Why is methadone dangerous? Methadone: action, overdose, consequences

Watch a video about methadone from doctor Timur Mamedov:

Methadone addiction ranks first on the list of severe forms of drug addiction. Most people mistakenly assume that this drug is not particularly dangerous. A persistent addiction to this drug develops very quickly, and it is many times stronger than heroin addiction, and also causes colossal harm to mental and physical health.

Methadone addiction is treatable, but this matter must be trusted exclusively professional specialists, practicing complex techniques. No fortune tellers, clairvoyants, hypnotists, or doctors with their miracle injections or pills can cope with this disease - their actions are initially aimed at luring money out of desperate relatives.

What is methadone?

Methadone is a synthetic opioid, created specifically to combat heroin addiction. This principle of substitution very soon yielded results: now it was necessary to treat heroin addicts for their addiction to methadone. In practice, it turned out that this drug is much more insidious and dangerous than traditional heroin. Addiction to methadone develops after just a few doses. It negatively affects the entire body and destroys it in a short period of time. According to statistics, methadone addicts do not live more than three years.

Stages of treatment

Family consultation

Initial consultation determines further move the entire rehabilitation of the addict. At this stage, you receive information about the timing, cost, and methods of treatment in our center.

Intervention

A necessary step to obtain the addict’s consent to treatment. Models of behavior of relatives in relation to the future rehabilitator are discussed.

Detoxification

Once the addict is ready to enter treatment, detoxification occurs. Those. cleansing the body of substances that alter consciousness. In each specific case, its duration varies. The procedure lasts from 2 to 7 days.

Inpatient rehabilitation

When an addict enters the center, his inpatient stay begins. He lives according to the regime established in the center, without access to narcotic substances. Treatment is carried out in a closed facility, so access to the patient is available to a strictly limited list of relatives on certain days.

Social adaptation

At this stage, the patient begins to leave the walls of the center, gradually increasing the period of stay in society. However, it is still closely connected with the center and a breakdown at this stage is unlikely. The addict learns to live soberly in society, without succumbing to temptations.

Lifetime support

Lifelong support is the very thing that keeps you from breaking down in difficult times. life situations. Such support is provided voluntarily by one dependent to another.

History of origin

Methadone was synthesized in Germany during World War II as a powerful pain reliever. In the 1960s, it began to be used as a substitute in the treatment of heroin addiction.

In the United States in 1961, the Single Convention on Narcotic Substances was adopted, then it was decided to prohibit any non-medical use of narcotic drugs, and illegal purchase and sale. This convention also prohibited substitution therapy with other “safer” drugs. The convention recommended banning the use of heroin and methadone for therapeutic purposes. However, adherents of methadone therapy ensured that this drug was placed under strict control, but was not prohibited for use in treatment.

Eight years later, a report on narcotic substances was presented at a UN session, it announced the results of a study of methadone, and also especially noted its extreme danger and the inappropriateness of the practice of methadone therapy. It was clear from the report that such treatment was nothing more than the usual substitution of one drug for another.

By the end of the seventies of the last century, methadone addiction began to spread throughout the world. It turns out that thanks to the efforts of narcologists, it appeared in circulation. new drug- methadone.

A huge number of studies have proven that taking methadone causes much more harm than the consequences of heroin addiction. For example, the duration of heroin withdrawal is no more than one week, but with methadone it is more than a month.

Effect of methadone

As a rule, drug addicts use methadone orally or intravenously, splitting the tablet and diluting it with water. The effect of taking the drug occurs after about 30 minutes. It should be noted that 90% of the drug is absorbed by the stomach. Maximum concentration occurs after approximately four hours. If you use this drug in the form of injections, a person will get the effect after 10 minutes, and in the next two hours the maximum concentration in the blood will be observed.

Methadone has its own peculiarity - it accumulates in the tissues of the body, resulting in a long-term narcotic effect. The effects of methadone can last up to 72 hours. Addicted people experience the following symptoms during this period of time:

• Tactile hallucinations;
• In some cases, auditory and visual hallucinations may occur;
• Carefree;
• Failure in the activity of the central nervous system;
• Euphoric effect.

Long-term use of this drug is addictive and tolerance is formed, as a result of which the addict needs to constantly increase the dose to obtain the desired effect.

Numerous studies have shown that methadone has the most acute period of withdrawal, compared to other opiates. As a result of such indicators, we can safely say that methadone addiction is stronger than other analgesics created on the basis of opiates.

Prices and treatment times

Persuasion for treatment

From 1 day
From 5000 rub/departure

Detoxification

From 1 day
From 3000 rub/day

Inpatient rehabilitation

From 1 month
From 1500 rub/day

Symptoms of methadone use

With methadone addiction, it is very difficult to identify the signs. Therefore, it will be quite difficult to find out through visual observation whether an addiction to this drug is developing. The most the right decision will hold laboratory research. Experts can determine the presence of a narcotic substance in blood, nails, urine or hair. This detection method will allow you to begin treatment on time and snatch your loved one from the embrace of this terrible disease.

In addition to laboratory methods for determining addiction, you can observe a person’s behavior, which can also indicate his addiction to methadone. Pay a little attention to your loved one to prevent real tragedy as addiction progresses.

The main signs of methadone use are the following:

• Constricted pupils;
• Traces of injections (for intravenous use);
• Intermittent and incoherent speech;
• Lack of appetite;
• Slow breathing;
• Lethargic, drowsy state;
• A drug addict constantly needs money because it is required to purchase the next dose.

The signs listed above can be called standard for most drugs belonging to the opioid group, and only a doctor can determine which drug your loved one is addicted to by performing laboratory tests. If you notice strange signs in the behavior of your loved one, then you need to immediately contact our drug treatment center. This is the only way you can not only save the fate of a person who has gone astray, but also save his life.

Consequences of methadone use

The effect of methadone is much weaker than the euphoria that drug addicts experience when taking heroin, but dependence on it develops much faster and stronger. After a little time, the addicted person begins to increase the dose, but the consequences of using methadone can become irreversible and very sad:

• Men experience sexual dysfunction;
• The kidneys stop functioning properly;
• Pathology of the lungs (suffocation, swelling);
• There are significant disturbances in the functioning of the heart muscle;
• Hepatitis;
• Infertility;
• Cirrhosis of the liver.

If you stop using a drug, a person begins to show symptoms of psychological and physical dependence. Withdrawal for a methadone addict lasts more than a month, which significantly affects health:

• Frequent headaches;
• Painful sensations in the joints and eyes;
• Fainting;
• Migraine;
• Vomiting and nausea;
• Fever;
• Suicidal tendencies;
• Depressive state.

Methadone addiction is treatable, but this process must be carried out in specialized clinics, under the strict supervision of treating staff. Only complex methods give positive results. Methadone addiction is so strong that it sometimes requires up to a year of rehabilitation programs.

Treatment of methadone addiction

The drug treatment center “Freedom”, despite the complexity of treating addiction to methadone, is ready to provide its professional services. We guarantee complete recovery of the addict from his addiction to this drug. Our center practices comprehensive treatment methods that have proven their effectiveness and guarantee complete recovery from addiction. The duration of therapy depends on how the treatment progresses with the patient - we will complete the course only if we are 100% sure of a positive result.

Our clinic practices exclusively voluntary treatment, no forced procedures. If your dear person refuses to undergo a course of treatment and does not give in to your threats and persuasion, then you can call us. We will send our psychologists to you; they know how to motivate a patient to undergo treatment.

Advantages of our drug treatment center:

• Qualified personnel with extensive experience;
• Each of our specialists works for a result in which they are no less interested in you, we do not put in hours - we do everything in our power;
• Guaranteed cure for addiction; in case of relapse, a repeat course is carried out at our expense;
• Complex techniques that have proven their effectiveness in practice;
• Each patient is assigned an individual treatment program and is provided with round-the-clock monitoring;
• Comfortable conditions of stay in our hospital;
• Modern equipment and the latest drugs;
• Each patient is provided with complete anonymity: you don’t even have to give your real name;
• Each of our patients can count on lifelong psychological support; such a program minimizes the percentage of breakdowns;
• Free psychological help needy relatives and friends of drug addicts;
• We are also ready to help with finding a job or starting your own business.

We are ready to provide a guarantee that after our treatment a person will completely get rid of his addiction and will not return to this business. We know our job and have saved thousands of lives and destinies.

Sign up for a free anonymous consultation

The modern market of narcotic substances is regularly replenished with new “products”. Surprisingly, the majority of street drugs are drugs that were invented with good intentions. Designed to relieve pain or eliminate anxiety and depression, they sooner or later come to the attention of those who are looking for new ways to get drunk. And methadone, developed to produce a strong analgesic, is just such a substance.

What is methadone? Chemical formula of methadone.

Methadone (6-(dimethylamino)-4,4-diphenylheptanone-3)- a long-acting synthetic drug from the group of opioids. For medical purposes it is used as an analgesic, as well as in replacement therapy, in the treatment of drug addiction.

Chemical formula methadone: C21H27NO.

Synonyms and analogues of methadone: amidone, anadone, heptadone, dolophine, phenadone, physeptone.

History of Methadone

Initially, methadone had nothing to do with the drug business. In 1937, a group of German scientists created a drug called Dolafin. The substance was synthesized from dimethylamine-2-chloropropane and diphenylacetonitrile. Subsequently, diphenylbutanesulfonic acid was used as the starting product for the synthesis, which significantly simplified the process of obtaining the drug.

Methadone, being relatively cheap and easy to produce, began to be used as a replacement for the more expensive morphine in pain therapy. And already in the 1940s it was put into mass production under the trade name “Amidon”.

The main advantage of amidon was its ability to exert its effect even when administered orally (unlike morphine, which provided an analgesic effect only in the form of injections).

Since 1954, the drug became known as methadone, and in the 1960s. M. Niswander and V. Dole developed a system that made it possible to use methadone as a replacement for heroin in the treatment of heroin addiction. The impressive effect that this system demonstrated at the beginning quickly became a collapse. Already in the 1970s. An increasing number of deaths caused by methadone began to be recorded. It didn’t take long to look for an explanation for this phenomenon: the use of the drug for medical purposes opened its way to the streets, where it began to be used en masse and uncontrollably by drug addicts. Only then did it become clear that methadone was no better than heroin, and as for the terrible consequences, it was even more dangerous.

Today, the most active participant in the methadone substitution therapy program is the United States, where this substance began to be used as part of the fight against HIV infection and crime among drug addicts. But even there there are more and more opponents of this method of treatment.

Narcologists of the Russian Federation consider it inappropriate to treat heroin addiction with methadone, and speak quite sharply on the topic that replacing one drug with another is not treating addiction, but its transition to a more dangerous level.

Methadone is on the list of narcotic substances prohibited for circulation on the territory of the Russian Federation, and therefore is not used for medical purposes.

However, it is worth noting that for some time methadone was still used in treatment in Russia as a substitute for heroin (in the 90s of the 20th century), however, after the drug was included in the “List of Narcotic Drugs, psychotropic substances and their precursors, subject to control in the Russian Federation and prohibition of its circulation”, ceased to be used. The rapid development of addiction to the drug, as well as its use for other purposes in order to obtain narcotic pleasure, were the main reasons for this decision.

Because the Federal law No. 3 of 01/08/98 “On Narcotic Drugs and Psychotropic Substances”, treatment of drug addiction with narcotic drugs is prohibited (Article 31, paragraph 6), methadone in Russia cannot be used in medical practice at all.

Effect of methadone

When taken orally, methadone is absorbed through the walls gastrointestinal tract and quickly enters the bloodstream. With this method of use, it begins to act within 30 minutes, having a massive effect on the central nervous and cardiovascular systems, as well as causing relaxation of smooth muscles. Its highest concentration in the blood is observed after 4 hours: the analgesic effect (when taking a therapeutic dose) occurs after 20-30 minutes and lasts about 4-6 hours.

When the drug is administered subcutaneously, the narcotic effect occurs within 10-15 minutes, and the concentration of methadone in the blood approaches peak values ​​after 1-2 hours.

Just like other drugs of the opioid group, methadone causes a feeling of complete relaxation and safety, euphoria, and its effect lasts from 1 to 3 days, depending on the individual characteristics CNS and the dose taken.

With regular use of methadone, the drug creates a “depot” in the tissues of the body. This means that with each subsequent use of the drug, its concentration in the body increases, and at the same time the likelihood of an overdose increases.

Harm and consequences of using methadone

As already mentioned, at a certain stage in its history, methadone was legal and even managed to try on the role of a panacea for heroin addiction. But experience in the treatment of drug addiction in general, and the use of methadone in particular, confirmed what was initially obvious: such substitution therapy did not lead to anything. Or rather, one addiction replaced another.

Moreover, compared to methadone, heroin turned out to be somewhat more “humane” - withdrawal symptoms (“withdrawal”) when quitting heroin last for several days. And without the opportunity to take methadone, the addict experiences all these symptoms (muscle and headache, convulsions, nausea and vomiting, extreme apathy, followed by attacks of aggression, etc.) for 3-4 weeks.

Like most drugs, methadone is addictive: over time, the degree of intoxication and euphoria after its use becomes weaker, which forces the addict to increase the dose. But addiction doesn't mean that Negative influence This substance weakens in the same way as the acuity of sensations. On the contrary, the body, already worn out by endless attempts to utilize the breakdown products of methadone and prevent it from causing irreparable harm, suffers even more. As a result, even a small overdose of this drug almost guarantees death.

The terrible consequences of using methadone and death await every person dependent on this substance. The only question is how soon the irreparable will happen.

But the causes of death as a result of methadone addiction are not limited to overdose. The effect of the drug on the central nervous system and smooth muscles often leads to suppression of the cough and gag reflex, which, in essence, are defense mechanisms. When "switched off" or ineffective in people using methadone, these reflexes lose their ability to stimulate the elimination of pathogens and toxins from the airways and stomach. As a consequence, death from sudden pneumonia, respiratory failure or basic food poisoning- not uncommon among people addicted to methadone.

Methadone video

7 facts about methadone

Living in hell. Methadone is the strongest and most dangerous synthetic drug

Methadone. Pros and cons of replacement therapy

Methadone addiction

Methadone is an “adult” drug. Its price on the black market is high enough for the most vulnerable category - children and adolescents - to be protected from it to some extent. But the area of ​​distribution of addiction among the adult population is almost limitless. Not only people who already use any drug can become dependent on the drug. narcotic substances(although this dramatically increases the likelihood of developing methadone addiction). Often, people who use methadone and its derivatives for medical purposes and neglect the doctor’s recommendations about the dosage and frequency of use of the drug become involved in drug addiction.

Dependence on methadone develops according to the classical pattern - drug use is resorted to against the background of any personal problems in order to alleviate psychological discomfort, or according to the principle “you have to try everything in life.” The first dose of the drug makes a person feel more relaxed, feel a sense of security and calm. Problems recede into the background, euphoria sets in - a state of bliss, joyful, spiritual uplift, inexplicable by external circumstances and reasons. After just one dose of methadone, a kind of “reminder” is formed in the psyche that there is a way to quickly and easily get rid of problems, mental or physical pain. And when negative feelings return, the decision to take another methadone seems natural.

But this does not last long: after 2-4 uses of the drug, a person ceases to need external incentives to take methadone - the addiction has already developed and requires “support” in the form of another dose.

Attention, methadone addiction develops very quickly: 2-3 injections are enough! If you are offered to try this drug, do not agree under any circumstances! The addiction to methadone develops rapidly, and it will be extremely difficult to quit using it on your own!

Symptoms and signs of methadone use

The use of methadone as a drug quickly manifests itself as dysfunction of internal organs. Especially noticeable are the symptoms indicating the effect of the drug on smooth muscle, which is a “component” of almost all systems and organs human body. Smooth or visceral muscles are the muscles of internal organs, muscles of the skin and skin glands, walls of blood vessels, excretory ducts of the genitourinary system, intestines, pharynx and heart.

The following are observed symptoms methadone use:

• breathing disorders (slow and shallow, and during sleep there is apnea, which often causes a complete stop of breathing);
• heart rhythm disturbances and blood pressure caused by changes in the tone of the vascular walls;
• negative changes in the gastrointestinal tract (intestinal atony, constipation, increased spasticity of the bile ducts, etc.);
• dysfunction of the urinary tract (urinary retention, painful spasms of the sphincter and bladder walls).

External signs that will help loved ones of a drug addict identify the problem are:

• An abnormally carefree attitude of a person towards everything that happens to him and what surrounds him. Ease of judgment can affect absolutely everything - from a broken cup to death loved one. A drug addict on methadone reacts equally complacently and calmly to both situations.
• Disorientation in space. Dependence on methadone can lead to loss or severe impairment of the ability to navigate the terrain. Even in familiar territory, for example, in one’s own apartment, a person may need some time to “remember” where the front door, kitchen, etc.
• Excessive sweating, not conditional physical activity or hot weather, which is accompanied shortness of breath- in general, one gets the impression that the person is extremely tired and exhausted.

Less obvious, but characteristic features addiction is absent-mindedness, inability to concentrate and maintain a conversation, unreasonable mood swings, gradual changes in a behavior pattern (a person begins to act in a way that is unusual for him). These manifestations become more obvious the longer the addiction lasts. At the so-called “point of no return,” changes become irreversible—some dysfunctions of the central nervous system cannot be treated—and certain personality characteristics may be lost forever.

Diagnosis and treatment of methadone addiction

Diagnosis of methadone addiction is carried out using special psychological, psychiatric and drug tests. So, to make a diagnosis, clinical picture should include the following items:

• the ever-increasing need for the drug;
• addiction to the drug and the need to increase its dosage/frequency of use;
• withdrawal syndrome that occurs when you voluntarily give up a drug or when you are unable to get another dose.

Treatment of methadone addiction usually carried out in a hospital setting, since the withdrawal syndrome is characterized by a long duration and extreme severity. Thus, if the drug is abruptly discontinued, cardiac, respiratory, and renal failure can quickly develop and coma may occur.

The duration of the course of therapy directly depends on the duration of taking methadone and the effect on the body that it managed to have, but in general, treatment rarely takes less than a year.

Although great importance has a composition individual programs therapy, they necessarily include the following stages:

Manufacturer: L. Molteni & C. dei F.lli Alitti Societa di Esercizio S.p.A

Anatomical-therapeutic-chemical classification: Methadone

Registration number: No. RK-LS-5No. 121922

Registration date: 11.12.2015 - 11.12.2020

Instructions

• Russian

Tradename

International nonproprietary name

Dosage form

Oral solution 5 mg/ml

Compound

1 ml of solution contains

active substance- methadone hydrochloride 5.0 mg,

Excipients: sucrose, glycerin, citric acid monohydrate, sodium benzoate, lemon flavor, purified water.

Description

A syrupy, colorless or slightly colored liquid with a characteristic lemon odor.

Pharmacotherapeutic group

Drugs for the treatment of diseases of the nervous system are different. Drugs for the treatment of addictive disorders. Means for the treatment of opiate addiction. Methadone

ATX code N07BC02

Pharmacological properties

Pharmacokinetics

After oral administration, the bioavailability of methadone ranges from 36 to 100%, the maximum concentration in the blood plasma is reached after 1 - 7.5 hours. After taking from 10 to 225 mg, the plasma concentration of methadone is from 65 to 630 ng/ml, respectively, the maximum concentration is from 124 to 1255 ng/ml. The effect of food on the bioavailability of methadone is unknown.

Methadone is a lipophilic drug, the volume of distribution ranges from 1 to 8 l/kg. In plasma, methadone is predominantly bound to α1-acid glycoprotein (85% to 90%). Methadone is detected in saliva, breast milk, amniotic fluid and umbilical cord plasma. Methadone is primarily metabolized by N-demethylation to the inactive metabolite, 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP). The conversion of methadone to EDDP and other inactive metabolites involves enzymes of the cytochrome P450 system, primarily CYP3A4, CYP2B6 and CYP2C19 and, to a lesser extent, CYP2C9 and CYP2D6. Metabolites are excreted mainly in the urine. Methadone is a substrate for P-glycoprotein, but its pharmacokinetics are virtually unchanged in the case of polymorphism or inhibition of P-glycoprotein. After repeated administration, the plasma concentration of methadone ranges from 1.4 to 126 l/h, the half-life (T1/2) is from 8 to 59 hours. Due to the lipophilicity of methadone, it is stored in the liver and other tissues. Slow release from the liver and other tissue may prolong the duration of action of methadone despite low plasma concentrations.

Pharmacodynamics

Methadone hydrochloride is a μ-agonist; a synthetic opioid analgesic with several actions qualitatively similar to morphine, the most pronounced of which are the effects on the central nervous system and smooth muscle organs. Methadone withdrawal syndrome, although qualitatively similar to morphine, differs in that it occurs more slowly, is more prolonged, and symptoms are less severe.

Indications for use

maintenance substitution therapy (MRT) for mental and behavioral disorders caused by opioid use, dependence syndrome

Directions for use and doses

Methadone - methadone hydrochloride solution only for oral administration.

Do not use for injection.

Maintenance replacement therapy for opioid addiction

Methadone is administered daily according to the clinical condition and treatment protocol. Drug regimens may be modified according to the clinical condition of the patient. Initially, a single dose of 15 to 20 mg (3 to 4 ml) is sufficient to relieve withdrawal symptoms. In case of recurrence of withdrawal symptoms or insufficient relief of the syndrome, the dose can be increased. If patients are physically dependent on high doses, they may require higher doses of methadone accordingly. Generally, 40 mg (8 mL) per day given as a single dose or divided doses is an adequate dosage level. Stabilization can continue for 2 - 3 days, then the amount of methadone must be gradually reduced. The frequency at which the amount of methadone is reduced is determined individually for each patient. In hospitalized patients, a daily reduction of 20% of the total daily dose is usually well tolerated. In outpatients, a slower decline is possible.

In the case of opioid-dependent patients with established stable drug addiction, maintenance therapy can be carried out only if previous multidisciplinary interventions are ineffective. This treatment is also suitable for patients with established opioid dependence and HIV infection, immunodeficiency syndrome, or AIDS if the doctor believes that another type of treatment has a less chance of abstinence from opioid use. Substitution therapy can eliminate "craving", that is, the compulsive seeking of heroin, and suppress the drug addict's anxiety. There is no need to perform a follow-up systemic naloxone test in individuals with severe psychophysical dependence on heroin, but it is important to screen for morphine-like substances in body fluids. It should be emphasized that urine testing to check for the presence of narcotic drugs and psychotropic substances is an integral part of methadone treatment. Excessive alcohol consumption should also be checked. If the urine test is positive for opioids, it is important to reevaluate the condition. The dosage should be determined by the doctor individually depending on each specific case to prevent the need for heroin, taking into account the psychophysical state and concomitant diseases of the patient. During maintenance therapy, some patients receive the same dose of methadone; for others, the dose is periodically adjusted up or down. In any case, the dose should be adjusted so that the therapeutic effect is maintained for at least 24 hours. As an example, most patients take a daily dose of 50 to 120 mg (10 to 24 ml), depending on their tolerance level and ability to metabolize the drug. Warning: unplanned or uncontrolled cessation of treatment may provoke an acute withdrawal syndrome.

Side effects

Often

Feeling calm, dizzy

Nausea, vomiting

Sweating, orthostatic hypotension,

Respiratory depression

Euphoria, dysphoria

Weakness, headache, insomnia

Agitation, disorientation

Visual impairment, miosis

Dry mouth, anorexia, constipation

Spasm of the biliary tract

Bradycardia, fluttering, syncope

Urinary retention, difficulty urinating

Antidiuretic effect

Decreased libido and/or sexual potency

Itching, hives and other skin reactions

Rarely

Stopping breathing

Shock, cardiac arrest

Prolongation of the QT interval, torsades de pointes (when taking large doses)

Hemorrhagic rash

Headache, stomach discomfort, diarrhea (when taking large doses, due to glycerin content)

Contraindications

Hypersensitivity to methadone hydrochloride or other components of the drug

Long-term constipation

Organic heart diseases

Severe liver and kidney failure

Decompensated diabetes mellitus

Porphyria

Hypotension

Intracranial hypertension

Traumatic brain injury

Acute asthma attack

Acute alcohol intoxication

Chronic obstructive pulmonary diseases

Respiratory failure

Pulmonary heart

Hypovolemia

Pregnancy, except for those cases indicated in the “Special Instructions” section, lactation and childbirth

Children's and adolescence up to 18 years old

Drug interactions

P-glycoprotein inhibitors

Methadone is a P-glycoprotein substrate; therefore, quinidine and verapamil can increase the concentration of methadone in the blood.

InductorsCYP3 A4

Methadone is metabolized by the CYP3A4 isoenzyme. Barbiturates, carbamazepine, phenytoin, nevirapine, rifampicin may promote hepatic metabolism of methadone, which may be more pronounced if an inducer is added after initiation of methadone therapy. These interactions do not exclude the occurrence of withdrawal syndrome, and therefore require an increase in the dose of methadone. If inducers of the CYP3A4 isoenzyme are discontinued, the dose of methadone may be reduced.

CYP3A4 enzyme inhibitors

Cannabinoid, clarithromycin, delavirdine, erythromycin, fluconazole, grapefruit juice, selective serotonin reuptake inhibitors, itraconazole, ketoconazole, nefazodone may increase methadone concentrations.

Excretion methadone is reduced by concomitant use of drugs that inhibit CYP3A4, such as some drugs for the treatment of HIV infection, macrolides, cimetidine, azole antifungals. Methadone reduces the AUC and Cmax of didanosine and stavudine, reducing the bioavailability of these drugs. In addition, methadone may slow the absorption and increase the first-pass effect of these drugs.

Antiretroviral drugs

Methadone increases plasma concentrations zidovudine for both oral and intravenous administration, and also causes an increase in the AUC of zidovudine for oral administration, more than for intravenous administration. These effects are due to inhibition of zidovudine glucuronidation and decreased renal clearance. In this regard, it is necessary to monitor the possible toxicity of zidovudine, and accordingly reduce the dosage of zidovudine. Patients taking both drugs may develop typical symptoms of opioid withdrawal (severe headache, myalgias, fatigue and irritability).

A protease inhibitor may interfere with the metabolism of methadone to some extent, but more significant responses are achieved with ritonavir.

Possible interaction with abacavir does not require dosage adjustments.

Efavirenz induces methadone metabolism via the cytochrome P4503A4 system. Therefore, it requires dose adjustment.

Methadone is weak foundation. Urine acidifiers ( ammonium chloride) may increase the renal clearance of methadone, so the dose of methadone should be increased.

Opioid antagonists

The pharmacological action of antagonists (naloxone and naltrexone) is opposite to the action of methadone. These drugs can block the effects of methadone and trigger withdrawal symptoms.

Agonists/antagonists(butorphanol, nalbuphine, pentazocine) may partially block the analgesic effect, respiratory depression and central nervous system (CNS) depression associated with methadone. Concomitant use may provoke and aggravate neurological, respiratory and hypotensive effects. The cumulative or opposite effect depends on the dose of methadone and becomes more common with low to moderate doses of methadone. These drugs may cause withdrawal symptoms in patients during long-term therapy.

Concomitant use of methadone with drugs having a depressive effect on the central nervous system may worsen respiratory depression, so it may be necessary to reduce the oses of one or both drugs. Disorders of the cardiovascular system may occur in patients simultaneously receiving methadone and drugs affecting cardiac output or electrolyte balance. In such cases, an ECG is recommended.

Antidiarrheal, antimuscarinic drugs

Diphenoxylate and loperamide can lead to serious cases of constipation, ileal paralysis, and worsening CNS depression, especially with long-term use.

Octreotide may reduce the analgesic effect of morphine and methadone, therefore, if a decrease or loss of pain control occurs, the use of octreotide suspension should be reconsidered.

special instructions

Patients at special risk.

In outpatients, methadone may cause orthostatic hypotension. Methadone should be used with caution with a reduced initial dose in elderly, debilitated patients, patients with hypothyroidism, Addison's disease, prostatic hypertrophy, and urethral stricture. During methadone treatment, QT prolongation and torsade de pointes (TdP) are possible, especially when using high doses (> 100 mg/day). Methadone should be used with caution in patients at risk of QT prolongation, such as advanced cardiovascular disease and a history of concomitant treatment with drugs known to prolong the QT interval.

Drug addiction

Methadone can cause morphine-like drug addiction. As a result of repeated use of methadone, psychophysical dependence and tolerance can develop, so it should be prescribed and used with the same caution that applies to morphine.

Use of narcotic antagonists.

In individuals with drug physical dependence, the use of normal doses of antagonists can cause an acute withdrawal syndrome. The severity of the syndrome will depend on the degree of physical dependence and on the dose of the antagonist administered. The use of an antagonist in these subjects may need to be avoided. If necessary for the treatment of severe respiratory depression in patients with physical dependence, the antagonist should be used with extreme caution and gradually from doses lower than recommended.

Interaction with other central nervous system depressants. Methadone should be used with caution and in reduced doses in patients concomitantly receiving other narcotic analgesics, general anesthetics, phenothiazines, other hypnotic sedative tranquilizers, tricyclic antidepressants and other central nervous system suppressors, including alcohol. In these cases, the development of depression and deep sedation or coma cannot be ruled out.

Anxiety.

Methadone does not have a sedative effect, so anxiety symptoms that appear during treatment should not be relieved by increasing the dose of methadone.

Traumatic brain injury and increased intracranial pressure.

The ability of methadone to depress respiration and increase cerebrospinal fluid pressure may be significantly increased in the presence of increased intracranial pressure, and the drug's side effects may obscure neurological symptoms in patients with traumatic brain injury (see section: Contraindications).

Asthma and other respiratory diseases.

In patients with acute attacks of asthma, with chronic obstructive pulmonary disease, cor pulmonale, in those with a significant decrease in lung volume due to existing respiratory depression, hypoxia or hypercapnia, even normal therapeutic doses of drugs can reduce the activity of the respiratory center and increase airway resistance before the onset of apnea (see section “Contraindications”).

Acute abdominal syndrome.

The use of methadone or other drugs may complicate the diagnosis or clinical course in patients with acute abdominal pathology.

Hypotensive effect.

The use of methadone may result in severe hypotension in patients with hypovolemia or concomitant medications such as phenothiazines or certain anesthetics. Methadone may cause orthostatic hypotension.

Athletes.

Use of this drug outside of therapeutic needs is doping. It can give a positive result in doping tests even in therapeutic doses.

Pregnancy

Methadone is contraindicated during pregnancy and lactation due to possible consequences for fetal development. However, if a pregnant addict is clearly unable to stop using heroin, the physician may decide to administer methadone maintenance therapy. This procedure should not be continued until the end of pregnancy at recommended doses, as it is necessary to prevent the onset of withdrawal symptoms in the mother and fetus.

If necessary, adjust the dose of methadone in the later stages of pregnancy until adequate drug levels are maintained to avoid possible withdrawal from therapy.

However, like any other drug, the risks and benefits it brings must be carefully assessed. Reducing the dose of the drug (if necessary) is carried out very gradually to avoid the development of withdrawal symptoms.

The final cessation of treatment is carried out under the supervision of a narcologist and obstetrician-gynecologist and should be carried out no earlier than the 14th week of pregnancy and no later than 32 weeks in order to avoid the risk of miscarriage and premature birth.

The use of methadone in pregnant women should be carried out under close medical supervision. Before using methadone, the patient must be informed about possible consequences use of the drug.

More than 60% of newborns born to opioid-dependent mothers have symptoms of neonatal abstinence syndrome (NAS), which tend to last 24-74 hours after birth and include the following: loud crying, fast breathing, hungry but ineffective sucking and increased restlessness and lack of sleep. Increased osmotic pressure and convulsions may also occur. The intensity of NAS does not correlate with the dose of methadone or other opioids used by a pregnant woman.

Lactation

Methadone penetrates into breast milk Therefore, the drug is not recommended for use during breastfeeding. Because of the risk of serious adverse reactions in infants and the benefits of treatment for the mother, it is recommended that either breastfeeding or methadone be avoided.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Considering the possible side effects, such as dizziness, agitation, disorientation, it is not recommended to drive a vehicle or operate potentially dangerous machinery.

Overdose

Symptoms: respiratory depression (decreased respiratory rate and/or vital capacity, Cheyne-Stokes respiration, cyanosis), deep drowsiness up to stupor or coma, distinct miosis, skeletal muscle flaccidity, cold and sticky sweat, sometimes bradycardia and hypotension.

Treatment: ensuring adequate respiratory exchange, if necessary, clearing the airways and establishing supportive artificial ventilation. In case of erroneous administration of methadone, especially a large dose, narcotic antagonists are needed that counteract respiratory depression. Methadone is a long-acting depressant (36-48 hours), whereas the antagonist effect is shorter lasting (1-3 hours). As a consequence, the patient requires constant monitoring to prevent or treat respiratory depression. An antagonist (naloxone, nalorphine or levallorphan) is administered intravenously and is the main drug to eliminate symptoms of intoxication. The use of naloxone is preferable due to the lower risk of respiratory depression. Depending on the clinical manifestations carry out symptomatic therapy (oxygen, infusions, vasopressors, etc.).

Release form and packaging

1000 ml of the drug in a non-plastic polyvinyl chloride bottle with a screw neck, sealed with a screw-on polypropylene cap with a control ring and a polyethylene gasket.

A label made of label or writing paper is affixed to each bottle and approved instructions for use are attached. medical use in the state and Russian languages. Each bottle comes with a polystyrene dispenser with graduations of 1-2-3-4-5-6 ml.

Bottles are placed in boxes made of cardboard for consumer packaging or corrugated cardboard.

Storage conditions

Store in a place protected from light at a temperature not exceeding 25 ° C, in original packaging.

Keep out of the reach of children!

Shelf life

After the first opening of the package 12 months.

Do not use after expiration date.

Conditions for dispensing from pharmacies

On prescription

Name and country of the organization - manufacturer

Name and country of the marketing authorization holder

L. Molteni & C. dei F.lli Alitti Società di Esercizio S.p.A., Italy

NameAnda countryorganizations - packer

L. Molteni & C. dei F.lli Alitti Società di Esercizio S.p.A., Italy

Address of the hosting organization on the territory of the Republic of Kazakhstan complaints from consumers regarding product (product) quality

JSC "Khimpharm", Republic of Kazakhstan,

Shymkent, st. Rashidova, 81

Phone number 7252 (561342)

Fax number 7252 (561342)

Address Email [email protected]

Attached files

663232501477976327_ru.doc	54.5 kb
974261671477977578_kz.doc	105 kb

Methadone is a potent drug of synthetic origin, part of the opioid group of analgesics. The main purpose is relief of severe pain syndrome and replacement therapy for heroin addiction. The drug is available in the form of a solution in ampoules, tablets, syrup and mixture.

Action

Methadone has direct impact on smooth muscle tissue, the central nervous system, the functioning of blood vessels and the heart. When taken orally, the drug is well absorbed through the walls of the stomach into the blood. The first effect is a pain reliever, which occurs after half an hour. The peak effect of the drug is observed after 3.5 hours. When administered by injection, the drug begins to act faster - the effect can be noticed after 10 minutes, the peak of action occurs in the second hour.

The analgesic effect lasts about 5 hours. The half-life of the drug is 14 hours. The narcotic effect can last 1-3 days. Here everything depends on the speed of metabolic processes, which occur differently in each organism, as well as on the dose taken.

Under the influence of Methadone, the addict has a feeling of security and carefree. There is also a feeling of intense euphoria. Higher nervous activity is disrupted, which leads to:

• to loss of orientation in space;
• to the development of auditory, visual, tactile hallucinations;
• to disruption of the visual organs.

Does Methadone Help You Quit Heroin Addiction?

In Russia, this drug has been withdrawn from circulation and included in the list of potent narcotic drugs. However, in some European countries it is widely used in the field of addiction medicine for the treatment of drug addicts during the rehabilitation period. Why did our country abandon the use of Methadone, and what frightens Russian doctors so much?

Firstly, the drug can accumulate in the body, so the dose must be reduced and the interval between doses increased. By using Methadone you cannot get the same sensations that are identical to the effect of taking heroin. The effect of the drug gives a less pronounced “high”. Therefore, drug addicts try to increase the dose in order to obtain more acute sensations. And even a slight excess of the dose leads to the development of an overdose and, as a consequence, to death. Methadone overdose has an extremely high mortality rate.

Secondly, dependence on the drug is several times stronger than the dependence that develops from taking heroin or cocaine. Treatment of methadone addiction is much more complex and lengthy than that of other drugs.

Thirdly, the consequences of taking Methadone are no easier than those of using heroin.

Fourthly, the technology for producing Methadone is more simplified than the technology for producing heroin, and is also much cheaper. Accordingly, more people will suffer from methadone addiction.

And, fifthly, Methadone, unlike heroin, can be used not only intravenously. This helps prevent infection various diseases common among drug addicts (hepatitis, HIV).

Signs of use

1. Euphoria.
2. Frivolity.
3. Muscle tissue spasms.
4. Hallucinations.
5. Disorientation in space.
6. Attacks of nausea and vomiting.
7. Increased heart rate.
8. Hyperhidrosis.
9. Visual impairment.
10. Concentration disorder.
11. Headache.
12. Skin itching.
13. Allergic manifestations in the form of urticaria and/or rashes.
14. Slow breathing.
15. Difficulty in defecation and urination.
16. Dryness of the oral mucosa.
17. General malaise.
18. Drowsiness.

Consequences of use

Methadone addiction develops faster than heroin addiction. Withdrawal is much more painful, especially since its duration is about a month, and as for heroin withdrawal, the syndrome lasts a maximum of 8-12 days.

If you take Methadone regularly, there may be consequences such as:

• decreased libido;
• problems with potency;
• infertility;
• renal failure;
• development of cardiovascular pathologies (angina pectoris, tachycardia, myocardial infarction);
• hepatitis/liver cirrhosis;
• sleep disturbances;
• pulmonary edema;
• suffocation.

How does methadone withdrawal syndrome manifest?

When you stop taking this drug, a person experiences withdrawal symptoms, which leads to disruption of the activity of almost all organs and systems of the body. Methodone withdrawal is characterized by the presence of:

• pain in the eyes;
• depression;
• increased anxiety and irritability;
• dizziness;
• fever;
• repeated vomiting;
• pain in tissues of joints and muscles;
• confused consciousness.

Overdose symptoms

The causes of an overdose of Methadone can be: a decrease in the degree of tolerance of the body, accidentally exceeding the dosage, mixing the drug with other drugs or taking it for the first time. To cause an overdose, it is enough to consume 30-50 mg of the drug; 9 out of 10 cases of poisoning end in coma and death.

Overdose symptoms are as follows:

• loss of consciousness;
• weakly palpable pulse;
• cold sweat;
• state of shock;
• constriction of the pupils;
• state of drowsiness;
• pale skin;
• foamy vomit;
• convulsions;
• suppression of respiratory and cardiac activity up to their complete stop.

What to do if you are poisoned by Methodon?

If intoxicated with this drug, the person who used it will not be able to help himself or herself. Therefore, the people around him are obliged to take action emergency measures, which may save the life of a drug addict.

The victim should be brought to consciousness. To do this, you can press on the painful point, which is located under the nose, or rub ears, pat on the cheeks. A drug addict can be brought out of his state of stupor by loud voice. Next, you need to immediately call a medical team.

The victim should be transferred to the bed and turned onto his right side. Bend left leg drug addict in the knee, and right hand– place it under his head and bend it at the elbow. The addict's lower jaw should be pushed forward. You need to stick out your tongue, and oral cavity release from vomit.

If doctors have not arrived yet, the victim urgently needs to be given an injection of Naloxone, which is an opiate antagonist. If no reaction is observed after 15 minutes, repeat the administration of Naloxone.

Monitor the addict's breathing. If it is absent, give artificial respiration. Also monitor your heartbeat. If the pulse cannot be felt, immediately begin the procedure of chest compressions.

Upon arrival of doctors, it is necessary to inform them which drug caused the overdose, and what measures were taken before their arrival.

Treatment of methadone addiction

It is almost impossible to cure methadone addiction at home. The drug addict must be placed in a specialized drug treatment clinic under the vigilant 24-hour supervision of medical personnel. Therapy for this addiction involves a number of relevant activities:

• First, the body is detoxified;
• then specialists provide drug treatment;
• The third stage is the psychologist’s help in adapting the drug addict to life in society.

The treatment process is strictly monitored by specialists. The duration of therapy is about a year.

If you suspect your loved one is using Methadone, but are not completely sure about it, take his biomaterial (nails, hair, urine, blood) to the laboratory. The analysis will allow you to accurately determine whether a given narcotic substance is present in the human body. If yes, contact the appropriate clinic immediately, because the sooner treatment begins, the higher the chances of a positive outcome.

Humanity has faced the problem of drug addiction since ancient times. According to statistics, Russian Federation There are more than 1.5 million people suffering from this disease. Methadone is considered a treatment for drug addiction in people; the outcome depends on the dosage; if abused, it can cause severe poisoning of the body, including death.

What is Methadone

The substance is a drug belonging to the group of synthetic opiates with a complex chemical structure. It is used as an analgesic and for the treatment of drug addiction in the West. In Russia, a decision was made in 2005 to include this drug on the WHO list in the section with psychotherapeutic drugs.

Chemical name

Methadone 6-(dimethylamino)-4,4-diphenylheptanone-3. Molecular mass substance is almost 310 grams per mole. The drug was synthesized by the Germans in 1937 and became widespread due to its good analgesic effect. Later they began to use it as a drug for the treatment of morphine and heroin addicts: addiction to it occurs quickly, abuse is dangerous to health.

Synthesis of Methadone

Dimethylamine-2-chloropropane and diphenylacetonitrile were used for the synthesis. The process was difficult due to the complexity chemical reactions, later changed to a more simplified and generally accessible method using diphenylbutanesulfonic acid. Compared to the well-known heroin, Methadone is cheaper, and addiction is more severe.

The drug is available in tablets or solution for intravenous administration. If taken orally, the risk of developing side effects, unlike injection drugs. The number of people infected with HIV and hepatitis C is decreasing. In the Russian Federation, methadone is subject to strict control by the Ministry for Combating Drug Trafficking, and the circulation of this drug is strictly prohibited.

Action

The drug activates opioid receptors and acts for approximately 5 hours. The medicine acts on the central nervous system, smooth muscles and the heart. It gradually accumulates in the body, and tolerance to it develops over a long time. Methadone is an effective analgesic. With single use, respiratory and cough reflexes are inhibited.

At withdrawal syndrome for other narcotic substances, it is able to suppress the signs of the disease for a long time. The drug affects muscle tone and motility of the gastrointestinal tract, and the function of the pituitary gland. Once in the bloodstream, the medicine is absorbed into the tissues of the liver, kidneys, lungs, spleen, and brain. Metabolism of the substance occurs in the liver, where the drug breaks down into active and inactive components.

After injection, Methadone can be detected in the blood after 10 minutes, when taken in tablet form after 30 minutes. It will reach its maximum concentration in plasma within 3 hours, then the amount will begin to decrease. The half-life is from 15 to 30 hours, depending on the duration of administration. Excretion occurs in urine and feces. First time use lethal dose of the drug - about 50 mg, and for drug addicts - more than 200 mg.

Indications for use

The drug has a strong analgesic and sedative effect. It is used to detoxify the body in case of opiate addiction, this is the so-called methadone therapy. The drug is used for the rehabilitation of drug addicts as a combination with other treatment methods. Often after such treatment, people begin to suffer from methadone addiction.

Instructions for use

The medicine is prescribed by the doctor. The drug is taken orally in tablets or in the form of a suspension (it must be diluted in 150 ml of clean water). To ease the withdrawal syndrome, 25 mg of the substance is first prescribed. The interval between doses is more than 4 hours; in addition, you can take no more than 10 mg. On initial stage the dosage on the first day is no more than 40 mg. For long-term therapy, a daily dose of 85-120 mg is prescribed.

The narcotic analgesic Methadone can be used for intravenous injection only when taking tablets or suspensions is not possible. The dose for administration of the drug is prescribed by the doctor, individually for each patient. Treatment is carried out strictly in a hospital setting and under the supervision of medical staff. If possible, the patient should be transferred to the tablet form.

special instructions

Before starting treatment with the drug, you must stop using any synthetic drugs. Symptoms may occur: nausea, vomiting, weakness, drowsiness, lacrimation, depression, weight loss, loss of appetite, tremors of the extremities. It is important to note heroin withdrawal from adverse drug reactions.

To eliminate physical pain from operations and injuries in patients undergoing methadone treatment, it is possible to use opioids of another group as pain relief. While being treated with this drug, you should refrain from administering any vehicles. Methadone and heroin withdrawal occur in the same way and are accompanied by insomnia, excitability, pain, and surges in blood pressure.

During pregnancy

There is no clear conclusion about the safety or harm of using this drug by pregnant women due to the lack of the required number of studies. Children of patients after treatment with Methadone during pregnancy were born with congenital malformations of internal organs. Newborns have physical dependence to a synthetic opiate. Their drug withdrawal syndrome manifests itself within a week after birth.

Interactions

Methadone is a potent drug; you should consult your doctor before using it with medications. Concomitant use with other medications leads to a decrease in plasma blood concentrations active substance and withdrawal syndrome occurs. List of these medications:

• Carbamazepine, Rifampicin, Phenytoin and Phenobarbital;
• Nelfinavir, Ritonavir, Efavirenz;
• mu-receptor antagonists (Naloxone, Pentazocine, Naltrexone, Butorphanol).

The substances that make up Methadone negatively affect the pharmacological properties of many medicines. These include:

• Zidovudine, Stavudine, Didanosine - lead to an increase in their toxicity.
• Monoamine oxidase inhibitors - increases the risk of severe adverse reactions.
• Azole antifungals, macrolide antibiotics and selective serotonin reuptake inhibitors - decreased drug clearance and increased adverse reactions; dosage adjustment is necessary.
• Antiarrhythmogenic drugs - cardiac interval prolongs.
• Antidepressants, antipsychotics, potassium channel blockers - cardiac conduction may be impaired.
• Diuretics, hormonal agents - caution should be exercised when combining.

Side effects

Methadone has a large number of undesirable reactions on the human body. With long-term use of the drug, malfunctions may occur different systems body:

• cardiovascular - arterial hypotension, tachycardia or bradycardia, arrhythmia, fibrillation, extrasystalia, heart failure.
• nervous – weakness, dizziness, agitation, euphoria or dysphoria, spatial disorientation, asthenia, headache, sleep disturbance, hallucinations, epileptic seizures.
• respiratory – swelling and inhibition of the drug addict’s breathing process.
• digestive – dry mouth, abdominal pain, dyspepsia (nausea, vomiting), constipation.
• genitourinary – amenorrhea in women, decreased libido, urinary retention.
• organs of vision – decreased acuity;
• allergic reactions - rash and itching of the skin.

Methadone poisoning

The drug Methadone can cause serious poisoning of the body. Accompanied by severe pain in the limbs and internal organs. This occurs due to excessive stimulation of opiate receptors in nervous system. In this case, depression of consciousness up to coma, constriction of the pupils, weakness, bradycardia, hypotension, and respiratory arrest are observed. In most cases, methadone addicts suffer from this problem; in severe cases, cardiac arrest and death can occur.

Methadone overdose

Exceeding the dose at the first dose - more than 50 mg and at the second dose - 200 mg, an overdose of this drug may occur. This condition is treated with artificial ventilation, Naloxone or Nalmefene is administered. Antagonist substances need to be reintroduced; Methadone is eliminated from the body more slowly than they are. When administering an antidote, it must be remembered that the patient may experience withdrawal syndrome. Health monitoring must be constant.

Contraindications

The drug is strictly contraindicated in the following conditions:

• heavy respiratory failure;
• bronchial asthma;
• disruption of the heart (arrhythmia, ventricular and atrial fibrillation);
• hypercapnia;
• individual intolerance to individual components of the drug;
• Tablets should not be taken if you have intestinal obstruction.

Terms of sale and storage

The tablets should be stored in a special closed container, protected from children. Avoid direct contact sun rays. Storage temperature – no more than +25 degrees. Shelf life – 2 years. You cannot buy Methadone at a pharmacy. The Russian government decided to add the medicine to the list of prohibited drugs.

Analogues

There are many drugs containing the same active ingredient. The names of these medicines:

• Amidon,
• Heptadon,
• Ada-non,
• Fenadon,
• Dolofin,
• Fisenton,
• Metadict,
• Methadol.

What does Methadone look like?

Video