Dolobene (sodium heparin) gel 20 g.

Description

Dolobene 20 g. Storage
active substances: sodium heparin, dimethyl sulfoxide, dexpanthenol;

100 g of gel contains 50,000 IU of sodium heparin, 15 g of dimethyl sulfoxide, 2.5 g of dexpanthenol;

Dolobene 20 g. Excipients: polyacrylic acid, trometamol, macrogol glyceryl hydroxystearate, isopropyl alcohol, rosemary oil, alpine pine oil, citronella oil, purified water.

Dolobene 20 g. Dosage form
Gel.

Main physical and chemical properties: transparent or cloudy, homogeneous, colorless or yellowish gel with a characteristic odor.

Pharmacotherapeutic group
Topical remedies for joint and muscle pain. ATX code M02A X.

Pharmacological properties

Pharmacodynamics.

Dimethyl sulfoxide (DMSO)

DMSO has anti-inflammatory, local analgesic and anti-edematous effects. The anti-inflammatory effect is based on several pharmacological effects, the main of which is the inactivation of hydroxyl radicals, which are formed in large quantities during inflammation and lead to tissue destruction.

DMSO has a local analgesic effect, reducing the rate of conduction of excitatory impulses in peripheral neurons. The anti-edematous effect is due to the inactivation of hydroxyl radicals and the consequent improvement of metabolic processes in the inflammatory focus. The hygroscopic properties of DMSO are also partly responsible for this.

Heparin

Heparin competitively inhibits hyaluronidase activity, which, in turn, prevents excessive connective tissue degeneration in inflammation. Thus, heparin has an anti-inflammatory effect and promotes healing. In addition, heparin has a dose-dependent antithrombotic effect, significantly increasing the inhibitory effect of antithrombin III on the activation of prothrombin and thrombin.

Dexpanthenol

When applied topically, dexpanthenol is converted in the skin to pantothenic acid, a B vitamin. Dexpanthenol has the same biological efficacy as pantothenic acid. Pantothenic acid, which is part of coenzyme A, in all tissues undergoes various reactions of formation and decomposition and promotes the regeneration processes in wound healing and epithelialization.

Pharmacokinetics.

Dimethyl sulfoxide (DMSO)

DMSO is present in human blood plasma as a natural substance at a concentration of approximately 40 ng / ml. After a single application of 1.5 g of Dolobene gel on the skin surface with an area of ​​400 cm² DMSO is absorbed with a half-life of 3-4 hours. At 6 hours after application, the plasma concentration reaches a plateau (approximately 120 ng / ml) and remains at this level until 12 hours after application. The half-life of DMSO from blood plasma is 11-14 hours. Endogenous plasma concentrations are reached again 60 hours after application.

12-25% of DMSO is excreted within the first 24 hours and 37-48% within 7 days in the urine unchanged as DMSO or as the main metabolite – dimethylsulfone (DMSO2). 3.5-6% of the total dose of DMSO is exhaled by the lungs within 6-12 hours after application in the form of dimethyl sulfide (LCA).

Heparin

Penetration of heparin through healthy skin is dependent on dosage and has been confirmed for dosages of 300 IU / g. There are no data on the pharmacokinetics of heparin after application to the skin.

Dexpanthenol

Dexpanthenol is absorbed faster than pantothenic acid. Rapid absorption of dexpanthenol was confirmed experimentally.

Indication
Dolobene, gel, is used to treat:

injuries (including sports), hematomas, injuries to muscles, periarticular structures or joints (without skin lesions);
tendinitis and tendovaginitis, bursitis, scapular periarthritis and epicondylitis of the shoulder (pathological basis of the clinical syndrome “tennis player’s elbow”);
acute neuralgia.

Contraindication
Hypersensitivity to any components of the drug; severe liver and / or kidney dysfunction; bronchial asthma; unstable hemodynamics, severe disorders of the cardiovascular system (severe angina, myocardial infarction, stroke, severe general atherosclerosis); trophic bleeding leg ulcers, open and / or infected wounds, hemorrhagic diathesis, purpura, thrombocytopenia, hemophilia, bleeding tendency; comatose states, glaucoma, cataracts; concomitant use with drugs containing sulindac; period of pregnancy or breastfeeding.