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Lidocaine is a pharmacologically active compound with anesthetic and antiarrhythmic properties. According to its chemical structure it is a substituted amide of acetanilide. The compound is a white or whitish powder of small crystals, almost insoluble in water. Used in the form of hydrated salt of hydrochloric acid, which is easily soluble in water, which makes it possible to obtain solutions of various concentrations.
Pharmaceutical industry produces mainly solutions of 1%, 2%, 10% concentration, with stationary treatment, dilution is possible to lower concentrations (up to 0.125%).
Synonyms: Lidocainum, 2- (diethylamino) -N- (2,6-dimethylphenyl) acetamide, lidocaine hydrochloride
Chemical formula of compound (gross): C14H22N2O
Molar mass: 234.3 g / mol
It is used as a local anesthetic, antiarrhythmic, ophthalmic. Antiarrhythmic activity appears due to an increase in permeability of cell membranes for potassium ions and as a result due to suppression of foci of excitation in cardiac fibres.
Lidocaine stabilises neurons’ membranes, increasing the permeability threshold for sodium ions. With its help blocking of nerve impulses can be achieved, which carry pain signals to the brain. The drug takes its effect faster than many other drugs (one minute if it is administered intravenously, 15 minutes – if intramuscularly).
The compound disintegrates rapidly in tissues with slightly alkaline medium. Time of analgesic effect of the drug varies: it is 15 minutes and more after intravenous administration, and 60 minutes and more after intramuscular injection. Lidocaine is effective in all types of its use as an anesthetic due to rapid distribution to surrounding tissues.A decrease in anesthetic effect is observed upon inflammation of tissues that have been in contact with lidocaine. It dilates blood vessels, doesn’t cause irritation at the injection site. In a selection of local anesthetics (novocaine-lidocaine-bupivacaine) lidocaine’s effect is stronger and longer than that of novocaine, but several times shorter than that of a aimilar drug of bupivacaine.
In the gastrointestinal tract lidocaine is absorbed really quickly, but it is already absorbed in the liver, and a really small amount of the drug can get into blood. Lidocaine is actively absorbed in different mucous membranes, which allows to apply and produce it in the form of aerosol. Once the drug enters the body, it quickly penetrates the brain, lungs, heart, liver and spleen, and then spreads into tissues. In lactating women the drug can be found in milk. Upon drug’s application to the intact skin, the analgesic effect of the drug is also observed.
Limitations and contraindications:
Lidocaine has list of contraindications:
• Severe muscle weakness
• The presence of violations of the kidneys and liver
• Hypersensitivity to amide anesthetics
• Severe hypertension or hypotension
• Cardiogenic shock, myasthenia gravis
• Bradycardia (weakness of the sinus node)
• Elderly age
Possible side effects
From the nervous system:
• speech and vision disturbance
• numbness of the tongue and oral cavity
From the cardiovascular system (only with an overdose):
• Reduced blood pressure
• Reduced heart rate
• Itching, rash
• Anaphylactic shock
• Cold, fever
• Numbness of the limbs
• Light and short burning in the place of application of lidocaine
Usually side effects terminate after the end of the drug, but in some particularly severe cases, drug therapy or even artificial pulmonary ventilation is necessary.
The drug intake should be strictly limited, and the doses must be calculated for each patient individually. The methods of administration and prescribed doses vary from diseases: during arrhythmia, intramuscularly and intravenously, for surface anesthesia, treatment with a weak solution, lidocaine plates are used for local effect at intervals of 12 hours.
Store in a cool, protected from light place.
List B .: At a temperature of 15-25 ° C.
Lidocaine’s safety and efficacy depends upon the proper dosage, correct technique, adequate precautionary measures and readiness to emergency situations. Low dosage should be applied to achieve a result of effective analgesia, but at the same time to avoid high levels of plasma and serious adverse effects.