Opioids are all synthetic and natural substances that are able to establish communication with the opioid receptors of the body, which are located in the digestive tract and central nervous system: to stimulate and block them. What are opioids? First of all, it is the most powerful analgesics, means that eliminate pain syndrome. In addition to sedative and analgesic effect, they can also weaken intestinal motility, inhibit the cough and respiratory center.
Do not confuse them with opiates (Latin opium is a powerful drug that is produced from dried milky juice extracted from unripe opium poppy capsules). This type includes only natural substances extracted from poppy. These are thebaine, morphine, oripavine, codeine, and so on. Thus, opiates can also be opioids, while opioids are not always opiates, since they also have a synthetic structure. The main disadvantage of opiates and opioids is the ability to induce a feeling of euphoria in a person. From this, some people are engaged in the use of opioids is not for medicinal purposes. This addiction leads to addiction and subsequent breaking (withdrawal syndrome).
Facts about opioids
Find out what opioids will help and this collection of facts from the World Health Organization: Opioids are psychoactive substances. An example is heroin and morphine. Every year, 69,000 people die in the world due to an overdose of these drugs. The average number of people suffering from opioid addiction worldwide was 15 million. However, not all of them use illicit heroin. Many use prescription opioids. Only 10% of addicts receive treatment for their addiction. The pharmacological effect of opioids is such that when taking a large dose of them, respiratory depression and subsequent death occurs. The consequences of opioid overdose (including death) can eliminate an inexpensive remedy called naloxone.
The negative effect of opioids
The main disadvantage of the drug is the appearance of opioid dependence. From this follows the following: Strong narcotic desire to use the drug. Violation of the ability to control their behavior. The appearance of adverse effects. Loss of the meaning of normal life in pursuit of the effect of an opioid. Breaking after stopping the use of drugs.
Dependence and its consequences can occur both after prolonged use of opioid anesthetics by prescription (for example, in case of severe chronic pain), and as a result of illegal diversion of the drug from the warehouses of enterprises, pharmacies, medical institutions. In our time, developed effective measures to combat it.
Opioids in the history
What is opioids, mankind knew 4 thousand years ago. It is known that in the Minoan civilization a goddess enjoyed special reverence, whose image was surrounded by a crown of opium poppy boxes. Also, opioids were known to later civilizations – Corinth (Greece) and Afyon (Turkey). From there, the extraction of opium from poppy spread to the East. It should be noted that until the middle of the 17th century, opioids were used exclusively as a painkiller, and not as a drug. But smoking opium in the desire to fall into euphoria began to spread in China in the second half of the XVII century. It is impossible not to recall the so-called Opium Wars, which broke out at the end of the XVIII century. The reason for them was that the British East India Company, taking advantage of its monopoly position, imported huge quantities of opium into China. Further, the history of drugs and opioid drugs developed as follows: 1804 – German pharmacist F. Serturner was able to extract from opium its main active component, called the discoverer “morphine” (the term “morphine” was introduced somewhat later by Gay-Lussac). 1898 – semi-synthetic morphine derivatives called “heroin” and “ethyl morphine” entered medical use. 1937 – The first fully synthetic opioid pethidine was obtained in Germany. A little later, the same nature of methadone was synthesized. In the Soviet Union, pethidine derivative, promedol, was used. The end of the 1950s – Fentanyl was synthesized in Belgium.
The structure of opioids
The chemical structure of opioids is the most diverse. Their most common component is the benzene ring, which is connected by a propyl or ethyl “bridge” to the nitrogen atom. This is what ensures the similarity of opioids with tyrosine, an amino acid that is part of enkephalin (the simplest opioid peptide) and plays an important role in its interaction with opioid receptors.
The nitrogen atom is most often represented here as a component of the piperidine ring. A large proportion of opioids are tertiary amines.
Graduation of opioids by origin So, opioids.
What concerns them in this group? Preparations divided into several smaller gradations: Natural, vegetable: opium alkaloids: thebaine, morphine, codeine; other plant opioids: salvinorin A, mitraginine. Synthetic, artificial: methadone, promedol, tramadol, fentanyl and so on. Semi-synthetic: heroin, ethyl morphine, hydromorphone and so on. Endogenous (those that directly produces the body itself): endorphin, nociceptin, enkephalin, endomorphin, dinorphin.
Graduation of opioids by action
Now consider the other opioids that belong to them according to this classification: Antagonists: nalmefene, naloxone, naltrexone. Partial agonists: oxycodone, propoxyphene, codeine, diphenoxylate, hydrocodone. Complete agonists: heroin, methadone, fentanyl, hydromorphone, oksidon, morphine, alfentanil, oxymorphone, levorfanol, alfentanil, meperidine, remifentanil. Mixed-effect agonist antagonists: pentazocine, buprenorphine, nalorphine, nalbuphine, butorphanol.
Graduation of opioids by structure
What drugs are opioids in this classification? Incorporating the following elements: Phenanthrenes (4,5α-epoxymorphinans) are natural or semi-synthetic opioids that are similar in structure to morphine, that is, they have a piperidine and aromatic ring. These are heroin, codeine, morphine, hydrocone, oxycodone, naloxone, 6-mono acetylmorphine, buprenorphine, nalbuphine, oxymorphone. Morphinanes, Their structure differs from the structure of morphine in epoxy remote “bridge”. It also distinguishes them from purely synthetic origin. These are dextromethorphan, levorphanol, butorphanol. Benzomorfan are compounds such as phenazocin, metazocin, pentazocine. Diphenylheptanones. Phenylpiperidine. 4-anildopiperidine.
Separation by Effect
What is opioid medication? It is also a means, divided by the intensity of its impact on the system of the human body. Within this, there are three groups: Potent drugs: fentanyl, buprenorphine, sufentanil, carfentanil, remifentanil, briefentanyl, alfentanil. Medium intensity drugs: pentazocine, codeine, trimeperidine, nalbuphine. Weak drugs – for example, tramadol.
Purpose of an opioid analgesic
To prescribe such an ambiguous remedy as an opioid analgesic, the attending physician is entitled in the following cases: The use of another type of analgesics does not bring the desired effect. This is typical, for example, for cancer patients suffering from chronic severe pain, which is why they are shown opioid agonists. On the scale of pain, the patient’s syndrome goes beyond the mark of mild pain (4 is the strongest, 3 is strong, 2 is moderate, 1 is weak, 0 is not present). For example, in Russia: for the mark “4”: fentanyl, morphine; for mark “3”: buprenorphine; for mark “2”: prosidol, tramadol.
Guidelines for choosing opioid treatment
If the treating doctor determined that without opioid analgesics, therapy will be ineffective, he should be guided by the following: At the start of treatment, these drugs should be taken for patients for a strictly limited time and only after unsuccessful attempts at therapy with other analgesics. Be sure to take into account all the contraindications: the nature of the pathology, dependence on drugs in the past of the patient, the presence or absence of home care and so on. Only one doctor assumes responsibility for the appointment and discharge of opioid drugs. The purpose of the drug should be clearly justified, and the doctor must comply with a number of guarantees to the patient. For this, in particular, the patient signs a written agreement on this therapy. Be sure to inform the patient about the possible development of addiction to the drug, especially if its reception is combined with sedatives, hypnotics. The patient should be aware of the possibility of physical dependence up to the stage of breaking when opioid use is stopped. A pregnant woman is instructed that her taking an opioid can cause dependence on her and the baby. Extraordinary use of opioids should be strictly prohibited. Therefore, in advance it is necessary to provide analgesia for acute short-term exacerbations of pain. Taking a dose of the drug to patients should be regular, strictly according to the schedule drawn up by the doctor. Extension of treatment with the adoption of opioid drugs occurs only after an agreement to the patient. Opioid treatment must necessarily be combined with a different anesthetic and rehabilitation therapy.
As we have already noted, due to the specific effects on the brain area responsible for breathing, high-dose opioids can lead to respiratory depression and death. Most people at risk are those with opioid addiction syndrome. Overdose is easy to identify on three main grounds: respiratory depression. Constricted pupils. Loss of consciousness. If taking a large dose of opioids combined with the adoption of other sedative drugs, alcohol, such an overdose in most cases is fatal. The following persons are considered to be at risk here: Having opioid dependence. The risk increases after cessation of treatment, detoxification, release from prison. Patients using injection-opioids. People who have been prescribed large doses of opioids by prescription from a doctor. Patients who are prescribed opioids, along with sedatives. Individuals who take opioids and are diagnosed with diseases such as HIV, lung and liver diseases, suffering from depression. Family members of the opioid receiving doctor.
How to save a person from an overdose
You can prevent a fatal outcome from an opioid overdose in two ways: Maintaining vital processes in the body. Timely administration of Naloxone, an opioid antagonist drug. “Naloxone” has a lot of advantages: It can be called almost an antidote for overdose with opioid drugs or drugs. With the timely introduction can almost completely eliminate all the negative effects of overdose. It is effective in various administrations: subcutaneous, intravenous, intramuscular, intranasal. It does not adversely affect the body when it is taken by a person who does not take opioids. painkillers opioids Cons are only in the limited availability of the drug, not only in Russia, but in a large number of other countries. This applies even ambulances and medical institutions. Only, for example, in Italy “Naloxone” is sold in pharmacies without a prescription. WHO seeks to urge the world’s ministries of health to make this opioid antagonist more accessible. After all, with the introduction of this drug to a person with an overdose of opioids, even accidental witnesses of the incident can save a dying person’s life, stretching precious time before the arrival of emergency medical care. This call has already found a response from the US government, Scotland.