In pharmacology, analgesics are usually divided into opioids and non-opioids. Non-narcotic (non-opioid) substances are called substances that relieve pain without having a strong negative effect on the functionality of the central nervous system. Such drugs do not have a psychotropic effect, which distinguishes them from narcotic compounds, and does not depress the nerve centers. Thanks to these nuances, the funds are widely used in medical practice today.
Efficiency and its features
Non-opioid - a group of analgesics, which has a relatively small effect of reducing pain in comparison with powerful narcotic drugs. If the syndrome is explained by visceral disorders, trauma, such drugs are practically ineffective.
The described category of drugs has not only an analgesic effect, but also an anti-inflammatory one. In addition, non-opioid analgesics are drugs that bring down fever. With the use of funds in a therapeutic dosage decreasesplatelet aggregation. Substances affect immune competence at the cellular level.
Efficiency nuances
Opioid and non-opioid analgesics have been researched by doctors for more than a decade. At present, it has not yet been possible to establish exactly what are the details of the pharmacological activity of non-narcotic drugs. There are a number of hypotheses that explain the effectiveness of the compounds. The most common option is as follows: under the influence of active compounds in the tissues of the body, the production of prostaglandins weakens, which leads to the desired relief of the condition as a whole.
The mechanism of action of non-opioid analgesics is associated with the functions of the thalamic centers. Due to the use of drugs, the conduction of pain impulses to the brain centers that receive them slows down. This central action is quite different from that inherent in narcotic compounds. Non-narcotic substances do not correct the ability of the CNS to summarize impulses.
Salicylates
Based on the classification of non-opioid analgesics, salicylates are substances that are able to correct different stages of the chain leading to the activity of the focus of inflammation. It has been established that the main effect in the effectiveness of these drugs is due to the inhibition of the biological production of prostaglandins. Clinical studies have shown that salicylates stabilize the lysosomal membrane, which slows down the reaction of irritation, inhibits the release of proteases.
Salicylates - analgesics, the action of which is associated with protein reactions: activecompounds prevent the denaturation of molecules. The drug has an anticomplementary effect. Inhibition of the production of prostaglandins causes a weakening of the activity of the inflammatory focus. At the same time, the algogenic effect of bradykinin decreases. Non-opioid drugs of this group activate the connection between the adrenal glands and the pituitary gland, due to which the release of corticoids becomes more active.
Options: lots of funds
The list of non-opioid analgesics is quite wide, and the effectiveness of these drugs varies greatly. Perhaps the most famous can be safely called:
- Acetylsalicylic acid.
- Nise.
- Ibufen.
The difference in potency is related to the ability of existing drugs to seep into organic tissues, which is different. It is customary to distinguish several main groups of painkillers: simple antipyretics, antiphlogistics, anti-inflammatory non-hormonal substances. The predominant percentage of drugs presented in pharmacies are weak acids that can easily penetrate into the focus of the pathological process. In diseased tissues, pharmacologically active compounds accumulate. Excretion from the body for the majority is characteristic of urine, a smaller percentage - with bile. Mostly non-opioid analgesics of central action are eliminated in the form of metabolic products of the liver. The substances obtained in such reactions do not have any effect.
Efficiency features: how does it work?
Having taken a central non-opioidanalgesic, the patient soon feels a decrease in pain, fever subsides. The desensitizing effect develops somewhat more slowly, the focus of inflammation is suppressed. To achieve a pronounced result in these two areas of activity, you will have to take sufficiently large doses of the drug. This is associated with the likelihood of complications, side effects due to inhibition of the production of prostaglandins. Most often, drugs lead to the accumulation of sodium, the formation of ulcerated areas in the gastrointestinal tract, swelling and a tendency to bleed. In addition, prolonged use of analgesics, especially in large doses, poisons the body. The chemicals contained in the preparations inhibit the hematopoietic function, stimulate methemoglobinemia and other serious conditions. All currently known centrally acting non-opioid analgesics can cause an allergic reaction and a para-allergic response of the body.
The use of formulations during the period of bearing a child can cause oppression, slow down labor activity, and close the ductus arteriosus ahead of time. As a rule, in the first third of the term, such drugs are not prescribed at all due to the increased risk of a pathogenic effect, although animal experiments have been conducted for the main percentage of medicines that have proven the absence of a teratogenic effect.
Science does not stand still
Exploring opioid and non-opioid analgesics, scientists have found that some substances can, in the absence of a narcotic effect, simultaneously inhibitthe production of not only prostacyclin, PG, thromboxane, but also leukotrienes. This quality is called "inhibition of lipoxygenesis". Drugs with both of these effects are relatively new, but the direction looks very promising. They show a more pronounced anti-inflammatory effect, but the likelihood of paraallergic responses is reduced to a minimum. It is almost impossible to develop asthma, rashes, runny nose, "aspirin triad".
No less promising are non-opioid analgesics that selectively influence the generation of various types of cyclooxygenases in the body. Compounds have already been developed that affect only thromboxane synthetases, PG F2-alpha, and COX-2 synthetases. The first type is Ibufen, based on ibutrin, the second is drugs on thiaprofen. They are less likely to develop swelling, ulceration, or bronchial spasm due to a lack of F2 PG. Finally, the last type is presented for sale by the Nise series, powered by nimesulide.
NSAIDs
The list of analgesic drugs in this category includes names that are known to almost every person who has used painkillers at least once in his life. Includes:
- Voltaren.
- Diclofenac.
- Ketoprofen.
Such funds are used if the pain syndrome in the articular, muscle tissues is disturbed, if the head hurts or neuralgia is detected. Substances are indicated for inflammatory processes in these areas of localization. As a fever relieverNSAIDs can be used if the patient has a fever, the temperature rises above 39 degrees. Non-opioid analgesics in this group can be combined with vasodilators, antihistamines, and antipsychotics to help increase the antipyretic effect.
Caution is an important aspect of treatment
Non-opioid analgesics - salicylates in the first place - can cause the development of Reye's syndrome, so it is necessary to prescribe such drugs very carefully to children. The risk group for complications includes patients under the age of twelve with a viral etiology of the disease. Amidopyrine, indomethacin can cause convulsions. Paracetamol is considered the optimal replacement.
In addition to the described non-opioid analgesics, desensitizing qualities and inhibition of inflammatory foci are characteristic of derivatives of indole-, phenylacetic, propionic, fenamic acids. When prescribing a therapeutic course based on the nuances and condition, the doctor must remember that aniline derivatives are practically not active in the foci of inflammation, and although pyrazolone can help in some cases, it is used extremely rarely due to its ability to inhibit hematopoietic function. In addition, the therapeutic effect inherent in this substance is rather narrow.
Any NSAIDs are strictly forbidden to use if an allergic reaction, a para-allergic response of the body was detected during the course or was observed in the past. You can not use these drugs with an ulcer in the stomach, disorders of the hematopoietic function of the body, as well as in the first third of the childbearing period.
Categories and types
To simplify orientation among the abundance of painkillers produced by the industry, it is customary to divide funds not only into opioid and non-opioid, but also mixed drugs. Among non-narcotic drugs, antipyretics, combined formulations, drugs with a central and peripheral effect are distinguished. Spasmoanalgesics are a group of drugs that contain several active substances. For example, Deegan is produced with the inclusion of nimesulide, dicyclomine in the formula.
Combination analgesics marketed under various trade names are based on the following substances:
- "Solpadeine" - paracetamol is combined with caffeine and codeine.
- "Benalgin" - caffeine is also added to metamizole, in addition, thiamine is present in the formula.
- "Paradik" - a combination of diclofenac, paracetamol.
- "Ibuklin" - a drug containing paracetamol, ibuprofen.
- "Alka-prim" is a medicine based on acetylsalicylic acid, to which aminoacetic acid is added.
- Alka-Seltzer is a product containing citric acid, acetylsalicylic acid and sodium carbonate water.
Features and differences
Non-opioid formulations do not affect opioid receptors and do not lead to addiction in the patient. They do not tend to have pharmacodynamic antagonists. Substances do not destabilize the work of the cough center and respiratory organs, do not lead to stool disorders (constipation). All of these properties distinguishthem on the background of narcotic painkillers.
Non-opioid drugs are prescribed for minor injuries - bruises and sprains. The drugs are effective in rupture of ligaments and help to alleviate the condition in case of soft tissue injury. Compositions can be used if pain bothers in the postoperative period, the syndrome is rated as average in level. Substances are indicated for pain in the head, toothache, with spasms of the flow of urine, bile. They are used for fever.
It so happened that non-narcotic painkillers are familiar to many and are often used as part of self-treatment, that is, there is no one to control the use of compounds. This makes the problem of complications and side effects especially relevant.
Salicylic acid and pyrazolone
Derivatives of these two substances are used to make a wide range of medicines. The best known to the layman is "Aspirin", whose effectiveness is due to acetylsalicylic acid. In addition, methyl salicylate, salicylamide are common in the pharmaceutical industry. Medicines based on sodium salicylate, acelysin are quite famous for their result. For all means of this class, a rather low poisoning ability is characteristic. Tests have shown: the lethal dosage of acetylsalicylic acid is 120 g. At the same time, there is also a weak point: increased irritant activity, which is likely to form bleeding and ulcerated areas. These funds are not used for patients under the age of twelve.
On substances derived from pyrazolone, made by everyoneknown "Analgin", whose main component is metamezol. No less popular is Butadion, which works by including phenylbutazone in the formula, and Antipyrin, made on phenazone. The drug "Amidopyrin" has a good reputation, the main compound of which is aminophenazone.
All of the listed drugs have a relatively narrow spectrum of therapeutic activity, however, the inhibitory effect of the hematopoietic function is estimated to be quite significant. This imposes restrictions on the duration of treatment: only short-term courses are allowed.
Metamezole in stationary conditions is more often prescribed injectively, since the substance is highly soluble in water. It can be injected into muscle tissue, a vein or under the skin if an urgent local anesthetic effect is needed, a decrease in temperature. When choosing a drug, you need to remember that in childhood, when using amidopyrine, the threshold for convulsions is corrected, diuresis decreases.
Para-aminophenol and indoleacetic acid
Paracetamol, phenacetin are obtained in chemical reactions involving para-aminophenol. Both of these drugs are ineffective against an active inflammatory focus, they do not have an antirheumatic effect and the ability to correct blood viscosity. The use of formulations is associated with a minimal risk of ulcer formation, and the substances are safe for the kidneys and do not inhibit the activity of the organ. The threshold of convulsive readiness practically does not change. At elevated temperatures, the mainThe drug of choice is paracetamol. This is especially true for the treatment of children. Prolonged use of phenacetin can cause a heart attack.
With the participation of indolacetic acid, sulindac, stodolac, indomethacin are obtained. The latter is a reference composition in terms of anti-inflammatory effect. It is believed that it is indomethacin that is inherent in the greatest strength. At the same time, the drug affects the metabolic processes with brain mediators, the concentration of GABA decreases. The use of an analgesic is accompanied by sleep disturbances, agitation, high blood pressure, convulsions. With psychosis, the likelihood of an exacerbation of the condition is high. Sulindac, getting into the human body, is transformed into indomethacin. This medicine has a slow, long-lasting effect.
Phenylacetic and propionic acids
The first one produces diclofenac sodium, the main component for Voltaren and Ortofen preparations. The substance relatively rarely provokes the appearance of ulceration in the gastrointestinal tract, more often the remedy is used to combat the inflammatory process and against rheumatism.
With the participation of propionic acid, the reactions of obtaining keto-, ibu-, pirprofen, naproxen, thiaprofenic acid proceed. The most pronounced activity in inflammatory foci is inherent in pirprofen, naproxen. For thiaprofen, a high selective activity was established, due to which an adverse reaction from the gastrointestinal tract, respiratory organs, and the reproductive system is less often observed. Ibuprofen is similar to diclofenac in many ways.
