Ketamine is a drug (solution), (pharmacological group - anesthetics). The instructions for use highlight the following features of the drug:
- Sold only with a doctor's prescription
- During pregnancy: contraindicated
- In childhood: contraindicated
- If renal function is impaired: with caution
Package
Ketamine - official instructions for use
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IndicationsContraindicationsDosageWarningsInteractionsManufacturer
INSTRUCTIONS
on medical use of the drug
Registration number:
Trade name of the drug: Ketamine
International (nonproprietary) name: ketamine
Dosage form: solution for intravenous and intramuscular administration
Composition: 1 ml of solution contains:
Active substance: ketamine hydrochloride, equivalent to 50 mg of ketamine - 57.6 mg.
Excipients: benzethonium chloride, sodium chloride, water for injection.
Description: transparent, colorless or slightly colored liquid.
Pharmacotherapeutic group: agent for non-inhalation general anesthesia.
ATX code:
Pharmacological properties
Pharmacodynamics. The drug causes an analgesic effect with incomplete depression of consciousness and preservation of spontaneous breathing, pharyngeal, laryngeal and cough reflexes (the dose of the drug that causes apnea is 8 times higher than the hypnotic dose). The surgical stage of general anesthesia does not develop when using ketamine (the visceral analgesic activity of ketamine is insufficient, which should be taken into account during abdominal operations).
Causes a specific set of symptoms: somatic analgesia, a condition reminiscent of neuroleptanalgesia, increases blood pressure, myocardial contractility, minute blood volume (MBV) and myocardial oxygen demand, relaxes bronchial smooth muscles. It practically does not reduce the tone of skeletal muscles and can cause involuntary muscle twitching.
In adults, the minimum dose that causes a hypnotic effect with a single intravenous injection is 0.5 mg/kg of body weight (depression of consciousness lasts one and a half minutes). At a dose of 1 mg/kg the drug depresses consciousness for 6 minutes, at a dose of 1.5 mg/kg - for 9 minutes, at a dose of 2 mg/kg - for 10-15 minutes. With intramuscular administration of 4-8 mg/kg, the effect occurs within 2-4 minutes (6-8 minutes) and lasts on average 12-25 minutes (up to 30-40 minutes).
In children, with intramuscular administration, general anesthesia occurs after 2-6 minutes, with intravenous administration - after 15-60 seconds, duration of action - 15-30 and 5-15 minutes, respectively.
During the period of recovery of consciousness, drowsiness is noted, against the background of which reactions often occur in the form of hallucinations, delusions, and vivid imaginative dreams. After awakening, patients may remain disoriented, sometimes for 6-8 hours. The frequency and severity of these reactions, as well as the cardiac stimulating effect, are reduced when ketamine is combined with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers) - droperidol, diazepam.
The analgesic effect of ketamine for somatic pain is manifested when prescribing subnarcotic doses. The maximum analgesic effect occurs 10 minutes after injection into a vein and lasts for 2-3 hours; with intramuscular administration, the effect is longer.
Pharmacokinetics. Ketamine, being a lipophilic compound, easily penetrates histohematic barriers, including the blood-brain barrier. Communication with plasma proteins – 12%. The volume of distribution is 1.8-2 l/kg, the half-life is 2.3 hours. Ketamine is metabolized by demethylation; the bulk of metabolic products are excreted within 2 hours in the urine; a small amount of metabolites can remain in the body for several days. Cumulation with repeated administration is not observed.
Indications for use
Introductory and basic general anesthesia (especially in patients with low blood pressure or when it is necessary to maintain spontaneous breathing, or when performing artificial ventilation of the lungs with breathing mixtures that do not contain dinitrogen oxide (nitrous oxide).
Emergency surgical interventions (including at the stages of evacuation, in particular in patients with traumatic shock and blood loss).
Various surgical operations with multicomponent intravenous anesthesia.
Painful diagnostic procedures (endoscopy, cardiac catheterization), minor surgical procedures for burns, dressings, etc. procedures.
Contraindications
Hypersensitivity to the drug, arterial hypertension (and other conditions in which an increase in blood pressure is contraindicated), angina pectoris or myocardial infarction (including in the last 6 months), severe renal failure, cerebrovascular accident (including history), preeclampsia, eclampsia, epilepsy and other convulsive conditions, alcoholism, pregnancy and lactation.
Contraindications to ketamine anesthesia in children are any diseases accompanied by convulsive activity.
With caution - decompensated chronic heart failure, operations on the larynx and pharynx.
Directions for use and doses
Ketamine is administered intravenously (simultaneously as a stream or fractionally and drip) or intramuscularly.
For adults the drug is administered intravenously at a rate of 2-3 mg/kg, intramuscularly at a rate of 4-8 mg/kg body weight. To maintain anesthesia, the drug is administered at 0.5-1 mg/kg intravenously or 3 mg/kg intramuscularly or intravenously drip at a rate of 2 mg/kg/h (using an infusion pump or by drip administration of a 0.1% ketamine solution (in 5 % dextrose solution (glucose) or 0.9% sodium chloride solution) at a rate of 20-50 drops/min.
In children the drug is used for induction of anesthesia for various types of combined anesthesia (administered intramuscularly once at the rate of 4-5 mg/kg in the form of a 5% solution after appropriate premedication). For basic anesthesia, ketamine is administered intramuscularly (5% solution) or intravenously (1% solution in a stream at once or 0.1% solution in a drip at a rate of 50-60 drops/min); when administered intramuscularly, the dose depends on the body weight and age of the children: newborns and infants - 8-12 mg/kg, children from 1 to 6 years old - 6-10 mg/kg, 7-14 years old - 4-8 mg/kg . It is administered intravenously at a dose of 2-3 mg/kg. Anesthesia is maintained with repeated injections of ketamine (3-5 mg/kg intramuscularly or 0.5-1 mg/kg intravenously by bolus or drip administration of a 0.1% solution of the drug at a rate of 30-60 drops/min).
To enhance the effect of ketamine, it is usually used in combination with antipsychotic drugs (droperidol) and analgesics (fentanyl, promedol, etc.), while the dose of ketamine should be reduced.
Side effect
From the nervous system: depression of the respiratory center, muscle rigidity, involuntary muscle activity (for prevention, diazepam should be pre-administered); during the period of recovery from general anesthesia - psychomotor agitation, hallucinations, prolonged disorientation, psychosis.
From the respiratory system: shortness of breath, obstruction of the upper respiratory tract due to spasm of the masticatory muscles and retraction of the tongue, increased bronchial secretion and salivation.
From the cardiovascular system: increased blood pressure, tachycardia.
From the digestive system: hypersalivation, nausea.
Local reactions: pain and hyperemia along the vein at the injection site.
Overdose
When ketamine is administered in high doses intravenously (3 mg/kg), respiratory depression may occur in some cases. In these cases, artificial ventilation is indicated. When hallucinations occur, it is advisable to use antipsychotic drugs (haloperidol), and for convulsive syndrome - diazepam. If necessary, carry out symptomatic therapy.
Interaction with other drugs
Ketamine enhances the effect of drugs for general anesthesia, narcotic analgesics, antipsychotic drugs (neuroleptics), anxiolytics (tranquilizers) and other drugs that depress the central nervous system.
Before using ketamine, it is necessary to discontinue lincomycin, lithium preparations (1-2 days before), monoamine oxidase inhibitors (15 days before). Do not mix in the same syringe with barbiturates (pharmaceutically incompatible - formation of sediment).
Droperidol and benzodiazepines, incl. sibazon, reduce the risk of psychomimetic and motor activity, as well as the occurrence of tachycardia and arterial hypertension.
It is not recommended to prescribe with sympathomimetics and drugs that have a stimulating effect on the cardiovascular system (increased hypertensive and arrhythmogenic effects, increased myocardial oxygen demand).
The cardiac stimulating effect of ketamine is weakened when combined with antipsychotic drugs and anxiolytics.
Ketamine enhances the muscle relaxant effect of tubocurarine and dithiline, but does not change the effect of pancuronium and suxamethonium.
During general anesthesia in patients taking iodine-containing drugs and thyroid hormones, there is a high likelihood of increased blood pressure and tachycardia (removed by beta-blockers).
Special instructions
Ketamine is used only in hospital or emergency settings.
To prevent increased secretion of the mucous membranes and salivary glands, atropine or methocinium iodide should be included in the premedication, and the main dose of the drug should be administered slowly (not exceeding 3 mg/kg). During ketamine anesthesia, inhale with a mixture of oxygen and air in a ratio of 1:2.
When using ketamine, you should monitor respiratory function, especially the patency of the upper respiratory tract (spasm of the masticatory muscles and retraction of the tongue are possible).
Caution should be exercised during operations on the larynx and pharynx (muscle relaxants are used).
To prevent muscle rigidity and involuntary twitching during premedication, diazepam is administered intramuscularly or intravenously.
To prevent the development of psychomimetic effects, droperidol and diazepam should be included in premedications.
Release form
Solution for intravenous and intramuscular administration 50 mg/ml. 2 ml and 5 ml in ampoules or 5 ml in vials. 5 ampoules or bottles in a blister pack.
1 or 2 blister packs (5 ampoules in each) with instructions for use in a cardboard pack; 20, 50 or 100 blister packs, respectively, with 10, 25 and 50 instructions for use in a cardboard box or cardboard box (for hospital use).
1 blister pack (5 bottles) and instructions for use in a cardboard pack; 30-50 blister packs (5 bottles each) with instructions for use (according to the number of packs) in a cardboard box or cardboard box (for a hospital).
Storage conditions
In a place protected from light and out of the reach of children. List II of the “List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation.”
Best before date
2 years. Do not use after the expiration date indicated on the packaging.
Conditions for dispensing from pharmacies
Use in a hospital setting.
Manufacturer:
Federal State Unitary Enterprise "Moscow Endocrine Plant",
Moscow, 109052, st. Novokhokhlovskaya, 25.
INN: Ketamine
Manufacturer: Farmak PJSC
Anatomical-therapeutic-chemical classification: Ketamine
Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 003486
Registration period: 31.03.2016 - 31.03.2021
Instructions
Trade name
International nonproprietary name
Dosage form
Solution for injection 50 mg/ml
Compound
1 ml of the drug contains
active substance- ketamine hydrochloride 57.6 mg (in terms of ketamine 50 mg),
excipients: benzethonium chloride, sodium chloride, water for injection.
Description
Clear, colorless or slightly colored liquid
Pharmacotherapeutic group
Anesthetics. General anesthetics. Other general anesthetics. Ketamine
ATX code N01AX03
Pharmacological properties
Pharmacokinetics
Ketamine is rapidly distributed into well-vascularized tissues, including the brain and placenta. Animal studies have shown that ketamine is highly concentrated in adipose tissue, liver and lungs. The cessation of the anesthetic effect occurs partly due to redistribution from the central nervous system to peripheral tissues, partly through biotransformation in the liver into active metabolites. The half-life is approximately 2-3 hours. It is excreted by the kidneys, mostly in the form of conjugated metabolites.
Pharmacodynamics
Ketamine is a fast-acting general anesthetic for intravenous and intramuscular use with a pronounced pharmacological effect. The drug causes so-called dissociative anesthesia, characterized by catalepsy, amnesia and severe anesthesia, which can persist during the period of recovery from anesthesia. When using Ketamine, pharyngeal-laryngeal reflexes remain normal; Skeletal muscle tone may be normal or increased to varying degrees.
There is slight stimulation of the cardiac and respiratory systems, and sometimes respiratory depression occurs.
Ketamine causes sedative and hypnotic effects, amnesia and significant analgesia. The state of anesthesia that Ketamine produces is called “dissociative anesthesia” due to the fact that it selectively interrupts associative connections in the brain before blocking proprioceptive deep sensation. It can selectively inhibit the thalamo-neocortical system before significantly blunting the centers and connections of the brain (activating the reticular formation and limbic system). Numerous theories attempt to explain Ketamine's effects, including binding to N-methyl-D-aspartate (NMDA) receptors in the central nervous system, interactions with opiate receptors, and interactions with norepinephrine, serotonin, and muscarinic cholinergic receptors. NMDA receptor activity may be responsible for the analgesic as well as psychiatric effects of Ketamine. Ketamine has sympathomimetic activity, which leads to tachycardia, hypertension, increased myocardial and cerebral oxygen consumption, increased cerebral circulation and increased intracranial and intraocular pressure. Ketamine is also a potent bronchodilator. Clinical effects that have been observed following Ketamine administration include: increased blood pressure, increased muscle tone (may resemble catatonia), eye opening (usually accompanied by nystagmus), and increased myocardial oxygen consumption.
Indications for use
As an anesthetic during diagnostic and surgical procedures. Intravenous and intramuscular injections are best for short procedures. When given in additional doses or given as an intravenous infusion, Ketamine can be used for longer procedures. If muscle relaxation is necessary, use a muscle relaxant and provide breathing support.
For induction of anesthesia before administration of other general anesthetics.
Specific indications for ketamine or types of procedures:
Carrying out anesthesia for patients who prefer intramuscular administration of the drug;
Wound care, painful procedures (dressing changes) and skin grafting in burn patients, as well as other superficial surgical procedures;
Neurodiagnostic procedures such as pneumoencephalography, ventriculography, myelography, lumbar punctures;
Diagnostic and surgical interventions in the eyes, ears, nose and mouth, including tooth extraction (note: eye movements may persist during an ophthalmic procedure);
Anesthesia for patients with a significant risk of deterioration or the need to avoid deterioration of vital functions;
Orthopedic procedures (closed reduction, manipulation, pin placement in the femur, amputation, biopsy);
Sigmoidoscopy and minor surgical procedures on the anus, rectum, circumcision and pilonidal sinus;
Cardiac catheterization procedures;
Introduction to anesthesia for caesarean section in the absence of high blood pressure;
During anesthesia in patients with asthma to minimize the risk of bronchospasm or in the presence of bronchospasm, if anesthesia cannot be delayed.
Directions for use and doses
Ketamine is administered intravenously (stream or drip) or intramuscularly.
Note: All doses are indicated in terms of the active substance ketamine.
The doses below apply to adults, elderly patients (over 65 years of age) and children. For surgical interventions in elderly patients, Ketamine can be used as monotherapy or in combination with other anesthetics.
Preoperative preparation
In emergency cases, Ketamine can be used as the only anesthetic not on an empty stomach. However, since the need to use other drugs and muscle relaxants cannot be predicted, when preparing for elective surgery, it is advisable not to consume food or liquid for 6 hours before anesthesia.
Premedication with anticholinergic drugs (for example, atropine, hyoscine, etc.) should be carried out at a certain interval before Ketamine administration in order to reduce ketamine-induced increased salivation.
Midazolam, diazepam, lorazepam or flunitrazepam, when used for premedication or as an adjunct to Ketamine, reduce the incidence of adverse reactions.
Onset of anesthesia and duration
Individual response to Ketamine may vary depending on the dose, route of administration and age of the patient, as well as concomitant use of other agents. Therefore, dose selection should be carried out individually. Ketamine is a fast-acting drug, so the patient must be in the optimal position for the procedure.
An intravenous dose of 2 mg/kg body weight provides surgical anesthesia 30 seconds after injection lasting 5-10 minutes. An intramuscular dose of 10 mg/kg body weight provides surgical anesthesia 3-4 minutes after injection lasting 12-25 minutes.
Ketamine as the sole anesthetic
Intravenous infusion
The use of Ketamine through continuous administration allows for a more precise dose selection compared to intermittent administration. This results in a shorter recovery time from anesthesia.
It is carried out at the rate of 1 mg/ml Ketamine, diluted in 0.9% sodium chloride solution or 5% dextrose.
General induction anesthesia
Administer as an infusion at a dose of 0.5-2 mg/kg.
Maintenance of anesthesia
Anesthesia can be maintained using an infusion pump at a rate of 10-45 mcg/kg/min (approximately 1-3 mg/min).
The rate of infusion depends on the patient's response to anesthesia. The dose may be reduced if a long-acting muscle relaxant is used.
Intermittent administration
Intravenous administration
The initial dose of Ketamine when administered intravenously can range from 1 mg/kg to 4.5 mg/kg (based on the active substance ketamine). The average dose required to provide surgical anesthesia lasting 5-10 minutes is 2.0 mg/kg. Slow intravenous administration (over 60 seconds) is recommended. More rapid administration may result in respiratory depression and increased blood pressure.
Intramuscular administration
The initial dose of Ketamine for intramuscular administration ranges from 6.5 mg/kg to 13 mg/kg (based on the active substance ketamine). A low initial intramuscular dose (4 mg/kg) is used for diagnostic procedures and procedures not associated with severe pain. A dose of 10 mg/kg typically provides anesthesia within 12-25 minutes.
Dosing for liver failure
The need for dose reduction should be considered in patients with liver cirrhosis or other types of liver failure (see section "Special Instructions").
Maintaining general anesthesia
Nystagmus, motor responses to stimulation and voice indicate weakening of anesthesia. To maintain anesthesia, additional doses of Ketamine are administered intravenously or intramuscularly.
Each additional dose should be one-half to the full original dose administered, regardless of route of administration.
However, involuntary movements of the limbs can occur regardless of the depth of anesthesia!
Ketamine as an inducing agent before the use of other general anesthetics
Induction is achieved by intravenous or intramuscular administration of a full dose of Ketamine. If Ketamine is administered intravenously and the primary anesthetic is delayed-acting, a repeat dose of Ketamine should be administered 5-8 minutes after the initial dose. If Ketamine is administered intramuscularly and the primary anesthetic is rapid acting, the primary anesthetic should be administered 15 minutes after the Ketamine injection.
Ketamine as an adjunct to anesthetics
Ketamine is clinically compatible with commonly used general and local anesthetics with appropriate respiratory support. The dose of Ketamine for use in combination with other anesthetics is generally in the same range, however the use of a different anesthetic may allow a lower dose of Ketamine.
Monitoring patients during the recovery period
After the procedure, the patient should be observed but not disturbed. This does not exclude monitoring of vital signs. If delirium occurs, diazepam (5 to 10 mg IV in adults) can be used. A hypnotic dose of thiobarbiturate (50 to 100 mg IV) may be used to reduce severe reactions during recovery. When using these drugs, recovery time from anesthesia may be longer.
Side effects
Adverse effects according to the frequency of occurrence are classified into the following categories: very often (>1/10); often (>1/100,<1/10); нечасто (>1/1000, <1/100), редко (>1/10000, <1/1000), очень редко (<1/10000, включая единичные случаи).
From the immune system
Rarely : anaphylactic reactions.
Metabolic disorders
Uncommon : anorexia.
Mental disorders
Often : hallucinations, abnormal or nightmares, confusion, psychomotor agitation, inappropriate behavior.
Uncommon: feeling of fear, anxiety.
Rarely: delirium, reverse frame symptom, dysphoria, insomnia, disorientation.
From the nervous system
Often : nystagmus, increased skeletal muscle tone and tonic-clonic convulsions.
From the organs of vision
Often : diplopia.
Unknown: increased intraocular pressure.
Cardiac disorders
Often : increased blood pressure and heart rate.
Uncommon: bradycardia, arrhythmia.
Vascular disorders
Uncommon : hypotension.
From the respiratory system
Often : increase in breathing rate.
Uncommon: respiratory depression, laryngospasm.
Rare: airway obstruction or respiratory arrest.
From the hepatobiliary system
Unknown : changes in laboratory parameters of liver function.
From the gastrointestinal tract
Often : nausea, vomiting.
Rarely: drooling.
From the outsideskin and subcutaneous tissues
Often: erythema and/or morbilliform rash.
Unknown: urticaria.
From the outsidekidneys and urination
Rarely : cystitis, hemorrhagic cystitis.
General disorders and reactions at the injection site
Uncommon : reactions at the injection site, including pain and/or rash at the injection site.
Contraindications
hypersensitivity to the active substance or to other components of the drug
eclampsia, preeclampsia
ketamine is contraindicated in patients in whom elevated blood pressure may pose a serious threat to life; patients with traumatic brain injury, intracranial hemorrhage, stroke, severe cardiovascular diseases, and cerebrovascular accidents.
Drug interactions
Concomitant use of barbiturates and/or other anesthesia with Ketamine causes prolongation of the time to awakening after anesthesia.
Ketamine in combination with atracurium and tubocurarine may potentiate the blockade of neuromuscular transmission, including respiratory depression and apnea.
Use of halogenated anesthetics concomitantly with Ketamine may prolong the half-life of Ketamine and increase the time to awakening from anesthesia. Concomitant use of Ketamine (especially at high doses or when administered rapidly) with halogenated anesthetics may increase the risk of bradycardia, hypotension, or decreased cardiac output.
The use of Ketamine with other drugs that reduce the activity of the central nervous system (for example, ethanol, phenothiazines, antihistamines or muscle relaxants) may enhance CNS depression and/or increase the risk of developing respiratory failure. It may be necessary to reduce the dose of the drug with the simultaneous use of sleeping pills, sedatives and tranquilizers. Ketamine has been reported to antagonize the hypnotic effects of thiopental.
In patients receiving thyroid hormone therapy, the risk of increased blood pressure and tachycardia when using Ketamine is increased.
Concomitant use of antihypertensive drugs and Ketamine increases the risk of hypotension.
When combined with aminophylline (theophylline), the seizure threshold may decrease. There is evidence of unpredictable extensor muscle cramps that were accompanied by the simultaneous use of these drugs.
Special instructions
Can be combined with any type of local anesthesia.
The drug must be prescribed by a specialist - an anesthesiologist.
As with other general anesthesia agents, resuscitation tools and equipment must be prepared when using Ketamine.
Since respiratory depression is possible when using the drug, it is necessary to have a device for artificial ventilation of the lungs. The use of the device should be combined with the use of analeptics.
Intravenous Ketamine must be administered slowly (over 1 minute). Rapid administration of the drug can lead to respiratory depression or arrest and a sharp increase in blood pressure.
Since pharyngeal reflexes are usually preserved during Ketamine therapy, mechanical irritation of the pharynx should be avoided. When intervening on the larynx, pharynx or trachea, a combination of Ketamine with muscle relaxants and careful monitoring of breathing is necessary.
During surgical interventions involving the visceral pain pathways, it may be necessary to administer other analgesics.
When using Ketamine on an outpatient basis, the patient can be released only after full recovery of consciousness and accompanied by an adult.
Ketamine should be used with extreme caution in the following conditions:
chronic alcoholism and acute alcohol intoxication;
Ketamine is metabolized in the liver and complete release through the liver results in cessation of clinical effects. Prolongation of action may occur in patients with liver cirrhosis or other types of liver failure. Therefore, the dose of Ketamine should be reduced in such patients. Abnormalities in liver function tests have also been reported that have been associated with long-term use of the drug, particularly in patients who have used the drug for more than 3 days or in individuals with drug dependence.
with increased pressure in the spinal canal;
in patients with penetrating ocular trauma and/or increased intraocular pressure (eg, glaucoma), because the pressure may increase significantly even after a single use of Ketamine;
patients with neurotic disorders or mental illnesses (for example: schizophrenia, acute psychosis);
patients with acute intermittent porphyria;
patients with epileptic seizures;
patients with hyperthyroidism or patients receiving thyroid replacement therapy (increases the risk of increased blood pressure and heart rate);
patients with infectious diseases of the upper respiratory tract or lungs (as Ketamine increases the sensitivity of the pharyngeal reflex, which in turn can cause laryngospasm).
patients with intracranial space-occupying lesions, head trauma or hydrocephalus.
Reactions and features that may be observed after the patient recovers from anesthesia.
Psychiatric disorders can range from mild to more severe, such as fantastical experiences such as those imagined in dreams, vivid visions, hallucinations, nightmares, post-anesthetic delirium (which often manifested as dissociative sensations and a feeling of free flight), in some cases these states are accompanied by confusion, psychomotor agitation and irrational behavior. The above manifestations were observed only in some patients.
During recovery from anesthesia, acute delirium may occur. This reaction can be prevented by administering benzodiazepines or reducing verbal, tactile and visual stimulation. However, this does not exclude monitoring of vital parameters.
Because Ketamine increases myocardial oxygen consumption, it should be used with caution in patients with hypovolemia, dehydration, or cardiac disease, especially those with coronary artery disease (eg, congestive heart failure, ischemic conditions, and myocardial infarction). Ketamine should also be used with caution in patients with mild to moderate hypertension and tachyarrhythmias.
Patients with hypertension or heart failure require constant monitoring of cardiac function during anesthesia. Premedication with diazepam reduces the hypertensive response. The maximum increase in blood pressure (20-25%) is observed a few minutes after intravenous administration of the drug, but after 15 minutes the blood pressure returns to initial values. Depending on the patient's condition, an increase in blood pressure may be considered a positive effect, or in other cases, an adverse reaction.
There are reported cases of cystitis, including hemorrhagic cystitis, in patients who received Ketamine over a long period (from 1 month to several years). Ketamine is not prescribed or recommended for long-term use.
Ketamine abuse has also been reported. There is evidence that ketamine contributes to symptoms such as dysphoria, hallucinations, flashback symptoms, fear and anxiety, insomnia or confusion, and cases of cystitis or hemorrhagic cystitis. Using Ketamine daily for several weeks may cause addiction, especially in individuals who have or have a history of drug addiction. Therefore, the drug must be used under close medical supervision and with caution in the above-mentioned conditions and diseases.
Incompatibility.
Due to chemical incompatibility, barbiturates cannot be administered in the same syringe with Ketamine.
If simultaneous use of Ketamine with diazepam is necessary, the drugs should be administered separately and should not be mixed in the same syringe or infusion.
Do not use solvents not specified in the section "Method of administration and dosage."
Use in pediatrics
The drug is used in pediatric practice.
Use during pregnancy and lactation
Ketamine crosses the placenta. This should be paid attention to during surgical obstetric procedures during pregnancy. With the exception of administration during cesarean section or vaginal delivery, safe use during pregnancy and lactation has not been established and such use is not recommended.
Features of the drug's effect onability to drive vehicles and potentially dangerous mechanisms
Patients should be warned not to drive or operate machinery or engage in any other hazardous activities for at least 24 hours after anesthesia.
Ketamine may impair cognitive function, which may affect your ability to drive.
Overdose
When using Ketamine, respiratory depression is possible, so a ventilator is necessary. Preference is given to mechanical respiratory support instead of the administration of analeptics.
Ketamine has a great safety factor; several cases of unintentional overdose of Ketamine (up to 10 times the required dose) were accompanied by a long but complete recovery from anesthesia.
Release form and packaging
2 ml in glass ampoules of 1 hydrolytic class with a ring or break point.
10 ml in clear glass bottles for injection, sealed with combination caps (with an aluminum cap with a rubber gasket and a plastic liner) or with a rubber stopper for injection bottles and an aluminum cap combined with a plastic cap.
Self-adhesive labels are placed on ampoules and vials.
10 ampoules, together with instructions for medical use in the state and Russian languages, are placed in a cardboard pack with corrugated inserts.
5 bottles each, along with instructions for medical use in the state and Russian languages, are placed in a cardboard pack with an insert.
Or 5 ampoules or 5 bottles are placed in a blister pack made of polymer material. 1 blister pack (with bottles) or 2 blister packs (with ampoules) together with instructions for medical use in the state and Russian languages are placed in a cardboard pack.
solution for injection 50 mg/ml: 2 ml amp. 10 pcs. or 10 ml fl. 5 pcs.Reg. No.: 8825/08/14 from 01/21/2014 - Expired
Solution for injection in the form of a clear, colorless or slightly colored liquid.
Excipients: benzethonium chloride, sodium chloride, water d/i.
2 ml - ampoules (10) - packs.
10 ml - bottles (5) - packs.
Description of active ingredients drug KETAMINE. The scientific information provided is general and cannot be used to make a decision about the possibility of using a particular drug. Update date: 01/14/2006
Means for non-inhalation anesthesia. With a single intravenous injection of ketamine, the narcotic effect occurs 30-60 seconds after administration and lasts 5-10 minutes (up to 15 minutes). With intramuscular administration of ketamine at a dose of 4-8 mg/kg, the effect occurs within 2-4 minutes (up to 6-8 minutes) and lasts on average 12-25 minutes (up to 30-40 minutes). Ketamine causes a pronounced analgesic effect (up to 2 hours), but insufficient muscle relaxation. When ketamine is administered, the pharyngeal, laryngeal and cough reflexes and independent adequate pulmonary ventilation are preserved. Metabolized in the liver.
Ketamine is a lipophilic compound and therefore is quickly distributed to organs well supplied with blood, incl. into the brain and then redistributed to tissues with reduced perfusion. Metabolized in the liver. T1/2 is 2-3 hours. It is excreted by the kidneys mainly in the form of conjugated metabolites.
For introductory and basic anesthesia, for short-term surgical interventions that require and do not require muscle relaxation, for painful instrumental and diagnostic manipulations, for transporting patients, and treating burn surfaces.
Depending on the indications, age of the patient, clinical situation, drugs used for premedication, a single dose for intravenous administration is 0.5-4.5 mg/kg, for intramuscular administration - 4-13 mg/kg.
From the cardiovascular system: increased blood pressure, tachycardia.
From the digestive system: hypersalivation.
From the side of the central nervous system: psychomotor agitation and hallucinations during recovery from anesthesia.
From the respiratory system: shortness of breath, respiratory depression.
Local reactions: extremely rarely, pain and hyperemia along the vein are possible at the injection site.
Cerebrovascular accidents, arterial hypertension, angina pectoris and heart failure in the decompensation phase, preeclampsia and eclampsia, epilepsy in childhood.
Dosage form: solution for intravenous and intramuscular administration Compound:1 ml of solution contains:
active substance
: ketamine hydrochloride (equivalent to 50 mg ketamine) 57.6 mg;excipients: benzethonium chloride 0.1 mg, sodium chloride 1.6 mg, water for injection up to 1 ml.
Description: Transparent colorless or slightly colored liquid. Pharmacotherapeutic group:means for non-inhalation general anesthesia ATX:N.01.A.X.03 Ketamine
Pharmacodynamics:Ketamine causes dissociative anesthesia - a condition in which some areas of the brain are excited and others are inhibited, which explains the manifestation of the analgesic effect with incomplete depression of consciousness and the preservation of spontaneous breathing, pharyngeal, laryngeal and cough reflexes (the dose of the drug that causes apnea is 8 times higher than hypnotic). The surgical stage of general anesthesia does not develop when using ketamine (the visceral analgesic activity of ketamine is insufficient, which should be taken into account during abdominal operations).
Causes a specific set of symptoms: somatic analgesia, a condition reminiscent of neuroleptanalgesia, increases blood pressure, myocardial contractility, minute blood volume and myocardial oxygen demand, relaxes the smooth muscles of the bronchi. It practically does not reduce the tone of skeletal muscles and can cause involuntary muscle twitching.
In adults, the minimum dose that causes a hypnotic effect with a single intravenous administration is 0.5 mg/kg of body weight (depression of consciousness lasts one and a half minutes). At a dose of 1 mg/kg, it depresses consciousness for 6 minutes, at a dose of 1.5 mg/kg - for 9 minutes, at a dose of 2 mg/kg - for 10-15 minutes. With intramuscular administration of 4-8 mg/kg, the effect occurs within 2-4 minutes (6-8 minutes) and lasts on average 12-25 minutes (up to 30-40 minutes).
In children, with intramuscular administration, general anesthesia occurs after 2-6 minutes, with intravenous administration - after 15-60 s, duration of action - 15-30 minutes and 5-15 minutes, respectively.
During the period of recovery of consciousness, drowsiness is noted, against the background of which reactions often occur in the form of hallucinations, delusions, and vivid imaginative dreams. After awakening, patients may remain disoriented, sometimes for 6-8 hours. The frequency and severity of these reactions, as well as the cardiac stimulating effect, are reduced when ketamine is combined with antipsychotics (neuroleptics) and anxiolytic drugs (tranquilizers) - droperidol, diazepam.
The analgesic effect of ketamine for somatic pain is manifested when prescribing subnarcotic doses. The maximum analgesic effect occurs 10 minutes after injection into a vein and lasts for 2-3 hours; with intramuscular administration, the effect is longer.
Pharmacokinetics:Ketamine is highly lipid-soluble, which ensures its rapid penetration into the central nervous system and easily penetrates histohematic barriers, including the blood-brain barrier. It also stimulates blood circulation. Plasma protein binding reaches 12%.
The volume of distribution is 1.8-2 l/kg, the half-life is 2-3 hours. The main part of the metabolic products is excreted within 2 hours in the urine. The main reason for the cessation of the central action of ketamine is the rapid redistribution of the drug from the brain to other tissues.
Biotransformation of ketamine is carried out by demethylation by hepatic microsomal enzymes with the formation of several metabolites, some of which retain 1/5-1/3 of the anesthetic activity of ketamine. Elimination of ketamine depends on the oxidase system of the smooth endoplasmic reticulum. The main metabolite, norketamine, has some hypnotic activity that is weaker than that of ketamine. In the process of further metabolism, norketamine is converted into hydroxylated derivatives (hydroxylation of the aromatic cyclohexylamine ring occurs in two different positions and “conjugation”), which form conjugates with glucuronic acid and are eliminated from the body.
A small amount of metabolites can remain in the body for several days; accumulation is not observed with repeated administration. With repeated anesthesia with ketamine, tolerance to the drug may occur, which is partly explained by the induction of liver enzymes.
Indications:Introductory and basic general anesthesia (especially in patients with low blood pressure or when it is necessary to maintain spontaneous breathing, or when performing artificial ventilation of the lungs with breathing mixtures that do not contain (nitrous oxide)).
Emergency surgical interventions (including at the stages of evacuation, in particular in patients with traumatic shock and blood loss).
Various surgical operations with multicomponent intravenous anesthesia.
Painful diagnostic procedures (endoscopy, catheterization of cardiac chambers), minor surgical procedures for burns, dressings and similar procedures.
Contraindications:Hypersensitivity to the drug.
Arterial hypertension and conditions accompanied by high blood pressure.
Angina pectoris, myocardial infarction (including in the last 6 months).
Chronic renal failure.
Cerebrovascular accident (including history).
Preeclampsia.
Epilepsy, epilepsy in childhood, eclampsia and other convulsive conditions.
Alcoholism.
With caution:Kidney diseases, decompensated chronic heart failure, operations on the larynx and pharynx.
Pregnancy and lactation:Ketamine crosses the placental barrier. The safety of ketamine during pregnancy has not been established. Use in this category of patients is not recommended.
Directions for use and dosage:Ketamine is administered intravenously (simultaneously as a stream or fractionally and drip) or intramuscularly.
For adults the drug is administered intravenously at a rate of 2-3 mg/kg, intramuscularly at a rate of 4-8 mg/kg body weight. To maintain anesthesia, the drug is administered at 0.5 mg/kg intravenously or 3 mg/kg intramuscularly or intravenously drip at a rate of 2 mg/kg/h (using an infusion pump or by drip administration of a solution with a concentration of 1 mg/ml (in 5 % dextrose solution (glucose) or 0.9% sodium chloride solution) at a rate of 20-50 drops/min.
In children the drug is used for induction of anesthesia for various types of combined anesthesia (administered intramuscularly once at a rate of 4-5 mg/kg in the form of a solution with a concentration of 50 mg/ml after appropriate premedication). For basic anesthesia, it is administered intramuscularly (a solution with a concentration of 50 mg/ml) or intravenously (a solution with a concentration of 10 mg/ml in a stream at once or a solution with a concentration of 1 mg/ml dropwise at a speed of 50-60 drops/min); when administered intramuscularly, the dose depends on the body weight and age of the children: newborns and infants - 8-12 mg/kg, children from 1 year to 6 years - 6-10 mg/kg, 7-14 years - 4-8 mg/kg. It is administered intravenously at a dose of 2-3 mg/kg. Anesthesia is maintained with repeated injections of ketamine (3-5 mg/kg intramuscularly or 0.5-1 mg/kg intravenously by bolus or drip injection of a solution with a concentration of 1 mg/ml at a rate of 30-60 drops/min).
To enhance the effect of ketamine, it is usually used in combination with antipsychotics () and narcotic analgesics (fentanyl, and others), and the dose of ketamine should be reduced.
Side effects:From the nervous system:
depression of the respiratory center, muscle rigidity, involuntary muscle activity (for prevention, you should pre-administer); during the period of recovery from general anesthesia - psychomotor agitation, hallucinations, prolonged disorientation, psychosis.From the side of the organ of vision: diplopia, nystagmus, increased intraocular pressure.
From the respiratory system: shortness of breath, obstruction of the upper respiratory tract due to spasm of the masticatory muscles and retraction of the tongue, increased bronchial secretion and salivation.
From the cardiovascular system: increased blood pressure, tachycardia.
From the digestive system: hypersalivation, nausea.
Local reactions: pain and hyperemia along the vein at the injection site. Overdose:When ketamine is administered in high doses intravenously (3 mg/kg), respiratory depression may occur in some cases. In these cases, artificial ventilation is indicated. When hallucinations occur, it is advisable to use antipsychotic drugs (), and for convulsive syndrome - diazepam. If necessary, carry out symptomatic therapy.
Interaction:Ketamine enhances the effect of drugs for general anesthesia, narcotic analgesics, antipsychotics (neuroleptics), anxiolytics (tranquilizers) and other drugs that depress the central nervous system.
Before using ketamine, it is necessary to discontinue lithium preparations (1-2 days before), monoamine oxidase inhibitors (15 days before). Do not mix with barbiturates in the same syringe (pharmaceutically incompatible - formation of sediment).
Droperidol and benzodiazepines, including, reduce the risk of psychotomimetic and motor activity, as well as the occurrence of tachycardia and increased blood pressure.
It is not recommended to prescribe with sympathomimetics and drugs that have a stimulating effect on the cardiovascular system (increased hypertensive and arrhythmogenic effects, increased myocardial oxygen demand).
The cardiac stimulating effect of ketamine is weakened when combined with antipsychotics and anxiolytics.
Ketamine enhances the muscle relaxant effect of tubocurarine chloride and suxamethonium iodide, but does not change the effect of pancuronium bromide.
During general anesthesia in patients taking iodine-containing drugs and thyroid hormones, there is a high likelihood of increased blood pressure and tachycardia (removed by beta-blockers).
Special instructions:Ketamine is used only in hospital or emergency settings.
To prevent increased secretion of the mucous membranes and salivary glands, the premedication should include or, and the main dose of the drug should be slowly administered (not exceeding 3 mg/kg). During ketamine anesthesia, inhale with a mixture of oxygen and air in a ratio of 1:2.
When using ketamine, it is necessary to monitor the function of external respiration, especially the patency of the upper respiratory tract (spasm of the masticatory muscles and retraction of the tongue are possible).
Caution should be exercised during operations on the larynx and pharynx (muscle relaxants are used).
To prevent muscle rigidity and involuntary twitching during premedication, diazepam is administered intramuscularly or intravenously.
To prevent the development of psychotomimetic effects, the composition of premedications should include,.
Increased intracranial pressure may occur after ketamine use.
The use of the drug may provoke the development of acute mental disorders during recovery from anesthesia. Caution must be exercised in patients with acute mental disorders (also in the presence of such indications in the anamnesis), in patients with alcohol intoxication.
Ketamine addiction may develop in patients with drug addiction or who have previously abused drugs.
Impact on the ability to drive vehicles. Wed and fur.:After using ketamine, patients should refrain from driving and other potentially hazardous activities for at least 24 hours. Release form/dosage:Solution for intravenous and intramuscular administration 50 mg/ml.
Package:In ampoules of 2 ml and 5 ml, in bottles of 5 ml.
5 ampoules in a blister pack.
1 or 2 blister packs with instructions for use, a knife or an ampoule scarifier in a cardboard pack.
20, 50 or 100 blister packs, respectively, with 20, 50 or 100 instructions for use, knives or ampoule scarifiers in a cardboard box or corrugated cardboard box.
A coupon with the packer's number is placed in a cardboard box or corrugated cardboard box.When packaging ampoules with notches, rings and break points, do not use knives or ampoule scarifiers.
5 bottles in a blister pack.
1 blister pack with instructions for use in a cardboard pack.
30 or 50 contour strip packs, respectively, with 30 or 50 instructions for use in a cardboard box or corrugated cardboard box.
A coupon with the packer's number is placed in a cardboard box or corrugated cardboard box.
Storage conditions:List II. "List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation", in specially equipped premises with a license for the specified type of activity.
In a place protected from light at a temperature not exceeding 25 ° C.
Best before date: Do not use after the expiration date stated on the packaging. Conditions for dispensing from pharmacies: For hospitals Registration number: P N000298/01 Registration date: 17.10.2011 Owner of the Registration Certificate:MOSCOW ENDOCRINE PLANT, FSUE Russia Manufacturer: Representative office: MOSCOW ENDOCRINE PLANT FSUE Russia Information update date: 17.10.2011 Illustrated instructions1 ml of 5% solution contains 50 mg of active ingredient ketamine hydrochloride .
Release form
Ketamine is available in ampoules of 2 and 10 ml. Each cardboard pack contains 10 ampoules.
Pharmacological action
What is Ketamine? This is a drug that, when administered intramuscularly or intravenously, can have narcotic (anesthetic) and analgesic effects. Pharmacological group – "Anesthetics" . The active substance has a short-term effect, and in narcotic doses allows you to maintain adequate independent breathing. The drug has dissociative general anesthesia, which is explained by its inhibitory effect on the subcortical formations of the thalamus and the associative zone.
Mechanism of action of Ketamine based on selective suppression of neuronal transmission in the structure of the cerebral cortex, as in thalamus , and in associative zones. At the same time, there is stimulation limbic system And hippocampus . As a result, functional separation of nonspecific connections develops in the structure of the thalamus and midbrain, incoming nociceptive afferent stimuli to the higher brain centers from the spinal cord are blocked, and impulse transmission to the medulla oblongata (reticular formation) is inhibited. It is believed that the analgesic and hypnotic effects of Ketamine are associated with the influence of the active substance on various types of receptors. The effects of the drug are not associated with blocking sodium channels in the nervous system and effects on GABA receptors. Wikipedia contains information on the history of Ketamine synthesis.
Pharmacodynamics and pharmacokinetics
Ketamine is a lipophilic compound that can be distributed quite quickly, first in well-supplied organs, and then in tissues with reduced perfusion. Metabolized in the hepatic system. It is excreted through the kidneys in the form of conjugated substances-metabolites.
Indications for use
Ketamine what is it? The medication is used both for mononarcosis (1 component) and for combined anesthesia, mainly in people with low blood pressure, or when it is necessary to maintain spontaneous breathing in the patient. Most often, Ketamine is used during evacuation during massive and traumatic shock, during short-term cardiac surgery, and in emergency surgery. Ketamine is prescribed for:
- cardiac catheterization ;
- endoscopic manipulations;
- dressings in otorhinolaryngology, ophthalmology and dentistry.
The medication can be used in obstetric practice.
Contraindications
- eclampsia in severe forms of circulatory decompensation;
- pronounced .
If necessary, use muscle relaxants During operations on the larynx, Ketamine is prescribed with caution. Mixing with barbiturate solutions is unacceptable due to the risk of precipitation.
Side effects
The medication has a general effect on the human body. When the solution is administered, a rise in blood pressure by 20-30%, an increase in heart rate, an increase in minute blood volume, and a decrease in peripheral vascular resistance are recorded. Application of Sibazon ( ) helps reduce the stimulating effect of Ketamine on cardiac activity. In most cases, the active component does not inhibit the reflexes of the upper respiratory tract and does not cause bronchospasm, laryngospasm, vomiting or nausea. Respiratory depression recorded with rapid intravenous infusion of solution. and Metacin can reduce salivation. When the medication is administered, hypertonicity and involuntary movements may be recorded (it can be stopped with the administration of tranquilizers). There may be redness of the skin along the vein at the injection site; upon awakening from anesthesia - prolonged disorientation And psychomotor agitation .
Instructions for use of Ketamine (Method and dosage)
The solution is administered intravenously (fractionally/in a stream) or intramuscularly. Adults are administered intravenously 2-3 mg, intramuscularly - 4-8 mg per 1 kg of weight. Repeated administration of Ketamine allows prolongation of anesthesia (rate 2 mg/kg/hour). This method of administration is possible in the presence of infusion pumps or is achieved by drip administration of a 1% Ketamine solution in sodium chloride solution or isotonic solution (30-60 drops per minute).
In pediatric practice, the solution is used for combined anesthesia. The calculation is made according to the following scheme: 4-5 mg/kg in the form of a 5% solution. Mandatory premedication is required.
The drug can be used in conjunction with analgesics ( , depidolor, etc.) and antipsychotics (for example, Droperidol), however, this requires a dose reduction.
Overdose
Registered respiratory depression , which requires timely artificial ventilation .
Interaction
Ketamine is chemically incompatible with barbiturates (a precipitate is formed). The medication is capable of potentiating the effect of all drugs used for inhalation anesthesia . The drug enhances the effect of tubocurarine, but does not affect the effectiveness of succinylcholine and pancuronium.
Terms of sale
Sold only for hospitals and medical institutions, not intended for free sale.
Storage conditions
Best before date
Special instructions
In case of pathology of the renal system, use with caution. During surgical interventions on the pharynx and larynx, the administration of muscle relaxants is mandatory. During the day after the administration of Ketamine, you should not drive a vehicle due to slow reaction and decreased attention.
Analogues
Level 4 ATX code matches:- Ketanest;
- Ketalar .
During pregnancy and lactation
The active component passes through the placental barrier. At the moment, the safety of Ketamine has not been established. Not recommended for pregnant women and .
