Suxamethonium-Biolek (Solution) Instructions for Use

Marketing Authorization Holder

Pharmstandard JSC (Russia)

Manufactured By

Pharmstandard-Biolek, PJSC (Ukraine)

ATC Code

M03AB01 (Suxamethonium chloride)

Active Substance

Suxamethonium iodide (PhBs Slovak Pharmacopoeia)

Dosage Form

Suxamethonium-Biolek

Solution for intravenous and intramuscular administration 20 mg/1 ml: amp. 5 ml 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for intravenous and intramuscular administration in the form of a transparent, colorless liquid.

Excipients: sodium chloride – 7 mg, disodium edetate – 0.05 mg, ascorbic acid – 0.05 mg, 0.1M hydrochloric acid solution – to adjust pH to 3.3-3.6, water for injection – up to 1 ml.

5 ml – ampoules (5) – cardboard packs.
5 ml – ampoules (10) – cardboard packs.

Clinical-Pharmacological Group

Peripherally acting depolarizing-type muscle relaxant

Pharmacotherapeutic Group

Depolarizing peripheral-acting muscle relaxant

Pharmacological Action

It is a short-acting depolarizing muscle relaxant. It causes blockade of neuromuscular transmission. By interacting with H-cholinergic receptors, it causes depolarization of the end plate. The process spreads to adjacent membranes, causing a generalized disorganized contraction of myofibrils (i.e., the development of blockade is preceded by muscle fasciculations – a result of short-term facilitation of neuromuscular transmission). The membranes, remaining depolarized, do not respond to additional impulses, since maintaining muscle tone requires the arrival of repeated impulses associated with repolarization of the end plate, leading to spastic paralysis.

After intravenous administration, muscle relaxation occurs in the following sequence: eyelid muscles, masticatory muscles, muscles of the fingers, eyes, limbs, neck, back and abdomen, vocal cords, then intercostal muscles and diaphragm.

It causes an increase in cerebral blood flow and an increase in intracranial pressure. After intravenous administration, the effect begins in 54-60 seconds, after 2-3 minutes muscle relaxation reaches its maximum and is maintained in full for 3 minutes. The duration of action is 5-10 minutes.

The severity of the action depends on the administered dose: 0.1 mg/ml – relaxation of skeletal muscles without significant effect on the respiratory system; 0.2-1 mg/kg – complete relaxation of the muscles of the abdominal wall and respiratory muscles (significant limitation or complete cessation of spontaneous breathing occurs). For prolonged muscle relaxation, repeated administration is necessary. The rapid onset of effect and subsequent rapid recovery of muscle tone allow for controlled and manageable muscle relaxation.

Pharmacokinetics

After intravenous administration, it is distributed in plasma and extracellular fluid. More than 90% is hydrolyzed by blood cholinesterase to succinic acid and choline. The half-life is 90 seconds with a normal level of pseudocholinesterase. It is excreted by the kidneys. It does not penetrate the intact blood-brain barrier. It does not accumulate.

Indications

• Cessation of spontaneous breathing (endotracheal intubation, bronchoscopy);
• Complete muscle relaxation (endoscopy, reduction of dislocations, reposition of fractures, gynecological, thoracic, abdominal surgical interventions);
• Prevention of convulsions during electroconvulsive therapy;
• Strychnine poisoning;
• Tetanus (symptomatic therapy).

ICD codes

Dosage Regimen

Adults: intravenously slowly, as a bolus or drip (for long-term drip infusion, a 0.1% solution is used). Depending on the clinical situation, with intravenous administration, a single dose varies from 100 mcg/kg to 1.5-2 mg/kg of body weight.

For tracheal intubation – 0.2-0.8 mg/kg; for muscle relaxation and cessation of spontaneous breathing – 0.2-1 mg/kg; for relaxation of skeletal muscles during reduction of dislocations and reposition of bone fragments in fractures – 0.1-0.2 mg/kg; for endoscopy – 0.2 mg/kg; for prevention of complications during electroconvulsive therapy (convulsions, muscle and tendon avulsion) – 0.1-1 mg/kg intravenously, but not more than 150 mg.

For prolonged muscle relaxation throughout the entire operation, it can be administered fractionally, every 5-7 minutes at 0.5-1 mg/kg. Repeated doses act for a longer duration.

Intramuscularly used in children in doses up to 2.5 mg/kg, but not more than 150 mg; intravenously – 1-2 mg/kg.

Adverse Reactions

Allergic reactions (anaphylactic shock, bronchospasm); hyperkalemia.

Decreased blood pressure, conduction disorders of the heart, arrhythmia, bradycardia (more often in children, with repeated administration – in children and adults), cardiogenic shock, increased intraocular pressure, hypersalivation, fever, myalgia (in the postoperative period); prolonged paralysis of the respiratory muscles (associated with genetically determined impairment of serum cholinesterase formation); rarely – rhabdomyolysis with the development of myoglobinemia and myoglobinuria. In children, young patients, and women (mainly vagotonics), short-term bradycardia may occur, in some cases asystole.

Muscle pain may occur 10-12 hours after drug administration. With repeated administration of the drug, excessively prolonged muscle relaxation and long-term apnea may sometimes develop.

Contraindications

• Hypersensitivity;
• Malignant hyperthermia (including in the anamnesis);
• Myasthenia gravis;
• Congenital and dystrophic myotonia;
• Duchenne muscular dystrophy;
• Closed-angle glaucoma;
• Acute hepatic failure;
• Pulmonary edema;
• Penetrating eye injuries;
• Bronchial asthma;
• Hyperkalemia;
• Children under 1 year of age;
• Pregnancy;
• Lactation period.

With caution: decreased activity of serum pseudocholinesterase (terminal stage of hepatic failure, anemia, cachexia, prolonged starvation, chronic infections, extensive burns, trauma), postpartum period, tetanus, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, systemic connective tissue diseases, condition after plasma transfusion, plasmapheresis, artificial circulation, acute and chronic intoxication with cholinesterase inhibitor insecticides (upon ingestion) or anticholinesterase agents (neostigmine, physostigmine, distigmine bromide), simultaneous use of drugs competing with succinylcholine for cholinesterase (procaine intravenously), emergency surgical interventions in patients with a “full stomach”.

Use in Pregnancy and Lactation

The use of this drug is prohibited during pregnancy and lactation.

Use in Hepatic Impairment

Contraindicated: acute hepatic failure. Use with caution in cases of decreased activity of serum pseudocholinesterase (terminal stage of hepatic failure).

Use in Renal Impairment

Use with caution: chronic renal failure. In patients with renal failure (without signs of hyperkalemia and neuropathy), the drug is administered once in average doses, but is not used for multiple administrations or in increased doses due to the risk of hyperkalemia.

Pediatric Use

The use of the drug is prohibited in children under 1 year of age.

Special Precautions

It is used only in specialized departments with equipment for artificial lung ventilation and against the background of general anesthesia. Preliminary administration of 3-4 mg of tubocurarine chloride or 10-15 mg of diplacin chloride 1 minute before the infusion of suxamethonium iodide prevents muscle fasciculations and the subsequent appearance of muscle pain. With an appropriate dose and repeated administration, it can also be used for longer operations; however, for prolonged muscle relaxation, non-depolarizing muscle relaxants are usually used, which are administered after preliminary tracheal intubation against the background of suxamethonium iodide.

Slow administration of the drug, as well as a preliminary intravenous injection of atropine at a dose of 1-1.5 mg, largely prevents bradycardia and increased bronchial secretion.

In patients with renal failure (without signs of hyperkalemia and neuropathy), the drug is administered once in average doses, but is not used for multiple administrations or in increased doses due to the risk of hyperkalemia. Prolonged muscle relaxation with possible apnea can be caused by several reasons: “atypical” serum cholinesterase, hereditary deficiency of serum cholinesterase, or a temporary decrease in its level. If the drug is administered repeatedly and 25-30 minutes after the last injection the patient’s muscle tone does not recover and breathing remains shallow, one may suspect the transition of a depolarizing block to an anti-depolarizing block (the occurrence of a “dual block”). To relieve this effect, proserin should be used according to the standard method: atropine is first administered intravenously at a dose of 0.5-0.7 mg (0.5-0.7 ml of a 0.1% solution), wait for an increase in pulse rate, and after 1-2 minutes, proserin is administered intravenously at a dose of 1.5 mg (3 ml of a 0.05% solution).

Overdose

Symptoms: increased severity of side effects, respiratory arrest.

Treatment: artificial lung ventilation, in case of decreased serum cholinesterase levels – transfusion of fresh blood.

Drug Interactions

Pharmaceutically incompatible with donor blood and blood products (hydrolysis occurs), with barbiturate solutions and alkaline solutions (precipitate forms).

Compatible with isotonic sodium chloride solutions, Ringer’s solution, 5% fructose solution and 6% dextran solution.

Anticholinesterase agents, procaine, procainamide, lidocaine, verapamil, beta-blockers, aminoglycoside antibiotics, amphotericin B, clindamycin, cyclopropane, propanidid, organophosphorus insecticides, Mg²⁺ and Li⁺ salts, quinidine, quinine, chloroquine, pancuronium potentiate and prolong the muscle relaxant effect.

Compatible with other muscle relaxants and narcotic analgesics.

It potentiates the cardiac effects of cardiac glycosides (bradycardia).

It reduces the effectiveness of antimyasthenic drugs.

Halogen-containing agents for general anesthesia potentiate, while sodium thiopental and atropine reduce the undesirable effect on the cardiovascular system.

Drugs with the potential ability to reduce blood cholinesterase activity (aprotinin, diphenhydramine, promethazine, estrogens, oxytocin, glucocorticosteroids in high doses, oral contraceptives) potentiate and prolong the muscle relaxant effect of suxamethonium iodide.

Storage Conditions

List A.

The drug should be stored in a light-protected place, out of the reach of children, at a temperature of +2 to +8°C (46.4°F). Freezing is not allowed.

Shelf Life

The shelf life is 1 year and 6 months. Do not use after the expiration date printed on the packaging.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.