Bystrumgel (Gel) Instructions for Use

Marketing Authorization Holder

Akrikhin Chemical and Pharmaceutical Plant, JSC (Russia)

Contact Information

AKRIKHIN JSC (Russia)

ATC Code

M02AA10 (Ketoprofen)

Active Substance

Ketoprofen (Rec.INN registered by WHO)

Dosage Form

Bystrumgel

Gel for external use 2.5%: tubes 30 g, 50 g or 100 g

Dosage Form, Packaging, and Composition

Gel for external use colorless, almost transparent, with a specific odor; opalescence is allowed.

Excipients: ethanol (rectified ethyl alcohol), carbomer 940 or 980, trometamol, methylparahydroxybenzoate (nipagin), lavender oil, orange blossom oil (neroli oil), purified water.

30 g – aluminum tubes (1) – cardboard packs.
50 g – aluminum tubes (1) – cardboard packs.
100 g – aluminum tubes (1) – cardboard packs.

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

Drugs for external use for muscle and joint pain; non-steroidal anti-inflammatory drugs for external use

Pharmacological Action

Ketoprofen is one of the most effective COX inhibitors. It also inhibits the activity of lipoxygenase and bradykinin. It stabilizes lysosomal membranes and prevents the release of enzymes involved in the inflammatory process.

The main properties of ketoprofen are analgesic, anti-inflammatory and anti-edema effects.

In back pain and ligament injuries, the analgesic effect of ketoprofen appears 15-30 minutes after application of the gel.

Ketoprofen does not have a negative effect on the condition of the articular cartilage.

Pharmacokinetics

Absorption and distribution

Ketoprofen does not accumulate in the body when applied topically as a gel. The bioavailability of the gel is about 5%. It penetrates into joint tissues, including the synovial fluid, and reaches therapeutic concentrations there. The concentration of the drug in blood plasma is extremely low.

Metabolism and excretion

Ketoprofen is metabolized in the liver to form conjugates, which are excreted mainly by the kidneys. The metabolism of ketoprofen does not depend on age, the presence of severe renal failure or liver cirrhosis. The excretion of ketoprofen by the kidneys is slow.

Indications

Symptomatic therapy – reduction of pain and inflammation at the time of use (does not affect the progression of the disease) – for the following conditions

• Joint pain in reactive arthritis (Reiter’s syndrome);
• Back and joint pain in osteoarthritis of various locations;
• Inflammation and swelling of soft tissues and joints in periarthritis, tendinitis, bursitis, muscle pain (myalgia), neuralgia, back pain in radiculitis;
• Inflammation and swelling of soft tissues and joints, pain in injuries of the musculoskeletal system (including sports injuries), muscle and ligament bruises, sprains, ligament and muscle tendon ruptures.

ICD codes

Dosage Regimen

For external use.

A small amount of gel (3-5 cm) is applied in a thin layer to the skin of the inflamed or painful area of the body 1-2 times/day and gently rubbed in.

The dose should be selected according to the area of the affected area: 5 cm of gel corresponds to 100 mg of ketoprofen, 10 cm – 200 mg of ketoprofen.

The maximum dose of ketoprofen is 200 mg/day.

Occlusive dressing is not recommended.

Do not use without consulting a doctor for more than 14 days.

If the patient forgot to apply the gel, it should be applied at the time when the next dose is due, but the dose should not be doubled.

Adverse Reactions

Definition of categories of frequency of adverse effects (according to WHO): very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1000), very rare (<1/10,000); frequency unknown - it was not possible to estimate the frequency from the available data.

Immune system disorders: frequency unknown – hypersensitivity reactions, anaphylactic shock, angioedema (Quincke’s edema).

Gastrointestinal disorders: very rare – peptic ulcer, bleeding, diarrhea.

Skin and subcutaneous tissue disorders: uncommon – local skin reactions such as erythema, eczema, itching and burning; rare – photosensitivity reactions, urticaria.

Rare reports of more severe reactions, such as bullous or phlyctenular eczema, which may spread beyond the application site or become generalized.

Renal and urinary disorders: very rare – deterioration of renal function in patients with chronic renal failure.

If any side effects occur, it is necessary to stop using the drug and consult a doctor.

Contraindications

• Hypersensitivity to ketoprofen or other components of the drug, as well as to salicylates, tiaprofenic acid or other NSAIDs, fenofibrate;
• History of skin allergy to sunscreens and perfumes;
• Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in history);
• III trimester of pregnancy;
• Children under 15 years of age;
• Violation of the integrity of the skin in the area of gel application (eczema, acne, weeping dermatitis, open or infected wound);
• History of photosensitivity reactions;
• Exposure to sunlight, including indirect sunlight and UV radiation in a solarium throughout the entire treatment period and for another 2 weeks after stopping treatment with the drug.

With caution impaired liver and/or kidney function; erosive and ulcerative lesions of the gastrointestinal tract; blood diseases; bronchial asthma; chronic heart failure; hepatic porphyria (exacerbation).

Use in Pregnancy and Lactation

Since the safety of ketoprofen use in pregnant women has not been evaluated, the use of ketoprofen in the I and II trimesters of pregnancy should be avoided.

The drug is contraindicated in the III trimester of pregnancy. In the III trimester of pregnancy, all prostaglandin synthetase inhibitors, including Ketoprofen, can have a toxic effect on the heart, lungs and kidneys of the fetus.

At the end of pregnancy, an increase in bleeding time in the mother and child is possible. NSAIDs may delay the onset of labor.

To date, there are no data on the excretion of ketoprofen in breast milk, so the use of the drug during breastfeeding is not recommended.

Use in Hepatic Impairment

The drug should be used with caution in case of impaired liver function.

Use in Renal Impairment

The drug should be used with caution in case of impaired renal function.

Pediatric Use

The use of the drug is contraindicated in children under 6 years of age.

Special Precautions

Avoid contact of the gel with the eyes, skin around the eyes, and mucous membranes.

If skin reactions occur, including those developed with the simultaneous use of octocrylene-containing drugs, treatment should be stopped immediately.

Patients suffering from bronchial asthma in combination with chronic rhinitis, chronic sinusitis and/or nasal or paranasal sinus polyposis have a higher risk of developing allergic reactions when using aspirin and/or NSAIDs than the rest of the population.

To reduce the risk of photosensitivity, it is recommended to protect the skin areas treated with the gel with clothing from exposure to UV radiation throughout the entire treatment period and for another 2 weeks after discontinuation of use.

The recommended duration of treatment should not be exceeded due to the increased risk of contact dermatitis and photosensitivity reactions over time.

Hands should be washed thoroughly after each application of the drug.

Effect on the ability to drive vehicles and mechanisms

There are no data on the negative effect of the drug on the ability to drive vehicles and engage in other potentially hazardous activities that require concentration and speed of psychomotor reactions.

Overdose

Overdose is unlikely with external use of the drug.

Symptoms in case of ingestion of the drug, systemic adverse reactions may develop.

Treatment in case of overdose, the skin should be thoroughly washed with running water. In case of ingestion of the drug, symptomatic treatment and supportive therapy are necessary, as in case of overdose of ketoprofen in oral dosage forms.

Drug Interactions

With external use of ketoprofen in the form of a gel, it is possible to enhance the effect of drugs that cause photosensitization.

Patients taking coumarin anticoagulants are recommended to regularly monitor INR.

Ketoprofen, like other NSAIDs, may reduce the excretion of methotrexate and contribute to an increase in its toxicity.

Interaction with other drugs and the effect on their excretion are not significant.

Storage Conditions

The drug should be stored out of the reach of children at a temperature from 15°C (59°F) to 25°C (77°F).

Shelf Life

Shelf life – 2 years. Do not use after the expiration date.

Dispensing Status

The drug is available without a prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.