient's allergy history should be asked before medication, and an intradermal test (intradermal injection of 0.1ml of 0.25% solution) should be performed on patients with allergic constitution.
    5. It is not suitable to be compatible with glucose solution as it may reduce its local anesthetic effect.

    Treat hemoptysis
    Intravenous infusion of procaine can dilate peripheral blood vessels and reduce the amount of blood returned to the heart. After instillation in patients with pulmonary tuberculosis hemoptysis, it expands the capillaries in the lungs and reduces the resistance of the pulmonary circulation, thus reducing the pulmonary artery pressure, reducing the blood flow of the lungs, and achieving hemostasis. Li Furong et al. reported that 16 patients with pulmonary tuberculosis and massive hemoptysis were treated. Method: procaine was prepared into a 0.25% solution of 200 m1 with normal saline, once/d, at a drip rate of 20 to 40 drops/min, until the hemoptysis stopped. Results: Among the 16 patients in this group, 12 were markedly effective, 3 were effective, and 1 was ineffective (6.2%). The total effective rate was 93.8%.
    Procaine can produce a continuous benign stimulation of acupoints through acupoint injection, maintain a certain "needle feeling" within 24 hours, and produce a moderate "vasoconstriction state" to achieve the purpose of stopping bleeding. Liu Liping reported: 52 patients with hemoptysis due to lung diseases were treated with 4ml of 2% procaine injection. Take Neiguan points on both sides and inject 1.5 to 2m1 into each one, once a day. Results: 29 cases were markedly effective, 15 cases were effective, the total effective rate was 84.6%, and 8 cases were ineffective, accounting for 15.33%.

Trade names	Benzoic acid, 4-amino-, 2-(diethylamino)ethyl ester; 4-aminobenzoic acid 2-diethylaminoethyl ester; PROCAINE; novocaine
CAS	59-46-1
Molar mass	236.315
MF	C13H20N2O2
Purity	Above 99%
Apprarance	White Crystals

 

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    Procaine is most often used as an anti-aging agent for conditions such as dementia, age-related decline in memory and thinking skills, quality of life, and many others, but there is no good scientific evidence to support these uses. As a prescription-only injection, procaine is used for local anesthesia.

 

 

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