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Fibrinolysin - Wikipedia

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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^N
DrugBank	DB08977^N
ChemSpider	none
UNII	A4028U842W
ChEMBL	ChEMBL1201505^N
ECHA InfoCard	100.029.661
Chemical and physical data
Molar mass	~ 13,800 g/mol
^NY (what is this?) (verify)

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.

Antithrombotics (thrombolytics, anticoagulants and antiplatelet drugs) (B01)

Antiplatelet drugs

Glycoprotein IIb/IIIa inhibitors	Abciximab Eptifibatide Orbofiban Roxifiban Sibrafiban^§ Tirofiban
ADP receptor/P2Y₁₂ inhibitors	Thienopyridines Clopidogrel Prasugrel Ticlopidine Nucleotide/nucleoside analogs Cangrelor Elinogrel Ticagrelor
Prostaglandin analogue (PGI2)	Beraprost Iloprost Prostacyclin Treprostinil
COX inhibitors	Acetylsalicylic acid/Aspirin^# Aloxiprin Carbasalate calcium Indobufen Triflusal
Thromboxane inhibitors	Thromboxane synthase inhibitors Dipyridamole (+ aspirin) Picotamide Terbogrel Receptor antagonists Terbogrel Terutroban^§
Phosphodiesterase inhibitors	Cilostazol Dipyridamole Triflusal
Other	Cloricromen Ditazole Vorapaxar

Anticoagulants

Vitamin K antagonists
(inhibit II, VII, IX, X)

Factor Xa inhibitors
(with some II inhibition)

Heparin group/ glycosaminoglycans/ (bind antithrombin)	Low-molecular-weight heparin Bemiparin Certoparin Dalteparin Enoxaparin Nadroparin Parnaparin Reviparin Tinzaparin Oligosaccharides Fondaparinux Idraparinux^§ Heparinoids Danaparoid Dermatan sulfate Sulodexide
Direct Xa inhibitors ("xabans")	Apixaban Betrixaban Darexaban^§ Edoxaban Otamixaban^§ Rivaroxaban

Direct thrombin (IIa) inhibitors

Bivalent: Hirudin
- Bivalirudin
- Desirudin
- Lepirudin^‡
Univalent: Argatroban
Dabigatran
Efegatran
Inogatran^§
Melagatran^‡
Ximelagatran^‡

Other

Thrombolytic drugs/
fibrinolytics

Plasminogen activators: r-tPA
- Alteplase^#
- Reteplase
- Tenecteplase
- Desmoteplase^†
UPA
- Saruplase
- Urokinase
Anistreplase
Monteplase
Streptokinase^#
Other serine endopeptidases: Ancrod^‡
Brinase
Fibrinolysin

Non-medicinal

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

v t e Endopeptidases: serine proteases/serine endopeptidases (EC 3.4.21)
Digestive enzymes	Enteropeptidase Trypsin Chymotrypsin Elastase Neutrophil Pancreatic
Coagulation	factors: Thrombin Factor VIIa Factor IXa Factor Xa Factor XIa Factor XIIa Kallikrein PSA KLK1 KLK2 KLK3 KLK4 KLK5 KLK6 KLK7 KLK8 KLK9 KLK10 KLK11 KLK12 KLK13 KLK14 KLK15 fibrinolysis: Plasmin Plasminogen activator Tissue plasminogen activator Urinary plasminogen activator
Complement system	Factor B Factor D Factor I MASP MASP1 MASP2 C3-convertase
Other immune system	Chymase Granzyme Tryptase Proteinase 3/Myeloblastin
Venombin	Ancrod Batroxobin
Other	Acrosin Prolyl endopeptidase Pronase Proprotein convertases 1 2 Prostasin Reelin Subtilisin/Furin/S1P4 Sedolisin/TPP1 Streptokinase Cathepsin A G

v t e Enzymes
Activity	Active site Binding site Catalytic triad Oxyanion hole Enzyme promiscuity Diffusion-limited enzyme Cofactor Enzyme catalysis
Regulation	Allosteric regulation Cooperativity Enzyme inhibitor Enzyme activator
Classification	EC number Enzyme superfamily Enzyme family List of enzymes
Kinetics	Enzyme kinetics Eadie–Hofstee diagram Hanes–Woolf plot Lineweaver–Burk plot Michaelis–Menten kinetics
Types	EC1 Oxidoreductases (list) EC2 Transferases (list) EC3 Hydrolases (list) EC4 Lyases (list) EC5 Isomerases (list) EC6 Ligases (list) EC7 Translocases (list)

Categories:

Hidden categories:

Indications

Contraindications and precautions

Side-effects

Interactions

See also

External links