Defibrase for Injection
is a single ingredient of thrombin-like enzyme separated and extracted
from the velum of Agkistrodon acutus. Defibrase acts on alpha chain
of fibrinogen and releases A peptide, but it can not activate X¢»
factor. As a result, a kind of cross-link fibrin comes into being which
is susceptible to clearance by fibrinolytic system. Defibrase also directly
degrades fibrin and activates fibrinolytic system.
Traditional thrombolytic agents are principally urokinase and streptokinase,
both of which are activators of extrinsic fibrinolytic system and lack
such functions as suppressing platelet aggregation and improving microcirculation.
Meanwhile both drugs interfere with blood coagulation system, and easily
result in hemorrhage which leaves the curative effect much to be desired.
As a new potent thrombolysin, defibrase is preferable to traditional
agents in that it can lower fibrinogen content, activate fibrinolytic
system and inhibits platelet adhesion and aggregation. By using advanced
bioengineering techniques including affinity chromatography, Our company
has developed high purity defibrase from velum of Agkistrodon acutus.
With properties of high quality, potency and safety, defibrase injection
is applicable for cerebral embolism, thromboangiitis obliterans, femoral
arterial embolism and pulmonary embolism with significantly curative
effects.
Clinical Indications
1. Cerebrovascular occlusion diseases such as cerebral thrombosis
and embolism.
2. Coronary heart disease, angina pectoris and cardiac infarction,
and thrombo-embolism caused by artificial valve.
3. Other kinds of arteriovenous thrombosis or embolism such as
thrombosis of deep vein, thrombosis of peripheral artery, thromboangiitis
obliterans, pulmonary embolism and obstruction of retinal vessel.
4. Blood hyper viscosity diseased such as sicklaremia and rheumatoid
arthritis.
5. Pulmonary heart disease.
6. In prevention of thrombosis again after surgical operation
and drug treatment, as well as in anticoagulant therapy.
7. Hypercoagulability such as disseminated intravascular coagulation(DIC),shock,
coagulation factors excessiveness or inactivation disturbance.
8. Other diseases such as glomerulonephritis, systemic lupus
erythematosus, diabetes and hypertension.
Pharmacokinetics
Plasma concentration of puerarin showed to be correlated with dosage
by comparing administration of a single dose and the initial dose in
continuous treatment. T 1/2 is about 6hr after the first administration
and 3hr after the second and third ones. Most of the motebolites is
excreted in urine.
Significant Properties
1.High quality.
The product is prepared with high purity by using advanced bioengineering
techniques including affinity chromatography.
The polyacrylamide gel concentration is 12%. 1-3 lines: defibrase of
different loading volume:2ug ,5ug,10ug. 4 line: protein molecular weight
marker.
a. Rrabbit phosphorylate.
b. Bovine serum albumin.
c. Rabbit actin.
d. Bovine carbonic anhydrase
e. Trypsin inhibitor f. Ovalbumin lysozyme
2. High Potency
Defibrase¡¦s Potency in fibrinolysis and thrombolysis at
lower dosage in longer half life gives out better therapeutic effective
ness than other thrombolytic agents.
3. Safety
Neurotoxin and hemorrhage are absolutely absent from our defibrase product
under rigorous test.
Adverse Reactions
No severe adverse reactions have been observed. Occasionally reactions
including fever, urticaria, gingival bleeding, positive occult blood
in stool and hematuria, menorrhea, and menostaxis occur. Most of the
adverse reaction occur 24-28hr after intravenous infusion and need no
treatment.
Cautions
1. As an highly purity enzyme preparation, Puerarin is safe in
administration. If symptoms such as headache occur during IV administration,
there will be remission without special treatment.
2. This preparation should be only used as directed. Regularly
checking of platelet, for instance once a week. Administration of defibrase
should be stopped if platelet count declines 80,000 per cubic meters
and resumed when platelet returns to normal.
Contradictions
It must not to be used in severe hepatic and renal insufficiency, while
prudently used in patients with allergic diathesis.
Administration and Dose
Dissolute the preparation in several milliliter of sterile water for
injection, then add it into 250ml normal saline before administration.
Acute attack stage: IV 10u/day in no less than 1hr for 2-3days. Non-acute
stage: IV 5-10u/day or every other day over 1hr for a course of two
weeks.