Ketoprofen – indications, contraindications, dosage and side effects

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Ketoprofen is a popular drug that is used in inflammatory conditions with high fever and severe headache. Ketoprofen is an ingredient in the most commonly available prescription drugs. What are the indications and contraindications for the use of ketoprofen? How to dose this drug? Is ketoprofen safe and how is its effectiveness assessed?

What is ketoprofen?

Ketoprofen is an organic chemical compound. Its chemical structure is a racemic mixture composed of a benzophenone residue and propionic acid. Ketoprofen is a non-steroidal anti-inflammatory drugwhich is abbreviated as an NSAID. As a drug from the NSAID group, it inhibits the activity of COX-1 and COX-2, i.e. enzymes responsible for the formation of chemical compounds that mediate inflammation.

Ketoprofen has antipyretic, analgesic and anti-inflammatory properties. Ketoprofen was introduced into the medical circulation as an oral pain reliever in the 1970s. Currently, over a dozen preparations are available on the Polish pharmaceutical market. which in their basic composition contain ketoprofen.

What are NSAIDs? Check: NSAIDs – non-steroidal anti-inflammatory drugs

How does ketoprofen work?

The mechanism of action of ketoprofen it is the same as the action of all drugs belonging to the NSAID group. This means that ketoprofen inhibits the activity of cyclooxygenase, an enzyme that is involved in the synthesis of prostaglandins from lipids in cell membranes. As mentioned before, there are two isoforms of this enzyme, they are COX-1 and COX-2.

The COX-1 isoform is active under physiological conditions in many human tissues, especially in platelets, kidneys, stomach and blood vessels. In turn, the COX-2 isoform is an enzyme whose activity increases rapidly when the inflammatory process begins and continues in the tissues. Drugs from the NSAID group differ mainly in the specificity of their action against COX-1 and COX-2. Ketoprofen is active against both COX-1 and COX-2 isoforms.

Inhibition of COX-2 activity is associated with a reduction in the synthesis of prostaglandins, which play a significant role in the development of inflammatory symptoms. The effect of ketoprofen in this case is analgesic and anti-inflammatory. In turn, inhibition of the COX-1 isoform in platelets leads to the inhibition of thromboxane synthesis. In this case, the anti-aggregation effect of ketoprofen is weaker and shorter than that of acetylsalicylic acid.

If you want to know more about pain relievers and anti-inflammatory drugs, read on: Anti-inflammatory drugs – which ones to choose for your ailment?

Ketoprofen – drug absorption mechanism

Ketoprofen is a drug that is very well absorbed from the digestive system. Ketoprofen starts working about half an hour after oral administration. In turn, the maximum concentration in the blood serum is reached two hours after administration. Ketoprofen will work much faster if given intramuscularly.

When administered intramuscularly, the effect of ketoprofen is already observed after 15 minutes, and its maximum concentration in the serum after 45 minutes. The half-life is about two hours after taking a tablet, suppository or intramuscular injection. Ketoprofen is more than 99% protein bound.

Ketoprofen is absorbed very slowly through the skin. In the case of topical administration of approx. 50-150 mg only after 5-8 hours, the plasma ketoprofen concentration will be 0,08–0,15 µg / mlwhich is only 5-10% of the concentration of this drug after oral administration. However, it has been shown that the ketoprofen gel is able to reach all joint tissues in the area of ​​the drug application.

After applying a layer of about 10 cm of ketoprofen in 2,5% gel to the knee joint, the concentration of the drug in the synovial fluid was comparable to the concentration after intramuscular administration.

How should drugs be used to be effective? Read: How to take medications effectively?

Indications for the use of ketoprofen

As already noted, ketoprofen is a pain reliever, anti-inflammatory and antipyretic drug. An indication for the use of ketoprofen is moderate muscle, joint and headache. Ketoprofen is also used in the case of rheumatoid arthritis or osteoarthritis.

This drug is very often used by patients with high fever or mild headache pain. In some cases, ketoprofen can be used to relieve the pain of menstruation. Ketoprofen is also widely used in the treatment of post-operative and traumatic pain and, less commonly, for the relief of other pain syndromes.

However, it should be remembered that ketoprofen is not a first-line drug that should be used in the case of these ailments. Use of ketoprofen is only recommended when milder, over-the-counter medications have failed to provide pain relief.

What types of headaches do we most often suffer from? Read on: You have a headache? It could be an allergy [INFOGRAPHICS]

Contraindications to the use of ketoprofen

Before starting the dose of ketoprofen, carefully read the package leaflet and discontinue use if there are any contraindications. Ketoprofen is a drug that acts non-selectively on both COX-1 and COX-2 isoforms, so its use may cause various side effects.

Among the contraindications to the use of ketoprofen lists:

1. allergy or hypersensitivity to ketoprofen;
2. any previous hypersensitivity reactions such as bronchospasm, bronchial asthma, rhinitis, urticaria and the like, especially if it has occurred with other NSAIDs or salicylates;
3. severe heart failure;
4. severe renal failure;
5. severe liver failure;
6. the third trimester of pregnancy – because the use of the drug may have a detrimental effect on the course of pregnancy and the development of the embryo and fetus
7. breast-feeding;
8. an active or a history of peptic ulcer of the stomach and duodenum;
9. gastrointestinal bleeding;
10. gastrointestinal perforation related to previous NSAID use;
11. bleeding tendency;
12. bronchial asthma and rhinitis;
13. planned exposure to the sun – because there is a high risk of skin allergic reactions;
14. hypersensitivity to any of the excipients of the drug;
15. elderly or too young age of the patient;
16. pain treatment after vascular bypass grafting.

What should you know about side effects of drugs? Check: Adverse drug reactions

How to dose ketoprofen?

Ketoprofen is a drug that can be used in patients from 15 years of age. The daily dose of ketoprofen is 200 mg. Ketoprofen is such a powerful drug that when deciding to use it, you should always choose the lowest dose and take it for the shortest possible time, preferably until symptoms improve or subside.

It is not recommended to take ketoprofen in doses higher than 200 mg. Additionally, you should not take this drug for more than 5 days. If you need to take ketoprofen for a long time, this decision should always be consulted with your doctor.

They are available on the Polish pharmaceutical market over-the-counter ketoprofen preparations. In the case of capsules, they contain 50 mg of ketoprofen, while the drug in a sachet contains 25 mg of the drug. Higher doses of ketoprofen are found in prescription suppositories, ointments, sachets, tablets and capsules.

Ketoprofen should be taken with a meal. The medicine is best washed down with a glass of water or milk. To reduce unpleasant gastric symptoms, when using ketoprofen, it is worth taking additional protective drugs for the gastric mucosa, e.g. pantoprazole or omeprazole.

If you want to know what makes painkillers different, read on: You often use painkillers, but do you know how they differ?

Ketoprofen – interactions with other preparations

Before starting the use of ketoprofen, you should check that you are not taking any medications that interact with it. So far, it has been shown that ketoprofen can cause:

1. when using lithium preparations – increase in the concentration of lithium in the blood plasma;
2. if you are taking diuretics – reducing their effectiveness;
3. when using ACE inhibitors, i.e. drugs for arterial hypertension – worsening of kidney function;
4. in the case of drugs for high blood pressure – reducing their effectiveness;
5. in the case of thrombolytic drugs, e.g. pentoxifylline – increased risk of bleeding;
6. in the case of anti-diabetic and some anti-epileptic drugs – the intensification of their action.

What mistakes do we most often make when using painkillers? Check: The Seven Deadly Sins of Painkillers

Ketoprofen and possible side effects

The use of ketoprofen, as with other drugs, can cause side effects. Malaise, indigestion, nausea, abdominal pain and vomiting were the most common in patients using ketoprofen. Less common side effects are skin allergic reactions, drowsiness, dizziness, constipation, diarrhea, tinnitus, edema, inflammation of the oral mucosa and hepatitis.

It is also worth remembering that the use of ketoprofen in the case of clearly indicated contraindications can also cause side effects. Severe heart failure increases the risk of thrombotic events, heart attacks and strokes. If the patient is struggling with renal failure, renal dysfunction, electrolyte disturbances and episodes of hypertension may occur. The use of the drug in the case of hepatic insufficiency, in turn, may lead to intoxication and intensification of the toxic effects of the drug.

In the case of bronchial asthma, inhibition of COX-1 in the bronchi leads to the intensification of the synthesis of leukotrienes, i.e. substances that strongly constrict the bronchi. This can trigger a seizure. aspirin asthma. Therefore, asthmatics and allergy sufferers should be especially careful, as the drug may aggravate breathing problems or breathlessness.

If you want to know how Ibuprofen works and how to properly dose it, check out: Ibuprofen – action and dosage rules

Ketoprofen – in what form is it available?

On the Polish pharmaceutical market and in Polish pharmacies, patients can buy over a dozen different preparations that contain ketoprofen. Currently ketoprofen can be purchased in the form of capsules or tablets for oral use, gel or spray for topical use on painful areas, and suppositories for rectal use.

In medical facilities or hospitals, the drug is also available in the form of an injection that is administered intramuscularly. Each of the above preparations may contain a different concentration of ketoprofen. The most common doses are 50, 100, 150 or 200 mg per tablet, capsule or suppository.

What should you know about intramuscular injections? Check: Intramuscular injection – what is it?

Do I need a prescription for ketoprofen?

The vast majority of drugs containing ketoprofen are available on prescription in Polish pharmacies. From October 1, 2017, the first over-the-counter capsules containing 50 mg of ketoprofen appeared.

Interestingly drugs with ketoprofen in some countries they are dispensed without a prescription. Ketoprofen bez recepty can be purchased in the United States of America, France, Italy and Slovakia.

What is an e-prescription and what is the procedure for issuing it? Read on: How does issuing an e-prescription look like during a TV visit? [WE EXPLAIN]

Is ketoprofen a safe drug?

Many patients, before deciding to use ketoprofen, wonder if it is a safe drug. As with any pharmacotherapy, the use of ketoprofen is also associated with the risk of various side effects. However, when using ketoprofen as recommended in the leaflet, i.e. in a dose of 50 mg, for no longer than 5 days, not exceeding 3 tablets a day, the risk of serious side effects is negligible.

Important information is that ketoprofen is a drug with a short half-life (about 2 hours), thanks to which the risk of side effects from the digestive system is lower than in the case of drugs with a long half-life. To reduce possible side effects, it is worth using antacids in the stomach at the same time. This will minimize the effect of this drug on the gastrointestinal mucosa.

Did you know that some over-the-counter medications can be dangerous? Check which ones! Read on: Dangerous over-the-counter drugs

Ketoprofen and other painkillers – effectiveness

In cases of intense pain or high fever, we are looking for an effective drug that will minimize or eliminate unpleasant ailments as soon as possible. The analgesic power of ketoprofen has been confirmed in many clinical trials. These studies have shown that ketoprofen is stronger and more effective than ibuprofen, diclofenac, paracetamol or aspirin.

An additional advantage of ketoprofen is that it works in low doses, i.e. from one capsule, while other drugs must be used in much higher doses. The strong effect of the drug means that you do not need to look for another preparation that will work harder and faster. The effects of ketoprofen can be felt as early as half an hour after taking the tablet.

What drugs should not be combined with each other? Check: Dangerous interactions

Ketoprofen – drugs available on the Polish market

Ketoprofen is a component of several drugs available in Polish pharmacies. Among them you can mention:

1. Bi-Profenid– modified release tablets. Price for 20 tablets: approx. PLN 13;
2. febr oven – prolonged release capsules. Price for 20 capsules: about PLN 12; 
3. Knocked – hard capsules. Price for 20 capsules (50 mg) about PLN 10;
4. Ketonal – gel 0,025g / g 50g. Price for 50 g: about PLN 18;
5. Ketonal – 50 mg / ml solution for injection. Price for 10 ampoules: approx. PLN 14;
6. Ketonal Active – hard capsules. Price for 10 capsules (50 mg): approx. PLN 10;
7. Ketonal DUO – prolonged release capsules. Price for 30 capsules (150 mg) – approx. PLN 22;
8. Ketonal Fast – granules for oral solution. Price for 30 sachets (50 mg): approx. PLN 17;
9. Ketonal forte – coated tablets. Price for 30 tablets (100 mg): approx. PLN 15;
10. Ketonal Sprint (granules for oral solution. Price for 12 sachets (25 mg): approx. PLN 8;
11. Ketoprofen LGO – 25 mg / g gel. Price for 50 g: approx. PLN 13;
12. Ketoprofen Ziaja – 25 mg / g gel. Price for 50 g: approx. PLN 14;
13. Ketoprofen-SF – hard capsules. Price for 20 capsules (50 mg): approx. PLN 12;
14. Ketoprofen-SF – 50 mg / ml solution for injection. Price for 10 ampoules: approx. PLN 15;
15. Ketoprofen Fastum – 25 mg / g gel. Price for 50 g: approx. PLN 16;
16. Ketospray Forte – dermal spray 100 mg / ml. Price for 25 g: about PLN 30;
17. Opokan-keto – gel 0,025 g / g. Price for 50 g: approx. PLN 12;
18. profenid – suppositories. Price for 10 suppositories (100 mg): approx. PLN 11;
19. Refastin – pills. Price for 30 tablets (100 mg): approx. PLN 15. 

You can read more about the drugs mentioned above here:

1. Bi-Profenid;
2. Ketonal Lek;
3. Ketonal forte – use, side effects, interactions with other drugs;
4. Fasting;
5. Opokan-keto gel – characteristics, action, side effects;
6. Profenid.

Before use, read the leaflet, which contains indications, contraindications, data on side effects and dosage as well as information on the use of the medicinal product, or consult your doctor or pharmacist, as each drug used improperly is a threat to your life or health. Do you need a medical consultation or an e-prescription? Go to halodoctor.pl, where you will get online help – quickly, safely and without leaving your home.