Ketoprofen, gel 2.5% 30 g

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID).

ATX code: M02AA10

Pharmacological properties

Pharmacodynamics

Ketoprofen, a derivative of propionic acid, has a local anti-inflammatory and analgesic effect. Inhibits the activity of cyclooxygenase-1 and cyclooxygenase-2 enzymes involved in the synthesis of prostaglandins (PG). Ketoprofen penetrates through the skin and reaches the center of inflammation, thus providing the possibility of local treatment of lesions (joints, tendons, ligaments and muscles) accompanied by pain syndrome.

Pharmacokinetics

It is slowly absorbed through the skin when applied topically and almost does not cumulate. The bioavailability of the gel is about 5%. After administration in a dose of 50-150 mg, plasma concentration after 5-8 hours is 0.08-0.15 mcg/ml. Binding to plasma proteins is approximately 99%. Metabolized by conjugation to glucuronic acid. No active metabolites are formed. Half-life period is 1-3 hours. It is excreted through the kidneys as a conjugated metabolite.

Indications

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.

Pharmacological effect

Pharmacotherapeutic group: non-steroidal anti-inflammatory drug (NSAID).

ATX code: M02AA10

Pharmacological properties

Pharmacodynamics

Ketoprofen is a propionic acid derivative that has a local anti-inflammatory and analgesic effect. Suppresses the activity of the enzymes cyclooxygenase-1 and cyclooxygenase-2 involved in the synthesis of prostaglandins (PG). Ketoprofen penetrates the skin, reaches the source of inflammation, thus providing the possibility of local treatment of lesions (joints, tendons, ligaments and muscles) accompanied by pain.

Pharmacokinetics

When applied topically, it is slowly absorbed through the skin and practically does not accumulate. The bioavailability of the gel is about 5%. After use at a dose of 50-150 mg, the plasma concentration after 5-8 hours is 0.08-0.15 mcg/ml. Plasma protein binding is approximately 99%. Metabolized by conjugation with glucuronic acid. No active metabolites are formed. The half-life is 1-3 hours. It is excreted through the kidneys in the form of a conjugated metabolite.

Special instructions

After applying the gel to the skin, you must wash your hands thoroughly. It is unacceptable to apply the gel to damaged (open wounds) and inflamed skin. Contact with the mucous membranes of the eyes should be avoided (risk of irritation of the conjunctiva). Should not be used with an occlusive dressing. Do not use sealed clothing when using Ketoprofen-Teva.

Long-term use of a topical product may result in increased sensitivity or local irritation. To avoid any manifestations of hypersensitivity or photosensitivity, exposure to sunlight should be avoided during the treatment period and 2 weeks after the end of treatment. It is recommended to cover the skin areas treated with the drug with clothing.

Caution should be exercised when using Ketoprofen-Teva in patients with severe renal failure.

You should stop using Ketoprofen-Teva 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, in very rare cases, systemic side effects may develop (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.

Impact on the ability to drive vehicles and machinery

The drug does not affect the ability to drive a car or use machinery.

Active ingredient

Ketoprofen

Composition

100 g of the drug contains: active ingredient ketoprofen 2,500 g; excipients: carbomer (carbopol 980) – 2,000 g, ethanol 96% – 28,500 g, lavender flavor – 0.028 g, triethanolamine – 3,700 g (up to pH 6.5), purified water – up to 100 g.

Pregnancy

Since NSAIDs that inhibit PG synthesis are known to have an adverse effect on the fetal cardiopulmonary system (pulmonary hypertension, premature closure of the ductus arteriosus), as well as on renal function (renal failure, combined with oligohydramnios), the use of ketoprofen should be avoided during pregnancy. There are no adequate and strictly controlled clinical studies in pregnant women. Use during pregnancy is contraindicated.

Women planning pregnancy should refrain from using ketoprofen, because taking it may reduce the likelihood of egg implantation.

It is not known whether ketoprofen is excreted in breast milk, therefore it is not recommended to use ketoprofen during breastfeeding.

Contraindications

Hypersensitivity to ketoprofen and other components of the drug, acetylsalicylic acid or other NSAIDs (history of bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid), to tiaprofenic acid, fenofibrate;
a history of increased skin sensitivity to solar radiation (photosensitivity);
history of skin allergies to ketoprofen, tiaprofenic acid, fenofibrate, sunscreens or perfumes;
complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (history);
exposure to the sun on treated areas, including solariums, during use of the drug and 2 weeks after;
weeping dermatoses, eczema, infected abrasions, wounds at the site of application of the gel; pregnancy and breastfeeding;
children under 12 years of age (no data on effectiveness and safety).

With caution

Severe renal failure, hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe liver dysfunction, chronic heart failure, bronchial asthma, old age.

Side Effects

Possible side effects are classified according to the following frequency: very often (≥ 10%), often (≥ 1%, < 10%); uncommon (≥ 0.1%, < 1%); rare (≥ 0.01%, < 0.1%); very rare (<0.01%).

From the skin: infrequently – skin itching, erythema, 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.

Interaction

Interaction of ketoprofen with other drugs is unlikely, because when used externally by applying to the surface of the skin, the concentration of ketoprofen in the blood plasma is very low. The effect of drugs that cause photosensitivity may be enhanced. No other interactions have been established. However, patients taking coumarin anticoagulants are advised to regularly monitor their international normalized ratio.

Overdose

The extremely low systemic absorption of ketoprofen when applied externally makes overdose almost impossible. If a large amount of the drug is accidentally ingested, systemic side effects may occur.
Treatment should be symptomatic.

Storage conditions

Store at a temperature not exceeding 25°C.
Keep out of the reach of children!

Shelf life

3 years.
Do not use after expiration date.

Manufacturer

Chemineau Laboratories, France