Dosing and uses of Kengreal (cangrelor)
Adult dosage forms and strengths
injection, lyophilized powder for reconstitution
- 50mg/vial
Percutaneous Coronary Intervention
Indicated as an adjunct to percutaneous coronary intervention (PCI) to reduce the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST) in patients who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor
30 mcg/kg IV bolus infused over 1 minute before PCI, THEn
Immediately follow bolus injection with 4 mcg/kg/min IV infusion; continue for at least 2 hr or duration of PCI, whichever is longer
Transition patients to oral P2Y12 platelet inhibitor
- Choose from 1 of the loading-dose regimens described below to initiate oral therapy:
- Ticagrelor: 180 mg PO at any time during cangrelor infusion or immediately after discontinuation
- Prasugrel: 60 mg PO immediately after discontinuing cangrelor; do not administer prasugrel prior to cangrelor discontinuation because of drug interaction
- Clopidogrel: 600 mg PO immediately after discontinuing cangrelor; do not administer clopidogrel prior to cangrelor discontinuation because of drug interaction
Pediatric dosage forms and strengths
Safety and efficacy not established
Kengreal (cangrelor) adverse (side) effects
Bleeding
GUSTO trial data
- Mild (14.9%)
- Moderate (0.4%)
- Severe/life-threatening (0.2%)
TIMI trial data
- Minor (0.6%)
- Major (0.2%)
1-10%
Worsening renal function in patients with CrCl <30 mL/min (3.2%)
<1%
Hypersensitivity
Warnings
Contraindications
Significant active bleeding
Hypersensitivity
Cautions
Increased risk of bleeding; bleeding events of all severities were more common with cangrelor than with clopidogreL
Pregnancy
Pregnancy category: C
Lactation: Unknown if distributed in human breast milk; use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Kengreal (cangrelor)
Mechanism of action
P2Y12 platelet inhibitor that blocks ADP-induced platelet activation and aggregation; it binds selectively and reversibly to the P2Y12 receptor to prevent further signaling and platelet activation
Absorption
Peak plasma concentration: 2 minutes
Onset of action: Within 2 minutes following 30 mcg/kg IV bolus followed by 4 mcg/kg/min IV infusion
After discontinuation of the infusion, the antiplatelet effect decreases rapidly and platelet function returns to normal within 1 hr
Distribution
Protein bound 97-98%
Vd: 3.9 L
Metabolism
Deactivated rapidly in the circulation by dephosphorylation to its primary metabolite, a nucleoside, which has negligible antiplatelet activity
Metabolism is independent of hepatic function and it does not interfere with other drugs metabolized by hepatic enzymes
Elimination
Half-life: 3-6 minutes
Excretion: 58% urine; 35% feces
Administration
IV Preparation
For each 50 mg/vial, reconstitute by adding 5 mL of sterile water for injection
Swirl gently until all material is dissolved; avoid vigorous mixing
Allow any foam to settle
Ensure that vial contents are fully dissolved and the reconstituted material is a clear, colorless to pale yellow solution
Do not use without dilution
Before administration, each reconstituted vial must be diluted further with 0.9% NaCl or D5W
Withdraw the contents from 1 reconstituted vial and add to 250-mL bag of 0.9% NaCl or D5W
Mix the bag thoroughly
This dilution results in a concentration of 200 mcg/mL and should be sufficient for at least 2 hr of dosing
Patients who weigh ≥100 kg require a minimum of 2 bags
IV Administration
Administer via a dedicated IV line
Administer the bolus volume rapidly (<1 minute), from the diluted bag via manual IV push or pump
Ensure the bolus is completely administered before the start of PCI
Start the IV infusion immediately after the bolus administration
Storage
Store at controlled room temperature (20-25°C [68-77°F]), with excursions between 15-30°C (59-86°F) permitted
