Otitis

Sodium thiopental maximum daily dose. Indications for use

Has restrictions during pregnancy

Has restrictions for children

Has restrictions for older people

Prohibited for liver problems

Prohibited for kidney problems

Selection of anesthetic drugs – important stage preparation for surgery. A good anesthetic should not only have a hypnotic and analgesic effect, but also be safe for the patient: cause as few side effects as possible and not slow down the subsequent recovery of the body in the postoperative period. One such anesthetic is sodium thiopental.

general information

The drug is a potent anesthetic drug. The use of this drug in Russia is limited. The medication is used to provide general anesthesia for surgical interventions and is often used against seizures (including epilepsy).

Sometimes it is used by doctors as a basic remedy, after which the patient is administered other drugs for anesthesia. Thiopental has muscle relaxant properties. It is not used as an analgesic, although it lowers the pain threshold.

The drug is valid for two years. The medicine should be stored in a dry place, out of reach of children, at an air temperature no higher than 25˚C. The medicine is dispensed only with a doctor's prescription.

Drug group, INN, scope of application

The product belongs to the group medicines, which are used in medicine for non-inhalation anesthesia. INN – Sodium thiopental. The medicine is used as anesthesia for short-term operations, has a hypnotic effect and muscle relaxation. Also used for epileptic seizures and to prevent brain hypoxia.

Forms and approximate prices for the drug, average in Russia

The medicine is an easily soluble powder in water, poured into a glass bottle. The color of the powder varies from white to light yellow. The average price of sodium thiopental in Russia is 2,500 rubles.

Basics active substance– Thiopental. Its content in one bottle is 0.5 or 0.1 g.

Pharmaco-properties

pharmachologic effect medication is:

blocking the convulsive impulse in the brain;
suppression of polysynaptic reflexes (due to which muscle relaxation occurs);
decreased metabolism and utilization of glucose by the brain;
accelerating the onset of sleep;
respiratory depression;
decrease in blood pressure.

The analgesic effect ends when the patient awakens. After the medication wears off, the patient experiences drowsiness and retrograde amnesia (memory impairment in which the patient is unable to remember what happened before the disease or its attack).

The pharmacokinetic characteristics of the drug are as follows:

After injection into a vein, Thiopental quickly penetrates into the brain, internal organs, as well as adipose tissue and skeletal muscle, muscles.
The drug binds to blood plasma proteins.
Metabolism of the drug mainly occurs in the liver with the formation of metabolites. It is carried out in children's body faster than in the body of an adult, which must be taken into account when calculating the dosage.

When the drug is slowly and carefully introduced into a person’s body, the effect is observed in an average of forty seconds. The onset of the anesthesia stage is expressed in:

muscle relaxation;
decreased depth of breathing and blood pressure;
absence of corneal reactions to irritation;
slight constriction of the pupils.

The effect of Thiopental on the cardiovascular system

As anesthesia deepens, the degree of the described manifestations increases. The duration of anesthesia is on average 15-25 minutes. When the patient recovers from anesthesia, the effect of the medication ends. The medicine is excreted from the body primarily by the kidneys.

Indications and contraindications

The drug is used for:

providing general anesthesia for short-term operations;
epileptic seizures;
performing neurosurgical operations;
epistatus (a series of epileptic seizures that follow one after another);
high intracranial pressure;
brain hypoxia and its prevention.

Contraindications for use are:

inflammation or tumors in the large intestine;
complications of bronchial asthma;
anemia;
diabetes;
inflammatory processes in the nasopharynx;
kidney and liver disorders;
alcohol poisoning;
state of shock;
decreased myocardial contractility.

Extreme caution must be exercised when administering medication to a patient who suffers from medical conditions. respiratory tract. IN similar cases Doctors perform tracheal intubation (insertion of a tube into it to ensure patency of the lungs).

The product cannot be used during breastfeeding. However, during pregnancy, taking the drug is possible if the benefit to the mother from the treatment is higher than the expected harm to the child. Possible intravenous use of the drug in childhood as anesthesia, especially for patients with high nervous excitability.

But when administering the drug to children, extreme caution should be exercised: the medicine depresses the child’s breathing much more strongly than the breathing of an adult, so there is high risk apnea (stopping breathing).

Rules for administration and dosage

This product is not intended for home use and can only be used qualified specialists in the hospital. The drug solution is water-based for injection and administered intravenously. The resulting solution should not have any impurities and be completely transparent, and the powder must be completely diluted.

For adults, a 2% solution is used, and for elderly people and children a 1% solution is prescribed. Before administering the drug, carry out preliminary preparation patient to general anesthesia using medications such as Atropine or Metacin.

The medication must be injected into the cubital vein slowly to avoid collapse. According to the instructions for using sodium Thiopental, for induction of anesthesia you need to slowly (in 15-20 seconds) inject an average of 100-150 mg of the drug, and if necessary, re-introduce the same dose after 40-60 seconds.

For older people, it is recommended to reduce the dose. For children maximum dose medication should not exceed 7 mg/kg. To relieve seizures in adults, a dose of 80-120 mg is used, which must be administered to the patient as soon as possible after the onset of seizures. As a rule, general anesthesia occurs 1.5-2 minutes after administration of the drug.

This medication cannot be combined with contraceptives (the effect of their use may be reduced), tranquilizers, antibiotics and antidepressants.

Possible side effects and overdose

Due to the fact that the drug depresses the central nervous system, side effects such as dizziness, decreased reaction speed, slowness of movements, lethargy, and ataxia (failures in coordination of movements) may occur. During the postoperative period, the patient's memory may deteriorate.

The respiratory system can also fail. Giving the medication too quickly depresses breathing or causes apnea. It is also possible that:

laryngospasm;
bronchospasm;
excess mucus in the bronchi.

Often people who used this drug experienced:

heart rhythm disturbances;
decrease in blood pressure;
nausea and vomiting;
drowsiness;
anxiety;
confusion;
stomach pain;
disorientation;
skin rash (manifestations of allergies).

Overdose of this anesthetic causes hypotension, acute vascular insufficiency and severe respiratory depression, in which it is necessary to carry out artificial ventilation oxygen.

If too high a dose is used, pulmonary edema and cardiac arrest are also possible. In case of overdose you need:

Administer a drug with a positive inotropic effect to the patient (for collapse).
Administer Diazepam in case of seizures. If the use of this medicine is ineffective, you need to ventilate the lungs and use muscle relaxants.
For laryngospasm, you also need to use muscle relaxants and apply oxygen under pressure.

What can be replaced?

There are analogues of this medication that are used as anesthesia for operations. The most famous and effective of them are:

The indications and restrictions for the use of these drugs are identical to Thiopental.

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

pharmachologic effect- 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. At reintroduction the action 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, disorder contractile function myocardium, severe anemia, shock and collaptoid conditions, myasthenia gravis, myxedema, Addison's disease, fever, inflammatory diseases 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 route of 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 one 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.

Drug for non-inhalation anesthesia

Active substance

Thiopental sodium

Release form, composition and packaging

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

Bottles with a volume of 10 ml (1) - cardboard packs.
Bottles with a volume of 10 ml (5) - cardboard packs.
Bottles with a volume of 10 ml (10) - cardboard packs.
Bottles with a volume of 10 ml (50) - cardboard packs.
Bottles with a volume of 20 ml (1) - cardboard packs.
Bottles with a volume of 20 ml (5) - cardboard packs.
Bottles with a volume of 20 ml (10) - cardboard packs.
Bottles with a volume of 20 ml (50) - cardboard packs.

pharmachologic effect

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

An ultra-short-acting non-inhalation general anesthesia agent, 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 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 propagation of convulsive impulses in 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. 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 and minute blood volumes and blood pressure. Increases the capacity of the venous bed, 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 after 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 onset time of Cmax is 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%. Penetrates the placental barrier and is excreted in 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.

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 27.5 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 (with subsequent use of muscle relaxants);

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

- prevention of cerebral hypoxia (during artificial circulation, neurosurgical operations).

Contraindications

- hypersensitivity;

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

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

— asthmatic status;

— malignant hypertension;

- lactation period.

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

Dosage

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.

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

For 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). For maintaining 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 minutes.

At brain hypoxia 1.5-3.5 mg/kg is administered 1 minute before temporary cessation of blood circulation.

At renal dysfunction(QC less than 10 ml/min) - 75% average dose.

Higher single dose drug for adults intravenously - 1 g (50 ml of 2% solution).

The intravenous solution should be administered slowly, at a rate of no more than 1 ml/min. At first, 1-2 ml is usually administered, 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. U children with decreased renal function (creatinine clearance 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 outside of cardio-vascular 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 outside 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 outside 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).

Others: hiccups

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; 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, pronounced decrease 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% oxygen; for laryngospasm - and 100% oxygen under pressure; in case of collapse or a pronounced decrease in blood pressure - plasma-substituting solutions, administration of vasopressors medicines and/or drugs with positive inotropic effects. For convulsions - intravenous administration of diazepam; if they are ineffective, use mechanical ventilation and muscle relaxants.

Drug interactions

Combined use with ethanol and drugs that depress the central nervous system leads to a mutual enhancement of pharmacological action (both to 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 - increased hypotensive effect; methotrexate - enhancement toxic effect the last one.

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

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

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; aminophylline, analeptics, some antidepressants - weaken.

Diazoxide increases the risk of low blood pressure.

Pharmaceutically incompatible with antibiotics (amikacin, benzylpenicillin, cephapirin), 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 one syringe and administered 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 a heparin solution intra-arterially into the lesion site, followed by anticoagulant therapy; glucocorticosteroid solution followed by systemic therapy; perform a sympathetic block or a brachial block nerve plexus(intra-arterial administration of rolled product).

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.

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 alcohol 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 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.

Can be used in combination with muscle relaxants, subject to artificial 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. The maximum permissible dose is 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 expected benefit to the mother outweighs the potential risk to the fetus.

The drug is contraindicated during lactation.

Use in childhood

Use with caution in children.

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. The use of the drug for basic anesthesia is especially indicated in children with increased nervous excitability

Among the various sleeping pills and painkillers of a narcotic nature, “sodium thiopental” occupies a special place. Instructions for using this serious potent drug interests 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 overdose? The answers to these questions are given by the instructions for using sodium thiopental.

Briefly about the drug

Before purchasing the drug, you will need to get a prescription for “Sodium Thiopental” from your doctor. Latin. This drug has a strong narcotic effect, so it cannot be purchased without a doctor’s prescription.

What is the medicine? On pharmaceutical 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

Active ingredient of interest to us pharmacological agent is the substance of the same name - Thiopental sodium. This is exactly how the name will be written in the recipe for “Sodium Thiopental” in Latin.

The active component is a derivative of barbituric acid. Used as How is the desired effect of the drug achieved?

Impact on the body

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

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

“Sodium thiopental” slows down the opening of channels that depend on exposure gamma-aminobutyric acid, and also increases the time of entry of chlorine ions into the nerve cell. The drug also reduces the stimulating effect of amino acids such as glutamate and aspartate.

It is noteworthy that the medicine we are interested in has anticonvulsant effect. This is achieved by increasing the threshold of neuronal excitability and blocking the conduction and propagation of convulsive impulses throughout the brain. The drug also reduces the intensity of some processes occurring in the brain.

How long does it take for sodium thiopental to take effect? When administered intravenously, the drug begins to act within thirty seconds, when rectal use- after eight to ten minutes.

How long does the medication last? As the instructions show, the duration of anesthesia varies between twenty to thirty minutes. Later 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 the moment the patient regains consciousness.

Pharmacokinetic features

When administered intravenously, the drug penetrates through the bloodstream into the brain, adipose tissue, liver, skeletal muscle 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 quickly.

The plasma protein binding of the drug is on average eighty percent. With a single administration, half-life active substance fluctuates between three and eight hours. In children, this process is 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 drug of interest to us is metabolized in the liver and excreted through the kidneys. It is noteworthy that the drug has a cumulative effect. This is possible with repeated administration of anesthesia. In this case, “sodium thiopental” accumulates in fatty tissues.

In what cases is it justified to prescribe this anesthetic?

Indications for use of the drug

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

In some cases, sodium thiopental can be used to treat a patient with status epilepticus or increased intracranial pressure. Sometimes injections are prescribed to prevent brain hypoxia. This is usually justified during neurosurgical operations performed on cerebral vessels, during artificial circulation or

Of course, the medication also has contraindications.

When not to use the drug

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

In addition, this medication should not be used as anesthesia for women who are breastfeeding, as well as for patients diagnosed with sodium thiopental intolerance or intoxication of various origins(due to increased doses of alcohol, sleeping pills, painkillers, etc.).

It is recommended to prescribe this drug with caution to pregnant women, children under twelve years of age, as well as people suffering from anemia, muscular dystrophy, chronic obstructive diseases of the respiratory system, obesity, severe diseases of the cardiovascular system (failure, myocardial diseases) 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 familiarize the patient with the possible negative manifestations which may occur during the use of sodium thiopental.

First of all we're talking about about dizziness and lethargy, as well as memory impairment. These symptoms are most often observed in postoperative period after using 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 drug people note that they have encountered such unpleasant phenomena as seizures, muscle twitching, drowsiness and anxiety. Quite rarely, patients were bothered by such negative reactions to anesthesia as hallucinations, back pain, confusion, and so on.

Also, according to patient reviews, after using the drug they were worried about interruptions in heart rhythm, low blood pressure, and collapse.

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

After using the medication, a person may experience abdominal pain, nausea, and vomiting.

Among other unpleasant symptoms, patients note skin rashes, hives, redness of the epidermis, and hiccups.

Directly upon administration of the drug, a person may experience pain or burning at the injection site, redness of the skin in the injection area, peeling, and vascular spasms.

How should you use it? anesthetic to reduce the number and severity of the symptoms mentioned above to a minimum?

General information

As mentioned above, the drug is administered intravenously. The manipulation should be carried out very carefully and slowly. Injections are carried out only in specialized conditions, that is, within the walls medical institutions, where the necessary devices for maintaining cardiac activity and breathing 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, weakened people and children are given a one percent solution.

How to dilute “Sodium Thiopental” to the required dosage?

The powder is diluted with special sterile water for injection, a five percent glucose solution, or a physiological solution of 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 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 bottle with the 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 specific dosages of the drug that can be prescribed by an anesthesiologist. As anesthesia for adults, at the first stage of anesthesia, a test 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 medication per kilogram of the patient’s body weight. On average, this is two hundred to four hundred milligrams of medication. Typically, 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 anesthesia. For the treatment of complex specific conditions, the drug is prescribed in the following dosages:

For cupping seizure 75-125 milligrams of medication are administered over ten minutes.
To relieve seizures that occur during local anesthesia, 125-250 milligrams are also prescribed for ten minutes.
In case of 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 for a minute until a temporary stop of blood circulation begins.
In some cases, the drug can be used for drug analysis, when a person is put into a semi-conscious state so that he answers the necessary questions. In such situations, one hundred milligrams of sodium thiopental is administered over one minute until the desired state is achieved.

Children and the drug

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

Children from one to twelve years of age are administered the drug at a 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 per year of life of a small patient (if the child’s age does not exceed three to seven years).

Cautions for use

Since “Sodium Thiopental” is a serious, potent drug for general anesthesia, its administration should only be carried out by professionals based on the prescription of an anesthesiologist. The specialist makes a decision regarding the dosage of the medication not only on the basis of the duration and depth of anesthesia required, as well as the individual sensitivity of the patient.

The drug can only be administered intravenously. If the solution gets into the artery, it can cause thrombosis of the vessel, necrosis and even gangrene.

How to determine in time that the medication has entered the artery? This can be detected if the conscious patient complains of a burning sensation in the vessel. If a person is in unconscious, then improper administration of anesthesia will be indicated by darkening of the epidermis, transient pallor or spotty cyanosis. In this case, it is necessary to urgently stop the manipulation and inject a Heparin solution into the affected area. Anticoagulant therapy and brachial plexus blockade should also be performed.

If the drug gets under the skin, then it is necessary to administer a local anesthetic, as well as 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 are difficult to respond to its influence, so the anesthetic effect may be short-lived.

When the medication is in effect, that is, general anesthesia is administered, 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.

Overdose of anesthetic

This happens very rarely, but it is still important to know unpleasant symptoms, accompanying the introduction too high dose drug. What should you pay attention to?

First of all, the patient may experience a sharp drop in blood pressure, tachycardia, respiratory depression, and bronchospasm. Even pulmonary edema and cardiac arrest are possible.

In such cases, as they say experienced anesthesiologists, it is important to administer bemegride, which is the antipode of sodium thiopental, in a timely manner. To eliminate unwanted symptoms, appropriate therapy is used. For example, if breathing stops, oxygen or artificial ventilation is prescribed, if there are convulsions, diazepam is administered, and so on. In some exceptional cases Muscle relaxants may be needed.

Interaction with other medications

According to the instructions, “sodium thiopental” can reduce the effect contraceptives, coumarin derivatives (indirect anticoagulants), glucocorticosteroids and griseofulvin. This medication should strictly not be taken 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 parallel administration 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 could be, for example, probenecid) enhance the effect of the anesthetic drug.

Latin name: thiopental sodium
ATX code: N01AF03
Active substance:
Manufacturer: Med Pro Inc., Latvia
Release from the pharmacy: On prescription
Storage conditions: up to 30 degrees Celsius
Best before date: 3 years.

Sodium thiopental is one of the methods of anesthesia before surgical manipulation.

Indications for use

These include:

Temporary anesthesia for a short period
Reduction of blood pressure and arrhythmias with increased intracranial pressure
Epilepsy, severe and frequent seizures
Prevention of hypoxia
Anesthesia with the use of painkillers and muscle relaxants.

Composition and release forms

Description of composition: lyophilized sodium thiopental powder in a bottle.

The lyophilized powder for reconstitution is packaged in transparent glass ampoules of 500 mg and 1000 mg, which are sealed with rubber stoppers.

Medicinal properties

The drug is used to obtain premedication. The pharmacological effect of the drug is manifested as a narcotic and hypnotic substance. The drug also exhibits moderate muscle relaxant and analgesic properties. The mechanism of action is to lengthen aminobutyric acid-dependent channels on the postsynaptic membrane. The drug resists the stimulating effects of amino acids, and also blocks the transmission of convulsive impulses to the brain, has anticonvulsant properties, and increases the excitatory threshold of neural connections.

The medication relaxes muscles well and blocks polysynaptic reflexes, and also slows down metabolic processes in the brain, reducing the ability of the brain to utilize glucose and oxygen. Due to this, the drug exhibits hypnotic properties, changes the structure of sleep and promotes sleep. Next, the function of oppression manifests itself in relation to respiratory center. The medicine also has a depressing effect on the functional cardiac component: the pressure drops noticeably and the output decreases. Since the product stimulates nervus vagus, then this can cause profuse laryngospasm. The speed of influence depends on the injection site. If injected intravenously, the effect appears after 40 seconds, but if administered rectally, then after 10 minutes. The duration of anesthesia is no more than 20-25 minutes.

During anesthesia, tendon and corneal reflexes may disappear almost or even completely, the eyes are in a motionless position, the frequency and depth of breathing is significantly reduced, the tongue sinks in, as the muscles of the pharynx completely relax. The analgesic effect, as well as the state of drowsiness, quickly disappears after the patient awakens, the recovery time does not take a long period. If you re-introduce the medication, it will continue. After intravenous administration, the medication quickly spreads throughout all organs, tissues and fluids of the body. The drug also bypasses the placental barrier and penetrates into breast milk, is processed by the liver into inactive metabolites, and is partially inactivated by the kidneys and brain. The half-life is 11 hours, excreted in the urine.

Directions for use and doses

The average cost in Russia is 250 mg per 10 ml bottle.

Sodium thiopental instructions for use indicate that the drug should be administered slowly and intravenously, no more than one milliliter per minute. If hit quickly, the patient collapses. Adults need a 2.5% solution for anesthesia, and 1% for anesthesia in children. The solution is injected into the cubital vein and diluted in glucose or saline. The proportions of the administered fluid are selected individually by doctors. If sleep does not occur, then a 5% solution is administered. The presence of renal dysfunction requires selection of a reduced dosage.

During pregnancy and breastfeeding

The drug should not be prescribed to pregnant and breastfeeding mothers.

Contraindications and precautions

The drug should not be prescribed for:

Asthmatic status
Addison's disease
For porphyria
Myxedema
Diabetes mellitus
Collapse
Bronchial asthma
Impaired liver or kidney function
Exhaustion
Shock states
Inflammatory processes in the nasopharynx
Pregnancy and breastfeeding.

Cross-drug interactions

The drug is compatible with muscle relaxants. It cannot be mixed with ditilin, diprazine, aminazine. Heparin solution and other anticoagulants lose part of their effectiveness, as anesthesia thickens the blood volume. In combination with ketamine, blood pressure is intensely reduced, and glucocorticosteroids and oral contraceptives weaken their effectiveness.

Side effects

Side effects typically include chills, increased heart rate, drowsiness, and nausea. Symptoms such as rectal bleeding, decreased blood pressure, laryngeal spasm, bronchospasm, headache and heart failure are considered more threatening to the patient’s health. There may also be allergic manifestations in the form of rashes, itching and anaphylactic shock.

Overdose

Severe depression of the central nervous system occurs, spasm of the larynx, acceleration of the heart rate, pulmonary edema, and subsequent cardiac arrest. There are several options for restoring life. The antidote Bemegride is prescribed, muscle relaxants are administered, and individual ventilation of the respiratory system is performed.