Runny nose

Sodium thiopental dilution instructions. Overdose of anesthetic

Dosage form: powder for preparing a solution for intravenous administration Compound:

1 bottle contains

active substance: sodium thiopental 0.5 g or 1.0 g, respectively

Description:

Yellowish-white crystalline hygroscopic powder.

Pharmacotherapeutic group:non-inhalation product general anesthesia ATX:

N.01.A.F Barbiturates

N.01.A.F.03 Sodium thiopental

Pharmacodynamics:

A drug for non-inhalation general anesthesia of ultra-short action, a derivative of thiobarbituric acid, has a pronounced hypnotic, some muscle relaxant and weak analgesic activity. Slows down the opening time of GABA (gamma-amino-butyric acid)-dependent channels on the postsynaptic membrane of brain neurons, lengthens the time of entry of chlorine ions into the nerve cell and causes hyperpolarization of the membrane.

Suppresses the stimulating effect of amino acids (aspartate and glutamate). In large doses, directly activating GABA receptors, it has a GABA-stimulating effect.

It has anticonvulsant activity, increasing the threshold of neuronal excitability and blocking the conduction and spread of convulsive impulses throughout the brain. Promotes muscle relaxation by suppressing polysynaptic reflexes and slowing down the conduction of interneurons to the spinal cord.

Reduces the intensity of metabolic processes in the brain, the brain's utilization of glucose and oxygen.

The drug is also characterized by a decrease intracranial pressure. The decrease in intracranial pressure appears to be mediated by a decrease in cerebral blood flow and volume coupled with an increase in cerebral vascular resistance.

After intravenous administration, a state of sleep occurs within 30-40 seconds, the depth of which can increase over the next 40 seconds. General anesthesia lasts 5-10 minutes. This is followed by a period of post-drug sleep lasting 10-30 minutes. The useful duration of general anesthesia (time of manipulation) is 5-8 minutes, characterized by short duration (after administration of a single dose, general anesthesia lasts 10-30 minutes) and awakening with some drowsiness and retrograde amnesia.

The surgical stage of general anesthesia is characterized by a decrease or disappearance of tendon and corneal reflexes, a slight narrowing (or normal sizes) pupils, fixed or “floating” position eyeballs, relaxation of the pharyngeal muscles with retraction of the tongue, decreased depth of breathing and decreased blood pressure(HELL). Upon recovery from general anesthesia, the analgesic effect ceases simultaneously with the patient's awakening. At reintroduction the action is prolonged (cumulates).

Pharmacokinetics:

When administered intravenously, it quickly penetrates into the brain, skeletal muscles, kidneys, liver and adipose tissue. The period to achieve maximum concentration (TCmax) is within 30 seconds (brain), 15-30 minutes (muscles). In fat depots, the concentration of the drug is 6-12 times higher than plasma concentration. Volume of distribution - 1.7-2.5 l/kg, during pregnancy - 4.1 l/kg, in obese patients - 7.9 l/kg. Communication with plasma proteins - 76-86%.

First, the drug enters organs with intense blood flow (brain, heart, liver, lungs), then quickly redistributed into muscle tissue. Equilibrium between plasma concentration and blood concentration muscle tissue achieved within 15-30 minutes after injection. Due to the fact that adipose tissue is poorly supplied with blood, plasma-adipose tissue concentration equilibrium is achieved after 1.5-2.5 hours. Penetrates the placental barrier and is secreted into breast milk. The maximum concentration of thiopental in the umbilical cord is achieved 2-3 minutes after intravenous administration. The concentration of thiopental in breast milk is low even when high doses are used.

Metabolized mainly in the liver with the formation of inactive metabolites, 3-5% of the administered dose is desulfurized to pentobarbital, which is also an anesthetic; a small part of the drug is inactivated in the kidneys and brain. Leaching from adipose tissue limits the rate of elimination of thiopental. Half-life (T 1\2) one-time intravenous dose is 3-8 hours. T1/2 in the distribution phase - 5-9 minutes, in the elimination phase - 3-8 hours (possibly extended to 10-12 hours; during pregnancy - up to 26.1 hours, in obese patients - up to 27.85 hours), in children - 6.1 hours. Clearance - 1.6-4.3 ml/kg/min, during pregnancy - 286 ml/min. It is excreted primarily by the kidneys by glomerular filtration. Upon repeated administration, it accumulates (associated with accumulation in adipose tissue).

Indications:

General anesthesia for short-term surgical interventions;
introductory and basic general anesthesia (followed by the use of analgesics and muscle relaxants);
relief of convulsive conditions observed during or after inhalation anesthesia;
relief of grand mal seizures, status epilepticus;
prevention of cerebral hypoxia (during artificial circulation, carotid endarterectomy And neurosurgical operations on the vessels of the brain);
narcoanalysis and narcosynthesis in psychiatry.

Contraindications:

Hypersensitivity to thiopental and other barbiturates;
acute intoxication with alcohol, sleeping pills, narcotic analgesics and drugs for general anesthesia;
diseases that are a contraindication for general anesthesia, status asthmaticus, shock. malignant hypertension;
porphyria, including acute intermittent (including a history of the patient or his immediate family).

With caution:

Hepatic and/or renal failure, diabetes mellitus, obesity, cachexia, adrenal insufficiency, myxedema, chronic obstructive pulmonary disease, bronchial asthma, heavy cardiovascular failure, pronounced violations contractile function myocardium, cardiovascular diseases, arterial hypotension, collapse, hypovolemia, excessive

premedication, myasthenia gravis, myotonia, muscular dystrophy, sepsis, inflammatory diseases of the nasopharynx, febrile conditions, anemia, childhood.

Pregnancy and lactation:

The use of Thiopental during pregnancy and lactation is possible if the expected benefit to the mother outweighs the potential risk to the fetus or infant. When using thiopental during lactation, you must refrain from breastfeeding for 24 hours after administration of the drug.

Directions for use and dosage:

For intravenous administration only.

The drug should be administered slowly to avoid a sharp drop in blood pressure and the development of collapse.

The dose of Thiopental is selected individually taking into account the patient’s body weight, concomitant diseases. Before administration, premedication with atropine or metacin is performed.

In adults, the dose for general anesthesia is usually 200-400 mg (50-100 mg at intervals of 30-40 seconds or once at a rate of 3-5 mg/kg body weight). To assess individual sensitivity to Thiopental, before administering the main dose, a test dose of 25 to 75 mg should be administered followed by observation for 60 seconds. To maintain anesthesia - 50-100 mg. Average dose for short operations it is 400 - 800 mg.

The maximum dose should not exceed 1 g (risk of accumulation).

To relieve seizures, 75 - 125 mg of Thiopental is administered intravenously over 10 minutes; for secondary convulsions during the administration of local anesthetics - 125 - 250 mg. Narcoanalysis and narcosynthesis: 100 mg intravenously over 1 minute. Patients should count down slowly, starting from 100. Thiopental should be discontinued when the patient begins to fall asleep. Patients should be half asleep and able to answer questions.

For general anesthesia in children, Thiopental is administered once at a rate of 3-5 mg/kg body weight (intravenously slowly, over 3-5 minutes); in children weighing 30-50 kg - at the rate of 4-5 mg/kg. Maintenance dose - 25-50 mg.

Before inhalation anesthesia without previous premedication, the drug is used in the following dosage: newborns - 3-4 mg/kg, children aged 1 to 12 months - 5-8 mg/kg, from 1 year to 12 years - 5-6 mg/kg. kg.

For patients with impaired renal function (creatinine clearance less than 10 ml/min), 75% of the average dose is administered.

Preparation of solutions.

The drug is used in the form of a 2.5-5% solution in water for injection, which is prepared immediately before use. Solutions must be absolutely transparent. When using solutions with a concentration of less than 2%, hemolysis may develop (with rapid administration).

Concentrations for clinical use are calculated as follows:

Required concentration in %	Concentration in mg/ml	Required quantity
		Thiopental (g)	For injection (ml)

Side effects:

Allergic reactions: skin hyperemia, skin rashes and itching; rarely - anaphylactic shock, hemolytic anemia with impaired renal function (pain in the lower back, legs and stomach, nausea, vomiting, loss of appetite, unusual weakness, fever, pallor skin).

From the outside cardiovascular system: decreased blood pressure, tachycardia, arrhythmia; with rapid administration, collapse may develop.

From the outside respiratory system: cough, sneezing, hypersecretion of bronchial mucus, laryngospasm, bronchospasm, pulmonary hypoventilation; due to too rapid administration, depression is possible respiratory center and apnea.

From the outside nervous system: headache, muscle twitching, epileptic seizures, dizziness, lethargy, ataxia, anterograde amnesia, drowsiness in postoperative period, anxiety (especially with pain in the postoperative period), increased tone vagus nerve; rarely - postoperative delirious psychosis (back pain, anxiety, confusion, agitation, hallucinations, anxiety, syndrome " restless legs"), radial nerve palsy.

From the outside digestive system: hypersalivation, hiccups, nausea,

abdominal pain in the postoperative period; rarely - vomiting.

Local reactions: with intravenous administration - pain at the injection site, thrombophlebitis (administration of solutions with high concentration drug), vascular spasm and thrombosis at the injection site, tissue irritation at the injection site (hyperemia and peeling of the skin), necrosis.

Overdose:

Symptoms: depression of the central nervous system, seizures, muscle

hyperreactivity, respiratory depression up to apnea, laryngospasm, water-electrolyte disturbances, marked decrease in blood pressure, tachycardia; post-anesthesia delirium. With a very large dose: pulmonary edema, circulatory collapse, cardiac arrest.

Treatment. The antidote is bemegride. If breathing stops - artificial pulmonary ventilation (ALV), 100%; for laryngospasm - muscle relaxants and 100% under pressure; in case of collapse or a pronounced decrease in blood pressure - plasma-substituting solutions, administration of vasopressor drugs and/or drugs with a positive inotropic effect. For convulsions - intravenous administration of diazepam or phenytoin; if they are ineffective, use mechanical ventilation and muscle relaxants.

Thiopental excretion can be enhanced by forced diuresis, peritoneal or hemodialysis.

Interaction:

Thiopental reduces the activity of glucocorticosteroids, hormonal contraceptives, indirect anticoagulants, griseofulvin, phenylbutazone, phenazone, phenytoin; increases the toxicity of methotrexate. Shows antagonism with bemegride.

Enhances the effect medicines, contributing to the development of hypothermia. Mutual enhancement of action is observed when joint use with ethanol, tranquilizers, antipsychotics, antihistamines and other drugs that inhibit the function of the central nervous system. The effect of Thiopental is enhanced and prolonged by valproic acid and MAO inhibitors.

Opioid analgesics reduce the strength of the analgesic effect of Thiopental.

Ketamine increases the risk of low blood pressure and respiratory depression. Diazoxide increases the risk of low blood pressure.

Simultaneous use with magnesium sulfate (for parenteral administration) is accompanied by an increased inhibitory effect on the central nervous system; With antihypertensive drugs and diuretics - enhancing the hypotensive effect.

Thiopental is pharmaceutically incompatible (cannot be mixed in the same syringe) with antibiotics (, cephalosporins), narcotic analgesics (,), ephedrine, muscle relaxants (suxamethonium, tubocurarine), tranquilizers, phenothiazine, epinephrine, ascorbic acid, dipyridamole, chlorpromazine, ketamine, atropine, scopolamine and tubocurarine chloride.

Chemically incompatible with solutions containing low values pH, and with oxidizing agents. Drugs that block tubular secretion (probenecid) and H1-histamine blockers enhance the effect: aminophylline, analeptics, and some antidepressants weaken the effect.

Diazoxide increases the risk of low blood pressure.

Special instructions:

Use only in a specialized department anesthesiologists-resuscitators, if available necessary funds to maintain cardiac activity, ensure patency respiratory tract and the possibility of performing mechanical ventilation. It should be borne in mind that achieving and maintaining general anesthesia of the required depth and duration depend on both the amount of the drug and the individual sensitivity of the patient to it.

Premedication should be carried out with any of the generally accepted agents, with the exception of phenothiazine derivatives.

At inflammatory diseases upper respiratory tract, it is indicated to ensure patency of the upper respiratory tract, up to tracheal intubation.

The dose should be reduced in patients taking diuretics, in patients who received diuretics as premedication, as well as after the administration of atropine, diazepam. In obese patients, as well as in patients who have already undergone general anesthesia within the last 36 hours, more than one may be sufficient to achieve the required depth of anesthesia. low doses Thiopental.

During prolonged anesthesia, when hypnotic effect induced by sodium thiopental is supported intravenous use anesthetics long acting and/or inhalational anesthetics, due to the danger of a cumulative effect, the dose of sodium thiopental should not exceed 1 g.

In the case of intravenous jet administration to children under 18 years of age, careful monitoring of the patient’s condition is necessary in order to timely identify symptoms of respiratory depression, hemolysis, and decreased blood pressure.

Can be used in combination with muscle relaxants, subject to mechanical ventilation.

In patients with severe alcohol and drug dependence, it is difficult to achieve general anesthesia with the isolated use of thiopental and additional agents for general anesthesia may be required.

Unintentional intra-arterial (i.a.) injection causes instant spasm of the vessel, accompanied by circulatory disturbances distal to the injection site (thrombosis of the main vessel with subsequent development of necrosis and gangrene is possible). The first sign of it in conscious patients: complaints of a burning sensation spreading along the artery; in patients under general anesthesia, the first symptoms are transient pallor, patchy cyanosis, or dark discoloration of the skin. Treatment: stop administration, inject a heparin solution into the lesion site, followed by anticoagulant therapy; glucocorticosteroid solution followed by systemic therapy; perform a sympathetic block or a brachial block nerve plexus(injection of procaine).

In case of chemical irritation of tissues (associated with high value pH of the solution (10-11) if the solution gets under the skin, in order to quickly resolve the infiltrate, inject local anesthetic and carry out warming (activation of local blood circulation). A sign of extravasation is subcutaneous swelling.

Impact on the ability to drive vehicles. Wed and fur.:

After outpatient use, patients should go out only with an accompanying person and be careful for 24 hours when driving vehicles and engaging in other potentially dangerous activities. dangerous species activities that require increased concentration and speed of psychomotor reactions.

Release form/dosage:

0.5 g or 1.0 g of powder for the preparation of a solution for intravenous administration in bottles;

Information update date: 09.09.2015 Illustrated instructions

Gross formula

C11H17N2O2SNa

Pharmacological group of the substance Sodium thiopental

Nosological classification (ICD-10)

CAS Code

71-73-8

Characteristics of the substance Sodium thiopental

Dry porous mass or powder of yellowish (yellowish-greenish) color with a peculiar odor. Easily soluble in water. Aqueous solutions have an alkaline reaction (pH about 10.0), are not stable (prepare immediately before use).

Pharmacology

Pharmacological action- anticonvulsant, anesthetic, hypnotic.

Prolongs the period of opening of GABA-dependent channels on the postsynaptic membrane of brain neurons, lengthens the time of entry of chlorine ions inside nerve cell and causes hyperpolarization of the membrane. In large doses, it has a GABA-mimetic effect (directly activates GABA A receptors) and suppresses the effects of excitatory amino acids (aspartate and glutamate).

Increases the threshold of neuronal excitability and blocks the conduction and propagation of convulsive impulses throughout the brain (anticonvulsant activity). Suppresses polysynaptic reflexes and slows down conduction interneurons spinal cord, promoting muscle relaxation. Reduces metabolic processes in the brain, the brain's utilization of glucose and oxygen. The hypnotic effect is manifested by accelerating the process of falling asleep and changing the structure of sleep. Depresses the respiratory center and reduces its sensitivity to carbon dioxide. Causes cardiodepression. Reduces stroke volume, cardiac output and blood pressure, increases the capacity of the venous bed; reduces hepatic blood flow and glomerular filtration rate.

After intravenous administration, it quickly penetrates into the brain and well-supplied blood (skeletal muscles, kidneys, liver) and adipose (concentration in fat depots is 6-12 times higher than plasma) tissue. Plasma protein binding - 80-86%; passes through the placental barrier and is secreted into breast milk. T 1/2 in the distribution phase - 5-9 minutes. It undergoes biotransformation in the liver with the formation of inactive metabolites (a small part is inactivated in the kidneys and brain). Elimination T1/2 is 10-12 hours. It is excreted mainly by the kidneys.

After intravenous administration, the effect develops after 40 s, and with rectal administration - after 8-10 minutes; Duration of anesthesia is up to 15 minutes. With repeated administration, the effect is prolonged (cumulates).

Application of the substance Sodium Thiopental

IV anesthesia for short-term surgical interventions, introductory and basic anesthesia with balanced anesthesia using analgesics and muscle relaxants, grand mal seizures, status epilepticus, increased intracranial pressure, prevention of brain hypoxia in traumatic brain injuries.

Contraindications

Hypersensitivity, bronchial asthma, status asthmaticus, liver and kidney dysfunction, impaired myocardial contractile function, severe anemia, shock and collaptoid conditions, myasthenia gravis, myxedema, Addison's disease, fever, inflammatory diseases of the nasopharynx, porphyria, pregnancy.

Use during pregnancy and breastfeeding

Side effects of sodium thiopental

Arrhythmia, hypotension, respiratory depression or arrest, laryngospasm, bronchospasm, nausea, vomiting; drowsiness, headache, chills, heart failure, rectal irritation and bleeding (with rectal administration), allergic reactions: urticaria, skin rashes and itching, anaphylactic shock.

Interaction

Enhances the effect of antihypertensive and hypothermic drugs, depresses the central nervous system under the influence of alcohol, sedatives, sleeping pills, ketamine, antipsychotics, magnesium sulfate. Activity is increased by probenecid and H1-blockers; weakened by aminophylline, analeptics and some antidepressants.

Pharmaceutically incompatible (cannot be mixed in the same syringe) with antibiotics (amikacin, benzylpenicillin, cephapirin), tranquilizers, muscle relaxants (suxamethonium, tubocurarine), analgesics (codeine), ephedrine, ascorbic acid, dipyridamole, chlorpromazine and ketamine.

Overdose

Symptoms: respiratory depression up to apnea, laryngospasm, hypotension, tachycardia, cardiac arrest, pulmonary edema; post-anesthesia delirium.

Treatment: bemegride (specific antagonist). If breathing stops - mechanical ventilation, 100% oxygen; laryngospasm - muscle relaxants and 100% oxygen under pressure; hypotension - plasma replacement solutions, hypertensive drugs.

Many surgical treatments require general anesthesia(anesthesia). During general anesthesia, pain sensitivity is temporarily switched off and relaxation occurs. muscle fibers, a person plunges into medicated sleep. This effect is impossible without narcotic analgesics acting at the level of the central nervous system. Currently, anesthesiology has wide choice drugs for anesthesia, with in different ways delivery and duration. Sodium thiopental is often used for anesthesia.

Means for non-inhalation anesthesia

Sodium thiopental belongs to the group of barbituric acid derivatives and is used for short-term non-inhalation anesthesia. The action of the drug is realized through the activation of GABA receptors in the neurons of the brain, resulting in an analgesic, hypnotic effect and muscle relaxation.

Sodium thiopental is administered intravenously; in children, the rectal route is also used. The drug is used in different concentrations and doses, in accordance with individual characteristics patient, maximum permissible single dose the drug is 1 gram. The drug is used for mononarcosis during short-term operations and in combination with other anesthetics during long operations. In combined anesthesia, sodium thiopental can be used as an induction agent.

The drug is rarely used as a basic anesthesia, since its duration of action does not exceed twenty minutes, therefore, for extensive operations, an additional dose of anesthetic is required during the process. surgical intervention, which in some cases can lead to uncontrollability of anesthesia. Only an experienced anesthesiologist can perform maintenance anesthesia with sodium thiopental.

Intravenous anesthesia

How does barbiturate anesthesia proceed?

When administered intravenously, the drug quickly reaches the brain and shows its effect within five seconds. The patient falls asleep quickly and easily. Anesthesia reaches within three minutes surgical stage allowing operations to be carried out. At this time, the patient’s eye movements stop, the pupils narrow slightly, the pharyngeal and corneal reflex are absent, and the tongue sinks. With a single dose, the duration of anesthesia is no more than half an hour. After recovery from anesthesia, the effect of the drug, including the analgesic effect, ceases immediately.

Complications of anesthesia using sodium thiopental

From the cardiovascular system. Sodium thiopental can provoke the development of arrhythmia, sharp decline blood pressure, depress cardiac activity.
From the respiratory system. Sodium thiopental depresses breathing and may cause laryngospasm.
Gastrointestinal tract: hypersalivation, nausea and vomiting, loss of appetite, hiccups.
Peripheral vascular system: phlebitis.

Contraindications and restrictions on the use of the drug

Sodium thiopental has a number of contraindications for use

In the blood, sodium thiopental is eighty to eighty-five percent bound to plasma proteins, providing the main effect due to fifteen percent of the free fraction, therefore, with severe exhaustion or other diseases in which the level of protein in the blood is reduced, the free fraction may increase, enhancing the effect of the drug, up to the development of overdose and toxic effect.

Sodium thiopental is utilized by the liver and excreted by the kidneys; dysfunction of these organs can also lead to an increase in the effect of the drug, therefore the drug is not used for liver and kidney failure.

Barbituric acid preparations, which include sodium thiopental, depress breathing during anesthesia and therefore are used only in conditions where there is a connection artificial ventilation lungs. Relative contraindication to anesthesia with sodium thiopental are chronic obstructive pulmonary diseases(bronchial asthma and COPD).

Also, the drug is not used for:

diseases of the nasopharynx;
diabetes mellitus;
circulatory disorders;
heart failure;
states of shock;
severe hypotension;
fever.

Other uses of Thiopental

Sodium thiopental, due to its pronounced anticonvulsant effect, used to relieve convulsive disorders after the use of local anesthetics and for epileptic seizures. For this purpose, the drug is administered at a dose of 75–125 mg intravenously. It is important to begin treatment as soon as possible after the onset of seizures. The drug is also used to reduce intracranial pressure in patients on mechanical ventilation.

In some US states, since 2009, sodium thiopental in a lethal dose has been used for death penalty. In Russia, the drug is used in veterinary medicine to euthanize animals.

Anesthesiology

Code in 1C

Name

Powder for the preparation of solution for intravenous administration 0.5 g, 1.0 g

Residue storage unit

Pharmacotherapeutic group

means for non-inhalation general anesthesia. The drug belongs to list No. 1 of potent substances of the Standing Committee for Drug Control of the Ministry of Health of the Russian Federation.

Trade name

Sodium thiopental

International nonproprietary name

Sodium thiopental

Dosage form

Powder for the preparation of solution for intravenous administration

Compound

Active substance: sodium thiopental - 0.5 g, 1 g.

ATX code

Pharmacological properties

Pharmacodynamics

An ultra-short-acting non-inhalation general anesthesia agent, a derivative of thiobarbituric acid. It has a pronounced hypnotic, some muscle relaxant and weak analgesic activity. Slows down the opening time of GABA-dependent channels on the postsynaptic membrane of brain neurons, lengthens the time of entry of chlorine ions into the nerve cell and causes hyperpolarization of the membrane. Suppresses the stimulating effect of amino acids (aspartate and glutamate). In large doses, directly activating GABA receptors, it has a GABA-stimulating effect. It has anticonvulsant activity, increasing the threshold of neuronal excitability and blocking the conduction and spread of convulsive impulses throughout the brain. Promotes muscle relaxation by suppressing polysynaptic reflexes and slowing down conduction along interneurons of the spinal cord. Reduces the intensity of metabolic processes in the brain, the brain's utilization of glucose and oxygen. It has a hypnotic effect, which is manifested by accelerating the process of falling asleep and changing the structure of sleep. Inhibits (dose-dependently) the respiratory center and reduces its sensitivity to carbon dioxide. It has a (dose-dependent) cardiodepressive effect: it reduces stroke volume, minute blood volume, and blood pressure. Increases capacity venous system, reduces hepatic blood flow and glomerular filtration rate. It has a stimulating effect on the n.vagus and can cause laryngospasm and copious secretion of mucus. After intravenous administration, general anesthesia develops within 30-40 seconds; after rectal - after 8-10 minutes, characterized by short duration (after administration of a single dose, general anesthesia lasts 10-30 minutes) and awakening with some drowsiness and retrograde amnesia. Upon recovery from general anesthesia, the analgesic effect ceases simultaneously with the patient's awakening.

Pharmacokinetics

When administered intravenously, it quickly penetrates into the brain, skeletal muscles, kidneys, liver and adipose tissue. The time for maximum concentration to occur is within 30 seconds (brain), 15-30 minutes (muscles). In fat depots, the concentration of the drug is 6-12 times higher than in blood plasma. Volume of distribution - 1.7-2.5 l/kg, during pregnancy - 4.1 l/kg, in obese patients - 7.9 l/kg. Communication with plasma proteins - 76-86%. Penetrates the placental barrier and is excreted breast milk. Metabolized mainly in the liver, with the formation of inactive metabolites, 3-5% of the dose is desulfurized to pentobarbital, a small part is inactivated in the kidneys and brain. The half-life in the distribution phase is 5-9 minutes, in the elimination phase - 3-8 hours (possibly extended to 10-12 hours; during pregnancy - up to 26.1 hours, in obese patients - up to 27.5 hours), in children - 6.1 h. Clearance - 1.6-4.3 ml/kg/min, during pregnancy - 286 ml/min. It is excreted primarily by the kidneys by glomerular filtration. Upon repeated administration, it accumulates (associated with accumulation in adipose tissue).

Indications for use

General anesthesia for short-term surgical interventions, introductory and basic general anesthesia (followed by the use of analgesics and muscle relaxants).
Grand mal seizures (grand mal), status epilepticus, increased intracranial pressure, prevention of cerebral hypoxia (during artificial circulation, carotid endarterectomy, neurosurgical operations on cerebral vessels), drug analysis and drug synthesis in psychiatry.

Contraindications

Increased sensitivity to the components of the drug; porphyria, including acute intermittent (including a history of the patient or his immediate family); diseases that are a contraindication for general anesthesia; intoxication with ethanol, narcotic analgesics, sleeping pills and drugs for general anesthesia; shock, status asthmaticus, malignant hypertension, pregnancy, lactation.

Use during pregnancy

Use during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus.
It is recommended to stop breast-feeding if necessary, prescribe the drug.

Directions for use and doses

Intravenously slowly (to avoid collapse), in adults use 2-2.5% solutions (less often 5% solution - a fractional administration technique is used); children and weakened elderly patients - 1% solution.
Solutions are prepared immediately before use using sterile water for injection. The prepared solution must be absolutely transparent. With rapid administration of solutions with a concentration of less than 2%, hemolysis may develop. Before administration, premedication with atropine or metacin is performed.
Adults for introduction to general anesthesia: test dose - 25-75 mg, followed by observation for 60 seconds before administering the main dose. Introductory general anesthesia - 200-400 mg (50-100 mg at intervals of 30-40 seconds until the desired effect is achieved or once at a rate of 3-5 mg/kg). To maintain anesthesia - 50-100 mg.
To relieve seizures - 75-125 mg intravenously over 10 minutes; development of seizures with local anesthesia- 125-250 mg over 10 minutes.
In case of brain hypoxia, 1.5-3.5 mg/kg is administered over 1 minute until blood circulation is temporarily stopped.
Narcoanalysis - 100 mg over 1 minute. Invite the patient to slowly count from 100 to 1. Interrupt the administration of thiopental immediately before falling asleep. The patient must remain half-awake and remain able to answer questions.
In case of impaired renal function (creatinine clearance less than 10 ml/min) - 75% of the average dose.
The highest single dose of the drug for adults intravenously is 1 g (50 ml of 2% solution).
The solution should be administered intravenously slowly, at a rate of no more than 1 ml/min. At first, 1-2 ml is usually injected, and after 20-30 seconds the remaining amount is administered.
For children - intravenously in a stream, slowly over 3-5 minutes, once at a rate of 3-5 mg/kg. Before inhalation anesthesia without previous premedication in newborns - 3-4 mg/kg, 1-12 months - 5-8 mg/kg, 1-12 years - 5-6 mg/kg; for general anesthesia in children weighing 30-50 kg - 4-5 mg/kg. Maintenance dose - 25-50 mg. In children with decreased renal function (creatinine clearance less than 10 ml/min) - 75% of the average dose.

Side effect

From the cardiovascular system: decreased blood pressure, arrhythmia, tachycardia, collapse.
From the respiratory system: cough, sneezing, hypersecretion of bronchial mucus, laryngospasm, bronchospasm, pulmonary hypoventilation, dyspnea, depression of the respiratory center, apnea.
From the nervous system: headache, muscle twitching, epileptic seizures, increased tone of the n.vagus, dizziness, lethargy, ataxia, anterograde amnesia, drowsiness in the postoperative period, anxiety, especially with pain in the postoperative period, rarely - postoperative delirious psychosis (pain in the back, anxiety, confusion, agitation, hallucinations, restlessness, restless legs syndrome), radial nerve palsy.
From the digestive system: hypersalivation, nausea, vomiting, abdominal pain in the postoperative period.
Allergic reactions: skin hyperemia, rash, itchy skin, urticaria, rhinitis, anaphylactic shock, rarely - hemolytic anemia with impaired renal function (pain in the lower back, legs and stomach, nausea, vomiting, loss of appetite, unusual weakness, fever, pale skin).
Other: hiccups.
Local reactions: with intravenous administration - pain at the injection site, thrombophlebitis (administration of solutions with a high concentration of the drug), vascular spasm and thrombosis at the injection site, tissue irritation at the injection site (hyperemia and peeling of the skin), necrosis; damage to the nerves approaching the injection site.

Overdose

Use with other drugs

Symptoms: depression of the central nervous system, convulsions, muscle hyperreactivity, respiratory depression up to apnea, laryngospasm, water and electrolyte disturbances, a pronounced decrease in blood pressure, a decrease in total peripheral vascular resistance (the toxic effect of an overdose begins from the first seconds), tachycardia; post-anesthesia delirium. At very high dose: pulmonary edema, circulatory collapse, cardiac arrest.
Treatment: antidote - bemegride. If breathing stops - artificial ventilation, 100% oxygen; for laryngospasm - muscle relaxants and 100% oxygen under pressure; in case of collapse or a pronounced decrease in blood pressure - plasma-substituting solutions, administration of vasopressor drugs and/or drugs with a positive inotropic effect. For convulsions - intravenous administration of diazepam; if they are ineffective - artificial ventilation and muscle relaxants.

Special instructions

Use only in a specialized department by anesthesiologists-resuscitators, in the presence of means to maintain cardiac activity and ensure airway patency, artificial ventilation. It should be borne in mind that achieving and maintaining general anesthesia of the required depth and duration depends on both the amount of the drug and the individual sensitivity of the patient to it.
For inflammatory diseases of the upper respiratory tract, it is indicated to ensure patency of the upper respiratory tract, up to tracheal intubation.
Unintentional intra-arterial injection causes instant spasm of the vessel, accompanied by impaired circulation distal to the injection site (thrombosis of the main vessel with subsequent development of necrosis and gangrene is possible). The first sign of it in conscious patients: complaints of a burning sensation spreading along the artery; in patients under general anesthesia, the first symptoms are transient pallor, patchy cyanosis, or dark discoloration of the skin.
Treatment: stop administration, inject intra-arterial heparin solution into the lesion site, followed by anticoagulant therapy; glucocorticosteroid solution followed by systemic therapy; perform a sympathetic block or a brachial plexus block (intra-arterial administration of procaine).
In case of chemical irritation of tissues (associated with a high pH value of the solution (10-11), if the solution gets under the skin, in order to quickly resolve the infiltrate, a local anesthetic is administered and warming is carried out (activation of local blood circulation).
A sign of extravasation is subcutaneous swelling.
In the case of intravenous jet administration to children under 18 years of age, careful monitoring of the patient’s condition is necessary in order to promptly identify symptoms of respiratory depression, hemolysis, decreased blood pressure, and extravasation.
The anesthetic effect is unreliable in ethanol abusers.
The dose should be reduced in patients taking digoxin and diuretics; in patients who received morphine as premedication, as well as after the administration of atropine and diazepam.
Premedication - any of the generally accepted drugs, with the exception of phenothiazine derivatives.
During prolonged anesthesia, when the hypnotic effect caused by sodium thiopental is maintained by intravenous use of long-acting anesthetics and/or inhalational anesthetics, due to the danger of a cumulative effect, the dose of sodium thiopental should not exceed 1 g.
Can be used in combination with muscle relaxants, subject to artificial ventilation.
Increases n.vagus tone, so an adequate dose of atropine should be administered before use. Immediately after the onset of general anesthesia, it is necessary to ensure patency of the airway. Habituation may develop.
Thiopental does not affect the tone of the pregnant uterus. After intravenous administration, the maximum concentration in the umbilical cord is observed after 2-3 minutes. The maximum permissible dose is 250 mg. When used in obstetric and gynecological surgery, it can cause depression of the central nervous system in newborns.

Dosage form: powder for the preparation of solution for intravenous administration Compound:

Active substance: sodium thiopental - 0.5 g, 1 g.

Description: The powder is white or almost white or yellowish-white to pale greenish-yellow. Hygroscopic. Pharmacotherapeutic group:Means for non-inhalation general anesthesia ATX:

N.01.A.F Barbiturates

N.01.A.F.03 Sodium thiopental

Pharmacodynamics:

Ultra-short-acting non-inhalation general anesthesia agent, derivative of thiobarbituric acid. Has a pronounced hypnotic effect,some muscle relaxant and weak analgesic activity. Slows downthe opening time of GABA-dependent channels on the postsynaptic membrane of brain neurons, prolongs the time of entry of chloride ions into the nerve cell and causes hyperpolarization of the membrane.

Suppresses the stimulating effect of amino acids (aspartate and glutamate).

In large doses, directly activating GABA receptors, it has a GABA-stimulating effect.

Has anticonvulsant activity, increasing the threshold of excitability neurons and blocking the conduction and propagation of the convulsive impulse throughout the brain.

Promotes muscle relaxation by suppressing polysynaptic reflexes and slowing down conduction along interneurons of the spinal cord.

Reduces the intensity of metabolic processes in the brain, the brain's utilization of glucose and oxygen.

It has a hypnotic effect, which is manifested by accelerating the process of falling asleep and changing the structure of sleep.

Inhibits (dose-dependently) the respiratory center and reduces its sensitivity to carbon dioxide.

It has a (dose-dependent) cardiodepressive effect: it reduces stroke volume, minute blood volume, and blood pressure.

Increases the capacity of the venous system, reduces hepatic blood flow and glomerular filtration rate.

It has a stimulating effect on the n.vagus and can cause laryngospasm and copious secretion of mucus.

After intravenous administration, general anesthesia develops within 30-40 seconds; after rectal - after 8-10 minutes, characterized by short duration (after administration of a single dose, general anesthesia lasts 10-30 minutes) and awakening with some drowsiness and retrograde amnesia. Upon recovery from general anesthesia, the analgesic effect ceases simultaneously with the patient's awakening. Pharmacokinetics:

Metabolized mainly in the liver, with the formation of inactive metabolites, 3-5% of the dose is desulfurized to pentobarbital, a small part is inactivated in the kidneys and brain.

The half-life in the distribution phase is 5-9 minutes, in the elimination phase - 3-8 hours (possibly extended to 10-12 hours; during pregnancy - up to 26.1 hours, in obese patients - up to 27.5 hours), in children - 6.1 hours. Clearance - 1.6-4.3 ml/kg/min, during pregnancy - 286 ml/min.

It is excreted primarily by the kidneys by glomerular filtration.

Upon repeated administration, it accumulates (associated with accumulation in adipose tissue).

Indications:

General anesthesia for short-term surgical interventions, introductory and basic general anesthesia (followed by the use of analgesics and muscle relaxants).

Grand mal seizures ( grand mal), status epilepticus, increased intracranial pressure, prevention of cerebral hypoxia (during artificial circulation, carotid endarterectomy, neurosurgical operations on cerebral vessels), drug analysis and drug synthesis in psychiatry.

Contraindications:

Hypersensitivity to the components of the drug; porphyria, includingacute intermittent (including a history of the patient or his immediate family); diseases that are a contraindication for general anesthesia; intoxication with ethanol, narcotic analgesics, sleeping pills and drugs for general anesthesia; shock, status asthmaticus, malignant hypertension, pregnancy, lactation.

With caution:

Chronic obstructive pulmonary diseases, bronchial asthma, severe disorders of myocardial contractile function, severe cardiovascular failure, arterial hypotension, collapse, hypovolemia, excessive premedication, liver 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, childhood.

Pregnancy and lactation:

Use during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus.

Directions for use and dosage:

Solutions are prepared immediately before use using sterile water for injection. The prepared solution must be absolutely transparent. With rapid administration of solutions with a concentration of less than 2%, hemolysis may develop. Before administration, premedication with atropine or metacin is performed.

Adults for induction into general anesthesia : test dose - 25-75 mg, followed by observation for 60 seconds before administering the main dose. Introductory general anesthesia - 200-400 mg (50-100 mg at intervals of 30-40 seconds until the desired effect is achieved or once at a rate of 3-5 mg/kg). To maintain anesthesia - 50-100 mg.

To relieve seizures - 75-125 mg intravenously over 10 minutes; development of seizures with local anesthesia - 125-250 mg over 10 minutes.

With brain hypoxia 1.5-3.5 mg/kg is administered 1 minute before temporary circulatory arrest.

Narcoanalysis - 100 mg over 1 minute. Invite the patient to slowly count from 100 to 1. Interrupt the administration of thiopental immediately before falling asleep. The patient must remain half-awake and remain able to answer questions.

If kidney function is impaired

The highest single dose of the drug for adults intravenously is 1 g (50 ml of 2% solution).

The solution should be administered intravenously slowly, at a rate of no more than 1 ml/min.

At first, 1-2 ml is usually injected, and after 20-30 seconds the remaining amount is administered.

For children - intravenously in a stream, slowly over 3-5 minutes, once at a rate of 3-5 mg/kg.

Before inhalation anesthesia without previous premedication in newborns - 3-4 mg/kg, 1-12 months - 5-8 mg/kg, 1-12 years - 5-6 mg/kg; for general anesthesia in children weighing 30-50 kg - 4-5 mg/kg. Maintenance dose - 25-50 mg.

In children with decreased kidney function(creatinine clearance less than 10 ml/min) - 75% of the average dose.

Side effects:

From the cardiovascular system: decreased blood pressure, arrhythmia, tachycardia collapse.

From the respiratory system: cough, sneezing, hypersecretion of bronchial mucus, laryngospasm, bronchospasm, pulmonary hypoventilation, dyspnea, depression of the respiratory center, apnea.

From the nervous system: headache, muscle twitching, epileptic seizures, increased tone n.vagus, dizziness, lethargy, ataxia, anterograde amnesia, drowsiness in the postoperative period, anxiety, especially with pain in the postoperative period; rarely - postoperative delirious psychosis (back pain, anxiety, confusion, agitation, hallucinations, anxiety, restless legs syndrome), radial nerve palsy.

From the digestive system: hypersalivation, nausea, vomiting, abdominal pain in the postoperative period.

Allergic reactions: skin hyperemia, rash, itching, urticaria, rhinitis, anaphylactic shock; rarely - hemolytic anemia with impaired renal function (pain in the lower back, legs and stomach, nausea, vomiting, loss of appetite, unusual weakness, fever, pale skin).

Others: hiccups.

Local reactions: with intravenous administration - pain at the injection site, thrombophlebitis (administration of solutions with a high concentration of the drug), vascular spasm and thrombosis at the injection site, tissue irritation at the injection site (hyperemia and peeling of the skin), necrosis; damage to the nerves approaching the injection site.

Overdose:

Symptoms : depression of the central nervous system, convulsions, muscle hyperreactivity, respiratory depression up to apnea, laryngospasm, water and electrolyte disturbances, marked decrease in blood pressure, decrease in total peripheral vascular resistance (toxic effects in case of overdose begin from the first seconds), tachycardia; post-anesthesia delirium.

At very high doses: pulmonary edema, circulatory collapse, cardiac arrest.

Treatment: antidote - bemegride. If breathing stops - artificial ventilation, 100%; for laryngospasm - muscle relaxants and 100% under pressure; in case of collapse or a pronounced decrease in blood pressure - plasma-substituting solutions, administration of vasopressor drugs and/or drugs with a positive inotropic effect. For convulsions - intravenous administration of diazepam; if they are ineffective - artificial ventilation and muscle relaxants.

Interaction:

Combined use with ethanol and drugs that depress the central nervous system leads to mutual enhancement pharmacological action(both to significant depression of the central nervous system, respiratory function, increased hypotensive effect, and the degree of anesthesia); with magnesium sulfate - increased inhibitory effect on the central nervous system; with ganggioblockers, diuretics and other antihypertensive drugs - enhanced hypotensive effect of methotrexate - enhanced toxic effect the last one.

Reduces the effect of indirect anticoagulants (coumarin derivatives), griseofulvin, contraceptives, glucocorticosteroids.

Enhances the effect of drugs that promote the development of hypothermia.

Shows antagonism with bemegride.

Opioid analgesics reduce the strength of the analgesic effect.

Ketamine increases the risk of low blood pressure and respiratory depression, and prolongs the time to recovery from general anesthesia.

Medicines that block tubular secretion (probenecid) and H1-histamine blockers enhance the effect; , analeptics, some antidepressants - weaken.

Diazoxide increases the risk of low blood pressure.

Pharmaceutically incompatible with antibiotics (cefapirin), anxiolytic medicines (tranquilizers), muscle relaxants (, tubocurarinechloride), narcotic analgesics (,), ephedrine,epinephrine, ascorbic acid, dipyridamole, chlorpromazine,ketamine, atropine, scopolamine and tubocurarine chloride (should not bemix in one syringe and inject through one needle with acidic solutions).

Special instructions:

Use only in a specialized department by anesthesiologists-resuscitators, in the presence of means to maintain cardiac activity and ensure airway patency, artificial ventilation.

It should be borne in mind that achieving and maintaining general anesthesia of the required depth and duration depends on both the amount of the drug and the individual sensitivity of the patient to it.

For inflammatory diseases of the upper respiratory tract, it is indicated to ensure patency of the upper respiratory tract, up to tracheal intubation.

Unintentional intra-arterial injection causes instant spasm of the vessel, accompanied by impaired circulation distal to the injection site (thrombosis of the main vessel with subsequent development of necrosis and gangrene is possible). The first sign of it in conscious patients: complaints of a burning sensation spreading along the artery; in patients under general anesthesia, the first symptoms are transient pallor, patchy cyanosis, or dark discoloration of the skin.

Treatment : stop administration, inject intra-arterial heparin solution into the lesion site, followed by anticoagulant therapy; glucocorticosteroid solution followed by systemic therapy; perform a sympathetic block or a brachial plexus block (intra-arterial administration of procaine).

In case of chemical irritation of tissues (associated with a high pH value of the solution (10-11)), if the solution gets under the skin, in order to quickly resolve the infiltrate, a local anesthetic is administered and warming is carried out (activation of local blood circulation).

A sign of extravasation is subcutaneous swelling.

In the case of intravenous jet administration to children under 18 years of age, careful monitoring of the patient’s condition is necessary in order to promptly identify symptoms of respiratory depression, hemolysis, decreased blood pressure, and extravasation.

The anesthetic effect is unreliable in ethanol abusers.

The dose should be reduced in patients taking diuretics; in patients who received premedication, as well as after the administration of atropine, diazepam.

Premedication - any of the generally accepted drugs, with the exception of phenothiazine derivatives.

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

Can be used in combination with muscle relaxants, subject to artificial ventilation.

Increases tone n.vagus Therefore, an adequate dose of atropine should be administered before use.

Immediately after the onset of general anesthesia, it is necessary to ensure patency of the airway.

Habituation may develop.

Thiopental does not affect the tone of the pregnant uterus. After intravenous administration, the maximum concentration in the umbilical cord is observed after 2-3 minutes. The maximum permissible dose is 250 mg. When used in obstetric and gynecological surgery, it can cause depression of the central nervous system in newborns.

Impact on the ability to drive vehicles. Wed and fur.:

After outpatient use, patients should go outside only with an accompanying person and be careful when driving for 24 hours. vehicles and engage in potentially hazardous activities that require increased concentrated attention and speed of psychomotor reactions.

Release form/dosage:

Powder for solution for intravenous administration, 0.5 g and 1 g.

Package:

0.5 g active substance in bottles with a capacity of 10 ml or 20 ml, 1 g of the active substance in bottles with a capacity of 20 ml, hermetically sealed with rubber stoppers, crimped aluminum caps or combined aluminum caps with plastic caps.

1.5 or 10 bottles with instructions for use are placed in a cardboard pack.

50 bottles with 5 instructions for use are placed in a cardboard box for delivery to hospitals.

Storage conditions:

List No. 1 ADD. In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

The drug belongs to list No. 1 of potent substances of the Standing Committee for Drug Control M3 of the Russian Federation.

Best before date:

Do not use after expiration date.

Conditions for dispensing from pharmacies: By prescription Registration number: LS-000748 Registration date: 23.07.2010 / 11.04.2012 Expiration date: Indefinite Owner of the Registration Certificate:SINTEZ, JSC Kurgan joint-stock company medical supplies and products Russia Manufacturer: Representative office: SYNTHESIS OJSC Kurgan Joint-Stock Company of Medical Preparations and Products Russia Information update date: 12.11.2018 Illustrated instructions