What are opioids? What drugs do they include?
This article will deal with ambiguous form of medicines. On the one hand, they are potent analgesics, on the other - drugs that cause addiction. Let's talk about what opioids are.
Opioids are all synthetic and natural substances that are able to establish links with opioid receptors in the body that are in the digestive tract and central nervous system: to stimulate and block them.
What is opioids? First of all, these are the most powerful analgesics, the remedies that eliminate pain syndrome. In addition to the sedative and analgesic effect, they can also weaken the intestinal peristalsis, depress the cough and respiratory center.
Do not confuse them with opiates( Latin opium - is a strong drug that is produced from dried, milky juice extracted from unripe opium poppy capsules).This type refers only to natural substances extracted from the poppy. It is 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 their ability to evoke a sense of euphoria. From this, some people are engaged in the use of opioids is not for medicinal purposes. Such a pernicious habit leads to addiction and subsequent withdrawal( withdrawal syndrome).
Facts about opioids
To find out 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 in the world, 69 thousand people die.
- The average number of people with opioid dependence around the world was 15 million. However, not all of them use illegal heroin. Many people use opioids prescribed by prescription.
- Only 10% of addicts receive treatment for their addiction.
- The pharmacological action of opioids is such that when taking a large dose of them, respiratory depression and subsequent death occurs.
- The consequences of opioid overdose( including lethal outcome) can eliminate an inexpensive remedy called Naloxone.
Negative effect of opioids
The most important negative of the drug is the appearance of dependence on opioids. From this follows the following:
- Strong narcotic desire to use the drug.
- A violation of the ability to control your behavior.
- Appearance of harmful effects.
- Loss of meaning of normal life in the pursuit of the effect of the opioid.
- Breaking after discontinuing drug use.
Dependence and its consequences can arise both after long-term use of analgesic opioids by prescription( for example, in case of severe chronic pain) and as a result of illegal diversion of the drug from warehouses of businesses, pharmacies, and medical institutions. In our time, effective measures to combat it have been developed.
Opioids in the history of
What is opioids, humanity knew 4 thousand years ago. It is known that in Minoan civilization, the goddess, whose image was surrounded by a crown of opium poppy capsules, enjoyed special reverence. Opioids were also known to later civilizations - Corinth( Greece) and Afyon( Turkey).From there, the extraction of opium from the poppy 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 the smoking of opium in a desire to fall into euphoria began to spread in China in the second half of the XVII century. One can not help but recall the so-called Opium Wars that broke out at the end of the 18th century. The reason for them was that the British East India Company, using its monopoly position, imported huge quantities of opium to China.
Further the history of narcotics and opioid drugs developed as follows:
- 1804 - German pharmacist F. Sertürner was able to extract from opium its main active ingredient, called the discoverer "morphine"( the term "morphine" was introduced somewhat later by Gay-Lussac).
- , 1898 - semi-synthetic derivatives of morphine, called "heroin" and "ethylmorphine", were introduced into medical practice.
- 1937 - the first completely synthetic opioid pethidine was obtained in Germany. A little later, methadone of the same nature was synthesized. In the Soviet Union, a derivative of pethidine, promedol, was used.
- The end of the 1950s.- Fentanyl was synthesized in Belgium.
Structure of opioids
The chemical structure of opioids is very diverse. The 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 to 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 constituent of the piperidine ring. A considerable part of opioids are tertiary amines.
The classification of opioids is somewhat:
- by origin;
- for action;
- on the structure.
Let's analyze each of them in detail.
Gradation of opioids by descent
So, opioids. What does this group include? Preparations divided into several smaller grades:
- Natural, vegetable:
- opium poppy alkaloids: tebain, morphine, codeine;
- other vegetable opioids: salvinorin A, mitragynine.
- Synthetic, artificial: methadone, promedol, tramadol, fentanyl and so on.
- Semisynthetic: heroin, ethylmorphine, hydromorphone and so on.
- Endogenous( those that are produced directly by the body itself): endorphin, nociceptin, enkephalin, endomorphine, dinorphine.
Degradation of opioids by the action of
Let us now consider other opioids that are classified according to this classification:
- Antagonists: nalmefene, naloxone, naltrexone.
- Partial agonists: oxycodone, propoxyphene, codeine, diphenoxylate, hydrocodone.
- Complete agonists: heroin, methadone, fentanyl, hydromorphone, oxydon, morphine, alfentanil, oxymorphone, levorphanol, alfentanil, meperidine, remifentanil.
- Antagonists-agonists of mixed effect: pentazocine, buprenorphine, nalorphine, nalbuphine, butorphanol.
Degradation of opioids in the structure of
What drugs are related to opioids within this classification? Comprising the following elements:
- Fenantrenes( 4,5 α- epoxymorphinans) are natural or semisynthetic opioids that are close in structure to morphine, i.e. having a piperidine and aromatic ring. These are heroin, codeine, morphine, hydrocone, oxycodone, naloxone, 6-monoacetylmorphine, buprenorphine, nalbuphine, oxymorphone.
- Morphinans, Their structure differs from the structure of morphine by an epoxy remote "bridge".They are also distinguished by a purely synthetic origin. This is dextromethorphan, levorphanol, butorphanol.
- Benzomorphs are compounds such as phenazocine, metazocine, pentazocine.
Separation by effects of
What are opioid preparations? It is also a means, divided by the intensity of its impact on the systems of the human body. Within this framework, three groups are distinguished:
- Strong drugs: fentanyl, buprenorphine, sufentanil, carfentanil, remifentanil, brifentanil, alfentanil.
- Medium-intensity drugs: pentazocine, codeine, trimiperidine, nalbuphine.
- Weak drugs - for example, tramadol.
Assignment of opioid analgesic
To designate an ambiguous agent as an opioid analgesic, the attending physician is entitled to:
- The use of analgesics of a different kind does not bring the desired effect. This is typical, for example, for cancer patients suffering from chronic severe pain, why they are shown opioid agonists.
- On the scale of pain the patient's syndrome goes beyond the mark of mild pain( 4 - the strongest, 3 - strong, 2 - moderate, 1 - weak, 0 - not present).For example, in Russia:
- for the "4" mark: fentanyl, morphine;
- for the "3" mark: buprenorphine;
- for the "2" mark: prosidol, tramadol.
Guidelines for the selection of opioid treatment for
If the treating doctor has determined that therapy is ineffective without opioid analgesics, he should be guided by the following:
- At the start of treatment, these drugs should be taken to the patient for a strictly limited time and only after unsuccessful attempts at therapy with other analgesics.
- It is necessary to take into account all contraindications: the nature of the pathology, the dependence on drugs in the past the patient, the presence or absence of home care and so on.
- Only one doctor takes responsibility for prescribing and discharging opioids.
- The administration of the drug should be clearly justified, and the physician must perform a number of safeguards in front of the patient. For this, in particular, the patient signs a written agreement for 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 the appearance of physical dependence before the stage of withdrawal when the use of the opioid is discontinued.
- A pregnant woman is instructed that her acceptance of an opioid can cause dependence on him and the child.
- The extraordinary adoption of opioids should be strictly prohibited. Therefore, it is necessary in advance to provide analgesia in case of acute short-term exacerbations of pain syndrome.
- Acceptance of a dose of a drug to the patient should be regular, strictly according to the schedule compiled by the doctor.
- Prolongation of treatment with the adoption of opioid drugs occurs only after agreement on the patient.
- Opioid treatment must necessarily be combined with other analgesic and rehabilitative therapy.
Overdose of opioids
As we have already noted, due to the specific effects on the brain area responsible for respiration, opioids in high doses can lead to respiratory depression and death. In general, people with opioid dependence depend on this risk. Overdose is easy to identify by three main symptoms:
- Respiratory depression.
- Narrowed pupils.
- Loss of consciousness.
If taking a large dose of opioids was combined with taking other sedatives, alcohol, then 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 opioid injections.
- People who are prescribed large doses of opioids by prescription from a doctor.
- Patients who are prescribed opioids along with sedatives.
- Persons who take opioids and who are diagnosed with such diseases as HIV, lung diseases, liver, suffering from depression.
- Family members of the opioid taking the doctor's prescription.
How to save a person from an overdose
The lethal outcome of an opioid overdose can be prevented in two ways:
- Maintaining vital processes in the body.
- Timely input of "Naloxone" - an opioid antagonist.
"Naloxone" has a lot of advantages:
- It can be called a practically antidote for an overdose of opioid drugs or drugs.
- With timely administration, it can almost completely eliminate all the negative effects of an overdose.
- Effective for various kinds of administration: subcutaneous, intravenous, intramuscular, intranasal.
- Does not have a negative effect on the body when taken by a person who did not take opioids.
Cons is limited only to 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 institutions. Only, for example, in Italy, "Naloxone" is sold in pharmacies without a prescription.
WHO is seeking to call ministries of health of world states to make this opioid antagonist more accessible. After the introduction of this remedy to a person with an overdose of opioids, even accidental witnesses of the incident can save the dying person, extend valuable time before the arrival of emergency medical care. This call has already found a response from the US government, Scotland.
Prevention of opioid overdose
In addition to preventive work among the population aimed at disseminating information about the deadly dangers of drugs, the following measures are considered to be effective enough:
- Reduction of the practice of irrational administration of opioids.
- Affordable treatment of opioid dependence, aimed not only at rehabilitation of drug addicts, but also on persons taking opioids as prescribed by a doctor.
- Strict control over the prescription and dispensing of opioids in pharmacies.
- Suppression of cases and severe punishment of those responsible for the sale of opioids without a prescription.
Opioids are ambiguous drugs. Strong analgesics, they cause and addiction. In addition, because of the effect of euphoria for a long time served as narcotic drugs, an overdose of which at the same time is fatal.