Rheumatic inflammation of soft periarticular tissues

Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most popular pharmaceutical products. They are prescribed during the treatment of a number of diseases and conditions, often in entire courses. Even with clear instructions from the attending physician, many compatriots have doubts and look for information about drugs on the Internet. And then they come to the pharmacy and ask the pharmacist questions, hoping to justify their guesses or dispel doubts. In this situation, the head manager needs, on the one hand, to help the pharmacy visitor, and on the other hand, not to take on the role of a doctor. It is in this vein that we will cover the topic of topical NSAIDs today - in the form of competent answers to customer questions.

What does “when used correctly” mean? Anointed, and that’s it.

It is advisable to rub in topical forms of NSAIDs for a while rather than just apply them. The analgesic and anti-inflammatory effect of the ointment will be much higher if you do not just “anoint” it, but actively rub the product into the skin over the sore spot for some time. In the course of relevant studies, it was found that even 45 seconds of rubbing diclofenac diethylamine gel five times increased the transdermal delivery of the drug compared to simple application to the skin. And you need to remember that pain-relieving ointments based on NSAIDs act on areas of pain located immediately under the skin. If we talk about joints, then these are the knees, elbows and small joints of the hands. The local form most likely “will not reach the hip joint.” It should be rubbed “around the circumference” of the limb, for example, not only into the dorsum, but also into the palmar surface of the interphalangeal joint [6, 7].

How to treat joint pain.

July 7, 2022
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Content
  • Why do my joints hurt?
  • The best ointments and gels for joint pain
  • Fastum gel
  • Viprosal
  • Finalgon
  • Voltaren Emulgel
  • Dolgit
  • Capsicam

Often joint pain (arthralgia) bothers people who do not have joint diseases. Pain can occur after excessive physical activity, during pregnancy, and in children and adolescents, “growing pains” may occur. In these cases, you don't have to worry. If the joints hurt due to some disease, treatment is necessary. Only a doctor can determine the cause of joint pain and select the correct therapy. So don't let things get worse.

Which topical NSAID is best?

Everything is individual. If the analgesic effect of oral and injectable forms of NSAIDs can be more or less ranked, then an objective comparative assessment of topical drugs is very difficult. The reason for this is that, along with the actual active substance, the intensity of rubbing, excipients (for example, dimethyl sulfoxide) and the placebo effect play a significant role. Most studies on the effectiveness of topical NSAIDs have focused on diclofenac and ketoprofen. The increased attention to them is due to the fact that diclofenac is the only NSAID whose topical forms are approved by the American Food and Drug Administration (FDA), and ketoprofen, accordingly, is approved in most other countries of the world. Reliable data comparing these two drugs with each other have not yet been published. No one questions the effectiveness of other non-steroidal anti-inflammatory drugs for external use (ibuprofen, phenylbutazone, piroxicam, nimesulide, etc.); each of them was the subject of several clinical trials at one time, but the geography of their use is much more modest and is often limited to a few developing countries [2, 8].

Do excipients in the local form of NSAIDs matter?

Yes, they improve skin permeability and perhaps enhance the therapeutic effect in a certain way. In separate studies, for example, topical formulations of diclofenac with dimethyl sulfoxide (DMSO) and diclofenac diethylamine 1.16% have been shown to penetrate the skin faster than “regular” diclofenac sodium gels. In addition, DMSO itself may have a slight anti-inflammatory effect. There is no solid evidence of an increase in the analgesic effect due to the listed supplements, but their use at least helps to overcome the individual characteristics of the skin [7, 9–11].

Viprosal

Many people suffering from joint diseases note that with prolonged use of one or another product, addiction occurs - after some time, the ointment or gel simply stops relieving pain, and you have to buy more and more new drugs. If this happens to you, try Viprosal for joints. This is an ointment made entirely of natural ingredients that will give the body a break from NSAIDs. Contains: viper venom, pine resin, camphor and salicylic acid. “Viprosal” has a good irritant effect, which stimulates tissue nutrition - and this is very important when the cartilage is worn out and depleted (with degenerative joint diseases). Viprosal relieves inflammation and reduces pain without the need to take medications.

Viprosal
Grindeks, Latvia

Locally irritating, analgesic, used topically for joint and muscle pain.
Causes irritation of sensitive receptors of the skin and subcutaneous tissue, dilates blood vessels, improves tissue trophism. from 205

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Can I take NSAID tablets and use the topical form at the same time?

This is not directly prohibited by the instructions for use, but it is not recommended, and, apparently, does not make sense. According to the only credible study on this topic, there was no significant increase in the analgesic effect when combining local and systemic forms of NSAIDs. At the same time, this use of drugs slightly increased the frequency of rectal bleeding. In clinical trials, oral administration of diclofenac and ibuprofen at doses 2 and 3 times higher than recommended also did not lead to increased pain relief. The effect of a combination of tablets and a topical form of NSAIDs will most likely not be pronounced. At the same time, the likelihood of unwanted reactions slightly increases. Therefore, this combination is not recommended. Usually, if a local remedy does not help, the doctor cancels it and transfers the patient to oral administration [12, 13].

Selected representatives of topical GCS

The list of drugs used in this group is quite large, so we will note the features of only those drugs that have over-the-counter forms.

Hydrocortisone

- a weak synthetic GCS, appropriate for use in acute and subacute skin processes without weeping. To improve penetration, it is recommended to apply with light massaging movements. When positive dynamics appear, the frequency of use is reduced from 1–3 times a day to 2–3 times a week. Approved for use in children over 2 years of age in courses of no longer than 7 days in minimally effective doses [6].

Alclomethasone

- GCS from weak to moderate degree of activity. Absorption through the skin depends on the integrity of the skin and the type of dosage form. In healthy people, 3% alklometasone is absorbed within 8 hours. Can be used on delicate and sensitive areas of the body - face, neck, chest, genital area. Recommended for acute and subacute inflammatory diseases, including those accompanied by weeping. Can be used during pregnancy (under medical supervision), breastfeeding, and in children over 6 months. The maximum duration of treatment in children is 3 weeks.

Betamethasone dipropionate

- strong corticosteroids, when used on the face, the course of treatment should not exceed 5 days to avoid the development of rosacea, perioral dermatitis or acne. Can be used in children from 1 year of age according to strict indications and under medical supervision.

Methylprednisolone aceponate

— GCS of medium strength, can be used in children from 4 months of age in courses of up to 4 weeks. It is available in the form of an emulsion, cream, ointment and fatty ointment, which allows you to select the drug individually, depending on the lesion.

Sources

  1. Adaskevich V. P. Local corticosteroids in the treatment of skin diseases // Bulletin of Pharmacy, 2006. No. 3. P. 33.
  2. Bardal, Stan K. Applied pharmacology / Elsevier Saunders, 2011.
  3. Clinical guidelines “Atopic dermatitis in children.” Union of Pediatricians of Russia. 2016. 60 p.
  4. Kondratieva T.S., Ivanova L.A., Zelikson Yu.I. Technology of dosage forms: Textbook in 2 volumes. Volume 1. Medicine. Moscow, 1991. 496 p.
  5. Kalyuzhnaya L. D. Should systemic side effects of topical corticosteroids be taken into account? //Ukrainian Journal of Dermatology, Venereology, Cosmetology, 2010. Vol. 1. No. 36. P. 28-31.
  6. According to GRLS data as of September 25, 2019.

Is it possible to use topical NSAIDs for stomach erosions or ulcers?

According to the instructions, it can be done “with caution.” The concentration of the active substance in the blood plasma after the use of topical NSAIDs is less than 10% of that achieved by oral administration. The incidence of adverse reactions from the gastrointestinal tract when using local forms of NSAIDs does not differ from that when rubbing placebo and is significantly lower than when using systemic agents. However, just in case, these drugs are not recommended to be applied to the skin during gastrointestinal bleeding and exacerbation of gastric or duodenal ulcers [5, 14].

How many times a day and for how long can you apply such drugs?

Typically three to four times a day for two weeks. Topical NSAIDs act quite quickly - the effect occurs within an hour - and help control acute somatic pain of moderate intensity. They cope worse with chronic pain. If there is no effect within two weeks of proper use, you should consult a doctor. There is a chance that he will recommend switching to oral forms or another group of drugs.

Sources

  1. Derry S, Conaghan P, Da Silva JA, et al. Topical NSAIDs for chronic musculoskeletal pain in adults. Cochrane Database Syst Rev. 2016; 4: CD007400. https://www.cochranelibrary.com/cdsr/doi/10.1002/14651858.CD007400.pub3/full
  2. Derry S, Wiffen PJ, Kalso EA, et al. Topical analgesics for acute and chronic pain in adults – an overview of Cochrane Reviews. Cochrane Database Syst Rev. 2017; 5: CD008609. https://www.cochranelibrary.com/cdsr/doi/10.1002/14651858.CD008609.pub2/full
  3. Klinge SA, Sawyer GA. Effectiveness and safety of topical versus oral nonsteroidal anti-inflammatory drugs: a comprehensive review. Phys Sportsmed. May 2013; 41(2): 64–74. https://www.ncbi.nlm.nih.gov/pubmed/23703519
  4. Kloppenburg M, Kroon FP, Blanco FJ, et al. 2022 update of the EULAR recommendations for the management of hand osteoarthritis Annals of the Rheumatic Diseases 2019; 78: 16–24. https://ard.bmj.com/content/78/1/16
  5. Honvo G, Leclercq V, Geerinck A, et al. Safety of Topical Non-steroidal Anti-Inflammatory Drugs in Osteoarthritis: Outcomes of a Systematic Review and Meta-Analysis. Drugs Aging. 2019; 36(Suppl 1): 45–64. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6509095/
  6. Hasler-Nguyen N, Fotopoulos G. Effect of rubbing on the in vitro skin permeation of diclofenac-diethylamine 1.16% gel. BMC Res Notes. 2012 Jun 21; 5: 321. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3424122/
  7. Hagen M, Baker M. Skin penetration and tissue permeation after topical administration of diclofenac. Curr Med Res Opin. 2022 Sep; 33(9):1623–1634. https://www.tandfonline.com/doi/full/10.1080/03007995.2017.1352497
  8. Rafanan BS Jr, Valdecañas BF, Lim BP, et al. Consensus recommendations for managing osteoarthritic pain with topical NSAIDs in Asia-Pacific. Pain Manag. 2018; 8 (2): 115–128. https://www.futuremedicine.com/doi/10.2217/pmt-2017-0047?url_ver=Z39.88-2003&rfr_id=ori:rid:…
  9. Pradal J, Vallet CM, Frappin G, Bariguian F, Lombardi MS. Importance of the formulation in the skin delivery of topical diclofenac: not all topical diclofenac formulations are the same. J Pain Res. 2019; 12: 1149–1154. https://www.dovepress.com/importance-of-the-formulation-in-the-skin-delivery-of-topical-diclofen-pee…
  10. Galer BS. A comparative subjective assessment study of PENNSAID® and Voltaren Gel®, two topical formulations of diclofenac sodium. Pain Pract. 2011; 11 (3): 252–60. https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1533-2500.2010.00420.x
  11. Tieppo Francio V, Davani S, Towery C, Brown TL. Oral Versus Topical Diclofenac Sodium in the Treatment of Osteoarthritis. J Pain Palliat Care Pharmacother. 2022 Jun; 31 (2): 113–120. https://www.tandfonline.com/doi/abs/10.1080/15360288.2017.1301616?journalCode=ippc20
  12. Simon LS, Grierson LM, Naseer Z, et al. Efficacy and safety of topical diclofenac containing dimethyl sulfoxide (DMSO) compared with those of topical placebo, DMSO vehicle and oral diclofenac for knee osteoarthritis. Pain. 2009; 143(3):238–45. https://insights.ovid.com/article/00006396-200906000-00016
  13. Van Amburgh J. Can Topical and Oral NSAIDs Be Combined for Pain Relief? Medscape. https://www.medscape.com/viewarticle/861740
  14. Roth SH. Nonsteroidal anti-inflammatory drug gastropathy: new avenues for safety. Clin Interv Aging. 2011; 6: 125–31. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3131982/
  15. Kowalski ML, Makowska JS, Blanca M, et al. Hypersensitivity to nonsteroidal anti-inflammatory drugs (NSAIDs) – classification, diagnosis and management: review of the EAACI/ENDA and GA2LEN/HANNA. Allergy 2011; 66:818–829. https://www.eaaci.org/attachments/668_Kowalski%20Hypersensitivity%20to%20nonsteroidal%20anti-inflamm…
  16. Rogers NV, Rowland K. An alternative to oral NSAIDs for acute musculoskeletal injuries. J Fam Pract. Mar 2011; 60 (3): 147–8. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3183960/
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