Composition:

Ticagrelor 90 mg

Presentation:

Film-coated tablets

Indications and Dosage:

Ticagrelor 90 mg co-administered with acetylsalicylic acid (ASA), 75-100 mg is indicated for the prevention of thrombotic events (cardiovascular death, myocardial infarction and stroke) in patients with acute coronary syndromes (unstable angina, non-ST-elevation myocardial infarction [NSTEMI] or ST-elevation myocardial infarction [STEMI]), including patients with percutaneous coronary intervention (PCI) or coronary artery by-pass grafting (CABG).

Patients taking Ticagrelor should also take a daily low maintenance dose of ASA 75 – 100 mg, unless specifically contraindicated. Initiate Ticagrelor treatment with a 180 mg (two 90 mg tablets) loading dose and continue treatment with 90 mg twice daily.

Contraindications:

· History of intracranial hemorrhage.

· Active bleeding

· Severe hepatic impairment

· Hypersensitivity

· Co-administration with strong CYP3A4 inhibitors

Warnings and Precautions:

· General risk of bleeding: drugs that inhibit platelet function including ticagrelor increase the risk of bleeding.

· Use ticagrelor with a maintenance dose of aspirin of 75-100 mg. Concomitant use with high maintenance dose of aspirin (>300 mg) is not recommended.

· Hepatic impairment: usage in patients with moderate hepatic impairment has not been studied, consider the risks and benefits of the treatment. Use of ticagrelor is contraindicated in patients with severe hepatic impairment.

· Dyspnea: If dyspnea is determined to be related to ticagrelor, no specific treatment is required, continue ticagrelor without interruption.

· Central Sleep Apnea: has been reported in the post-marketing setting, further clinical assessment may be considered.

· Discontinuation of ticagrelor: will increase the risk of myocardial infarct, stent thrombosis, and death. If ticagrelor must be temporarily discontinued, restart it as soon as possible.

· Avoid use with strong CYP3A inhibitors.

· Avoid use with potent CYP3A inducers.

· Surgery: should be advised to inform physicians and dentists that they are taking ticagrelor before any surgery is scheduled.

· Patients with prior ischaemic stroke can be treated with ticagrelor for up to 12 months.

· Ticagrelor should be used with caution in patients at risk for bradycardic events.

· Creatinine levels may increase during treatment with ticagrelor.

· Hyperuricaemia may occur during treatment with ticagrelor.

· Treatment with ticagrelor has been reported to cause false negative result on functional tests for Heparin Induced Thrombocytopenia (HIT) or platelet functional tests.

Side Effects:

· Bleeding

· Non-hemorrhagic common adverse events (3% or more): dyspnea, headache, cough, dizziness, nausea, atrial fibrillation, hypertension, non-cardiac chest pain, diarrhea, back pain, hypotension, fatigue, chest pain.

Drug Interactions:

· Avoid use of strong inhibitors of CYP3A (e.g. ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir, dan telithromycin).

· Avoid use of potent inducers of CYP3A (e.g. rifampin, dexamethasone, phenytoin, carbamazepine, dan phenobarbital).

· Use of ticagrelor with aspirin maintenance dose above 100 mg reduced the effectiveness of ticagrelor.

· Ticagrelor is an inhibitor of CYP3A4/5 and the P-glycoprotein transporter.

· Simvastatin and lovastatin: avoid simvastatin and lovastatin doses greater than 40 mg.

· Digoxin: because of inhibition of the P-glycoprotein transporter, monitor digoxin levels with initiation of or any change in ticagrelor therapy.

· Cyclosporine: coadministration of cyclosporine (600 mg) with ticagrelor increased ticagrelor Cmax and AUC equal to 2.3 fold and 2.8 fold, respectively. If the association cannot be avoided, their concomitant use should be made with caution.

· Oral contraceptives: no clinically relevant effect on oral contraceptive efficacy is expected when levonorgestrel and ethinyl estradiol are coadministered with ticagrelor.

· Medicinal products known to induce bradycardia: caution should be exercised when administering ticagrelor concomitantly with medicinal products known to induce bradycardia.

FAQ

Pharmacology

What is the mechanism of action of Ticagrelor?

Ticagrelor and its main metabolite reversibly interacts with platelet ADP P2Y12 receptor to prevent signal transduction and platelet activation. Ticagrelor and its main metabolite is approximately equipotent.

Indication/Usage

What is the objective of consuming Ticagrelor?

Ticagrelor is to be given with aspirin to prevent thrombotic events in patients with acute coronary syndrome, including patients who are treated with percutaneous coronary intervention (PCI) or coronary artery bypass graft surgery (CABG).

Dosage & Administration

How frequent should Ticagrelor be consumed daily?

Ticagrelor should be consumed twice daily for its maintenance dose. Your Doctor will explain to you about the exact dose and frequency of ticagrelor that you should take.

What is the appropriate dose of Ticagrelor that should be consumed?

Your Doctor will decide the appropriate dose of Ticagrelor that you should take.

When is the appropriate time to consume Ticagrelor, before or after meal?

Ticagrelor could be consumed with or without meal.

Special Warnings & Precautions

Could Ticagrelor be given for children?

Safety and efficacy of Ticagrelor for children has not been established.

Could Ticagrelor be given for elderly?

There is no difference overall in terms of safety or efficacy that is observed between elderly or younger patients. Higher risk of sensitivity in several elderly individuals could not be ruled out.

Could Ticagrelor be given for pregnant and breastfeeding women?

Pregnancy category: C. Ticagrelor should only be given in pregnancy only if the potential benefit justified the treatment against the potential risk to the fetus. It is unknown whether ticagrelor or its active metabolite is excreted in breastmilk. Ticagrelor is excreted in breastmilk in mice. Due to numerous drug excreted in human breastmilk and due to potential serious side effects of Ticagrelor to the breastfed infants, decision has to be made whether to stop breastfeeding or the cessation of the drug.

Could Ticagrelor be given for patients with liver impairment?

Ticagrelor has not been studied in patients with moderate to severe liver impairment. Ticagrelor is contraindicated in patients with severe liver impairment. Dose adjustment for patients with mild liver impairment is unnecessary.

Could Ticagrelor be given for patients with renal impairment?

Dose adjustment for patients with renal impairment is unnecessary. Patients undergoing dialysis have not been studied.

Drug Interaction

How is the drug interaction between Ticagrelor and other drugs?

Ticagrelor is an inhibitor of CYP3A4/5 and p-glycoprotein transporter. Avoid concomitant use with strong inhibitors of CYP3A (e.g. ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir, and telithromycin) and strong inducers of CYP3A (e.g. rifampin, dexamethasone, phenytoin, carbamazepine, and phenobarbital). Avoid concomitant use of ticagrelor with aspirin maintenance dose above 100 mg, or simvastatin and lovastatin with dose greater than 40 mg. Be cautious with concomitant use with digoxin, cyclosporine, and other drugs known to cause bradycardia.

Side Effects

What are the common reported side effects of Ticagrelor?

The common reported side effects are: bleeding, dyspnea, headache, cough, dizziness, nausea, atrial fibrillation, hypertension, non-cardiac chest pain, diarrhea, back pain, hypotension, fatigue, and chest pain.

Storage

How should Ticagrelor be stored?

Ticagrelor should be stored in temperatures below 30 degrees Celsius

TICAGRELOR