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Ticagrelor: Uses,Dosage,Side Effects

Generic Name
Ticagrelor
Therapeutic Class:
Cardiovascular

Indications:
Acute Coronary Syndromes

Ticagrelor is a P2Y12 platelet inhibitor indicated to reduce the rate of thrombotic cardiovascular events in patients with the acute coronary syndrome (ACS) (unstable angina, non-ST elevation myocardial infarction, or ST-elevation myocardial infarction). Ticagrelor has been shown to reduce the rate of a combined endpoint of cardiovascular death, myocardial infarction, or stroke in ACS patients. In patients treated with percutaneous coronary intervention (PCI), it also reduces the rate of stent thrombosis.

Presentation:
Ticagrelor 90: Each tablet contains Ticagrelor INN 90 mg.

Description:
Ticagrelor, a cyclopentyl-triazolopyrimidine which is a reversible platelet aggregation inhibitor. Ticagrelor reversibly binds with the platelet P2Y12 adenosine diphosphate (ADP) receptor and thereby inhibits signal transduction and platelet aggregation.

Dosage & Administration:
Initiate Ticagrelor treatment with a 180 mg (two 90 mg tablets) loading dose and continue treatment with 90 mg twice daily. After the initial loading dose of aspirin (usually 325 mg), use Ticagrelor with a daily maintenance dose of aspirin of 75-100 mg.

Side Effects:
• Bleeding
• Dyspnea
• Other side effects (Headache, Back pain, Nausea, Dizziness, Cough, Hypotension, Fatigue, Atrial fibrillation)

Precautions:
• General Risk of Bleeding
Drugs that inhibit platelet function including Ticagrelor increase the risk of bleeding.
• Concomitant Aspirin Maintenance Dose
Use of Ticagrelor with maintenance doses of aspirin above 100 mg decreased the effectiveness of Ticagrelor. Therefore, after the initial loading dose of aspirin (usually 325 mg), use Ticagrelor with a maintenance dose of aspirin of 75-100 mg.
• Moderate Hepatic Impairment
Ticagrelor has not been studied in patients with moderate hepatic impairment.
• Discontinuation of Ticagrelor
Discontinuation of Ticagrelor will increase the risk of myocardial infarction, stent thrombosis, and death.

Use in Pregnancy & Lactation:
Pregnancy Category C, There are no adequate and well-controlled studies of Ticagrelor used in pregnant women. It is not known whether ticagrelor or its active metabolites are excreted in human milk.
Pediatric Use
The safety and effectiveness of Ticagrelor in pediatric patients have not been established.
Geriatric Use
No overall differences in safety or effectiveness were observed in patients of
Hepatic Impairment
Ticagrelor has not been studied in patients with moderate or severe hepatic impairment. Ticagrelor is metabolized by the liver and impaired hepatic function can increase risks for bleeding and other adverse events. Hence,
Renal Impairment
No dosage adjustment is needed in patients with renal impairment. Patients receiving dialysis have not been studied.

Interaction:
Avoid the use of strong inhibitors of CYP3A (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir, and telithromycin). Use of Ticagrelor with aspirin maintenance doses above 100 mg reduced the effectiveness of Ticagrelor. Ticagrelor will result in higher serum concentrations of simvastatin or rosuvastatin because these drugs are metabolized by CYP3A.

Overdose:
Other effects of an overdose may include gastrointestinal effects (e.g- nausea, diarrhea) or ventricular pauses. Proper management should be taken through ECG monitoring in severe bleeding.

Storage:
Protect from light & moisture. Store below 25° C. Keep out of reach of children

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