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After absorption, procaine is hydrolyzed to p-aminobenzoic acid and diethylaminoethanol by plasma pseudocholinesterase. The former can compete against the antibacterial action of sulfonamides and weaken the curative effect of sulfonamides. The latter can enhance the effect of digitalis, and patients who have taken sufficient digitalis should use this drug with caution. When procaine is combined with succincholine, both drugs are hydrolyzed by plasma pseudocholinesterase. In the case of intravenous infusion of large amounts of procaine, it is possible to compete with the hydrolytic enzyme and reduce the hydrolytic inactivation of succincholine, significantly strengthen and prolong its muscle relaxation effect, resulting in respiratory paralysis.
Uses of Procaine.
Local anesthetic. Its toxicity is low, the action is rapid and safe. It is suitable for local anesthesia, eye, ear, nose, teeth and other surgeries, for infiltration anesthesia, mentor anesthesia and block therapy. It is also used in the production of procaine penicillin.
Pharmacological action of Procaine.
This product is an ester local anesthetic, which can temporarily block the conduction of nerve fibers and has anesthetic effect. This product has weak penetration to skin and mucous membrane and is not suitable for surface anesthesia. This product on central nervous system macroinhibition, excessive excitation. First causes sedation, dizziness, pain threshold increases, and then causes vertigo, disorientation, ataxia, central inhibition continues to deepen, there is numbness, blurred consciousness, and then into a coma. If the dose continues to increase, the toxic symptoms of central excitation such as muscle tremor, irritability and convulsion may appear.
The small dose of this product has the effect of excitatory sympathetic nerve, which makes the heart rate increase and blood pressure rise. The dose increases, and the blood pressure decreases and the heart rate increases due to myocardial inhibition, peripheral vascular dilation and mild ganglion blockade. This product inhibits the release of acetylcholine in the presynaptic membrane, resulting in certain neuromuscular blockade, which can enhance the effect of non-depolarizing muscle relaxants, and directly inhibit smooth muscle and relieve smooth muscle spasm.
Product method of Bulk Procaine Powder.
P-nitrobenzoic acid and diethylaminoethanol are reflow esterified in xylene to obtain nitrocaine, then reduced to procaine by iron powder, and then obtained by hydrochloride.
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