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Activase (Genentech Inc)

Activase (Genentech Inc) - General Information

Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells

 

Pharmacology of Activase (Genentech Inc)

Activase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin. It also produces limited conversion of plasminogen in the absence of fibrin.

 

Activase (Genentech Inc) for patients

Activase is a drug that is only administered intravenously by trained doctors to patients in acute emergency situations. These doctors are trained to treat blood clots that need to be dissolved quickly. See indications for its use under Indications and Dosages.

 

Activase (Genentech Inc) Interactions

The interaction of Activase with other cardioactive or cerebroactive drugs has not been studied. In addition to bleeding associated with heparin and vitamin K antagonists, drugs that alter platelet function (such as acetylsalicylic acid, dipyridamole and Abciximab) may increase the risk of bleeding if administered prior to, during, or after Activase therapy.

Use of Antithrombotics

Aspirin and heparin have been administered concomitantly with and following infusions of Activase in the management of acute myocardial infarction or pulmonary embolism. Because heparin, aspirin, or Activase may cause bleeding complications, careful monitoring for bleeding is advised, especially at arterial puncture sites.

The concomitant use of heparin or aspirin during the first 24 hours following symptom onset were prohibited in The NINDS t-PA Stroke Trial. The safety of such concomitant use with Activase for the management of acute ischemic stroke is unknown.

 

Activase (Genentech Inc) Contraindications

Acute Myocardial Infarction or Pulmonary Embolism

Activase®, Alteplase, recombinant, therapy in patients with acute myocardial infarction or pulmonary embolism is contraindicated in the following situations because of an increased risk of bleeding:

Acute Ischemic Stroke

Activase therapy in patients with acute ischemic stroke is contraindicated in the following situations because of an increased risk of bleeding, which could result in significant disability or death:

  • Evidence of intracranial hemorrhage on pretreatment evaluation
  • Suspicion of subarachnoid hemorrhage
  • Recent intracranial surgery or serious head trauma or recent previous stroke
  • History of intracranial hemorrhage
  • Uncontrolled hypertension at time of treatment (e.g., > 185 mm Hg systolic or > 110 mm Hg diastolic)
  • Seizure at the onset of stroke
  • Active internal bleeding
  • Intracranial neoplasm, arteriovenous malformation, or aneurysm
  • Known bleeding diathesis including but not limited to:
    • Current use of oral anticoagulants (e.g., warfarin sodium) with prothrombin time (PT) > 15 seconds
    • Administration of heparin within 48 hours preceding the onset of stroke and have an elevated activated partial thromboplastin time (aPTT) at presentation

 

 

Additional information about Activase (Genentech Inc)

Activase (Genentech Inc) Indication: For management of acute myocardial infarction, acute ischemic strok and for lysis of acute pulmonary emboli
Mechanism Of Action: Cleaves the Arg-Val bond in plasminogen to produce active plasmin.
Drug Interactions: Nitroglycerin IV nitroglycerin decreases the effect
Food Interactions: Not Available
Generic Name: Alteplase
Synonyms: Tissue-type plasminogen activator precursor; t-PA; t-plasminogen activator; tPA
Drug Category: Thrombolytic Agents
Drug Type: Biotech; Approved
Other Brand Names containing Alteplase: Activase (Genentech Inc);
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Activase (Genentech Inc): Powder, for solution Intravenous drip
Chemical IUPAC Name: Not Available
Chemical Formula: C2569H3928N746O781S40
Alteplase on Wikipedia: http://en.wikipedia.org/wiki/Alteplase
Organisms Affected: Humans and other mammals