Intravenous anesthesia with ketamine. Calypsol, solution for injection (ampoules) Interactions with other drugs

Kalipsol: instructions for use and reviews

Latin name: Calypsol

ATX Code: N01AX03

Active substance: ketamine (ketamine)

Manufacturer: Gedeon Richter (Hungary)

Description and photo update: 23.11.2018

Calypsol is a drug for non-inhalation anesthesia.

Release form and composition

Release form Calipsol - solution for injection (10 ml in dark glass bottles, in a cardboard pack 5 bottles).

Composition per 1 ml of solution:

• active ingredient: ketamine hydrochloride - 57.67 mg (in terms of ketamine - 50 mg);
• auxiliary ingredients: sodium chloride, benzethonium chloride, water for injection.

Pharmacological properties

Pharmacodynamics

The active component of Calypsol, ketamine, causes the so-called. dissociative anesthesia, which is a functional dissociation between the thalamo-neocortical and limbic systems. Its analgesic effect is manifested already at a subdissociative dose and is longer in time than anesthesia. Sedative and hypnotic effects are less pronounced. In the region of peripheral nerves and spinal cord, the substance exhibits a local anesthetic effect.

As a result of the use of ketamine, muscle tone does not change or may increase, and therefore protective reflexes are usually not affected. The threshold of convulsive readiness does not decrease. Spontaneous breathing can cause an increase in intracranial pressure, so it is recommended to use the method of controlled breathing.

The ability of ketamine to cause sympathicotonia can lead to an increase in blood pressure (BP) and heart rate (HR), an increase in coronary blood flow increases myocardial oxygen demand. Ketamine has a direct antiarrhythmic effect on the heart and has a negative inotropic effect. The total peripheral vascular resistance (OPVR) remains unchanged.

The consequence of the use of ketamine is significant hyperventilation, while the parameters of blood gases do not change significantly. Calypsol has a relaxing effect on the muscles of the bronchi.

Ketamine does not affect metabolism, kidneys, liver, endocrine glands, gastrointestinal tract (GIT) and blood clotting.

Pharmacokinetics

• absorption: ketamine is a fat-soluble compound; after intravenous (in / in) administration, its maximum concentration (Cmax) in blood plasma is determined after 1 min, after intramuscular (i / m) administration - after 5-30 (average 20) minutes; bioavailability with i / m administration - 93%;
• distribution and metabolism: the substance binds to plasma proteins by about 47%; The α-phase, clinically manifested by an anesthetic effect, lasts 45 minutes. In tissues with a good blood supply (for example, in the brain), ketamine is distributed quickly. Its concentration in tissues corresponds to an open two-phase model. The cessation of the anesthetic effect occurs as a result of the redistribution of the active substance from the central nervous system (CNS) to peripheral tissues with a weaker blood supply and its biotransformation in the liver with the formation of active metabolites, one of which has a hypnotic effect;
• excretion: the substance is excreted by the kidneys, mainly (up to 90%) in the form of metabolites; the half-life (T 1/2) in the α-phase for ketamine is 10-15 minutes, in the β-phase - about 2.5 hours.

Indications for use

According to the instructions, Calypsol is recommended for induction and basic anesthesia during the following short-term surgical interventions, painful diagnostic and instrumental manipulations (in combination with other anesthetics and local anesthetics or as monotherapy):

• painful procedures (including dressing changes in patients with burns);
• endoscopy;
• neurodiagnostic examination (including pneumoencephalography, ventriculography, myelography);
• painful manipulations in ophthalmology;
• surgical interventions in the oral cavity or neck;
• painful procedures on the ENT organs;
• gynecological extraperitoneal surgical interventions (including colpopexy);
• operations in obstetrics, introduction to anesthesia during caesarean section;
• painful manipulations in traumatology and orthopedics;
• anesthesia in patients with arterial hypotension in a state of shock (due to the peculiarities of the effect of ketamine on cardiac activity and blood circulation);
• anesthesia in patients for whom intramuscular administration of the drug is preferable (for example, in children).

Contraindications

• severe/poorly controlled hypertension with BP > 180/100 mmHg Art.;
• diseases / conditions that can be complicated due to arterial hypertension (including congestive heart failure, severe cardiovascular pathologies, traumatic brain injury, intracranial hemorrhage, brain tumors, stroke);
• anamnestic data on mental illness (schizophrenia, acute psychosis), convulsions;
• eclampsia or preeclampsia;
• hyperthyroidism (untreated or undertreated);
• hypersensitivity to the components of the drug.

Instructions for use Calipsol: method and dosage

• intravenous administration: initial dose - 0.7-2 mg / kg of body weight, the surgical stage of anesthesia lasts from 5 to 10 minutes, the effect after administration begins in about 30 seconds. For patients in serious condition (including in a state of shock) and elderly patients, a dose of 0.5 mg / kg of body weight is recommended;
• i / m administration: initial dose - 4-8 mg / kg of body weight, the surgical stage of anesthesia lasts from 12 to 25 minutes, the effect after administration begins in a few minutes;
• IV drip: 1 vial (500 mg) of ketamine is diluted with 500 ml of saline or 5% dextrose/glucose solution. The initial dose is 80–100 drops per minute, the maintenance dose is 20–60 drops per minute (2–6 mg/kg/h).

If it is necessary to maintain general anesthesia, Calypsol is administered intramuscularly or intravenously repeatedly in an amount from half to the entire initial dose.

Nystagmus and the patient's motor response to stimuli indicate an insufficiency of anesthesia, in which case it may be necessary to administer it in a second dose. However, involuntary limb movements may occur regardless of the depth of anesthesia.

Side effects

• cardiovascular system: often - tachycardia, arterial hypertension; possibly - arterial hypotension, bradycardia, arrhythmia. The maximum increase in blood pressure is observed a few minutes after the on / in the introduction of Calypsol, after 15 minutes, blood pressure decreases to its original value; cardiostimulatory efficacy can be prevented by the previous intravenous administration of diazepam at a dose of 0.2–0.25 mg/kg of body weight;
• central and peripheral nervous system: an increase in skeletal muscle tone, often accompanied by tonic / clonic convulsive movements (does not indicate a decrease in the depth of anesthesia, does not require an additional dose of Calypsol); during awakening, visual hallucinations, vivid dreams, emotional disturbances, psychomotor agitation, delirium, disorientation are possible (less often observed in patients under 15 years of age and after 65 years of age);
• digestive system: nausea, salivation, vomiting, loss of appetite;
• respiratory system (due to rapid administration or in case of overdose): often - depression or respiratory arrest; rarely - laryngospasm;
• organ of vision: possible - nystagmus, diplopia, moderate increase in intraocular pressure;
• allergic and local reactions: rarely at the injection site - pain, rash; in isolated cases - transient erythema / morbilliform rash, anaphylaxis;
• other reactions: tolerance to the drug (as a rule, with repeated use of Calypsol for a short period; especially in young children; the desired effect in this case is achieved by an appropriate increase in dose).

Overdose

Calypsol has a wide therapeutic index.

Overdose symptoms are respiratory depression/stopping.

special instructions

Calypsol can only be used by an experienced anesthesiologist in a specialized intensive care unit equipped with the necessary facilities.

Only after evaluating the benefit / risk ratio of anesthesia with special care should an anesthetic be used in the following cases: within six months after the state of unstable angina, myocardial infarction; in patients with increased intracranial pressure, glaucoma or penetrating eye injury; in case of alcohol intoxication.

In / in the drug is administered slowly (for 1 minute). With the rapid introduction of Calipsol, respiratory depression and a sharp increase in blood pressure are possible.

In case of arterial hypertension or heart failure, continuous monitoring of cardiac function is required during anesthesia.

Since the introduction of Calypsol usually does not affect pharyngeal reflexes, mechanical irritation of the pharynx must be avoided. During surgical interventions on the pharynx, trachea or larynx, the combined use of Calypsol with other muscle relaxants, as well as careful control of breathing, is necessary.

Operations involving visceral transmission of pain sensitivity may require the introduction of other painkillers.

In obstetric interventions, during which complete relaxation of the muscles of the uterus is necessary, it is not recommended to administer ketamine as monotherapy.

Diagnostic/therapeutic interventions on the organ of vision are usually not performed under local anesthesia.

When you come out of anesthesia, acute delirium may begin. Such a reaction can be prevented by the administration of benzodiazepines or by reducing the effect of tactile, verbal and visual stimuli. This requires monitoring of vital signs of the state of the body.

After using Calypsol in an outpatient setting, the patient is released only after full recovery of consciousness, always accompanied by an adult.

Influence on the ability to drive vehicles and complex mechanisms

To restore the cognitive and psychophysical functions of the body after the use of Calypsol, the patient needs at least 12 hours. At this time, you should avoid driving vehicles, as well as performing other types of work that require an increased concentration of attention and speed of psychomotor reactions.

Use during pregnancy and lactation

When conducting experimental studies on animals, no teratogenic effect of ketamine was observed.

The use of Calypsol for anesthesia during pregnancy is permissible after assessing the ratio of benefit to the mother and risk to the fetus. Ketamine crosses the placental barrier quickly. In obstetrics, it should be used in low doses. Doses of 2 mg/kg or more may cause respiratory depression in the newborn.

Data on the release of ketamine during lactation are not available.

drug interaction

When used simultaneously with barbiturates and opioid analgesics, ketamine potentiates their muscle relaxant effect, enhances the effectiveness of tubocurarine and ergometrine, but does not affect the effect of pipecuronium, pancuronium and succinylcholine.

The duration of action of ketamine is increased by inhalation anesthetics, including fluorinated hydrocarbons (enflurane, ftorothane, isoflurane, methoxyflurane), and barbiturates.

Sleeping pills (especially benzodiazepine derivatives) and antipsychotics (antipsychotics) prolong the effect of ketamine, reducing the chance of side effects.

The simultaneous use of Calypsol with aminofillin can reduce the threshold for convulsive readiness.

Calypsol is pharmacologically compatible with other muscle relaxants and anesthetics.

The use of Calypsol in patients receiving thyroid hormones may lead to an increase in blood pressure and tachycardia.

Pharmaceutical interaction:

• barbiturates: they show chemical incompatibility with ketamine, they cannot be administered in one syringe;
• diazepam: should not be mixed with ketamine in the same syringe or infusion solution, they must be administered separately.

Analogues

Analogues of Calypsol are: Ketalar, Ketamine, Ketagest, Velonarkon, Ketanest, etc.

Terms and conditions of storage

Store in a place protected from light at a temperature of 15–30 °C. Keep away from children.

Shelf life - 5 years.

Terms of dispensing from pharmacies

The drug is intended for use in a hospital only.

Ketamine (2-(2-chlorophenyl)-2-(methylamino)-cyclohexanone hydrochloride) is a general anesthetic with a pronounced analgesic effect. The drug causes the so-called dissociative anesthesia, which is described as a functional dissociation between the thalamo-neocortical and limbic systems. The analgesic effect of the drug is already manifested when it is used in a subdissociative dose and lasts longer than anesthesia. Sedative and hypnotic effects are less pronounced. In the region of the spinal cord and peripheral nerves, the drug has a local anesthetic effect.
When using ketamine, muscle tone remains unchanged or may increase. Therefore, protective reflexes are usually not affected. The seizure threshold is not reduced. Spontaneous breathing may increase intracranial pressure. This can be avoided with controlled breathing.
Since ketamine causes sympathicotonia, blood pressure and heart rate may increase, along with an increase in coronary blood flow, myocardial oxygen demand increases. Ketamine exhibits a negative inotropic effect, has an antiarrhythmic effect, and does not affect the peripheral vascular resistance.
After the use of ketamine, significant hyperventilation is noted without large deviations in the blood gas composition. Ketamine relaxes the smooth muscles of the bronchi.
Ketamine is fat soluble. The maximum concentration of ketamine in the blood plasma is determined 20 (5-30) minutes after the intravenous administration of the first dose. When administered intramuscularly, bioavailability is 93%. About 47% of ketamine binds to plasma proteins. The first phase of action (alpha phase) lasts about 45 minutes, the half-life is 10-15 minutes. Clinically, the first phase is manifested by the anesthetic effect of the drug. Ketamine is rapidly distributed to well-vascularized tissues (eg, the brain). The concentration of ketamine in tissues corresponds to a biphasic open model. The anesthetic effect is terminated due to redistribution from the central nervous system to less blood-supplying peripheral tissues and biotransformation in the liver into active metabolites. One of the metabolites of ketamine has a hypnotic effect. The half-life in the second phase (beta phase) is about 2.5 hours. 90% of the metabolites are excreted in the urine. Ketamine crosses the placenta.

Indications for the use of the drug Calypsol

As an independent tool for short-term surgical interventions for diagnostic or therapeutic purposes in children and, in special cases, in adults.
For the introduction into anesthesia and its maintenance (for anesthesia in combination with other drugs, especially with benzodiazepines, the drug is prescribed in a reduced dose).
Special indications for which ketamine is prescribed alone or in combination with another drug:

• painful procedures (change of dressing for burns, etc.);
• neurodiagnostic procedures (pneumoencephalography, ventriculography, myelography, etc.);
• endoscopy;
• some procedures on the organ of vision;
• surgical interventions in the neck or oral cavity;
• otorhinolaryngological interventions;
• gynecological extraperitoneal interventions;
• interventions in obstetrics, introduction to anesthesia during caesarean section;
• interventions in orthopedics and traumatology;
• conducting anesthesia in patients in a state of shock, with arterial hypotension (due to the peculiarities of the action of ketamine on the heart and blood circulation);
• conducting anesthesia in patients in whom intramuscular administration of the drug is preferable (for example, in children).

The use of the drug Calypsol

The individual response to Calypsol, as well as to other general anesthetics, varies depending on the dose, route of administration and age of the patient. Therefore, it is necessary to prescribe the drug individually. When using ketamine in combination with other agents, its dose should be reduced.
In / in the introduction
An initial dose of 0.7-2 mg/kg body weight provides adequate surgical anesthesia lasting 5-10 minutes approximately 30 seconds after administration (in patients at high risk, the elderly or in a state of shock, the dose is 0.5 mg/kg).
V / m introduction
An initial dose of 4-8 mg/kg provides surgical anesthesia lasting 12-25 minutes a few minutes after administration.
In/in drip
500 mg ketamine + 500 ml isotonic solution of sodium chloride or glucose.
The initial dose is 80-100 drops per minute.
Maintenance dose - 20-60 drops per minute (2-6 mg / kg / h).
The dose for an adult is 2-6 mg / kg / h.
Maintenance of anesthesia
If necessary, re-introduce / m or / in half the initial dose or the full initial dose.
Involuntary movements of the limbs are possible regardless of the depth of anesthesia, but nystagmus or a motor reaction to irritation indicate its insufficient depth. In this case, it may be necessary to re-administer the drug.

Contraindications to the use of the drug Calipsol

Hypersensitivity to ketamine, severe or poorly controlled hypertension (arterial hypertension) (BP 180/100 mm Hg at rest), pathology in which an increase in blood pressure can worsen the patient's condition (congestive heart failure, severe diseases of the cardiovascular system , traumatic brain injury, intracranial hemorrhage, stroke), eclampsia or preeclampsia, insufficiently controlled hyperthyroidism, a history of seizures, mental illness (schizophrenia, acute psychosis).

Side effects of Calipsol

From the side of the cardiovascular system: transient increases in blood pressure and heart rate are often noted. The maximum increase in blood pressure (by 20-25%) is detected a few minutes after the intravenous administration of the drug, but after 15 minutes the blood pressure returns to its original values. This effect of ketamine can be prevented by pre-in / in the introduction of diazepam at a dose of 0.2-0.25 mg / kg. Possible bradycardia, arterial hypotension, arrhythmia.
From the respiratory system: with rapid on / in the introduction or in case of overdose, depression or respiratory arrest is often noted. Laryngospasm is rare.
From the organ of vision: diplopia, nystagmus, moderate increase in intraocular pressure.
From the nervous system: an increase in skeletal muscle tone can often cause tonic and clonic movements that do not indicate a decrease in the depth of anesthesia and do not require the introduction of an additional dose of the drug.
During the period of recovery from anesthesia, vivid dreams, visual hallucinations, emotional disturbances, delirium, psychomotor agitation, and a feeling of confusion may occur. These phenomena are noted less frequently in patients under the age of 15 and over 65 years.
From the digestive tract: anorexia, nausea, vomiting, salivation.
Other: rarely - pain at the injection site, rash. Cases of transient erythema and/or measles-like rash have been described, and one case was an anaphylactoid reaction.
With repeated use over a short period, especially in young children, tolerance to the drug was noted. In these cases, the desired effect can be achieved by an appropriate dose increase.

Special instructions for the use of the drug Calypsol

Calypsol can only be administered by an anesthesiologist in a specially equipped medical institution. The drug can be used in combination with any type of local anesthesia. Calypsol is prescribed with caution, after assessing the benefit-risk ratio, within 6 months after myocardial infarction or unstable angina, with increased intracranial pressure, glaucoma or penetrating eye injury.
The duration of the / in the introduction of Calipsol - 1 min. Rapid administration can cause respiratory depression and a sharp increase in blood pressure.
In patients with hypertension (arterial hypertension) or heart failure during anesthesia, continuous monitoring of cardiac function is necessary.
Due to the fact that with the independent use of Calypsol, pharyngeal reflexes are usually preserved, mechanical irritation of the pharynx should be avoided. For interventions on the larynx, pharynx or trachea, Calypsol should be used in combination with muscle relaxants and monitoring of breathing should be carried out.
In surgical interventions involving the visceral pathways of pain sensitivity, the introduction of other analgesics may be required.
In obstetric interventions requiring complete relaxation of the uterus, the use of ketamine alone is not indicated.
For diagnostic or therapeutic interventions on the organ of vision, the use of local anesthetics is not indicated.
Ketamine should be used with extreme caution in alcohol intoxication.
In the period of recovery from anesthesia, acute delirium is possible. Its occurrence can be prevented by the administration of benzodiazepines or the reduction of verbal, tactile and visual stimuli. This does not exclude monitoring of vital parameters.
When using Calypsol on an outpatient basis, the patient can be released home only after full recovery of consciousness with the accompanying person.
Within 12 hours after the use of ketamine, you can not drive vehicles.
Ketamine quickly crosses the placenta. During pregnancy, it can be used only after assessing the benefit / risk ratio, although it has not been experimentally established that it has a teratogenic effect. When anesthesia in obstetric practice, the drug should be used in lower doses. A dose of 2 mg/kg body weight can lead to respiratory depression in the newborn. There is no data on whether ketamine passes into breast milk.

Interactions of the drug Calypsol

Ketamine potentiates the neuromuscular effect of barbiturates, opioids, and also enhances the action of tubocurarine and ergometrine, but does not affect the action of pancuronium and succinylcholine.
Barbiturates and inhalational anesthetics, in particular fluorinated carbohydrates (halothane, enflurane, isoflurane, methoxyflurane), increase the duration of action of ketamine.
Sleeping pills (especially benzodiazepine derivatives) or neuroleptics increase the duration of action of ketamine and reduce the chance of side effects.
Calypsol is compatible with other anesthetics and muscle relaxants.
With simultaneous therapy with thyroid hormones, an increase in blood pressure and tachycardia are possible.
When combined with aminophylline, the convulsive threshold may decrease.
Due to the chemical incompatibility of barbiturates with ketamine, they cannot be administered in the same syringe.
If necessary, the simultaneous use of ketamine with diazepam drugs should be administered separately, without mixing in one volume.

Overdose of the drug Calypsol, symptoms and treatment

With rapid administration or with the introduction of high doses, respiratory depression or cessation is possible. In this case, mechanical ventilation is used until adequate spontaneous breathing is restored.

Storage conditions of the drug Calypsol

In a place protected from light at a temperature of 15-30 ° C.

List of pharmacies where you can buy Calypsol:

• St. Petersburg

A drug that is used primarily for induction of anesthesia. Calypsol is also used as an anesthetic for patients who are contraindicated in the use of opioid and barbiturate drugs.

Release form and composition

Solution for intravenous, intramuscular and drip injections. Produced in bottles of 10 ml.

One bottle (10 ml) of the solution contains 576.7 ketamine hydrochloride, which corresponds to 500 mg of ketamine.

pharmachologic effect

Means for non-inhalation anesthesia. Provides an analgesic effect in case of insufficient muscle relaxation and preservation of reflexes and self-ventilation of the lungs.

Pharmacodynamics

• • The active substance acts quickly, but the effect lasts for a short time
  • With intravenous injection, the duration of action is 10-15 minutes, with intramuscular injection - 25-30 minutes

• Visceral analgesic activity is insufficient, therefore, Calypsol is rarely used in abdominal operations.
• There are often stories about terrible hallucinations after anesthesia with Calypsol - this side effect takes place and is facilitated by the combination of the drug with antipsychotics
• In addition to general analgesia, the features of anesthesia with Calypsol are some specific symptoms - a bronchodilatory effect, increased blood pressure and heart rate, catalepsy, somatic analgesia.

Pharmacokinetics

• Since the active substance is a lipophilic compound, it quickly penetrates into the central nervous system, and then into the blood-supplying peripheral tissues.
• Bioavailability with intramuscular injection - 93%
• Communication with plasma proteins - 47%
• The maximum concentration in the blood plasma of the active substance reaches 20 minutes after intravenous injection.
• Metabolized in the liver to active metabolites, one of which has a hypnotic effect
• Half-life - 2.5 hours
• 90% of metabolites are excreted by the kidneys
• Crosses the placental barrier, found in breast milk

Indications

Alone or in combination with other drugs, Calypsol is prescribed in the following cases:

• • Medical procedures that are characterized by severe pain
  • Endoscopy
  • Neurodiagnostic procedures
  • Some procedures on the organs of vision
  • Otorhinolaryngological procedures
  • Operations on the neck and in the oral cavity
  • C-section

• Operations in orthopedics and traumatology
• The use of anesthesia with Calypsol is indicated for patients with low blood pressure.
• In cases where intramuscular administration of an anesthetic is more preferable

Contraindications

• High blood pressure
• Eclampsia
• Hyperfunction of the thyroid gland
• Pathologies of the central nervous system, which are characterized by increased intracranial pressure
• Diseases of the liver and kidneys
• Severe decompensation of systemic circulation
• Diseases of the cardiovascular system
• Having a history of mental illness
• Epilepsy

Side effects

The cardiovascular system

1. Increase in blood pressure
2. Increased heart rate
3. Bradycardia
4. Arrhythmia
5. Lowering blood pressure

Nervous system

1. vivid dreams
2. hallucinations
3. Delirium
4. psychomotor agitation
5. Emotional disorders

Respiratory system

1. With rapid intravenous administration - depression or respiratory arrest
2. laryngospasm

sense organs

1. Slight increase in intraocular pressure
2. nystagmus
3. Diplopia

Digestive system

1. Nausea
2. Vomit
3. Salivation
4. Anorexia

Instructions for use

Important! Application is possible only in a hospital or during an ambulance.

For introduction into anesthesia, Calypsol is administered intravenously or intramuscularly, to maintain it - only drip.

• Intravenous administration: 0.7-2 mg per kilogram of body weight. For the elderly and patients in shock, the dosage is reduced to 0.5 mg / kg
• Intramuscular administration: 4-8 mg/kg
• Maintenance dose: 500 mg Ketamine and 500 ml saline, initially 80-100 drops per minute, later 20-60 drops per minute (2-6 mg/kg/h)
• A second injection of the drug may be required only if, after the first dose, an insufficient depth of anesthesia is recorded.

Overdose

With too rapid intravenous administration or an increased dosage of Calypsol, the center of respiration is strongly inhibited, up to the cessation of respiratory activity. A ventilator is used to restore spontaneous breathing.

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Instructions for medical use

medicinal product

Calypsol ®

Tradename

Calypsol ®

International non-proprietary name

Ketamine

Dosage form

Solution for injection, 50 mg/ml

Compound

One bottle of the drug contains:

active substance : ketamine 500 mg (as ketamine hydrochloride 576.7 mg)

Excipients : benzethonium chloride, sodium chloride, water for injection

Description

Clear colorless or almost colorless solution

Pharmacotherapeutic group

Anesthetics. General anesthetics. Other general anesthetics. Ketamine

ATX code N01A X03

Pharmacological properties

Pharmacokinetics

Ketamine is fat soluble. The maximum plasma concentration is observed one minute after intravenous administration and 20 (5-30) minutes after intramuscular administration. When administered intramuscularly, the bioavailability is 93%. About 47% of ketamine binds to blood proteins. The first phase of the drug (alpha phase) lasts about 45 minutes, t 1/2 = 10-15 minutes. Clinically, the first phase is manifested by the anesthetic effect of the drug. Ketamine is distributed rapidly in well-vascularized tissues (eg, the brain). The concentration of Calypsol ® in tissues corresponds to a two-phase open model. The cessation of the anesthetic effect occurs due to redistribution from the central nervous system to less blood-supplying peripheral tissues and biotransformation in the liver into active metabolites. Among the metabolites of ketamine, there is one that has a hypnotic effect. The half-life of the second phase (beta phase) is about 2.5 hours. 90% of metabolites are excreted through the kidneys. Ketamine crosses the placenta.

Pharmacodynamics

Ketamine is an anesthetic with analgesic action. The drug causes the so-called dissociative anesthesia, which is described as a functional dissociation between the thalamo-neocortical and limbic systems. The analgesic effect of the drug is already manifested at a subdissociative dose and lasts longer than anesthesia. Sedative and hypnotic effects are less pronounced. In the region of the spinal cord and peripheral nerves, the drug exhibits a local anesthetic effect.

When using ketamine, muscle tone remains unchanged or may increase, so protective reflexes are usually not affected. The seizure threshold does not decrease. Spontaneous breathing may increase intracranial pressure, which can be avoided by controlled breathing.

Since ketamine causes sympathicotonia, blood pressure and heart rate may increase, along with an increase in coronary blood flow in the myocardium, oxygen demand increases. Ketamine has a negative inotropic effect and an antiarrhythmic effect (direct cardiac effect). Due to the antagonistic action, peripheral vascular resistance does not change.

After the use of ketamine, there is significant hyperventilation, without significant deviations in the parameters of blood gases. Ketamine relaxes the bronchial muscles.

Ketamine does not affect metabolism, liver, kidneys, endocrine glands, gastrointestinal tract and blood clotting.

Indications for use

As monotherapy for short diagnostic or therapeutic interventions in childhood and in some special cases in adults: induction and maintenance of anesthesia

In a reduced dose in combination with other drugs used for general anesthesia (especially with a benzodiazepine). Can be combined with any type of local anesthesia.

Special indications in which ketamine is indicated (in monotherapy or in combination with another drug):

Painful procedures (for example, changing a dressing for a patient with burns)

Neurodiagnostic procedures (eg, pneumoencephalography, ventriculography, myelography)

Endoscopy

Some procedures on the organ of vision

Surgery in the neck or mouth

Otorhinolaryngological interventions

Gynecological extraperitoneal interventions

Interventions in obstetrics, anesthesia for caesarean section

Interventions in orthopedics and traumatology

In connection with the peculiarities of the action of ketamine on the heart and blood circulation: anesthesia in patients in a state of shock, with hypotension

Conducting anesthesia in patients in whom intramuscular administration of the drug is preferable (for example, in children)

Dosage and administration

The individual response to Calypsol ®, as with other systemic anesthetics, varies depending on the dose, route of administration and age of the patient. Therefore, the appointment of the drug should be made individually.

When used in combination, the dose of ketamine should be reduced.

Intravenous administration

An initial dose of 0.7-2 mg per kg of body weight, which provides adequate surgical anesthesia for 5-10 minutes approximately 30 seconds after administration. (In patients at high risk, the elderly, or those in shock, the recommended dose is 0.5 mg/kg body.) Kalypsol ® intravenously should be administered slowly (over 1 minute).

Intramuscular administration

An initial dose of 4-8 mg/kg body weight, which provides surgical anesthesia lasting 12-25 minutes a few minutes after administration.

Drip

500 mg of ketamine + 500 ml of glucose solution or sodium chloride solution. Recommended starting dose: 2-6 mg/kg body hour.

Anesthesia Support

If necessary, half of the initial dose or the initial dose can be re-administered intramuscularly or intravenously.

(The appearance of nystagmus, a motor reaction to stimuli indicate a lack of anesthesia, so in this case a second dose may be required. However, involuntary movements of the limbs may occur regardless of the depth of anesthesia!)

Side effects

- vivid dreams, visual hallucinations, emotional disturbances, delirium, psychomotor agitation, confusion (these phenomena are observed less often in patients younger than 15 years and older than 65 years)

An increase in skeletal muscle tone can often cause tonic and clonic movements, which do not indicate a decrease in the depth of anesthesia, and therefore do not require the introduction of an additional dose of the drug.

Diplopia, nystagmus, moderate increase in intraocular pressure

There is often a temporary increase in blood pressure and heart rate. The maximum increase in blood pressure (20-25%) is observed a few minutes after the intravenous administration of the drug, but after 15 minutes the blood pressure returns to its original values. The cardiac stimulating effect of ketamine can be prevented by preliminary intravenous administration of diazepam at a dose of 0.2-0.25 mg/kg of body weight. Bradycardia, hypotension, arrhythmia may occur

With rapid administration or overdose, respiratory depression or cessation has often been observed. Laryngospasm was rarely observed

Loss of appetite, nausea, vomiting, drooling

Rarely, pain, rash, transient erythema and/or morbilliform rash and, in one case, an anaphylactoid reaction have been noted at the injection site.

With repeated use over a short period, especially in young children, tolerance to the drug was noted. In these cases, the desired effect can be achieved by an appropriate dose increase.

Contraindications

- hypersensitivity to the active substance or to any of the components of the drug

Severe or poorly controlled hypertension (BP >180/100 mmHg at rest), patients in whom an increase in blood pressure may worsen the condition (congestive heart failure, severe cardiovascular disorders, traumatic brain injury, brain tumors , intracranial hemorrhage, stroke)

Eclampsia or preeclampsia

Undertreated or untreated hyperthyroidism

History of seizures, mental illness (schizophrenia, acute psychosis)

Drug Interactions

Ketamine potentiates the neuromuscular effect of barbiturates, opiates, and also enhances the action of tubocurarine and ergometrine, but does not affect the action of pancuronium and succinylcholine.

Barbiturates and inhaled general analgesics, fluorinated hydrocarbons (halothane, enflurane, isoflurane, methoxyflurane) increase the duration of action of ketamine.

Sleeping pills (especially benzodiazepine derivatives) or neuroleptics increase the duration of action of ketamine and reduce the likelihood of side effects.

During therapy with thyroid hormones, an increase in blood pressure and tachycardia can be observed.

When used together with aminophylline, the seizure threshold may decrease.

Calypsol ® compatible with other anesthetics and muscle relaxants.

Ketamine is pharmaceutically incompatible with barbiturates and diazepam (precipitation), so the drugs should not be mixed in the same syringe or infusion.

special instructions

The drug should be prescribed by a specialist - an anesthesiologist. As with the use of other general anesthetics, when using Calypsol ®, it is necessary to prepare instruments for resuscitation.

Calypsol ® is prescribed with caution, after assessing the balance of benefits and risks, within 6 months after unstable angina and myocardial infarction, with increased intracranial pressure, glaucoma or penetrating eye injury.

Intravenous Calypsol ® should be administered slowly (over 1 minute). Rapid administration of the drug can lead to respiratory depression and a sharp increase in blood pressure.

Patients with hypertension or heart failure require constant monitoring of cardiac function during anesthesia. Since pharyngeal reflexes are usually preserved with Calipsol ® monotherapy, mechanical irritation of the pharynx should be avoided. Interventions on the larynx, pharynx or trachea require a combination of Calypsol ® with muscle relaxants and careful control of breathing.

In surgical interventions involving the visceral pathways of pain sensitivity, it may be necessary to administer other analgesics.

For those obstetric interventions that require complete relaxation of the muscles of the uterus, the introduction of ketamine in monotherapy is not indicated.

For diagnostic or therapeutic interventions on the organ of vision, the use of local analgesics is not indicated.

Ketamine should be used with extreme caution in alcohol intoxication.

During the period of recovery from anesthesia, acute delirium may occur. This reaction can be prevented by administering benzodiazepines or reducing verbal, tactile, and visual stimuli. This does not exclude monitoring of vital parameters.

When using Calypsol ® on an outpatient basis, the patient can be released only after full recovery of consciousness, accompanied by an adult.

Pregnancy and lactation

Ketamine quickly crosses the placenta. During pregnancy, it can be used only after weighing the ratio of benefits and risks, although no teratogenic effects were observed in animal tests. For obstetric anesthesia, smaller doses should be used. A dose of 2 mg/kg body weight or more may lead to respiratory depression in the newborn.

There is no data on whether ketamine passes into breast milk.

Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Within 12 hours after the use of ketamine monotherapy, you can not drive a car.

Overdose

Symptoms:with rapid intravenous administration or with the introduction of large doses, respiratory depression or cessation may be observed.

Treatment: until adequate spontaneous breathing is restored, it should be supported mechanically.

Release form and packaging

10 ml of the drug in brown glass bottles, sealed with combined flip-off caps.

Instructions for the medical use of the drug

Description of the pharmacological action

Blocks thalamo-cortical connections, reduces the afferent sensitivity of the brain. Activates opiate and serotonin receptors in the central nervous system.

Indications for use

Anesthesia of short-term operations and diagnostic interventions; induction anesthesia.

Release form

Solution for intravenous and intramuscular administration 500 mg / 10 ml; vial (vial) 10 ml carton pack 5;

Pharmacodynamics

Acts quickly, but not for long (12-25 minutes). Causes pronounced and prolonged (up to 2 hours) analgesia.

Slightly increases the tone of the skeletal muscles and sympathoadrenal system; in the anesthesia phase, pharyngeal, laryngeal, cough reflexes and self-ventilation of the lungs are preserved.

Contraindications for use

Arterial hypertension, severe decompensation of cerebral and / or systemic circulation, eclampsia.

Side effects

From the nervous system and sensory organs: depression of the respiratory center, upon awakening - hallucinations, psychomotor agitation, impaired consciousness.

From the digestive tract: salivation, nausea.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): increased blood pressure, tachycardia.

Dosage and administration

The dosing regimen is set individually.

In / in, slowly (for more than 60 s) for adults - 1-3 mg / kg, for children - 0.5-3 mg / kg; the average dose for anesthesia lasting 5–10 minutes is 2 mg / kg. V / m, adults - 6.5-8 mg / kg, children - 2-5 mg / kg.

Overdose

Symptoms: respiratory depression.

Treatment: IVL.

Interactions with other drugs

Enhances the effect of inhalation anesthetics, the muscle relaxant effect of tubocurarine; does not change - pancuronium and succinylcholine.

Precautions for use

Should only be used by an experienced anesthesiologist in a well-equipped medical facility.

Storage conditions

List A .: In a place protected from light, at a temperature of 15–25 ° C.

Best before date

Belonging to ATX-classification:

** The Medication Guide is for informational purposes only. For more information, please refer to the manufacturer's annotation. Do not self-medicate; Before you start using Calypsol, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of the information posted on the portal. Any information on the site does not replace the advice of a doctor and cannot serve as a guarantee of the positive effect of the drug.

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** Attention! The information provided in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of the drug Calypsol is given for informational purposes and is not intended for prescribing treatment without the participation of a doctor. Patients need specialist advice!

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