Ketaminum hydrochloride

General characteristics. Structure:

Active ingredient: ketamine;

1 ml of solution contains Ketaminum of a hydrochloride 57,6 mg (in terms of Ketaminum of 50,0 mg);

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

Pharmacological properties:

Pharmacodynamics. Ketamine – anesthetic with the expressed anesthetizing action. Drug causes so-called dissociative anesthesia which is described as functional dissociation between talamo-neocortical and limbic systems. Analgesic effect of drug is shown already at a subdissociative dose and anesthesia proceeds longer, than. Sedative and hypnotic actions are expressed less. In the site of a spinal cord and peripheral nerves drug shows mestnoanesteziruyushchy action.

At Ketaminum use the muscle tone remains invariable or can raise. Therefore protective reflexes are, as a rule, not mentioned. The convulsive threshold does not decrease. At spontaneous breath the intracranial pressure which can be avoided on the managed breath can increase.

As Ketaminum causes a sympathicotonia, the arterial pressure and heart rate can increase; along with increase in a coronary blood-groove in a myocardium oxygen requirement increases. Ketaminum has a negative inotropic effect and antiarrhytmic action (direct cardial effect).

Thanks to antagonistic action, peripheric vascular resistance does not change.

After use of Ketaminum the expressed hyperventilation without considerable deviations in parameters of blood gases is observed. Ketaminum relaxes muscles of bronchial tubes.

Pharmacokinetics. Ketaminum – zhirorastvory. The maximum concentration in a blood plasma is observed in 20 (5-30) minutes after intravenous administration of the first dose. At intramuscular introduction biological availability of drug makes

93%. About 47% of Ketaminum contact blood proteins. The first phase of effect of drug (alpha phase) lasts about 45 minutes, T1/2=10-15 minutes. Clinically the first phase is shown by anesthetic effect of drug. Ketaminum is quickly distributed in fabrics which krovosnabzhatsya well (for example, in a brain). Concentration of Ketaminum in fabrics answers two-phase open model. The termination of the anesthetizing effect arises owing to redistribution from TsNS in peripheral fabrics in which blood supply is less, and biotransformations in a liver in active metabolites. Among metabolites of Ketaminum is such which has somnolent effect. Time of semi-removal of the second phase (beta phase) makes about 2,5 hours. 90% of metabolites are removed through kidneys. Ketaminum gets through a placenta.

Pharmaceutical characteristics.

Main physical and chemical properties: the transparent colourless or slightly painted liquid.

Incompatibility.

In view of chemical incompatibility barbiturates cannot be entered in one syringe together with Ketaminum.

In case of need simultaneous use of Ketaminum with diazepam the drugs should be administered separately and it is impossible to mix in one syringe or infusion.

To apply the solvents specified in the section "Route of Administration and Doses".

Indications to use:

Apply as monotherapy to carrying out short diagnostic or therapeutic interventions at children and in some special cases at adults: introduction to an anesthesia and its maintenance.

For introduction to an anesthesia and its maintenance in a combination with other drugs, especially with benzodiazepines, drug is appointed in the reduced dose.

Special indications for Ketaminum use (independently or in a combination with other drug):
painful procedures (for example, change of a bandage at the patient with burns);
neurodiagnostic procedures (for example, pneumoencephalography, ventrikulografiya, miyelografiya);
endoscopy;
some procedures in ophthalmology;
surgical interventions in a neck and an oral cavity, at dental care;
otolaryngologic interventions;
gynecologic ekstraperitonealny interventions;
intervention in obstetrics, introduction to an anesthesia for operation of kesarevy section;
intervention in orthopedics and traumatology;
in connection with features of effect of ketamine on heart and blood circulation: carrying out an anesthesia at patients in a depressed case, with hypotension;
carrying out an anesthesia by the patient at which preference is given to intramuscular administration of drug (for example, to children).

Route of administration and doses:

Individual reaction to Ketaminum, as well as to other anesthetics of systemic action, depends on a dose, a way of introduction and age of the patient. Therefore selection of a dose of drug has to be carried out individually.

At use in a combination the dose of Ketaminum has to be lowered.

Below-mentioned doses concern adults, patients of advanced age (65 years are more senior) and children.

Intravenous administration. It is necessary to enter slowly within 1 minute.

The initial dose of 0,7-2 mg/kg of body weight which provides surgical anesthesia for 5-10 minutes approximately in 30 seconds after introduction (the patient with high risk, elderly or sick which are in state of shock is recommended a dose of 0,5 mg/kg of body weight).

Intramuscular introduction.

Initial dose of 4-8 mg/kg of body weight which provides surgical anesthesia for 12-25 minutes in a few minutes after introduction.

Intravenously kapelno.

To add 500 mg of Ketaminum to 500 ml 0,9% of solution of sodium of chloride or 5% of solution of glucose.

Initial dose: 80-100 drops a minute.

Maintenance dose: 20-60 drops a minute (2-6 mg/kg of body weight an hour).

The dose for the adult makes 2-6 mg/kg of body weight an hour.

The supporting anesthesia.

In case of need a half of an initial dose or an initial dose can be entered repeatedly intramusculary or intravenously.

Emergence of a nystagmus, motor reactions on irritation indicate insufficiency of an anesthesia therefore in this case need for repeated introduction of a dose can appear. However the involuntary movements of extremities can appear irrespective of anesthesia depth!

Features of use:

It is possible to combine with any kind of local anesthesia.

The specialist – the anesthesiologist has to appoint drug.

Ketaminum is appointed with care after assessment of a ratio of advantage and risk at the following states: for 6 months after unstable stenocardia and a myocardial infarction, with the increased intracranial pressure, glaucoma or the getting eye injury.

Intravenously Ketaminum needs to be entered slowly (within 1 minute). Bystry administration of drug can lead to respiratory depression and sharp increase in arterial pressure.

At patients with hypertensia or heart failure during an anesthesia continuous monitoring of cordial function is necessary. Premedication diazepam reduces hypertensive reaction.

As at monotherapy by Ketaminum pharyngeal reflexes are, as a rule, kept, it is necessary to avoid mechanical irritation of a throat. At intervention on a throat, a throat or a trachea Ketaminum combination with muscle relaxants and careful control of breath is necessary.

At surgical interventions with involvement of visceral ways of painful sensitivity there can be necessary an introduction of other analgetik.

For those obstetric interventions at which full relaxation of muscles of a uterus is necessary, use of Ketaminum as monotherapy it is not shown.

At diagnostic or therapeutic interventions on an organ of sight use of local analgetik is not shown.

Ketaminum should be applied with extra care at a drunkenness.

In the period of an exit from an anesthesia the acute delirium can be observed. This reaction can be prevented by administration of benzodiazepines or decrease in verbal, tactile and visual stimulations. But it does not exclude  need of observation on zhiznenovazhny parameters.

At use of Ketaminum in out-patient conditions it is possible to release the patient only after full recovery of consciousness and accompanied by the adult.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

For 12 hours after use of Ketaminum in the form of monotherapy it is impossible to manage motor transport or to work with other mechanisms.

Side effects:

Cardiovascular system: short-term increase in the arterial pressure (AP) and heart rate is often observed. The maximum of increase in arterial pressure (20-25%) is observed  in a few minutes after intravenous administration of drug, but in 15 minutes of the ABP is returned to initial values. For prevention of a cardiopromoting effect of Ketaminum previously intravenously enter diazepam in a dose of 0,2-0,25 mg/kg of body weight. Bradycardia, hypotension and arrhythmia can be observed.

Respiratory system: often - oppression or an apnoea at bystry introduction or at overdose. Seldom - a laryngospasm.

Sight: diplopia, nystagmus, moderate increase in intraocular pressure.

Nervous system: increase in a tone of skeletal muscles can often cause the tonic and clonic movements which do not point to reduction of depth of an anesthesia therefore they do not need introduction of an additional dose of drug.

During return to consciousness there can be bright dreams, visual hallucinations, emotional disturbances, a delirium, psychomotor excitement, feeling of confusion. These phenomena are observed less often at patients  aged up to 15 years or 65 years are more senior.

Digestive tract: appetite loss, nausea, vomiting, the increased hypersalivation.

Others: seldom on site a prick pain, rash is noted. The tranzitorny erythema and/or korepodobny rashes, in one case - anaphylactoid reaction were described.

At repeated use throughout the short period, especially at small children, tolerance to drug is noted. In such cases of desirable effect it is possible to reach the corresponding increase in a dose.

Interaction with other medicines:

Ketaminum exponentiates neuromuscular effect of barbiturates, opiates, and also strengthens effect of tubocurarine and ergometrine, but the pankuroniya and a suktsinilkholina does not influence action.

Barbiturates and the inhalation all-anesthetizing drugs, the fluorinated carbohydrates (Ftorotanum, энфлуран, изофлуран, метоксифлуран) increase duration of effect of ketamine.

Hypnotic drugs (especially derivative benzodiazepine) or neuroleptics increase duration of effect of ketamine and reduce probability of emergence of side effects.

Ketaminum is combined with other anesthetics and muscle relaxants.

At therapy increase in arterial pressure and tachycardia can be observed by thyroid hormones.

At a combination with Aminophyllinum the convulsive threshold can decrease.

Contraindications:

Hypersensitivity to active ingredient or other components of drug.
Ketaminum is contraindicated to patients with heavy hypertensia (at adult ABP> 180/100 mm of mercury. at rest) which badly is exposed to control; to patients at whom arterial pressure is increased Ketaminum can worsen a state (congestive heart failure, heavy cardiovascular disturbances, a craniocereberal injury, brain tumors, intracraneal hemorrhage, a stroke).
Eclampsia, preeclampsia.
The hyperthyroidism which was treated insufficiently or will not respond to treatment.
Existence in the anamnesis of spasms, mental diseases (schizophrenia, acute psychosis).
Disturbances of cerebral circulation.
The increased  intracranial pressure.

Overdose:

Ketaminum has a wide therapeutic index.

At bystry intravenous administration or at introduction of high doses oppression or an apnoea can be observed. In that case for recovery of adequate spontaneous breath it is necessary to carry out artificial ventilation of the lungs.

Use during pregnancy and feeding by a breast.

There are no data on safety of use of Ketaminum during pregnancy or feeding by a breast therefore pregnant women and women who nurse should not use drug.

Children.

Drug is used in pediatric practice.

Storage conditions:

Period of validity. 2 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature from 15 ºС to 25 ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in ampoules, on 10 ampoules in a pack. On 10 ml in bottles, on 5 bottles in a pack.