The drug "Ketamine": instructions for use, description, composition

History of creation

A substance called “Ketamine” was first synthesized in 1962 by the American researcher Kelvin Stevens. The scientist worked at Parke-Davis, trying to find a safe anesthetic formula that could be an alternative to phencyclidine, which had a number of dangerous side effects (the drug caused hallucinations, could trigger an epileptic seizure, and was neurotoxic).

Three years later, Ketamine, then known under the working title CI-581 (clinical investigation 581), was first tested in practice. After the first use in the clinic, the drug was used by American military personnel who served in Vietnam in the late 1960s. In 1970, when Ketamine in the United States was allowed to be widely used, the drug became the first non-inhalation anesthetic, with the introduction of which there was a minimal effect on blood circulation and respiration.Subsequently, the drug began to be actively used in psychiatry.

The use of Ketamine was significantly reduced due to deaths that were identified between 1987 and 2000 in the United States and European countries. The dead applied the drug in a dosage that was much higher than recommended, due to some side effects of the drug. The fact is that “Ketamine” by that time had acquired dubious popularity as a drug after the publication of the books “Journey to the Bright World” by Marcia Moore and Howard Altounian, and “The Scientist” by John Lilly. Nowadays, the drug is used primarily in veterinary medicine and as an anesthetic in military medicine (in developing countries).

Use in the Soviet Union and Russia

In the USSR, the first studies related to the use of "Ketamine" in the treatment of alcoholism and drug addiction, in the mid-1980s, Yevgeny Krupitsky began to conduct. The work, which lasted for about two decades, was discontinued due to the tightening of Russian legislation. Since the early 1990s, against the background of the emergence in our country of so-called psychedelic literature, Ketamine has become increasingly used as a narcotic drug.

According to the Federal Law of 08.01.1998 No. 3-FZ “On Narcotic Drugs and Psychotropic Substances”, the drug was included in the list of psychotropic drugs. Five years later, when the Federal Drug Control Service was created, and the law made a number of amendments, the use of Ketamine in veterinary medicine sharply decreased in Russia.

Now the use of this drug for medical purposes is strictly regulated, penalties are imposed for breaking the rules. "Ketamine" can be used only by licensed institutions, including veterinary. The drug should be stored in a safe equipped with dual alarms.

In the past, domestic veterinarians widely used "Ketamine" as an anesthetic. The forced refusal of most specialists from the drug, which proved to be one of the most effective and at the same time soft anesthetics, provoked a lot of protests from animal protection, pet lovers and pet owners, as well as veterinarians themselves. However, government agencies have not listened to their arguments for the past ten years.

Composition and release form

The active ingredient of the drug is NMDA antagonist ketamine (in the form of hydrochloride).The drug is made in the form of a solution intended for intravenous and intramuscular administration.

Ketamine is available in 5 ml vials. 1 ml of solution contains 250 mg of the active substance. The bottle is packed in a pack of cardboard.

pharmachologic effect

Ketamine is a remedy for non-inhalational anesthesia. In some cases, the drug is used as an analgesic (mainly in emergency medicine and in patients who cannot be prescribed opioid analgesics and barbiturates), as well as for the treatment of bronchospasm.

Being a noncompetitive antagonist of direct-acting NMDA receptors (blocking the ion channel of receptors), Ketamine is able to exert an inhibitory effect on the function of the neurons of the associative cortex and thalamus responsible for switching sensory impulses from the reticular activating system to the cortex of the large hemispheres.

At the same time, Ketamine has a stimulating effect on the part of the limbic system involved in the awareness of sensations, including the hippocampus. As a result, the patient develops functional disorganization of non-specific connections in the midbrain and thalamus (dissociative anesthesia).Clinically, this is expressed as follows: the patient looks awake, he is able, in particular, to swallow and open his eyes, but loses the ability to analyze sensory stimuli, reacting adequately to them.

In the course of research, it was previously confirmed that Ketamine has the ability to bind to opioid receptors in the brain and horny horns of the spinal cord. It is assumed that this explains the analyzing effect of the drug.

A higher level of ketamine activity in relation to the cortex than the thalamus may be due, probably, to an uneven distribution of NMDA receptors in the central nervous system.

Pharmacokinetics

After a single intravenous administration of Ketamine, the narcotic effect usually occurs within 30-60 seconds and lasts for 5-10 minutes (sometimes up to 15 minutes).

With intramuscular use of the drug in the dosage of 4-8 mg / kg, Ketamine takes effect in 2-4 minutes (up to 6-8 minutes). The effect lasts 12-25 minutes (sometimes up to 40 minutes).

The pronounced analgesic effect of Ketamine can last for up to two hours. After the introduction of the drug, the patient has pharyngeal, laryngeal and cough reflexes, the level of independent pulmonary ventilation remains adequate.

After the introduction of "Ketamine", entering the group of lipophilic compounds, is quickly distributed to organs well supplied with blood, including the brain. Then the tool begins to be redistributed in tissue with a low level of perfusion.

Metabolized drug in the liver. The half-life of the drug is usually from two to three hours. The patient's body "Ketamine" leaves mainly through the kidneys in the form of conjugated metabolites.

Indications

In modern medicine, the drug "Ketamine" is used:

  • for introductory and basic anesthesia for short-term surgical interventions, regardless of whether muscle relaxation is required;
  • during painful instrumental and diagnostic procedures;
  • when transporting patients;
  • when processing burn surfaces.

Dosing regimen

"Ketamine" is appointed by the attending physician on an individual basis, taking into account the indications, the patient's age, the clinical situation and the drugs used for premedication.

For intravenous administration, a single dosage is usually 0.5–4.5 mg / kg, and a formula of 4–13 mg / kg is usually used for administration to a muscle.

Side effects

In patients who are prescribed the drug "ketamine", various undesirable effects can be observed. The most common ones are:

  • on the part of the cardiovascular system: increased blood pressure, tachycardia;
  • on the part of the digestive system: salivation (hypersalivation);
  • on the part of the central nervous system: psychomotor agitation and hallucinations (when leaving anesthesia);
  • respiratory system: shortness of breath, respiratory depression;

In extremely rare cases, local reactions may occur - painful sensations at the injection site and hyperemia along the vein.

Contraindications

The drug "Ketamine" does not apply if the patient is diagnosed with:

  • disorders of cerebral circulation;
  • arterial hypertension;
  • angina and heart failure (in the phase of decompensation);
  • preeclampsia and eclampsia;
  • epilepsy in childhood.

special instructions

After the appointment of "Ketamine" patients are recommended to refrain from driving vehicles and other potentially dangerous activities that require a high level of concentration and quick reactions, at least during the day.

Given the ability of Ketamine to penetrate the placental barrier, and research on the efficacy and safety of the drug in pregnant women has not yet been conducted, the use of the drug in patients in this category is not recommended.



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