Anesthetics Tetracaine hydrochloride raw powder

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Tetracaine hydrochloride powder Usage and Synthesis.

Tetracaine hydrochloride is used for mucosal surface anesthesia, conduction anesthesia, epidural anesthesia and subarachnoid anesthesia. It is used for ophthalmic surface anesthesia without constricting blood vessels, damaging corneal epithelium and increasing intraocular pressure.

Tetracaine hydrochloride is a kind of long-acting ester local anesthetic, which has the characteristics of strong penetration of mucosa and is suitable for surface anesthesia, and is often used in ophthalmology. After injection, the anesthetic effect appears slow (about 10 minutes), the post-absorption metabolism is also slow, and the local anesthesia time is up to 3 IJ, H,-J. Around. There were no adverse reactions such as vasoconstriction, dilated pupil and corneal injury after tetracaine hydrochloride, and the local anesthetic effect and toxicity were about 10 times greater than that of procaine. It is mainly used for surface anesthesia of the mucous membranes of the eyes, nose and throat, and rarely used for conduction anesthesia and epidural anesthesia. It is generally not used for infiltration anesthesia due to high toxicity.

Drug interaction of Tetracaine hydrochloride powder.

1. This drug can enhance the nerve blocking effect of cisatracurium, and the dosage of the latter should be reduced when combined.

2. In combination with adrenaline, blood vessels can be constricted, blood flow is reduced, drug absorption is slowed down, and the duration of action is prolonged. However, they are not suitable for patients with heart disease, hypertension, hyperthyroidism and peripheral vascular disease.

3. Hyaluronidase can effectively increase the diffusion of this drug, accelerate the effect of anesthesia, reduce local swelling, and prevent the formation of hematoma, however, hyaluronidase can also accelerate the absorption of this drug, resulting in increased toxic reactions of this drug.

4. This drug is a derivative of p-aminobenzoic acid (PABA), and sulfonamides play an antibacterial role by inhibiting PABA of bacteria. When this drug is combined with sulfonamides, the antibacterial effect of the latter will be inhibited, so the two are not suitable for use.

5. This medicine is acidic and should not be mixed with alkaline liquid. Even if it is an acidic drug, the dissociation value of the drug can be affected due to the difference in pH, so that the effect is reduced, or the onset time is delayed.

6. Iodine preparation can cause the precipitation of this drug, so the injection site of this drug can not use iodine.

Preparation of Tetracaine hydrochloride powder.

Methyl isobutyl ketone 320.0kg was added to the reactor, followed by p-butylaminobenzoic acid 40.0kg(207mol) and anhydrous potassium carbonate 56.8kg. The oil bath was heated to 116℃ for reflux reaction for 4h, the heating was stopped and slightly cooled for 0.5h, and then 38.3 kg(266mol) dimethylamine hydrochloride was added. Continue heating to 116℃ for reflux reaction for 4h, after the reaction is completed and cooled to below 30℃, add 127.0kg of deionized water and stir for 30min, stand for 1h, separate the organic layer, and obtain oil after drying and concentrating, add 169.0kg of acetone and stir, adjust the pH value to 3-4 with concentrated hydrochloric acid, and precipitate a large number of crystals. After freezing for 12h, the 53.0kg white solid was obtained by centrifugation, filtration and drying. The yield was 85.07% and the HPLC purity was 99.34%.

Preparation method of Bulk Tetracaine hydrochloride powder.

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