Thiopental sodium (Thiopentalum Natrium)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Means for anesthesia

Included in the formulation
  • Thiopental
    powder in / in 
    Sandoz GmbH     Austria
  • Thiopental sodium
    powder in / in 
    SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    N.01.A.F   Barbiturates

    N.01.A. F.03   Thiopental sodium

    Pharmacodynamics:

    Means for non-anional anesthesia, a derivative of barbituric acid. Has a hypnotic and general anesthetic effect.

    Has a depressing effect on the respiratory and vasomotor centers, as well as on the myocardium. As a result, blood pressure and stroke volume decrease with simultaneous compensatory increase in the heart rate, as well as peripheral vasodilation. The degree of these changes increases with the deepening of anesthesia. After a single dose, anesthesia lasts 20-25 minutes.

    Pharmacokinetics:

    After intravenous administration, sodium thiopental rapidly penetrates the blood-brain barrier. Equilibrium concentrations in plasma and in the brain are achieved very quickly (approximately 1 minute) due to the high solubility of sodium thiopental in lipids. Rapidly, by diffusion, it is redistributed from the brain and other well-supplied areas into the muscles, fatty tissue and, ultimately, into all tissues. Due to rapid removal from the brain tissue, a single dose of thiopental sodium acts briefly.

    The metabolism of sodium thiopental is much 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 a means for anesthesia with short surgical interventions. For introductory and basic anesthesia with subsequent use of other means for anesthesia.

    ICD-10

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    Contraindications:

    Hypersensitivity; porphyria, including acute intermittent (including anamnesis in the patient or his immediate family); diseases that are a contraindication for general anesthesia; intoxication with ethanol, narcotic analgesics, sleeping pills and preparations for general anesthesia; shock, asthmatic status, malignant hypertension.

    With rectal administration: surgical interventions on the rectum; inflammatory, erosive and ulcerative diseases and tumors of the large intestine.

    Carefully:

    Chronic obstructive pulmonary disease, bronchial asthma, severe myocardial contractility, severe cardiovascular insufficiency, cardiovascular diseases, arterial hypotension, collapse, hypovolemia, excessive premedication, hepatic and / or renal failure, Addison's disease, myxedema, diabetes mellitus, anemia, myasthenia gravis, myotonia, muscular dystrophy, cachexia, febrile syndrome, inflammatory diseases of the nasopharynx, obesity, pregnancy, children's age.

    Pregnancy and lactation:

    Adequate and well-controlled studies in humans and animals have not been conducted. Penetrates into breast milk. Do not apply!

    Category of recommendations FDA is not defined.

    Dosing and Administration:

    Enter intravenously, children can be administered rectally.

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

    The maximum single dose for adults is 1 g.

    Side effects:

    From the side CNS: most often - dizziness, blocking, ataxia. These effects are associated with a dose-dependent depression of the central nervous system. Possible memory impairment in the postoperative period.

    From the side respiratory system: Laryngospasm, bronchospasm, hypersecretion of mucus in bronchial tubes, respiratory depression of various degrees of severity are possible, with rapid administration - up to apnea.

    From the side of cardio-vascular system: dose-dependent decrease in blood pressure, with rapid administration, the development of collapse is possible.

    From the side digestive system: hypersalivation.

    Allergic reactions: skin manifestations are possible.

    Overdose:

    Symptoms: severe depression of the central nervous system, severe hypotension, a sharp decrease in the total peripheral resistance of blood vessels, severe respiratory depression right up to apnea. At a very high dose: pulmonary edema, a circulatory collapse with a fall total peripheral resistance of blood vessels, cardiac arrest.

    Treatment symptomatic, including artificial ventilation, artificial circulation.

    Interaction:

    Alcohol, CNS depressant drugs, including those used during anesthesia - increased oppressive effects on the central nervous system, increased risk of respiratory depression and hypotensive effect.

    Antihypertensive drugs (including ganglion blockers, diuretics, etc.) - additive dose-dependent antihypertensive effect; clonidine, methyldopa, rauwolfia alkaloids and other antihypertensive agents, depressing the central nervous system - enhancing the depressant effect on the central nervous system.

    Acetylsalicylic acid, probenecid - potentiation of barbiturate anesthesia (due to a high bond with plasma proteins for acetylsalicylic acid and probenecid).

    Ketamine - increased risk of hypotension and respiratory depression, antagonism of the hypnotic effect of barbiturates.

    Acid and oxidizing substances, including some antimicrobial agents, muscle relaxants and analgesics: amikacin, benzylpenicillin, cefapyrine, codeine, ephedrine, fentanyl, morphine, pentazocine, prochlorperazine, suxamethonium and others - pharmaceutical incompatibility with thiopental.

    Magnesium sulfate is an additive inhibitory effect on the central nervous system.

    The drugs that cause hypothermia are an increased risk of hypothermia.

    Phenothiazines (especially promethazine) - potentiation of the depressing effect on the central nervous system, hypotensive effect

    Special instructions:

    The most common barbiturate for introductory anesthesia is a representative of thiobarbiturate class.Barbiturate ultrashort action (with a single intravenous administration).

    Instructions
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