What Are Nonsteroidal Anti-Inflammatory Drugs?

Nonsteroidal Antiinflammatory Drugs (NSAIDs) are a class of anti-inflammatory drugs that do not contain a steroid structure. NSAIDs have been synthesized since the first aspirin in 1898. There have been more than a hundred kinds of brands on the market in more than 100 years. Such drugs include aspirin, acetaminophen, indomethacin, naproxen, naproxen, diclofenac, ibuprofen, nimesulide, rofecoxib, and celecoxib. Anti-inflammatory, anti-rheumatic, analgesic, antipyretic and anti-coagulant effects are widely used in clinical practice for osteoarthritis, rheumatoid arthritis, various fevers and alleviation of various pain symptoms.

Introduction to non-steroidal anti-inflammatory drugs

NSAIDs are currently one of the most widely used drugs in the world. Approximately 30 million people worldwide use it every day. With the increase in the use of NSAIDs, the issue of the safe use of these drugs has also attracted increasing attention from clinicians, pharmacists, patients, society and governments. In particular, Merck Corporation announced in October 2004 that it would actively withdraw Manro (Rofecoxib) from the global market; the US Food and Drug Administration (FDA) recently identified NSAIDs as having potential cardiovascular and gastrointestinal bleeding risks and requested these drugs. Manufacturers have raised warnings in their instructions, which makes the safe use of NSAIDs a hot issue in the global medical community.

Non-steroidal anti-inflammatory pharmacological effects

NSAIDs have different chemical structures, but they all exert their antipyretic, analgesic, and anti-inflammatory effects by inhibiting the synthesis of prostaglandins.

Antipyretic effect of non-steroidal anti-inflammatory drugs

NSAIDs play an antipyretic effect by inhibiting the synthesis of central prostaglandins. These drugs can only reduce the body temperature of fever patients, but have no effect on normal body temperature. Antipyretics are only symptomatic treatments, and the body temperature will rise again after the in vivo medications are eliminated. Therefore, patients with fever should focus on the cause of the disease and only be used in high fever.

Analgesic effect of non-steroidal anti-inflammatory drugs

NSAIDs produce a moderate degree of analgesic action, with the analgesic site being mainly peripheral. It is not effective for severe pain caused by various traumas and visceral smooth muscle colic. It has better effect on chronic pain such as headache, joint muscle pain, toothache and so on. During tissue damage or inflammation, pain-producing substances are locally produced and released, while prostaglandin synthesis is increased. Prostaglandins increase the sensitivity of pain receptors to pain-causing substances and amplify inflammatory pain. At the same time, PGE1, PGE2 and PGF2 are pain-causing substances and cause pain. The analgesic mechanism of NSAIDs is: inhibit the synthesis of prostaglandins; inhibit the activity of lymphocytes and the differentiation of activated T lymphocytes, reduce the stimulation of afferent nerve endings; directly affect nociceptors and prevent the pain-causing substances Formation and release.

Anti- inflammatory effects of non-steroidal anti-inflammatory drugs

Most NSAIDs have anti-inflammatory effects. NSAIDs exert anti-inflammatory effects by inhibiting the synthesis of prostaglandins, inhibiting the aggregation of white blood cells, reducing the formation of bradykinin, and inhibiting the aggregation of platelets. It is definitely effective in controlling the symptoms of rheumatoid and rheumatoid arthritis.

Preventive effects of non-steroidal anti-inflammatory drugs on tumors

NSAIDs have inhibitory effects on tumor occurrence, development and metastasis, and have synergistic effects with other anti-tumor drugs.

Mechanism: Inhibits the production of PGS and induces apoptosis of tumor cells. COX-1 RNA in colon tumor tissues induced by oxazomethane in rats is of equivalent intensity between tumors and normal tissues, and COX-2 RNA in early tumors is significantly higher than normal mucosa. In ulcerative colitis with early tumors (not visible to the naked eye), increased COX-2 expression was detected at the tumor site by in situ hybridization and immunohistochemistry. These studies suggest that COX-2 may be a target for the early diagnosis and prevention of colorectal cancer.

From in vitro to in vivo animal experiments to human epidemiological population data, it has been proven that COX inhibitors and selective COX-2 inhibitors with a small response to the digestive system prevent at least one type of colon tumor and rectal cancer. valuable.

Non-steroidal anti-inflammatory drug adverse reactions

The pharmacological action mechanism of NSAIDs is mainly through the inhibition of cyclooxygenase, reducing the production of inflammatory mediator prostaglandin, and producing anti-inflammatory, analgesic, and antipyretic effects. Like any other drug, NSAIDs, while exerting a therapeutic effect, will also produce some adverse reactions that are not related to the purpose of the drug, that is, adverse drug reactions. The adverse reactions of NSAIDs are mainly manifested in the following aspects.

NSAID gastrointestinal tract

There may be symptoms of indigestion such as upper abdominal discomfort, pain, nausea, vomiting, fullness, belching, and loss of appetite. About 10% to 25% of patients with long-term oral non-steroidal anti-inflammatory drugs develop peptic ulcers, and less than 1% of them have serious complications such as bleeding or perforation.

Non-steroidal anti-inflammatory liver

At the treatment dose, 10% of the patients can cause mild liver damage, but the incidence of alanine aminotransferase is significantly lower than 2%.

Non-steroidal anti-inflammatory drugs nervous system

May have headache, dizziness, tinnitus, deafness, amblyopia, drowsiness, insomnia, paresthesia, numbness and so on. Some symptoms are not common, such as hyperactivity, excitement, hallucinations, tremors, etc., and the incidence is generally less than 5%.

Non-steroidal anti-inflammatory drugs urinary system

Can cause urinary protein, cast, red and white blood cells can appear in the urine, and severe cases can cause interstitial nephritis. In a multi-center clinical study, patients with long-term oral NSAIDs were 2.1 times more likely to have kidney disease than the general population.

Non-steroidal anti-inflammatory drugs blood system

Some NSAIDs can cause granulocytopenia, aplastic anemia, and coagulopathy.

Nonsteroidal anti-inflammatory drug allergy

People with specific constitutions may develop allergic reactions such as rash, angioedema, and asthma.

Non-steroidal anti-inflammatory drugs cardiovascular system

Studies have found that NSAIDs can significantly interfere with blood pressure and increase mean arterial pressure. It has also been reported that after 18 months of taking rofecoxib, patients have an increased relative risk of cardiovascular events such as heart attacks and strokes.

Non-steroidal anti-inflammatory drugs during pregnancy

NSAIDs are considered to be a potential cause of acute fatty liver during pregnancy; aspirin taken by pregnant women can cause prenatal, postpartum and postpartum bleeding; indomethacin may cause some fetal short limb deformities and penile hypoplasia.

Although NSAIDs can cause many of the above-mentioned adverse reactions, the majority of patients have mild side-effects when taking this class of drugs for a short period of time, can tolerate them, and the adverse reactions will disappear after stopping the drug, and will not play on the drugs. The effect has an impact. Many NSAIDs are now available as over-the-counter (OTC) drugs, and patients can purchase OTC varieties directly from pharmacies without the need for a physician's prescription. Therefore, it is necessary to remind patients to pay attention to the safe use of NSAIDs and understand the safe use of NSAIDs.

Nonsteroidal anti-inflammatory medicinal drugs

In the actual use of NSAIDs, adverse drug reactions should be prevented from the following aspects.

(1) Try to avoid unnecessary large-dose, long-term application of NSAIDs. When long-term medication is needed, it should be used under the guidance of a physician or pharmacist. During the medication, pay attention to monitoring the possible damage to various systems, organs and tissues. When using OTC varieties, you should read the drug instructions carefully, and strictly follow the dosage and treatment course of the drug instructions.

(2) NSAIDs should be forbidden or taken with caution: those with active peptic ulcers and recent gastrointestinal bleeding, those allergic to aspirin or other NSAIDs, those with liver dysfunction, those with renal dysfunction, severe hypertension and congestion Patients with heart failure, hypocytopenia, pregnant and lactating women.

(3) If a suspicious adverse reaction occurs during the medication, the drug should be immediately discontinued. After consulting the physician or pharmacist, decide whether to continue the medication and give appropriate treatment to the adverse reaction if necessary.

(4) It is not advisable to drink alcohol during the medication, otherwise it will aggravate the gastrointestinal mucosa. It should not be used in combination with anticoagulants, such as warfarin, as it may increase the risk of bleeding.

(5) It is not advisable to use two or more NSAIDs at the same time, because it will cause the superposition of adverse reactions. Pay special attention to more than one drug, drugs with the same chemical composition may appear under different trade names to avoid repeated medication. For example, acetaminophen is also known as paracetamol, and its trade names are Baifuning, Tylenol, Bristol, etc .; Diclofenac is also known as Diclofenac, and its trade names are Yingtaiqing, Futalin, Daifen, and Obe.

(6) We cannot blindly believe that there are no hidden dangers in new drugs, imported drugs and high-priced varieties of NSAIDs. New varieties of NSAIDs are constantly on the market. New varieties are often imported drugs and expensive, but there are also some potential dangers. Merck's announcement in October 2004 of its active withdrawal from global markets of rovoloxib (rofecoxib) is a good example.

(7) Facing the hot issue of safe use of NSAIDs, patients need not worry too much about NSAIDs increasing the risk of cardiovascular adverse events and gastrointestinal bleeding. China's NSAIDs case reports and literature resources related to the digestive system, cardiovascular system, blood system, central nervous system and other aspects of adverse reactions, of which cardiovascular incidents and gastrointestinal bleeding accounted for a large proportion small. Therefore, not all patients who have used NSAIDs are at risk of cardiovascular events and gastrointestinal bleeding.

In short, only when doctors, pharmacists, patients, and the community pay attention to the issue of safe medication, adhere to rational medication, and try to avoid and reduce the harm of adverse drug reactions, can truly build a barrier to safe medication.