Sulfoprokain (Solution) Instructions for Use

Marketing Authorization Holder

Biosintez, PJSC (Russia)

ATC Code

R07AB (Respiratory stimulants)

Active Substances

Procaine (Rec.INN registered by WHO)

Sulphocamphoric acid (Grouping name)

Dosage Form

Sulfoprokain

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

Dosage Form, Packaging, and Composition

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

Excipients: water for injection up to 1 ml.

2 ml – ampoules (10) – cardboard boxes.
2 ml – ampoules (10) – cardboard packs.

Clinical-Pharmacological Group

Analeptic

Pharmacotherapeutic Group

Analeptic agent

Pharmacological Action

A combined medicinal product with analeptic action.

Procaine is a local anesthetic agent 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 impulses 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 areas 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 by 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 the 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 vasodilatory 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 Sulfoprokain by subcutaneous, intramuscular, or intravenous routes; intravenous administration may be bolus or drip infusion.

Determine the specific route and frequency based on the indication and clinical severity of the patient’s condition.

For adult patients, the typical single dose is 2 ml to 4 ml of the solution.

Administer subcutaneously or intramuscularly once or twice daily as required by the patient’s status.

For intravenous bolus injection, administer the solution slowly over several minutes.

For intravenous drip infusion, dilute the required dose in an appropriate volume of 0.9% sodium chloride solution or 5% dextrose solution.

The maximum daily dose should generally not exceed 10 ml of the solution.

Adjust the dosage regimen for elderly or debilitated patients, potentially using lower doses.

Perform individual sensitivity testing prior to the first administration of the drug.

Continuously 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, local anesthetics of ester structure (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 in 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 measures. 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, 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.