Integrilin (Millennium Pharm): Full Drug Profile
Integrilin (Millennium Pharm) - General Information
Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.
Pharmacology of Integrilin (Millennium Pharm)
Integrilin (Millennium Pharm) is an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Integrilin (Millennium Pharm) is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarus barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets.
Integrilin (Millennium Pharm) for patients
Integrilin (Millennium Pharm) Interactions
Enoxaparin dosed as a 1.0 mg/kg subcutaneous injection q12h for four doses did not alter the pharmacokinetics of eptifibatide or the level of platelet aggregation in healthy adults.
Integrilin (Millennium Pharm) Contraindications
Treatment with eptifibatide is contraindicated in patients with:
- A history of bleeding diathesis, or evidence of active abnormal bleeding within the previous 30 days.
- Severe hypertension (systolic blood pressure >200 mm Hg or diastolic blood pressure >110 mm Hg) not adequately controlled on antihypertensive therapy.
- Major surgery within the preceding 6 weeks.
- History of stroke within 30 days or any history of hemorrhagic stroke.
- Current or planned administration of another parenteral GP IIb/IIIa inhibitor.
- Dependency on renal dialysis.
- Known hypersensitivity to any component of the product.
Additional information about Integrilin (Millennium Pharm)
- Integrilin (Millennium Pharm) Indication
For treatment of myocardial infarction and acute coronary syndrome.
- Mechanism Of Action
- Integrilin (Millennium Pharm) inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner.
- Generic Name
- Eptifibatide
- Synonyms
- Integrelin; Intrifiban
- Drug Category
- Anticoagulants; Antiplatelet Agents
- Drug Type
- Biotech; Approved; Investigational
- Other Brand Names containing Eptifibatide
- Integrilin (Millennium Pharm);
- Toxicity (Overdose)
- Eptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis)
- Protein Binding
- Approximately 25%
- Biotransformation
- No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.
- Half Life
- Approximately 2.5 hours
- Dosage Forms of Integrilin (Millennium Pharm)
- Solution Intravenous
- Chemical IUPAC Name
- 2-[20-carbamoyl-12-[4-(diaminomethylideneamino)butyl]-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,22-hexaoxo-17,18-dithia-1,4,7,10,13,21-hexazabicyclo[21.3.0]hexacosan-6-yl]acetic acid
- Chemical Formula
- C35H49N11O9S2
- Eptifibatide on Wikipedia
- https://en.wikipedia.org/wiki/Eptifibatide
- Organisms Affected
- Humans and other mammals
