Thus defined to distinguish them from anti-inflammatories belonging to the group of corticosteroids, including cortisone and its analogues, non-steroidal anti-inflammatory drugs, abbreviated NSAIDs, are a large and diversified class of compounds united by the more or less accentuated ability to reduce inflammation and pain. To these properties, is also added the ability to lower body temperature in case of fever (antipyretic action).
The most commonly used NSAIDs are acetylsalicylic acid (ASA) and ibuprofen (usually used mainly for analgesic and antipyretic purposes), naproxen, ketoprofen and diclofenac (more markedly anti-inflammatory and painkillers, ideal against joint disorders, intense headaches, toothache and neuralgia).
Almost all of them are available both in the form of OTC preparations (without prescription), freely purchased without a prescription, and as prescription drugs at higher doses, to be used in case a particularly marked anti-inflammatory action is required.
Since inflammation is a fundamental physiological mechanism of the organism that can develop both in a precise point of the body (in response to accidental trauma or more or less evident and significant lesions affecting organs and tissues) and at a systemic level (usually, due to inflammatory diseases on an immune basis), NSAIDs find an extremely extensive and diversified use in the treatment of many common disorders.
To make the most of its properties, over the years, multiple formulations have been developed for each of the different active ingredients that allow optimal use in relation to the health problem that must be managed.
Mechanism of action of NSAIDs
Despite being different from each other in chemical structure, all NSAIDs share the same mechanism of action, consisting of the inhibition of a group of enzymes called cyclooxygenase (COX) type 1 and 2, present in many tissues of the body.
The blockade of COX type 2 (COX-2) prevents the transformation of arachidonic acid into prostaglandins and prostacyclins, substances naturally produced by the body in case of trauma or acute or chronic tissue damage and on which the initiation and maintenance of the inflammatory process depends.
Inhibition of COX type 1 (COX-1), on the other hand, is less beneficial because this enzyme mediates the production of thromboxanes and protective prostaglandins, which protect the balance of the stomach mucosa, kidneys and platelet aggregation.
The desired therapeutic effects of NSAIDs depend on the inhibition of COX-2, while the possible side effects depend on the inhibition of COX-1, which can differ greatly in type and intensity in relation to the dosage taken, the individual sensitivity of the person using them, whether NSAIDs are used alone or together with other drugs / substances and whether it is applied topically or taken by mouth.
The antipyretic effect of NSAIDs is also established through a mechanism in which prostaglandins are involved, but in this case the action of the drug is carried out at the level of the central nervous system and, more precisely, in the brain center that regulates body temperature. When the concentration of prostaglandins in the blood increases, the endogenous thermostat is reset to a higher level, allowing the body temperature to rise above the normal threshold (37.0-37.5°C). By blocking the production of prostaglandins, NSAIDs restore (indirectly) the normal threshold of the internal thermostat which, by recording a body temperature higher than the maximum expected, triggers a whole series of compensation mechanisms that help to disperse heat, reducing fever (vasodilation, sweating, etc.).
Therapeutic effects of NSAIDs
From a qualitative point of view, all NSAIDs are substantially similar to each other both in terms of therapeutic effects and side effects, while in relation to some molecular specificities and potency, the extent of anti-inflammatory/analgesic action and the risk of developing some side effects may change.
The main therapeutic effects of NSAIDs are essentially three:
| Therapeutic effect | Benefits |
|---|---|
| Anti-inflammatory | Reduction of vasodilation, redness, burning and edema in tissues and joints |
| Analgesic | Alleviation of pain, especially that of origin inflammatory (trauma, osteoarthritis, neuralgia, menstrual pain, etc.) |
| Antipyretic | Reduction of fever (except that associated with bacterial infections, against which it is necessary to also use antibiotics) |
Effects
Accanto ai sicuri benefici della loro assunzione in casi di necessità, i FANS possono comportare alcuni effetti collaterali. I più comuni sono quelli a carico dell’apparato gastrointestinale e comprendono principalmente dolore e/o bruciore a livello dello stomaco o nausea.
Nelle persone più sensibili, negli anziani, nei soggetti predisposti o che già presentano disturbi gastroenterici e in chi è in terapia con farmaci anticoagulanti, l’assunzione di FANS può favorire lo sviluppo di ulcera gastrica o intestinale, con possibile sanguinamento. In genere, però, anche in questi casi, effetti collaterali di una certa importanza non riguardano chi assume FANS a dosaggio medio-basso, in modo occasionale, per uno o pochi giorni, ma soltanto chi deve farne un uso protratto e/o a dosaggi medio-alti per il trattamento di condizioni infiammatorie severe o croniche.
In the vast majority of cases, for the prevention of gastrointestinal discomfort in adults without specific disorders, it is sufficient to take traditional NSAIDs on a full stomach (just a light and non-acid snack, such as 2-3 biscuits or a piece of bread) and do not exceed the dosages and treatment times indicated on the package or prescribed by the doctor (generally, up to 3-4 days of intake there is no significant risk).
More generally, following a healthy diet, based on fresh and nutritious foods, but light and digestible, is certainly advisable in order to minimize the most common gastrointestinal discomfort associated with the use of NSAIDs, as well as to put the body in the best conditions to deal with any disease.
Other possible side effects of NSAIDs include:
– skin reactions, such as erythema and urticaria (on an allergic basis), in predisposed subjects;
– impairment of varying degrees of renal and/or hepatic function (linked to specific toxicity to these organs), especially in the elderly, in neonates and in those who already present disorders at these levels.
Many NSAIDs taken systemically are associated with a slight increase in cardiovascular risk, which varies depending on the specific active ingredient used and the dosage. This drawback, which has emerged only in recent years from extensive post-marketing use assessments, mainly concerns those who have to take NSAIDs for long periods of time, while it can be considered negligible for occasional treatments of a few days (as NSAID therapies should always ideally be).
A further cutaneous side effect of NSAIDs, almost certain if you are exposed to the sun during their use or in the 2 days immediately following, concerns the development of erythema and burns, made much more likely by the photosensitizing effect of all the principles of this class, both when they are applied locally on the skin and when they are taken systemically. In order not to have problems, especially in summer, it is sufficient to avoid exposure to the sun for a few days, wear fairly opaque clothing and apply sunscreens with a high protection index (SPF >30).
What are NSAIDs and how to use them
By virtue of their mechanism of action and their therapeutic effects, the range of disorders that can be alleviated by NSAIDs is extremely wide and diverse. They range from toothache to menstrual pain, from low back pain to headache, from fever to osteoarthritis flare-ups, from post-operative pain to rheumatoid arthritis, up to common sprains.
In all cases, it should be remembered that the effect of NSAIDs is purely symptomatic, which means that the drug can temporarily reduce the malaise associated with a pathology, but does not remove its causes or accelerate healing, which must occur spontaneously (thanks to the intervention of the immune system and / or the natural repair processes of the organism) or with the support of other targeted treatments, used in combination.
In relation to the indication of use, the localization and extent of inflammation or pain, from time to time it may be more useful and practical to opt for a topical or systemic formulation. In the first case, NSAIDs can be used in the form of gel or cream, to be gently massaged on the affected area 2-4 times a day (provided that the skin is intact and there are no abrasions or wounds), or as a slow-release patch, to be applied with a slight pressure and left in place for several hours.
These formulations are particularly suitable for the treatment of inflammatory pain at joint and skeletal muscle level, both acute (such as that resulting from trauma, bruises, sprains, muscle contractures, etc.) and chronic (low back pain, osteoarthritis of the knee or shoulder, tendinopathies, etc.).
To relieve sore throat, very practical, welcome and effective topical formulations are those that see NSAIDs inserted in sprays or candies. An important warning in this case is not to be misled by the apparently “light” formulation: even if the spray or candy can give the idea of a “mild” treatment, in reality, it is in effect drugs to be used with the usual caution, respecting the indications and dosages reported on the packages or prescribed by the doctor.
Compared to formulations to be taken by mouth, topical preparations have the advantage of concentrating their action directly at the point where it is needed, quickly and not mediated by intestinal absorption, and not causing systemic side effects, since the share of drug that reaches the general bloodstream is negligible.
On the other hand, it should be noted that, if used with criterion and only when they are actually necessary, even NSAIDs taken systemically are safe and valuable drugs to alleviate many mild-moderate to severe pain/inflammatory syndromes. In this case, you can take them in the form of tablets to be swallowed with a little water or chewed, as tablets or effervescent granules to be dissolved in water or mouth (depending on the preparations), or as suppositories.
There are also systemic formulations of NSAIDs with intravenous administration, whose use is however reserved for the hospital environment and, in particular, for the management of peri-operative pain, alone or in association with opioid analgesics.
Contraindications
The active ingredients NSAIDs currently available on the world market are about fifty and are classified into various groups according to their chemical structure.
Depending on the specific class to which they belong, NSAIDs may have specific contraindications, but in general not having to take NSAIDs or to do so with extreme caution and only under medical supervision are:
- children under 12 years old;
- pregnant women;
- people on anticoagulant therapy and / or suffering from cardiovascular diseases or coagulation disorders of various kinds;
- frail elderly people suffering from several pathologies at the same time;
- people with gastrointestinal hypersensitivity or disorders such as gastritis, gastroesophageal reflux, gastric or duodenal ulcer, chronic inflammatory bowel diseases (Crohn’s disease, irritable bowel syndrome, etc.);
- people with a history of asthma or allergies (especially to acetylsalicylic acid).
For those who cannot take conventional NSAIDs, in relation to the present problem and the therapeutic objective, the general practitioner may indicate alternative pharmacological solutions.
For example, to limit the discomfort affecting the gastrointestinal tract, you can opt for a class of anti-inflammatories that selectively inhibits COX-2, responsible for inflammation, but not COX-1, protective of the gastric mucosa (even for these drugs, however, cautious use is recommended due to possible negative effects on the cardiovascular level). Alternatively, the doctor may prescribe a steroidal (cortisone) active ingredient, after making a careful balance between the clinical benefits and the numerous systemic side effects of this class of drugs.
When the goal is exclusively to treat pain, analgesics of different types can be used, such as weak and strong opioids, while in the presence of muscle contracture pain, muscle relaxant drugs can be used. A further effective, safe and harmless approach to relieve pain and contractures not associated with inflammation is heat, which can be applied with common compresses or with more practical self-heating patches, which can be purchased in pharmacies without a prescription, to be left on the painful area for several hours.
Joycelyn Elders is the author and creator of EmpowerEssence, a health and wellness blog. Elders is a respected public health advocate and pediatrician dedicated to promoting general health and well-being.
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