In pharmacology, analgesics are usually divided into opioid and non-opioid. Non-narcotic (non-opioid) substances are substances that weaken the pain syndrome without exerting 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 do not inhibit 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 is characterized by a relatively small effect of the weakening of pain in comparison with powerful drugs. If the syndrome is due to visceral disorders, trauma, such drugs are practically ineffective.
The described category of drugs is characterized not only by an analgesic effect, but also by anti-inflammatory. In addition, non-opioid analgesics are fever-reducing drugs. When using drugs in a therapeutic dosage, platelet aggregation decreases. Substances affect immune competency at the cellular level.
Performance Nuances
Opioid and non-opioid analgesics have been studied 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 variant 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 thalamic centers. Through the use of drugs, the conduction of pain impulses to the brain centers receiving them slows down. This central action is quite different from that inherent in narcotic formulations. Non-narcotic substances do not correct the ability of the central nervous system to summarize impulses.
Salicylates
Based on the classification of non-opioid analgesics, salicylates are those 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 in the effectiveness of these agents the main effect 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 irritation reaction and inhibits the release of proteases.
Salicylates are analgesics whose action is associated with protein reactions: active compounds prevent the denaturation of molecules. The drug has an anti-complementary effect. Inhibition of prostaglandin production causes a weakening of the activity of the inflammatory focus. At the same time, the algogenic effect of bradykinin is reduced. Non-opioid preparations of this group activate the connection between the adrenal gland and the pituitary gland, due to which the secretion of corticoids becomes more active.
Options: many funds
The list of non-opioid analgesics is quite wide, and the effectiveness of these drugs varies greatly. Perhaps the most famous can safely be called:
- Acetylsalicylic acid.
- Nise.
- Ibufen.
The difference in the strength of action is related to the different ability for existing drugs to seep into organic tissues. It is customary to distinguish several main groups of painkillers: simple antipyretics, antiflogistics, anti-inflammatory non-hormonal substances. The predominant percentage of the drugs presented in pharmacies is weak acids, which can easily penetrate the focus of the pathological process. In diseased tissues, the accumulation of pharmacologically active compounds occurs. Excretion for the majority is characteristic of urine, a smaller percentage - with bile. Mostly non-opioid central analgesics are eliminated as metabolic products of the liver. The substances obtained in such reactions do not have any effect.
Performance features: how does it all work?
Having adopted a central non-opioid analgesic, the patient soon feels a weakening of pain, the heat subsides. The desensitizing effect develops somewhat more slowly, the focus of inflammation is inhibited. To achieve a pronounced result in these two areas of activity, you will have to take quite large doses of the drug. This is associated with the likelihood of complications, side effects due to inhibition of prostaglandin production. Most often, drugs lead to the accumulation of sodium, the formation of ulcerated areas in the digestive tract, swelling and a tendency to bleeding. In addition, prolonged use of analgesics, especially in large doses, poisons the body. The chemicals contained in the drugs inhibit hematopoietic function, stimulate methemoglobinemia and other serious conditions. All currently known non-opioid analgesics of central action can cause an allergic reaction and a para-allergic response of the body.
The use of compounds during the period of bearing a child can cause inhibition, slowdown of labor, closure of the ductus arteriosus ahead of time. As a rule, in the first third of the term, such drugs are not prescribed at all because of the increased risk of a pathogenic effect, although animal experiments were carried out for the main percentage of medications, which proved the absence of teratogenic effects.
Science does not stand still
Studying opioid and non-opioid analgesics, scientists found that some substances can simultaneously inhibit the production of not only prostacyclin, PG, thromboxane, but also leukotrienes in the absence of a narcotic effect. This quality is called "inhibition of lipoxygenesis." Drugs that are characterized by both of these effects have begun to be produced relatively recently, but the direction looks extremely promising. They show a more pronounced anti-inflammatory effect, but the likelihood of para-allergic responses is reduced to a minimum. It is almost impossible to develop asthma, rash, runny nose, and the “aspirin triad.”
Not less promising are non-opioid analgesics that selectively affect the generation of various types of cyclooxygenases in the body. Already developed compounds that affect only thromboxane synthetase, synthetase PG F2-alpha, COX-2. The first type is Ibufen, based on ibutrin, the second is tiaprofen preparations. They are less likely to cause swelling, ulceration, or bronchial spasm due to a lack of GHG F2. Finally, the latter type is on sale by the Nise series operating on nimesulide.
NSAIDs
The list of analgesic drugs in this category includes names that are known to almost every person who has used pain medication at least once in their life. It includes:
- Voltaren.
- Diclofenac.
- Ketoprofen.
Such drugs are used if pain in the articular and muscle tissues is bothering, if the head hurts or neuralgia is detected. Substances are indicated for inflammatory processes in these areas of localization. As a means to relieve heat, NSAIDs can be used if the patient is in fever, the temperature rises above 39 degrees. Non-opioid analgesics of this group can be combined with vasodilators, antihistamines and antipsychotics - this helps to increase the antipyretic effect.
Caution is an important aspect of treatment.
Non-periodical analgesics - salicylates in the first place - can cause the development of Reye's syndrome, therefore, it is extremely necessary to prescribe such funds to children. The risk group for complication includes patients under the age of twelve with a viral etiology of the disease. Amidopyrine, indomethacin can cause convulsions. Paracetamol is considered an optimal substitute.
In addition to the described non-opioid analgesics, desensitizing qualities and inhibition of foci of inflammation are characteristic of derivatives of indole, phenylacetic, propionic, and phenamic 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 pyrazolone, although it can help in some cases, is rarely used due to the ability to inhibit hematopoietic function. In addition, the therapeutic effect inherent in this substance is rather narrow.
It is strictly forbidden to use any NSAIDs if an allergic reaction, a para-allergic response of the body are identified during the course or in the past was observed. You can not use these drugs with an ulcer in the stomach, impaired hematopoietic function of the body, as well as in the first third of the period of gestation.
Categories and types
To simplify the orientation, among the whole abundance of painkillers manufactured by the industry, it is customary to divide the funds not only into opioid and non-opioid ones, but also mixed drugs. Among non-narcotic drugs, antipyretics, combined formulations, and medications with a central and peripheral effect are distinguished. Antispasmodics are a group of drugs that contain several active substances. For example, "Digan" is produced with the inclusion in the formula of nimesulide, dicyclomine.
Combined analgesics sold under various trade names are manufactured on the following substances:
- "Solpadein" - paracetamol is combined with caffeine and codeine.
- “Benalgin” - caffeine is also added to metamizole, in addition, thiamine is present in the formula.
- "Paradic" is a combination of diclofenac, paracetamol.
- "Ibuklin" - a drug containing paracetamol, ibuprofen.
- Alka-prim is a medication based on acetylsalicylic acid, to which aminoacetic acid is added.
- "Alka-Seltzer" - a product containing citric, acetylsalicylic acid and sodium aqueous carbonate.
Features and differences
Non-opioid formulations do not affect opioid receptors and do not lead to the formation of dependence in the patient. They are not characterized by the presence of pharmacodynamic antagonists. Substances do not destabilize the work of the cough center and respiratory organs, do not lead to stool disturbance (constipation). All these properties distinguish them against the background of narcotic painkillers.
Non-opioid agents are prescribed for minor injuries - bruises and sprains. The drugs are effective in tearing ligaments and help alleviate the condition in case of soft tissue injury. You can use the compounds, if the pain is disturbing in the postoperative period, the syndrome is assessed 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-medication, that is, there is no one control over the use of the compounds. This makes the problem of complications and side effects especially urgent.
Salicylic acid and pyrazolone
Derivatives of these two substances are used to make a wide range of medicines. The most famous inhabitant is “Aspirin”, whose effectiveness is due to acetylsalicylic acid. In addition, methyl salicylate, salicylamide are common in the pharmaceutical industry. Medications based on sodium salicylate, acecelisine, are quite famous for their results. All means of this class are characterized by a rather low poisoning ability. Tests have shown: the lethal dosage of acetylsalicylic acid is 120 g. At the same time, there is a weak point: increased irritating activity, which is likely to form bleeding and ulcerated areas. These funds are not used for patients younger than twelve years of age.
On substances obtained from pyrazolone, the well-known “Analgin” was made, whose main component is metamezole. No less popular is Butadion, which works by incorporating phenylbutazone into the formula, and Antipyrine made on phenazone. The drug "Amidopyrine" has a good reputation, the main compound in which is aminophenazone.
A relatively narrow spectrum of therapeutic activity is inherent in all of the listed remedies, but at the same time, the quite inhibitory effect of the hematopoietic function is evaluated. This imposes restrictions on the duration of treatment: only short-term courses are permissible.
In stationary conditions, metamezole is often prescribed injectively, since the substance is highly soluble in water. It can be injected into muscle tissue, a vein or under the skin in case an urgent local anesthetic effect is needed, lowering the temperature. When choosing a medicine, you need to remember that in childhood, when using amidopyrine, the threshold for seizure readiness is adjusted, diuresis is reduced.
Paraaminophenol and Indole Acetic Acid
In chemical reactions involving paraaminophenol get paracetamol, phenacetin. Both of these drugs are ineffective against the active inflammatory focus, they do not have an antirheumatic effect and the ability to adjust blood viscosity. The use of compounds is associated with a minimal risk of ulcer formation, and for the kidneys substances are safe and do not inhibit the activity of the organ. The threshold for convulsive readiness remains virtually unchanged. At elevated temperatures, the main means of choice is precisely 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 inherent in the greatest strength. At the same time, the medication affects metabolic processes with brain mediators, and the concentration of GABA decreases. The use of analgesics is accompanied by sleep disturbances, agitation, high blood pressure, and convulsions. With psychosis, there is a high probability of an exacerbation of the condition. Sulindac, entering the human body, is transformed into indomethacin. This medication has a slow, lasting effect.
Phenylacetic acid and propionic acid
At the first, diclofenac sodium is made - the main component for the Voltaren, Ortofen preparations. The substance relatively rarely provokes the appearance of ulceration sites in the gastrointestinal tract, more often the drug is used to combat the inflammatory process and against rheumatism.
With the participation of propionic acid, reactions are taking place to obtain keto, ibu, pyrprofen, naproxen, thiaprofen acid. The most pronounced activity in inflammatory foci is inherent in pirprofen, naproxen. For tiaprofen, high selective activity was established, due to which an adverse reaction from the gastrointestinal tract, respiratory organs, and reproductive system is less often observed. Ibuprofen is very similar to diclofenac.