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Active ingredients
Sodium Heparin + Dexpanthenol + Dimethyl Sulfoxide
Release form
Gel
Composition
100 g sodium heparin 50,000 IU dexpanthenol 2.5 g dimethyl sulfoxide, 10% H2O 16.66 g corresponds to dimethyl sulphoxide 15 g. Auxiliary substances: polyacrylic acid - 1-1.
Pharmacological effect
Combined preparation for external use. The action of the drug is due to its active ingredients: heparin sodium, dexpanthenol, dimethyl sulfoxide. Dimethyl sulfoxide has anti-inflammatory, anti-edematous and local analgesic action. Anti-inflammatory activity associated with some pharmacological effects, the most significant of which is the inactivation of hydroxyl radicals, produced in large quantities during the process of inflammation and have a destructive effect on tissue. Dimethyl sulfoxide has a local analgesic effect by reducing the speed of nociceptive (pain) impulses in peripheral neurons. The anti-edema effect is provided by the inactivation of hydroxyl radicals and the improvement of the subcutaneous metabolic reaction at the site of the drug. To a certain extent, the anti-edema effect of dimethyl sulfoxide is due to its hygroscopic properties. Dimethyl sulfoxide (50% or more) penetrates biological membranes, incl. through the skin, contributing to a better and deeper penetration into the tissue of other drugs used simultaneously with it. Heparin has an anti-inflammatory effect, promotes the regeneration of connective tissue by inhibiting the activity of hyaluronidase. It has a dose-dependent antithrombotic effect, enhancing the inhibitory activity of antithrombin III on the activation of prothrombin and thrombin. The penetration of heparin through healthy skin is dose-dependent and is confirmed for a dose starting at 300 IU / g. Dexpanthenol, when applied topically, is transformed in the skin into pantothenic acid (a vitamin of group B). The effectiveness of dexpanthenol is comparable to the effectiveness of pantothenic acid. Pantothenic acid as a component of coenzyme A is involved in various catabolic and anabolic processes in tissues; by improving the processes of granulation and epithelization, it promotes the regeneration of damaged skin.
Pharmacokinetics
Absorption and distribution: The physiological concentration of dimethyl sulfoxide in the blood plasma is normally 40 ng / ml.6 hours after the application of the drug, Cmax in the blood plasma reaches 120 ng / ml and lasts up to 12 hours after application. After 60 h after application, the concentration of dimethyl sulfoxide in the blood plasma reaches a physiological level of 40 ng / ml. When using dimethyl sulfoxide 1 g 3 times / day for 5 days, its average content at the site of application on the skin is 3 mg / g, the average content in the underlying muscle tissues and synovial membrane at the site of the synovial compound is 7-10 μg / ml, in the synovial liquids - 0.8 mcg / g. The concentration of dimethyl sulfoxide in the blood plasma is 0.5 mcg / g. Heparin when used externally, heparin is absorbed slightly. When applied externally, dexpanthenol is transformed into pantothenic acid in the skin. Good absorption of dexpanthenol is confirmed experimentally. Withdrawal: T1 / 2 dimethyl sulfoxide is 11-14 hours. 12-25% of absorbed dimethyl sulfoxide is excreted within the first 24 hours and 37-48% is excreted within 7 days unchanged by the kidneys or as a metabolite (dimethyl sulfone). 3.5-6% of total dimethyl sulfoxide is excreted through the lungs in the form of dimethyl sulfide 6-12 hours after the use of the drug.
Indications
- swelling, bruising, and inflammation of the soft tissues, muscles, tendons, tendon sheaths - contusions, bruises - joint injuries from sprained ligaments and tendons - epicondylitis shoulder ( "tennis elbow"), tendonitis (tendon inflammation), tenosynovitis (inflammation of the tendon sheath) , bursitis (inflammation of the mucous bag of the joint) - periarthritis of the shoulder joint - acute neuralgia.
Contraindications
- severe liver dysfunction - severe kidney dysfunction - bronchial asthma - marked disorders of the cardiovascular system - open wounds at the site of application - pregnancy - lactation period - children under 5 years old - hypersensitivity to the drug.
Use during pregnancy and lactation
The use of the drug Dolobene contraindicated in pregnancy due to the lack of data from clinical studies. The use of Dolobene during breastfeeding is contraindicated, since dimethyl sulfoxide is excreted in breast milk.
Dosage and administration
Dolobene should be applied with a surface layer on the skin over the affected skin area 2-4 times / day.When using the gel under the dressing, apply the gel and wait a few minutes for it to be absorbed by the skin and the isopropanol evaporated. Then you can impose a tight bandage. Dolobene can be used in iontophoresis. The drug is applied under the cathode. Dolobene as a contact gel can be used in ultrasound therapy (phonophoresis). Gel active ingredients complement the therapeutic effects of ultrasound waves. The duration of treatment depends on the severity of the symptoms and the severity of the disease.
Side effects
Local reactions: possible skin reactions (redness, itching, burning sensation at the site of application of the gel), which usually disappear during further treatment. Allergic reactions: sometimes - skin manifestations, incl. hives; in isolated cases - angioedema. Other: in rare cases - the smell of garlic from the mouth (caused by dimethyl sulphide, which is a product of dimethyl sulfoxide metabolism), a change in taste is possible (disappear a few minutes after applying the gel); when applying the drug to large areas of the body is extremely rare - nausea, diarrhea, difficulty breathing, headache, chills.
Overdose
There are no data on drug overdose Dolobene.
Interaction with other drugs
When used jointly, Dolobene may enhance penetration of other drugs through the skin. With the simultaneous use of drugs containing sulindak (NSAIDs) with Dolobene drug, the development of peripheral neuropathy is possible.
special instructions
Before applying Dolobene, you should thoroughly clean the skin from other drugs, cosmetics or any chemical agents. Dolobene should not be applied to the mucous membranes of the eyes, nose, mouth, open wounds or damaged skin (due to radiation, severe sunburn, postoperative scars). During treatment with the drug, the photosensitivity of the skin may increase, so during its use it is necessary to limit intensive sunbathing and a visit to the tanning bed. If skin reactions occur, treatment should be discontinued. Due to the high absorption of dimethyl sulfoxide, Dolobene should not be used in combination with other ointments and gels.