Valusal^® (Gel) Instructions for Use

Marketing Authorization Holder

Grindeks, JSC (Latvia)

Manufactured By

Tallinn Pharmaceutical Plant, JSC (Estonia)

Or

Grindeks, JSC (Latvia)

ATC Code

M02AA10 (Ketoprofen)

Active Substance

Ketoprofen (Rec.INN registered by WHO)

Dosage Form

Valusal®

Gel for external use 2.5%: tube 50 g

Dosage Form, Packaging, and Composition

Gel for external use transparent or slightly cloudy, colorless or with a yellowish tint, with a specific odor.

Excipients : ethanol 96% – 339 mg, carbomer – 20 mg, diethanolamine – 20 mg, lavender oil – 0.88 mg, methylparaben – 0.8 mg, orange oil – 0.46 mg, propylparaben – 0.2 mg, purified water – up to 1 g.

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

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

NSAID

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.

Ketoprofen has analgesic, anti-inflammatory, and anti-edematous effects. It 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%. The C_max of ketoprofen in blood plasma is reached 6 hours after application of the drug. It penetrates into joint tissues, including 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 – to reduce pain and inflammation at the time of use (does not affect the progression of the disease) for the following diseases and conditions

• Diseases of the musculoskeletal system (osteoarthritis, osteochondrosis with radicular syndrome, radiculitis, inflammatory lesions of ligaments, tendons, lumbago, bursitis, sciatica);
• Injuries of the musculoskeletal system (including sports injuries), muscle and ligament contusions, ligament sprains, ligament and muscle tendon ruptures, post-traumatic inflammation of soft tissues;
• Muscle pain of rheumatic and non-rheumatic origin.

If necessary, before using the drug, the patient should consult a doctor.

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 corresponds to 200 mg of ketoprofen.

If necessary, the gel can be combined with other dosage forms of ketoprofen (capsules, tablets, rectal suppositories, solution for intramuscular injection).

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.

If improvement does not occur after treatment or new symptoms appear, the patient should consult a doctor.

The drug should be used in accordance with the recommended method of application and dosage regimen. If necessary, before using the drug, the patient should consult a doctor.

Adverse Reactions

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

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

Gastrointestinal system 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 area or become generalized.

Urinary system disorders very rare – deterioration of renal function in patients with chronic renal failure.

If any of the indicated adverse effects worsen, or the patient notices any other adverse effects, he/she should inform the 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);
• 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;
• III trimester of pregnancy;
• Children under 15 years of age;
• Exposure to sunlight, including indirect sunlight and UV radiation in a solarium throughout the entire treatment period and for another 2 weeks after discontinuation of the drug.

With caution

Before using Valusal^® gel, the patient should consult a doctor in the following cases

• Impaired liver and/or kidney function;
• Erosive and ulcerative lesions of the gastrointestinal tract;
• Blood diseases;
• Bronchial asthma;
• Chronic heart failure;
• Hepatic porphyria.

Use in Pregnancy and Lactation

The drug Valusal^® is contraindicated in the III trimester of pregnancy.

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

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 Valusal^® during breastfeeding is not recommended.

Pediatric Use

Contraindication: children under 15 years of age.

Special Precautions

Avoid getting the gel into the eyes, on the skin around the eyes, and mucous membranes.

If skin reactions occur, including those developed with the concomitant 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 UV exposure 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. If systemic adverse reactions develop, symptomatic and supportive therapy should be carried out, as in case of overdose of oral dosage forms.

Drug Interactions

With external use of ketoprofen in the form of a gel, the effect of drugs that cause photosensitization may be enhanced.

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 not exceeding 25°C (77°F). Do not freeze.

Shelf Life

Shelf life – 2 years.

Precautions when disposing of unused medicines

Medicines should not be disposed of in the sewer or with household waste.

Dispensing Status

The drug is dispensed 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.