|
| Primary information |
|---|
| ID | 10057 |
| Therapeutic ID | Th1009 |
| Protein Name | Alteplase |
| Sequence | >Th1009_Alteplase
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
|
| Molecular Weight | 59042.3 |
| Chemical Formula | C2569H3928N746O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.516 |
| Melting point | 60 |
| Half-life | NA |
| Description | Glycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells. |
| Indication/Disease | To manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli |
| Pharmacodynamics | Alteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin, thus limited conversion of plasminogen takes place in the absence of fibrin. |
| Mechanism of Action | Alteplase on binding to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain cleaves (domain) the Arg/Val bond in plasminogen to form plasmin which in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| NA |
| Clearance | NA |
| Categories | Agents causing angioedema, Amino Acids, Peptides, and Proteins, Anticoagulants, Blood and Blood Forming Organs, Blood Proteins, Cardiovascular Agents, Endopeptidases, Enzymes, Enzymes and Coenzymes, Fibrin Modulating Agents, Fibrinolytic Agents, Hematologic Agents, Hydrolases, Ophthalmologicals, Peptide Hydrolases, Plasminogen Activators, Proteins, Sensory Organs, Serine Endopeptidases, Serine Proteases, Tissue Plasminogen Activator, Tissue Plasminogen Activator, antagonists & inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Ticlopidine.Increased bleeding risk. Monitor for signs of bleeding. |
| Target | NA |
| Brand Name | Cathflo Activase |
| Company | Genentech, Inc |
| Brand Description | Genentech, Inc |
| Prescribed For | Used to treat the symptoms of Acute Myocardial Infarction, Pulmonary Embolism, Acute Ischemic Stroke, and Central Venous Catheter Occlusion |
| Chemical Name | NA |
| Formulation | Each vial of Cathflo Activase contains 2.2 mg of Alteplase (which includes a 10% overfill), 77 mg of Larginine, 0.2 mg of polysorbate 80, and phosphoric acid for pH adjustment. Each reconstituted vial will deliver 2 mg of Cathflo Activase, at a pH of approximately 7.3. |
| Physical Appearance | sterile, white to pale yellow, lyophilized powder |
| Route of Administration | Injection for intracatheter instillation for restoration of function to central venous access devices following reconstitution with Sterile Water for Injection, USP. |
| Recommended Dosage | Cathflo® Activase® (Alteplase) is for instillation into the dysfunctional catheter at a concentration of 1 mg/mL. Patients weighing ≥30 kg: 2 mg in 2 mL Patients weighing <30 kg: 110% of the internal lumen volume of the catheter, not to exceed 2 mg in 2 mL |
| Contraindication | Cathflo Activase should not be administered to patients with known hypersensitivity to Alteplase or any component of the formulation |
| Side Effects | hives, difficulty breathing, swelling of your face, lips, tongue, or throat, any bleeding that will not stop, sudden headache, weakness, dizziness, bleeding gums, nosebleeds, easy bruising, bleeding from a wound, incision, catheter, or needle injection, bloody or tarry stools, coughing up blood, vomit that looks like coffee grounds, red or pink urine, heavy menstrual periods, abnormal vaginal bleeding, sudden numbness or weakness (especially on one side of the body), slurred speech, problems with vision or balance, chest pain or pressure, pain spreading to the jaw or shoulder, nausea, sweating, general ill feeling, sudden severe back pain, muscle weakness, numbness or loss of feeling in your arms or legs, swelling, rapid weight gain, little or nor urination, severe stomach pain, vomiting, darkening or purple discoloration of your fingers or toes, very slow heartbeats, shortness of breath, lightheadedness, sudden severe back pain, severe headache, blurred vision, pounding in your neck or ears, and anxiety |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |