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PHARMACOLOGICAL PROPERTIES AND REGISTERED FORMS OF
LIDOCAINE IN UZBEKISTAN
Obidova Ruxsorabonu Olimjon kizi
Central Asian Medical University, Department of Chemistry and Pharmacology, Assistant
INTRODUCTION
Lidocaine (Lidocaine) is a local anesthetic agent of amide type, widely used in medical
practice for local, regional and conduction anesthesia, as well as for the treatment of
ventricular arrhythmias. A wide range of lidocaine-based drugs including different dosage
forms, manufacturers and pharmacological characteristics are registered in Uzbekistan. The
aim of this article is to analyze the pharmacological properties and registered forms of
lidocaine in Uzbekistan.
METHODS.
Data from the State Register of Medicinal Products including tables of registered
preparations containing lidocaine were used for analysis. Pharmacologic information was
compiled from official instructions and annotated reference books.
RESULTS
More than 20 names of medicinal products containing lidocaine are registered in Uzbekistan.
The most common form of release are solutions for injection with concentration of 1% and
2%, produced in glass and polyethylene ampoules. Eye drops, aerosols, sprays and patches
are also registered. The manufacturers are both local (Radiks, LLC; Merrymed Farm, LLC;
Uzgermed Pharm, JV LLC, etc.) and foreign companies from China, India, Armenia,
Hungary, Belarus, Russia and other countries.
All preparations are classified in the pharmacotherapeutic group 'Local anesthetic agent' and
are dispensed by prescription. Main ATX codes: C01BB01, N01BB02, S01HA07.
Pharmacologically, lidocaine is characterized by rapid onset of action (1 min when
administered intravenously), medium duration (up to 90 minutes) and effective blockade of
sodium channels, providing reversible local anesthesia.
All drugs are available by prescription.
The drugs cover local and foreign manufacturers from Uzbekistan, China, India, Armenia,
Belarus, Hungary, Russia, Italy, Georgia and Moldova.
Dosage Form
Concentrations Packaging
Manufacturers
Injection solutions 1%, 2%
Ampoules (5, 10, 25, 50 Radiks,
MerryMed,
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Dosage Form
Concentrations Packaging
Manufacturers
pcs), glass/plastic
Mediofarm, etc.
Eye drops
4%, 0.5 ml
Dropper bottles
Jurabek Laboratories, Alfa
Intes
Sprays
and
aerosols
5%, 10%
Bottles with mechanical
sprayer
Egis, Arpimed, Flumed-
Pharm
Patches
3.6%
Patch packages
Rusan Pharma (India)
Solutions for local
application
—
Ampoules,
aerosols,
bottles
Various manufacturers
Table 1.
Registered forms of lidocaine in Uzbekistan
The pharmacological action of lidocaine lies in its ability to block sodium channels located
in the membrane of neurons, thereby reducing its permeability to sodium ions. Lidocaine
also has a pronounced antiarrhythmic effect and belongs to class 1B according to the
classification of antiarrhythmics, reducing automaticity and excitability of the heart muscle
by shortening the action potential, especially in ischemic areas of myocardium. The drug is
characterized by a rapid onset of action: approximately 1 minute after intravenous
administration and 10-15 minutes after intramuscular administration. Duration of its effect
varies from 20 minutes (intravenous/m) to 60-90 minutes (intravenous). Due to its high
lipophilicity, it is rapidly distributed in div tissues, providing a stable and predictable
clinical effect.
Pharmacokinetics of lidocaine depends on the route of administration: the highest absorption
is noted at intercostal blockade, lower - at epidural and subcutaneous administration. The
drug is intensively metabolized in the liver - about 90% of the dose with the formation of
metabolites (monoethylglycinexylidide, glycinexylidide), which may accumulate in case of
liver and kidney dysfunction. Excreted predominantly with urine, less than 10% is
unchanged. Half-life (T½) - on average 1.5-2 hours, in case of prolonged infusion may reach
3 hours. Maximum dose for adults - up to 300 mg, in children and elderly patients - reduced.
Side effects are possible in the heart (bradycardia, hypotension, cardiac arrest), CNS
(convulsions, tremor), respiration (bronchospasm, respiratory depression), immune system
(rash, anaphylaxis), vision (double vision, blurred vision). Contraindications include
hypersensitivity, severe cardiac conduction disorders, shock, age under 1 year (1% solution)
and under 18 years (2% solution), infections at the injection site. In pregnancy it is allowed
to use by indications, especially with caution in the III trimester. With prolonged use
requires monitoring of liver and kidney function. Caution is required in combination with
antiarrhythmics, opioids, sedatives and anticoagulants.
DISCUSSION
Analysis of drugs registered in Uzbekistan has shown that 23 names of drugs containing the
active substance lidocaine are present in the national pharmaceutical market. About 70% of
them (16 preparations) are presented in the form of solution for injection with concentration
of 1% or 2%, which confirms their dominant use in clinical practice for infiltration,
conduction and regional anesthesia. Three preparations (13%) are available in the form of
sprays or aerosols, which is convenient for outpatient anesthesia of mucous membranes and
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skin. There are also eye drops (2 preparations) and one preparation in the form of a
transdermal patch, which indicates the expansion of the range of lidocaine use beyond the
traditional injectable form. The manufacturers are both local pharmaceutical companies
(about 50%), such as Radiks, Merrymed Farm, Jurabek Laboratories, and foreign
manufacturers from Hungary, China, India, Armenia and other countries, which indicates a
wide international representation and high demand for this active substance.
Pharmacological characteristics of lidocaine - rapid onset of action (1 min for IV, 10-15 min
for IM), duration up to 90 minutes - make it an optimal choice for short-term anesthesia. At
the same time, its T½ is about 3 hours, and less than 10% of the substance is excreted
unchanged, which requires caution when administering to patients with hepatic and renal
dysfunction. The maximum recommended dose is 300 mg in adults and should be reduced in
children and elderly patients. Side effects from the cardiovascular, nervous and respiratory
systems, including bradycardia, seizures, bronchospasm, have been reported, which requires
anesthesia to be administered only by experienced professionals.
CONCLUSIONS.
Thus, lidocaine remains one of the most versatile and sought-after drugs in anesthesiology
and urgent care. Its widespread use is confirmed by the variety of registered forms of release
in Uzbekistan, half of which are produced by domestic companies, which ensures stable
availability of the drug. Due to the combination of high efficacy, rapid action and acceptable
safety profile, lidocaine occupies an important place in the list of essential drugs. However,
its use requires an individualized approach to dosage, assessment of the risks of side effects
and strict medical control, especially when used in vulnerable categories of patients -
children, the elderly, pregnant women and people with chronic liver and kidney diseases.
LITERATURE
1.
State Register of Medicines of the Republic of Uzbekistan. [Online resource] – URL:
2.
Goodman & Gilman's: The Pharmacological Basis of Therapeutics. 13th ed. – New
York: McGraw-Hill, 2018. – 1632 p.
3.
Brunton L.L., Hilal-Dandan R., Knollmann B.C. Goodman & Gilman's Manual of
Pharmacology and Therapeutics. – McGraw-Hill Education, 2021. – 1264 p.
4.
British National Formulary (BNF) 85. – BMJ Publishing Group and Royal
Pharmaceutical Society, 2023.
5.
DrugBank Online. Lidocaine – https://go.drugbank.com/drugs/DB00281
