study [1:<1 minute. 1 Continuous IV infusion: Administer for at least 2 hours or for duration of PCI, whichever is longer. 1 2 Dosage Available as cangrelor tetrasodium; dosage expressed in terms of cangrelor. 1 Adults Acute Ischemic Complications of PCI IV 30 mcg/kg by rapid IV ( bolus ) injection prior to PCI, immediately followed by 4 mcg/kg per minute by continuous IV infusion for at least 2 hours or for the duration of the procedure, whichever is longer. 1 2 13 14 Transitioning to Oral Therapy After discontinuance of cangrelor infusion, administer an oral P2Y12-receptor antagonist (clopidogrel, prasugrel, or ticagrelor) to maintain platelet inhibition. 1 16 17 If ticagrelor used, administer 180 mg any time during cangrelor infusion or immediately after discontinuance of the infusion. 1 If clopidogrel used, administer 600 mg immediately after discontinuance of cangrelor infusion; do not administer concurrently with cangrelor. 1 (See Specific Drugs under Interactions.) If prasugrel used, administer 60 mg immediately after discontinuance of cangrelor infusion; do not administer concurrently with cangrelor. 1 (See Specific Drugs under Interactions.) Special Populations Renal Impairment Dosage adjustment not required. 1 Hepatic Impairment Dosage adjustment not required. 1 (See Hepatic Impairment under Cautions.) Cautions for Cangrelor tetrasodium Contraindications Substantial active bleeding. 1 Known hypersensitivity to cangrelor or any ingredient in the formulation. 1 Warnings/Precautions Bleeding Possible bleeding, especially hematoma at the site of vascular access. 1 2 3 4 6 8 9 10 11 (See Contraindications.) In pivotal clinical trial, greater incidence of bleeding events of all severities with cangrelor compared with clopidogrel; however, rate of severe bleeding (per the Global Use of Strategies to Open Occluded Coronary Arteries [GUSTO] criteria) not substantially different between treatment groups. 1 2 6 Antiplatelet effect negligible 1 hour after discontinuance of cangrelor infusion. 1 6 11 14 16 18 Sensitivity Reactions Hypersensitivity Hypersensitivity reactions (e.g., anaphylaxis, bronchospasm, angioedema, stridor) reported. 1 (See Contraindications.) Specific Populations Pregnancy Category C. 1 No adequate and well-controlled studies of cangrelor in pregnant women. 1 In animal studies, cangrelor produced dose-related fetal growth retardation and increased incidences of abortion and/or intrauterine losses, but did not produce malformations; not considered to be a teratogen. 1 Lactation Not known whether cangrelor is distributed into human milk; discontinue nursing or the drug. 1 Pediatric Use Safety and efficacy not established. 1 2 Geriatric Use No substantial differences in safety or efficacy relative to younger adults. 1 Renal Impairment No dosage adjustment required; however, worsening renal function reported in some patients with severe renal impairment (Cl cr> <30 mL/minute) receiving cangrelor in clinical studies. 1 (See Renal Impairment under Dosage and Administration.) Hepatic Impairment Safety and efficacy not established in patients with hepatic impairment. 1 Hepatic impairment not expected to affect pharmacokinetics because metabolism not dependent on hepatic function. 1 11 Common Adverse Effects Bleeding; transient dyspnea reported in some patients. 1 2 3 4 16 Interactions for Cangrelor tetrasodium Drugs Metabolized by Hepatic Microsomal Enzymes Neither cangrelor nor its major metabolites inhibit activity of the hepatic CYP isoenzymes at therapeutic concentrations in vitro. 1 Cangrelor not expected to interact with drugs metabolized by these microsomal enzymes. 1 Specific Drugs Drug Interaction Comments Aspirin No effect on pharmacokinetics or pharmacodynamics of cangrelor 1 11 Bivalirudin No clinically detectable interactions 1 Heparin No effect on pharmacokinetics or pharmacodynamics of cangrelor 1 11 Heparin, low molecular weight No clinically detectable interactions 1 11 Nitroglycerin No effect on pharmacokinetics or pharmacodynamics of cangrelor 1 Ticagrelor Antiplatelet effect of ticagrelor 180 mg not substantially altered when given during cangrelor infusion 1 11 16 Administer ticagrelor at any time during or immediately after cangrelor infusion 1 Thienopyridines (clopidogrel, prasugrel) Decreased antiplatelet effect of clopidogrel 600 mg or prasugrel 60 mg when given during cangrelor infusion 1 6 16 Do not administer clopidogrel or prasugrel until cangrelor infusion discontinued 1 Cangrelor tetrasodium Pharmacokinetics Absorption Bioavailability Peak plasma concentrations achieved within 2 minutes after administration of rapid IV ( bolus ) injection followed by continuous infusion. 1 9 Onset Immediate antiplatelet effect. 1 9 Duration Platelet function returns to normal within 1 hour after discontinuance of infusion. 1 9 18 Distribution Extent Not known whether the drug is distributed into human milk. 1 Plasma Protein Binding Approximately 97 98%. 1 Elimination Metabolism Rapidly deactivated in circulation by dephosphorylation to its primary metabolite, which has negligible antiplatelet activity. 1 9 11 16 Elimination Route Excreted in urine (58%) and feces (35%). 1 11 Half-life 3 6 minutes. 1 6 11 14 16 18 Special Populations Pharmacokinetics not affected by gender, age, renal status, or hepatic function. 1 11 Body weight has effect on pharmacokinetics but accounted for by weight-based infusion regimen. 1 11 Stability Storage Parenteral Powder for Injection 20 25 C (may be exposed to 15 30 C). 1 Diluted IV solutions (200 mcg/mL) are stable at room temperature for 12 hours in 5% dextrose injection and 24 hours in 0.9% sodium chloride injection. 1 Compatibility For information on systemic interactions resulting from concomitant use, see Interactions. Parenteral Solution Compatibility 1 Compatible Dextrose 5% in water Sodium chloride 0.9% Actions Nonthienopyridine, direct-acting P2Y12 platelet ADP-receptor antagonist; unlike thienopyridines (e.g., clopidogrel, prasugrel), but like ticagrelor, cangrelor binds reversibly to P2Y12 receptor and does not require hepatic transformation to exert its pharmacologic effects. 1 2 6 9 13 Prevents signal transduction of the cyclic adenosine monophosphate (cAMP) pathway, resulting in reduced exposure of fibrinogen binding sites to the GP IIb/IIIa complex and subsequent inhibition of platelet activation and aggregation. 13 19 Compared with clopidogrel, cangrelor produces more rapid and effective inhibition of platelet aggregation and has a faster onset and offset of action. 1 18 20 Advice to Patients Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 Importance of patients informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant diseases. 1 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Cangrelor Tetrasodium Routes Dosage Forms Strengths Brand Names Manufacturer Parenteral For injection, for IV use 50 mg (of cangrelor) Kengreal Medicines Company AHFS DI Essentials. Copyright 2017, Selected Revisions September 1, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. The Medicines Company. Kengreal (cangrelor) for injection prescribing information. Parsippany, NJ; 2015 Jun. 2. Bhatt DL, Stone GW, Mahaffey KW et al. Effect of platelet inhibition with cangrelor during PCI on ischemic events. N Engl J Med . 2013; 368:1303-13. [PubMed 23473369] 3. Harrington RA, Stone GW, McNulty S et al. Platelet inhibition with cangrelor in patients undergoing PCI. N Engl J Med . 2009; 361:2318-29. [PubMed 19915221] 4. Bhatt DL, Lincoff AM, Gibson CM et al. Intravenous platelet blockade with cangrelor during PCI. N Engl J Med . 2009; 361:2330-41. [PubMed 19915222] 5. Levine GN, Bates ER, Blankenship JC et al. 2011 ACCF/AHA/SCAI Guideline for Percutaneous Coronary Intervention. A report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines and the Society for Cardiovascular Angiography and Interventions. J Am Coll Cardiol . 2011; 58:e44-122. [PubMed 22070834] 6. Franchi F, Rollini F, Muñiz-Lozano A et al. Cangrelor: a review on pharmacology and clinical trial development. Expert Rev Cardiovasc Ther . 2013; 11:1279-91. [PubMed 24138516] 7. Kastrati A, Ndrepepa G. Cangrelor - a champion lost in translation?. N Engl J Med . 2009; 361:2382-4. [PubMed 19915223] 8. Mehta SR. Cangrelor: a new CHAMPION for percutaneous coronary intervention. Lancet . 2013; 382:1960-2. [PubMed 24011550] 9. Oestreich JH, Dobesh PP. Cangrelor for treatment during percutaneous coronary intervention. Future Cardiol . 2014; 10:201-13. [PubMed 24762247] 10. Steg PG, Bhatt DL, Hamm CW et al. Effect of cangrelor on periprocedural outcomes in percutaneous coronary interventions: a pooled analysis of patient-level data. Lancet . 2013; 382:1981-92. [PubMed 24011551] 11. Waite LH, Phan YL, Spinler SA. Cangrelor: a novel intravenous antiplatelet agent with a questionable future. Pharmacotherapy . 2014; 34:1061-76. [PubMed 25123696] 12. Hamm CW, Bassand JP, Agewall S et al. ESC Guidelines for the management of acute coronary syndromes in patients presenting without persistent ST-segment elevation: The Task Force for the management of acute coronary syndromes (ACS) in patients presenting without persistent ST-segment elevation of the European Society of Cardiology (ESC). Eur Heart J . 2011; 32:2999-3054. [PubMed 21873419] 13. Wallentin L. P2Y(12) inhibitors: differences in properties and mechanisms of action and potential consequences for clinical use. Eur Heart J . 2009; 30:1964-77. [PubMed 19633016] 14. Bonadei I, Sciatti E, Vizzardi E et al. New frontiers in the management of acute coronary syndromes: cangrelor and elinogrel. Recent Pat Cardiovasc Drug Discov . 2014; 9:22-7. [PubMed 24915974] 15. Lange RA, Hillis LD. The duel between dual antiplatelet therapies. N Engl J Med . 2013; 368:1356-7. [PubMed 23473370] 16. Kubica J, Kozinski M, Navarese EP et al. Cangrelor: an emerging therapeutic option for patients with coronary artery disease. Curr Med Res Opin . 2014; 30:813-28. [PubMed 24393016] 17. Schneider DJ, Seecheran N, Raza SS et al. Pharmacodynamic effects during the transition between cangrelor and prasugrel. Coron Artery Dis . 2015; 26:42-8. [PubMed 25089928] 18. Lhermusier T, Baker NC, Waksman R. Overview of the 2014 Food and Drug Administration Cardiovascular and Renal Drugs Advisory Committee meeting regarding cangrelor. Am J Cardiol . 2015; 115:1154-61. [PubMed 25728646] 19. Angiolillo DJ, Capranzano P. Pharmacology of emerging novel platelet inhibitors. Am Heart J . 2008; 156(2 Suppl):S10-5. [PubMed 18657681] 20. Tang Y, Zhang YC, Chen Y et al. Efficacy and safety of cangrelor for patients with coronary artery disease: a meta-analysis of four randomized trials. Int J Clin Exp Med . 2015; 8:800-8. [PubMed 25785060] 21. Cattaneo M. New P2Y(12) inhibitors. Circulation . 2010; 121:171-9. [PubMed 20048234] Next Interactions Print this page Add to My Med List More about cangrelor Side Effects During Pregnancy Drug Interactions Support Group 0 Reviews Add your own review/rating Drug class: platelet aggregation inhibitors Consumer resources Cangrelor Cangrelor Intravenous (Advanced Reading) Professional resources Cangrelor (Wolters Kluwer) Other brands: Kengreal Related treatment guides Percutaneous Coronary Intervention> ]} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Platelet aggregation inhibitors Related Drugs Percutaneous Coronary Intervention Plavix , clopidogrel , bivalirudin , Integrilin , cangrelor , Angiomax , eptifibatide , More... Cangrelor Rating No Reviews - Be the first! No Reviews - Be the first! 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