ticagrelor


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Related to ticagrelor: Prasugrel

ticagrelor

(tye-ka-grel-or) ,

Brilinta

(trade name)

Classification

Therapeutic: antiplatelet agents
Pharmacologic: platelet aggregation inhibitors
Pregnancy Category: C

Indications

To decrease the incidence of thrombotic cardiovascular events associated with acute coronary syndrome (ACS).

Action

Both parent drug and its active metabolite inhibit platelet aggregation by reversibly interacting with platelet P2Y12ADP-receptors, preventing signal transduction and platelet activation.

Therapeutic effects

Reduced sequelae of ACS including cardiovascular death, MI and stroke.

Pharmacokinetics

Absorption: 36% absorbed following oral administration.
Distribution: Unknown.
Protein Binding: 99% for ticagrelor and its active metabolite.
Metabolism and Excretion: Mostly metabolized in the liver (CYP3A4 enzyme system, some metabolism by CYP3A5) with conversion to an active metabolite (AR-C124910XX); excretion primarily via biliary secretion; <1% excreted unchanged or as active metabolite in urine.
Half-life: Ticagrelor—7 hr; Active metabolite—9 hr.

Time/action profile (inhibition of platelet aggregation)

ROUTEONSETPEAKDURATION
POwithin 30 min4 hr5 days†
† Following discontinuation.

Contraindications/Precautions

Contraindicated in: HypersensitivityActive bleeding;History of intracranial bleeding;Severe hepatic impairment (increased risk of bleeding);Impending coronary artery bypass graft (CABG) surgery or other surgery (discontinue 5 days prior); Lactation: Avoid breast feeding;Strong inhibitors/inducers of CYP3A enzyme system (avoid concurrent use if possible).
Use Cautiously in: Moderate hepatic impairment (consider risks of increased levels);Hypotension following recent CABG or percutaneous coronary intervention (PCI) in patients receiving ticagrelor (consider bleeding as a cause); Geriatric: Some elderly patients may be more sensitive to effects; Obstetric: Use only during pregnancy if potential maternal benefit justifies potential risk to fetus; Pediatric: Safe and effective use has not been established.

Adverse Reactions/Side Effects

Cardiovascular

  • bradycardia

Respiratory

  • dyspnea (most frequent)

Endocrinologic

  • gynecomastia

Hematologic

  • bleeding (life-threatening)

Miscellaneous

  • hypersensitivity reactions including angioedema (life-threatening)

Interactions

Drug-Drug interaction

Strong inhibitors of CYP3A4/5 including atazanavir, clarithromycin, indinavir, intraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin and voriconazole ↑ levels and the risk of bleeding and should be avoided.Potent inducers of CYP3A including carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin may ↓ levels and effectiveness and should be avoided.Concurrent use of lovastatin or simvastatin in doses >40 mg/day ↑ risk of statin-related adverse reactions.Effectiveness is ↓ by aspirin >100 mg/day (maintain aspirin at 75–100 mg/day).May alter digoxin levels (monitoring recommended).Risk of bleeding ↑ by anticoagulants, fibrinolytics and chronic NSAIDs.

Route/Dosage

Oral (Adults) Loading dose—180 mg ; followed by maintenance dose—90 mg twice daily.

Availability

Tablets : 90 mg

Nursing implications

Nursing assessment

  • Assess patient for symptoms of stroke, peripheral vascular disease, or MI periodically during therapy.
  • Observe patient for signs and symptoms of hypersensitivity reactions (rash, facial swelling, pruritus, laryngeal edema, wheezing). Discontinue drug and notify health care professional immediately if symptoms occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in case of anaphylactic reaction.
  • Lab Test Considerations: May cause ↑ serum uric acid and ↑ serum creatinine.

Potential Nursing Diagnoses

Risk for injury (Adverse Reactions)

Implementation

  • Administer 180 mg (two 90 mg tablets) as a loading dose, followed by 90 mg twice daily. After initial 325 mg loading dose of aspirin, administer maintenance dose of 75–100 mg daily. Administer without regard for food.
    • Patients who have received a loading dose of clopidogrel may be started on ticagrelor.
    • Discontinue ticagrelor 5 days before planned surgical procedures. If ticagrelor must be temporarily discontinued, restart as soon as possible. Premature discontinuation of therapy may increase risk of myocardial infarction, stent thrombosis, and death.

Patient/Family Teaching

  • Instruct patient to take ticagrelor exactly as directed. Take missed doses as soon as possible unless almost time for next dose; do not double doses. Do not discontinue ticagrelor without consulting health care professional; may increase risk of cardiovascular events. Advise patient to read the Medication Guide before starting therapy and with each Rx refill in case of changes.
  • Advise patient that daily aspirin should not exceed 100 mg and to avoid taking other medications that contain aspirin.
  • Inform patient that they will bleed and bruise more easily and it will take longer to stop bleeding. Advise patient to notify health care professional promptly if unusual, prolonged, or excessive bleeding or blood in stool or urine occurs.
  • Inform patient that ticagrelor may cause shortness of breath which usually resolved during therapy. Advise patient to notify health care professional if unexpected or severe shortness of breath or symptoms of hypersensitivity reactions occur.
  • Advise patient to notify health care professional of medication regimen prior to treatment or surgery or dental procedure. Prescriber should be consulted before stopping ticagrelor.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially aspirin or NSAIDs.
  • Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Decreased thrombotic cardiovascular events in patients with acute coronary syndrome (ACS).
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References in periodicals archive ?
There were several reasons for ticagrelor monotherapy as an alternative for long-term platelet inhibition in this patient receiving primary PCI and thrombus aspiration.
The study's design gave each participating clinician free rein on whether to prescribe clopidogrel or ticagrelor (Brilinta) initially, and switching between the drugs was possible at any time after the initial prescription.
The study determined that ticagrelor was no better than aspirin in preventing recurrent stroke, heart attack, or death in patients who had a transient ischemic attack.
Biomarkers in relation to the effects of ticagrelor in comparison with clopidogrel in non-ST-elevation acute coronary syndrome patients managed with or without in-hospital revascularization: a substudy from the Prospective Randomized Platelet Inhibition and Patient Outcomes (PLATO)trial.
Clopidogrel: 600 mg bolus, 75 mg/day maintenance (if prasugrel and ticagrelor are contraindicated or not available) (Class IC)
Among post-MI patients with diabetes, treatment with ticagrelor plus aspirin led to an absolute 1.
We suspected clopidogrel resistance; hence the patient was treated with aspirin and ticagrelor therapy.
Astrazeneca Philippines introduces an exciting addition to its patient support program (PSP) to help more Filipino patients benefit from ticagrelor, an innovative medicine that can help save the lives of patients with acute coronary syndrome (ACS).
Ticagrelor is the newest ADP receptor antagonist and is in the cyclopentyltriazolopyrimidine class.
Ticagrelor (AZD 6140): New nonthienopyridinic antiplatelet drug with some pharmacokinetic advantages over prasugrel and clopidogrel (mainly because is not a pro-drug and does not need hepatic transformation into an active metabolite and its reversible platelet inhibition).
CARDIOVASCULAR DRUGS THAT MAY REACT WITH GRAPEFRUIT RISK DRUG POTENTIAL COMPLICATION VERY HIGH dronedarone (Multaq) torsades de pointes lovastatin (Mevacor) rhabdomyolysis simvastatin (Zocor) rhabdomyolysis HIGH amiodarone torsades de pointes (Cordarone) atorvastatin rhabdomyolysis (Lipitor) clopidogrel (Plavix) loss of efficacy * eplerenone (Inspra) high blood calcium levels, serious arrhythmias ticagrelor gastrointestinal or (Brilinta) kidney bleeding INTERMEDIATE felodipine (Plendil) low blood pressure, peripheral edema nifedipine low blood pressure, (Procardia) peripheral edema quinidine torsades de pointes (Quinidine) rivaroxaban gastrointestinal (Xarelto) bleeding * In 2010, it was reported that grapefruit renders certain drugs less effective or ineffective.