In medical practice, situations occur in which the use of drugs leads to an overdose or negative reaction from various organs and systems. Especially often, opioid drugs cause such complications. To speed up their withdrawal from the body, doctors use special medicines. The drug "Naloxone" is a tool that helps to correct the situation with an overdose of opioid analgesics. What is it and what is the mechanism of its effect? Let's try to understand these issues.
Description of the drug, composition and form
The medicine “Naloxone” refers to the instructions for use as an opioid receptor antagonist. Its active ingredient is naloxone hydrochloride. Dosage forms that can be found on the pharmaceutical market are not so diverse, this is an injection and tablets. The latter are very rarely used in medical practice. The liquid form for intravenous or intramuscular administration, in contrast, is 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 salts.
The drug "Naloxone" is available in ampoules of transparent glass with a volume of 1 ml each. The concentration of the active substance in a single dose is 0.4 mg.
The drug is packaged in contour packaging of varnished transparent plastic with a plug made of aluminum foil or without it. Each such package holds 5 ampoules.
1 or 2 contour packs are placed in a cardboard box along with instructions for the use of the drug and an ampoule scarifier. If the ampoules are equipped with a special ring or break point, the knives for opening them in the box are not put.
The mechanism of action of the drug "Naloxone"
As mentioned above, the drug "Naloxone" instructions for use relates to antagonists of opioid receptors. This means that this agent 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 patients with drug addiction.
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 in 1-2 minutes, with intramuscular injection in 5 minutes. The duration of the therapeutic effect also depends on the method of administration of the solution. If the solution was injected into the muscle, the medicine lasts about 45 minutes, and with intravenous infusion - at least 4 hours.
Specialists most often use Naloxone solution to treat patients. Tablets, unlike him, act weakly and for a short time.
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
In what cases is the use of Naloxone medication recommended? Instructions for use of the drug contain a detailed list of situations in which its use is highly desirable. First of all, it is prescribed to patients after surgery. The use of the drug "Naloxone" (analogues are also often used in the postoperative period) in this case helps to quickly remove the patient from the state of drug sleep. The medicine "Naloxone" is also used to eliminate the effects of ethanol poisoning, an overdose of analgesics, barbiturates and benzodiazepines.
Often, its use is justified in the case of the birth of a child in conditions when opioid analgesics were administered to the mother during childbirth. As a rule, these children have difficulty breathing independently. The drug "Naloxone" eliminates them and helps activate respiratory function. The solution is often used as a diagnostic tool in cases of suspected drug addiction in a patient.
It is worth noting that the only condition for using this tool is strict evidence. That is why in medical practice it is used strictly according to a doctor’s 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 opoid analgesics.
With caution, the drug should be prescribed to pregnant women with drug addiction, since the manifestations of withdrawal symptoms resulting from the introduction of the solution can adversely affect the condition of the fetus. The same applies to the use in newborns whose mothers have abused opoid drugs throughout their 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 drug Naloxone is practiced. A prescription written in the appropriate form by the attending physician implies that the patient does not have serious contraindications to the use of this drug.
Dosage and administration
The dosage of the drug and the method of its administration are determined by a specialist based on the current condition of the patient. Here are the generally accepted treatment regimens with Naloxone solution.
An 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 a patient from medical sleep (in the postoperative period), the drug is administered intravenously in the following amounts: for adults, at a dose of 0.1 mg, followed by repeated administration to restore spontaneous breathing, for children, 0.01 mg / kg of body weight until breathing is restored.
For newborns, the solution is administered intravenously, intramuscularly or percussion in an amount of 0.1 mg / kg of body weight once.
If it is necessary to diagnose drug dependence, 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;
- increase in blood pressure;
- heart rhythm disturbances;
- tremors and cramps;
- increased sweating.
In patients with opioid dependence, the use of the drug can cause diarrhea, pain of unclear localization, swelling of the nasal mucosa, a feeling of extreme fatigue, chills, stomach and intestinal cramps. The specified phenomena are considered typical for a narcotic “breaking”. They pass within a few tens of minutes.
Analogues of the drug "Naloxone"
Is it possible to replace the drug "Naloxone" with similar composition of drugs? Analogues of this tool are not numerous today. These include Narcan, Naltrexone, Cyclosocin and Narcantin. Their pharmacological properties, indications and contraindications are similar to those of the Naloxone solution and tablets. That is why they are undesirable to use if patients have an allergy to a compound such as naloxone hydrochloride.
Nevertheless, they have their own merits. For example, the drug "Naltrexone" acts for a long time (about 24 hours) and is available mainly in the form of tablets or capsules for oral administration. It is often used to code for drug addiction by stitching a capsule with a solution under the skin.
Reviews about the drug
Among doctors, the drug "Naloxone" has a good reputation. According to them, it helps 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 you can reveal hidden drug addiction.