Thiopental-KMP (Lyophilisate, Powder) Instructions for Use

ATC Code

N05CA19 (Thiopental)

Active Substance

Thiopental sodium (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Agent for non-inhalation anesthesia

Pharmacotherapeutic Group

Non-inhalation anesthetic agent

Pharmacological Action

A non-inhalation anesthetic agent, a derivative of barbituric acid. It has a hypnotic and general anesthetic effect.

It exerts a depressant effect on the respiratory and vasomotor centers, as well as on the myocardium. As a result, blood pressure and stroke volume decrease with a simultaneous compensatory increase in heart rate, as well as peripheral vasodilation. The degree of these changes increases as anesthesia deepens.

It causes stronger muscle relaxation than hexobarbital.

Compared to hexobarbital, it has a stronger stimulating effect on the vagus nerve, can cause laryngospasm, profuse mucus secretion, and other signs of vagotonia; therefore, for bronchoscopy, Thiopental sodium is less suitable than hexobarbital.

After a single dose, anesthesia lasts for 20-25 minutes.

Pharmacokinetics

After intravenous administration, Thiopental sodium quickly penetrates the blood-brain barrier. Equilibrium concentrations in plasma and in the brain are reached very quickly (within approximately 1 minute) due to the high lipid solubility of sodium thiopental. It is rapidly redistributed by diffusion from the brain and other well-perfused areas into muscles, adipose tissue, and ultimately into all tissues. Due to rapid elimination from brain tissue, a single dose of sodium thiopental has a short duration of action.

The metabolism of sodium thiopental occurs significantly slower than its redistribution and occurs mainly in the liver. After a single injection, it is metabolized at a rate of 12-16% per hour. Less than 1% is excreted by the kidneys unchanged.

Indications

As an agent for anesthesia during short surgical interventions. For induction and basal anesthesia with subsequent use of other anesthetic agents.

ICD codes

Dosage Regimen

Lyophilisate, Powder

Administered intravenously; in children, it can be administered rectally.

A single dose for intravenous administration is 3-10 mg/kg depending on the patient’s condition and age. Rectally – as a warm solution for children under 3 years of age at a dose of 40 mg per 1 year of life, for children aged 3-7 years – at a dose of 50 mg per 1 year of life.

The maximum single dose for adults is 1 g.

Adverse Reactions

From the central nervous system most frequently – dizziness, lethargy, ataxia. These effects are associated with dose-dependent depression of the CNS. Memory impairment in the postoperative period is possible.

From the respiratory system laryngospasm, bronchospasm, hypersecretion of mucus in the bronchi, respiratory depression of varying severity, and with rapid administration – up to apnea are possible.

From the cardiovascular system dose-dependent decrease in blood pressure; with rapid administration, collapse may develop.

From the digestive system hypersalivation.

Allergic reactions skin manifestations are possible.

Contraindications

Organic diseases of the liver and kidneys, diabetes mellitus, severe exhaustion, shock, collapse, bronchial asthma, inflammatory diseases of the nasopharynx, febrile conditions, severely pronounced circulatory disorders.

History of acute porphyria attacks in the patient or their relatives.

Use in Pregnancy and Lactation

If it is necessary to use during pregnancy and lactation, the expected benefit for the mother and the potential risk to the fetus or child should be carefully weighed.

Use in Hepatic Impairment

Contraindicated in organic liver diseases.

Use in Renal Impairment

Contraindicated in organic kidney diseases.

Pediatric Use

As an agent for basal anesthesia in children, Thiopental sodium is indicated mainly for increased nervous excitability.

Special Precautions

Thiopental sodium should be used with special caution in inflammatory diseases of the upper respiratory tract (in these cases, tracheal intubation is indicated).

Thiopental sodium may increase the tone of the parasympathetic nervous system, therefore, an adequate dose of atropine should be administered before its use. Immediately after the onset of anesthetic sleep, it is necessary to ensure airway patency.

During prolonged anesthesia, when the hypnotic effect caused by sodium thiopental is maintained by intravenous administration of long-acting anesthetics and/or inhalation anesthetics, due to the danger of a cumulative effect, the dose of sodium thiopental should not exceed 1 g.

Thiopental sodium can be used in combination with muscle relaxants provided that artificial ventilation is performed.

The duration of action of barbiturates increases with impaired liver function, kidney function, protein metabolism, as well as in elderly patients.

Administration of sodium thiopental into an artery causes an instantaneous spasm of the vessel, which is accompanied by impaired circulation distal to the injection site, so thrombosis of the main vessel is possible. Immediately upon symptoms of this complication, administration should be stopped and therapy aimed at relieving the spasm with simultaneous administration of an anticoagulant should be immediately initiated.

As an agent for basal anesthesia in children, Thiopental sodium is indicated mainly for increased nervous excitability.

Drug Interactions

Due to the strong alkaline reaction (pH 10.5 and above), barbiturates are incompatible with drugs having an acidic reaction (including ascorbic acid, phenothiazines, epinephrine).

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.