Heparin ointment with bruises

External drugs with heparin, above all, are an anticoagulant, antithrombotic method for treating a variety of diseases. Heparin is an active anti-coagulant blocking aggregation and synthesis of platelets, thrombin, heparin sodium can prevent the production of fibrin, thereby providing a normal consistency of blood, preventing the formation of blood clots.

Heparin ointment with bruises has an anti-inflammatory and pronounced antithrombotic effect, without irritating the skin in the area of trauma. In addition, the drug with heparin can remove puffiness due to the antiexudative effect and accelerate the process of regeneration of the affected subcutaneous tissue.

The composition of external preparations with heparin includes components that help intensive absorption and penetration of active substances into the bloodstream, this is usually benzilnicotinate and benzocaine for local anesthetic action.

[1], [2]

Indications for use

In the heparin ointment, the most active component is heparin, a substance that inhibits plasma clotting factors. Heparin as a coagulant slows the process of blood clotting (coagulation), contributing to the improvement of rheological parameters, preventing the formation of new blood clots. In the form of an ointment or gel, heparin is used as one of the methods of external treatment of diseases associated with thrombosis in the vascular system.

Heparin ointment (heparin ointment) belongs to the group of direct anticoagulants, it includes such components:

• Heparin sodium (heparin sodium).
• Benzocaine (benzocaine).
• Benzylnicotinate (benzylnicotinate).
• Auxiliary components.

Heparin ointment has the following indications for use:

• Preventive treatment of thrombophlebitis.
• Prevention of thrombosis in the background of varicose veins.
• Postpartum complications in the form of hemorrhoids.
• External (external) hemorrhoids.
• Periphlebitis is an inflammatory process in the walls of the veins.
• Postinjectional phlebitis.
• Mastitis.
• Trophic ulcers.
• Lymphadenitis.
• Hematomas.
• Migrating phlebitis.
• Contusions, injuries of closed type, including damage to joints, tendons, ligaments, muscles.
• Infiltrates of aseptic type.

How does heparin ointment work?

• Heparin sodium reduces puffiness, has a locally anti-inflammatory effect, affects the rate of resolution of thrombi. The component works directly in the bloodstream as an inhibitor of the biosynthesis of coagulation factors - thrombins.
• Benzylnicotinate promotes vasodilation, which provides good absorption of heparin.
• Benzocaine reduces pain symptoms that occur with vascular thrombosis and local inflammatory process.

Thus, all external means containing heparin have a positive effect on blood flow and the state of the vascular system, helping to overcome the inflammatory process and the associated dysfunctions of the blood supply system of tissues.

Pharmacodynamics

Heparin as the main active substance of the ointment is primarily an endogenous anticoagulant component of direct action. The pharmacodynamics of heparin is due to its ability to inhibit the whole process of blood coagulation by forming complexes with such substances:

• Procoagulants.
• Antithrombin III.
• All components of the fibrinolysis system are plasmin, activators and inhibitors of fibrinolysis.

In addition to the prevention of thrombi, all drugs with heparin have an antiproliferative effect - it inhibits the growth and reproduction of new, often atypical cells at the site of injury.

Getting into the systemic bloodstream, heparin starts to activate the protein factor of the plasma (antithrombin), which in turn inhibits the process of clotting and thickening of the blood. Pharmacodynamics of Heparinum are associated with such changes in the blood flow:

• Activation of products of heparin cofactor, antithrombin.
• Formation of complexes with fibrinolysis proteins.
• Binding of blood thrombins formed by heparin complexes.
• Deceleration of prothrombinase production.
• Oppression of plasma factors - factor of Christmas (factor IX) - antihemophilic globulin.
• Oppression of the Stuart-Prower factor X factor.
• Oppression of activation of the factor Rosenthal (factor XI) - the previous thromboplastin component.
• Oppression factor XII - factor Hageman.
• Binding of complexes and inhibition of factors of the prothrombinase process leads to inhibition of thrombin generation.
• Stabilization of the level of fibrinogen and inhibition of its transition to fibrin.
• Reduction of the connection between thrombin and fibrinogen due to the negative molecular charge of heparin.
• Inhibition of fibrin-stabilizing factor (XIII) - plasma transglutaminase.
• Maintain the integrity and stability of the vascular wall by feeding its electronegative potential.
• Has a definite immunosuppressive effect on the inflammatory process at the site of the injury.

In addition to the fact that heparin ointment prevents thrombosis, its pharmacodynamics is associated with the disaggregation of already existing thrombotic clots. As a consequence, microcirculation is activated in the damaged tissues, bruises and bruises dissolve more rapidly, puffiness decreases, and general trophism improves.

Pharmacokinetics

Like all external drugs, heparin ointment works only with shallow layers of the dermis, subcutaneous tissue, however its pharmacokinetics has its own peculiarities. Applicative application of the gel or ointment is provided for many diseases associated with the state of the vascular system and the composition of the blood, so heparin in the form of an external agent is able to be absorbed deeper and enter the systemic bloodstream. The maximum amount of heparin in the blood plasma is observed in 6-8 hours after application, the normalization of rheological indicators is possible in a day. However, such indicators are not dangerous, because heparin has a large molecular weight and is not able to significantly disrupt the work of internal organs and systems, especially if it is used as an ointment or gel. In addition, a positive characteristic of heparin ointment can be considered its relative safety in the treatment of various problems with blood vessels and soft tissues during pregnancy, heparin molecules do not overcome the placental barrier and are unable to disrupt the development of the fetus.

Pharmacokinetics of heparin ointment:

• Quite fast absorption without disrupting the functions of internal organs.
• Neutralization of serotonin after ingestion into the bloodstream after 4-6 hours.
• Formation of complexes with plasma proteins.
• Adsorption of protein complexes in the liver.
• Excretion in the form of urogeparin kidney by urine.

External drugs with heparin

Currently, the pharmaceutical industry produces many external products containing the same active component - heparin. Almost all of them are identical in composition, the difference can only be in the form, weight or concentration of the main active substance.

Forms of heparin as an external agent:

• Heparin ointment.
• Heparin Gel.
• Gel is an aerosol.

External drugs with heparin, most commonly used with soft tissue injuries:

1. Heparin ointment is a combined remedy containing heparin sodium, benzocaine, Benzonicotinic acid - benzonikonitonic acid.
2. Hepatothrombin, which includes Heparin sodium - heparin sodium, Allantoin - allantoin, dexpanthenol.
3. Thrombophobe - in 100 grams of ointment contains 5000 units of Heparin sodium, 250 milligrams of benzyl nicotinate (benzyl nicotinic acid ester).
4. Lyoton-1000, in addition to heparin, the gel includes methyl parahydroxybenzoate, carbomer, ethanol, propyl parahydroxybenzoate, essential oil of orange blossoms, triethanolamine, lavender oil.

For convenience, we offer such a table, which briefly describes the most effective external preparations containing heparin:

[6],

How to apply?

Most bruises are treated with a gel form, the drug is absorbed more quickly and has a positive effect on the injured zones.

Method of administration and dose of heparin ointment with bruises:

• A gel or ointment is used as an external drug.
• Skin integument must be intact, intact. Any scratch or cut is a contraindication to the application of the drug.
• The gel or ointment is applied with a small strip up to 10 cm in length to the area of the injury.
• Calculation of the drug - 0,5-1 grams to 3-4 centimeters of the affected area.
• The agent should be applied with light rubbing movements.
• Heparin gel is applied up to 4 times a day.
• Heparin ointment is applied no more often than 3 times a day.
• The course of treatment of contusions should not exceed 10 days.
• If after the application of the drug for 7 days the symptomatology does not disappear, you should consult a doctor to prescribe another more effective remedy or for additional diagnosis of trauma and to identify a hidden disease, soft tissue damage

Use during pregnancy

Before discussing the use of heparin ointment with bruises during pregnancy, it should be determined for what purpose this remedy can in principle be used during gestation:

1. It's no secret that during the entire pregnancy the weight of a woman somehow varies, and the load on the cardiovascular system, and, consequently, also on the venous system, also increases significantly. The expansion of veins, which temporarily lose the ability to contract, is a typical phenomenon for pregnant women. Thrombosis is not just a cosmetic defect, but a dangerous phenomenon for the whole organism of a future mother. Complications, which are possible with thrombosis, are associated with torn off thrombi, emboli, with occlusion of important blood channels. Heparin ointment helps prevent these conditions.
2. Another delicate problem during pregnancy is hemorrhoids, which can develop against a background of digestive disorders, constipation due to the action of progesterone. Pressure on the venous system of the rectum leads to the formation of hemorrhoids, their infringement. These phenomena are also stopped by heparin ointment.
3. Striae or stretch marks due to rupture of collagen fibers can also be prevented with external means containing heparin.
4. Contusions of soft tissues. Perhaps, heparin ointment is the only relatively safe remedy that helps a pregnant woman to quickly remove puffiness at the site of an injury, stop the development of a hematoma and accelerate the regeneration of damaged subcutaneous tissue.

Contraindications, which involves the use of ointments with heparin in pregnancy, are due to individual intolerance to the main active substance, which is rare. Also, the ointment can not be applied to irritated skin or to wounds, scratches, cuts. It is strictly forbidden to use heparin in any form with a low level of blood coagulability. In general, the drug is considered a rather effective way to help pregnant women get rid of not only the symptoms of varicose veins, but also of all types of closed injuries - bruises, sprains, tendons. During lactation, heparin ointment can also be prescribed, but it should be applied no more than 5 days. Medical control is very important, because heparin in the form of external medicines is more actively absorbed than other ointments, and the organism of the future or nursing mother is extremely vulnerable and unstable, self-medication can lead to undesirable side effects.

Contraindications for use

Parenteral administration of heparin has many contraindications. External application of the agent with heparin is the safest in connection with the slower absorption, not by the ability of active substances to influence the basic functions of the organs and systems of the body.

Heparin ointment, contraindications for use:

• Any irritation, cuts, wounds on the skin.
• Ulcerative necrotic formations in the zone of injury or in the area of thrombophlebitis.
• Hypersensitivity to the components of ointment, gel.
• Caution if there is a clotting disorder, increased bleeding in the anamnesis.
• Thrombocytopenia.
• It is not used on mucous membranes.
• Purulent wounds, abscesses.
• During the gestation period and during breastfeeding, heparin ointment is administered under the strict supervision of a doctor.
• Trophic ulcers.
• Increased permeability of the vascular system.
• Anemia.
• Necrosis of hemorrhoids.
• Extensive hematomas.
• Hemorrhagic diathesis.

Heparin gel or ointment has an effective effect on the process of blood coagulation, therefore, despite the popularity and effectiveness of this remedy, ointment should be used with caution. Given the good absorption capacity of the drug and its effect on reducing local immunity (anti-inflammatory effect) when applied to damaged skin, there is a risk of infection and related complications. In addition, heparin is a strong anti-proliferative component, any wound, a scratch when it is applied will heal very slowly and hard, this refers to bruises of soft tissues accompanied by damage and suppuration of the skin. If the patient has a history of diseases associated with thrombocytopenia, a bleeding disorder (bleeding), a heparin ointment applied to the hematoma can only activate the internal subcutaneous hemorrhage. Indications or contraindications to the use of external means with heparin are indicated in the instructions, however it is more expedient that the ointment be prescribed by the doctor after examining the injury and assessing the general condition of the patient.

[3], [4], [5]

Side effects

Heparin ointment is considered one of the safe and effective anticoagulants used as external treatment of bruises, diseases associated with blood clotting disorders - thrombosis. However, heparin is an active, high molecular weight component whose properties should be taken into account to prevent complications.

Side effects of heparin ointment with bruises can be as follows:

• Increased subcutaneous bleeding with thrombocytopenia, other disorders in the hematopoiesis system.
• Local allergic reaction.
• Urticaria, swelling, itching.
• Dermatitis.
• Accession of infection in case of ointment application to damaged skin (wounds, cuts).

In general, with proper use of the drug, side effects are extremely rare, currently heparin ointment is dispensed in pharmacies as an over-the-counter drug.

Overdose

Overdosing with the use of a heparin ointment can be associated with excessively zealous application, when the drug is applied often, thickly or over large areas of the body. In connection with good absorption, the heparin ointment or gel quickly reaches the lesion of small vessels and can cause a backlash - not a reduction in swelling and arrest of the hematoma, but, on the contrary, development of edema, flushing of the skin and an increase in the hemorrhage zone. In addition, a thick layer of the drug creates a kind of film, under which can develop a variety of negative reactions, even allergic. If atypical signs appear when applying the ointment, discontinue use immediately and consult a doctor for an adequate replacement of the anticoagulant.

With extreme caution, you should apply ointment to people who have a history of at least one case of allergy. Heparin as a high-molecular component is a fairly active substance that suppresses the resistance of local immunity, which can provoke the appearance of urticaria, itching, dermatosis. Before using the ointment, it is advisable to test it on a small area of the skin if a hypersensitive reaction does not appear within 12 hours, heparin ointment can be used according to the doctor's recommendations or as described in the instructions in the manual.

Interactions with other drugs

Heparin ointment is not used in combination with external drugs containing NSAIDs (non-steroidal anti-inflammatory drugs), and the ointment is not combined with drugs that include tetracycline or antihistamine components.

The interaction with other drugs is due not only to the pharmacochemical properties of the active substances, but also to pharmacodynamics, the specificity of the absorption of heparin ointment. For example, external use of a gel with heparin and simultaneous administration of oral anticoagulants may lead to a change in the prothrombin index. There is also interaction with other drugs - non-steroidal anti-inflammatory drugs, antiaggregants in both tableted and injectable form.

To reduce the activity of heparin as the main active substance in the form of ointment, gel, external or tablet preparations containing tetracycline, nicotine, thyroxine, ergot alkaloids are capable.

As a rule, drugs with heparin with bruises are used in the first 3-5 days after injury, if it becomes necessary to apply ointment with NSAIDs on a damaged area in parallel, heparin ointment alternates with these preparations, the interval is 4-6 hours.

How is it stored?

Heparin ointment is stored according to the standards and rules described in the technical documentation and accepted in almost all pharmacy institutions in the world. The storage conditions do not change even when the ointment is purchased and used at home. The drug should be stored in a place protected from direct sunlight at a temperature of not more than +15 degrees Celsius. The gel form of heparin is very influenced by environmental factors that can affect the activity and quality of the drug. Too low a temperature as well as high leads to the fact that the gel or ointment stratifies and loses its properties. Therefore, external drugs containing heparin should be stored in a dry place, not in the refrigerator, preferably in a special medicine cabinet, in a zone inaccessible to children. If all the rules are followed, the heparin ointment retains all its pharmacochemical characteristics until the expiration date.

Shelf life

The expiration date of the heparin ointment is indicated on the original packaging, as a rule, it does not exceed 3 years. After the expiration of the date specified by the manufacturer as the final date of sale, the ointment or gel should be disposed of.

Heparin ointment as an effective anticoagulant is very widely used to treat many vascular diseases associated with increased thrombosis, which often develops with bruises. Depending on the degree of severity of soft tissue damage, an ointment or gel form is used, the latter is considered the most effective, since the gel is a dispersive system that can quickly penetrate into the subcutaneous tissue. The choice of analogues of heparin ointment is great, therefore, with the timely use of anticoagulant, the symptomatology of the injury is treated within 3-5 days.

Means containing heparin or its analogues, similar in pharmacodynamics of substance

Name of the drug	The form	Manufacturer
Heparin ointment	Ointment - in a tuba 25g, in 1g - 100ED heparin	Different countries
Lyoton 1000	Gel - in a tube 50 g, 1000 units in 1 g	Italy Menarini
Lyoton 1000	Gel - in tuba 30 g	Italy Menarini
Lyoton 1000	Gel - in tuba 100g	Italy Menarini
Trombleys	Gel - in tuba 50g	Russia
Trombleys	Gel, in a tube - 30 g	Russia
Hepatrombin	Gel - 40g, options - 300 or 500M of heparin	Serbia HEMOFARM
Heparoid Zentiva	Ointment, in a tube 30 g	Czech Republic Zentiva