Pennsaid vs voltaren: Voltaren Gel vs. Pennsaid for Arthritis: Differences & Side Effects

15.06.202311.06.2023 by alexxlab

Содержание

A comparative subjective assessment study of PENNSAID® and Voltaren Gel®, two topical formulations of diclofenac sodium

Randomized Controlled Trial

. 2011 May-Jun;11(3):252-60.

doi: 10.1111/j.1533-2500.2010.00420.x.

Epub 2010 Sep 20.

Bradley S Galer¹

Affiliations

Affiliation

¹ Nuvo Research Inc., West Chester, Pennsylvania 19382, USA. [email protected]

PMID:
20854305
DOI:
10.1111/j.1533-2500.2010.00420.x

Randomized Controlled Trial

Bradley S Galer.

Pain Pract.

2011 May-Jun.

. 2011 May-Jun;11(3):252-60.

doi: 10.1111/j.1533-2500.2010.00420.x.

Epub 2010 Sep 20.

Author

Bradley S Galer¹

Affiliation

¹ Nuvo Research Inc., West Chester, Pennsylvania 19382, USA. [email protected]

PMID:
20854305
DOI:
10.1111/j.1533-2500.2010.00420.x

Abstract

Osteoarthritis (OA) is a chronic degenerative joint disease that is debilitating for many individuals. While oral nonsteroidal anti-inflammatory drugs (NSAIDs) remain a common and effective treatment approach to managing OA, concerns over cardiovascular and gastrointestinal adverse events can potentially limit their use. Various formulations of topical NSAIDs have been shown to provide effective localized treatment with minimal adverse events. A patient perception study was conducted to evaluate patient preference between topical diclofenac sodium gel and that of diclofenac sodium topical solution with the penetration enhancer dimethyl sulfoxide (DMSO). Twenty-four healthy volunteers were randomized and asked to administer one dose of the topical products. Surveys were provided and assessed immediately after application, 5 minutes after application, and after the application had dried to gauge subjects’ overall experience with the topical preparation. Overall, each drug’s application was well tolerated and no adverse events were reported. Results of the patient preference survey demonstrated that topical diclofenac solution with DMSO had a number of characteristics that were rated significantly better than for diclofenac sodium gel. Mean subjective responses to topical diclofenac solution with DMSO were also more favorable for most items in the questionnaire, and more subjects preferred or highly preferred topical diclofenac solution with DMSO over diclofenac sodium gel.

Cited by

Topical Diclofenac Solution for Osteoarthritis of the Knee: An Updated Meta-Analysis of Randomized Controlled Trials.
Ling T, Li JJ, Xu RJ, Wang B, Ge WH.
Ling T, et al.
Biomed Res Int. 2020 Nov 24;2020:1758071. doi: 10.1155/2020/1758071. eCollection 2020.
Biomed Res Int. 2020.
PMID: 33299860
Free PMC article.
Topical NSAIDs for chronic musculoskeletal pain in adults.
Derry S, Conaghan P, Da Silva JA, Wiffen PJ, Moore RA.
Derry S, et al.
Cochrane Database Syst Rev. 2016 Apr 22;4(4):CD007400. doi: 10.1002/14651858.CD007400.pub3.
Cochrane Database Syst Rev. 2016.
PMID: 27103611
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Review.
Evaluation of diclofenac prodrugs for enhancing transdermal delivery.
Lobo S, Li H, Farhan N, Yan G.
Lobo S, et al.
Drug Dev Ind Pharm. 2014 Mar;40(3):425-32. doi: 10.3109/03639045.2013.767828. Epub 2013 Apr 23.
Drug Dev Ind Pharm. 2014.
PMID: 24517636
Free PMC article.
Topical NSAIDs for chronic musculoskeletal pain in adults.
Derry S, Moore RA, Rabbie R.
Derry S, et al.
Cochrane Database Syst Rev. 2012 Sep 12;9(9):CD007400. doi: 10.1002/14651858.CD007400.pub2.
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Publication types

MeSH terms

Substances

PENNSAID® 2% HOME | The PENNSAID (diclofenac sodium topical solution) 2% w/w official site

PENNSAID 2% is a topical NSAID designed to target your OA knee pain and deliver relief right where it hurts.

NSAID=nonsteroidal anti-inflammatory drug; OA=osteoarthritis.

Download our Brochure

INDICATIONS AND USAGE

What is PENNSAID

^® (diclofenac sodium topical solution) 2% w/w?

PENNSAID^® (diclofenac sodium topical solution) 2% w/w is a nonsteroidal anti-inflammatory drug (NSAID) applied to the skin, used for treating the pain of osteoarthritis of the knee(s).

IMPORTANT SAFETY INFORMATION

What is the most important information I should know about PENNSAID?

NSAIDs can cause an increased risk of a heart attack or stroke that can lead to death. This risk may occur early in treatment and may increase with longer use and with increasing doses.
NSAIDs can cause an increased risk of bleeding, ulcers, and tears (perforation) of the esophagus, stomach and intestines. These events can occur at any time during use, without warning symptoms and may cause death. Elderly patients and patients with a history of ulcer disease or stomach or intestine bleeding are at greater risk for getting an ulcer or bleeding.
You should take PENNSAID exactly as prescribed, at the lowest dose possible and for the shortest time needed.

PENNSAID can cause serious side effects. Stop taking PENNSAID and call your doctor or go to your emergency department right away if you get:

Difficulty breathing, swelling of the face or throat. These could be signs of a serious allergic reaction.
Chest pain, shortness of breath, weakness in one part or side of your body, or slurring of speech. These could be signs of a serious blood clotting event.
Upper stomach pain, upset stomach, black, tarry stools, or vomiting of blood. These could be signs of an esophagus, stomach, or intestinal ulcer, bleed, or tear. Note: if you are also taking low-dose aspirin, you are at increased risk for esophagus, stomach, or intestinal bleeding.
Nausea, more tired or weaker than usual, itching, yellowing of the skin or eyes, right upper abdomen tenderness, and “flu-like” symptoms. These could be signs of a liver problem.
Shortness of breath, unexplained weight gain, or swelling of the arms, legs, hands or feet. These could be signs of a serious heart problem.
Any type of rash. This could be a sign of a serious skin reaction.

These are not all of the possible side effects of PENNSAID. Please talk to your doctor if you experience any symptoms that bother you or that do not go away.

Who should not use PENNSAID?

DO NOT USE PENNSAID if you

are in the hospital for a certain heart surgery called coronary artery bypass graft surgery.
know you are allergic to diclofenac or any other ingredient of PENNSAID.
have experienced asthma, hives, or allergic-type reactions after taking aspirin or other NSAIDs. Serious allergic reactions to NSAIDs, including death, have been reported in such patients.
are in the 30th week of pregnancy until delivery

How should I use PENNSAID?

PENNSAID is applied directly to the front, back, and sides of your knee(s). Avoid contact of PENNSAID with the eyes, nose, and mouth. If eye contact occurs, immediately wash out the eye with water and contact your health care provider if irritation persists for more than an hour. Avoid skin-to-skin contact between other people and the knee(s) to which PENNSAID was applied until the knee(s) is completely dry. DO NOT apply PENNSAID to open wounds, infections, or rashes. DO NOT shower for at least 30 minutes after applying PENNSAID or wear clothing over the PENNSAID treated knee(s) until the treated knee(s) is dry. DO wash and dry hands before and after use, protect your treated knee(s) from natural or artificial sunlight, and wait until the treated knee(s) is completely dry before applying sunscreen, insect repellant, lotion, moisturizer, cosmetics, or other topical medication.

What are the possible side effects of PENNSAID?

The most common side effects of PENNSAID are application site reactions, such as dryness, peeling, redness, itching, pain, skin hardening, rash, blisters, and scabbing. Other side effects are bladder infection, bruising, sinus congestion, nausea, upset stomach, stomach pain, gas, constipation, and diarrhea.

What other medications might interact with PENNSAID?

Avoid using PENNSAID while taking other NSAIDs unless your doctor says it is OK. NSAIDs may be present in over-the-counter medications for treatment of colds, fever, or insomnia; refer to the label of over-the-counter medications you are taking or ask your pharmacist. Do not use PENNSAID and low-dose aspirin until you talk to your health care provider. Tell your doctor about all of the medicines you take as some medicines can react with NSAIDs and cause serious side effects.

What should I tell my health care provider?

Before starting PENNSAID, tell your health care provider if you have a history of ulcer disease or esophagus, stomach, or intestine bleeding, liver or kidney problems, high blood pressure, asthma, or are pregnant, trying to become pregnant, or breast feeding. Taking NSAIDs, such as PENNSAID, at about 20 weeks of pregnancy or later may harm your unborn baby. If you need to use PENNSAID for more than 2 days when you are between 20 and 30 weeks of pregnancy, your healthcare provider may need to monitor the amount of fluid in your womb around your baby. You should not use PENNSAID after about 30 weeks of pregnancy. Also tell your doctor about all of the medicines you take, including prescription or over-the-counter medicines, vitamins, or herbal supplements. Do not start taking new medicines without talking to your health care provider first.

INDICATIONS AND USAGE

What is PENNSAID

^® (diclofenac sodium topical solution) 2% w/w?

PENNSAID^® (diclofenac sodium topical solution) 2% w/w is a nonsteroidal anti-inflammatory drug (NSAID) applied to the skin, used for treating the pain of osteoarthritis of the knee(s).

IMPORTANT SAFETY INFORMATION

What is the most important information I should know about PENNSAID?

NSAIDs can cause an increased risk of a heart attack or stroke that can lead to death. This risk may occur early in treatment and may increase with longer use and with increasing doses.
NSAIDs can cause an increased risk of bleeding, ulcers, and tears (perforation) of the esophagus, stomach and intestines. These events can occur at any time during use, without warning symptoms and may cause death. Elderly patients and patients with a history of ulcer disease or stomach or intestine bleeding are at greater risk for getting an ulcer or bleeding.
You should take PENNSAID exactly as prescribed, at the lowest dose possible and for the shortest time needed.

PENNSAID can cause serious side effects. Stop taking PENNSAID and call your doctor or go to your emergency department right away if you get:

Difficulty breathing, swelling of the face or throat. These could be signs of a serious allergic reaction.
Chest pain, shortness of breath, weakness in one part or side of your body, or slurring of speech. These could be signs of a serious blood clotting event.
Upper stomach pain, upset stomach, black, tarry stools, or vomiting of blood. These could be signs of an esophagus, stomach, or intestinal ulcer, bleed, or tear. Note: if you are also taking low-dose aspirin, you are at increased risk for esophagus, stomach, or intestinal bleeding.
Nausea, more tired or weaker than usual, itching, yellowing of the skin or eyes, right upper abdomen tenderness, and “flu-like” symptoms. These could be signs of a liver problem.
Shortness of breath, unexplained weight gain, or swelling of the arms, legs, hands or feet. These could be signs of a serious heart problem.
Any type of rash. This could be a sign of a serious skin reaction.

These are not all of the possible side effects of PENNSAID. Please talk to your doctor if you experience any symptoms that bother you or that do not go away.

Who should not use PENNSAID?

DO NOT USE PENNSAID if you

are in the hospital for a certain heart surgery called coronary artery bypass graft surgery.
know you are allergic to diclofenac or any other ingredient of PENNSAID.
have experienced asthma, hives, or allergic-type reactions after taking aspirin or other NSAIDs. Serious allergic reactions to NSAIDs, including death, have been reported in such patients.
are in the 30th week of pregnancy until delivery

How should I use PENNSAID?

What are the possible side effects of PENNSAID?

What other medications might interact with PENNSAID?

What should I tell my health care provider?

Voltaren as a standard of NSAIDs in modern rheumatology | Badokin V.V.

Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs in clinical practice. They are indispensable for diseases accompanied by inflammation, pain and fever. But their main property is to prevent the development or reduce the intensity of inflammation. These drugs are widely used primarily in inflammatory and degenerative diseases of the joints and spine (rheumatoid arthritis, seronegative spondyloarthritis, osteoarthritis, intervertebral osteochondrosis and spondylosis deformans), acute rheumatic fever, microcrystalline arthropathies, soft tissue diseases, a large group of diseases accompanied by pain in the lower part back. Recently, the field of application of NSAIDs has expanded significantly and they have been used not only in rheumatology, but also in cardiology to prevent the development of thrombosis and to prevent the early development of atherosclerosis in immunoinflammatory diseases [1]. Their use is advisable in minor surgery, in the treatment of migraine, painful menses and oligomenorrhea, dementia of the Alzheimer’s type, in oncology (in particular, for the prevention of colon cancer and possible metastasis of malignant tumors of various localizations).

The class of NSAIDs includes a large number of drugs that are characterized by common and distinctive features. They differ from each other in the severity of analgesic and anti-inflammatory activity, the spectrum of adverse events, the routes of administration of the drug into the body, the scope and category of cyclooxygenase (COX) inhibition, the main mechanism of action of these pharmacological agents. So, according to the severity of inhibition of two COX isoforms, they are all divided into drugs with selective inhibition of COX-1, COX-2 non-selective, COX-2 selective and COX-2 specific. The range of adverse events when taking NSAIDs is largely associated with the predominant inhibition of one or another isoform of COX. The most studied COX-2 non-selective NSAID is Voltaren (diclofenac sodium), which is most commonly used compared to other drugs in this group of drugs [2,3].
Despite the significant advances in modern anti-inflammatory therapy for rheumatic diseases, some drugs that were introduced into clinical practice in the 1920s and 1930s have not lost their significance. last century and later – in 60-70 years. As you know, gold salts, D-penicillamine and aminoquinoline derivatives were proposed for the treatment of rheumatoid arthritis long before the justification for the need for basic or slow-acting therapy in this disease. Later, NSAIDs were developed and widely used, which are now considered as “standard” or “classic”. These drugs include, first of all, Voltaren.
The history of Voltaren began in 1964, when the company Geigy (Geigy) carried out the synthesis of a new NSAID, codenamed GP 45840. Subsequent preclinical studies revealed high therapeutic efficacy and good tolerability of GP 45840, named Voltaren. Since 1974, this drug has been widely introduced into clinical practice. Already in 1976, the results of 166 clinical trials in 21 countries were summarized, which clearly showed the high efficacy of Voltaren in relatively rare and mild adverse reactions. In the same year, domestic rheumatologists presented the results of testing Voltaren for rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, and rheumatism, noting its rather high therapeutic potential and quite satisfactory tolerability [4].
Voltaren (diclofenac sodium) is a derivative of phenylacetic acid. 95.7% of the drug binds to serum proteins. Features of its pharmacodynamics are in a short half-life, which, in turn, helps to reduce the number of undesirable effects due to rapid elimination from the body. The maximum concentration of Voltaren in plasma reaches 1180 ng / ml. In the body, it is transformed into inactive metabolites, which are excreted in the urine and bile [5]. It does not accumulate with prolonged use.
A positive property of Voltaren is its sufficient full compatibility with a number of drugs. However, it should be borne in mind that when combined with oral anticoagulants, it can lead to prolongation of prothrombin time and increased risk of bleeding, with hypoglycemic drugs – to the development of hypo- or hyperglycemia [6]. In some patients, Voltaren increases the toxicity of methotrexate due to the prolongation of its half-life, which leads to a decrease in the excretion of methotrexate and endogenous creatinine. However, this phenomenon occurs when prescribing medium and high doses of methotrexate, and when prescribing 7.5-10 mg / week. violations of the excretory function of the kidneys are usually not observed.
When Voltaren is taken orally, its absorption occurs in the duodenum, as the tablets are produced with a coating that is resistant to the action of gastric juice. This coating helps to reduce the frequency and severity of gastrointestinal toxicity. After 30 min. after administration, the maximum level of Voltaren in plasma is reached. The adsorption of Voltaren and its distribution in the body do not depend on food intake. There is no significant difference in its content in young and old people [5].
All NSAIDs are conventionally divided into short- and long-lived. However, there is no clear relationship between the half-life of the drug and its clinical efficacy. Short-lived drugs can accumulate in high concentrations in the focus of inflammation. In Voltaren, although it belongs to short-lived drugs, the duration of anti-inflammatory action exceeds the time of circulation in the blood plasma due to its redistribution and accumulation in inflamed tissues. When taken orally, its half-life does not exceed 2 hours and is approximately the same as that of ketoprofen and ibuprofen, while for many other NSAIDs (in particular, indomethacin and ketorolac), this period is 2.5-3 times more. Naturally, drugs with a short half-life pose less of a risk to patients due to their rapid elimination from the body. In the synovial fluid, the maximum concentration of Voltaren after a single intramuscular injection appears after 4 hours, and its half-life from the tissues of the joint is 8 hours. Thus, the drug persists much longer in the synovial membrane and in the joint fluid than in plasma, while the concentration in tissues is 4–5 times higher than the concentration in the blood [7]. These data are of great importance for the treatment of rheumatic diseases in general and, in particular, diseases of the joints.
The main mechanism of action of Voltaren (diclofenac sodium), like other NSAIDs, is inhibition of cyclooxygenase (COX) activity [8]. This enzyme is involved in the synthesis of prostaglandins, including PGE2. Prostaglandins are of great importance for the development of inflammation, the onset of pain and fever (Table 1). As you know, the blockade of COX-2 plays a decisive role in the fight against inflammation and pain. One of the powerful inhibitors of COX-2 is Voltaren [9,10,11]. It is shown that five days after the start of therapy with Voltaren at a dose of 150 mg / day. blockade of PGE2, which can be used to judge the inhibition of COX-2, is 93.9%, while when using other NSAIDs (ibuprofen, naproxen, rofecoxib, meloxicam), this figure ranges from 66.7 to 77.0%. Suppression of PGE2 in the synovial fluid lasts from 8 to 12 hours after a single dose of it. Voltaren inhibits the release of intracellular arachidonic acid without affecting the expression of lipoxygenase [11]. The experiment found that it is a potential inhibitor of platelet aggregation. However, under clinical conditions, its effect on platelet aggregation and adhesion, as well as on the activation of prothrombin time, has not been revealed [5]. The pharmacological activity of Voltaren is not limited to the suppression of prostaglandin synthesis. In addition, it inhibits the synthesis of leukotrienes, the formation of superoxide radicals and the release of lysosomal enzymes, affects the activation of cell membranes, the aggregation and adhesion of neutrophils, and the function of lymphocytes.
When choosing NSAIDs, the following factors should be taken into account: the severity of the anti-inflammatory and analgesic effect, the presence and nature of risk factors for adverse events, as well as their possible range, the presence of concomitant diseases, the nature of interactions with other drugs and, of course, cost. According to these parameters, Voltaren (diclofenac sodium) has established itself as one of the most acceptable NSAIDs and continues to be considered as the “gold standard” for inflammatory and degenerative diseases of the joints and spine, especially since it surpasses most NSAIDs in its anti-inflammatory and analgesic activity [12 ].
In the treatment of rheumatoid arthritis, Voltaren (diclofenac) is considered the drug of choice. According to a double-blind study comparing Voltaren and indomethacin in patients with rheumatoid arthritis, it turned out that both drugs significantly reduced the number of inflamed joints and increased the grip strength of the hand [13]. However, such a significant indicator of a truly anti-inflammatory effect, as the dynamics of the total circumference of the proximal interphalangeal joints, significantly underwent reverse dynamics only during treatment with Voltaren. It is believed that anti-inflammatory therapy for rheumatoid arthritis should begin with the appointment of Voltaren, tk. it has a significant anti-inflammatory effect [14]. In the presence of a high activity of the inflammatory process, accompanied by a pronounced pain syndrome, it is advisable to prescribe Voltaren in the form of intramuscular injections, which accelerates the onset of the therapeutic effect. Parenteral or rectal administration of the drug significantly reduces the risk of gastroenterological complications, but does not completely eliminate them.
Equally important is Voltaren in the treatment of ankylosing spondylitis (Bekhterev’s disease). Symptom-modifying therapy for this disease primarily includes NSAIDs, which are considered first-line drugs and an essential component of combination therapy for ankylosing spondylitis. Patients with this diagnosis take NSAIDs almost continuously for many months and even years. These drugs are the basis of drug therapy, especially since in Bechterew’s disease, effective basic therapy is limited only by sulfasalazine, which has a positive effect on the manifestations of peripheral arthritis and practically does not affect the symptoms of spondylitis. As for NSAIDs, they are effective not only in suppressing the inflammatory process in the joints, but also in the axial skeleton, while they significantly reduce the intensity of pain in the spine and its mobility, as well as the severity and duration of morning stiffness.
Phenylbutazone and indomethacin have long been considered the most effective NSAIDs in the treatment of ankylosing spondylitis. However, this point of view is not obvious. In controlled double-blind studies, diclofenac showed the same efficacy as these drugs, with better tolerability of the latter. In another randomized controlled trial of piroxicam, naproxen, and Voltaren at equivalent doses, they appeared to be approximately equally symptom-modifying. However, when assessing adverse events, the majority of patients preferred Voltaren [15].
The possibility of active influence of NSAIDs on the prognosis of ankylosing spondylitis requires clarification. For a long time it was generally accepted that they have only a symptomatic effect in this disease, not controlling the progression of structural changes in the spine, including those patients who have a pronounced clinical (anti-inflammatory) effect. However, recently there have been reports in which NSAIDs are considered as drugs that can reduce the rate of radiographic progression of ankylosing spondylitis. In this regard, they can be considered as disease-modifying agents [16].
A clear positive effect of NSAIDs on the symptoms of spondylitis during the first 48 hours after taking them is considered as one of the diagnostic criteria for Bechterew’s disease. In a study of 741 patients with pain in the spine, it turned out that this sign occurred in the vast majority of patients with ankylosing spondylitis and only in 15% of patients with pain in the spine caused by other pathological conditions [17]. In ankylosing spondylitis, the sensitivity of this symptom is 77%, and the specificity is 85%. Interestingly, if the intensity of back pain is not reduced by taking NSAIDs in the first 48 hours of treatment, then the probability of this disease is only 3%. The presented data emphasize the importance of this group of drugs in the treatment of Bechterew’s disease.
Another indication for Voltaren is acute gouty arthritis. To suppress it, not only NSAIDs are used, but colchicine, corticosteroids and some other drugs. The bright and fast (within 48 hours) effect of colchicine was considered as one of the diagnostic signs of this disease. However, the efficacy of NSAIDs and colchicine appears to be similar. These funds are able to prevent the further development of an acute attack of gout if they are timely prescribed, i.e. within 30–60 min. from the start of the attack. In Europe, rheumatologists prefer to use colchicine or a combination of colchicine with NSAIDs, while in North America NSAIDs are preferred. NSAIDs are used for gout not only to relieve an acute attack, but also to treat chronic arthritis. Of the NSAIDs, preference is given to indomethacin and Voltaren. Conducted controlled studies have not revealed a higher efficacy of traditional NSAIDs compared to selective COX-2 inhibitors (for example, coxibs).
Conducting effective therapy for osteoarthritis is a difficult task, which is associated with its chronic and steadily progressive course, which is so typical for this disease. One of the most important areas of drug therapy for osteoarthritis is the suppression of persistent inflammation of the joint tissues with its localization in cartilage, bone, entheses and synovium. Such an impact involves the appointment of anti-inflammatory therapy, and especially NSAIDs. As you know, NSAIDs occupy a central place among the symptom-modifying drugs for osteoarthritis. In this disease, NSAIDs are prescribed, predominantly rapidly absorbed and short-lived, with a pronounced analgesic effect. At the same time, these drugs should not have a chondronegative effect at prescribed doses.
The effect of NSAIDs on cartilage metabolism appears to be multifaceted. Some NSAIDs have a negative effect on the synthesis of the cartilage matrix and thereby contribute to the progression of osteoarthritis, others have a chondroneutral effect, and still others have a chondroprotective effect. Thus, indomethacin inhibits the synthesis of proteoglycans, type II collagen, and hyaluronic acid by chondrocytes, and also contributes to the premature death of chondrocytes [18]. Huskisson E.C. et al. in a randomized controlled trial, the width of the joint space was assessed in 812 patients with osteoarthritis of the knee [19]. While taking indomethacin, narrowing of the gap was observed in 47% of patients and only in 22% – on placebo. There are observations according to which the use of indomethacin in patients with osteoarthritis quickly leads to a rapid and significant dysfunction of the hip joint and its subsequent prosthetics compared to those patients who were treated only with simple analgesics.
However, not all NSAIDs contribute to the progression of osteoarthritis. It has been shown that some of them stimulate the anabolic function of cartilage tissue by inhibiting the production of interleukin (IL)-1 and the expression of the receptor of this cytokine, promote the intensification of the synthesis of growth factors, including transforming growth factor-1, inhibit the degradation of aggrecan, inhibit cartilage catabolism, neutralize action of metalloproteinases and reduce the intensity of chondrocyte apoptosis [20]. These drugs include diclofenac, meloxicam, ketoprofen, aceclofenac. It has been shown that in vitro diclofenac does not inhibit the biosynthesis of proteoglycans at concentrations equivalent to those in humans, while in vivo it inhibits the activity of costal cartilage chondrocytes, but stimulates articular cartilage chondrocytes [21].
Great importance is attached to NSAIDs in the treatment of a large group of diseases accompanied by pain in the lower back. The literature presents the results of studying the effect of NSAIDs on the central mechanisms of pain that are not associated with inhibition of prostaglandin synthesis, although the inhibition of their production seems to be one of the main mechanisms of analgesic action. In this regard, of particular interest are data on the presence of dissociation between anti-inflammatory (COX-dependent) and analgesic (antinoceptive) effects of NSAIDs [1]. Activation of prostaglandin synthesis in the central nervous system (including the spinal cord) occurs with any peripheral stimulus and inflammation. Voltaren, by suppressing the activity of COX-2, contributes to the development of a pronounced analgesic effect, which is pathogenetic in pain in the lower back. When managing such patients, Voltaren is initially prescribed parenterally, and only when the pain subsides should one switch to taking this drug orally.
A doctor has a large number of different forms of Voltaren at his disposal. It can be used as oral tablets, suppositories, parenteral solution, topical gel and eye drops. The drug is available in various concentrations, which creates certain convenience in the treatment of patients. The maximum daily dose of Voltaren is 0.15 g. This dose is divided into 2-4 doses. Voltaren emulgel is a topical product. It gives a high concentration of the drug in the subcutaneously located target tissues, which is of some importance for improving the tolerability of the drug. Thus, the concentration of diclofenac in the affected structures of the joint and periarticular tissues after repeated use of Voltaren emulgel in the synovial fluid is 770 ng / ml (110–2960), and in plasma only 27.6 ng/ml. These new dosage forms contain special modifications of diclofenac.
The tolerability of Voltaren (diclofenac sodium) has been studied in a large number of controlled studies comparing it with other non-selective and selective COX-2 inhibitors. In terms of tolerability, Voltaren surpasses most non-selective NSAIDs and takes 2nd place after ibuprofen. Voltaren and indomethacin showed the same therapeutic potential in patients with rheumatoid arthritis at 36 months. study [22]. However, better tolerability was observed with Voltaren treatment. Particularly after 12 months. treatment in the indomethacin group, 41% of patients discontinued treatment, and only 19% in the Voltaren group%.
The risk of developing adverse events of Voltaren is not significantly higher than when taking placebo [23]. In general, the manifestations of drug intolerance to this drug are close to those of other NSAIDs. However, it should be borne in mind that the frequency of occurrence of adverse events and their severity significantly differ between Voltaren and numerous generics, and this applies not only to complaints actively presented by patients or complaints identified during questioning, but also to objective symptoms of drug intolerance. So, according to the Institute of Rheumatology, for 2002-2005, in patients taking Voltaren, the frequency of detection of single erosions was 7.1% and multiple erosions and ulcers – 11.1%, while in the treatment of diclofenac generics 13, 3 and 14. 9%, respectively.
A comparative study of the efficacy and tolerability of Voltaren (diclofenac) and selective COX-2 inhibitors, for example, rofecoxib and celecoxib, showed that diclofenac was more effective in patients with osteoarthritis, while there were no significant differences in the frequency of adverse reactions. An interesting study by R.L. Dreiser et al. (2000). The authors reported the results of a randomized, double-blind study evaluating the tolerability of diclofenac sodium 150 mg/day. and two doses of meloxicam – 7.5 and 15 mg / day. at 489patients with acute pain in the lower back. The duration of therapy was 14 days. According to doctors, the good and satisfactory tolerability of the selective COX-2 inhibitor and diclofenac, which is not such, was the same and corresponded to 96 and 95%. A similar assessment was obtained in the opinion of patients. In another placebo-controlled, randomized, double-blind study, diclofenac 150 mg/day was compared in patients with osteoarthritis. (group 1) and celecoxib 200 mg/day. (Group 2) [24]. Gastrointestinal complications were more common in patients of group 1, as well as an increase in serum aminotransferases and anemia. In group 2, on the contrary, peripheral edema was observed 2 times more often, dizziness was also almost 2 times more frequent, infections of the upper respiratory tract were 3 times more frequent, back pain was 5 times more common. In general, it can be noted that Voltaren demonstrates good tolerance at sufficiently high doses (150 mg) and long-term use (up to 8 months or more).
Thus, diclofenac at the beginning of the 21st century has not lost its relevance and continues to be considered as a standard in the treatment of diseases of the joints and spine. It has an optimal combination of anti-inflammatory and analgesic effects, has a large arsenal of various dosage forms, allows you to optimize therapy and effectively monitor the safety of treatment.

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11. Schwartz JI, Van Hecken A, De Leperieri I et al. Ann Rheum Dis 1999; 206: abstract 857.
12. Nasonova V.A. Difficult patient 2004; 2(3):6–10.
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15. Calin A, Eastmond J. J. Rheumatol 1990; 17:801–803.
16 Wanders A et al. Arthritis Rheum 2005;52: 1756–1765.
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24. McKenna F., Borenstein D., Wendt H. et al. Scand. J. Rheumatol, 2001; 30:11–18.

Osteoarthritis drug list – asia-pharm.ru

Osteoarthritis (OA) is the most common form of arthritis. It is characterized by wear and tear on the joints and loss of cartilage, causing bones to rub against each other. The damage cannot be reversed.

OA can occur naturally with age, but can also occur in younger people.

It can also be the result of frequent injuries.

Obesity is a risk factor for developing OA, as being overweight can put pressure on the joints. OA causes pain and inflammation, which can make daily movement difficult.

Medicines can help by reducing pain and inflammation.

Your doctor will likely recommend over-the-counter (OTC) pain relievers and anti-inflammatory drugs to start with. If these medicines do not work or if you have a severe case of OA, your doctor may prescribe prescription medicines for you.

There are many different pain and anti-inflammatory medications available to treat OA.

Learn about your options here and work with your doctor to find the best option for you.

Non-steroidal anti-inflammatory drugs (NSAIDs) treat pain. They also help prevent painful inflammation and joint damage. They are the best choice for treating OA because they are effective and do not cause sedation.

NSAIDs are oral and topical. There are many options and some of them are available without a prescription.

Your doctor will likely recommend that you start with an over-the-counter NSAID. If that doesn’t work, your doctor may give you a prescription NSAID.

NSAIDs carry risks, even over-the-counter versions.

Side effects may include:

stomach irritation, erosion, or ulcers (this can lead to stomach bleeding and death)
kidney problems

If you have kidney disease, ask your doctor if NSAIDs are safe for you.

If you are allergic to aspirin, you should not take NSAIDs.

Do not take NSAIDs for a long time without talking to your doctor. Your doctor will monitor you during treatment.

Examples of NSAIDs include:

Aspirin

Aspirin is an over-the-counter NSAID that treats pain and inflammation. It can help treat the symptoms of OA to improve your quality of life.

Ibuprofen (Advil, Motrin, IBU-Tab)

Ibuprofen (Advil, Motrin, IBU-Tab) is an NSAID available in both OTC and prescription strengths. Long-term use of ibuprofen is not recommended due to the risk of stomach bleeding and heart attack.

The Food and Drug Administration (FDA) Reliable source recommends taking the lowest dose that works for you and taking it for no more than 10 days. You should not take ibuprofen for more than 10 days unless your doctor tells you to.

Naproxen (Naprosyn) and naproxen sodium (Aleve)

Naproxen (Naprosyn) and naproxen sodium (Aleve) are used to treat pain and inflammation in OA.

Naproxen is available by prescription only. Naproxen sodium is available without a prescription, and higher doses are also available in prescription forms.

Some side effects of naproxen and naproxen sodium include:

heartburn
abdominal pain
nausea
diarrhea
headaches
headache diclofenac (Zipsor, Voltaren) and diclofenac-misoprostol ( Artrotek)
Diclofenac (Zipsor, Voltaren) is an NSAID that is available both in oral and topical form.
Oral Zipsor is available by prescription and topical Voltaren is available without a prescription.
Oral diclofenac-misoprostol (Artrotek) combines diclofenac with a drug that protects against stomach ulcers.
Diclofenac may cause side effects including:
- abdominal pain
- diarrhea
- nausea
Other prescription NSAIDs for OA
prescription NSAIDs approved for OA symptoms:
- celecoxib (celebrex)
- forked
- Etodolac
- fenoprofen (nalfon)
- flurbiprofen
- indomethacin (Indocin)
- ketoprofen
- ketorolac
- meclofenamate
- meloxicam (Mobic)
- nabumetone
- oxaprozin (Daipro)
- piroxicam ( Felden)
- sulindac
- I interpreted
Analgesic is another type of pain reliever. Unlike NSAIDs, analgesics do not treat inflammation.
This class of drugs works by blocking signals in your body that cause pain.
Examples of analgesics include:
Acetaminophen (Tylenol)
Acetaminophen (Tylenol) is an over-the-counter analgesic. You take it by mouth as:
- softgel
- tablet
- liquid strength
In 2011, the FDA set the maximum dosage for acetaminophen at 4,000 milligrams (mg) per day.
Following the FDA’s announcement of McNeil Consumer Healthcare, the Tylenol company has set the maximum daily dose of acetaminophen at 3,000 mg.
It is important to monitor your daily acetaminophen intake. Taking high doses of acetaminophen for a long time can lead to liver damage or liver failure, which can be fatal.
Do not drink more than three alcoholic drinks a day while you are taking this drug. Drinking more fluids than recommended can increase your risk of liver problems.
Duloxetine (Cymbalta)
Duloxetine (Cymbalta) is used to treat depression. However, it is also used off-label to treat chronic pain caused by OA.
Side effects include:
- fatigue
- nausea
- constipation
Off-label drug use 90 002 Off-label use means that a drug approved by the FDA for one purpose is used for another. goal that has not yet been approved.
However, the doctor may still use the drug for this purpose. This is because the FDA regulates drug testing and approval, not how doctors use drugs to treat their patients. This way, your doctor can prescribe the medication that he thinks is best for your treatment.
These topical pain medications are:
- ointments
- creams
- gels
- patches
They are an alternative to oral or injectable drugs used to treat OA.
They are available over the counter and by prescription. Some topical treatments provide immediate short term relief while others provide long term relief.
Local analgesics include:
- Capsaicin (Capzasin, Zostrix, Icy Hot). Derived from cayenne pepper, this over-the-counter product is available as a cream.
- Diclofenac sodium gel and solution (Voltaren, Solarase, Pennside). This topical NSAID is available over-the-counter and by prescription.
- Lidocaine patch . Lidocaine can treat a specific area of pain in OA, but is not usually given as the first treatment.
- Methyl salicylate and menthol (Bengai). This medicated cream is made from mint plants and also contains a topical aspirin-like NSAID.
- Trolamine salicylate (Aspercreme). This cream contains an aspirin-like drug that relieves inflammation and pain.
The American College of Rheumatology (ACR) and the Arthritis Foundation (AF) Reliable source recommend topical capsaicin for knee OA, but do not recommend it for hand OA.
Corticosteroids, also known as steroids, are sometimes used briefly for severe OA flare-ups. However, they have many risks if they are used for long term treatment.
Like NSAIDs, steroids reduce inflammation but are bad for the stomach. Unlike NSAIDs, they do not cause kidney problems. This means they may be a safer choice for people with kidney disease.
Injectable corticosteroids are used to treat OA. They are injected directly into the joints.
Side effects of all steroids may include:
- high blood sugar
- stomach ulcer
- high blood pressure
- irritability and depression
- cataracts or clouding of the lens of the eye
- osteoporosis
Corticosteroids include:
- betamethasone (Celestone Soluspan)
- dexamethasone
- hydrocortisone (Solu-Cortef)
- methylprednisolone (Depo- Medrol, Solu-Medrol)
- prednisolone
- triamcinolone acetonide (Kenalog-40, Zilretta)
These prescription pain relievers change how you feel pain but do not prevent inflammation.

Pennsaid vs voltaren: Voltaren Gel vs. Pennsaid for Arthritis: Differences & Side Effects

A comparative subjective assessment study of PENNSAID® and Voltaren Gel®, two topical formulations of diclofenac sodium

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PENNSAID® 2% HOME | The PENNSAID (diclofenac sodium topical solution) 2% w/w official site

PENNSAID 2% is a topical NSAID designed to target your OA knee pain and deliver relief right where it hurts.

INDICATIONS AND USAGE

What is PENNSAID

IMPORTANT SAFETY INFORMATION

What is the most important information I should know about PENNSAID?

PENNSAID can cause serious side effects. Stop taking PENNSAID and call your doctor or go to your emergency department right away if you get:

These are not all of the possible side effects of PENNSAID. Please talk to your doctor if you experience any symptoms that bother you or that do not go away.

Who should not use PENNSAID?

How should I use PENNSAID?

What are the possible side effects of PENNSAID?

What other medications might interact with PENNSAID?

What should I tell my health care provider?

INDICATIONS AND USAGE

What is PENNSAID

IMPORTANT SAFETY INFORMATION

What is the most important information I should know about PENNSAID?

PENNSAID can cause serious side effects. Stop taking PENNSAID and call your doctor or go to your emergency department right away if you get:

These are not all of the possible side effects of PENNSAID. Please talk to your doctor if you experience any symptoms that bother you or that do not go away.

Who should not use PENNSAID?

How should I use PENNSAID?

What are the possible side effects of PENNSAID?

What other medications might interact with PENNSAID?

What should I tell my health care provider?

Voltaren as a standard of NSAIDs in modern rheumatology | Badokin V.V.

Osteoarthritis drug list – asia-pharm.ru

Aspirin

Ibuprofen (Advil, Motrin, IBU-Tab)

Naproxen (Naprosyn) and naproxen sodium (Aleve)

Other prescription NSAIDs for OA

Acetaminophen (Tylenol)

Duloxetine (Cymbalta)

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