Instructions for Novocaine injection solution 0.5% bottle 200 ml
Composition
active ingredient: procaine hydrochloride (novocaine);
100 ml of solution contain procaine hydrochloride (novocaine) 0.5 g or 0.25 g;
Excipients: 0.1 M hydrochloric acid solution, water for injection.
Dosage form
Solution for infusion.
Main physicochemical properties: clear colorless or slightly yellowish liquid.
Pharmacotherapeutic group
Local anesthetics. ATX code N01B A02.
Pharmacological properties
Pharmacodynamics.
Local anesthetic with moderate activity and a wide therapeutic range. The mechanism of anesthetic action is associated with the blockade of sodium channels, inhibition of potassium current, competition with calcium, reduction of the surface tension of the phospholipid layer of membranes, inhibition of redox processes and generation of impulses. When entering the blood, it reduces the formation of acetylcholine, reduces the excitability of peripheral cholinergic systems, has a blocking effect on vegetative ganglia, reduces spasms of smooth muscles, reduces the excitability of the cardiac muscle and motor zones of the cerebral cortex.
Pharmacokinetics.
When administered parenterally, it is well absorbed. The degree of absorption depends on the site and route of administration (especially on vascularization and blood flow velocity at the injection site) and the final dose (amount and concentration). It is rapidly hydrolyzed by esterases and cholinesterases of blood plasma and tissues with the formation of two main pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilator effect) and para-aminobenzoic acid (is a competitive antagonist of sulfonamide chemotherapeutic drugs and can weaken their antimicrobial effect). The half-life is 30-50 seconds, in the neonatal period - 54-114 seconds.
It is excreted mainly by the kidneys in the form of metabolites (80%); no more than 2% is excreted unchanged.
Poorly absorbed by mucous membranes.
Indication
Local and infiltration anesthesia, therapeutic blockades.
Contraindication
Increased individual sensitivity to any components of the drug.
Myasthenia gravis; arterial hypotension; purulent process at the injection site; urgent surgical interventions accompanied by acute blood loss; pronounced fibrous changes in tissues (for anesthesia by the method of creeping infiltrate).
Interaction with other medicinal products and other types of interactions
The drug reduces the effect of anticholinesterase drugs on neuromuscular transmission. Prolongs the neuromuscular blockade caused by suxamethonium (since both drugs are hydrolyzed by plasma cholinesterase). The metabolite of procaine (para-aminobenzoic acid) is a competitive antagonist of sulfonamide drugs and can weaken their antimicrobial effect. Concomitant use with MAO inhibitors increases the risk of developing arterial hypotension. The toxicity of procaine is increased by anticholinesterase drugs (inhibiting its hydrolysis). Cross-sensitization is possible. Intravenous administration of novocaine potentiates the effect of anesthetics.
When treating the injection site of novocaine with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of soreness and swelling increases. Potentiates the effect of direct anticoagulants.
Application features
To reduce systemic effects, toxicity, and prolong the effect of local anesthesia, procaine should be used in combination with vasoconstrictors (0.1% epinephrine hydrochloride solution at the rate of 1 drop per 2-5 ml of solution).
Skin tests with local anesthetics should be performed in individuals with a history of reactions to these drugs. Particular care is required when testing local anesthetics containing adrenaline because of the increased incidence of false-negative reactions. It is recommended that skin tests be performed if skin tests are negative. Testing of patients with a history of allergy to local anesthetics should only be performed by allergists experienced in drug allergy.
There is no international consensus on the procedure for performing and interpreting drug skin tests. No multicenter study has been conducted to determine drug concentrations, test protocols, specificity, sensitivity, and safety. For most drugs, there are no validated test procedures for diagnosing drug hypersensitivity, including test concentrations.
To reduce and eliminate adverse reactions, antihistamines and corticosteroids should be used.
The drug is not suitable for superficial anesthesia due to its poor ability to penetrate intact mucous membranes.
When performing local anesthesia, the toxicity of procaine is higher with the same total dose, the more concentrated the solution used. Therefore, with increasing solution concentration, it is recommended to reduce the total dose or dilute the drug solution to a lower concentration (sterile 0.9% sodium chloride solution).
The drug should be used with caution in patients with a history of severe allergies, in conditions accompanied by decreased hepatic blood flow, progression of cardiovascular failure (usually due to the development of heart block and shock), inflammatory diseases or infection of the injection site, pseudocholinesterase deficiency, renal failure, in elderly patients (over 65 years of age), seriously ill, debilitated patients, during pregnancy or breastfeeding, and during childbirth.
Use during pregnancy or breastfeeding
The use of the drug during pregnancy or breastfeeding is possible after a thorough assessment of the expected benefit of therapy for the mother and the potential risk to the fetus/child.
When used during childbirth, bradycardia, apnea, and seizures may develop in the newborn.
Ability to influence reaction speed when driving vehicles or other mechanisms
During the treatment period, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions, as adverse reactions from the nervous system may develop (dizziness, drowsiness - see the "Adverse Reactions" section).
Method of administration and doses
With local anesthesia, the dose of the drug depends on the concentration, nature of the surgical intervention, method of administration, condition and age of the patient.
In case of paranephral blockade, 50-70 ml of 0.5% or 100-150 ml of 0.25% novocaine solution should be injected into the perirenal tissue in adults.
For infiltration anesthesia, the following higher doses are established (for adults): the first single dose at the beginning of the operation is 0.75 g of 0.5% novocaine solution (i.e. 150 ml) or 1.25 g of 0.25% novocaine solution (i.e. 500 ml). Subsequently, during each hour of the operation, no more than 2 g of 0.5% novocaine solution (i.e. 400 ml) or no more than 2.5 g of 0.25% novocaine solution (i.e. 1000 ml).
Children.
Use by children is prohibited.
Overdose
In cases of overdose, the administration of the drug should be stopped immediately. When performing local anesthesia, the injection site can be pricked with adrenaline.
Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, increased nervous excitability, "cold" sweat, tachycardia, decrease in blood pressure almost to the point of collapse, tremor, convulsions, apnea, methemoglobinemia, respiratory depression, sudden cardiovascular collapse.
The effect on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, and motor agitation.
Treatment: general resuscitation measures, including oxygen inhalation, if necessary - artificial ventilation of the lungs. If convulsions last more than 15-20 seconds, they should be stopped by intravenous administration of thiopental (100-150 mg) or diazepam (5-20 mg). In case of arterial hypotension and/or myocardial depression, intravenous administration of ephedrine (15-30 mg), in severe cases - detoxification and symptomatic therapy.
In the event of intoxication after injection of novocaine into the leg or arm muscles, urgent application of a tourniquet is recommended to reduce further entry of the drug into the general circulation.
Side effects
The drug is usually well tolerated, but sometimes the following adverse reactions may develop.
From the sensory organs: visual and auditory disturbances, nystagmus.
From the nervous system: headache, dizziness, drowsiness, weakness, motor restlessness, loss of consciousness, convulsions, trismus, tremor, cauda equina syndrome (paralysis of the legs, paresthesias), paralysis of the respiratory muscles, motor and sensory block, return of pain, persistent anesthesia.
Cardiovascular system: increase or decrease in blood pressure, peripheral vasodilation, collapse, bradycardia, arrhythmias, chest pain.
From the urinary system: involuntary urination.
On the part of the digestive system: nausea, vomiting, involuntary defecation.
From the blood system: methemoglobinemia.
Immune system disorders: hypersensitivity reactions, including angioedema (including laryngeal edema), other anaphylactic reactions (including anaphylactic shock), urticaria (on the skin and mucous membranes).
Skin and subcutaneous tissue disorders: skin itching, rash, dermatitis, skin peeling, erythema, hyperemia.
General disorders: hypothermia, increased sweating.
Injection site reactions: when treating the injection site of the drug with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of soreness and swelling increases.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in a dark place, out of the reach of children.
Incompatibility
Do not use during treatment with sulfonamides.
Novocaine solution is compatible with 0.9% sodium chloride solution (see section "Special instructions for use").
Packaging
200 ml and 400 ml bottles.
Vacation category
According to the recipe.
Producer
Private Joint Stock Company "Infusion".
Address
Ukraine, 23219, Vinnytsia region, Vinnytsia district, village Vinnytskie Khutory, Nemyrivske highway st., bldg. 84A.
