Drugs affecting
fibrinolysis
Classification
I.
Fibrinilytic drugs
a)
Direct-acting: Fibrinolysin
b)
Indirect-acting (activators of profibrinolysin)
a)
Non-selective: Streptokinase, Streptoliase
b)
Selective: Alteplase
II.
Inhibitors of
fibrinolysis
a)
Direct –acting: Contrical
b)
Indirect- acting: Aminocaproic acid, Amben
FIBRINOLYSIN
It is protein from donors’ plasma, the active factor of
fibrinolysis & administered by IV infusion. It has direct action on fibrin
and dissolves fibrin clot in the first hours after thrombosis. It is used for treatment
of acute thrombosis, acute miocardial infarction, thrombophlebitis. It may
cause bleeding resulting from increase in fibrinilysis, allergy, anaphylaxis, arrythmia,
hypotension.
Contraindications: bleeding, cerebral vascular accident, recent trauma of
brain, surgery, uncontrolled hypertension.
activators of
fibrinolysis
steptokinase
It is the proteolytic enzyme from haemolytic streptococcus.
It acts indirectly, inhibits the conversion of plasminogen to plasmin &
degradation both of fibrin and fibrinogen to systemic activation of
fibrinolysis and dissolving of thrombus.
Plasma half-life is 23 min; is administered by IV infusion
(intracoronary infusion in myocardial infarction). It is more active than
fibrinolysin, does not cause arrhythmia.
Alteplase (ACTILISE)
It is tissue plasminogen activator, product of
biotechnology, half-life is 5 min& is administered by IV infusion. It has
high affinity for fibrin and selectively acts only on plasminogen, bound with
thrombus.
Inhibitors of
fibrinolysis
Contrical (Aprotinin)
It is direct acting inhibitor of fibrinolysis and
proteolysis & administered IV slowly or by IV infusion.It binds with
plasmin and inactivates it, inhibits activity of trypsin and kallikrein. It
inhibits fibrinilysis and decreases bleeding caused by activation of
fibrinolysis; inhibits proteolysis and inflammation.
indications: bleeding resulting from activation of proteolysis,
myocardial infarction, acute pancreatitis, prophylaxis of proteolytic
complications after surgeries on pancreas, thyroid glands, prevention of
proteolysis activation after the surgery on bigger salivary glands;
paradontitis (topically)
Side-effects: allergy, nausea, vomiting, hypotension, tachycardia
Aminocaproic acid
It is
indirect-acting inhibitor of fibrinolysis & administered orally and by IV
infusion, acts during 4-6 hr, is not metabolized and excreted with
urine.It interacts with plasminogen and
inhibits its transformation into plasmin, particularly inhibits plasmin;
inhibits proteolytic enzymes and kallikrein. It inhibits fibrinolysis and
decreases bleeding caused by the activation of fibrinolysis; suppresses
proteolysis, decreases inflammation, has anti-allergic action, stimulates
antitoxic function of the liver.
Indications: They are similar to the same to contrykal and also
syndrome of dessemenated intranasal blood coagulation, obstetrics pathology
(ablation placenta, uterine haemorrhages), liver diseases, hypoplastic
anaemia.It is use in dentistry is applied topically to treat parodontitis and
to stop bleeding from dental root channels.
Side-effects: Dizziness, hypotension, bradycardia, arrhythmia, skin
rash, vomiting , nausea.
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