Ketoprofen
Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID), a derivative of methylacetic acid. It is used mainly for the treatment of inflammatory and degenerative diseases of the musculoskeletal system, diseases of the joints and spine. It has analgesic, anti-inflammatory and antipyretic effects. It is used as a symptomatic remedy, i.e. in order to eliminate the negative manifestations of the disease, but not its causes. One of the main objectives of the drug is pain relief. Pain is the main reason for seeking medical help. First of all, this applies to elderly patients, whose general condition is affected by the presence of multiple concomitant pathologies. And given the trend towards an aging population, the relevance of effective pain management will only increase in the future. The elimination of mild and moderate pain has traditionally relied on the use of NSAIDs. If the pain does not subside, or, on the contrary, intensifies, they resort to the help of heavy analgesic “artillery” in the form of more serious drugs, including narcotics. NSAIDs are the first choice drugs for pain relief in rheumatic diseases. The “classic” side effect of this group of drugs - a negative effect on the mucous membrane of the gastrointestinal tract - can be neutralized by careful monitoring of the dose taken and duration of treatment, as well as the adequacy of concomitant therapeutic measures.
The mechanism of action of ketoprofen is due to the suppression of the activity of the enzyme cyclooxygenase, which is involved in the metabolism of the prostaglandin “substrate” - arachidonic acid. Prostaglandins are known to be mediators of pain and inflammation. The pronounced analgesic effect of the drug is due to a dual mechanism of action: through inhibition of prostaglandin synthesis in the periphery (peripheral component) and in the central nervous system (central component).
In addition, the drug affects the biological activity of various neurotropic substances involved in the secretion of pain mediators in the spinal cord. In addition to this, ketoprofen is endowed with antibradykinin activity, normalizes the state of lysosome membranes, and significantly suppresses the activity of neutrophils in patients suffering from rheumatoid arthritis. Inhibits the ability of platelets to aggregate. When taken orally, ketoprofen is well absorbed from the digestive tract. The maximum concentration of the active substance in the blood plasma is observed after 1-5 hours (for the tablet form), after 20-30 minutes (for the injection form with intramuscular administration), after 5 minutes (for the injection form with intravenous administration). Ketoprofen is available in three dosage forms: in addition to the already mentioned tablets and solution for injection, it is a gel for external use. The dosage regimen of the drug is established individually depending on the nature of the disease. For the tablet form, the initial daily dose is 300 mg 2-3 times a day. For the treatment of acute pain syndrome or exacerbation of chronic pain, preference is given to an injectable dosage form, which is administered as a single intramuscular injection in an amount of 100 mg. Ketoprofen in the form of an injection solution should not be used for more than 2-3 days. Then the patient is transferred to the tablet form of the drug. The maximum daily dose of injectable ketoprofen is 200 mg. Ketoprofen gel is applied to the surface of the skin in the area of the inflammatory focus 2 times a day. Pharmacotherapy with ketoprofen provides for a number of restrictions on taking other medications. Thus, the drug is incompatible with injectable tramadol. Ketoprofen increases the side effects of gluco- and mineralocorticosteroids, female sex hormones, and reduces the effectiveness of antihypertensive and diuretic drugs.
Reviews of Ketoprofen
Gel for external use Ketoprofen – Amazingly helps when used in complex therapy. My parents are at that age when something regularly aches, shoots, creaks and aches. Especially joints, back and neck. After all, over the years, these particular parts of the body have worked a lot. And it is not possible to cure many diseases completely, because the body has not yet learned how to overcome aging. You can only numb and treat.
My mother’s knees have been bothering me for a long time. First we tried traditional methods of treatment: burdock leaves, cabbage leaves, apple cider vinegar, compresses. But if there was an effect, it was temporary. And then everything started all over again. The disease especially makes itself felt in spring and autumn, that is, during the season of intensive gardening work. And although now everything can be bought in a store, and pensions seem to be normal, we are very much accustomed to growing our own products.
I also noticed that the expression “movement is life” is not empty words. The peak of all exacerbations, according to my observations, begins precisely in the season when physical activity is minimal. That is, in early spring. In winter, people don’t have to dig in their gardens (I’m talking about pensioners), so they sit at home, and after a few months of sedentary life, everything starts to hurt.
I begin to put my parents on “combat readiness” in early spring. As a rule, for the father it is the back, and for the mother the arms and legs. So this spring, after lengthy persuasion to visit a doctor (here for some reason you have to use all your eloquence, and this process is long, for some reason the older generation does not want to go to the doctor, even if something hurts), doctor, among other drugs recommended gel for external use “Ketoprofen”. It is used as an analgesic and anti-inflammatory drug for joint pain, arthritis, radiculitis, damage to ligaments and tendons.
Of course, using it without other drugs that will specifically treat is pointless. Because it will only numb the pain, and the problem needs to be treated. But it relieves pain wonderfully. And the back, and the neck, and (in my mother’s case, the knees).
It is also important that it is not expensive - in our pharmacies it costs 60 rubles. It has some contraindications: infected abrasions and wounds, pregnancy, breastfeeding.
Ketoprofen should not be applied to open wounds. Regarding absorption. This gel absorbs amazingly. After a couple of minutes of rubbing, no traces remain on the skin. And on your hands too. It’s not like other ointments: you rub it, and you walk around all day slippery and sticky, and you get your clothes dirty. Here you don’t even have to wash your hands afterwards.
Shows good results when used together with Chondroxide.
One nourishes and restores cartilage tissue, the other relieves pain. Mom, thanks to these ointments, is showing good activity this season). More details on Review: konovalov.kardan
Ketoprofen gel for external use 2.5% 30g
Compound
Active substance: ketoprofen 2.5 g.
Excipients: carbomer - 1.5 g, ethanol 95% - 32 g, trolamine - 2.9 g, lavender oil - 0.1 g, water - up to 100 g.
Pharmacokinetics
Ketoprofen is absorbed very slowly and practically does not accumulate in the body. Bioavailability is 5%. Ketoprofen penetrates into the subcutaneous tissue, ligaments and muscles, synovial fluid and reaches therapeutic concentrations there. The concentration of the drug in the blood plasma is extremely low. Ketoprofen is metabolized in the liver to form conjugates, which are mainly excreted in the urine. Ketoprofen is characterized by slow excretion in urine.
Indications for use
- Acute and chronic inflammatory diseases of the musculoskeletal system (articular syndrome with exacerbation of gout, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, osteoarthritis, osteochondrosis with radicular syndrome, radiculitis, inflammatory damage to ligaments and tendons, bursitis, sciatica, lumbago);
- muscle pain of rheumatic and non-rheumatic origin;
- post-traumatic inflammation of soft tissues and the musculoskeletal system (damage and rupture of ligaments, bruises).
The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.
Contraindications
- Individual hypersensitivity to ketoprofen or other components of the drug, acetylsalicylic acid or other NSAIDs (history of bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid), tiaprofenic acid and fenofibrate;
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history);
- a history of increased skin sensitivity to solar radiation (photosensitivity);
- history of skin allergies to sunscreens or perfumes;
- exposure to the sun on the treated areas, including solariums, during the course of using the drug and 2 weeks after;
- weeping dermatoses, eczema, infected abrasions, wounds (at the site of application of the gel);
- children under 12 years of age (efficacy and safety have not been studied);
- pregnancy (III trimester) and breastfeeding period.
With caution:
Hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe dysfunction of the liver and kidneys, chronic heart failure, bronchial asthma, old age, pregnancy (I and II trimester).
Directions for use and doses
For external use.
A strip of gel 5-10 cm long is applied in a thin layer to the affected area or skin over the source of inflammation 2 times a day and rubbed in lightly.
The amount of gel applied depends on the size of the area being treated.
It is possible to use ketoprofen in combination with physiotherapy (phonophoresis and iontophoresis).
The dosage in children over 12 years of age corresponds to that in adults and depends on the area of application and the doctor’s recommendations.
Storage conditions
In a dark place at a temperature not exceeding 25° C. Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date.
special instructions
Do not apply to damaged (including open wounds) and inflamed skin!
Avoid contact with eyes (risk of conjunctival irritation).
It is recommended to wash your hands thoroughly after using the drug.
Do not use as hermetic dressings. Do not use in combination with sealed clothing.
Long-term use of topical agents may result in sensitization or local irritation.
To avoid any manifestations of hypersensitivity or photosensitivity, exposure to direct sunlight (including visiting a solarium) should be avoided during the treatment period and for two weeks after using the drug, and it is recommended to cover the treated areas with clothing. Patients with severe renal, cardiac or hepatic impairment should be careful when using ketoprofen.
You should stop using the drug if any skin reaction occurs, including reactions when simultaneously applying sunscreen or other cosmetics containing the organic sunscreen filter octocrylene to the skin.
When using the drug in large quantities, it is possible, in very rare cases, to develop systemic side effects (hypersensitivity, bronchial asthma, gastrointestinal disorders, aggravation of renal failure).
The risk of systemic side effects increases depending on the amount of gel applied, the area of the skin being treated, the condition of the skin, and the duration of treatment.
Avoid exposure of treated areas to sunlight or UV rays, including tanning beds, during treatment and for two weeks after treatment.
Description
Non-steroidal anti-inflammatory drug (NSAID).
Use in children
Contraindicated in children under 12 years of age (efficacy and safety have not been studied).
Pharmacodynamics
NSAIDs. It has analgesic, anti-inflammatory and anti-edema effects. Inhibits the activity of COX, which leads to inhibition of prostaglandin synthesis. In addition, ketoprofen inhibits lipoxygenase, bradykinin synthesis, stabilizes lysosomal membranes and prevents the release of enzymes involved in the inflammatory process.
Ketoprofen does not have a negative effect on the condition of articular cartilage.
Side effects
Possible side effects are listed in descending frequency of occurrence: very common (> 10%), common (> 1%, < 10%), uncommon (> 0.1%, < 1%), rare (> 0.01%, < 0.1%), very rare (<0.01%).
From the skin: infrequently - erythema, itching, eczema; rarely - photosensitivity, bullous dermatitis, urticaria; very rarely - contact dermatitis, angioedema.
From the gastrointestinal tract: very rarely - peptic ulcer, bleeding, diarrhea.
From the immune system: very rarely - anaphylactic reactions, hypersensitivity reactions.
From the urinary system: very rarely - aggravation of renal failure.
Use during pregnancy and breastfeeding
The use of the drug during breastfeeding is not recommended.
Interaction
When ketoprofen is used externally in the form of a gel, it is possible to enhance the effect of drugs that cause photosensitivity. Other interactions have not been established, however, patients taking coumarin anticoagulants are recommended to regularly monitor the international normalized ratio (INR).
Overdose
The extremely low systemic absorption of the active components of the drug when used externally makes overdose almost impossible.
If large quantities of the drug (more than 20 g) are accidentally ingested, systemic adverse reactions characteristic of NSAIDs may occur. It is necessary to lavage the stomach and take activated charcoal. Treatment is symptomatic.
Release form
Gel for external use, 2.5%.
Impact on the ability to drive vehicles and operate machinery
The drug does not affect the ability to drive a car or use other mechanical means.
KETOPROFEN (gel)
The steroidal anti-inflammatory drug forms the basis of modern “Bystrumgel” and “Fastumgel”, only the difference between the newfangled components and simple “Ketoprofen” is 200 rubles, if not more.
A tube of 50 grams is packed in a box.
The box contains clear instructions, which amateurs must read, because there are enough contraindications in it (we especially take into account the categories of pregnant women in the 3rd trimester, nursing, children under 12 years of age), notes “with caution”...
... and possible side effects you should be aware of.
The indications for the drug are good and necessary. Pain in the musculoskeletal system, like muscle pain, can be unbearable. It is a great misfortune when you are not able to get out of bed, or when you cannot straighten up when bending over - I know this from my own experience. And pain on a more modest scale (pulled, just bruised, etc.) also complicates life. However, I have to admit that gels and ointments for significant ailments (that pain that makes you twist, pierce) are not always able to significantly alleviate the condition, nor can they cure, for example, chronically diseased joints. Painful effect of mild to moderate severity - yes! - pacify. “Ketoprofen” is no different from most tube products. My husband likes to smear it on his knee, which has been sore since his youth, usually aching due to bad weather. Also, with the help of "Ketoprofen" it relieves moderate pain in the lower back after physical activity. “Ketoprofen” saved me from the unpleasant whining of a bruised elbow, a slightly cold neck and a twisted foot. But this gel didn’t save me from the hellish pain, when I suddenly got a “shot” in the back so much so that I thought I had been shot. The beloved somehow severely “torn” his lower back - “Ketoprofen” didn’t help much either. In general, there are cases when only injections can save you.
The gel is generally pleasant: transparent, colorless, sticky, with an amazing aroma of lavender oil. Oh, that's lavender oil! How I adore him in any way! But I felt it for the first time in a non-steroidal external remedy. It’s cool that the manufacturer did not skimp on adding lavender oil to such a budget product. In the case of “Bystrumgel” and “Fastumgel”, the presence of this oil in the composition is more understandable due to the expensive cost. True, these gels contain another oil - neroli oil (orange flower oil). Isn't it what consumers are overpaying for? 
After applying “Ketoprofen” to the sore spot, after a while, the numbness of this area begins to be felt, and the patient will feel relief. If possible, it is better to wrap the painful part with something warm - this will be many times more effective.
In general, the gel is like a gel. This product is a must have in your home medicine cabinet. There was only one thing that upset me about the last tube: after a long period of non-use, the cap stuck firmly to the tube and subsequent unscrewing led to its involuntary dismemberment.
But this is probably a special case. There was nothing like this before.
Don’t get sick, take care of yourself and, if possible, don’t overpay for expensive analogues. Tested on myself: “Bystrumgel” and “Ketoprofen” have the same effect. Does it make sense to overpay in this case?! For me the answer is obvious.
