In the XIX century, when opium addiction swept the whole world, doctors found a medicine that was supposed to cope with opium addiction. This substance was called morphine. But it soon turned out that morphine leads to even greater problems than opium. They created a new drug for morphine addiction, which, according to experts, differed in the absence of dependence and good effect. The name was given to this drug sonorous – heroin. A new stage in the rise of drug addiction and crime began. With this diabolical product, psychiatrists could not cope for a very long time. But the decision has come. True, it came from fascist Germany. A new drug was named after Dolphin in honor of Adolf Hitler. After the war, the name changed. It began to be called methadone and is used to “treat” heroin addiction. For many years, methadone has been touted in many countries as a tool that helps alleviate heroin addiction. Today it is recognized not only useless, but also the most powerful and dangerous drug. This “medicine” does not eliminate dependence, but only makes the “buzz” states less vivid. At the same time, the consequences of methadone use are more dangerous and prevalent than in the case of heroin.
Methadone is a narcotic drug that is used to relieve dependence on more complex drugs like heroin or amphetamine. In order for a drug addict to quit using heroin, it is replaced with methadone. Sensations from methadone are not so sharp and it is easier for a drug addict to give up a drug.
The essence of substitution treatment programs is that a person who is dependent on opioids is transferred from using illegal drugs to using legal “substitute drugs” of the same kind that are provided in medical institutions. Yes, opioid dependence persists, but the legal use of “substitute drugs” under the control of doctors allows a person to function fully, does less harm to his health, and strengthens his social and legal status. And when methadone is already introduced into the environment of drug users, and it is worth noting that dependence on it comes very quickly and it is very persistent. The legislative framework has been adopted and it is necessary to continue providing methadone to drug addicts. Now in the US, methadone is on Schedule II of narcotic drugs, i.e. the use of methadone strictly for medical purposes, according to a prescription. Do not store or use without prescription. Schedule II drugs, substances, or chemicals are defined as drugs with a high potential for abuse, with use potentially leading to severe psychological or physical dependence. These drugs are also considered dangerous (Drug scheduling, 2017).
The low effectiveness of curative and rehabilitation programs for people with substance dependence caused the introduction of so-called substitution therapy into medical practice, which implies the delivery of a drug to patients in order to prevent their consumption of drugs purchased in the illegal market. The beginning of replacement therapy should be attributed to 1964, when V. P. Dole and M.E. Nyswander proposed methadone for patients with heroin addiction. Methadone helps opioid dependent individuals to lead a more socially active and productive life, and also to keep jobs and maintain relationships with loved ones. Methadone has many positive effects. Treatment of opiate dependence with methadone is done in one of two ways. MMT (methadone maintenance treatment) is designed for people who want to quit illicit drug use but who are unable to abstain from opiates for a long time. The duration of methadone maintenance therapy may be several months or even years. There are also programs to reduce methadone dependence for drug addicts who want to completely stop using drugs. The duration of such program will depend on the initial dose and rate of reduction of dependence, which depends on the clinic and on the individual patient. In addition, participation in methadone therapy can help reduce the transmission of infectious diseases associated with opiate injections, such as hepatitis and HIV. The main effects of methadone therapy are the reduction of drug cravings, the suppression of withdrawal symptoms and the blocking of euphoric effects associated with the use of opiates. When used correctly, methadone maintenance treatment is considered safe and non-sedative from a medical point of view.
There is no disagreement about methadone detoxification. This process should be slow, and closely monitored. The pain associated with methadone detoxification can be intense. Opioid detoxification cannot be life threatening, but it is always difficult, painful and it is a psychological test for an addict. Detoxification, developed by a narcologist, will help alleviate pain and discomfort. Such detoxification also provides for the rejection of all medications that are not needed. To determine the person’s individual needs, a deep assessment of psycho / bio / social factors should be conducted. It is important to remember that it is not a change of one addiction to another, and any mental disorders should not be left without attention. Finally, detoxification is the process of removing toxins from the body. This is not a cure. The underlying predilections and mental disorders that contributed to the emergence of dependence are still intact.
Methadone acts similarly to morphine on people who are not used to opioids. Methadone suppresses the function of the central nervous system, causing blurred consciousness and a sense of pleasure, which drug addicts seek. Nausea, vomiting and intestinal obstruction are common harmful effects, like lack of appetite, dry mouth, sweating and fatigue. Also, there may be violations of sexual functions, lowering blood pressure, slowing of the heartbeat and muscle cramps. In addition to clouding consciousness, methadone can cause respiratory depression, which is considered one of the most serious harmful effects. Because of the effect on the serotonin system, the use of methadone increases the risk of so-called serotonin syndrome. With prolonged use, the body becomes accustomed to methadone, so the consumer must take ever-increasing doses to achieve the desired effect. The body also gets used to most harmful influences, except for some (intestinal obstruction and miosis, narrowing of the pupil of the eye). With prolonged use, methadone no longer causes a sense of pleasure, but, most likely, prevents the emergence of an abstinence syndrome.
Abstinence syndrome with methadone dependence occurs after 1.5-2 months of daily intake. The first signs of abstinence appear one day after the last use. There is irritation, fear, anxiety and stress, accompanied by an irresistible craving for methadone. When objective examination reveals a slight narrowing of the pupils and a lack of response to light. After a while there is tachycardia, blood pressure rises. Mental tension continues to increase, and vegetative symptoms join it. There is lacrimation, nasal congestion, nausea and vomiting. On 3-4 days there are pains, reaching a maximum for 5 days. The patient suffers not only from pain, but also from severe dysphoria, as well as from a compulsive craving for methadone. There is psychomotor agitation, possible aggression and autoaggression. By the end of the first week in some patients with methadone addiction develops psychosis, accompanied by anxiety, confusion, visual and auditory hallucinations. After exiting psychosis, the pains disappear, within a month, mood disturbances, a decrease in criticism to one’s condition and a poorly expressed neurological symptomatology remain.
In case of overdose there is a weakness, drowsiness, perhaps dizziness, double vision or unclear objects. It is also characterized by urinary retention. Symptoms may progress slowly and not cause particular concern for patients and their relatives. Subsequently, there is an increasing respiratory insufficiency, death can occur due to stopping breathing or pulmonary edema. In some cases, due to hypersensitivity to the drug, an overdose is possible even when taking a therapeutic treatment dose. Respiratory depression due to an overdose can be treated with naloxone. Naloxone is more preferable compared to the new longer-acting antagonist naltrexone. Naltrexone has a longer half-life and its use is associated with difficulties in terms of titration dose. Taking too much of an opioid antagonist in dependent patients can lead to an abstinence syndrome (perhaps very severe). When using naloxone, the drug is rapidly excreted from the body, resulting in abstinence will be short. Dosing of naltrexone from the body takes longer. A common problem in the treatment of methadone overdose is that, given the short action of naloxone (compared to the extremely long-acting effect of methadone), the dosage of naloxone is selected so as to withdraw the patient from an overdose, but once naloxone ceases to function unless a new patient is given dose, the patient may again experience an overdose (depending on the time of taking methadone and dosage).
Pharmacology and its mechanism; metabolism
The antinociceptive system is the central mechanism of pain regulation and changes in the body’s response to it. In turn, pain nociceptive effects are those main factors that trigger and activate endogenous analgesic systems. In the membranes of neurons involved in carrying out painful impulses, there are specific “opiate” receptors. They are excited by endogenous neuropeptides – enkephalins (therefore sometimes they are called “enkephalin” receptors) or endorphins having a more complex structure. Excitation of opiate receptors reduces the release of mediators – chemical agents that cause pain (serotonin, histamine, acetylcholine, prostacyclin, substance P, etc.). There are several types of these receptors: m (mu), d (delta), k (kappa), s (sigma), e (epsilon) have various functional significance. It is proved that when acting on m-receptors, there is an analgesic effect, respiratory depression and physical dependence; the excitation of k-receptors causes analgesia, a calming effect. Narcotic analgesics, due to their structural similarity to enkephalin and endorphin molecules (the presence of a tyrosine residue), interact and excite opiate receptors, in addition, bind enkephalinases, enzymes that destroy enkephalins, thus increasing the level of these mediators.
The drugs stimulate the activity of the antinociceptive system, strengthening the inhibitory effect on the pain and its emotional manifestation. Basically, narcotic analgesics act on the nonspecific multi-neuronal pathway of the nociceptive system. The drugs inhibit the carrying out of painful impulses to the non-specific nuclei of the thalamus, the hypothalamus, the amygdala complex (reduce the vegetative and emotional reaction to pain, increase the pain tolerance threshold) and to a lesser extent affect the neurons of the horn of the spinal cord, raising the threshold of pain sensitivity. Strong analgesics (fentanyl, lofentanil, buprenorphine, etc.) are expressed suppress pain impulses and the specific nociceptive pathway. Under the influence of morphine-like substances, the flow of pain impulses in the thalamus region, the reticular formation is inhibited, and their holding in the cerebral cortex is inhibited. Great importance in the formation and regulation of pain has a thalamus. Three major nuclear thalamic complexes participate in pain integration: ventrobasal complex, posterior group of nuclei, medial and intralaminar nuclei. Neurons of the posterior group of nuclei respond to painful skin irritations and tooth pulp, facilitate the transmission and evaluation of localization of pain. Medial and intralaminar nuclei perceive somatic, visceral, auditory, visual and painful stimuli. They also take part in the perception of painful irritations of the tooth pulp. This group of nuclei plays an important role in the integration of “secondary”, poorly localized pain: they form complex vegetative and protective reactions to pain, as well as behavioral manifestations of it. Morphine-like substances inhibit the carrying out of only painful impulses in the thalamus region. Perception of other sensory modalities (sound, light) they do not eliminate (even in large doses). Since opiate receptors are found not only in the ways of pain, but also in the cerebral cortex, hypothalamus, hippocampus, amygdala and other parts of the brain, narcotic analgesics give a variety of psychotropic effects: marked sedation (sedative effect), euphoria, hallucinations, etc. Tolerance pain, the emotional coloring of pain sensations changes significantly, anxiety disappears, expectation of pain. All this is largely due to the sedative properties of the drugs, the state of euphoria (good, pleasant state of health), the subjective sensation of physical and mental rest, mental comfort, and eventually leads to the oppression of emotionally negative manifestations of pain.
Methadone acts mainly through the ?-opioid receptor of the central nervous system. Methadone is also able to prevent the transport of both serotonin and norepinephrine into the cell. Prevention of transport to the cell increases the effectiveness of analgesic action. Methadone, when taken by mouth, absorbs quickly and well, although significant individual deviations occur. The effect of methadone begins within 30-60 minutes. The effect of a single dose, used to alleviate pain, lasts about 4 hours, but there may be significant individual deviations. With continued use, the agent lasts longer due to its accumulation in the tissues; for example, with opioid substitution therapy, methadone is given only once a day. The approximate half-life is about 24 hours. The taste of the drug is bitter.
Tolerance and dependence
Methadone is a drug that falls into the same category as other synthetic and naturally occurring drugs such as pethidine, heroin, morphine, codeine, etc. Methadone has cross-tolerance and cross-dependence with these substances. This means that a person develops tolerance to opiates in general, and not just to the one that he uses. With prolonged use, the methadone property causes a sense of pleasure to weaken, but with intravenous use this property is preserved to some extent. At an intravenous reception is also enough a smaller dose. For these reasons, methadone is used as a drug intravenously. Injecting easily addictive. Methadone, being a potent opioid of long-term action, is considered especially dangerous for intravenous use, but it is also very dangerous when taken through the mouth. Doses used in opioid substitution therapy are fatal for people who accidentally use opioids and are dangerous to experienced consumers, especially if there are breaks in use. For people who are not used to opioids, the lethal dose is about 50-100 mg. At intravenous reception this dose is less. With methadone replacement therapy, daily doses at the beginning of the course for oral administration are 10-40 mg, and during maintenance therapy 60-120 mg. If several sessions are missed during therapy, subsequent doses should be reduced by 25-50% in order to prepare for a decrease in tolerability. By the end of the course of replacement therapy, the doses decrease gradually, for example, 2.5-5 mg per week. Since methadone preparations (tablets, solution) are not intended for intravenous use, as a result of using the intravenous method, auxiliary substances enter the body, which can clog the blood vessels and cause various infections. Eye injuries are also possible.
Society and culture
Methadone programs after a period of unjustified “big expectations”, “hopes” and first successes began to cause increasing and greater criticism from both doctors and other professionals, and the public of those countries where they were introduced. Reasons for not using them widely: relatively high methadone toxicity, which leads to quite dangerous complications from internal organs; slow rate of its excretion from the body, which significantly increases the risk of overdose with simultaneous use of methadone and heroin (in the event that the patient violates the prescribed regimen of participation in the methadone program, the abstinence from self-admission of other drugs). Substitution therapy has two options. The first: the use of methadone for the purpose of arresting acute manifestations of heroin withdrawal with a lytic reduction in doses – and the second: for the purpose of prolonged replacement therapy, since it is believed that the appointment of methadone leads to an end to the consumption of “street drugs” (which is rather doubtful). The Beyond Methadone study in New York City monitored 29 locations where patients had been stopped by police, all near treatment clinics. For a period in 2010, 40 percent of people surveyed had reported being checked by law enforcement while 70 percent of others said they witnessed such activity (What to Know about Methadone Clinics, 2017).
Even with a short application of opiates, a person enters the circle with lightning speed, from which it is very difficult to escape. Constantly required for a satisfactory state of the drug dose is a lot of money for the extraction of which a patient with drug addiction often goes to criminal activities. Almost all drug addicts steal, take part in robberies and frauds, or draw money from their parents, sell things from their homes, or engage in prostitution, or participate in the distribution of drugs, getting their “dose” for it. With such antisocial and antisocial activities, the social, moral, intellectual degradation of the individual naturally develops. The natural outcome of such processes is death either from extreme exhaustion of the nervous system, marked changes in the cardiovascular and other systems, or from an overdose of a narcotic drug or related toxic products. Among other things, through one syringe, in the absence of other possible options, several people inject the drug intravenously, which sooner or later leads to infection with viral hepatitis, HIV infection, and in some cases syphilis.
Opioid crisis – 2017
On October 26, 2017 US President Donald Trump announced the opioid crisis in the United States as a national disaster requiring emergency measures. Every year, tens of thousands of people die from overdoses in the United States. According to the preliminary assessment of The New York Times, in 2016, 59 to 65 thousand people became victims of overdoses; this is more than every year they die in car accidents. Approximately two-thirds of all deaths from overdoses are associated with heroin and other opioids. The number of deaths has been growing steadily since the early 1990s; in the last 10 years the number of deaths of heavy drugs has been increasing faster and faster (Katz, 2017). Opioid crisis is well researched, for work on it was given the Pulitzer Prize to Eric Eyre (Eric Eyre of Charleston Gazette-Mail, Charleston, WV, 2017). Researchers and journalists associate the spread of opioid dependence primarily with prescription analgesics, such as oxycontin and vicodin. Since the early 1990s, the US has developed a medical practice prescribing to help patients with chronic pain – and prescribe them strong painkillers with opioids. As follows from the claim of the state of Ohio to the manufacturers of painkillers, pharmacological companies downplayed the dangers of drugs and argued that dependence in patients is extremely rare and does not pose a serious problem (Lopez, 2017). Sooner or later, any doctor understands that the patient goes to him not for a cure for pain, but for a drug – and stops prescribing medications or refuses to increase dosage.
Thus, after all, I think that the methadone program: does not solve the problem of drug dependence; actually legalizes the use of a dangerous drug and legalizes its spread; does not solve the problem of AIDS prevention; does not stimulate the development and implementation of new course methods of treatment of drug addiction as a disease; forms a large risk of diversion into the illicit traffic of a dangerous drug; promotes the emergence of underground narco-laboratories in the country; forms a new form of drug addiction – methadone; excludes from society people who can still be cured and socially adapted, and deprives them of the prospect of a return to a healthy lifestyle, makes them doomed.
If carefully to consider the moment of appearance, creation of narcotic substances including methadone, it is visible that people, scientists created the synthetic drugs (methadone, amphetamines and others), in most cases, of course, in search of a new medical device. And as a result, there are thousands of people dying from drugs. Now the situation is this way, that there are people who create new synthetic drugs daily, and no longer for any scientific purposes, namely to sell their potion on the black market. To date, a new generation is under real threat, with each year growing both the number of drugs consumed, and the number of their consumers. And methadone is not the last drug that is not legally promoted and sold. A person will never get into a trouble if he realizes and understands that the drug is in front of him and that consequences are inevitable. Some believe that enlightenment does not make any sense. But enlightenment is prevention. “This campaign, including aggressive television and social media outreach, must focus on telling our children of the dangers of these drugs and addiction, and on removing stigma as a barrier to treatment by emphasizing that addiction is not a moral failing, but rather a chronic brain disease with evidence-based treatment options…” (Powerpoint, 2017).