cangrelor, Kengreal

 Indications

Adjunct to percutaneous coronary intervention (PCI) to

prisk of periprocedural MI, repeat coronary revascularization

or stent thrombosis in patients not currently

receiving a P2Y12 platelet inhibitor and are not receiving

a glycoprotein IIb/IIIa inhibitor.

Action

Inhibits platelet aggregation by reversibly interacting

with platelet P2Y12ADP-receptors, preventing signal

transduction and platelet activation. Therapeutic

Effects:prisk of periprocedural MI, repeat coronary

revascularization or stent thrombosis associated with

PCI.

Pharmacokinetics

Absorption: IV administration results in complete

bioavailability.

Distribution: Unk.

Protein Binding: 97–98%.

Metabolism and Excretion: Metabolized rapidly

in the blood stream; metabolites do not have antiplatelet

activity. 58% excreted by kidneys, 35% in feces. 

Half-life: 3–6 min.

TIME/ACTION PROFILE (antiplatelet effect)

ROUTE ONSET PEAK DURATION

IV rapid 2 min 1 hr†

† following discontinuation.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Significant

severe bleeding.

Use Cautiously in: CCr 30 mL/min (qrisk of further

decline in renal function); OB: Consider potential

maternal benefits and fetal risks; Pedi: Safe and effective

use in children has not been established.

Adverse Reactions/Side Effects

Resp: dyspnea. Hemat: bleeding. Misc: allergic reactions

including ANAPHYLAXIS.

Interactions

Drug-Drug: Concurrent use of other P2Y12 inhibitors

including clopidogrel, prasugrel, or tigagrelorqrisk

of bleeding. Blocks antiplatelet effects of concurrently

administered clopidogrel or prasugrel.

Route/Dosage

IV (Adults): 30 mcg/kg bolus prior to PCI, then 4

mcg/kg/min infusion for 2 hr or duration of procedure,

whichever is longer; should be followed by initiation of

an oral P2Y12 platelet inhibitor.

Availability

Lyophilized powder for IV injection (requires reconstitution):

50 mg/vial.