home All hormones Trimecaine in Latin. Trimekain. Mechanism of action, side effects, release forms. Special instructions and precautions

Trimecaine in Latin. Trimekain. Mechanism of action, side effects, release forms. Special instructions and precautions

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 nerve fiber sheath, 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 mucous membrane oral cavity, 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 ®

Included in the preparations

ATX:

N.01.B.B Amides

Pharmacodynamics:

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

Pharmacokinetics:Has not been studied for topical use. Indications: Superficial anesthesia of mucous membranes.

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

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 mucous membranes, 2-5% solutions are used topically: in ophthalmological practice- 4-8 drops, in otorhinolaryngology - 2-8 drops, it is possible to add a 0.1% epinephrine solution (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 with rapid absorption into 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

Trimecaine is a white or white with a yellow tint fine-crystalline powder. It dissolves well in alcohol and water.

pharmachologic effect

Local anesthetic, antiarrhythmic.

Pharmacodynamics and pharmacokinetics

Trimecaine is a highly lipophilic compound; it is able to penetrate the membrane of nerve fibers, bind to specific receptors and disrupt depolarization processes. Thus, the transmission of the nerve impulse along the fiber is blocked.

The substance also has antiarrhythmic activity due to its ability to stabilize the membranes of cardiomyocytes and slow down the sodium, slow ion current. In this case, the excretion of potassium is observed and the automatism of ectopic pacemakers is suppressed, the time of the action potential and the value of the effective refractory period are reduced.

Indications for use

Trimecaine is used for conduction, epidural, infiltration and spinal.

In cardiology, the drug is used:

during cardiac catheterization and other surgical interventions;
for elimination ventricular arrhythmia for acute;
at ventricular arrhythmias , which do not depend on the potassium content in the blood, and arose as a result of drug intoxication digitalis ;
for the treatment of ventricular.

Contraindications

The medicine is contraindicated for use:

Side effects

Trimecaine may cause the following adverse reactions:

decrease, ;
, tinnitus, feeling of restlessness;
numbness of the mucous membrane of the mouth and tongue, decreased visual acuity;
convulsions , ;
bradycardia , nausea ;
, other allergic reactions, ;
pale face and weakness.

Instructions for use of Trimecaine (Method and dosage)

Depending on the indications, type of anesthesia or arrhythmias , the dosage regimen is determined individually.

Trimecaine as a drug for superficial anesthesia used in a concentration of 2-5%. At infiltration anesthesia – 0.1-.5% solution in different dosage(determined by the doctor). For conduction anesthesia use 1-2% solution, from 20 ml to 0.1 l. Spinal anesthesia carried out with 5% solution, 2 or 3 ml.

At cardiac arrhythmia Trimecaine preparations are administered slowly, at a rate of no more than 2 mg per minute at a dosage of 80-120 mg. 2% solution is used.

Overdose

There is no information about overdose.

Interaction

Trimecaine is often found in medicines in combination with . This leads to local vasoconstriction, which reduces the rate of absorption of Trimecaine into the systemic circulation and prolongs its analgesic effect.

Combined use of the substance with vasoconstrictors causes prolongation and intensification of the effect of the drug.

Terms of sale

Need a recipe.

special instructions

When using Trimecaine, a number of restrictions on use should be taken into account:
cannot be combined with vasoconstrictors with high blood pressure, with peripheral vascular diseases;
it is impossible to anesthetize the tissues supplied terminal arteries(phalanxes of fingers, penis, etc.).

Analogs (generics, synonyms)

Mesocaine, Trimecaine hydrochloride, Mesdicaine, Mezidicaine

Recipe (international)

Rp.: Sol. Trimekaini 5% 2 ml
D.t. d. N. 6 in ampull.
S. Administer 2-3 ml of solution during spinal anesthesia.

Rp.: Sol. Trimecaini hydrochloridi 2% - 5 ml
D.t.d. No. 6 in ampull.
S. For regional anesthesia

pharmachologic effect

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, ventricular extrasystole in patients with acute myocardial infarction, it is less effective than lidocaine.

Mode of application

For adults: 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, 80-120 mg of a 2% solution is administered intravenously at a rate of 2 mg/min.
In case of renal and liver failure, due to the danger of accumulation, the dose is reduced.

Indications

Conduction (pain relief by applying an anesthetic to the area of the nerve trunk innervating the surgical field or painful area) or infiltration (pain relief by soaking the tissue surgical field local anesthetic solution) anesthesia.

Contraindications

Hypersensitivity, SSSU, severe sinus bradycardia, AV block, cardiogenic shock. With caution. Liver failure, chronic renal failure, heart failure.

Side effects

From the side of the central nervous system: headache, dizziness.

Allergic reactions: urticaria, anaphylactic shock.

Other: pale skin, nausea.

Release form

ATTENTION!

The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to provide healthcare workers with additional information about certain medications, thereby increasing their level of professionalism. Use of the drug " Trimekain“mandatorily requires consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.

Clinical and pharmacological groups

29.011 (Drug with antimicrobial and local anesthetic action for external and local application)
29.006 (A drug with antibacterial, local anesthetic and tissue regeneration-improving effects for external use)
27.008 (Drug with anti-inflammatory, astringent, drying and local anesthetic effect for local use in proctology)
01.057 (Local anesthetic. Antiarrhythmic drug. Class I B)

pharmachologic effect

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. It has a more intense and long-lasting effect than procaine. 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, for 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.

Dosage

Individual, depending on the type of anesthesia and indications.

Drug interactions

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.

Use during pregnancy and lactation

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

Side effects

From the side of the central nervous system: headache, dizziness.

Allergic reactions: urticaria, anaphylactic shock.

Other: pale skin, nausea.

Indications

Conduction, infiltration, epidural and spinal anesthesia.

Ventricular arrhythmias with acute heart attack myocardium, ventricular arrhythmias(independent of the concentration of potassium in the blood) in case of intoxication with digitalis preparations, ventricular tachycardia, arrhythmias during surgical interventions and cardiac catheterization.

Contraindications

Increased sensitivity to trimecaine.

special instructions

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).

Preparations containing TRIMECAINE

. SIMETRIDE® ◊ rectal suppositories: 10 pcs.

. DIOXYSOL solution for local and external use. approx. 12 mg+60 mg/1 g: vial. 50 g
. TRIMECAINE solution for injection. 2% (100 mg/5 ml): amp. 10 pieces.
. TRIMECAINE solution for injection. 2% (40 mg/2 ml): amp. 10 pieces.
. TRIMECAINE solution for injection. 2% (200 mg/10 ml): amp. 10 pieces.
. DIOXYSOL aerosol for local and external use. approx. 12 mg+60 mg/1 g: 30 g or 60 g cylinders
. TRIMECAINE solution for injection. 2% (20 mg/1 ml): amp. 10 pieces.
. LEVOSIN® ◊ ointment for external use. note: tube 40 g, cans 50 g or 100 g
. TRIMECAINE solution for injection. 2% (40 mg/2 ml): amp. 10 pieces.