Riedelat-C - instructions for use, doses, side effects, contraindications

Nondepolarizing muscle relaxant of peripheral action. Reducing the sensitivity of n-holinoretseptorov skeletal muscles to acetylcholine, blocks neuromuscular transmission, causes a temporary relaxation of skeletal muscles (including respiratory). It has a rapid onset of action (within 2-2.5 minutes), which allows intubation of the trachea in the first 90 seconds from the moment of its administration in doses of 0.5-0.6 mg / kg.

In doses 0,2-0,6 mg / kg causes the predicted, proportional to the amount of the administered dose, the relaxation of skeletal muscles of duration 20-35 min. The rate of recovery of the neuromuscular transmission after the administration of atracurium bezylate (single and repeated) is constant, which allows the administration of repeated doses at predetermined time intervals. Restoration of normal neuromuscular transmission without the use of cholinesterase inhibitors - through 35 min, does not depend on the value of the total dose and the function of the excretory and metabolism organs. Promotes the release of histamine.

The clinical duration of action after intravenous administration (the period of spontaneous recovery of 25% contractility of skeletal muscles) is 35-45 min, the total duration (the period of spontaneous recovery of 90% contractile capacity of skeletal muscles) is 60-70 min.

Pharmacokinetics:

The connection with plasma proteins is high. Time to reach the maximum concentration in the blood plasma (TCmah) - 1.7-10 minutes (on average 3-5 minutes). The duration of neuromuscular blocking action does not depend on the intensity of hepatic metabolism and the rate of excretion by the kidneys.At physiological values, the pH of the blood and body temperature without the participation of enzymes decays (Hoffman's elimination) into laudanosine and quaternary monoacrylate; in a small degree hydrolyzed by butyrylcholinesterase, therefore the duration of action does not depend on the function of the liver and kidneys. Metabolites are pharmacologically inactive. Physiological changes in blood pH have little effect on the duration of action. Under hypothermia (body temperature 25-26 ° C), the rate of inactivation decreases. Do not cumulate. Do not penetrate the placental barrier at clinically significant concentrations. The half-distribution period is 2-3.4 min. The half-life (T1 / 2) is 20 min. It is excreted by the kidneys and intestines (less than 10% - unchanged).

Indications:

- for maintenance of myoplegia and intubation of the trachea and artificial ventilation (IVL) during surgical operations;

- for carrying out ventilation in intensive care units.

Contraindications:

- High sensitivity to the drug (or its components) and to histamine (see, "Interaction with other drugs", "Special instructions");

- newborns and children under 1 month, (more sensitive to the effects of nondepolarizing muscle relaxants, doses for children under 1 month are not established).

Carefully:

- cancer of the bronchi;

- violation of the function of the respiratory system (including respiratory depression);

- dehydration;

- severe disturbances of acid-base balance (KChR);

- arterial hypotension;

- hypothermia;

- myasthenia gravis gravis;

- pregnancy, lactation (see the section "Application in pregnancy and lactation").

Pregnancy and lactation:

Ridelat®-C should not be used during pregnancy if the potential benefit to the mother does not exceed the possible risk to the fetus.

Ridelat®-C can be used for the purpose of miorelaxation in a caesarean section, since when administered at the recommended dose range, it penetrates the placenta in small amounts.

Penetrating through the placenta in small amounts, does not cause side effects in newborns, so it can be used during caesarean section (always bear in mind the potential for respiratory depression and decreased muscle activity in newborns).

There are no data on the penetration of the drug into breast milk.

Dosing and Administration:

Intravenously (intravenously).

Adults

The doses of Ridelat®-C are set individually and depend on the necessary duration and depth of the neuromuscular blockade.

Bolus injection

Recommended doses for adults are 0.3-0.6 mg / kg (depending on the required duration of neuromuscular blockade), which provide adequate myoplegia for 15-35 minutes.

Intubation of the trachea can be performed within 90 seconds after intravenous administration of Ridelat®-C in a dose of 0.5-0.6 mg / kg.

The duration of complete neuromuscular blockade can be increased by the addition of additional doses of Ridelat®-C at a rate of 0.1-0.2 mg / kg, which is not accompanied by a cumulation of the drug.

Neuromuscular conduction can be rapidly restored under the influence of cholinesterase inhibitors (neostigmine methylsulfate and eudrophonia chloride) in combination with atropine (without the appearance of signs of recurrence).

Infusion introduction

After initial bolus administration of Ridelat®-C at a dose of 0.3-0.6 mg / kg, it can be administered by continuous infusion at a rate of 0.3-0.6 mg / kg / hr to maintain neuromuscular blockade during prolonged surgical operations.This method of administration of Ridelat®-C can be recommended for operations on the lungs and heart.

With artificial hypothermia, to maintain complete myoplegia, the infusion rate should be reduced approximately 2-fold.

Children

The dose in children 1-24 months - 0,3-0,4 mg / kg; Children older than one year of Ridelat®-S are given in the same doses as adults, in terms of body weight. Doses for children younger than 1 month are not established (see the section "Contraindications").

Elderly people

Elderly patients of Ridelat®-C are prescribed in standard doses, however, it is preferable to use the lower level of the recommended dose range and administer the drug slowly.

Application for violations of the liver or kidney function

If the liver and / or kidney function is impaired, including at the terminal stage of hepatic or renal failure, Ridelat®-C is administered in standard doses.

Application for diseases of the cardiovascular system

In patients with severe cardiovascular disease, the initial dose of Ridelat-C should be administered for at least 60 seconds.

Application in intensive care units

To maintain myoplegia after initial bolus administration at a dose of 0.3-0.6 mg / kg, Ridelat®-C can be administered by continuous infusion at a rate of 11-13 μg / kg / min (0.65-0.78 mg / kg / hour).In different patients, the dose is not the same and may change over time. Some patients may require such low dose as 4.5 μg / kg / min (0.27 mg / kg / h), and such high doses as 29.5 μg / kg / min (1.77 mg / kg / h). Spontaneous recovery of neuromuscular conduction usually occurs approximately 60 minutes after the infusion of Ridelat®-C and its rate does not depend on the duration of administration of the drug.

Instruction for breeding

Ridelat®-C is compatible with the following infusion solutions.

Infusion solutions	Stability period
Sodium chloride solution for intravenous infusions (0.9%)	24 hours
Dextrose solution for intravenous infusion (5%)	8 ocloc'k
Ringer's injection solution	8 ocloc'k
A solution of sodium chloride (0.18%) and dextrose (4%) for intravenous infusions	8 ocloc'k
Hartmann Solution for Injection	4 hours

The solution of Ridelat®-C when diluted with compatible infusion solutions until atraquarium besylate concentration is not less than 0.5 mg / ml remains stable for a specified period of time under normal illumination at temperatures up to 30 ° C.

Side effects:

From the cardiovascular system: decrease or increase in blood pressure (BP), moderate tachycardia; arrhythmia.

Allergic reactions: bronchospasm, laryngospasm, edema, erythema, skin rash, hives, itchy skin, anaphylactoid reactions.

Other: increased intraocular pressure, drooling, rhabdomyolysis, manifested by myoglobinemia and myoglobinuria (may, especially in children, lead to the development of acute renal failure), malignant hyperthermia; convulsions.

Local reactions: Hyperemia at the injection site.

Overdose:

Symptoms: lengthening of the neuromuscular block and its consequences (excessive decrease in blood pressure, collapse, respiratory arrest, paralysis of muscles, shock).

Treatment: IVL on the background of sedative therapy to restore spontaneous breathing, the introduction of antagonists - inhibitors of cholinesterase in combination with atropine, with collapse and shock - the restoration of the volume of circulating blood, the appointment of hypertensive drugs (LS), symptomatic therapy.

Interaction:

Pharmacodynamic

Diethyl ether, to a lesser degree halothane, hexobarbital, thiopental sodium intensify and prolong the action of atracurium bezilate.

Aminoglycosides and polypeptide antibiotics (polymyxins), spectinomycin, capreomycin, amphotericin B, trimethoprim, tetracyclines, lincomycin, clindamycin, antiarrhythmic drugs (propranolol, blockers of "slow" calcium channels (BCC), lidocaine, procainamide, quinidine), procaine (in / in), diuretics (furosemide, ethacrynic acid, indapamide, mannitol, thiazide, acetazolamide), glucocorticosteroids (GCS), mineralocorticoids, magnesium sulfate, ketamine, lithium salts, ganglion blockers (trimetaphane camsylate, hexamethonium benzenesulfonate), depolarizing muscle relaxants, citrates strengthen neuromuscular blockade, Atracuria bezylate reduces the effect of cholinesterase inhibitors, incl. eudrophonia chloride (you may need to adjust their doses).

Antibiotics, beta-blockers (propranolol, oxprenolol), antiarrhythmic drugs (procainamide, quinidine), antirheumatic drugs (chloroquine, D-phenicylamine), trimetaphane camsylate, chlorpromazine, steroids, phenytoin, lithium preparations can enhance or unmask a latent myasthenia gravis or cause a myasthenic syndrome, which can lead to hypersensitivity to the drug.

Opioid analgesics increase respiratory depression.High doses of sufentanil reduce the need for high initial doses of nondepolarizing muscle relaxants. Non-polarizing muscle relaxants prevent or reduce the rigidity of muscles caused by high doses of opioid analgesics (including alfentanil, fentanyl, sufentanil), while the risk of bradycardia and lowering blood pressure caused by narcotic analgesics (especially in patients with impaired myocardial function and / or on the background of the appointment of beta-adrenoblockers), moreover - increases the risk of arterial hypotension (the use of H1 or H2-histamine-receptor blockers can prevent the development or reduce the severity of these adverse effects).

Atracuria bezilat enhances histamine-dependent side effects caused by narcotic analgesics (except for alfentanil, fentanyl and sufentanil, not causing histamine release) (see section "Special instructions").

Inhalation anesthetics (including enflurane, isoflurane) increase the effect (the dose of peripheral muscle relaxants should be reduced to 1 / 3-1 / 2 of the usually recommended). Calcium preparations reduce the effect.Doxapram temporarily masks the residual effects of muscle relaxants.

Depolarizing Muscle Relaxant suxamethonium chloride should not be prescribed to increase the duration of neuromuscular conduction caused by nondepolarizing blockers, as this can cause a blockade that is complex for the inhibition of cholinesterase inhibitors and its elongation.

Pharmaceutical

Do not mix in one syringe with thiopental sodium or other alkaline solution (inactivation). Ridelat®-C solution is hypotonic and should not be applied simultaneously through the same system with blood transfusions (see section "Special instructions"). Compatible with the following solutions for infusions (at a concentration of 0.5-0.9 mg / ml in daylight and temperature up to + 30 ° C): 0.9% sodium chloride solution for IV administration - for at least 24 hours , 5% dextrose solution for intravenous administration -8 hours, Ringer's injection solution -8 hours, sodium chloride solution 0.18%, and dextrose 4% for iv administration -8 hours, solution of sodium salt of lactic acid (Hartman's solution ) for iv introduction -4 hours.

Special instructions:

Like other muscle relaxants, atracurium bezylate causes paralysis of skeletal muscles, including the respiratory muscles, but does not affect consciousness, atracurium bezylate should be used only during general anesthesia under the supervision of a qualified anesthesiologist in the departments where there is equipment for intubation of the trachea and ventilation.

With the introduction of drugs for general anesthesia through the same needle or catheter, it is necessary to wash the catheter after injection of each drug with a 0.9% solution of sodium chloride. The advantage over other non-depolarizing muscle relaxants is the absence of cumulation in repeated injections (with repeated bolus and drip administration there is no need to change the dosage regimen). The evoked neuromuscular block is quickly and completely eliminated by neostigmine bromide, which is preceded by the administration of atropine (complete neuromuscular blockade is eliminated after 5-10 min and does not depend on the total amount of administered dose, from age of the patient and on the presence of hepatic-renal pathology). In patients with severe myasthenia gravis, other neuromuscular diseases and severe electrolyte imbalance, hypersensitivity phenomena can occur. It does not affect consciousness, therefore the drug should be used only in combination with adequate general anesthesia,under the supervision of an experienced anesthesiologist and with the availability of funds for endotracheal intubation and mechanical ventilation.

When administered at the recommended dosage range atracurium bezylate does not block the vagus nerve and nerve ganglia, does not significantly affect the heart rate and does not prevent bradycardia caused by anesthetics or vagal nerve stimulation during surgery.

Atracurium bezylate is inactivated in an alkaline medium and should not be mixed in one syringe with sodium thiopental or alkaline solutions. The solution of atracurium bezylate is hypotonic and should not be applied simultaneously through the same system with blood transfusions (see section "Interaction with other drugs").

In patients with burns, resistance to non-depolarizing muscle relaxants may develop, which will require an increase in the doses of these drugs, the magnitude of which depends on the length of time since the burn and on the surface area of the burn.

Form release / dosage:

Solution for intravenous administration 10 mg / ml.

Packaging:

5 ml per ampoule of colorless neutral glass with a color fracture ring or with a colored dot and a notch.

One, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional bar code, and alphanumeric coding are additionally applied to the ampoules.

By 5 ampoules in a contoured cell pack of a polyvinylchloride film and aluminum foil, or a polymer transparent film, or without an aluminum foil and a polymer film.

For 1 or 2 contour mesh packages together with instructions for use in a pack of cardboard.

In the case of production of the drug at LLC "COMPANY" DECO ".

5 ml per ampoule of colorless neutral glass with a color fracture ring or with a colored dot and a notch. One, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional bar code, and alphanumeric coding are additionally applied to the ampoules.

By 5 or 10 ampoules in a contiguous cell pack of a polyvinylchloride film and aluminum foil, or a polymer transparent film, or without an aluminum foil and a polymer film.

1 contour pack together with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of 2 to 8 ° C, Do not freeze. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000551

Date of registration:25.05.2011 / 14.11.2014

Expiration Date:25.05.2016

The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia

Manufacturer: & nbsp

FarmSirma Soteks, ZAO Russia

Information update date: & nbsp14.11.2014

Illustrated instructions

Instructions

Ridelat®-C (Ridelat®-C)