Each film coated tablets contains:
(Ticagrelor IP 90 mg)
Tablet for Oral Use
Ticagrelor is a novel non-thienopyridine platelet P2Y12 receptor antagonist, is the first oral agent in a new chemical class of cyclopentyl-triazolo-pyrimidines (CPTP). Ticagrelor selectively blocks the platelet P2Y12 receptor by interacting with a binding site different from ADP (non-competitive inhibition) and thus, inhibits the prothrombotic effects of ADP. Unlike thienopyridines, the binding of Ticagrelor to P2Y12 receptor is reversible.
Absorption: Ticagrelor is absorbed quickly from the gut, with a bioavailability of 36%. The peak plasma levels are reached in 1.5-3.0 hours. The antiplatelet effect is low at 48 hours after the last dose.
Distribution: Volume of distribution: (steady-state): 88 L
Protein bound: >99% (Ticagrelor and active metabolite).
Metabolism &Excretion: Ticagrelor is predominantly metabolized by CYP3A4 and to some extent by CYP3A5. Elimination occurs through biliary excretion.
Half Life: Its half-life is approximately 12 hours.
- To reduce the risk of cardiovascular death, myocardial infraction, and stroke in patients with acute coronary syndrome or a history of myocardial infarction
- To reduce the risk of a first myocardial infarction or stroke in high risk patients with coronary artery disease
- Indicated to reduce risk of stroke in patients with acute ischemic stroke or high-risk transient ischemic attack (TIA)
- Bleeding more easily than normal – nosebleeds, bruising or bleeding that takes longer to stop
- Unexpected shortness of breath while resting – this can sometimes happen in the first few weeks of taking Ticagrelor and is usually mild
- Pain and swelling in your joints – these can be signs of gout (this is because Ticagrelor can lead to high levels of uric acid in your blood
- Headaches, Dizziness, Feeling sick or indigestion, Diarrhea, Constipation, Mild rash
DOSAGE AND ADMINISTRATION: 180 mg loading dose followed by 90 mg BD
- Hypersensitivity (eg, angioedema)
- History of intracranial hemorrhage (ICH)
- Active pathologic bleeding (eg, peptic ulcer, ICH)
WARNINGS AND PRECAUTIONS
- Increases bleeding risk
- When possible, discontinue 5 days prior to 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
- Avoid use with severe hepatic impairment, which may increase Ticagrelor serum levels
- If central sleep apnea suspected, consider further clinical assessment
Pregnancy Category: C
- Ticagrelor increases serum concentrations of drugs metabolized by CYP3A4
- Coadministration of opioid agonists delay and reduce the absorption of Ticagrelor
- Strong CYP3A inducers substantially reduce Ticagrelor exposure and efficacy
- Aspirin maintenance doses >100 mg/day reduces Ticagrelor efficacy