TICABIT

Ticagrelor Tablets

Composition

Each film coated tablets contains:

(Ticagrelor  IP 90 mg)

Dosage Form

Tablet for Oral Use

Pharmacodynamics

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.

Pharmacokinetics

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.

Indications

  • 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)

Other Information

ADVERSE EFFECTS:

  • 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

    CONTRAINDICATIONS:

    • 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

    Drug Interaction:

    • 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