Novocaine injection 0.5% 5ml N10
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Active ingredients
Procaine
Release form
Solution
Composition
1 ml of betaxolol hydrochloride 5.6 mg, which corresponds to the content of betaxolol 5 mg. Excipients: benzalkonium chloride - 0.1 mg, sodium chloride - 5.49 mg, disodium phosphate dihydrate - 3.579 mg, disodium edetate (Trilon B) - 0.5 mg, sodium dihydrogen phosphate dihydrate - 3.165 mg, water d / and - up to 1 ml.
Pharmacological effect
Local anesthetic with moderate anesthetic activity and a wide breadth of therapeutic action. Being a weak base, it blocks sodium channels, interferes with the generation of impulses in the terminations of sensory nerves and the conduction of impulses along the nerve fibers. Changes the action potential in the membranes of nerve cells without a pronounced effect on the resting potential. Suppresses the holding of not only pain, but also pulses of another modality. With absorption and direct vascular injection into the blood stream, it reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (it has some ganglion-blocking action), eliminates smooth muscle spasm, reduces the excitability of the myocardium and motor cortex. Eliminates the downward inhibitory effects of the reticular formation of the brain stem. Inhibits polysinantic reflexes. In large doses, it can cause convulsions. It has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h).
Pharmacokinetics
Subject to complete systemic absorption. The degree of absorption depends on the place and route of administration (especially on vascularization and blood flow velocity in the area of administration) and the bovine dose (amount and concentration). It is rapidly hydrolyzed by plasma and liver esterases to form two main pharmacologically active metabolites: diethylaminoethanol (it has a moderate vasodilating effect) and para-aminobenzoic acid (it is a competitive antagonist of sulfanilamide chemotherapeutic drugs and can weaken their antimicrobial effect). The half-life of the drug - 30-50 s, in the neonatal period - 54-114 s. It is excreted mainly by the kidneys as metabolites, not more than 2% is excreted unchanged.
Indications
infiltration (including intraosseous) anesthesia; vagosympathetic cervical, perirephral, circular and paravertebral blockade,
Contraindications
Hypersensitivity (including para-aminobenzoic acid and other local anesthetics); children up to 12 years; pronounced fibrous changes in tissues Use during pregnancy and during breastfeeding During pregnancy and during breastfeeding, safety and efficacy and the drug has not been established. The use of the drug during pregnancy and during breastfeeding is possible only but prescribed by a doctor if the intended benefit to the mother outweighs the potential risk to the fetus or child.
Precautionary measures
With care the Emergency operations which are followed by an acute blood loss; conditions accompanied by a decrease in hepatic blood flow (for example, in chronic heart failure, liver disease); the progression of cardiovascular failure (usually due to the development of heart block and current); inflammatory diseases or infection of the injection site; pseudocholinesterase deficiency; renal failure; children's age (from 12 to 18 years); elderly patients (over 65 years old); debilitated patients.
Dosage and administration
For infiltration anesthesia, 0.25% and 0.5% solutions are used; for anesthesia according to the Vishnevsky method (tight creeping infiltration) - 0.125% and 0.25% solutions. To reduce the absorption and lengthen the action under local anesthesia, a 0.1% solution of epinephrine is additionally injected - 1 drop per 2-5-10 ml of procaine solution. In case of perirenal blockade (according to A. V. Vishnevsky), 50-80 ml of a 0.5% solution or 100-150 ml of 0.25% is injected into the peri-renal cellulose tissue, and 30 to 100 ml of a 0.25% solution in the vagosympathetic blockade. For circulatory or paravertebral blockade, a 0.25% or 0.5% solution is intradermally injected. Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation is no more than 500 ml of a 0.25% solution and 150 ml of a 0.5% solution. The maximum dose for use in children over 12 years old is 15 mg / kg.
Side effects
From the central and peripheral systems: headache, dizziness, drowsiness, weakness, trisism, tremor, nystagmus, persistent anesthesia, motor restlessness, loss of consciousness, convulsions, visual and auditory disturbances.Since the cardiovascular system: increase or decrease in blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, changes in the spread of excitation in the heart, which manifest on the ECG in the form of a flat E wave or shortening of the ST segment. On the part of the respiratory system: spasms of the respiratory tract or difficulty breathing. On the part of the urinary system: involuntary urination. On the part of the digestive system: nausea, vomiting. Cp of the side of blood: methemoglobinemia. Allergic reactions: allergic reactions, up to anaphylactic shock. Other: return of pain, persistent anesthesia, hypothermia, tremor, swelling of the lips. face, mouth, tongue throat.
Overdose
When used in high doses, excessive absorption is possible. symptoms: pallor of the skin and mucous membranes, dizziness, nausea. vomiting, “cold” sweat, increased breathing, tachycardia, lowering blood pressure until collapse, apnea, methemoglobinemia. The effect on the neutral nervous system is manifested by a sense of fear, hallucinations, convulsions, motor agitation. Treatment: maintaining adequate pulmonary ventilation, detoxification symptomatic therapy.
Interaction with other drugs
Strengthens the inhibitory effect on the central nervous system of general anesthetic drugs, hypnotics and sedatives, narcotic analgesics and tranquilizers. Anticoagulants (ardeparin sodium, dalteparin sodium, danaparoid sodium, enoxaparin atrium, heparin, warfarin) increase the risk of bleeding, while processing the local anesthetic injection site with disinfectant solutions containing heavy metals, increases the risk of local reaction in the form of pain and swelling. Simultaneous use with monoamine oxidase inhibitors (furazolidone, and eokarbazin, selegilin) increases the risk of hypotension. Strengthen and lengthen the action of muscle relaxants. When using procaine together with narcotic analgesics, an additive effect is noted, which is used during spinal and epidural anesthesia, while respiratory depression is enhanced. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect.Procaine reduces the anti-myasthenic effect of drugs, especially when used in high doses, which requires an additional correction for the treatment of myasthenia. Cholinestease inhibitors the risk of developing a sharp decrease in blood pressure and bradycardia.
special instructions
Anesthesia should be carried out by experienced specialists in a properly equipped room with the availability of ready for immediate use equipment and preparations necessary for cardiomonitoring and resuscitation. To prevent accidental intravascular injection, it is recommended to conduct an aspiration test (in two stages). Patients are required to monitor the functions of the cardiovascular, respiratory and central nervous systems. The use of monoamine oxidase inhibitors at least 10 days prior to the administration of a local anesthetic is contraindicated. Before use, mandatory testing of individual sensitivity to the drug. It should be borne in mind that when carrying out local anesthesia when applying the same total dose, the toxicity of procaine is the higher, the more concentrated the solution is used. The drug should be stored in the secondary packaging.