Pentalgin extra-gel for external use 5%, 50g

Composition

Active ingredient:

• ketoprofen – 50.0 mg.

Auxiliary substances:

• the fruit of capsicum tincture (of Cayenne pepper tincture) – 40,0 mg,
• dimethyl sulfoxide (dimexide) was 30.0 mg,
• camphor – 30,0 mg
• peppermint leaf oil (peppermint oil) – 9.0 mg,
• hypromellose – 20,0 mg,
• sodium hydroxide – 7.5 mg,
• ethanol 96% – to 350.0 mg,
• purified water – to 1000.0 mg.

Pharmacological properties

Pharmacotherapeutic group: non-steroidal anti-inflammatory agent for topical use.

ATX code: M 02 AA 10

Pharmacological properties

Pharmacodynamics

Ketoprofen is a non-steroidal anti-inflammatory drug that, when applied topically, has analgesic, anti-inflammatory and decongestant effects. The mechanism of action is associated with the suppression of the activity of cyclooxygenase 1 and cyclooxygenase 2 enzymes that regulate prostaglandin synthesis.

When applied as a gel, it provides a local therapeutic effect on affected joints, tendons, ligaments, and muscles. In joint syndrome, it reduces joint pain at rest and during movement, morning stiffness and joint swelling. It has no damaging effect on the articular cartilage.

The tincture and camphor included in the excipients of capsicum fruits can have a slight warming effect at the application site.

Dimethyl sulfoxide, which is part of the excipients, enhances the penetration of drugs through the skin.

Pharmacokinetics

When applied topically as a gel, it penetrates the inflammatory focus through the skin and is absorbed from the inflammatory focus extremely slowly and practically does not accumulate in the body. Bioavailability of ketoprofen is about 5%. After external use at a dose of 50-150 mg, the plasma concentration after 5-8 hours is 0.08-0.15 mcg / ml.

Indications

• Acute and chronic inflammatory diseases of musculoskeletal system (inflammation of ligaments and tendons, osteoarthritis, osteochondrosis with radicular syndrome, sciatica, bursitis, sciatica, lumbago, articular syndrome with exacerbation of gout);
• muscle pain of rheumatic and non-rheumatic origin;
• post-traumatic inflammation of soft tissue and musculoskeletal system (damage and torn 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.

Use during 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 consulting a doctor, if the intended benefit to the mother exceeds the potential risk to the fetus.

If you need to use the drug during breastfeeding, you should stop breastfeeding.

Contraindications

• Individual hypersensitivity to ketoprofen or other components of the drug;
• hypersensitivity to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs (NSAIDs) (a history of bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid), thiaprofenic acid and fenofibrate; 
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid or other NSAIDs (including in the anamnesis);
• -hypersensitivity of the skin to sunlight (photosensitivity) in history;
• skin Allergy in the history of sunscreen or perfume;
• the impact of sunlight on treated areas, including Solarium, during the course of treatment and 2 weeks after; 
• damage to the skin (wet dermatoses, eczema, infected abrasions, wounds) at the site of the intended application;
• pregnancy (third trimester), breastfeeding;
• children under 18 years of age.

With caution

Erosive and ulcerative lesions of the gastrointestinal tract, severe renal and hepatic dysfunction, hepatic porphyria, chronic heart failure, bronchial asthma, old age, pregnancy (I and II trimester).

If you have any of these diseases / conditions, please consult your doctor before taking this medicine.

Side effects

Adverse reactions are listed with an indication of the frequency of occurrence according to the WHO classification: very common (with a frequency of more than 1/10), common (with a frequency of at least 1/100, but less than 1/10), infrequent (with a frequency of at least 1/1000, but less than 1/100), rare (with a frequency of at least 1/10000, but less than 1/1000), very rare (with a frequency of less than 1/10000, including isolated reports), frequency unknown (cannot be determined from available data).

From the side of the skin:  

infrequently: erythema, pruritus, eczema; rarely: photosensitization, bullous dermatitis, urticaria; very rarely: contact dermatitis, angioedema.

From the gastrointestinal tract:  

very rare: peptic ulcer, bleeding, diarrhea.

From the immune system:  

very rare: anaphylactic reactions, hypersensitivity reactions.

From the urinary system:

very rare: worsening of the course of renal failure.

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

Interaction

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

Despite the low 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 combined with other NSAIDs, glucocorticoids, ethanol, corticotropin, ulceration in the gastrointestinal tract and the development of gastrointestinal bleeding may occur.

Patients taking coumarin-type anticoagulants are advised to regularly monitor the international normalized ratio (INR).

When used together, ketoprofen increases the toxicity of methotrexate.

Dimethyl sulfoxide, which is part of the excipients, enhances the penetration of drugs through the skin.

How to take, course of use and dosage

The drug is intended for external use.

The gel should be applied to clean, dry skin. A small amount of gel (3-5 cm) is applied in a thin layer, followed by careful rubbing into inflamed or painful areas of the body. The drug should be applied 2-3 times a day.

The duration of treatment should not exceed 14 days.

Overdose

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

If local side effects occur, the drug should be discontinued and the application site should be washed.

If large amounts of the gel are accidentally ingested, systemic adverse reactions characteristic of NSAIDs may occur. It is necessary to wash the stomach, take activated charcoal.

Special instructions

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

After applying the drug, wash your hands.

It is allowed to form a transparent film on the skin at the place of applying the gel.

Do not use with occlusive dressings.

It can be used for phonophoresis.

When applied to the skin, there may be a feeling of warmth and, in rare cases, a burning sensation in the area of application, which may be associated with the warming effect of capsicum, tincture and camphor.

Prolonged use of topical products can lead to increased sensitivity and symptoms of skin irritation at the site of application.

To avoid photosensitivity, it is recommended to avoid exposure to direct sunlight during the course of treatment, as well as after two weeks after the last use of the drug (including not going to a tanning salon).

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

Caution should be exercised in patients with severe renal, cardiac or hepatic insufficiency when using ketoprofen.

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

You should stop using the drug in case of any skin reaction, including reactions with simultaneous application of sunscreens or other cosmetics containing the organic sunscreen filter octocrylene.

Influence on the ability to drive vehicles and mechanisms

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

Form of production

Gel for external use,5%.

Gel of 30 g,50 g or 100 g in aluminum tubes with polymer bushons, according to TU 9467-004-32807885-2008.

The tube together with the instructions for use is placed in a pack of cardboard.

Storage conditions

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

Shelf

life is 2 years.

Active ingredient

Ketoprofen

Dosage form

gel for external use