In medical practice, there are situations in which the use of drugs leads to an overdose or a negative reaction from various organs and systems. Opioid medications are especially common. To speed up their removal from the body, doctors use special medications. The drug "Naloxone" is a remedy that helps to correct the situation with an overdose of opioid analgesics. What is it and what is the mechanism of its action? Let's try to understand these issues.
Drug description, composition and forms
The drug "Naloxone" instructions for use refers to an opioid receptor antagonist. Its active ingredient is naloxone hydrochloride. Dosage forms that can be found on the pharmaceutical market are not so diverse, these are injections and tablets. The latter are very rarely used in medical practice. Liquid form for intravenous or intramuscular injectionintroductions, on the contrary, are very much in demand. The composition of the solution, in addition to the active substance, includes a set of standard auxiliary components: sodium chloride, purified water, organic acids and s alts.
Naloxone medicine is produced in transparent glass ampoules with a volume of 1 ml each. The concentration of the active substance in one dose is 0.4 mg.
The drug is packed in blisters made of lacquered transparent plastic with or without an aluminum foil plug. Each such package contains 5 ampoules.
1 or 2 contour packs are placed in a cardboard box along with instructions for using the drug and an ampoule scarifier. If the ampoules are equipped with a special ring or a break point, the knives for opening them are not put in the box.
Mechanism of action of Naloxone
As mentioned above, the drug "Naloxone" instructions for use refer to opioid receptor antagonists. This means that this drug is able to block these receptors, thereby eliminating the central and peripheral effects of compounds from the opioid group. In addition, the drug, when administered, can cause withdrawal symptoms in drug dependent patients.
When using the Naloxone solution, the mechanism of action of which is described above, the effect occurs within a short time. With intravenous administration, the drug begins to act after 1-2 minutes, with intramuscular injection after 5 minutes. The duration of the therapeutic effect is alsodepends on the method of introduction of the solution. If the solution was injected into the muscle, the drug acts for about 45 minutes, and for intravenous infusion - at least 4 hours.
Specialists most often use Naloxone solution to treat patients. Tablets, unlike him, are weak and short-lived.
The active substance of the drug breaks down into metabolites in the liver. Its half-life is short, only 30-80 minutes. 70% of the administered dose of Naloxone is excreted by the kidneys within 3 days.
The main advantage of the drug "Naloxone" is the impossibility of forming dependence on it.
Indications for use
When is Naloxone recommended? Instructions for use of the drug contains a detailed list of situations in which its use is highly desirable. First of all, it is prescribed to patients after a surgical operation. The use of the drug "Naloxone" (analogues are also often used in the postoperative period) in this case helps to quickly bring the patient out of the state of drug-induced sleep. The drug "Naloxone" is also used to eliminate the consequences of ethanol poisoning, overdose of analgesics, barbiturates and benzodiazepines.
Often its use is also justified in the case of the birth of a child in conditions where opioid analgesics were introduced to the mother during childbirth. As a rule, these children have difficulty breathing on their own. The drug "Naloxone" eliminates them and helps to activate the respiratory system.function. The solution is often used as a diagnostic tool for suspected drug addiction in a patient.
It is worth noting that the only condition for the use of this remedy is strict indications. That is why in medical practice it is used strictly by prescription and under his supervision.
Contraindications
Among the contraindications to the use of the drug "Naloxone" instructions for use mention the following conditions and diseases:
- hypersensitivity to the active substance or one of the components of the drug;
- heart disease (organic);
- severe liver and kidney disease;
- physical dependence on opioid analgesics.
With caution, the drug should be prescribed to pregnant women with drug addiction, since the manifestations of the withdrawal syndrome resulting from the introduction of the solution can adversely affect the condition of the fetus. The same applies to use in neonates whose mothers have abused opioids throughout pregnancy.
In any case, the benefit of the drug should exceed the possible risk of complications in the patient. We remind you that only prescription dispensing of the drug "Naloxone" is practiced. A prescription written in the appropriate form by the attending physician implies that the patient has no serious contraindications to the use of this drug.
Methods of application and dosage
The dosage of the drug and the method of its administration are determined by the specialist based on the current condition of the patient. Here are the generally accepted treatment regimens with the Naloxone solution.
Overdose of analgesic drugs in adults requires the administration of 0.4 to 2 mg of the drug (1-4 ampoules) intravenously or intramuscularly. A single dose for children is calculated based on body weight, it is 0.005-0.01 mg / kg.
To remove the patient from medical sleep (in the postoperative period), the drug is administered intravenously in the following amounts: adults at a dose of 0.1 mg, followed by repeated administration until spontaneous breathing is restored, children - 0.01 mg / kg of body weight up to breathing recovery.
For newborns, the solution is administered intravenously, intramuscularly or percussion in the amount of 0.1 mg/kg of body weight once.
If it is necessary to diagnose drug addiction, the drug is administered intravenously at a dose of 0.08 mg.
Adverse reactions
Among the negative consequences of using the Naloxone medication, the instruction mentions the following conditions:
- nausea, possibly with the urge to vomit;
- increased blood pressure;
- heart rhythm disturbances;
- tremor and convulsions;
- excessive sweating.
In patients with opioid dependence, the use of the drug can cause diarrhea, pain of unclear localization, swelling of the nasal mucosa, feeling very tired, chills, stomach and intestinal cramps. Mentioned phenomenaare considered typical for drug withdrawal. They pass within a few tens of minutes.
Analogues of the drug "Naloxone"
Is it possible to replace the drug "Naloxone" with similar drugs? Analogues of this tool are few today. These include the drugs Narcan, N altrexone, Cyclozocin and Narcantin. Their pharmacological properties, indications and contraindications are similar to those of the Naloxone solution and tablets. That is why they are not recommended for patients who are allergic to a compound such as naloxone hydrochloride.
However, they also have their merits. For example, the drug N altrexone has a long duration of action (about 24 hours) and is available mainly in the form of tablets or capsules for oral administration. It is often used for coding from drug addiction by sewing a capsule with a solution under the skin.
Reviews about the drug
Naloxone has a good reputation among doctors. According to them, it helps to save many patients in case of accidental or deliberate overdose of drugs from the group of analgesics and / or opioids. Despite contraindications and a large number of side effects, the drug is considered relatively safe to use. In addition, it is with its help that hidden drug addiction can be revealed.