drug-information.ru

|Streptokinase

Streptokinase

Trade Names:
Streptase
- Powder for Injection 250,000 IU
- Powder for Injection 750,000 IU
- Powder for Injection 1,500,000 IU

Mechanism of Action

Pharmacology

Converts plasminogen to the enzyme plasmin, which aids in dissolution of blood clots.

Pharmacokinetics

Metabolism

No metabolites identified.

Elimination

Streptokinase is cleared by the liver. The t _½ is approximately 23 min (for activator complex).

Indications and Usage

Acute MI, lysis of intracoronary thrombi, improvement of ventricular function, and reduction of mortality associated with acute MI (IV or intracoronary route); reduction of infarct size and CHF associated with acute MI (IV); lysis of objectively diagnosed (eg, angiography) pulmonary emboli (involving obstruction of blood flow to a lobe or multiple segments, with or without unstable hemodynamics); lysis of objectively diagnosed (eg, ascending venography), acute, extensive thrombi of the deep veins (eg, those involving the popliteal vessels); lysis of acute arterial thrombi and emboli; alternative to surgical revision for clearing totally or partially occluded arteriovenous cannulae when acceptable flow cannot be achieved.

Contraindications

Active internal bleeding; recent cerebrovascular accident (within 2 mo); intracranial or intraspinal surgery; intracranial neoplasm; severe uncontrolled hypertension.

Dosage and Administration

IV infusion Administer as soon as possible after symptom onset (greatest benefit when administered within 4 hr, but benefit has been reported up to 24 hr). Infuse a total dose of 1,500,000 IU within 60 min. Intracoronary infusion Administer 20,000 IU by bolus followed by 2000 IU/min for 60 min (total dose, 140,000 IU).

IV infusion Administer as soon as possible after onset of thrombolic event, preferably within 7 days. A loading dose of 250,000 IU infused into a peripheral vein over 30 minutes has been found appropriate in over 90% of patients. If thrombin time or any parameter of lysis after 4 hr of therapy is not significantly different from the normal control level, discontinue streptokinase because excessive resistance is present. Dose and duration of therapy (following the loading dose of 250,000 IU/30 min): pulmonary embolism 100,000 IU/hr for 24 hr (72 hr if concurrent DVT is suspected); DVT 100,000 IU/hr for 72 hr; arterial thrombosis or embolism 100,000 IU/hr for 24 to 72 hr.

Slowly instill 250,000 in 2 mL of solution into each occluded limb of the cannula. Clamp off cannula limb(s) for 2 hr. Closely observe patient for adverse effects. After treatment, aspirate contents of infused cannula limb(s) and flush with saline before reconnecting cannula.

Storage/Stability

Store unopened vials at controlled room temperature (59° to 86°F). Use reconstituted solution immediately or within 8 hr if stored at 36° to 46°F. Discard any unused solution.

Drug Interactions

May increase the risk of bleeding.

Incompatibility

Do not add other medication to the streptokinase container.

Laboratory Test Interactions

Will cause marked decreases in plasminogen and fibrinogen levels and increases in thrombin time, activated partial thromboplastin time, and prothrombin time, which usually normalize within 12 to 24 hr.

Adverse Reactions

Cardiovascular

Hypotension (sometimes severe).

Hematologic

Bleeding (major and minor).

Respiratory

Respiratory depression.

Miscellaneous

Allergic reactions (eg, fever and shivering, urticaria, itching, flushing, nausea, headache, musculoskeletal pain); anaphylactic and anaphylactoid reactions (ranging from minor breathing difficulty to bronchospasm, periorbital swelling or angioneurotic edema); transient elevations of serum transaminases; back pain.

Precautions

Pregnancy

Category C .

Children

Safety and efficacy not established.

Special Risk Patients

Use with caution in patients with recent (within 10 days) major surgery, obstetrical delivery, organ biopsy, previous puncture of noncompressible vessels; recent (within 10 days) serious GI bleeding, recent (within 10 days) trauma including cardiopulmonary resuscitation, hypertension (systolic BP greater than 180 mm Hg or diastolic BP greater then 110 mm Hg), high likelihood of left heart thrombus (eg, mitral stenosis with atrial fibrillation), subacute bacterial endocarditis, hemostatic defects including those secondary to severe hepatic or renal disease, cerebrovascular disease, diabetic hemorrhagic retinopathy, septic thrombophlebitis, occluded AV cannula at seriously infected site, or any condition in which bleeding constitutes a significant hazard or would be particularly difficult to manage because of location; use with caution in patients who are pregnant or over age 75 yr.

Arrhythmia

Rapid lysis of coronary thrombi has been shown to cause reperfusion arterial or ventricular dysrhythmias, requiring immediate treatment.

Bleeding

Major and minor bleeding may occur. Severe, sometimes fatal, internal bleeding involving GI, hepatic, GU, or intracerebral sites has occurred.

Cholesterol embolism

Serious and fatal cholesterol embolism may occur.

Repeat administration

Because of increased likelihood of resistance caused by antistreptokinase antibodies, streptokinase may not be effective if administered within 5 days to 12 mo of prior streptokinase or anistreplase administration, or streptococcal infections (eg, streptococcal pharyngitis).

Patient Information

• Explain name, dose, action, and potential side effects of drug.
• Advise patient, family, or caregiver that medication will be prepared and administered by a health care professional in a medical setting.
• Instruct patient, family member, or caregiver to report any signs of bleeding or allergic reaction immediately.