Ticagrelor

Ticagrelor is a prescription medication used to treat Acute Coronary Syndrome or History of Myocardial Infarction (MI), Coronary Artery Disease, Acute Ischemic Stroke, or Transient Ischemic Attack (TIA). 

• Ticagrelor is available under the following different brand names: Brilinta

Dosages of Ticagrelor:

Adult dosage

Tablet

• 60mg
• 90mg

Acute Coronary Syndrome or History of Myocardial Infarction (MI)

Adult dosage

• Loading dose (following ACS event); 180 mg orally x 1 dose
• The maintenance dose (for the first year following ACS event): 90 mg orally twice daily
• The maintenance dose (after 1 year of maintenance): 60 mg orally twice daily
• Administer with a daily maintenance dose of aspirin 75-100 mg; the use of aspirin above 100 mg decreases the effectiveness of Ticagrelor

Coronary Artery Disease (CAD)

Adult dosage

• CAD, but no prior stroke or MI: 60 mg orally twice daily
• Administer with a daily maintenance dose of aspirin 75-100 mg
• For patients with ACS, use that specific dosing instead

Acute Ischemic Stroke or Transient Ischemic Attack (TIA)

Adult dosage

• Loading dose: 180 mg orally x 1 dose
• Maintenance dose: 90 mg orally twice for up to 30 days
• Use with a loading dose of aspirin (300-325 mg) and daily maintenance dose of 75-100 mg

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”.

Common side effects of Ticagrelor include:

• bleeding, and 
• shortness of breath 

Serious side effects of Ticagrelor include:

• hives, 
• difficulty breathing, 
• swelling of the face, lips, tongue, or throat, 
• slow heartbeats, 
• nosebleeds, 
• any bleeding that will not stop, 
• shortness of breath, 
• easy bruising, 
• unusual bleeding, 
• purple or red spots under the skin, 
• red, pink, or brown urine, 
• black, bloody, or tarry stools, 
• coughing up blood, and
• vomit that looks like coffee grounds

Rare side effects of Ticagrelor include:

• none 

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them.  Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Ticagrelor has severe interactions with the following other drugs:
  • flibanserin
  • itraconazole
  • lomitapide 
• Ticagrelor has serious interactions with at least 31 other drugs. 
• Ticagrelor has moderate interactions with at least 125 other drugs.
• Ticagrelor has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drugs interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use.  Keep a list of all your medications with you, and share this information with your doctor and pharmacist.  Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns.

Contraindications

• Hypersensitivity (eg, angioedema)
• History of intracranial hemorrhage (ICH)
• Active pathological bleeding (eg, peptic ulcer, ICH)

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Ticagrelor?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Ticagrelor?”

Cautions

• Inhibits platelet function, and thereby, increases bleeding risk; if possible, manage bleeding without discontinuing drug; stopping ticagrelor increases risk of subsequent cardiovascular events
• Discontinuation of therapy will increase the risk of myocardial infarction, stroke, and death in patients being treated for coronary artery disease; if drug must be temporarily discontinued (eg, to treat bleeding or for significant surgery), restart it as soon as possible; when possible, interrupt therapy for five days before surgery that has a major risk of bleeding and resumes therapy as soon as hemostasis is achieved
• Surgery: When possible, discontinue 5 days before surgery
• 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
• Can cause ventricular pauses; bradyarrhythmias, including AV block, reported; patients with a history of sick sinus syndrome, 2nd or 3rd degree AV block, or bradycardia-related syncope who were 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 may increase ticagrelor serum levels
• Reported to cause false-negative results in platelet functional tests (eg, HIPA assay for HIT)
• Central sleep apnea (CSA) including Cheyne-Stokes respiration (CSR) reported in post-marketing setting, including recurrence or worsening of CSA/CSR the following rechallenge; if central sleep apnea is suspected, consider further clinical assessment

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 over 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 over 100 mg/day reduce ticagrelor efficacy

Pregnancy and Lactation

• There are no adequate and well-controlled studies of Ticagrelor in pregnant women
• Available data from case reports on use in pregnant females have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
• 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 is no information regarding the presence of Ticagrelor in human milk, the effects on the breastfed infant, or the effects 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, the drug will likely be present in human milk
• Advise a nursing woman not to breastfeed during treatment