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ticagrelor (Rx)Brand and Other Names:Brilinta

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 60mg
  • 90mg
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Acute Coronary Syndrome

P2Y(12) platelet inhibitor 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

For at least the first 12 months following ACS, it is superior to clopidogrel

Ticagrelor also reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS

Loading dose (following ACS event): 180 mg PO (two 90 mg tablets)

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

Maintenance dose (after 1 year with history of MI): 60 mg PO BID

Administer with aspirin: Initial loading dose of 325 mg, then maintenance dose of aspirin of 75-100 mg/day; DO NOT exceed aspirin dose of 100 mg/day (see Black Box Warnings)

Dosage Modifications

Renal impairment

  • No dosage adjustment needed
  • Dialysis: Not studied

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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Interactions

Interaction Checker

ticagrelor and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dyspnea (13.8%)

            Bleeding (see specific data listed below)

            1-10%

            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%)

            <1%

            Dyspena (0.9%)

            Bleeding

            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)

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            Warnings

            Black Box Warnings

            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

            Contraindications

            Hypersensitivity (eg, angioedema)

            History of intracranial hemorrhage (ICH)

            Active pathologic bleeding (eg, peptic ulcer, ICH)

            Cautions

            In clinical trials, increased overall risk of bleeding (major + minor) to a somewhat greater extent than did clopidogrel

            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

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

            CYP3A4/5 substrate

            • Metabolized by CYP3A4/5
            • Avoid coadministration with strong CYP3A inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole)
            • Avoid coadministration with potent CYP3A inducers (eg, rifampin, dexamethasone, phenytoin, carbamazepine, phenobarbital)
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            Pregnancy & Lactation

            Pregnancy Category: C

            In animal studies, caused structural abnormalities at maternal doses about 5-7 times the maximum recommended human dose (MRHD) based on body surface area

            Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus

            Lactation: Unknown whether distributed in human breast milk; potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue drug, taking into account the importance of the drug to the mother

            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.

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            Pharmacology

            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%

            Pharmacokinetics

            Bioavailability: 36%

            Peak Plasma Time: 1.5 hr; 2.5 hr (active metabolite)

            Protein Bound: >99% (including active metabolite)

            Vd: 88 L

            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)

            Excretion (ticagrelor): feces (58%); urine (26%)

            Excretion (active metabolite): Primarily by biliary excretion; urine (<1%)

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            Administration

            Instructions

            If patient has received a loading dose of clopidogrel, may be started on ticagrelor

            May administer with or without food

            If dose is missed, instruct patient to take one tablet (their next dose) at its scheduled time

            Unable to swallow tablet whole

            For patients who are unable to swallow the tablet(s) whole, tablets can be crushed, mixed with water, and drunk immediately

            The glass should be refilled with water, stirred and the contents drunk to ensure the complete dose is consumed

            The mixture can also be administered via a nasogastric tube (≥CH8)

            It is important to flush the nasogastric tube through with water after administration of the mixture

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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