TICABIT

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)

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