Wonderful first look!

*Only for medical professionals to read and reference, finally released, fast forward! Osteoarthritis (OA) is a degenerative disease, which is caused by many factors such as age, obesity, strain, trauma, joint congenital abnormalities, joint deformities and other factors.
.

This disease is more common in middle-aged and elderly people, and it is more common in weight-bearing joints and joints with a lot of activity (such as cervical spine, lumbar spine, knee joint, hip joint, etc.
).

Excessive weight bearing or use of these joints can promote the occurrence of degenerative changes.

The clinical manifestations are slow development of joint pain, tenderness, stiffness, joint swelling, restricted mobility and joint deformities.

It is estimated that nearly 400 million people will suffer from OA in 2030.

In recent years, the American College of Rheumatology (ACR), European Union Against Rheumatism (EULAR), American Academy of Orthopaedic Surgeons (AAOS), International Society for Osteoarthritis Research (OARSI), Chinese Academy of Rheumatology, and Joint Surgery Group of Chinese Orthopaedic Association They formulated or revised their respective OA diagnosis and treatment guidelines, which provided an important reference for the clinical diagnosis and treatment of OA.

The 2019 Chinese OA Guidelines make up for the deficiencies of other guidelines.
However, some of the guidelines have some problems, such as incomplete retrieval evidence, unclear investigation of clinical problems, lack of grading of the quality of evidence and the strength of recommendations, etc.

In response to this, the "Guidelines for the Diagnosis and Treatment of Osteoarthritis in China (2019 Edition)" (full text in English published in Annals of Translational Medicine) [1] can make up for the above shortcomings and provide Chinese clinicians with OA diagnosis and treatment.
The best decision-making tool.

This guideline addresses the 16 issues that clinicians are most concerned about, and makes recommendations based on the latest clinical evidence.
The editor has compiled them for your reference.Table 1 Recommendations of the "Guidelines for the Diagnosis and Treatment of Osteoarthritis in China".
Among them, the treatment of OA is a hot topic.
According to the location and extent of the disease in patients with OA, the internal and external combination should be used for individualized and stepwise drug treatment.

The current treatment of OA is divided into four ascending steps of basic treatment, drug treatment, restorative treatment and reconstruction treatment [2].

Among them, drug therapy mainly includes analgesics, intra-articular injection of drugs, slow-acting drugs to relieve symptoms, and proprietary Chinese medicines.

Figure 1 Schematic diagram of OA step-by-step treatment NSAIDs are the most commonly used drugs for OA patients to relieve pain and improve joint function.

Including topical drugs and systemic drugs.

In the "Guidelines for the Diagnosis and Treatment of Osteoarthritis in China", for patients with mild pain symptoms, topical NASIDs are recommended to reduce local pain in patients.

Not only that, many international societies (such as ACR, AAOS, OARSI, the National Institute of Health and Clinical Optimization (NICE) and EUIAR) have formulated guidelines for the diagnosis and treatment of OA.
All recommend the use of topical NSAIDs for the treatment of hand and knee OA.
Among them, topical NSAIDs It can be used as a local short-term treatment or as an initial treatment before oral NSAIDs.

So, what are the benefits of topical NSAIDs? How does it work? Topical NSAIDs have fast onset and fewer adverse reactions! 1.
Although topical NSAIDs mainly act locally and do not have the systemic efficacy of oral NSAIDs and cannot be a substitute for them, topical NSAIDs can be used as a local potentiator for oral NSAIDs.
Compared with oral routes, topical topical preparations are directly used.
In the skin of the diseased area, it penetrates through the skin to reach the painful tissue and exerts an analgesic effect.
It has the advantages of fast onset, high local concentration, and low system exposure.
It is more suitable for the treatment of acute and chronic pain in the musculoskeletal system.

Among all topical analgesics, topical NSAIDs are the most effective.

2.
The adverse drug reactions of NSAIDs are mainly gastrointestinal reactions, liver and kidney damage and cardiovascular adverse events. According to statistics from the US Food and Drug Administration (FDA), the incidence of gastrointestinal ulcers, bleeding and perforation in patients taking NSAIDs for 3 months is 1%~2%, and the incidence of patients taking NSAIDs for 1 year increases to 2%~ 5%.

The topical NSAIDs can reduce the risk of adverse reactions such as the gastrointestinal tract.

Although topical NSAIDs occasionally have adverse reactions such as local skin irritation, most of them can be relieved after stopping the drug.

How do topical NSAIDs work? NSAIDs for external use must penetrate the skin and penetrate to the diseased site to exert their pharmacological effects.

Different formulations of topical NSAIDs have different skin penetration characteristics.

When penetrating each layer of the skin, the active agent needs to have an ideal permeability coefficient (logarithm P≤2), which is also the most reliable parameter for determining transdermal administration, that is, topical NSAIDs must be between lipophilicity and hydrophilicity Achieve balance, its skin penetration will be better.

In topical NSAIDs, the logarithm P of ketoprofen gel is 0.
97, and the proportion of active substances released after transdermal diffusion can reach 22%; followed by diclofenac (11%) and niflufenamic acid (4%) And piroxicam.

In addition to the permeability coefficient, the transdermal effect of topical NSAIDs is also related to the dosage form-related factors such as water content and whether it contributes to the dissolution and migration of active drugs.

The transdermal properties of topical NSAIDs are closely related to their local anti-inflammatory activity.

An animal experiment comparing the anti-inflammatory effects of different topical NSAIDs showed that the ability of ketoprofen gel and diclofenac gel to inhibit the synthesis of prostaglandin E2 (PGE2) and tissue swelling was significantly stronger than that of placebo, while piroxicam gel and diclofenac gel were significantly stronger than placebo.
Flufenamic acid gel and ibuprofen gel are equivalent to placebo [3-6].

Summary OA is a common disease in middle-aged and elderly people, which seriously affects the quality of life of patients.

NSAIDs are the most commonly used drugs for OA patients to relieve pain and improve joint function.

While maintaining the same efficacy as oral NSAIDs, the risk of systemic adverse reactions of topical NSAIDs is low, and local skin reactions are mostly mild or transient.

Therefore, topical NSAIDs can be used as one of the best choices for those who cannot tolerate oral NSAIDs or have oral NSAIDs contraindications.

The release of the "Guidelines for the Diagnosis and Treatment of Osteoarthritis in China" may become an excellent clinical decision-making tool for clinicians, which will greatly help improve the function and quality of life of patients with OA.

References: [1]Zhang Z, Huang C, Jiang Q, et al.
Guidelines for the diagnosis and treatment of osteoarthritis in China (2019 edition).
Ann Transl Med.
2020 Oct;8(19):1213.
[2] Joint Surgery Group, Orthopedic Branch of Chinese Medical Association.
Guidelines for the diagnosis and treatment of osteoarthritis (2018 edition) [J].
Chinese Journal of Orthopaedics, 2018, 38(12): 705-715.
[3] Beetge E, du Plessis J, Müller DG, et al.
The influence of the physicochemical characteristics and pharmacokinetic properties of selected NSAID's on their transdermal absorption[J].
Int J Pharm, 2000, 193(2):261-264 .
[4] Montastier P.
In vitro diffusion kinetics of four NSAIDs by percutaneous route[J].
Med du Sport, 1994, 68:40-42.
[5] Mehta R.
Topical and transdermal drug delivery: What a pharmacist needs to know[EB/OL].
inetce.
com/articles/pdf/ 221-146-04-054-H01.
pdf.
[6] Komatsu T, Sakurada T.
Comparison of the efficacy and skin permeability of topical NSAID preparations used in Europe [J].
Eur J Pharm Sci,