Pentalgin Extra, gel 5% 50 g

Pharmacotherapeutic group: Non-steroidal anti-inflammatory agent for local use.

The ATX code: M02AA10

Pharmacological properties

Pharmacodynamics

Ketoprofen is a non-steroidal anti-inflammatory drug; when used topically it has analgesic, anti-inflammatory and anti-edema effects. The mechanism of action is associated with inhibition of the activity of cyclooxygenase 1 and cyclooxygenase 2 enzymes that regulate the synthesis of prostaglandins.

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

The adjuvant tincture of the chilli pepper and camphor may have a mild warming effect at the site of application.

The excipients in the composition of dimethyl sulfoxide increase penetration of the medicines through the skin.

Pharmacokinetics

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

Indications

The drug is intended as symptomatic therapy, to reduce pain and inflammation at the time of use, does not affect the progression of the disease.

Active ingredient

Composition

Active ingredient:

Excipients:

How to take, the dosage

The product is 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 gentle rubbing into the inflamed or painful areas of the body. The drug should be applied 2-3 times a day.

The course of treatment should not exceed 14 days.

Interaction

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

While there is little absorption of ketoprofen through the skin, with frequent and prolonged use there may be symptoms of interaction with other drugs (the same as with systemic use).

When co-administered with other NSAIDs, glucocorticoids, ethanol, corticotropin, gastrointestinal ulceration and gastrointestinal bleeding may occur.

Patients taking coumarin anticoagulants are recommended to have regular monitoring of the international normalized ratio (INR).

Ketoprofen increases the toxicity of methotrexate when used together.

The excipients in the formulation of dimethyl sulfoxide increase penetration of drugs through the skin.

Special Instructions

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

Wash hands after application.

A transparent film can form on the skin where the gel was applied.

Do not use with occlusive dressings.

Possible to use with phonophoresis.

A sensation of warmth and, in rare cases, burning sensation may be felt in the area of application, which may be due to the warming effect of the chilli pepper fruit tincture and camphor.

Long-term use of topical products may result in increased sensitivity and symptoms of skin irritation at the site of application.

In order to avoid photosensitivity, it is recommended to avoid exposing the skin to direct sunlight during treatment, and for two weeks after the last treatment session (including no tanning beds).

In prolonged and large doses of the drug, systemic side effects (hypersensitivity reactions, gastrointestinal disorders, worsening of renal failure) may occur in very rare cases.

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

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

The product should be discontinued if any skin reactions occur, including reactions if sunscreens or other cosmetics containing the organic sunscreen octocrylene are applied at the same time.

Influence on driving and operating machinery

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

Contraindications

Side effects

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

Skin disorders:

infrequent: erythema, pruritus, eczema; rare: photosensitization, bullous dermatitis, urticaria; very rare: contact dermatitis, angioedema.

Gastrointestinal tract:

very rarely: peptic ulcer, bleeding, diarrhea.

The immune system:

very rare: anaphylactic reactions, hypersensitivity reactions.

Urinary system disorders:

very rarely: aggravation of the course of renal failure.

If these or other side effects occur, discontinue use of the drug and consult a physician.

Overdose

In case of accidental use of the drug in a dose higher than recommended, the risk of overdose symptoms is minimal due to the very low systemic absorption of ketoprofen when used externally.

If local side effects occur, discontinue the drug and wash the area of application.

If large amounts of the gel are accidentally swallowed, systemic adverse reactions typical of NSAIDs may occur. It is necessary to rinse the stomach, taking activated charcoal.

Pregnancy use

The use of the drug is contraindicated in the III trimester of pregnancy. In I and II trimesters of pregnancy the drug may be used only after consultation with a physician if the estimated benefits to the mother exceed the potential risk to the fetus.

Similarities