Sodium thiopental dose. Sodium thiopental: instructions for use of the powder

Sodium thiopental is a pharmaceutical drug used for general anesthesia, also used in some other conditions. Especially for readers of “Popular about Health”, I will consider the description of this medicine.

So, the instructions for sodium thiopental:

What is sodium thiopental composition and form of release?

The active ingredient in the pharmaceutical preparation sodium thiopental is represented by the medicinal substance of the same name, the amount of which is 1000 or 500 milligrams in a vial. Sodium thiopental contains no excipients.

Sodium thiopental is available as a lyophilized hygroscopic powder. white-yellow color sold in vials of 20 or 10 milliliters. Pharmaceutical drug dispensed by prescription.

What is the effect of sodium thiopental?

The drug sodium thiopental is used as an anesthetic, anticonvulsant and sleeping pills. Pharmaceutical action of the drug is based on its ability to lengthen the closing period of GABA-dependent channels in the synapses of the central nervous system which leads to hyperpolarization of nerve cell membranes.

Hyperpolarization causes a significant increase in the threshold of excitability of neurons, which leads to the predominance of inhibition over excitation. This phenomenon contributes to the suppression of convulsive activity of the brain, the development of deep muscle relaxation, inhibits the activity of all metabolic reactions in the nervous system.

The hypnotic effect of the drug is expressed in reducing the time to fall asleep, preventing spontaneous nocturnal impulses. Under the influence of sodium thiopental, the patient becomes less sensitive to external stimuli.

The predominance of inhibition processes in the nervous system extends to most structures of the brain. Thus, the activity of the respiratory center is suppressed, by reducing its susceptibility to carbon dioxide.

Sodium thiopental is able to suppress cardiac activity, which is expressed in a decrease in cardiac output, slowing the pulse, increasing the volume of the venous bed and other cardiotropic effects.

When administered intravenously, the active substance quickly penetrates the central nervous system. The onset of general anesthesia is about 40 seconds, the duration is at least 15 minutes.

The maximum concentrations of sodium thiopental are determined in the following anatomical formations: kidneys, liver, skeletal muscles, adipose tissue. The active substance is determined in most biological fluids such as breast milk and amniotic fluid.

Sodium thiopental is rapidly metabolized in the human body. After 6 minutes, at least 50 percent of the administered dose is excreted. It is prone to cumulation, and because of this, repeated administration is accompanied by a longer anesthesia.

What are the indications for use of sodium thiopental?

In the indications of sodium thiopental, its annotation includes the following cases:

Administration of general anesthesia for surgical interventions or diagnostic procedures;

Relief of epileptic seizures;

Prevention of the development of hypoxic states of the brain in neuro surgical interventions.

The use of sodium thiopental should be carried out under constant supervision an experienced doctor and under conditions medical institution.

What are the contraindications for the use of thiopental sodium?

Instructions for use prohibit the use of the drug in the cases listed below:

Intolerance to the active ingredient;

Asthmatic status;

Shock conditions of any genesis;

malignant hypertension;

lactation period;

Intoxication with narcotic analgesics or alcohol.

Relative contraindications Sodium thiopental: severe malnutrition, fever, childhood, bronchial asthma, heavy cardiovascular failure, obstructive pulmonary disease, hepatic or kidney failure, inflammatory diseases of the nasopharynx.

What is the use and dosage of Thiopental Sodium?

The dosage of thiopental sodium is determined by the indications, as well as the age of the patient. Only water for injection should be used as a solvent. The solution is prepared immediately before use. Adult patients are prescribed a 2% solution, children - 1%.

For general anesthesia, 25-75 mg of the drug is administered. The total dose is 200 to 400 mg. The drug is administered fractionally, 50-100 mg every minute until the desired effect is achieved.

To suppress seizures, intravenous administration of 25–75 mg of sodium thiopental is prescribed. For the prevention of cerebral hypoxia - from one and a half to 3.5 mg per unit body weight of the patient.

Sodium thiopental - drug overdose

Overdose symptoms of sodium thiopental: convulsions, abnormal breathing, spasm of the larynx, decreased blood pressure, severe tachycardia, delirious state, respiratory and cardiac arrest.

The specific antidote is bemegride. When breathing stops, artificial ventilation of the lungs is indicated, vasoconstrictor drugs to increase blood pressure, correction electrolyte disturbances, anticonvulsant therapy.

What are thiopental sodium side effects ?

Side effects of sodium thiopental: arterial hypotension, drowsiness, muscle twitching, headaches, psychosis, nausea, vomiting, abdominal pain, skin rashes, anaphylactic shock thrombophlebitis, skin redness, muscle weakness.

How to replace sodium thiopental, what analogues does the drug have?

Pentotal, Thiopental-KMP are analogues of Thiopental sodium.

Conclusion

Anesthetic medicinal substances are used only in a stationary medical institution and under constant supervision by an experienced anesthesiologist.

Drug for non-inhalation anesthesia

Active substance

Thiopental sodium (thiopental sodium)

Release form, composition and packaging

Lyophilisate for solution for intravenous administration in the form of a white or almost white powder, or from yellowish white to pale greenish yellow, hygroscopic.

Vials of 10 ml (1) - packs of cardboard.
Vials of 10 ml (5) - packs of cardboard.
Vials of 10 ml (10) - packs of cardboard.
Vials of 10 ml (50) - packs of cardboard.
Vials of 20 ml (1) - packs of cardboard.
Vials of 20 ml (5) - packs of cardboard.
Vials of 20 ml (10) - packs of cardboard.
Vials of 20 ml (50) - packs of cardboard.

pharmachologic effect

Refers to the list of potent substances (list No. 1).

Means for non-inhalation general anesthesia of ultrashort action, a derivative of thiobarbituric acid. It has a pronounced hypnotic, and weak muscle relaxant and analgesic activity. Slows down the opening time of GABA-dependent channels on the postsynaptic membrane of brain neurons, lengthens the entry time of chloride ions inside nerve cell and causes membrane hyperpolarization. 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 excitability threshold of neurons and blocking the conduction and propagation of a convulsive impulse in the brain. Promotes muscle relaxation by suppressing polysynaptic reflexes and slowing down conduction through interneurons spinal cord. Reduces the intensity of metabolic processes in the brain. It has a hypnotic effect, which is manifested by accelerating the process of falling asleep and changing the structure of sleep. Oppresses (dose-dependently) the respiratory center and reduces its sensitivity to carbon dioxide. It has a (dose-dependent) cardiodepressive effect: it reduces stroke and minute blood volumes, blood pressure. Increases the capacity of the venous bed, reduces hepatic blood flow and glomerular filtration rate. It has an exciting effect on n.vagus and can cause laryngospasm, copious secretion of mucus. After intravenous administration general anesthesia develops in 30-40 seconds; after rectal - after 8-10 minutes, characterized by short duration (after a single dose, general anesthesia lasts 10-30 minutes) and awakening with some drowsiness and retrograde amnesia. When leaving general anesthesia, the analgesic effect ceases simultaneously with the awakening of the patient.

Pharmacokinetics

When administered intravenously, it quickly penetrates the brain, skeletal muscles, kidneys, liver and adipose tissue. The onset of Cmax - within 30 seconds (brain), 15-30 minutes (muscles). In fat depots, the concentration of the drug is 6-12 times higher than in the blood. V d -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%. Crosses the placental barrier and is excreted breast milk.

It is 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.

T 1 / 2 in the distribution phase - 5-9 minutes, in the elimination phase - 3-8 hours (it is possible to lengthen up to 10-12 hours; during pregnancy - up to 26.1 hours, in patients with obesity - 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 mainly by the kidneys by glomerular filtration. With repeated administration, it accumulates (associated with accumulation in adipose tissue).

Indications

- general anesthesia for short-term surgical interventions, introductory and basic general anesthesia (with subsequent use of muscle relaxants);

- large epileptic seizures(grand mal), status epilepticus;

- prevention of cerebral hypoxia (with cardiopulmonary bypass, neurosurgical operations).

Contraindications

- hypersensitivity;

- porphyria, including acute intermittent (including history in the patient or his immediate family);

- intoxication with ethanol, narcotic analgesics, sleeping pills and drugs for general anesthesia;

- status asthmaticus;

— malignant hypertension;

- lactation period.

Carefully: chronic obstructive pulmonary disease, bronchial asthma, pronounced violations contractile function of the myocardium, severe cardiovascular failure, arterial hypotension, collapse, hypovolemia, excessive premedication, liver and / or kidney failure, Addison's disease, myxedema, diabetes, anemia, myasthenia gravis, myotonia, muscular dystrophy, cachexia, febrile syndrome, inflammatory diseases of the nasopharynx, obesity, pregnancy, childhood.

Dosage

Intravenously slowly (to avoid collapse), in adults, 2-2.5% solutions are used (less often a 5% solution - the fractional administration method is used); children and debilitated elderly patients - 1% solution.

Solutions are prepared immediately before use.

The prepared solution must be absolutely transparent. With the rapid introduction of solutions with a concentration of less than 2%, hemolysis may develop. Before administration, premedication or metacin is carried out.

Adults for introduction to general anesthesia: trial dose - 25-75 mg, followed by observation for 60 seconds before the introduction of 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 the rate of 3-5 mg / kg). For maintenance of anesthesia- 50-100 mg.

For relief of seizures- 75-125 mg IV over 10 minutes; with the development of seizures local anesthesia-125-250 mg for 10 min.

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

At kidney dysfunction(CC less than 10 ml / min) - 75% of the average dose.

The highest single dose of the drug for adults in / in - 1 g (50 ml of a 2% solution).

The intravenous solution should be administered slowly, at a rate of no more than 1 ml / min. Initially, 1-2 ml is usually injected, and after 20-30 seconds, the rest of the amount.

children- in / 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. At children with decreased kidney function (CC less than 10 ml / min)- 75% of the average dose. The use of the drug for basic anesthesia is especially indicated in children with increased nervous excitability and in patients with thyrotoxicosis.

Side effects

From the side of cardio-vascular system: decrease in blood pressure, arrhythmia, tachycardia, collapse.

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

From the side of the nervous system : headache, muscle twitching, epileptic seizures, increased n.vagus tone, dizziness, lethargy, ataxia, anterograde amnesia, drowsiness in postoperative period, anxiety, especially with pain in the postoperative period; rarely - postoperative delirious psychosis.

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

allergic reactions: skin hyperemia, rash, pruritus, 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, pallor skin).

Others: hiccups.

Local reactions: when administered intravenously, pain at the injection site, thrombophlebitis (injection of solutions with a high concentration of the drug), vasospasm and thrombosis at the injection site, tissue irritation at the injection site (hyperemia and peeling of the skin), necrosis; nerve damage to the injection site.

Overdose

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 (toxic effect in overdose begins from the first seconds), tachycardia; postanesthesia delirium. At a very high dose: pulmonary edema, circulatory collapse, cardiac arrest.

Treatment: antidote - bemegrid. When breathing stops - artificial ventilation of the lungs, 100% oxygen; with laryngospasm - and 100% oxygen under pressure; with collapse or a pronounced decrease in blood pressure - plasma-substituting solutions, the introduction of vasopressor medicines and/or drugs with a positive inotropic effect. With convulsions - in / in the introduction of diazepam; with their inefficiency - mechanical ventilation and muscle relaxants.

drug interaction

Combined use with ethanol and drugs that depress the central nervous system leads to mutual reinforcement pharmacological action(both to a significant depression of the central nervous system, respiratory function, increased hypotensive effect, and the degree of anesthesia); c - increased inhibitory effect on the central nervous system; with gangioblockers, diuretics and other antihypertensive drugs - strengthening hypotensive action; methotrexate - amplification toxic action the last one.

Reduces action indirect anticoagulants(coumarin derivatives), griseofulvin, contraceptives, GCS.

Enhances the effect of drugs that promote the development of hypothermia. Shows antagonism with bemegrid.

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

Drugs that block tubular secretion (probenecid) and H 1 -histamine blockers enhance the effect; aminophylline, analeptics, some antidepressants - weaken.

Diazoxide increases the risk of lowering blood pressure.

Pharmaceutically incompatible with antibiotics (amikacin, benzylpenicillin, cefapirin), anxiolytic drugs (tranquilizers), muscle relaxants (suxamethonium, tubocurarine), narcotic analgesics (codeine, morphine), ephedrine, epinephrine, dipyridamole, chlorpromazine, ketamine, atropine, scopolamine and tubocurarine chloride (should not be mixed in the same syringe and administered through the same needle with acidic solutions).

special instructions

Use only in the conditions of a specialized department by anesthesiologists-resuscitators, if there are means to maintain cardiac activity and ensure patency respiratory tract, artificial ventilation lungs. It should be borne in mind that the achievement and maintenance of general anesthesia of the required depth and duration depends both on the amount of the drug and on the individual sensitivity of the patient to it.

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

Unintentional intra-arterial injection causes an instant spasm of the vessel, accompanied by circulatory disorders distal to the injection site (thrombosis of the main vessel is possible, followed by the development of necrosis, gangrene). The first sign of it in patients who are conscious: complaints of a burning sensation that spreads along the artery; in patients under general anesthesia, the first symptoms are transient blanching, patchy cyanosis, or dark skin coloration.

Treatment: stop the introduction; inject intra-arterially into the site of the lesion a solution of heparin, followed by anticoagulant therapy; glucocorticosteroid solution followed by systemic therapy; perform a sympathetic or shoulder block nerve plexus(intra-arterial introduction of rental).

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

In the case of intravenous jet administration, children under 18 years of age should carefully monitor the patient's condition in order to timely detect symptoms of respiratory depression, hemolysis, lowering blood pressure, extravasation.

The anesthetic effect is unreliable in persons who abuse alcohol.

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

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

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

It can be used in combination with muscle relaxants under the condition of artificial lung ventilation.

Sodium 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. Maximum allowable dose- 250 mg. When used in obstetric and gynecological surgery, it can cause CNS depression in newborns.

Pregnancy and lactation

In pregnant women, use the drug only if the intended benefit to the mother outweighs the potential risk to the fetus.

The drug is contraindicated during lactation.

Application in childhood

Use with caution in childhood.

Children - in / in a stream, slowly over 3-5 minutes, once at the 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 (CC less than 10 ml / min) - 75% of the average dose. The use of the drug for basic anesthesia is especially indicated in children with increased nervous excitability.

Anesthesiology

Code in 1C

Name

Powder for 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 the list No. 1 of potent substances of the Standing Committee for Drug Control of the Ministry of Health of the Russian Federation.

Tradename

Sodium thiopental

International non-proprietary name

Sodium thiopental

Dosage form

Powder for solution for intravenous administration

Compound

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

ATX Code

Pharmacological properties

Pharmacodynamics

Means for non-inhalation general anesthesia of ultrashort action, a derivative of thiobarbituric acid. It has a pronounced hypnotic, some muscle relaxant and weak analgesic activity. It slows down the opening time of GABA-dependent channels on the postsynaptic membrane of brain neurons, lengthens the entry time of chloride ions into the nerve cell and causes membrane hyperpolarization. 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 excitability threshold of neurons and blocking the conduction and spread of a convulsive impulse in the brain. It promotes muscle relaxation by suppressing polysynaptic reflexes and slowing down conduction through the intercalary neurons of the spinal cord. Reduces the intensity of metabolic processes in the brain, the utilization of glucose and oxygen by the brain. It has a hypnotic effect, which is manifested by accelerating the process of falling asleep and changing the structure of sleep. Oppresses (dose-dependently) the respiratory center and reduces its sensitivity to carbon dioxide. It has a (dose-dependent) cardiodepressive effect: it reduces stroke volume, minute volume of blood, and arterial pressure. Increases the capacity of the venous system, reduces hepatic blood flow and glomerular filtration rate. It has an exciting effect on n.vagus and can cause laryngospasm, copious secretion of mucus. After intravenous administration, general anesthesia develops in 30-40 seconds; after rectal - after 8-10 minutes, characterized by short duration (after a single dose, general anesthesia lasts 10-30 minutes) and awakening with some drowsiness and retrograde amnesia. When leaving general anesthesia, the analgesic effect ceases simultaneously with the awakening of the patient.

Pharmacokinetics

When administered intravenously, it quickly penetrates into the brain, skeletal muscles, kidneys, liver and adipose tissue. The time of onset of maximum concentration 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. The volume of distribution is 1.7-2.5 l / kg, during pregnancy - 4.1 l / kg, in patients with obesity - 7.9 l / kg. Communication with plasma proteins - 76-86%. Penetrates through the placental barrier and excreted in breast milk. It is 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 (it is possible to lengthen up to 10-12 hours; during pregnancy - up to 26.1 hours, in patients with obesity - 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 mainly by the kidneys by glomerular filtration. With 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 (with the subsequent use of analgesics and muscle relaxants).
Grand mal seizures, status epilepticus, increased intracranial pressure, prevention of cerebral hypoxia (with cardiopulmonary bypass, carotid endarterectomy, neurosurgical operations on cerebral vessels), drug analysis and narcosynthesis in psychiatry.

Contraindications

Hypersensitivity 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.

Application during pregnancy

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

Dosage and administration

Intravenously slowly (to avoid collapse), in adults, 2-2.5% solutions are used (less often a 5% solution - the fractional administration technique is used); children and debilitated elderly patients - 1% solution.
Solutions are prepared immediately before use in sterile water for injection. The prepared solution must be absolutely transparent. With the rapid introduction of solutions with a concentration of less than 2%, hemolysis may develop. Before administration, premedication with atropine or metacin is carried out.
Adults for general anesthesia: trial dose - 25-75 mg, followed by observation for 60 seconds before 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 the rate of 3-5 mg / kg). To maintain anesthesia - 50-100 mg.
For the relief of seizures - 75-125 mg intravenously for 10 minutes; the development of seizures with local anesthesia - 125-250 mg for 10 minutes.
In case of cerebral hypoxia, 1.5-3.5 mg/kg is administered for 1 minute until the blood circulation stops temporarily.
Drug analysis - 100 mg for 1 min. Invite the patient to slowly count from 100 to 1. Interrupt the administration of thiopental just before falling asleep. The patient should be semi-awake and 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 - 1 g (50 ml of a 2% solution).
The solution should be administered intravenously slowly, at a rate of no more than 1 ml / min. Initially, 1-2 ml is usually injected, and after 20-30 seconds, the rest of the amount.
Children - intravenously by stream, slowly over 3-5 minutes, once at the 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 side of the cardiovascular system: lowering blood pressure, arrhythmia, tachycardia, collapse.
From the respiratory system: cough, sneezing, hypersecretion of bronchial mucus, laryngospasm, bronchospasm, hypoventilation of the lungs, dyspnea, depression of the respiratory center, apnea.
From the nervous system: headache, muscle twitching, epileptic seizures, increased n.vagus tone, 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, syndrome restless legs), radial nerve palsy.
From the digestive system: hypersalivation, nausea, vomiting, abdominal pain in the postoperative period.
Allergic reactions: skin flushing, rash, pruritus, 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, pallor of the skin ).
Other: hiccups.
Local reactions: with intravenous administration - soreness at the injection site, thrombophlebitis (introduction of solutions with a high concentration of the drug), vasospasm and thrombosis at the injection site, tissue irritation at the injection site (hyperemia and peeling of the skin), necrosis; nerve damage to 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 (toxic effect in overdose begins from the first seconds), tachycardia; postanesthesia delirium. At a very high dose: pulmonary edema, circulatory collapse, cardiac arrest.
Treatment: antidote - bemegrid. When breathing stops - artificial ventilation of the lungs, 100% oxygen; with laryngospasm - muscle relaxants and 100% oxygen under pressure; with collapse or a pronounced decrease in blood pressure - plasma-substituting solutions, the introduction of vasopressor drugs and / or drugs with a positive inotropic effect. With convulsions - intravenous administration of diazepam; if they are ineffective - artificial ventilation of the lungs and muscle relaxants.

special instructions

Use only in the conditions of a specialized department by anesthesiologists-resuscitators, if there are means to maintain cardiac activity and ensure airway patency, artificial ventilation of the lungs. It should be borne in mind that the achievement and maintenance of general anesthesia of the required depth and duration depends both on the amount of the drug and on the individual sensitivity of the patient to it.
In inflammatory diseases of the upper respiratory tract, it is shown to ensure the patency of the upper respiratory tract, up to tracheal intubation.
Unintentional intra-arterial injection causes an instant spasm of the vessel, accompanied by circulatory disorders distal to the injection site (thrombosis of the main vessel is possible, followed by the development of necrosis, gangrene). The first sign of it in patients who are conscious: complaints of a burning sensation that spreads along the artery; in patients under general anesthesia, the first symptoms are transient blanching, patchy cyanosis, or dark skin coloration.
Treatment: stop the administration, inject intra-arterially into the site of the lesion a solution of heparin, followed by anticoagulant therapy; glucocorticosteroid solution followed by systemic therapy; conduct a sympathetic blockade or blockade of the brachial plexus (intra-arterial administration of procaine).
In case of chemical irritation of tissues (associated with a high pH value of the solution (10-11) in case of contact with the solution under the skin, a local anesthetic is administered in order to quickly resolve the infiltrate 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 timely detect symptoms of respiratory depression, hemolysis, lowering blood pressure, extravasation.
The anesthetic effect is unreliable in ethanol abusers.
The dose should be reduced in patients taking digoxin, diuretics; in patients who received morphine in premedication, as well as after the administration of atropine, diazepam.
Premedication - any of the conventional drugs, with the exception of phenothiazine derivatives.
With prolonged anesthesia, when the hypnotic effect caused by sodium thiopental is maintained by intravenous use 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.
It can be used in combination with muscle relaxants under the condition of artificial lung ventilation.
Increases the tone of n.vagus, so an adequate dose of atropine should be administered before use. Immediately after the onset of general anesthesia, it is necessary to ensure the patency of the airways. 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 allowable dose is 250 mg. When used in obstetric and gynecological surgery, it can cause depression of the central nervous system in newborns.

Among the various sleeping pills and painkillers of a narcotic nature special place occupies "Thiopental sodium". Instructions for using this serious strong drug of interest to many patients. What is this pharmacological agent? In what cases is its appointment justified? What is the mechanism of action of Sodium Thiopental and how should it be used? Can the drug cause side effects and what to do in case of an overdose? The answers to these questions are given by the instructions for the use of sodium thiopental.

Briefly about the drug

Before you buy the drug, you will need to take a prescription for sodium thiopental from your doctor. Latin. This tool has a strong narcotic effect, so it can not be purchased without a doctor's prescription.

What is a medication? On the pharmacological market, it is sold in the form of a light hygroscopic powder, from which a solution for intravenous administration can be prepared. The powder, one or half a gram, is packaged in glass bottles with a capacity of ten or twenty milliliters.

Briefly about the composition

The active component of the pharmacological agent is the substance of the same name - Thiopental sodium. This is how the name will be written in the recipe for “Sodium Thiopental” in Latin.

The active ingredient is a derivative of barbituric acid. Used as What is the desired effect of the drug?

Impact on the body

What happens when the drug enters the bloodstream? How does it affect human body"thiopental sodium"? Pharmacological group of this drug - anesthesia for intravenous administration with a general anesthetic and hypnotic effect of short action.

Entering the bloodstream active substance depresses the respiratory and as well as the myocardium itself. Gradually, as a result of this effect, the patient's blood pressure and pulse decrease, and muscle relaxation is felt.

"Thiopental sodium" slows down the opening of channels that depend on exposure gamma-aminobutyric acid, and also increases the time of entry of chloride ions into the nerve cell. Also, the drug reduces the stimulating effect of amino acids such as glutamate and aspartate.

It is noteworthy that the drug of interest to us has an anticonvulsant effect. This is achieved by increasing the threshold of excitability of neurons and blocking the conduction and propagation of convulsive impulses throughout the brain. Also, the drug reduces the intensity of some processes occurring in the brain.

How long to wait for the effect of sodium thiopental? The drug, when administered intravenously, begins to act within thirty seconds, with rectal use - after eight to ten minutes.

How long does the effect of the drug last? As the instructions show, the duration of anesthesia varies between twenty to thirty minutes. After this period, the patient wakes up. According to the instructions, sodium thiopental does not cause drowsiness after waking up. The duration of the analgesic effect ends at the moment when the patient wakes up.

Pharmacokinetic features

When administered intravenously, the drug penetrates through the bloodstream into the brain, adipose tissue, liver, skeletal muscles and kidneys in forty to sixty seconds. Due to the fact that the active substance spreads quickly throughout all tissues of the body, its effect wears off fairly soon.

The plasma protein binding of the drug is on average eighty percent. With a single dose, the elimination half-life active substance fluctuates between three and eight hours. In children this process it goes by the fastest - a little over an hour. This time period increases in women carrying babies (up to 26 hours), and in people suffering from obesity (about 27 hours).

The agent of interest to us is metabolized in the liver, excreted through the kidneys. It is noteworthy that the drug has a cumulative effect. This is possible with the repeated introduction of anesthesia. In this case, sodium thiopental accumulates in fatty tissues.

In what cases is the appointment of this anesthetic justified?

Indications for the use of the drug

Most often, the drug is prescribed for short surgical interventions as a general anesthetic. In some cases, the drug acts as an introductory or basic anesthesia. That is, after its introduction, it will be necessary to use other, more potent drugs for anesthesia or anesthesia.

In some cases, sodium thiopental may be used to treat a patient with status epilepticus or increased intracranial pressure. Sometimes injections are prescribed as a prevention of cerebral hypoxia. This is usually justified in neurosurgical operations performed on the vessels of the brain, with cardiopulmonary bypass or

Of course, the drug has contraindications.

When not to use the drug

Among the main contraindications of the drug, doctors note serious pathologies of the kidneys and liver, diabetes mellitus, bronchial asthma, collapse, severe exhaustion of the body, inflammatory diseases of the nasopharynx, fever, acute disorders blood circulation, attacks of acute porphyria in history both in the patient and his relatives.

In addition, this medication should not be used as an anesthetic for women who are breastfeeding, as well as for patients who are diagnosed with sodium thiopental intolerance or intoxication. various genesis(due to the increased dose of alcohol, sleeping pills, painkillers, and so on).

With caution, it is recommended to prescribe this remedy to pregnant women, children under twelve years of age, as well as people suffering from anemia, muscular dystrophy, chronic obstructive respiratory diseases, obesity, severe diseases of the cardiovascular system (failure, myocardial disease) and so on.

In addition to contraindications, the drug has a number of side effects, which will be discussed in the next subheading.

Negative reactions to medication

Before use this tool as anesthesia, the attending physician will acquaint the patient with possible negative manifestations that may occur during the use of sodium thiopental.

Primarily we are talking about dizziness and lethargy, as well as memory impairment. These symptoms are most often observed in the postoperative period after the use of anesthesia. This is due to dose-dependent depression of the central nervous system. What do patients say about the use of sodium thiopental? In reviews about this preparation people report that they have encountered such unpleasant phenomena like seizures, muscle twitching, drowsiness and anxiety. Quite rarely, patients were disturbed by such negative reactions on anesthesia like hallucinations, back pain, confusion and so on.

Also, according to patients' reviews, after using the drug, they were worried about interruptions in the heart rhythm, a decrease in pressure, and collapse.

The respiratory system may react negatively to the use of anesthesia with bronchospasm, difficulty breathing, sneezing or coughing.

After using the drug, a person may be disturbed by abdominal pain, nausea, and vomiting.

Among other unpleasant symptoms, patients note skin rashes, urticaria, reddening of the epidermis, and hiccups.

Directly with the introduction of the drug, a person may experience soreness or burning at the injection site, redness on the skin in the injection area, peeling, vasospasm.

How should an anesthetic be used to minimize the number and severity of the symptoms mentioned above?

General information

As mentioned above, the drug is administered intravenously. Manipulation should be carried out very carefully and slowly. Injections are carried out only in specialized conditions, that is, in the walls medical institutions where the necessary devices for maintaining cardiac activity and respiration are located.

Children are allowed to use the drug rectally, that is, inject the solution into the rectum.

What is the required dose of sodium thiopental to provide high-quality anesthesia? According to the instructions for use, adults are prescribed a 2-2.5% solution, but in some cases the dosage can be increased to five percent. Elderly patients, debilitated people and children are administered a one percent solution.

How to dilute sodium thiopental to the required dosage?

The powder is diluted with special sterile water for injection, a 5% glucose solution, or saline sodium chloride. The prepared product must be used immediately after dilution. It is unacceptable to save it or freeze it.

To prepare a five percent solution, you need to dilute one gram of powder in twenty milliliters of injection water. To prepare 1.25% of the drug, it is recommended to add forty milliliters of water to 0.5 grams of powder.

How does the breeding process take place? Everything is very simple.

The required amount of liquid is drawn into the syringe, and then added to the vial of powder, after which everything is thoroughly mixed by vigorously shaking the container with the medication. The medicine must completely dissolve and become transparent, otherwise it cannot be used.

Specific dosage

Now let's talk about the specific dosages of the drug, which can be prescribed by an anesthetist. As anesthesia for adults, at the first stage of anesthesia, a trial amount of the drug is administered - about 25-75 milligrams. Then, after a minute, the so-called main dose is administered at the rate of three to five milligrams of the drug per kilogram of the patient's body weight. On average, this is two hundred to four hundred milligrams of the drug. Usually this dosage is divided into two to four times and injected into a vein every thirty to forty seconds until the desired effect is obtained.

However, as mentioned above, sodium thiopental is used not only as an anesthetic. For the treatment of complex specific conditions, the drug is prescribed in the following dosages:

• For cupping seizure 75-125 milligrams of the drug is administered over ten minutes.
• For the relief of convulsions that have arisen against the background of local anesthesia, 125-250 milligrams are prescribed also for ten minutes.
• With brain hypoxia, the medication of interest to us is administered at the rate of 1.5-3.5 milligrams per kilogram of the patient's weight. The injection is carried out within a minute, until a temporary circulatory arrest begins.
• In some cases, the drug can be used for drug analysis when a person is injected into semiconscious state to answer the necessary questions. In such situations, one hundred milligrams of sodium thiopental is administered over one minute until the desired state is reached.

Children and drug

Although they try not to use the medication to treat small patients, if anesthesia is necessary, the drug is prescribed at a dosage of three to five milligrams per kilogram of weight. The drug is injected intravenously in a stream for three to five minutes once. This dosage applies to babies up to a year.

Children from one to twelve years old are injected with the drug at the rate of five to eight milligrams per kilogram of body weight.

A five percent solution of sodium thiopental is prescribed rectally. The dosage of the medicine is calculated as follows: 0.04-0.05 grams for one year of life of a small patient (if the child's age does not exceed three to seven years).

Usage Precautions

Since “thiopental sodium” is a serious potent agent for general anesthesia, only professionals should carry out its introduction on the basis of the appointment of an anesthesiologist. The specialist makes a decision regarding the dosage of the drug not only on the basis of the duration and depth necessary anesthesia, as well as the individual sensitivity of the patient.

The drug can only be administered intravenously. The entry of the solution into the artery can provoke vessel thrombosis, necrosis and even gangrene.

How to determine in time that the medication has entered the artery? This can be detected if a conscious patient complains of a burning sensation in the vessel. If a person is in unconscious, then the darkening of the epidermis, transient blanching or spotty cyanosis will indicate the incorrect administration of anesthesia. In this case, it is necessary to urgently stop the manipulation, and inject a solution of "Heparin" into the site of the lesion. Also, anticoagulant therapy should be carried out and blockade of the brachial plexus should be performed.

If the drug has got under the skin, then it is necessary to introduce a local anesthetic, as well as to warm the surface of the epidermis. This activates blood circulation and contributes to the resorption of the infiltrate.

When prescribing the drug, one should take into account the fact that people suffering from alcoholism do not respond well to its effects, so the anesthetic effect may be short-lived.

Under the action of the drug, that is, the introduction of general anesthesia, it is necessary to ensure the patient's access to oxygen.

When using the drug in medicinal purposes You need to be aware that it is addictive.

An overdose of an anesthetic

This is very rare, but still important to know unpleasant symptoms accompanying the introduction of too high a dose of the drug. What do you need to pay attention to?

First of all, the patient's blood pressure may drop sharply, tachycardia, respiratory depression, and bronchospasm may appear. Even pulmonary edema and cardiac arrest are possible.

In such cases, as experienced anesthesiologists say, it is important to introduce bemegride, which is the antipode of sodium thiopental, on time. Appropriate therapy is used to eliminate unwanted symptoms. For example, when breathing stops, oxygen or artificial ventilation of the lungs is prescribed, with convulsions, diazepam is administered, and so on. In some exceptional cases may need muscle relaxants.

Interaction with other medicines

According to the instructions, sodium thiopental is able to reduce the effect of contraceptives, coumarin derivatives (indirect anticoagulants), glucocorticosteroids and griseofulvin. It is strictly impossible to take this medication with muscle relaxants, ascorbic acid, atropine, antibiotics, tranquilizers, tubocurarine chloride, scopolamine, ephedrine and so on.

If an anesthetic is used together with antihypertensives or diuretics, it is possible sharp decline pressure. This is also possible with the parallel appointment of the drug of interest to us and diazoxide.

Taking antidepressants and analeptics reduces the effect of sodium thiopental. H1-histamine blockers and drugs that block tubular secretion (this may be, for example, probenecid) increase the effect of an anesthetic drug.

N.01.A.F Barbiturates

N.01.A.F.03 Sodium thiopental