Novokain-Zdorovye, solution for infection 2% on 2 ml No. 10

General characteristics. Structure:

International and chemical names: procaine; 2 (diethyl amines) of ethyl-4-aminobenzoate hydrochloride;
main physical and chemical properties: transparent colourless liquid;
structure: 1 ml of solution contains Procainum of a hydrochloride 5 mg or 20 mg;
excipients: 0,1 M acid solution hydrochloric, water for injections.

Pharmacological properties:

Pharmacodynamics. Mestnoanesteziruyushchy means with moderate activity and a big range of therapeutic action. At intravenous administration shows analgeziruyushchy and antishock activity, hypotensive and antiarrhytmic action.
Interferes with generation of impulses in the terminations of sensory nerves and to carrying out impulses on nerve fibrils. Changes action potential in membranes of nervous cells without the expressed influence on rest potential.
At absorption and direct vascular introduction to a blood flow reduces excitability of peripheral cholinergic systems, reduces education and release of acetylcholine from the preganglionic terminations, reduces a spasm of smooth muscles, excitability of a myocardium and motor zones of a cerebral cortex oppresses. Eliminates the descending brake influences of a reticular formation of a brainstem. Oppresses polisinaptichesky reflexes. In high doses can break neuromuscular conductivity, cause spasms.
Shows the short anesthetizing activity (duration of an infiltration anesthesia makes 0,5–1 h).
In comparison with lidocaine and buvikainy Procainum has less expressed anesthetic effect in this connection, has rather small toxicity and bigger therapeutic width.
Antiarrhytmic action is caused by increase in the refractory period, decrease in excitability and automatism of a myocardium.
At intramuscular introduction it is effective for treatment of elderly patients at early stages of the diseases connected with functional disturbances of the central nervous system (arterial hypertension, spasms of coronary vessels and vessels of a brain, etc.).

Pharmacokinetics. At parenteral administration it is well soaked up. Extent of absorption depends on the place and a way of introduction (especially on vascularization and the speed of a blood-groove in the field of introduction) and a final dose (quantity and concentration). It is quickly hydrolyzed by esterases and cholinesterases of plasma and fabrics with education of two main pharmacological of active metabolites: diethylaminoethanol (possesses moderate vasodilating action) and paraaminobenzoic acid (is a competitive antagonist of sulfanamide chemotherapeutic medicines and can weaken their antimicrobic action). An elimination half-life – 30–50 with, in the neonatal period – 54–114 pages. It is allocated preferential with kidneys in the form of metabolites (80%); in not changed look no more than 2% are removed.
Metabolism of Procainum is broken at patients with genetic insufficiency of cholinesterase of plasma.
It is badly absorbed through mucous membranes.

Indications to use:

Infiltration, conduction, epidural anesthesia; vagosympathetic and perinephric blockade; circulator and juxtaspinal blockade at eczemas, neurodermatitis, an ischialgia. Potentiation of effect of anesthetics at the general anesthesia; a pain syndrome of various genesis (including at a peptic ulcer of a stomach and duodenum). As a part of complex therapy of early stages of the diseases meeting at advanced age (an endarteritis, atherosclerosis, arterial hypertension, spasms of coronary vessels and vessels of a brain, a disease of joints of rheumatic and infectious genesis) more often.

Route of administration and doses:

Novokain-Zdorovye apply vnutrikozhno, intramusculary, intravenously. To an infiltration anesthesia apply 0,25–0,5% solution, to anesthesia by Vishnevsky's method (hard creeping infiltration) – 0,125–0,25% solutions, to conduction anesthesia – 1–2% solutions, to Epi - or peridural anesthesia – 2% solution. Appointment for intra bone anesthesia is possible.
In need of use of lower concentration of Procainum (0,125% or 0,25%) Novokain-Zdorovye solutions before use part with sterile isotonic solution of sodium of chloride to required concentration.
Intravenous administration is carried out slowly, better in isotonic solution of sodium of chloride.
At local anesthesia the dosing mode individual, depending on a type of anesthesia, a way of introduction, indications, a state and age of the patient.
For conduction anesthesia enter 2% of solution to 25 ml; for epidural – 20–25 ml of 2% of solution. The highest doses of Procainum at conduction blockade of nerves and textures, epidural anesthesia – no more than 0,5 g once without Epinephrinum or 1 g with Epinephrinum.
At perinephric blockade (according to Vishnevsky) enter 50–80 ml of 0,5% of solution into pararenal cellulose, at vagosympathetic blockade – 30–100 ml of 0,25% of solution.
Apply to stopping of a pain syndrome intramusculary or intravenously. Intravenously enter from 1 ml to 10–15 ml 0,5% of solution.
At eczemas and neurodermatitis apply Novokain-Zdorovye of 0,5% to circulator and juxtaspinal blockade vnutrikozhno.
For treatment of early stages of the diseases meeting at advanced age more often (an endarteritis, atherosclerosis, arterial hypertension, spasms of coronary vessels and vessels of a brain, a disease of a rheumatic and infectious origin, etc.) enter intramusculary 2% solution on 5 ml 2 times a week, a course – 12 injections, a break – 10 days (within a year carrying out four courses is possible). At a ciliary arrhythmia enter intravenously 0,25% solution on 2–4 ml of 4-5 times a day.
For adults the maximum single doses at intramuscular introduction – 0,1 g, intravenous – 0,05 g; the maximum daily doses at both ways of introduction – 0,1 g.
Doses depending on age and body weight are not developed for children.
Novokain-Zdorovye apply also to dissolution of antibiotics of group of penicillin for the purpose of prolongation of their action.

Features of use:

Before use of Procainum obligatory there is a conducting skin test on individual sensitivity to drug to which hypostasis and reddening of the place of an injection testifies.
At use of drug control of functions cardiovascular, respiratory and central nervous systems is required.
At local anesthesia Procainum is applied to decrease in systemic action, toxicity and prolongation of effect in a combination with vasoconstrictors (0,1% hydrochloride Epinephrinum solution at the rate of 1 drop on 2–5 ml of Novokaina-Zdorovye solution).
When carrying out local anesthesia at use of the same general dose toxicity of Procainum of subjects is higher, than the applied solution is more concentrated. In this regard with increase in concentration of solution drug solution to smaller concentration (sterile isotonic solution of sodium of chloride) is recommended to reduce or part the general dose.
For the prevention of development of reactions of hypersensitivity therapy begin with introduction 2 ml of 2% of solution, in 3 days (in the absence of by-effects) enter 3 ml, then pass to introduction of a full dose – 5 ml to an injection.
Drug is used with care at the immediate surgeries which are followed by acute blood loss, the states which are followed by decrease in a hepatic blood-groove, progressing of cardiovascular insufficiency (usually owing to development of heart blocks and shock), inflammatory diseases or infection of the place of an injection, deficit of pseudo-cholinesterase, a renal failure, children's age (up to 18 years), at elderly patients (65 years), the seriously ill patients weakened patients are more senior at pregnancy, during childbirth and a lactation (feeding by a breast)
Procainum slowly gets through the unimpaired mucous membranes owing to what does not provide surface anesthesia.
In the period of out-patient treatment it is necessary to abstain from control of vehicles and the performance of work requiring special attention, speed of mental and motor reactions.

Side effects:

Novokain-Zdorovye it is usually well transferred, however the following side effects are sometimes possible. From the central and peripheral nervous system: headache, dizziness, drowsiness, weakness, motive concern, loss of consciousness, spasms, lockjaw, tremor, visual and acoustical disturbances, nystagmus, syndrome of a horse tail (paralysis of legs, paresthesias), paralysis of respiratory muscles, block motor and sensitive. From cardiovascular system: increase or lowering of arterial pressure, peripheral vazodilatation, collapse, bradycardia, arrhythmias, thorax pain. From an urinary system: involuntary urination. From the alimentary system: nausea, vomiting, involuntary defecation. From system of blood: methemoglobinemia. Allergic reactions: a skin itch, skin rash, other anaphylactic reactions (including an acute anaphylaxis), a small tortoiseshell (on skin and mucous membranes). Others: return of pain, resistant anesthesia, hypothermia.

Interaction with other medicines:

At intravenous administration Procainum strengthens the oppressing action on the central nervous system of means for the general anesthesia, hypnotic drugs, sedative drugs, narcotic analgetics and tranquilizers. Prolongs the neuromuscular blockade caused by succinylcholine (since both drugs are hydrolyzed by plasma cholinesterase). Use with MAO inhibitors (furasolidone, Procarbazinum, селегилин) increases risk of development of hypotension. Toxicity of Procainum is increased by antikholinesterazny drugs (slow down its hydrolysis). Procainum metabolite (paraaminobenzoic acid) is a competitive antagonist of sulfanamide drugs and can weaken their antimicrobic action. When processing the place of an injection of local anesthetic the disinfecting solutions containing heavy metals the risk of development of local reaction in the form of morbidity and hypostasis increases.

Contraindications:

Individual sensitivity.

Overdose:

It is possible only at use of Novokaina-Zdorovye in high doses.
Symptoms: pallor of integuments and mucous membranes, dizziness, nausea, vomiting, the increased nervous irritability, "cold" sweat, tachycardia, a tremor, spasms, respiratory depression, a sudden cardiovascular collapse.
Treatment: general resuscitation actions: oxygen inhalations, if necessary – carrying out artificial ventilation of the lungs. If spasms proceed more than 15-20 with, stop them intravenous administration of thiopental (100–150 mg) or diazepam (5–20 mg). At arterial hypotension and/or a depression of a myocardium intravenously enter ephedrine (15–30 mg).
In case of development of intoxication after an injection in muscles of a leg or a hand the urgent applying a tourniquet for decrease in further intake of drug in the general blood stream is recommended.

Storage conditions:

To store in the place protected from light at a temperature from 15 °C to 25 °C. To store in the place, unavailable to children.
Period of validity – 3 years.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 0,5% on 2 ml and 5 ml or 2% on 2 ml in ampoules No. 5 2, No. 10.