Thiopental sodium (Thiopental sodium)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceThiopental sodiumThiopental sodium
Dosage form: & nbsppowder for solution for intravenous administration
Composition:
Active substance: thiopental sodium - 0.5 g, 1 g,

Description:The powder is white or almost white or from yellowish white to pale greenish yellow. Hygroscopic.
Pharmacotherapeutic group:means for non-induction general anesthesia
ATX: & nbsp

N.01.A.F   Barbiturates

N.01.A. F.03   Thiopental sodium

Pharmacodynamics:
Means for non-induction general anesthesia of ultrashort; action, a derivative of thiobarbituric acid. Has a pronounced hypnotic, some miorelaxing and weak analgesic activity. Slows the opening time of GABA-dependent - channels on the postsynaptic membrane of neurons of the brain, lengthens the entry time of chloride ions into the nerve cell and causes hyperpolarization of the membrane.
Suppresses the stimulating effect of amino acids (aspartate and glutamate). In large doses, directly activating GABA receptors, it has a GABA-stimulating effect.
Has anticonvulsant activity, increasing the threshold of excitability of neurons and blocking the conduction and spreading of convulsive impulse over the brain.
Promotes muscle relaxation, suppressing polysynaptic reflexes and slowing down the insertion of the spinal cord by the neurons.
Reduces the intensity of metabolic processes in the brain, the utilization of glucose and oxygen by the brain.
Has a hypnotic effect, which is manifested by accelerating the process of falling asleep and changing the structure of sleep.
Oppresses (dose-dependent) the respiratory center and reduces its sensitivity to carbon dioxide.
Provides (dose-dependent) cardiodepressant effect: reduces the shock volume of blood, minute blood volume, blood pressure.
Increases the capacity of the venous system, reduces hepatic blood flow and the rate of glomerular filtration.
, Has an arousing effect on n.vagus and can cause laryngospasm, an abundant secretion of mucus.
After intravenous administration, general anesthesia develops after 30-40 seconds; after rectal - after 8-10 minutes, characterized by a short-term (after the introduction of a single dose of the general, anesthesia lasts 10-30 minutes) and awakening with some drowsiness and retrograde amnesia. Upon exiting the general anesthesia, the analgesic effect ceases simultaneously with the awakening of the patient.
Pharmacokinetics:
With intravenous injection, quickly penetrates the brain, 'skeletal muscles, kidneys, liver and adipose tissue. The time of maximum concentration is 30 seconds (brain), 15-30 minutes (muscles). In fat stores, the concentration of the drug is 6-12 times higher than in blood plasma. The volume of distribution - 1.7-2.5 l / kg, during pregnancy - 4.1 l / kg, in obese patients - 7.9 l / kg. The connection with plasma proteins is 76-86%. It penetrates through 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.
The half-life in the distribution phase is 5-9 minutes, in the elimination phase it is 3-8 hours (lengthening up to 10-12 hours, during pregnancy up to 26.1 hours, in obese patients up to 27.5 hours), in children - 6.1 h. Clearance - 1.6-4.3 ml / kg / min, 'during pregnancy - 286 ml / min. It is excreted mainly by the kidneys by glomerular filtration. When repeated administration is cumulated (associated with accumulation in adipose tissue).

Indications:
General anesthesia for short-term surgical interventions, introductory and basic general anesthesia (with the subsequent use of analgesics and muscle relaxants).
Large epileptic seizures (grand mal), epileptic status, increased intracranial pressure, prevention of brain hypoxia, (with artificial circulation, carotid endarterectomy, neurosurgical operations on the vessels of the brain), drug analysis and drug synthesis in psychiatry.

Contraindications:
Hypersensitivity to the components of the drug; porphyria, including acute intermittent (including in the anamnesis of the patient or his immediate family); diseases that are contraindicated for general anesthesia; intoxication with ethanol, narcotic analgesics, hypnotics and medicines for general anesthesia; shock, asthmatic status, malignant hypertension, pregnancy, lactation.

Carefully:
Chronic obstructive pulmonary diseases, bronchial asthma, expressed. disorders of myocardial contractility, 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, children's age.

Pregnancy and lactation:
Use in pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. It is recommended to stop breastfeeding when it is necessary to prescribe the drug. ’

Dosing and Administration:
Intravenously slow (to avoid collapse), adults use 2-2.5% solutions (less often, 5% solution - use the procedure of fractional administration), children, and a weakened elderly patient - 1% solution.
The solutions are prepared immediately before use on sterile water for injection. The prepared solution should be absolutely transparent. With the rapid introduction of solutions with concentration! less than 2% * possible development of hemolysis. Before administration, premedication is carried out with atropine or methacin. Adults for the introduction of a general anesthetic: a test dose of 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 to achieve the desired effect, or once at a dose of 3-5 mg / kg).To maintain anesthesia, 50-100 mg.
For cramping seizures - 75-125 mg intravenously for 10 minutes; the development of seizures with local anesthesia - 125-250 mg for 10 minutes.
When hypoxia of the brain for 1 minute is administered 1.5-3.5 mg / kg before the temporary stop of blood circulation.
Drug analysis - 100 mg for 1 min. Offer the patient to slowly count from 100 to 1. Interrupt the injection, thiopental immediately before falling asleep. The patient should be in a half-awake and be able to answer questions. '
If the renal function is impaired (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 2% solution).
Enter the solution intravenously slowly, at a rate of no more than 1 ml / min. Initially, usually 1-2 ml are administered, and after 20-30 seconds - the rest. - - For children - intravenously sprayed, slowly for 3-5 minutes, once for 3-5 mg / kg. Before carrying out the 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, with a body weight of 30-50 kg - 4-5 mg / kg / Supporting dose - 25-50 mg In children with a decrease in kidney function (creatinine clearance less than 10 ml / min) - 75% of the average dose.
Side effects:
From the cardiovascular system: lowering blood pressure, arrhythmia, tachycardia; collapse. '
On the part of the respiratory system: coughing, sneezing, hypersecretion of bronchial mucus laryngospasm, bronchospasm ,. hypoventilation of the lungs, dyspnea, oppression of the respiratory center, apnea.
From the side of the nervous system: headache, muscle twitching, epileptic seizures, n.vagus tone increase, dizziness, retardation, ataxia, anterograde amnesia, drowsiness at
postoperative period, anxiety, special with pain, at
postoperative period, rarely postoperative delirious * psychosis (back pain, anxiety, confusion, agitation, hallucinations, restlessness, restless legs syndrome), paralysis of the radial nerve.
On the part of the digestive system: hypersalivation, nausea, vomiting, abdominal pain in the postoperative period.
Allergic reactions: skin hyperemia, rash, skin itch, hives, rhinitis, anaphylactic shock, rarely - hemolytic anemia with impaired renal function (pain in the lower back, legs and stomach, nausea, vomiting, loss of appetite, unusual weakness, fever, pale skin ).
Other: hiccough.
Local reactions: with intravenous administration - soreness at the injection site, thrombophlebitis (administration of solutions with a high concentration of the drug), vasospasm and thrombosis at the injection site, tissue irritation c. place of injection (flushing and flaking, skin), necrosis; defeat of nerves, suitable to the injection site.

Overdose:
Symptoms: depression of the central nervous system, convulsions, muscle hyperreactivity, respiratory depression up to apnea, laryngospasm, water-electrolyte disorders, marked decrease in blood pressure, decrease in total peripheral vascular resistance (toxic effect in overdose starts from the first seconds), tachycardia;
postnarcotic delirium. At a very high dose: pulmonary edema, circulatory collapse, cardiac arrest.
Treatment: antidote - bemegrid. When breathing is stopped - artificial ventilation, 100% oxygen; with laryngospasm - muscle relaxants and 100% oxygen under
pressure; at a collapse or expressed. decrease of arterial pressure - plasma-substituting solutions, introduction of vasopressor drugs and / or preparations with a positive inotropic effect.With convulsions - intravenous diazepam; with them; inefficiency - artificial ventilation of lungs and muscle relaxants

Interaction:
Joint application with ethanol and drugs that depress the central nervous system leads to a mutual enhancement of the pharmacological effect (both to a significant inhibition of the central nervous system, respiratory function, increased hypotensive effect, and the degree of anesthesia); c, magnesium sulfate - intensification of the depressing, action, on the central nervous system; with gangioblokatorami, diuretics, etc. 'hypotensive drugs - strengthening of hypotensive action; methotrexate - increased toxic effect of the latter.
Reduces the effect of indirect anticoagulants, (coumarin derivatives), griseofulvin, contraceptives, glucocorticosteroids. '
Strengthens the effect of drugs that contribute to the development of hypothermia. It shows antagonism with the bemegrid.
Opioid analgesics reduce the strength of the analgesic effect.
Ketamine increases the risk of lowering blood pressure and respiratory depression, lengthening the recovery time of functions after leaving the general anesthesia.Drugs that block tubular secretion (probenecid), and H1-histaminoblockers enhance the effect; aminophylline, analeptics, some antidepressants - weaken.
Diazoxide increases the risk of lowering blood pressure.
Pharmaceutically incompatible with antibiotics (amikacin, benzylpenicillin, cefapyrine), anxiolytic medicinal means (tranquilizers), muscle relaxants (suxamethonium chloride, tubocurarine chloride), narcotic analgesics (codeine, morphine), ephedrine, epinephrine, ascorbic acid, dipyridamole, chlorpromazine, ketamine, atropine, scopolamine and tubocurarine chloride (should not be mixed in the same syringe and injected through a single needle with acidic solutions).

Special instructions:
To use only in the conditions of a specialized department of anesthetists-resuscitators, with the availability of funds to maintain cardiac activity and provide airway patency, artificial ventilation. It should be borne in mind that the achievement and maintenance of general anesthesia of the required depth and duration depends on the amount of the drug, and on the individual sensitivity to the patient.
In inflammatory diseases, the upper respiratory tract, it is shown that the upper airways are passable, up to the intubation of the trachea.
Unintentional, intraarterial, administration, causes an instantaneous spasm of the vessel, accompanied by a circulatory disturbance distal to the injection site (possible thrombosis of the main vessel 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 course of the artery; in patients in a state of general anesthesia, the first symptoms are transient blanching, spotted cyanosis, or dark skin color.
Treatment: stop the introduction, enter intraarterially into the place of the lesion solution of heparin followed by anticoagulant therapy; 1, glucocorticosteroid solution followed by systemic, therapy; conduct a sympathetic blockade or blockade of the brachial plexus (intra-arterial administration of procaine).
At a chemical irritation of tissues (associated with a high pH value of the solution (10-11) in case of contact, a solution under the skin, a local anesthetic is injected to quickly dissolve the infiltrate, and warming is performed (activation of the local circulation).
Sign of extravasation - subcutaneous swelling!
In the case of an intravenous bolus of children under 18 years requires careful monitoring of the patient for the purpose of early detection of respiratory depression symptoms, hemolysis, blood pressure lowering, extravasation.
Anesthetic effect is unreliable in persons abusing ethanol.
It is necessary to reduce the dose in patients taking digoxin, diuretics; in patients who received a premedication morphine, and also after the administration of atropine, diazepam.
Premedication - any of the common drugs, except for phenothiazine derivatives. ,
When prolonged anesthesia when the hypnotic effect induced by sodium thiopental, maintained by intravenous application of long acting anesthetics and / or anesthetic gases, due to the risk of cumulative effect dose of thiopental sodium should not exceed 1 g
It can be used in combination with muscle relaxants provided that artificial ventilation is provided. ' .
Increases the .tonus n.vagus, therefore, before administration, an adequate dose of atropine should be administered. Immediately after the onset of general anesthesia, it is necessary to provide airway patency. There can be addiction.
Thiopental does not affect the tone of a pregnant woman. After intravenous administration, the maximum concentration in the umbilical cord is noted after> 2-3 min. The maximum allowable dose is 250 mg. When used in obstetric and gynecological surgery, it can cause central nervous system depression in newborns.

Effect on the ability to drive transp. cf. and fur:
After outpatient use, patients should go out with an escort only and for 24 hours be careful when driving vehicles and engage in potentially dangerous activities that require increased concentrated attention and speed of psychomotor reactions.

Form release / dosage:
Powder for the preparation of a solution for intravenous administration 0.5 g, 1 g. '

Packaging:
0.5 g of active substance in bottles with a capacity of 10 ml or 20 ml, 1 g of active substance in bottles with a capacity of 20 ml, hermetically sealed with stoppers rubber, crimped caps aluminum or caps combined aluminum with plastic caps.
1. 5 or 10 bottles with instructions for use are placed in a pack of cardboard.
50 bottles with 5 instructions for use are placed in a carton box for delivery to hospitals.

Storage conditions:
List № 1 ADD. In a dry, protected from light place, at a temperature not higher
25 ° C.
Keep out of the reach of children. '
The drug belongs to the list of No. 1 potent substances of the Standing Committee on Drug Control M3 RF.

Shelf life:
2 years. Do not use after the expiration date. ’

Terms of leave from pharmacies:On prescription
Registration number:LS-000748
Date of registration:23.07.2010
The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia
Manufacturer: & nbsp
Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia
Information update date: & nbsp09.09.2015
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