Sulfocamphocaine^® (Solution) Instructions for Use

Marketing Authorization Holder

Pharmstandard-UfaVITA OJSC (Russia)

ATC Code

R07AB (Respiratory stimulants)

Active Substances

Procaine (Rec.INN registered by WHO)

Sulphocamphoric acid (Grouping name)

Dosage Form

Sulfocamphocaine®

Solution for injection 50.4 mg+49.6 mg/ml: amp. 2 ml 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for injection in the form of a transparent, colorless or slightly yellowish liquid.

Excipients: water for injection – up to 1 ml.

2 ml – ampoules of colorless glass (5) – contour cell packs (1) – cardboard packs.
2 ml – ampoules of colorless glass (5) – contour cell packs (2) – cardboard packs.
2 ml – ampoules of colorless glass (10) – contour cell packs (1) – cardboard packs.
2 ml – polymer ampoules (10) – cardboard packs.
2 ml – polymer ampoules (10) – foil film bags (1) – cardboard packs.

Clinical-Pharmacological Group

Analeptic

Pharmacotherapeutic Group

Analeptic agent

Pharmacological Action

Combined medicinal product, has an analeptic effect.

Procaine is a local anesthetic with moderate anesthetic activity and a wide therapeutic range. Being a weak base, it blocks sodium channels, prevents impulse generation in sensory nerve endings and impulse conduction along nerve fibers. It alters the action potential in nerve cell membranes without a pronounced effect on the resting potential. It suppresses the conduction of not only pain but also impulses of other modalities. Upon absorption and direct vascular administration into the bloodstream, it reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (has some ganglion-blocking action), relieves smooth muscle spasm, reduces myocardial excitability and the excitability of the motor zones of the cerebral cortex. It eliminates the descending inhibitory influences of the brainstem reticular formation. It depresses polysynaptic reflexes. In high doses, it can cause convulsions. It has short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 hour).

Sulfocamphoric acid has an analeptic effect. It stimulates the respiratory and vasomotor centers of the medulla oblongata. It has a cardiotonic effect, enhancing metabolic processes in the myocardium, improving its function and increasing its sensitivity to sympathetic impulses. It increases the tone of peripheral blood vessels. It improves pulmonary ventilation and pulmonary blood flow. It increases the secretion of bronchial glands.

Pharmacokinetics

Procaine undergoes complete systemic absorption. The degree of absorption depends on the site and route of administration (especially on vascularization and blood flow rate at the injection site) and the final dose (amount and concentration). It is rapidly hydrolyzed by plasma and liver esterases to form two main pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating effect) and para-aminobenzoic acid (is a competitive antagonist of sulfonamide drugs and may weaken their antimicrobial effect). T_1/2 is 30-50 sec, in the neonatal period – 54-114 sec. It is excreted mainly by the kidneys in the form of metabolites, no more than 2% is excreted unchanged.

Sulfocamphoric acid is rapidly absorbed after subcutaneous and intramuscular administration.

Indications

As a symptomatic agent in the complex therapy of acute and chronic heart failure, acute and chronic respiratory failure; cardiogenic and anaphylactic shock.

ICD codes

Dosage Regimen

Administer Sulfocamphocaine^® subcutaneously, intramuscularly, or intravenously as a bolus or drip infusion.

For subcutaneous and intramuscular injections, use a dose of 2 ml to 4 ml per administration.

For intravenous bolus injection, administer 2 ml to 4 ml slowly.

For intravenous drip infusion, dilute the required dose in a 100-150 ml volume of 0.9% sodium chloride solution or 5% dextrose solution.

The frequency of administration is one to two times per day; adjust based on the clinical situation and patient response.

The maximum single dose is 4 ml; the maximum daily dose is 8 ml.

The duration of therapy is determined by the treating physician according to the indication and clinical efficacy.

Perform a test for individual sensitivity before the first administration.

Monitor the patient’s cardiovascular and respiratory systems during and after administration.

Adverse Reactions

Blood and lymphatic system disorders frequency unknown – methemoglobinemia.

Immune system disorders frequency unknown – allergic reactions (including urticaria), angioedema, anaphylactic reactions (including anaphylactic shock).

Nervous system disorders frequency unknown – headache, dizziness, drowsiness, persistent anesthesia, weakness, motor restlessness, nervousness, loss of consciousness, convulsions, trismus, tremor, visual and auditory disturbances, nystagmus, cauda equina syndrome (leg paralysis, paresthesia), respiratory muscle paralysis, motor and sensory block.

Cardiac disorders frequency unknown – bradycardia, arrhythmias, chest pain, changes in the process of excitation propagation in the heart, which are manifested on the ECG as a flat T wave or shortening of the ST segment, decreased blood pressure (especially in patients with initial arterial hypotension), increased blood pressure, collapse, peripheral vasodilation.

Respiratory, thoracic and mediastinal disorders frequency unknown – respiratory tract spasms or difficulty breathing.

Gastrointestinal disorders frequency unknown – dyspeptic symptoms, nausea, vomiting.

Renal and urinary disorders frequency unknown – involuntary urination.

Skin and subcutaneous tissue disorders frequency unknown – skin itching, skin rash.

General disorders and administration site conditions frequency unknown – hypothermia, shivering.

Contraindications

Hypersensitivity to procaine, ester-type local anesthetics (tetracaine, benzocaine), PABA, sulfocamphoric acid; pregnancy, breastfeeding period; children and adolescents under 18 years of age.

With caution

Arterial hypotension; emergency surgeries accompanied by acute blood loss; conditions accompanied by reduced hepatic blood flow (e.g., in chronic heart failure, liver diseases); progression of cardiovascular failure (usually due to the development of heart block and shock); inflammatory diseases or infection at the injection site; pseudocholinesterase deficiency; renal failure; elderly patients over 65 years of age; debilitated patients.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Pediatric Use

The drug is contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Use with caution in patients over 65 years of age.

Special Precautions

Caution should be exercised when administering the drug containing this combination to patients with low blood pressure due to the possible development of the hypotensive effect of procaine.

This agent is not a first-line drug for the treatment of acute and chronic heart failure, acute and chronic respiratory failure, cardiogenic and anaphylactic shock, and its use for these diseases/pathological conditions is not strictly necessary.

The use of this agent does not cancel the need for the use of other methods of treatment of acute and chronic heart failure, acute and chronic respiratory failure, cardiogenic and anaphylactic shock in accordance with current standards of medical care and national clinical guidelines.

No favorable effect of the use of this combination on the survival of patients with acute and chronic heart failure, acute and chronic respiratory failure, cardiogenic and anaphylactic shock has been established.

The use of this agent should be carried out by experienced specialists in a properly equipped room with readily available equipment and drugs necessary for monitoring cardiac activity and resuscitation. Patients require monitoring of the functions of the central nervous system, cardiovascular system and respiratory system.

Testing for individual sensitivity to the drug containing this combination is recommended before use.

Drug Interactions

The use of drugs containing this combination in combination with cardiac glycosides, steroid hormones, and analgesics enhances the analeptic effect of the drug.

Procaine enhances the depressant effect on the central nervous system of general anesthetics, hypnotics and sedatives, narcotic analgesics and tranquilizers.

Anticoagulants (ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) increase the risk of bleeding.

When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.

Concomitant use with MAO inhibitors (furazolidone, procarbazine, selegiline) increases the risk of arterial hypotension.

This combination enhances and prolongs the action of muscle relaxants.

When procaine is used together with narcotic analgesics, an additive effect is noted, while respiratory depression is enhanced.

Procaine reduces the antimyasthenic effect of drugs, especially when used in high doses, which requires additional correction of myasthenia treatment.

Cholinesterase inhibitors (antimyasthenic drugs, cyclophosphamide, demecarium, echothiophate, thiotepa) reduce the metabolism of procaine.

The metabolite of procaine (PABA) is an antagonist of sulfonamides.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.