What are opioids? What drugs belong to them?

This article will discuss the ambiguous form of drugs. On the one hand, these are potent analgesics, on the other hand, addictive drugs. Let's talk about what opioids are.

What is it?

Opioids are all synthetic and natural substances that are able to communicate 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, these are the most powerful analgesics, pain relievers. In addition to the sedative and analgesic effect, they can also weaken intestinal motility, inhibit the cough and respiratory center.

what are opioids

Do not confuse them with opiates (lat. Opium - a strong drug that is produced from dried milky juice extracted from immature boxes of opium poppy). This type includes only natural substances extracted from poppies. These are thebaine, morphine, oripavine, codeine and so on. Thus, opiates can also be opioids, while opioids are not always opiates, because they also have a synthetic structure.

The main minus of opiates and opioids is the ability to cause a person to feel euphoric. From this, some people are involved in the use of opioids far from medicinal purposes. This addiction leads to addiction and subsequent withdrawal (withdrawal symptoms).

Opioid Facts

To learn what opioids are, this collection of facts from the World Health Organization will also help:

  • Opioids are psychoactive substances. An example is heroin and morphine.
  • Every year, due to an overdose of these drugs, 69 thousand people die in the world.
  • The average number of people with opioid dependence worldwide was 15 million. However, far from all of them use illegal heroin. Many people use prescription opioids.
  • Only 10% of addicts receive treatment for their addiction.
  • The pharmacological effect of opioids is such that when a large dose is taken, respiratory depression and subsequent death occurs.
  • The consequences of an opioid overdose (including death) can be eliminated by an inexpensive drug called "Naloxone".

The negative effect of opioids

The main disadvantage of the drug is the appearance of dependence on opioids. This implies the following:

  • Strong narcotic desire to use the drug.
  • Impaired ability to control one’s behavior.
  • The appearance of harmful consequences.
  • The loss of the meaning of a normal life in pursuit of the effect of an opioid.
  • Breaking after stopping the use of the medicine.

opioids what applies to them

Dependence and its consequences can arise both after prolonged use of painkillers with prescription opioids (for example, in case of severe chronic pain), or as a result of illegal leakage of the drug from the warehouses of enterprises, pharmacies, and medical institutions. Nowadays, effective measures have been developed to combat it.

Opioids in History

What are opioids, mankind knew 4 thousand years ago. It is known that in the Minoan civilization the goddess was especially respected, whose image was surrounded by a crown from boxes of opium poppies. Opioids were also known to later civilizations - Corinth (Greece) and Afyon (Turkey). From there, the extraction of opium from poppies spread to the East.

It should be noted that until the middle of the XVII century, opioids were used exclusively as an anesthetic, and not as a drug. But smoking opium in a desire to fall into euphoria began to spread in China in the second half of the XVII century. One cannot but recall the so-called Opium Wars that erupted at the end of the 18th century. Their reason was that the British East India Company, taking advantage of its monopoly position, imported huge consignments of opium to 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 ingredient, called the pioneer "morphine" (the term "morphine" was introduced somewhat later by Gay-Lussac).
  • 1898 - Semisynthetic derivatives of morphine called "heroin" and "ethylmorphine" came into medical use.
  • 1937 - the first fully synthetic opioid pethidine was obtained in Germany. Methadone of the same nature was synthesized a little later. In the Soviet Union, a derivative of pethidine, promedol, was used.
  • The end of the 1950s - In Belgium, fentanyl was synthesized.

The structure of opioids

The chemical structure of opioids is the most diverse. Their most common component is a benzene ring, which is connected by a propyl or ethyl "bridge" with a nitrogen atom. It is this that 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.

opioids classification

The nitrogen atom is most often represented here by the piperidine ring moiety. A considerable part of opioids is tertiary amines.

Classifications

There are several classifications of opioids:

  • by origin;
  • by action;
  • by structure.

We will analyze each of them in detail.

Grade of Opioid Origin

So, opioids. What is their concern in this group? Drugs, divided into several smaller grades:

  • Natural, vegetable:
    • alkaloids of opium poppy: thebaine, morphine, codeine;
    • other plant opioids: salvinorin A, mitraginin.
  • Synthetic, artificial: methadone, promedol, tramadol, fentanyl and so on.
  • Semi-synthetic: heroin, ethylmorphine, hydromorphone, etc.
  • Endogenous (those produced directly by the body itself): endorphin, nociceptin, enkephalin, endomorphine, dynorphin.

Opioid Gradation by Action

Now consider other opioids that relate to this classification:

  • Antagonists: nalmefen, naloxone, naltrexone.
  • Partial agonists: oxycodone, propoxyphene, codeine, diphenoxylate, hydrocodone.
  • Complete agonists: heroin, methadone, fentanyl, hydromorphone, oxydone, morphine, alfentanil, oxymorphone, levorphanol, alfentanil, meperidine, remifentanil.
  • Mixed effect agonist antagonists: pentazocine, buprenorphine, nalorphine, nalbuphine, butorphanol.

what drugs are opioids

Structure of opioids by structure

What drugs are opioids in this classification? Including the following elements:

  • Phenanthrenes (4,5 α- epoxymorphinans) are natural or semi-synthetic opioids that are close in structure to morphine, i.e., having a piperidine and aromatic ring. These are heroin, codeine, morphine, hydrocon, oxycodone, naloxone, 6-monoacetylmorphine, buprenorphine, nalbuphine, oxymorphone.
  • Morphinans. Their structure differs from that of morphine by an epoxy remote "bridge". A purely synthetic origin also makes them stand out. These are dextromethorphan, levorphanol, butorphanol.
  • Benzomorphans are compounds such as phenazocine, metazocine, pentazocine.
  • Diphenylheptanones.
  • Phenylpiperidines.
  • 4-anyldopiperidines.

Impact separation

What are opioids? It is also a means of sharing in the intensity of its effect on the systems of the human body. Within this framework, three groups are distinguished:

  • Potent drugs: fentanyl, buprenorphine, sufentanil, carfentanil, remifentanil, brifentanil, alfentanil.
  • Medium-intensity drugs: pentazocine, codeine, trimeperidine, nalbuphine.
  • Weak drugs - for example, tramadol.

opioids drugs

Prescribing an Opioid Analgesic

To appoint such an ambiguous tool as an opioid analgesic, the attending physician has the right in the following cases:

  • The use of another type of analgesic 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.
  • According to the pain scale, the patient’s syndrome goes beyond the mark of mild pain (4 - the most severe, 3 - severe, 2 - moderate, 1 - weak, 0 - not present). So, for example, in Russia:
    • for mark "4": fentanyl, morphine;
    • for mark "3": buprenorphine;
    • for mark "2": prosidol, tramadol.

Guidelines for opioid treatment

If the attending physician has determined that without opioid analgesics, the therapy will be ineffective, he should be guided by the following:

  • At the start of treatment, these drugs should be taken by 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, drug dependence in the patient’s past, the presence or absence of home care, and so on.
  • Only one doctor is responsible for prescribing and prescribing opioid drugs.
  • The purpose of the drug should be clearly justified, and the doctor must fulfill 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 intake is combined with sedatives, hypnotics. The patient should be aware of the possibility of physical dependence before the stage of withdrawal upon cessation of opioid use.
  • A pregnant woman is instructed that taking an opioid can cause dependence on him and the child.
  • Extraordinary administration of opioid agents should be strictly prohibited. Therefore, it is necessary in advance to provide analgesia for sharp short-term exacerbations of the pain syndrome.
  • Taking a dose of the drug to patients should be regular, strictly according to the schedule drawn up by the doctor.
  • Prolongation of treatment with the use of opioid drugs occurs only after the patient agrees.
  • Opioid treatment must necessarily be combined with other analgesic and rehabilitation therapy.

opioid use

Opioid overdose

As we have already noted, due to the specific effects on the part of the brain responsible for respiration, opioids in high doses can lead to respiratory depression and death. Mostly at risk are people with opioid dependence syndrome. An overdose is easily identified by three main signs:

  • Respiratory depression.
  • Narrowed pupils.
  • Loss of consciousness.

If taking a large dose of opioids was combined with taking other sedatives, alcohol, then such an overdose in most cases is fatal.

The following persons are considered a risk group here:

  • Having opioid dependence. The risk increases after cessation of treatment, detoxification, release from prison.
  • Patients using opioid injections.
  • People who have been prescribed large doses of prescription opioids from their healthcare provider.
  • Patients for whom opioids are prescribed together with sedatives.
  • People who take opioids and are diagnosed with diseases such as HIV, lung, liver, and depression.
  • Family members of the opioid host as directed by the doctor.

How to save a person from an overdose

The lethal outcome from an opioid overdose can be prevented in two ways:

  1. Maintaining vital processes in the body.
  2. Timely administration of "Naloxone" - an opioid antagonist drug.

"Naloxone" has a lot of advantages:

  • It can be called almost an antidote in case of an overdose of opioid drugs or drugs.
  • With timely administration, it can almost completely eliminate all the negative consequences of an overdose.
  • Effective with various kinds of injections: subcutaneous, intravenous, intramuscular, intranasal.
  • It does not adversely affect the body when taken by a person who has not taken opioids.

analgesic opioids

The disadvantages are only in the limited availability of the drug, not only in Russia, but in a large number of other countries. This applies even to ambulances and medical facilities. Only, for example, in Italy, "Naloxone" is sold in pharmacies without a prescription.

WHO seeks to urge ministries of health around the world to make this opioid antagonist more accessible. After all, with the introduction of this tool to a person with an overdose of opioids, even accidental witnesses of the incident can save a dying person's life, stretch precious time until the arrival of emergency medical care. This appeal has already resonated with the governments of the United States and Scotland.

Opioid Overdose Prevention

In addition to preventive work among the population aimed at disseminating information about the deadly harm of drugs, the following measures are considered quite effective:

  • Reducing the practice of irrational administration of opioids to patients.
  • Affordable treatment of opioid dependence, aimed not only at the rehabilitation of drug addicts, but also at those who take opioids as directed by a doctor.
  • Strict control over the administration of opioids and their dispensing in pharmacies.
  • Suppression and severe punishment of offenders selling over-the-counter opioids.

Opioids are controversial drugs. Strong analgesics, they are addictive. In addition, because of the effect of euphoria, it has long been a narcotic drug, an overdose of which at the same time is fatal.


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