ticagrelor (Rx)

Brand and Other Names:Brilinta
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Dosing & Uses


Dosage Forms & Strengths


  • 60mg
  • 90mg

Acute Coronary Syndrome

Indicated to reduce the rate of thrombotic cardiovascular events in patients with ACS (unstable angina, non-ST elevation MI, or ST elevation MI) or a history of MI

Also, reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS

For at least the first 12 months following ACS, it is superior to clopidogrel to lower risk of further major adverse cardiovascular events (MACE) (PLATO study)

Loading dose (following ACS event): 180 mg PO x 1 dose

Maintenance dose (for first year following ACS event): 90 mg PO BID

Maintenance dose (after 1 year of maintenance): 60 mg PO BID

Administer with a daily maintenance dose of aspirin 75-100 mg

Coronary Artery Disease

Indicated to reduce the risk of a first MI or stroke in patients with coronary artery disease (CAD) at high risk for such events

While use is not limited to this setting, efficacy was established in the type 2 diabetes mellitus (T2DM) population

For all ACS patients

  • Loading dose: 180 mg PO x 1 dose
  • Maintenance dose (for first year following the loading dose): 90 mg PO BID
  • Maintenance dose (after 1 year of maintenance): 60 mg PO BID

Dosage Modifications

Renal impairment

  • No dosage adjustment needed
  • End-stage renal disease
    • Clinical efficacy and safety studies did not enroll patients with end-stage renal disease (ESRD) on dialysis
    • Intermittent hemodialysis: No clinically significant difference in concentrations of ticagrelor and its metabolite and platelet inhibition are expected compared to those observed in patients with normal renal function

Hepatic impairment

  • Mild: No dose adjustment required
  • Moderate: Data are limited; caution advised
  • Severe: Not studied; avoid use due to likely increase systemic exposure to ticagrelor

Safety and efficacy not established



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            Adverse Effects


            Dyspnea (13.8%)

            Bleeding (see specific data listed below)


            Headache (6.5%)

            Cough (4.9%)

            Dizziness (4.5%)

            Nausea (4.3%)

            Atrial fibrillation (4.2%)

            Hypertension (3.8%)

            Noncardiac chest pain (3.7%)

            Diarrhea (3.7%)

            Back pain (3.6%)

            Hypotension (3.2%)

            Fatigue (3.2%)

            Chest pain (3.1%)

            Syncope (1.7%)


            Dyspena (0.9%)


            Non-CABG related bleeds

            • Total bleeds (major + minor) (8.7%)
            • Major bleeds (4.5%)
            • Fatal/life-threatening (2.1%)
            • Fatal (0.2%)
            • Intracranial (fatal/life-threatening) (0.3%)

            CABG related bleeds

            • Total major bleeds (85.8%)
            • Major bleeds when antiplatelet therapy stopped 5 days before CABG (75%)
            • Fatal/life-threatening (48.1%)
            • Fatal (0.9%)

            Postmarketing Reports

            Immune system disorders: Hypersensitivity reactions including angioedema (see Contraindications)

            Skin and subcutaneous tissue disorders: Rash

            Blood and lymphatic system disorders: Thrombotic thrombocytopenic purpura (rare)



            Black Box Warnings

            Bleeding risk

            • Like other antiplatelet agents, can cause significant, sometimes fatal, bleeding
            • Do not use with active pathological bleeding or a history of intracranial hemorrhage
            • Do not start in patients planned to undergo urgent coronary artery bypass graft surgery (CABG); when possible, discontinue at least 5 days prior to any surgery
            • Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures after starting ticagrelor
            • If possible, manage bleeding without discontinuing; stopping ticagrelor increases risk of subsequent cardiovascular events

            Aspirin dose and ticagrelor effectiveness

            • Aspirin maintenance dose >100 mg reduces the effectiveness of ticagrelor and should be avoided
            • After any initial loading dose, use with aspirin 75-100 mg/day


            Hypersensitivity (eg, angioedema)

            History of intracranial hemorrhage (ICH)

            Active pathologic bleeding (eg, peptic ulcer, ICH)


            Drugs that inhibit platelet function, including ticagrelor, increase bleeding risk; if possible, manage bleeding without discontinuing drug; stopping ticagrelor increases the risk of subsequent cardiovascular events

            Avoid interruption of treatment; if ticagrelor must be temporarily discontinued (eg, to treat bleeding or for elective surgery), restart as soon as possible; discontinuation will increase the risk of myocardial infarction, stent thrombosis, and death

            Surgery: When possible, discontinue 5 days prior to surgery

            Aspirin maintenance doses >100 mg decrease ticagrelor effectiveness; therefore, after initial aspirin loading dose (usually 325 mg), use with aspirin maintenance dose of 75-100 mg/day (see Black Box Warnings)

            Dyspnea reported; intensity described as usually mild-to-moderate and decreases/resolves during continued treatment; if dyspnea symptoms intolerable consider administering a different antiplatelet agent

            Ticagrelor can cause ventricular pauses

            Bradyarrhythmias including AV block have been reported in the post- Marketing setting; Patients with a history of sick sinus syndrome, 2nd or 3rd degree AV block or bradycardia-related syncope not protected by a pacemaker were excluded from PLATO and PEGASUS and may be at increased risk of developing bradyarrhythmias with ticagrelor

            Avoid use with severe hepatic impairment, which is likely to increase ticagrelor serum levels

            Drug interaction overview

            • Ticagrelor is a CYP3A4 substrate and weak CYP3A4 inhibitor
            • May cause false negative results in platelet functional tests (to include, but may not be limited to, the heparin-induced platelet aggregation [HIPA] assay) for patients with heparin-induced thrombocytopenia (HIT)
            • Simvastatin or lovastatin
              • Ticagrelor increases serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4
              • Avoid simvastatin and lovastatin doses >40 mg
            • Digoxin
              • Ticagrelor inhibits the P-glycoprotein transporter
              • Monitor digoxin levels with initiation of, or change in ticagrelor dose
            • Opioids
              • As with other oral P2Y12 inhibitors, coadministration of opioid agonists delay and reduce the absorption of ticagrelor and its active metabolite presumably because of slowed gastric emptying
              • Consider the use of a parenteral antiplatelet agent in ACS patients requiring coadministration of morphine or other opioid agonists
            • Strong CYP3A4 inhibitors
              • Avoid coadministration
              • Strong CYP3A inhibitors substantially increase ticagrelor exposure and therefore increase the risk of adverse effects (eg, dyspnea, bleeding)
            • Strong CYP3A4 inducers
              • Avoid coadministration
              • Strong CYP3A inducers substantially reduce ticagrelor exposure and efficacy
            • Aspirin
              • Aspirin maintenance doses >100 mg/day reduces ticagrelor efficacy

            Pregnancy & Lactation


            Available data from case reports on use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

            Animal data

            • Drug given to pregnant rats and pregnant rabbits during organogenesis caused structural abnormalities in the offspring at maternal doses about 5 to 7 times maximum recommended human dose (MRHD) based on body surface area; when given to rats during late gestation and lactation, pup death and effects on pup growth were seen at ~10 times the MRHD


            There are no data on presence of drug or metabolites in human milk, effects on breastfed infant, or on milk production

            Ticagrelor and its metabolites were present in rat milk at higher concentrations than in maternal plasma; when a drug is present in animal milk, it is likely that the drug will be present in human milk

            Breastfeeding is not recommended during therapy

            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.



            Mechanism of Action

            Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation

            Ticagrelor and its active metabolite are approximately equipotent

            Patients can be transitioned from clopidogrel to ticagrelor without interruption of antiplatelet effect

            Inhibition of platelet aggregation (IPA)

            • Transitioning from clopidogrel to ticagrelor resulted in an absolute IPA increase of 26.4%
            • Transitioning from ticagrelor to clopidogrel an absolute IPA decrease of 24.5%


            Peak plasma time: 1.5 hr (ticagrelor); 2.5 hr (AR-C124910XX [active])

            Bioavailability: 36%


            Vd (steady-state): 88 L

            Protein bound: >99% (ticagrelor and active metabolite)


            Metabolized by: CYP3A4 is the major enzyme responsible for formation of its major active metabolite (AR-C124910XX); metabolized by CYP3A5 to a lesser extent

            Systemic exposure to AR-C124910XX accounts for approximately 30-40%

            Ticagrelor and its major active metabolite are weak P-gp substrates and inhibitors


            Half-life elimination: 7 hr (ticagrelor); 9 hr (active metabolite)


            • Ticagrelor: Feces (58%); urine (26%)
            • Active metabolite: Primarily by biliary excretion; urine (<1%)


            Oral Administration

            Do not administer with another oral P2Y12 platelet inhibitor

            May administer with or without food

            Missed dose: Skip missed dose and take next dose at its scheduled time

            Unable to swallow tablet whole

            • Tablets can be crushed, mixed with water, and drunk immediately
            • Refill glass with water, stir, and drink contents to ensure complete dose is consumed
            • May be administered via nasogastric (NG) tube (≥CH8)
            • Important to flush NG tube through with water after administration of the mixture


            Store at 25ºC (77ºF); excursions permitted to 15-30ºC (59-86ºF)





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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
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