Topical NSAIDs (creams, gels)

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].

Vulvovaginitis: symptoms

Symptoms do not depend on the cause of the disease. Signs of an inflammatory process in the vulva and vaginal mucosa:

itching
burning
painful sensations in the area of the external genitalia, aggravated by walking
pain during intercourse
scanty purulent discharge from the vagina (with mechanical damage to the mucous membrane, it can be abundant)
increase in body temperature

Little girls may experience neurotic manifestations: sleep disturbance, increased excitability, tearfulness.

The disease can be acute or chronic. Symptoms of the forms of pathology differ only in the degree of severity.

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].

Causes of the disease

Inflammation of the vulva and vagina appears due to the influence of such factors:

violation of intimate hygiene rules, wearing underwear made of low-quality synthetics
frequent change of sexual partners without the use of barrier contraception
diseases of the metabolic system that can affect the vaginal microflora (diabetes mellitus, thyroid problems)
hormonal imbalances characteristic of puberty and menopause
taking antibacterial drugs (while taking antibiotics, a fungus like Candida is activated)
chemotherapy and radiation therapy
intoxication due to chronic infectious diseases
mechanical injuries of the vulva and vagina, especially regular ones

The presence of more than two risk factors increases the likelihood of the occurrence of pathology several times.

Allergic vaginitis is also possible. Pathology is diagnosed in the presence of helminths.

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].

What complications can there be?

Untreated vulvovaginitis can lead to serious consequences. In girls, the formation of dense adhesions of the labia minora is possible. Such a deformation will make sexual life difficult. In addition, this pathology is one of the factors that provoke cystitis.

The disease is especially dangerous during pregnancy. The expectant mother is at risk of spontaneous abortion, endometritis, or the birth of an infected baby.

Chronic vulvovaginitis leads to hardening of the mucous membranes. With this course, cracks and erosions occur more often, and prerequisites for the appearance of oncology appear.

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].

Vulvovaginitis

Vulvovaginitis is a disease of the female genital organs.
Inflammation may be of bacterial origin or be the result of mechanical irritation of the vulvar and vaginal mucosa. The natural structure of the female body allows us to protect the genitals from microorganisms from the external environment. The vaginal microflora of a healthy woman easily inhibits the growth of opportunistic bacteria that live on the mucous membranes. A decrease in immunity due to stress, intoxication or a viral disease can provoke a surge in the activity of pathogens, resulting in the development of acute vulvovaginitis.

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].

Contraindications

Before using antibacterial ointment, you need to know what contraindications there may be. Each drug has a different list, but there are some common points:

allergic reaction to one or more components of the drug;
oncological diseases;
lupus;
early age of children up to 12-24 months;
tissue death in the area of application;
during pregnancy and lactation. You should definitely consult your doctor.

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

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
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
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
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
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/
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/
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
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:…
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…
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
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
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
Van Amburgh J. Can Topical and Oral NSAIDs Be Combined for Pain Relief? Medscape. https://www.medscape.com/viewarticle/861740
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/
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…
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/

Mode of application

Methods of using antibacterial liniments depend on the specific drug and the inflammatory process. The process is described in the instructions.

Basically, ointments are applied as follows:

For burn and wound injuries, ointments are applied in a layer 1-2 mm thick. The procedure is repeated 1-3 times during the day. The course of treatment is 7 days;
for inflammation of the mucous membranes of the eye, liniment is placed under both eyelids no more than 3 times a day. The course ranges from 3 days to a week. In case of complications, it can be extended to 2 weeks;
for skin inflammations, liniments are used up to three times a day for no longer than one week;
for dermatological diseases, the drugs are used 2 times a day, for up to 7 days. Ointments are applied in a thin layer or pointwise.