Fibrinolysin

Last updated
Fibrinolysin
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy
category
  • C
Routes of
administration
ointment for local application, in combination with deoxyribonuclease
ATC code
Legal status
Legal status
  • Rx only (where available)
Pharmacokinetic data
Bioavailability virtually none
Metabolism local inactivation
Elimination half-life almost completely inactivated after 24 hours
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
ChEMBL
ECHA InfoCard 100.029.661 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Molar mass ~ 13,800 g/mol
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Fibrinolysin is an enzyme derived from plasma of bovine origin (plasmin) or extracted from cultures of certain bacteria. It is used locally only and exclusively together with the enzyme desoxyribonuclease (extracted from bovine pancreas). Fibrinolysin and desoxyribonuclease both act as lytic enzymes. The combination is available as ointment containing 1 BU (Biological Unit) fibrinolysin and 666 BUs desoxyribonuclease per gram.

Plasmin protein-coding gene in the humans

Plasmin is an important enzyme present in blood that degrades many blood plasma proteins, including fibrin clots. The degradation of fibrin is termed fibrinolysis. In humans, the plasmin protein is encoded by the PLG gene.

Bacteria A domain of prokaryotes – single celled organisms without a nucleus

Bacteria are a type of biological cell. They constitute a large domain of prokaryotic microorganisms. Typically a few micrometres in length, bacteria have a number of shapes, ranging from spheres to rods and spirals. Bacteria were among the first life forms to appear on Earth, and are present in most of its habitats. Bacteria inhabit soil, water, acidic hot springs, radioactive waste, and the deep portions of Earth's crust. Bacteria also live in symbiotic and parasitic relationships with plants and animals. Most bacteria have not been characterised, and only about 27 percent of the bacterial phyla have species that can be grown in the laboratory . The study of bacteria is known as bacteriology, a branch of microbiology.

Contents

Fibrinolysin attacks and inactivates fibrin molecules occurring in undesirable exudates on the surface of the human body and on human mucosa, e.g., in superficial wounds and burns, while desoxyribonuclease targets and destroys (human) DNA. The combination of the two enzymes has a synergistic effect on necrotic but not on living tissue. According to the manufacturer the ointment provides enhanced wound cleaning and accelerates the healing process.

Fibrin fibrous, non-globular protein involved in the clotting of blood.

Fibrin is a fibrous, non-globular protein involved in the clotting of blood. It is formed by the action of the protease thrombin on fibrinogen which causes it to polymerize. The polymerized fibrin together with platelets forms a hemostatic plug or clot over a wound site.

Exudate

An exudate is a fluid emitted by an organism through pores or a wound, a process known as exuding or exudation. Exudate is derived from exude, "to ooze," from the Latin exsūdāre, "to sweat".

DNA Molecule that encodes the genetic instructions used in the development and functioning of all known organisms and many viruses

Deoxyribonucleic acid is a molecule composed of two chains that coil around each other to form a double helix carrying genetic instructions for the development, functioning, growth and reproduction of all known organisms and many viruses. DNA and ribonucleic acid (RNA) are nucleic acids; alongside proteins, lipids and complex carbohydrates (polysaccharides), nucleic acids are one of the four major types of macromolecules that are essential for all known forms of life.

Both enzymes are marginally resorbed into systemic circulation because of their very high molecular weight and their macromolecular structure.

The activity of both enzymes is almost completely exhausted after 24 hours. Usually, it is necessary to repeat the application (and renew the dressing) every 6 to 8 hours until healing becomes complete.

The ointment is marketed by Pfizer under the brand name Fibrolan in a variety of countries (e.g. Switzerland). It is currently not approved in the USA.

Pfizer American multinational pharmaceutical corporation

Pfizer Inc. is an American multinational pharmaceutical corporation headquartered in New York City, with its research headquarters in Groton, Connecticut. It is one of the world's largest pharmaceutical companies. It is listed on the New York Stock Exchange, and its shares have been a component of the Dow Jones Industrial Average since 2004. Pfizer ranked No. 57 on the 2018 Fortune 500 list of the largest United States corporations by total revenue.

Where approved, Fibrolan has been licensed on the basis of claimed good therapeutical experience, but adequate and well controlled studies are still lacking.

In the past, combinations with the antibiotic chloramphenicol were available, but because chloramphenicol in any form of application has led to aplastic anemia and death, these were banned. Additionally, combinations with the antifibrinolytic agent tranexamic acid have been withdrawn from pharmaceutic markets.

Chloramphenicol chemical compound

Chloramphenicol is an antibiotic useful for the treatment of a number of bacterial infections. This includes use as an eye ointment to treat conjunctivitis. By mouth or by injection into a vein, it is used to treat meningitis, plague, cholera, and typhoid fever. Its use by mouth or by injection is only recommended when safer antibiotics cannot be used. Monitoring both blood levels of the medication and blood cell levels every two days is recommended during treatment.

Aplastic anemia is an autoimmune disease in which the body fails to produce blood cells in sufficient numbers. Blood cells are produced in the bone marrow by stem cells that reside there. Aplastic anaemia causes a deficiency of all blood cell types: red blood cells, white blood cells, and platelets.

Tranexamic acid chemical compound used to treat or prevent blood loss

Tranexamic acid (TXA) is a medication used to treat or prevent excessive blood loss from major trauma, postpartum bleeding, surgery, tooth removal, nosebleeds, and heavy menstruation. It is also used for hereditary angioedema. It is taken either by mouth or injection into a vein.

Indications

Enzymatic wound cleaning to assist healing of minor burns, superficial wounds, ulcus cruris, and superficial hematoma.

Hematoma localized collection of blood outside the blood vessels

A hematoma or haematoma is a localized bleeding outside of blood vessels, due to either disease or trauma including injury or surgery and may involve blood continuing to seep from broken capillaries. A hematoma is benign and is initially in liquid form spread among the tissues including in sacs between tissues where it may coagulate and solidify before blood is reabsorbed into blood vessels. An ecchymosis is a hematoma of the skin larger than 10mm.

Contraindications and Precautions

The ointment should not be used in patients with a known hypersensitivity to any ingredient. It should be used with caution in patients with hypersensitivity to bovine proteins in general and in pregnant women (category C), because no human data is available.

Hypersensitivity refers to undesirable reactions produced by the normal immune system, including allergies and autoimmunity. They are usually referred to as an over-reaction of the immune system and these reactions may be damaging, uncomfortable, or occasionally fatal. Hypersensitivity reactions require a pre-sensitized (immune) state of the host. They are classified in four groups after the proposal of P. G. H. Gell and Robin Coombs in 1963.

Side-Effects

Infrequently, local reactions such as increased pain or a stitching/burning sensation are noticed. No systemic anticoagulant activity has been seen due to the exclusively local character of treatment.

Interactions

Not known.

See also

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