Actilyse

Thrombolytic treatment in acute MI, acute massive pulmonary embolism w/ haemodynamic instability, & acute ischaemic stroke.

IV Acute MI 90-min dose regimen (start w/in 6 hr after symptom onset): Patient weighing ≥65 kg 15 mg as IV bolus immediately followed by 50 mg as IV infusion over the 1st 30 min, then 35 mg IV infusion over 60 min until max total dose of 100 mg, <65 kg 15 mg as IV bolus immediately followed by 0.75 mg/kg as IV infusion over the 1st 30 min (max: 50 mg), then 0.5 mg/kg IV infusion over 60 min up to max of 35 mg. 3-hr dose regimen (start between 6-12 hr after symptom onset): Patient weighing ≥65 kg 10 mg as IV bolus immediately followed by 50 mg IV infusion over the 1st hr, then 40 mg as IV infusion over 2 hr until max total dose of 100 mg, <65 kg 10 mg as IV bolus immediately followed by IV infusion over 3 hr up to max total dose of 1.5 mg/kg. Acute massive pulmonary embolism Patient weighing ≥65 kg Total dose: 100 mg administered in 2 hr. Dose regimen: 10 mg as IV bolus over 1-2 min immediately followed by 90 mg as IV infusion over 2 hr until max total dose of 100 mg, <65 kg 10 mg as IV bolus over 1-2 min immediately followed by IV infusion over 2 hr up to max total dose of 1.5 mg/kg. Acute ischaemic stroke Recommended total dose: 0.9 mg/kg (max: 90 mg) starting w/ 10% of total dose as initial IV bolus immediately followed by remainder of total dose as IV infusion over 60 min. Initiate treatment as early as possible w/in 4.5 hr of symptom onset.

Hypersensitivity. Present significant bleeding disorder or w/in the past 6 mth, known haemorrhagic diathesis; any history of CNS damage ie, neoplasm, aneurysm, intracranial or spinal surgery; history, evidence or suspicion of intracranial haemorrhage including subarachnoid haemorrhage; severe uncontrolled arterial HTN; major surgery or significant trauma in the past 10 days, recent head or cranial trauma; prolonged or traumatic CPR (>2 min), obstetrical delivery w/in the past 10 days, recent puncture of non-compressible blood vessel eg, subclavian or jugular vein puncture; bacterial endocarditis, pericarditis; acute pancreatitis; documented ulcerative GI disease during last 3 mth; arterial aneurysms, arterial/venous malformations; neoplasm w/ increased bleeding risk. Patients receiving effective oral anticoagulants (eg, warfarin Na w/ INR >1.3). Severe hepatic dysfunction including hepatic failure, cirrhosis, portal HTN (oesophageal varices) & active hepatitis. Acute MI &/or acute massive pulmonary embolism: Haemorrhagic stroke or stroke of unknown origin; ischaemic stroke or transient ischemic attack in preceding 6 mth, except current acute ischaemic stroke w/in 4.5 hr. Acute ischaemic stroke: Symptoms of ischaemic attack beginning >4.5 hr prior to infusion start or when time of symptom onset is unknown; acute ischaemic stroke rapidly improving or only minor before start of infusion; severe stroke (eg, NIHSS >25); seizure at onset of stroke; history of previous stroke or serious head-trauma w/in 3 mth; combination of previous stroke & DM; heparin administration w/in 48 hr preceding onset of stroke w/ elevated aPTT; platelet count <100,000/mm³; systolic BP >185 mmHg, or diastolic BP >110 mmHg, or aggressive management (IV medication) necessary to reduce BP to these limits; blood glucose <50 or >400 mg/dL. Childn <16 yr.

Immune-mediated hypersensitivity reactions. Enhanced risk of hypersensitivity especially in acute ischaemic stroke &/or by concomitant use w/ ACE inhibitors. Discontinue treatment in case of severe hypersensitivity reaction (eg, angioedema); if serious bleeding particularly cerebral haemorrhage occurs & terminate concomitant heparin administration. Not to be given >100 mg dose in acute MI & pulmonary embolism, & >90 mg in acute ischaemic stroke. Avoid use of rigid catheters, IM inj & non-essential handling of patient during treatment. Bleeding from puncture sites. Recent IM inj or small recent traumas eg, biopsies, puncture of major vessels, cardiac massage for resuscitation; conditions w/ increased haemorrhagic risk. Monitor for angioedema during & for up to 24 hr after infusion. Consider protamine administration if heparin has been administered w/in 4 hr before onset of bleeding; cryoprecipitate, fresh frozen plasma, & platelet transfusion after each administration; antifibrinolytics. Patients receiving oral anticoagulants. Concomitant use w/ other active substances affecting coagulation or platelet function. Pregnancy & lactation. Acute MI & acute massive pulmonary embolism: Systolic BP >160 mmHg. Increased risk of intracerebral haemorrhage w/ advanced age. Acute MI: Reperfusion arrhythmia. Increased risk of bleeding w/ concomitant use of GPIIb/IIIa antagonists; thromboembolic events in patients w/ left heart thrombus eg, mitral stenosis or atrial fibrillation. Acute ischaemic stroke: Not to be initiated later than 4.5 hr after symptom onset. Avoid administration of IV heparin or platelet aggregation inhibitors (eg, ASA) in the 1st 24 hr after treatment. Increased risk of intracranial haemorrhage particularly in late time-to-treatment onset, patients pre-treated w/ ASA or >80 yr. Patients w/ prior stroke or uncontrolled diabetes; extensive infarctions. Cerebral oedema may occur upon ischaemic area reperfusion. Monitor BP during treatment & up to 24 hr. Initiate IV antihypertensive therapy if systolic BP >180 mmHg or diastolic BP >105 mmHg. Childn ≥16 yr.

Superficial or internal bleeding. Rash, urticaria, bronchospasm, angiooedema, hypotension, shock or any hypersensitivity-associated symptom; intracranial haemorrhage eg, cerebral & subarachnoid haemorrhage, cerebral & intracranial haematoma, haemorrhagic & haemorrhagic transformation stroke; eye haemorrhage; pericardial haemorrhage; haemorrhage (eg, haematoma), embolism, parenchymatous organ bleeding eg, hepatic haemorrhage; resp tract haemorrhage eg, pharyngeal & pulmonary haemorrhage, haemoptysis, epistaxis; GI haemorrhage (eg, gastric, gastric ulcer, rectal & mouth haemorrhage, haematemesis, melaena, gingival bleeding), retroperitoneal haemorrhage (eg, retroperitoneal haematoma), nausea, vomiting; ecchymosis; urogenital haemorrhage eg, haematuria, urinary tract haemorrhage; inj & puncture site haemorrhage eg, catheter site haematoma & haemorrhage; decreased BP, increased body temp; fat embolism; transfusion. Acute MI: Reperfusion arrhythmia eg, arrhythmia, extrasystoles, atrial fibrillation, 1st degree AV block to AV block complete, bradycardia, tachycardia, ventricular arrhythmia, fibrillation & tachycardia.

Increased risk of bleeding w/ medicinal products affecting coagulation or altering platelet function. Enhanced risk of hypersensitivity reaction w/ ACE inhibitors.

Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)

B01AD02 - alteplase ; Belongs to the class of enzymes. Used in the treatment of thrombosis.

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