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Ketoprofen

Generality

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory and antipyretic activity.

Ketoprofen - Chemical Structure

It is a drug available in many pharmaceutical formulations suitable for different routes of administration (oral, topical, rectal and parenteral).

From the chemical point of view, ketoprofen is a derivative of 2- (para-amino-phenyl) propionic acid.

Examples of medicinal specialties containing Ketoprofen

  • Arthrosylene ®
  • Fastum gel ®
  • Flexen "Retard" ®
  • Ketodol ®
  • Oki ®
  • Orudis ®

Indications

For what it uses

The use of ketoprofen is indicated for the symptomatic treatment of:

  • Inflammatory and painful states caused by trauma;
  • Rheumatic pain and inflammation;
  • neuralgia;
  • Menstrual cramps;
  • Headache;
  • Rheumatoid arthritis;
  • Ankylosing spondylitis;
  • Painful osteoarthritis;
  • Extra-articular rheumatism;
  • Osteoarthritis;
  • Tendinitis and tenosynovitis;
  • Capsulitis and bursitis;
  • Backache and sciatica;
  • Acute gout;
  • Post-operative pain;
  • Neoplastic pain.

Warnings

Ketoprofen can cause perforation, ulceration and gastrointestinal bleeding. Therefore, should any gastrointestinal symptom appear, it is necessary to immediately inform the doctor. It is important to note that ketoprofen is able to induce a greater gastrointestinal toxicity than other NSAIDs.

In patients in whom there is a greater risk of gastrointestinal damage, concomitant therapy with gastroprotective drugs may be considered.

Should any type of allergic reaction occur during treatment with ketoprofen, treatment with the drug should be immediately suspended and the doctor should be contacted immediately.

Furthermore, before starting treatment with ketoprofen, you must inform your doctor if you are in one of the following conditions:

  • If you are suffering from heart disease;
  • If you have ulcerative colitis or Crohn's disease;
  • If you have a history (even family history) of hypertension and / or congestive heart failure;
  • If you are suffering from liver disease or liver cirrhosis;
  • If you are suffering from nephrosis;
  • If you have asthma associated with chronic rhinitis, chronic sinusitis and / or nasal polyposis.

Finally, ketoprofen could cause side effects that could alter the ability to drive and / or use machinery, so great care should be taken.

Interactions

Concomitant administration of ketoprofen and the following drugs is not recommended due to the dangerous side effects that may occur;

  • Other NSAIDs ;
  • Oral anticoagulants (such as, for example, warfarin and heparin);
  • Antiplatelet agents (such as, for example, clopidogrel and ticlopidine);
  • Lithium (a drug used to treat bipolar disorder);
  • Methotrexate (an anticancer).

Concomitant administration of ketoprofen and the following drugs, on the other hand, should be carried out with great caution:

  • Antihypertensive drugs;
  • Corticosteroids ;
  • Pentoxifylline (an antithrombotic);
  • Thrombolytic drugs;
  • Probenecid (an anti-gout drug);
  • SSRIs (selective serotonin reuptake inhibitors, antidepressant drugs);
  • Phenytoin (an anti-epileptic);
  • Sulfonamides (antibiotic drugs);
  • Ciclosporin and tacrolimus (immunosuppressive drugs);
  • Zidovudine (used in the treatment of HIV);
  • Sulfonylureas (drugs used against diabetes).

In any case, it is still advisable to inform your doctor if you are taking - or if you have recently been - drugs of any kind, including medicines without a prescription and herbal and homeopathic products.

Side effects

Ketoprofen can cause different types of side effects, although not all patients experience them. The type of adverse effects and the intensity with which they occur depend on the sensitivity that each individual has towards the drug.

The main side effects that may occur during treatment with ketoprofen are listed below.

Blood and lymphatic system disorders

Ketoprofen therapy can promote the onset of:

  • Hemorrhagic anemia;
  • Leukopenia, ie the decrease in the number of leukocytes in the bloodstream;
  • Piastrinopenia, ie the decrease in the number of platelets in the blood;
  • Agranulocytosis, ie the decrease in the number of granulocytes in the bloodstream.

Gastrointestinal disorders

Treatment with ketoprofen can lead to:

  • Nausea;
  • He retched;
  • Dyspepsia;
  • Abdominal pain;
  • Diarrhea or constipation;
  • Flatulence;
  • Gastritis;
  • Melena;
  • Hematemesis;
  • Peptic ulcer;
  • Gastrointestinal perforation and hemorrhage;
  • Exacerbation of colitis and Crohn's disease in patients suffering from it.

Cardiovascular disorders

Ketoprofen therapy can cause heart failure, hypertension and vasodilation.

Kidney and urinary tract disorders

Treatment with ketoprofen can cause:

  • Acute renal failure;
  • Alterations in renal function tests;
  • Tubulo-interstitial nephritis;
  • Nephritic syndrome.

Skin and subcutaneous tissue disorders

Ketoprofen therapy may cause:

  • Skin rash;
  • Itch;
  • Photosensitivity reactions;
  • Urticaria;
  • Alopecia;
  • Rash;
  • Stevens-Johnson syndrome;
  • Toxic epidermal necrolysis.

Nervous system disorders

Treatment with ketoprofen can promote the onset of:

  • Headache;
  • Dizziness;
  • paresthesia;
  • Drowsiness;
  • Alteration of the sense of taste;
  • Convulsions.

Hepatobiliary disorders

Ketoprofen therapy can cause an increase in blood levels of liver enzymes and may promote the occurrence of hepatitis and jaundice.

Other side effects

Other side effects that may occur during treatment with ketoprofen are:

  • Allergic reactions, even serious, in sensitive individuals;
  • Angioedema;
  • Edema;
  • Tinnitus;
  • Blurred vision;
  • Mouth ulcers;
  • Increased body weight;
  • Mood changes;
  • Asthma;
  • bronchospasm;
  • Rhinitis.

Overdose

The symptoms that can occur in case of ketoprofen overdose are:

  • Nausea and vomit;
  • Diarrhea;
  • Headache;
  • Dizziness;
  • Drowsiness;
  • Abdominal pain.

Hypotension, respiratory depression and gastrointestinal bleeding have also been reported in case of very serious poisoning.

There is no specific antidote against ketoprofen overdosage, therefore, the treatment is only symptomatic and supportive.

In any case, if you suspect you have taken an overdose of medication, you must contact your doctor immediately or contact your nearest hospital.

Action mechanism

Ketoprofen is a non-steroidal anti-inflammatory drug and - as such - carries out its anti-inflammatory and analgesic action by inhibiting cyclooxygenase (or COX).

Cyclooxygenase is an enzyme of which three different isoforms are known: COX-1, COX-2 and COX-3.

COX-1 is a constitutive isoform, normally present in cells and involved in the mechanisms of cellular homeostasis.

COX-2, on the other hand, is an inducible isoform that is produced by inflammatory cells (inflammatory cytokines) activated.

The task of these enzymes is to convert the arachidonic acid present in our body into prostaglandins, prostacyclines and thromboxanes.

Prostaglandins - and especially prostaglandins G2 and H2 (respectively PGG2 and PGH2) - are involved in inflammatory processes and mediate pain responses. While prostaglandins E (PGE) induce an increase in body temperature, therefore, they induce fever.

Therefore, with the inhibition of COX-2 activity, ketoprofen prevents the synthesis of prostaglandins responsible for inflammation and pain.

However, ketoprofen is not selective for COX-2, therefore it is also able to inhibit COX-1. This latter inhibition is at the origin of some of the side effects typical of all non-selective NSAIDs (such as gastrointestinal side effects).

Furthermore, ketoprofen also exerts an antagonistic action against bradykinin, a neurotransmitter released during inflammatory processes responsible for activating peripheral pain receptors.

Finally, ketoprofen is also able to inhibit the synthesis of leukotrienes (molecules implicated in inflammatory processes) and to reduce the migration of leukocytes to inflamed joints.

Mode of Use - Posology

As mentioned, ketoprofen is available in different pharmaceutical formulations suitable for different administration routes. More precisely, the drug is available for:

  • Oral administration in the form of tablets, hard capsules, soft capsules, powder or granules for oral solution, oral drops and effervescent granules.
  • Topical administration in the form of skin foam, cream, skin spray, gel, cutaneous solution and medicated plaster (these formulations should only be applied to the skin) and in the form of oral mucosa spray and mouthwash (to be used only on the oral mucosa).
  • Rectal administration in the form of suppositories.
  • Intravenous or intramuscular administration in the form of a solution for injection or powder and solvent for solution for injection which must be mixed just before using the drug.

To avoid the occurrence of dangerous side effects, during treatment with ketoprofen, it is essential to scrupulously follow the indications provided by the doctor, both as regards the amount of drug to be used, both as regards the frequency of administration and the duration of the same treatment.

Below are some indications on the doses of ketoprofen usually used in therapy. However, to know the exact posology of each pharmaceutical formulation, see the illustrative leaflets of the individual medicinal products.

Oral administration

When ketoprofen is administered orally, the dose usually used in adults ranges from 25 mg to 200 mg of drug, depending on the severity of the pain and inflammation.

The frequency of administration depends on the amount of drug taken, since in no case should the maximum daily dose of 200 mg of ketoprofen be exceeded.

Topical administration

When using ketoprofen for cutaneous use in the form of cream, gel, spray, solution or skin foam, generally, it is recommended to carry out 1-3 applications a day, according to medical prescription.

When, on the other hand, ketoprofen is used in the form of a medicated plaster, it is advisable to apply only one patch at a time, unless otherwise prescribed by the doctor.

It is very important to remember that when using ketoprofen for cutaneous use, the treated part must not be exposed to sunlight and UV rays, both during the treatment and for a period of at least two weeks from the end of the same. This is due to the photosensitivity reactions that can occur.

When using ketoprofen-based oral mucosa spray, the recommended dose is 1-2 sprays up to three times a day.

When using ketoprofen based mouthwash, however, it is advisable to rinse twice a day.

Rectal administration

When ketoprofen is used in the form of suppositories, the recommended daily dose varies from 100 to 200 mg of active ingredient per day.

Also in this case - as for oral administration - the maximum dose of 200 mg of ketoprofen per day should never be exceeded.

Parenteral administration

When using the ketoprofen-based solution for injection, the usual dose of the drug is 100-200 mg a day, to be administered intravenously or intramuscularly.

Pregnancy and breastfeeding

Generally, the use of ketoprofen is not recommended during the first and second trimester of pregnancy, however, if the doctor considers it absolutely necessary, he can still decide to prescribe it.

The use of the drug in the third trimester of pregnancy, on the other hand, is contraindicated due to the damage that ketoprofen itself can cause to the fetus (cardiopulmonary toxicity, renal dysfunction and prolongation of bleeding time after birth) and to the mother (extension of time of bleeding and inhibition of uterine contractions, with consequent delay or prolongation of labor).

The use of ketoprofen is also contraindicated in mothers who are breast-feeding.

Furthermore, the drug negatively affects female fertility, therefore it should not be taken by women who intend to become pregnant.

Contraindications

The use of ketoprofen is contraindicated in the following cases:

  • In patients with known hypersensitivity to the same ketoprofen;
  • In patients with known hypersensitivity to acetylsalicylic acid or to other NSAIDs;
  • In patients with peptic ulcers;
  • In patients who have suffered from gastrointestinal bleeding, ulceration or perforation or who have suffered from chronic dyspepsia;
  • In patients with gastritis;
  • In patients with severe heart failure;
  • In patients with hepatic and / or renal insufficiency;
  • In patients with severe coagulation disorders;
  • In patients with pre-existing leukopenia and / or thrombocytopenia;
  • In patients who have recently suffered from proctitis or in patients suffering from hemorrhoid disorders;
  • In the last trimester of pregnancy;
  • During breastfeeding.

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