Pentalgin^® extra-gel (Gel) Instructions for Use

Marketing Authorization Holder

Otisipharm, JSC (Russia)

Manufactured By

Lekko, CJS (Russia)

ATC Code

M02AA10 (Ketoprofen)

Active Substance

Ketoprofen (Rec.INN registered by WHO)

Dosage Form

Pentalgin® extra-gel

Gel for external use 5%: tubes 30 g, 50 g, or 100 g

Dosage Form, Packaging, and Composition

Gel for external use from yellowish to reddish-brown in color, transparent or semi-transparent, homogeneous, with a characteristic odor; the presence of opalescence and air bubbles is allowed.

Excipients: Capsicum fruit tincture – 40 mg, Dimethyl sulfoxide – 30 mg, Camphor – 30 mg, Peppermint leaf oil – 9 mg, Carbomer type A – 15 mg, Diisopropanolamine – 46.3 mg, Ethanol (ethyl alcohol) 95% – 350 mg, Purified water – up to 1000 mg.

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

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

Nonsteroidal anti-inflammatory drug for topical use

Pharmacological Action

NSAID. When applied topically, it has an analgesic, anti-inflammatory, and anti-edematous effect.

The mechanism of action is associated with the suppression of the activity of COX-1 and COX-2 enzymes, which regulate the synthesis of prostaglandins.

When used as a gel, it provides a local therapeutic effect on the affected joints, tendons, ligaments, and muscles.

In joint syndrome, it reduces joint pain at rest and during movement, morning stiffness, and joint swelling. It does not have a damaging effect on articular cartilage.

Pharmacokinetics

When applied topically as a gel, it penetrates into the site of inflammation through the skin and is absorbed from the site of inflammation extremely slowly and practically does not accumulate in the body.

The bioavailability of ketoprofen is about 5%. After external application in a dose of 50-150 mg, the plasma concentration after 5-8 hours is 0.08-0.15 µg/ml.

Indications

• Acute and chronic inflammatory diseases of the musculoskeletal system (inflammatory lesions of ligaments and tendons, osteoarthritis, osteochondrosis with radicular syndrome, radiculitis, bursitis, sciatica, lumbago, joint syndrome during exacerbation of gout);
• Muscle pain of rheumatic and non-rheumatic origin;
• Post-traumatic inflammation of soft tissues and the musculoskeletal system (ligament injuries and ruptures, contusions).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use; it does not affect the progression of the disease.

ICD codes

Dosage Regimen

The drug is intended for external use only.

Apply the gel to clean, dry, intact skin.

Apply a small amount of gel, a strip of 3-5 cm, to the affected area.

Gently rub in a thin layer until completely absorbed.

Apply the gel 2-3 times per day.

The maximum duration of continuous treatment is 14 days.

Do not apply to open wounds, mucous membranes, or eyes.

Avoid the use of occlusive dressings.

After application, wash hands thoroughly.

Avoid exposing treated skin areas to direct sunlight or UV radiation (e.g., solarium) during treatment and for two weeks after the last application.

Discontinue use and consult a physician if skin irritation or any adverse reactions occur.

Adverse Reactions

Adverse reactions are listed indicating the frequency of occurrence according to the WHO classification: very common (≥1/10), common (≥1/100 but <1/10), uncommon (≥1/1000 but <1/100), rare (≥1/10,000 but <1/1000), very rare (<1/10,000, including isolated reports), frequency unknown (cannot be estimated from the available data).

Skin and subcutaneous tissue disorders uncommon – erythema, pruritus, eczema; rare – photosensitivity, bullous dermatitis, urticaria; very rare – contact dermatitis, angioedema.

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

Immune system disorders very rare – anaphylactic reactions, hypersensitivity reactions.

Renal and urinary disorders very rare – worsening of renal failure.

If these or other side effects occur, the patient should stop using the drug and consult a doctor.

Contraindications

• Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including history);
• History of increased skin sensitivity to solar radiation (photosensitivity);
• History of skin allergy to sunscreens or perfumes;
• Exposure of the treated areas to sunlight, including solarium, during the course of drug application and for 2 weeks after;
• Damage to the skin (weeping dermatoses, eczema, infected abrasions, wounds) at the intended site of application;
• Third trimester of pregnancy;
• Breastfeeding period;
• Age under 18 years.
• Hypersensitivity to acetylsalicylic acid or other NSAIDs (history of bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid), tiaprofenic acid and fenofibrate;
• Individual hypersensitivity to ketoprofen or other components of the drug.

With caution erosive and ulcerative lesions of the gastrointestinal tract, severe impairment of renal and liver function, hepatic porphyria, chronic heart failure, bronchial asthma, elderly age, first and second trimesters of pregnancy.

Use in Pregnancy and Lactation

The use of the drug is contraindicated in the third trimester of pregnancy. In the first and second trimesters of pregnancy, the use of the drug is possible only after consultation with a doctor, if the intended benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to use the drug during breastfeeding, breastfeeding should be discontinued.

Use in Hepatic Impairment

The drug should be used with caution in severe liver impairment, hepatic porphyria.

Use in Renal Impairment

The drug should be used with caution in severe renal impairment.

Pediatric Use

The use of the drug is contraindicated under the age of 18 years.

Geriatric Use

The drug should be used with caution in elderly patients.

Special Precautions

The gel should be applied only to intact skin areas, avoiding contact with open wounds, eyes, and mucous membranes.

After applying the drug, wash your hands.

The formation of a transparent film on the skin at the site of gel application is allowed.

Do not use with occlusive dressings.

Can be used with phonophoresis.

Long-term use of topical agents can lead to increased sensitivity and the appearance of skin irritation symptoms at the application site.

To avoid manifestations of photosensitivity, it is recommended to avoid exposure of the skin to direct sunlight during the course of treatment, as well as for 2 weeks after the last application of the drug (including not visiting a solarium).

With long-term use of the drug in large quantities, in very rare cases, systemic side effects may occur (hypersensitivity reactions, gastrointestinal disorders, worsening of renal failure).

Patients with severe renal, cardiac, or hepatic insufficiency should use ketoprofen with caution.

The risk of systemic side effects increases depending on the amount of gel applied, the area of the treated skin area, the condition of the skin, and the duration of use.

The use of the drug should be discontinued in case of any skin reaction, including reactions when simultaneously applying sunscreens or other cosmetic products containing the organic sunscreen filter octocrylene.

Effect on ability to drive vehicles and operate machinery

The drug does not affect the ability to drive vehicles and work with machinery.

Overdose

In case of accidental use of the drug in a dose exceeding the recommended one, the risk of developing overdose symptoms is minimal due to the extremely low systemic absorption of ketoprofen when applied externally.

Treatment if local side effects appear, the drug should be discontinued and the application site should be washed. If large amounts of the gel are accidentally swallowed, systemic adverse reactions characteristic of NSAIDs may occur. Gastric lavage and activated charcoal intake are necessary.

Drug Interactions

The drug may enhance the effect of drugs that cause photosensitivity.

Despite the insignificant degree of absorption of ketoprofen through the skin, with frequent and prolonged use, symptoms of interaction with other drugs may appear (the same as with systemic use).

When used concomitantly with other NSAIDs, corticosteroids, ethanol, and corticotropin, the formation of ulcers in the gastrointestinal tract and the development of gastrointestinal bleeding are possible.

Patients taking coumarin anticoagulants are recommended to regularly monitor INR.

When used concomitantly, Ketoprofen enhances the toxicity of methotrexate.

The excipient dimethyl sulfoxide included in the composition enhances the penetration of drugs through the skin.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf Life

The shelf life is 2 years. Do not use after the expiration date printed on the package.

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.