Fibrinolytics

Synonym(s)

Rt-PA; Streptokinase; Urokinase

Definition
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Substances capable of dissolving fresh venous or arterial vascular occlusions (see Table 1).

Indication
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Acute heart attack or limb occlusion, deep vein thrombosis (not older than 24 hours).

Remember!

Therapy only in the intensive care unit by experienced therapists!

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Limited indication
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Second and third trimester pregnancies.

Undesirable effects
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Bleeding complications, fever, chills, allergic reactions (especially with streptokinase, possibly pre-treatment with 250 mg prednisolone i.v.), nausea, cephalgias, myalgias.

Remember!

In case of bleeding complications: Tranexamic acid (Cyklokapron) 4 times 500 mg/day i.v. over 2 days!

Interactions
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s. Table 2.

Contraindication
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Aneurysms, hypertension (> 200 mm Hg systolic, > 100 mm Hg diastolic), apoplexy in the last 3 months, poorly controlled diabetes mellitus, epilepsy, early pregnancy, Z.n. arterial vascular puncture, hemorrhagic diathesis, intestinal bleeding, consuming disease, severe liver or kidney failure, surgery within the last 8-10 days, acute pancreatitis, resuscitation within the last 4 weeks, sepsis, tuberculosis, ventricular ulcer, atrial fibrillation, severe cerebral sclerosis.

Tables
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Overview of the most important fibrinolytics

Substance	Effect	HWZ	Dosage	Example preparations
Old plasma (rt-PA)	Activation of thrombin-bound plasminogen to plasmin	Three or four minutes.	Initially 15 mg IV bolus, then 50 mg short infusion over 30 minutes, then 35 mg IV over 60 minutes.	Actilysis
Tenecteplase (TNK-t-PA)	Activation of thrombin-bound plasminogen to plasmin	24 minutes.	One-time bolus of about 10 seconds. Dosage: 0.5 mg/kg bw (maximum dose: 50 mg)	Metalysis
Streptokinase	Plasminogen to plasmin conversion	15 minutes.	Initial 250,000 IU i.v. over 30 min., then 1.5 million IU per hour over 6 hours, repeated every 6 hours if necessary	Streptase
Urokinase	Direct activation of the conversion of plasminogen into plasmin	15 minutes.	Initially 250,000-600,000 IU over 20 minutes, then maintenance dose 80,000-150,000 IU/hour	Urokinase

Essential interactions of fibrinolytics

Antirheumatic drugs, non-steroidal	Bleeding tendency ↑
Coumarins	Bleeding tendency ↑
Glycerol trinitrate	rt-PA effect ↓
Heparin	Bleeding tendency ↑
Valproic acid	Bleeding tendency ↑