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| {{drugbox
| | #REDIRECT [[Eptifibatide#Pharmacology]] |
| | IUPAC_name = N 6 -(aminoiminomethyl)-N 2 -(3-mercapto-1-oxopropyl-L-lysylglycyl-L-a-aspartyl-L- tryptophyl-L -prolyl-L-cysteinamide
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| | image = Eptifibatide_svg.png
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| | CAS_number = 188627-80-7
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| | ATC_prefix = B01
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| | ATC_suffix = AC16
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| | ATC_supplemental =
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| | PubChem = 123610
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| | DrugBank = BTD00063
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| | C = 35 | H = 49 | N = 11 | O = 9 | S = 2
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| | molecular_weight = 831.96 g/mol
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| | bioavailability = n/a
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| | protein_bound = ~25%
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| | metabolism =
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| | elimination_half-life = ~2.5 hours
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| | excretion = [[Kidney|Renal]]
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| | licence_EU = Integrilin
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| | licence_US = Eptifibatide
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| | pregnancy_US = B
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| | legal_status = Rx-only
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| | routes_of_administration = [[Intravenous therapy|IV only]]
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| }}
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| {{SI}}
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| {{CMG}}
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| ==[[Eptifibatide (patient information)|For patient information, click here]]==
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| ==Overview==
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| '''Eptifibatide''' ('''Integrilin®''', [[Millennium Pharmaceuticals]], also co-promoted by Schering-Plough/Essex), is an [[antiplatelet drug]] that selectively blocks the [[platelet]] [[glycoprotein IIb/IIIa]] receptor. Eptifibatide 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. Eptifibatide has a short [[half-life]]. The drug is the third inhibitor of GPIIb/IIIa that has found broad acceptance after the specific antibody [[abciximab]] and the non-peptide [[tirofiban]] entered the global market.
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| Integrilin® is sold in two strengthes: vials containing 2 mg/ml (20 mg totally) and 0.75 mg/ml (75 mg totally).
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| ==Indications==
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| Eptifibatide is used to reduce the risk of acute cardiac ischemic events (death and/or myocardial infarction) in patients with unstable angina or non-ST-segment-elevation (e.g., non-Q-wave) myocardial infarction (i.e., non-ST-segment elevation acute coronary syndromes) both in patients who are to receive non surgery (conservative) medical treatment and those undergoing [[percutaneous coronary intervention]] (PCI).
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| The drug is always applied together with [[aspirin]] or [[clopidogrel]] and ([[low molecular weight heparin]] or [[unfractionated heparin]]. Additionally, the usual supportive treatment consisting of applications of [[nitrates]], [[beta-blockers]], [[lidocaine]], opioid analgesics and/or [[benzodiazepines]] should be employeed as indicated. Angiographic evaluation and other intensive diagnostic procedures may be considered a first line task before initiating therapy with [[eptifibatide]].
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| The drug should exclusively be used in hospitalized patients both because of the serious degree of patients' illness and because of the possible side-effects of [[eptifibatide]].
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| ==Contraindications and precautions==
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| * [[Thrombocytopenia]] : The drug is contraindicated in patients with platelet counts of less than 100,000 because no clinial experience exists regarding such patients.
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| * [[Renal insufficiency]] : Eptifibatide undergoes renal elimination. In such patients with renal insufficiency where a glycoprotein IIb/IIIa inhibitor is likely to provide benefit, [[Abciximab]] (trade name: [[Reopro]]) is an alternative medication.
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| * Current bleeding tendencies or abnormally prolonged coagulation parameters observed within 30 days before starting therapy with [[eptifibatide]] is intended.
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| * Coagulation parameters such as Activated Clotting Time, [[aPTT]], TT, and [[PT]] should be followed closely during therapy and afterwards.
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| * [[Allergy]] to eptifibatide and/or other ingredients.
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| * Severe, uncontrolled [[hypertension]].
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| * [[Pregnancy]] : No experience exists. Pregnant patients should be treated only when clearly needed.
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| * [[Lactation]] : No human data exists. Breast-feeding should be avoided during treatment in order to prevent damage to the newborn.
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| * Geriatric patients : No differences in side effects compared with younger patients have been seen. Nevertheless, geriatric patients should be very closely observed for bleeding and other side-effects.
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| * Pediatric patients : [[Eptifibatide]] is not indicated in patients below 18 years of age, because no experience exists.
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| ==Side effects==
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| It should be noticed that all patients receiving [[eptifibatide]] were seriously ill and most of them were concomitantly treated with other drugs known to have the potential to cause significant [[adverse drug reaction|side effect]]s. Therefore, not all side effects listed as follows may be attributable to [[eptifibatide]] treatment alone:
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| The major adverse event in the PURSUIT study was severe [[bleeding]]. Bleeding occurred as well at sites of clinical intervention (local sites) as at other sites (systemically) like urogenital bleedings. Sometimes, these events were severe enough to require [[Blood transfusion|transfusion]] of blood or plasma concentrates to stop bleeding and counteract [[anemia]]. Severe bleedings occurred in 4.4 and 4.7 % of patients respectively depending on the infusion rate (0.5 µg/kg and minute vs. 0.75 µg/kg and minute). A few cases of death due to severe bleeding events attributable to drug therapy were reported. No cases of hemorrhagic stroke were seen. [[Thrombocytopenia]] of unknown origin (allergic reaction?) was also noticed in 0.2 % of patients.
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| Additionally, [[hypotension]] was seen frequently (6 %). Cardiovascular failure was also frequent (2 %) as were serious arrhythmias ([[ventricular fibrillation]] 1.5 %, [[atrial fibrillation]] 6 %). Severe allergic (anaphylactic) reactions occurred in almost 0.2 % of patients. These reactions can be life-threatening and may be due to the peptide character of [[eptifibatide]]. Other side effects were rare and mild in nature and may not be connected to [[eptifibatide]] therapy.
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| ==Dosage regime==
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| The recommended adult dosage is an i.v. loading dose of 180 µg/kg over 1 to 2 minutes immediately after diagnosis, followed by continuous i.v.-infusion of 2 µg/kg and minute until either hospital discharge or initiation of coronary artery bypass grafting, or for up to 72 hours. At least 4 hours before discharge all local or systemic bleedings should have been controlled and terminated.
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| ==Study results==
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| Eptifibatide was licensed due to the positive results of the so called PURSUIT study encompassing 10,948 patients. In this study all patients had suffered either unstable angina or a non-ST-segment-elevation myocardial infarction. Significantly less patients developed a myocardial infarction under therapy with eptifibatide. Death rates showed a tendency in favour of eptifibatide, but this superiority was not statistically significant. | |
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| ==Additional information==
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| Sometimes the treating physicians require the patient after discharge from hospital to continue treatment with aspirin or clopidrogel or heparin for a few weeks, some months or even for life (as usually is the case with aspirin) to prevent recurrence of symptoms, development of myocardial infarction and/or death related to cardiovascular disease. These advises should be adhered to strictly.
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| ==References==
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| * AHFS Database Online
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| * Arzneimittel Datenbank (in German)
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| * http://www.pharmazeutische-zeitung.de/index.php?id=352&type=0 (in German)
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| * http://www.chemsoc.org/chembytes/ezine/1999/berressem_apr99.htm (information on the biological origin of eptifibatide)
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| ==See also==
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| *[[Glycoprotein IIb/IIIa inhibitors]]
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| {{Antithrombotics}}
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| [[Category:Cardiology]]
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| [[Category:gpIIb/IIIa inhibitors]]
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| [[Category:Drugs]]
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