Fibrinolysin

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	B01AD05 (WHO) ;
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	9004-09-5 ;
DrugBank	DB08977 ;
ChemSpider	none;
UNII	A4028U842W;
ChEMBL	ChEMBL1201505 ;
ECHA InfoCard	100.029.661
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.

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.

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.

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 Additionally, combinations with the antifibrinolytic agent tranexamic acid have been withdrawn from pharmaceutic markets.

Indications

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

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.

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.

External links

Swiss scientific product information
Birk Y, Khalef S, Jibson MD (September 1983). "Purification and properties of protease F, a bacterial enzyme with chymotrypsin and elastase specificities". Arch. Biochem. Biophys. 225 (2): 451–7. doi:10.1016/0003-9861(83)90053-X. PMID 6226244.