NOVOCAINE (Novocainum, synonym: Jenacain, Polocainum, Procaini Hydrochloridum, Procaine Hydrochloride etc., GFH; SI. B) — mestnoanesteziruyushchy means. Beta and Diethylaminoethyl ether n-aminobenzoic to - you are a hydrochloride; With 13 H 20 O 2 N 2 - HCl:
Colourless crystals or inodorous white crystal powder. Let's very easily dissolve in water, it is easily alcohol-soluble. Water solutions will sterilize fluid steam at t ° 100 ° within 30 min. or in the autoclave under pressure of 1 atm within 20 min. N. is easily hydrolyzed in alkaline condition. For stabilization add 0,1 N solution salt to - you to pH 3,8-4,5.
On activity and duration of action at infiltration, conduction, peridural and spinal anesthesia H. concedes to Trimecainum (see) and to a xycain (see). At surface anesthesia H. it is ineffective. N.'s toxicity and Trimecainum in 0,125 — 0,25% solutions is identical; in 0,5 — 1% solutions H. by 1,2 — 1,4 times is less toxic, than Trimecainum.
On a number of properties (short duration of action, small efficiency at terminal anesthesia, instability, etc.) concedes to drugs from group of aromatic amides in solutions (to Trimecainum, etc.).
At various ways of introduction of N. it is easily soaked up in blood, having resorptive effect. At resorptive action of N. reduces formation of acetylcholine, also spasmolytic action has holinoblokiruyushchy effect on smooth muscles on vegetative a ganglion, lowers excitability of a muscle of heart and motor zones of a cerebral cortex. For braking of absorption and lengthening of effect of solutions H. at local anesthesia to them usually add 0,1% solution of Adrenalinum hydrochloricum (on 1 drop on 2 — 5 — 10 ml of solution H.). N.'s biotransformation occurs hl. obr. by hydrolysis under the influence of cholinesterase of a blood plasma. Products of euzymatic hydrolysis of N. — paraaminobenzoic to - that (PABK) and dnetilaminoeta-nol — pharmacological active agents. PABK (to 80%) in not changed or conjugated form and diethylaminoethanol (to 30%) are allocated with urine, other part of metabolites breaks up.
N apply to carrying out all types of local anesthesia (see. Anesthesia local ) (except terminal). During the carrying out an infiltration anesthesia of N. apply in the form of 0,25 and 0,5% of solutions. The first single dose of N. at the beginning of operation shall be no more than 1,25 g that corresponds 500 ml of 0,25% of solution, or 0,75 g that corresponds to 150 ml of 0,5% of solution. Further for each hour of operation it is possible to enter no more than 2,5 g of novocaine, i.e. 1000 ml of 0,25% of solution or 400 ml of 0,5% of solution.
For anesthesia by Vishnevsky's method (a method of hard creeping infiltrate) solutions, for conduction anesthesia — 1 — 2% solutions t (to 20 — 25 ml), for peridural — 2% solution (20 — 25 ml), for spinal — 5% solution (2 — 3 ml), for intradermal — 0,25 and 0,5% solutions (for anesthesia of upper extremities enter 25 — 90 ml, for anesthesia of the lower extremities — 45 — 120 ml) use 0,125 and 0,25%.
Besides, solutions H. apply at treatment of an idiopathic hypertensia, late toxicoses of pregnancy with a hypertensive syndrome, spasms of blood vessels, an endarteritis, a ciliary arrhythmia, a peptic ulcer of a stomach and duodenum, pancreatitis, nonspecific ulcer colitis, glaucoma, etc. At this N. appoint in the form of 0,25 and 0,5% of solutions on 1 — 15 ml, to-ry enter intravenously (slowly), or in the form of 2% of solution, to-ry enter intramusculary 5 ml 3 times a week. Treatment is carried out by courses on 12 injections with breaks between courses for 10 days. Sometimes N. appoint in (0,25% and 0,5% solutions on 30 — 5O ml 2 — 3 times a day). For novocainic blockade (see) use 0,25% solution in number of no more than 100 — 150 ml or 0,5% solution in number of no more than 50 — 80 ml. For treatment by method electrophoresis (see) solutions, a dia-dinamoforeza — 2 and 5% solutions apply 5 and 10%.
The highest doses of N. for adults: inside — one-time 0,25 g, daily 0,75 g; intramusculary — one-time and daily 0,1 g (5 ml of 2% of solution); intravenously — one-time 0,05 g (20 ml of 0,25% of solution), daily — 0,1 g (40 ml of 0,25% of solution). At all ways of introduction of N. it is necessary to apply with care since to it hypersensitivity is often observed, the first signs a cut the general weakness, dizziness, a sonitus, nausea, vomiting, decrease in the ABP, etc. are. For detection of hypersensitivity to N. it is appointed in the reduced doses in the beginning.
At to overdose N are observed a collapse, clonic spasms and respiratory depression. The help at N.'s poisoning comes down to purpose of symptomatic operating means. The N is incompatible with sulfanamide drugs. It is contraindicated at individual intolerance and existence of purulent process on site of introduction.
Forms of release: powder; ampoules on 1; 2; 5; 10 and 20 ml of 0,25% and 0,5% of solution and on 1; 2; 5 and 10 ml of 1% and 2% of solution; the bottles containing sterile 0,25 and 0,5% solution; 5 and 10% ointment; the candles containing 0,1 g of N. Sokhranyayut in well corked banks of orange glass; ampoules and candles — in the place protected from light.
See also Anesthetics .
Bibliography: Mashkovsky M. D. Pharmaceuticals, p.1, page 289, M., 1977; Adriani J. The clinical pharmacology of local anesthetics, Clin. Pharm. Ther., v. 1, p. 645, 1960; International encyclopedia of pharmacology and therapeutics, sect. 8, v. 1 — Local anesthetics, contrib. J. Biichi a. o., Oxford, 1971; d e Jong R. H. Physiology and pharmacology of local anesthesia, Springfield, 1970; The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, p. 388, N. Y. a. o., 1975.
H. T. Pryanishnikova.