Indicated to reduce the rate of cardiovascular death, myocardial infarction (MI), and stroke in patients with acute coronary syndrome (ACS) or a history of myocardial infarction.
platelet aggregation inhibitor
Ticagrelor is a P2Y12 receptor antagonist. The P2Y12 receptor couples with Gαi2 and other Gi proteins which inhibit adenylyl cyclase. Gi mediated signalling also activates PI3K, Akt, Rap1b, and potassium channels. The downstream effects of these activities mediate hemostasis and lead to platelet aggregation. Antagonism of the P2Y12 receptor reduces development of occlusive thromboses, which can reduce the risk of myocardial infarction and ischemic stroke.
In combination with aspirin for the prevention of atherothrombotic events in patients with acute coronary syndrome BY MOUTH Adult: Initially 180 mg for 1 dose, then 90 mg twice daily usually for up to 12 months Alternative to clopidogrel in patients undergoing percutaneous coronary intervention BY MOUTH Adult: 180 mg, as a single dose
Effects of medicinal and other products on ticagrelor;
CYP3A4 inhibitors: Concomitant use of strong CYP3A4 clarithromycin, nefazodone, ritonavir, and atazanavir) inhibitors with ticagrelor is contraindicated.
CYP3A inducers: Co-administration of ticagrelor with potent CYP3A inducers (rifampicin)may decrease exposure and efficacy of ticagrelor, therefore, their concomitant use with ticagrelor is discouraged.
Cyclosporine (P-gp and CYP3A inhibitor): No data are available on concomitant use of ticagrelor with other active substances that also are potent P-gp inhibitors and moderate CYP3A4 inhibitors (e.g. verapamil, quinidine) that also may increase ticagrelor exposure. If the association cannot be avoided, their concomitant use should be made with caution.
Effects of ticagrelor on other medicinal products: Medicinal products metabolised by CYP3A4: The concomitant use of ticagrelor with doses of simvastatin or lovastatin greater than 40 mg is not recommended. Atorvastatin: Co-administration of atorvastatin and ticagrelor increased atorvastatin acid Cmax by 23% and AUC by 36%. Similar increases in AUC and Cmax were observed for all atorvastatin acid metabolites. These increases are not considered clinically significant. Ticagrelor is a mild CYP3A4 inhibitor. Co-administration of ticagrelor and CYP3A4 substrates with narrow therapeutic indices (i.e. cisapride or ergot alkaloids) is not recommended, as ticagrelor may increase the exposure to this medicinal products.
P-gp substrates (including digoxin, cyclosporine): Appropriate clinical and/or laboratory monitoring is recommended when giving narrow therapeutic index P-gp dependent medicinal products like digoxin concomitantly with ticagrelor.
Medicinal products metabolised by CYP2C9: Co-administration of ticagrelor with tolbutamide resulted in no change in the plasma levels of either medicinal product, which suggests that ticagrelor is not a CYP2C9 inhibitor and unlikely to alter the CYP2C9 mediated metabolism of medicinal products like warfarin and tolbutamide.
Oral contraceptives: No clinically relevant effect on oral contraceptive efficacy is expected when levonorgestrel and ethinyl estradiol is co-administered with ticagrelor.
Medicinal products known to induce bradycardia: No evidence of clinically significant adverse reactions were observed in the PLATO trial after concomitant administration with one or more medicinal products known to induce bradycardia (e.g. 96% beta blockers, 33% calcium channel blockers diltiazem and verapamil, and 4% digoxin).
Other concomitant therapy: No evidence of clinically significant adverse interactions with these medicinal products (acetylsalicylic acid, proton pump inhibitors, statins, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors and angiotensin receptor blockers) was observed. Due to potential pharmacodynamic interactions, caution should be exercised with the concomitant administration of ticagrelor with medicinal products (heparin, enoxaparin or desmopressin) known to alter haemostasis. Due to reports of cutaneous bleeding abnormalities with SSRIs (e.g. paroxetine, sertraline and citalopram), caution is advised when administering SSRIs with ticagrelor as this may increase the risk of bleeding.
Active bleeding . history of intracranial haemorrhage. Asthma . bradycardia (unless pacemaker fitted) . chronic obstructive pulmonary disease . discontinue 7 days before elective surgery if antiplatelet effect not desirable . history of hyperuricaemia . patients at increased risk of bleeding (e.g. from recent trauma, surgery, gastrointestinal bleeding, or coagulation disorders) . second- or third-degree AV block (unless pacemaker fitted) . sick sinus syndrome (unless pacemaker fitted)
Common or very common Bruising . dyspnoea . haemorrhage Uncommon Abdominal pain . diarrhoea . dizziness . dyspepsia . gastritis . headache . nausea . pruritus . rash . vomiting Rare Confusion . constipation . hyperuricaemia . paraesthesia . raised serum creatinine . vertigo
Manufacturer advises avoid?toxicity in animal studies. Manufacturer advises avoid?present in milk in animal studies
Ticagrelor is well tolerated in single doses up to 900 mg. Gastrointestinal toxicity was dose-limiting in a single ascending dose study. Other clinically meaningful adverse reactions which may occur with overdose include dyspnoea and ventricular pauses.
Store in a cool and dry place, protected from light.
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