Trimecaine: instructions for use. Instructions for use Special instructions and precautions

Included in the preparations

ATX:

N.01.B.B Amides

Pharmacodynamics:

Local anesthetic. Blockade of the initiation and conduction of nerve impulses: a decrease in the permeability of neuronal cell membranes for Na + ions, probably through attachment to sodium channels, and an increase in permeability for K +, which reversibly stabilizes the cell membrane and inhibits its depolarization, disrupts the propagation of the action potential and leads to conduction blockade .

Pharmacokinetics:At local application not studied. Indications: Superficial anesthesia of mucous membranes.

XXI.Z40-Z54.Z51.4 Preparatory procedures for subsequent treatment, not classified elsewhere

Contraindications:

Hypersensitivity, including to other amide local anesthetics.

Carefully:Hypersensitivity. Pregnancy and lactation:

Adequate and well-controlled studies in humans and animals have not been conducted. Use during pregnancy and lactation is not recommended ( breastfeeding).

Directions for use and dosage:For superficial anesthesia of the mucous membranes, 2-5% solutions are used locally: in ophthalmological practice - 4-8 drops, in otorhinolaryngology - 2-8 drops, it is possible to add a 0.1% solution of epinephrine (1 drop per 2 ml of trimecaine solution) . Side effects:

Possibly: skin allergic reactions; at intravenous administration- short-term fainting.

Overdose:

Apnea, collapse (low blood pressure, low or irregular pulse, pallor, sweating, possible cardiac arrest), methemoglobinemia, central neurotoxicity (double vision, confusion, convulsions, dizziness, ringing or buzzing in the ears, trembling, irritability, agitation, nervousness ; possible stimulation and then depression of the central nervous system, as well as loss of consciousness and respiratory arrest).

Interaction:

Antimyasthenic drugs - local anesthetics, especially when rapidly absorbed in large quantities, inhibit the transmission of nerve impulses, acting as antagonists of the action of antimyasthenic drugs on skeletal muscles. Adequate control of myasthenia gravis may require temporary dosage adjustments of antimyasthenic medications.

Neuromuscular transmission blockers - local anesthetics, especially when rapidly absorbed in large quantities, inhibit the transmission of nerve impulses, which prolongs the effect of neuromuscular transmission blockers.

Vasoconstrictors (methoxamine, ) - it is not recommended to combine methoxamine and local anesthetics, since the effect of both drugs is prolonged, and long-term exposure to methoxamine is accompanied by inhibition of circulation and desquamation of the skin. When combining trimecaine with other vasoconstrictors, it is necessary to carefully observe the proportions, especially when anesthetizing areas of peripheral arteries (fingers, nose, penis), where disturbances in the blood supply to tissues, including gangrene, are more likely.

Patients receiving ganglion-blocking antihypertensive agents (guanagrel, guanethidine, mecamylamine, trimethaphan) may develop severe hypotension and/or bradycardia when receiving spinal or epidural anesthesia with trimecaine at levels sufficient to produce sympathetic blockade.

special instructions:

The effectiveness and safety of local anesthetics depends on the accuracy of their dosage and compliance with the administration technique. Local anesthetics should be administered by specialists experienced in diagnosis and treatment adverse reactions, violations heart rate and conductivity and others acute conditions. It is necessary to have equipment and medications to relieve severe toxic reactions.

Instructions

Local anesthetic. Causes a rapid onset of long conduction, infiltration, epidural, spinal anesthesia. The mechanism of action is due to the stabilization of neuronal membranes and the prevention of the occurrence and conduction of a nerve impulse. It has a more intense and long-lasting effect than procaine (novocaine). Low toxicity, does not cause local tissue irritation. It has an antiarrhythmic effect and belongs to class IB.

Experimental studies have shown that its antiarrhythmic effect is 1.5 times stronger than that of lidocaine. However, when ventricular extrasystole in patients with acute myocardial infarction, it is less effective than lidocaine.

Pharmacokinetics

With intravenous administration, T1/2 in the α-phase is about 8.3 minutes, in the β-phase - about 168 minutes.

Indications

Local anesthesia - superficial, infiltration, conduction and spinal; ventricular arrhythmias during acute myocardial infarction, ventricular arrhythmias (independent of the concentration of potassium in the blood) during intoxication with digitalis preparations, ventricular tachycardia, arrhythmias with surgical interventions and cardiac catheterization.

Contraindications

Hypersensitivity, sinus node weakness, AV block, severe bradycardia, cardiogenic shock, liver pathology.

Directions for use and doses

For superficial anesthesia, a 2-5% solution is used, for infiltration - 0.125-0.25-0.5% solution in an amount of up to 1500-800-400 ml, respectively;

• with conduction - 1-2% solution in an amount of 100-20 ml;
• spinal - 5% solution in an amount of 2-3 ml.

To stop rhythm disturbances, 80-120 mg is administered in the form of a 2% solution at a rate of 2 mg/min.

Side effect

Hypotension, headache, dizziness, drowsiness, anxiety, tinnitus, numbness of the tongue and mucous membrane oral cavity, blurred vision, convulsive twitching, tremor, bradycardia.

Special instructions and precautions

Trimecaine (like other local anesthetics) in combination with vasoconstrictors is not used in patients with arterial hypertension, diseases of peripheral vessels, as well as for anesthesia of tissues supplied by terminal arteries (terminal phalanges, penis).

Use during pregnancy and breastfeeding

The safety of trimecaine during pregnancy and lactation (breastfeeding) has not been established.

Interaction with other drugs

Norepinephrine, which is often used in combination with trimecaine, causes local vasoconstriction, which leads to a slowdown in the absorption of trimecaine, enhancing and prolonging its anesthetic effect and reducing the systemic effect.

Pharmacodynamics: Local anesthetic. Causes fast-onset long-term conduction, infiltration, epidural, spinal anesthesia. The mechanism of action is due to the stabilization of neuronal membranes and the prevention of the occurrence and conduction of a nerve impulse. Lasts longer than .

It has an antiarrhythmic effect and belongs to class IB. Antiarrhythmic effect 1.5 times stronger than lidocaine.

Mechanism of action

Mechanism of action: The mechanism of the local anesthetic effect is to stabilize the neuronal membrane, reducing its permeability to sodium ions, which prevents the occurrence of action potentials and the conduction of impulses.

Antagonism with calcium ions is possible. It hydrolyzes quickly in a slightly alkaline tissue environment and, after a short latent period, acts for 60–90 minutes. With inflammation (tissue acidosis), anesthetic activity decreases. Effective for all types of local anesthesia. Dilates blood vessels. Does not irritate fabrics.

Toxicity

Toxicity: Low

Side effects

Side effect:

• A sharp decrease in blood pressure,
• collapse,
• dizziness,
• drowsiness,
• anxiety,
• noise in ears,
• numbness of the tongue and oral mucosa,
• convulsive twitching,
• tremor,
• bradycardia.

Release forms

Release forms: Solutions for injections in ampoules (0.25% - 10 ml, 0.5% - 2.5 and 10 ml; 1 and 2% - 1, 2, 5, 10 ml; 5% - 1 and 2 ml).

Trimecaine recipe example

Rp.: Sol. Trimekaini 5% 2 ml

D.t. d. N. 6 in ampull.

S. Administer 2-3 ml of solution during spinal anesthesia.

Gross formula

C15H24N2O

Pharmacological group of the substance Trimecaine

Nosological classification (ICD-10)

CAS code

616-68-2

Characteristics of the substance Trimecain

White or white with a yellowish tint crystalline powder. Soluble in water and alcohol.

Pharmacology

pharmachologic effect- local anesthetic, antiarrhythmic.

Possessing sufficient lipophilicity, it penetrates the membrane nerve fiber, binds to receptors and disrupts depolarization processes, blocking the conduction of a nerve impulse. It has antiarrhythmic activity due to the stabilization of cardiomyocyte membranes and inhibition of the “slow” sodium current. Promotes the release of potassium, suppresses the automaticity of ectopic pacemakers, shortens the duration of the action potential and the effective refractory period.

Use of the substance Trimecain

Local anesthesia - superficial, infiltration, conduction and spinal; ventricular extrasystoles, tachycardia.

Contraindications

Hypersensitivity, sinus node weakness, AV block, severe bradycardia, cardiogenic shock, liver pathology.

Side effects of the substance Trimecain

Hypotension, headache, dizziness, drowsiness, anxiety, tinnitus, numbness of the tongue and oral mucosa, blurred vision, convulsive twitching, tremor, bradycardia.

Interaction

Vasoconstrictors enhance and prolong the effect.

Routes of administration

Parenterally.

Interactions with other active ingredients

Trade names

Name	The value of the Vyshkowski Index ®

Trimekain

Trimecaine:: Dosage form

injection

Trimecaine:: Pharmacological action

Local anesthetic, has an antiarrhythmic effect. Causes quickly onset long-lasting superficial, conduction, infiltration, epidural and spinal anesthesia. Possessing sufficient lipophilicity, it penetrates the nerve fiber sheath, binds to receptors and disrupts depolarization processes. Provides more intense and long action than procaine. Does not cause local tissue irritation and is relatively low-toxic. According to the classification of antiarrhythmic drugs, it belongs to class Ib. Antiarrhythmic activity is due to the stabilization of cardiomyocyte membranes and inhibition of the “slow” sodium current. Promotes the release of K+, suppresses the automaticity of ectopic pacemakers, shortens the duration of the action potential and the effective refractory period. The antiarrhythmic effect of trimecaine is 1.5 times stronger than that of lidocaine, however, in case of ventricular extrasystole in patients with acute myocardial infarction, it is less effective than lidocaine.

Trimecaine:: Indications

Superficial, infiltration, conduction, epidural and spinal anesthesia; ventricular extrasystole, paroxysmal ventricular tachycardia, incl. for intoxication with cardiac glycosides, arrhythmias during surgical interventions and cardiac catheterization.

Trimecaine:: Contraindications

Hypersensitivity, SSSS, severe sinus bradycardia, AV block, cardiogenic shock. Caution. Liver failure, chronic renal failure, heart failure.

Trimecaine:: Side effects

Headache, dizziness, drowsiness, anxiety, tinnitus, numbness of the tongue and oral mucosa, blurred vision, muscle twitching, clonic convulsions, tremor, nausea, vomiting, pallor skin and mucous membranes, decreased blood pressure, bradycardia, allergic reactions (urticaria, anaphylactic shock).

Trimecaine:: Method of administration and dosage

For conduction anesthesia - from 20 to 100 ml of 1-2% solution, for spinal anesthesia - 2-3 ml of 5% solution, for surface anesthesia - 2-5% solutions; for infiltration - 0.125-0.25-0.5% solution in amounts up to 1500-800-400 ml, respectively; for epidural anesthesia - 1%, 2% solution (add epinephrine hydrochloride 5-8 drops per 20-25 ml of trimecaine solution), administered fractionally: 1% solution - first in a dose of 5 ml, then 10-50 ml, 2% solution - up to 20-25 ml. To relieve rhythm disturbances - intravenous drip, 80-120 mg of a 2% solution at a rate of 2 mg/min. For renal and liver failure Due to the danger of accumulation, doses are reduced.

Trimekain:: Special instructions

Trimecaine (like other local anesthetics) in combination with vasoconstrictors is not used in patients with arterial hypertension, peripheral vascular diseases, or for anesthesia of tissues supplied by terminal arteries (terminal phalanges, penis). With the development of clonic convulsions, the administration of trimecaine is stopped and, if necessary, vasoconstrictors and analeptic drugs, oxygen are prescribed, and in case of severe convulsions, muscle relaxants and mechanical ventilation are prescribed. The safety of trimecaine during pregnancy and lactation has not been established.

Trimecaine:: Interaction

Vasoconstrictors, incl. norepinephrine, enhance and prolong the effect, reduce the systemic effect.