Ketaminum

General characteristics. Structure:

Active ingredient: 50 mg of Ketaminum (in the form of a hydrochloride).

Excipients: a benzetoniya chloride, sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Ketaminum causes dissociative anesthesia - a state at which one sites of a brain are excited, and others - are oppressed that explains manifestation of analgeziruyushchy effect at incomplete oppression of consciousness and a sokhrayoneniya of spontaneous breath, pharyngeal, guttural and tussive reflexes (the drug dose causing an apnoea is 8 times higher than hypnotic). The surgical stage of the general anesthesia when using Ketaminum does not develop (visceral analgeziruyushchy activity of Ketaminum is insufficient that should be considered at polostyony operations).

Causes a specific complex of symptoms: the somatic analgesia, the state reminding a neuroleptanalgesia is raised by the arterial pressure, contractility of a myocardium, minute volume of blood and the need of a myocardium for a kisloroyoda, relaxes smooth muscles of bronchial tubes. Practically does not reduce a tone of skeyoletny muscles, can cause involuntary muscular twitchings.

Adults have a minimum dose causing hypnotic effect at odnoyokratny intravenous administration, makes 0,5 mg/kg of body weight (oppression the soznayoniya lasts one and a half minutes). In a dose of 1 mg/kg consciousness for 6 min., in a dose of 1,5 mg/kg - for 9 min., in a dose of 2 mg/kg - for 10-15 min. oppresses. At intramuscular introduction of 4-8 mg/kg the effect occurs in 2-4 min. (6-8 min.) and proceeds on average 12-25 min. (up to 30-40 min.).

At children at intramuscular introduction the general anesthesia comes in 2-6 min., at intravenous - through 15-60 with, action duration - 15-30 min. and 5-15 min. according to.

During recovery of consciousness drowsiness against the background of which quite often there are reactions in the form of hallucinations, nonsense, bright figurative snovideyoniya is noted. After awakening at patients the disorientation, sometimes for 6-8 h can remain. Frequency and expressiveness of these reactions, and also kardiostimuliyoruyushchy effect decrease at Ketaminum combination to antipsychotic means (neuroleptics) and anxiolytic medicines (tranquilizers) - Droperidolum, diazepam.

The Analgeziruyushchy effect of Ketaminum at a somatic pain is shown at purpose of subnarcotic doses. The maximum of analgeziruyushchy action nastupayot in 10 min. after introduction to a vein and remains during 2-3 h, at vnutriyomyshechny introduction effect more long.

Pharmacokinetics. Ketaminum differs in high solubility in fats that provides its bystry penetration into the central nervous system, easily gets through gistogematichesky barriers, including a blood-brain barrier. Also it stiyomulirut blood circulation. Communication with proteins of plasma reaches 12%.

Rasyopredeleniye volume - 1,8-2 l/kg, an elimination half-life - 2-3 h. The main part of products of metabolism is allocated during 2 h with urine. Bystry redistribution of drug from a brain in other fabrics is the main reason for the termination of the central effect of ketamine.

Biotransformation of Ketaminum is carried out by a demetiyolirovaniye by liver microsomal enzymes with formation of several metabolites, some of them keep 1/5-1/3 anestetichesky activities of a keyotamin. Elimination of Ketaminum depends on system of oxidases of a smooth endoplazmatiyochesky reticulum. The main metabolite, норкетамин, has some gipnotiyochesky activity which is weaker, than at Ketaminum. In the course of further metabolism Ketaminum and норкетамин turn into hydroxylated derivatives (there is a hydroxylation of an aromatic cyclohexylamine ring in two various positions and "interface"), which form conjugates with glucuronic acid and eliminirutsya from an organism.

The insignificant quantity of meyotabolit can remain in an organism within several days, cumulation at repeated introduction is not observed. At repeated anesteziya tolerance to drug can arise Ketaminum that is partially explained with induction of liver enzymes.

Indications to use:

Introduction and basic general anesthesia (especially at patients with low arterialyyony pressure or in need of preservation of independent breath, ли­бо when carrying out artificial ventilation of the lungs by the respiratory mixes which are not containing a dinitrogene oxide (nitrous oxide)).

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

Various surgeries at multicomponent intravenous anesthesia.

Painful diagnostic procedures (endoscopy, catheterization of cameras of heart), small surgical manipulations at burns, bandagings and to that similar procedures.

Route of administration and doses:

Ketaminum is entered intravenously (in one step struyno or fractionally and - pelno) or intramusculary.

The adult the drug is administered intravenously, at the rate of 2-3 mg/kg, intramusculary - 4-8 mg/kg of body weight. For anesthesia maintenance the drug is administered on 0,5 mg/kg intravenously or 3 mg/kg intramusculary or intravenously kapelno, with a speed of 2 mg/kg/h (with use of an infuzomat or by drop administration of solution with concentration of 1 mg/ml (in 5% solution of a dextrose (glucose) or 0,9% chloride sodium solution) with a speed of 20-50 of cap/min.

At children drug is used for introduction anesthesia at different types of a balanced anesthesia (enter intramusculary once at the rate of 4-5 mg/kg in the form of solution with concentration 50 mg/ml after sootvetstvuyuyoshchy premedication). For the main anesthesia Ketaminum is entered intramusculary (a rasyotvor with concentration of 50 mg/ml) or intravenously (solution with concentration of 10 mg/ml it is struyno single-step or solution with concentration of 1 mg/ml kapelno with a skoyorost of 50-60 caps/min.); at intramuscular introduction the dose depends on body weight and age of children: to newborns and babies - 8-12 mg/kg, to children from 1 year to 6 years - 6-10 mg/kg, 7-14 years - 4-8 mg/kg. Intravenously enter 2-3 mg/kg in a dose. Maintenance of anesthesia provide with repeated injections of Ketaminum (on 3-5 mg/kg vnutriyomyshechno either 0,5-1 mg/kg intravenously struyno or drop introduction of a rasyotvor with concentration of 1 mg/ml with a speed of 30-60 of caps/mines).

To strengthening of effect of ketamine it is usually applied in a combination with antiyopsikhotichesky means (Droperidolum) and narcotic analgetics (fentayonit, trimeperidine and others), at the same time the dose of Ketaminum should be reduced.

Features of use:

Ketaminum is applied only in the conditions of a hospital or ambulance.

For the prevention of strengthening of secretion of mucous membranes and salivary же­лез it is necessary to include in structure of means of premedication atropine or a metotsiniya iodide, and also to slowly enter the main dose of drug (which is not exceeding 3 mg/kg). During ketamine anesthesia to carry out inhalation by oxygen mix with air in the ratio 1:2.

When using Ketaminum it is necessary to monitor function of external respiration, especially behind passability of upper respiratory tracts (the spasm of chewing muscles and retraction of language are possible).

It is necessary to be careful at throat and drink operations (primeyonyat muscle relaxants).

For prevention of muscular rigidity and involuntary twitchings when carrying out premedication intramusculary or intravenously enter to diazeyopa.

For the prevention of development of psychotomimetic action it is necessary to include Droperidolum, diazepam in structure of means of premedication.

After use of Ketaminum increase intracranial a davleyoniya is possible.

Use of drug can provoke development of acute mental disorders at removal from anesthesia. It is necessary to be careful to payotsiyenta with acute disorders of mentality (also in the presence of such instructions in the anamnesis), to patients with a drunkenness.

Development of ketamine dependence in patients with drug addiction or earlier abusing narcotic substances is possible.

Influence on ability to manage vehicles and mechanisms. After Ketaminum use, at least, during 24 h to patients sleyodut to abstain from driving of motor transport and other potentially dangerous types of activity.

Side effects:

From a nervous system: oppression of a respiratory center, a muscular riyogidnost, involuntary muscular activity (for prevention it is predyovaritelno necessary to enter diazepam); in the period of an exit from the general anesthesia - psychomotor excitement, a hallucination, a long disorientation, psychosis.

From an organ of sight: diplopia, nystagmus, increase in intraocular pressure.

From respiratory system: an asthma, obturation of upper respiratory tracts because of a spasm of chewing muscles and sticking of language, the increased bronyokhialny secretion and a sialosis.

From cardiovascular system: increase arterial davleyoniya, tachycardia.

From the alimentary system: hypersalivation, nausea.

Local reactions: morbidity and a hyperemia on the vein course in an injection site.

Interaction with other medicines:

Ketaminum strengthens effect of medicines for the general anesthesia, narcotic analgetics, antipsychotic means (neuroleptics), anxiolytics (tranquilizers) and other medicines oppressing a tsenyotralny nervous system.

Before use of Ketaminum it is necessary to cancel lincomycin, lithium drugs (in 1-2 days), monoamine oxidase inhibitors (in 15 days). It is impossible to mix in one syringe with barbiturates (pharmaceutical it is incompatible - formation of a deposit).

Droperidolum and benzodiazepines, including diazepam, weaken risk of a proyavyoleniye of psychotomimetic and motor activity, and also emergence of a takhiyokardiya and increase in arterial pressure.

It is not recommended to appoint with the sympathomimetics and medicinal sredstyova possessing the stimulating impact on a cardiovascular sisteyoma (strengthening of hypertensive and aritmogenny action, increase in need of a myocardium for oxygen).

The cardiostimulating effect of Ketaminum is weakened at a combination with antipsychotic means, anxiolytics.

Ketaminum strengthens myorelaxation effect of Tubocurarini chloridum and succinylcholine of iodide, does not change - a bromide pankuroniya.

During the general anesthesia at the patients accepting iodinated prepayorata and hormones of a thyroid gland the probability of increase in arterial pressure and tachycardia is high (are eliminated with beta adrenoblockers).

Contraindications:

- Hypersensitivity to drug.

- The arterial hypertension and states which are followed by the increased aryoterialny pressure.

- Stenocardia, a myocardial infarction (including in the last 6 months).

- Chronic renal failure.

- Disturbance of cerebral circulation (including in the anamnesis).

- Preeclampsia.

- Epilepsy, epilepsy at children's age, an eclampsia and other convulsive states.

- Alcoholism.

With care. Diseases of kidneys, dekompensirovanny chronic heart failure, throat and drink operations.

Overdose:

At administration of ketamine in high doses intravenously (3 mg/kg) respiratory depression in some cases can be observed. In these cases iskusstyovenny ventilation of the lungs is shown.

At emergence of hallucinations it is reasonable to ispolzoyovat antipsychotic means (haloperidol), at a convulsive syndrome - to diazeyopa. If necessary carry out symptomatic therapy.

Storage conditions:

List II. "The list of the drugs, psychotropic substances and their precursors which are subject to control in the Russian Federation" in specially oborudoyovanny rooms in the presence of the license for the specified type of activity. In the place protected from light at a temperature not above 25 °C. A period of validity - 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 50 mg/ml. Packaging: in ampuyola on 2 ml and 5 ml, in bottles on 5 ml. 5 ampoules in a blister strip packaging. 1 or 2 blister strip packagings with the application instruction, a knife or the scarificator ampoule in a pack from a cardboard. 20, 50 or 100 blister strip packagings according to 20, 50 or 100 application instructions, knives or scarificators ampoule in a korobyoka from a cardboard or in a box from corrugated fibreboard. From a cardboard or in a box from corrugated fibreboard put in a box та­лон with number of the packer. When packaging ampoules with notches, rings and points of a break knives or skayorifikator ampoule do not put. 5 bottles in a blister strip packaging. 1 blister strip packaging with the application instruction in a pack from a cardboard. 30 or 50 blister strip packagings according to 30 or 50 instyoruktion on use in a box from a cardboard or in a box from a corrugated karyoton. From a cardboard or in a box from corrugated fibreboard put in a box та­лон with number of the packer.