Ketamine - instructions for use, dose, side effects, contraindications

Active substanceKetamineKetamine

Similar drugsTo uncover

Ketamine

solution w / m in / in

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Dosage form: & nbspsolution for intravenous and intramuscular administration

Composition:

1 ml of the solution contains:

active substance: ketamine hydrochloride (equivalent to 50 mg of 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-induction general anesthesia

ATX: & nbsp

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 depressed, which explains the manifestation of the analgesic effect with incomplete inhibition of consciousness and the preservation of spontaneous breathing, pharyngeal, laryngeal and cough reflexes (the dose of the drug causing apnea is 8 times above the hypnotic). Surgical stage of general anesthesia with the use of ketamine does not develop (visceral analgesic activity of ketamine is insufficient, which should be taken into account in cavitary operations).

Causes a specific complex of symptoms: somatic analgesia, a condition resembling neuroleptanalgesia, raises blood pressure,myocardial contractility, minute blood volume and myocardial oxygen demand, relaxes the smooth musculature of the bronchi. Almost does not reduce the tone of the skeletal muscles, it 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 (inhibition of consciousness lasts a minute and a half). At a dose of 1 mg / kg inhibits 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 injection of 4-8 mg / kg, the effect occurs after 2-4 minutes (6-8 minutes) and lasts an average of 12-25 minutes (up to 30-40 minutes).

In children with intramuscular injection, general anesthesia occurs after 2-6 minutes, with intravenous injection after 15-60 seconds, duration of action is 15-30 minutes and 5-15 minutes, respectively.

During the restoration of consciousness, drowsiness occurs, against which often there are reactions in the form of hallucinations, delusions, bright figurative dreams. After awakening, disorientation may persist in patients, sometimes within 6-8 hours. The frequency and severity of these reactions, as well as the pacemaker effect, decrease with the combination of ketamine with antipsychotics (antipsychotics) and anxiolytic drugs (tranquilizers) - droperidol, diazepam.

The analgesic effect of ketamine with somatic pain is manifested when subnarcotic doses are prescribed. The maximum analgesic effect occurs 10 minutes after the introduction into the vein and persists for 2-3 hours, with intramuscular injection the effect is longer.

Pharmacokinetics:

Ketamine is highly soluble in fats, which ensures its rapid penetration into the central nervous system, easily penetrates through the histohematological barriers, including the blood-brain barrier. It also stimulates blood circulation. The connection with plasma proteins reaches 12%.

The volume of distribution is 1.8-2 l / kg, the half-life period is 2-3 hours. The main part of metabolic products is released within 2 hours with urine. The main reason for stopping 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 with hepatic microsomal enzymes with the formation of several metabolites, some of them retain 1 / 5-1 / 3 anesthetic activity of ketamine. Elimination of ketamine depends on the system of oxidases of the smooth endoplasmic reticulum.The main metabolite, norketamine, has some hypnotic activity, which is weaker than that of ketamine. In the process of further metabolism ketamine and norketamine are converted to 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 number of metabolites can remain in the body for several days, cumulation after repeated administration is not observed. With multiple anesthetics, ketamine may cause tolerance to the drug, which is partly explained by the induction of hepatic enzymes.

Indications:

Introductory and basic general anesthesia (especially in patients with low blood pressure or when it is necessary to maintain independent breathing, or when performing artificial lung ventilation with respiratory mixtures that do not contain dinitrogen oxide (nitrous oxide)).

Emergency surgical interventions (including at evacuation stages, in particular, in patients with traumatic shock and blood loss).

Various surgical operations with multicomponent intravenous anesthesia.

Painful diagnostic procedures (endoscopy, catheterization of the heart chambers), small surgical manipulations for burns, bandages and similar procedures.

Contraindications:

Hypersensitivity to the drug.

Arterial hypertension and conditions accompanied by high blood pressure.

Angina pectoris, myocardial infarction (including the last 6 months).

Chronic renal failure.

Violation of cerebral circulation (including in history).

Preeclampsia.

Epilepsy, epilepsy in childhood, eclampsia and other convulsive conditions.

Alcoholism.

Carefully:

Kidney disease, decompensated chronic heart failure, operations on the larynx and pharynx.

Pregnancy and lactation:

Ketamine penetrates the placental barrier. The safety of ketamine during pregnancy is not established. Use in this category of patients is not recommended.

Dosing and Administration:

Ketamine is administered intravenously (either instantaneously, either fractionally or in droplets) or by intramuscular injection.

Adults the drug is administered intravenously, at the rate of 2-3 mg / kg, intramuscularly - 4-8 mg / kg body weight. To maintain anesthesia, the drug is administered 0.5 mg / kg intravenously or 3 mg / kg by intramuscular or intravenous drip, at a rate of 2 mg / kg / h (using an infusomat or by dropping a solution at a concentration of 1 mg / ml (5 % solution of dextrose (glucose) or 0.9% solution of sodium chloride) at a rate of 20-50 cap / min.

Children the drug is used for introductory anesthesia with various types of combined analgesia (administered intramuscularly once, at a rate of 4-5 mg / kg as a solution at a concentration of 50 mg / ml after appropriate premedication). For basic anesthesia ketamine injected intramuscularly (solution with a concentration of 50 mg / ml) or intravenously (solution with a concentration of 10 mg / ml at one time or a solution at a concentration of 1 mg / ml at a rate of 50-60 cap / 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 - 6-10 mg / kg, 7-14 years - 4-8 mg / kg. Intravenously administered at a dose of 2-3 mg / kg. Maintenance of anesthesia is provided by repeated injections of ketamine (3-5 mg / kg intramuscularly or 0.5-1 mg / kg intravenously by jet or dropwise administration of a solution at a concentration of 1 mg / ml at a rate of 30-60 cap / min).

To enhance the action of ketamine it is usually used in combination with antipsychotic agents (droperidol) and narcotic analgesics (fentanyl, trimeridine and others), while the dose of ketamine should be reduced.

Side effects:

From the nervous system: oppression of the respiratory center, muscle rigidity, involuntary muscular activity (for prevention, diazepam); in the period of withdrawal 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, obturation of the upper respiratory tract due to spasm of chewing muscles and tongue sagging, increased bronchial secretion and salivation.

From the cardiovascular system: increased blood pressure, tachycardia.

From the digestive system: hypersalivation, nausea.

Local Reactions: soreness and congestion along the vein at the site of injection.

Overdose:

When ketamine is administered at 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 antipsychotics (haloperidol), with convulsive syndrome - diazepam. If necessary, conduct symptomatic therapy.

Interaction:

Ketamine enhances the effect of drugs for general anesthesia, narcotic analgesics, antipsychotics (antipsychotics), anxiolytics (tranquilizers) and other drugs that depress the central nervous system.

Before applying ketamine it is necessary to cancel lincomycin, lithium preparations (for 1-2 days), monoamine oxidase inhibitors (for 15 days). It is impossible to mix in one syringe with barbiturates (pharmaceutically incompatible - the formation of sediment).

Droperidol and benzodiazepines, including diazepam, reduce the risk of manifestations of psychotomimetic and motor activity, as well as the occurrence of tachycardia and increased blood pressure.

It is not recommended to appoint with sympathomimetics and drugs that have a stimulating effect on the cardiovascular system (increased hypertensive and arrhythmogenic action, increased myocardial oxygen demand).

The cardiostimulating effect of ketamine is weakened when combined with antipsychotic drugs, anxiolytics.

Ketamine increases the myorelaxing effect of tubocurarine chloride and suxamethonium iodide, does not change - pancuronium bromide.

During general anesthesia in patients taking iodine-containing drugs and thyroid hormones, there is a high probability of high blood pressure and tachycardia (they are eliminated by beta-blockers).

Special instructions:

Ketamine is used only in a hospital or ambulance.

To prevent increased secretion of mucous membranes and salivary glands in the composition of premedication should be included atropine or metocinium iodide, and also slowly enter the main dose of the drug (not exceeding 3 mg / kg). During ketamine anesthesia, inhalation 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 for the upper respiratory tract (spasm of chewing musculature and tongue twisting are possible).

Care should be taken when performing operations on the larynx and pharynx (muscle relaxants are used).

To prevent muscle stiffness and involuntary twitching during premedication intramuscular or intravenous diazepam is administered.

To prevent the development of psychotomimetic action, premedication should include droperidol, diazepam.

After using ketamine, an increase in intracranial pressure is possible.

The use of the drug can provoke the development of acute mental disorders when removed from anesthesia. Care should be taken in patients with acute mental disorders (also if there are such indications in the history), patients with alcohol intoxication.

Perhaps the development of ketamine dependence in patients with drug dependence or previously abused drugs.

Effect on the ability to drive transp. cf. and fur:After using ketamine for at least 24 hours, patients should refrain from driving vehicles and other potentially hazardous activities.

Form release / dosage:

Solution for intravenous and intramuscular injection 50 mg / ml.

Packaging:

In ampoules of 2 ml and 5 ml, in vials of 5 ml.

5 ampoules in the outline of the cell.

1 or 2 contour squares with instructions for use, with a knife or scarifier ampoule in a pack of cardboard.

20, 50 or 100 contour mesh packages, respectively, with 20, 50 or 100 instructions for use, knives or scarifiers ampouled into a cardboard box or into a box of corrugated cardboard.

In a box of cardboard or in a box of corrugated cardboard, insert a coupon with the number of the packer.

When packing ampoules with notches, rings and break points, knives or scarifier ampoules do not.

5 bottles in a planar cell pack.

1 circuit cell pack with instructions for use in a pack of cardboard.

30 or 50 contour squares, respectively, with 30 or 50 instructions for use in a cardboard box or in a box of corrugated cardboard.

In a box of cardboard or in a box of corrugated cardboard, insert a coupon with the number of the packer.

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 the dark place at a temperature of no higher than 25 ° C.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:For hospitals

Registration number:P N000298 / 01

Date of registration:17.10.2011

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Representation: & nbspMOSCOW ENDOCRINE FACTORY FGUP MOSCOW ENDOCRINE FACTORY FGUP Russia

Information update date: & nbsp17.10.2011

Illustrated instructions

Instructions

Ketamine (Ketamine)