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 ?
Thus, it can be speculated that ticagrelor may reduce the incidence of no-reflow by mediating the effects of increasing endogenous adenosine, thereby reducing the in-hospital mortality.
AstraZeneca will continue to work closely with the FDA to support the review of the new drug application (NDA) for ticagrelor, the company said.
The panel did not directly address other indications being sought by ticagrelor's maker, AstraZeneca, including in unstable angina and after a coronary artery bypass graft (CABG).
Ticagrelor was strongly recommended for patients with acute coronary syndrome (ACS),[1],[2] mainly according to the results of the PLATO trial.[3],[4] Consistent results were also reported in real-world studies such as the PRACTICAL study from the SWEDEHEART registry.[5] However, there was also conflicting evidence on the efficacy of ticagrelor among the East Asian population with ACS.
Among post-MI patients with diabetes, treatment with ticagrelor plus aspirin led to an absolute 1.5% reduction in the rate of cardiovascular death, another MI, or stroke during a median 33-month follow-up, compared with an absolute 1.1% cut in patients without diabetes, Dr.
"We believe that ticagrelor may become a new standard of care for the management of patients with STEMI intended for primary PCI," Dr.
Senior author Professor Philippe Gabriel Steg of Hospital Bichat, Paris, France said: Treatment with ticagrelor and aspirin also increased major bleeding relative to aspirin alone, but there was a net clinical benefit with dual antiplatelet therapy.
3, 2019 (HealthDay News) -- Ticagrelor plus aspirin compared with placebo plus aspirin is associated with a lower incidence of ischemic cardiovascular events but a higher incidence of major bleeding among patients with stable coronary artery disease and type 2 diabetes, according to a study published online Sept.
PhaseBio Pharmaceuticals announced that data from an evaluation of the pharmacodynamics of PB2452, a novel reversal agent for the antiplatelet drug ticagrelor, were presented by Lisa K.
Astra said Phase III THEMIS trial showed Brilinta, or ticagrelor, plus aspirin reduced the relative risk of cardiovascular death, heart attack, or stroke by 10% compared with aspirin alone in patients with coronary artery disease and type-2 diabetes.
AstraZeneca today announced detailed results from the positive Phase III THEMIS trial which showed Brilinta (ticagrelor) plus aspirin reduced the relative risk for the composite of cardiovascular (CV) death, heart attack, or stroke by 10% compared with aspirin alone, a statistically significant reduction.
PhaseBio Pharmaceuticals Inc (NASDAQ: PHAS): Phase 1 data for PB2452 as a reversal agent for AstraZeneca's ticagrelor.