BRILINTA Ticagrelor 90mg Film-Coated Tablet 1's
We recognize that purchasing medications can be a deeply personal matter. To respect your privacy, we ensure that all orders are packaged discreetly, with no indication of the contents on the packaging. This means that even our couriers remain unaware of the package contents.
Furthermore, we uphold strict confidentiality standards. We guarantee that your order information will never be disclosed to any third party. Your trust is paramount to us, and we are committed to safeguarding your privacy at every step of the process. Our dedication to discretion and confidentiality is part of our unwavering commitment to you, our valued customer.
Features
- Ticagrelor
Description
Indications/Uses
Dosage/Direction for Use
Patients taking Ticagrelor (BRILINTA) should also take a daily low maintenance dose of acetyl-salicylic acid (ASA) of 75-150 mg, unless specifically contraindicated. An initial loading dose of ASA is recommended for patients with ACS (see Pharmacology: Pharmacodynamics under Actions).
Missed dose: Lapses in therapy should be avoided. A patient who misses a dose of Ticagrelor (BRILINTA) should take their next dose at its scheduled time.
Premature discontinuation: Premature discontinuation with any antiplatelet therapy, including Ticagrelor (BRILINTA), could result in an increased risk of cardiovascular (CV) death, myocardial infarction (MI), or stroke due to the patient's underlying disease (see Precautions).
Switching: In patients having an ACS event, the loading dose of 180 mg should be given as soon as possible regardless of any previous antiplatelet treatment.
Physicians who desire to switch patients, with a prior ACS event to Ticagrelor (BRILINTA), should administer the first dose of Ticagrelor (BRILINTA) 24 hours following the last dose of the other anti-platelet medication.
Special Populations: Paediatric patients: Safety and efficacy in children below the age of 18 have not been established.
Elderly patients: No dose adjustment is required.
Patients with renal impairment: No dose adjustment is necessary for patients with renal impairment (see Pharmacology: Pharmacokinetics under Actions).
Patients with hepatic impairment: No dose adjustment is necessary for patients with mild hepatic impairment. Ticagrelor (BRILINTA) has not been studied in patients with severe hepatic impairment and there is limited information on treatment of patients with moderate hepatic impairment (see Contraindications, Precautions and Pharmacology: Pharmacokinetics under Actions).
Administration: For oral use. Ticagrelor (BRILINTA) can be taken with or without food.
For patients who are unable to swallow the tablet(s) whole, Ticagrelor (BRILINTA) tablets can be crushed to a fine powder and mixed in half a glass of water and drunk immediately. The glass should be rinsed with a further half glass of water and the contents drunk. The mixture can also be administered via a nasogastric tube (CH8 or greater). It is important to flush the nasogastric tube through with water after administration of the mixture.
Overdosage
Ticagrelor is well tolerated in single doses up to 900 mg. GI toxicity was dose-limiting in a single ascending dose study. Other clinically meaningful adverse effects which may occur with overdose include dyspnoea and ventricular pauses.
In the event of overdose, observe for these potential adverse effects and consider ECG monitoring.
Administration
Contraindications
Active pathological bleeding.
History of intracranial haemorrhage (see Adverse Reactions).
Severe hepatic impairment (see Dosage & Administration, Precautions and Pharmacology: Pharmacokinetics under Actions).
Special Precautions
Use In Pregnancy & Lactation
Pregnancy: No clinical study has been conducted in pregnant or lactating women.
Limited clinical data on exposure to Ticagrelor (BRILINTA) during pregnancy are available.
Animal studies do not indicate direct harmful effects with respect to pregnancy, embryonal/foetal development, parturition, or postnatal development.
Because animal reproduction studies are not always predictive of a human response, Ticagrelor should be used during pregnancy only if the potential benefit to the mother justifies any potential risks to the foetus.
Lactation: It is not known whether this medicinal product is excreted in human milk. Studies in rats have shown that Ticagrelor and active metabolites are excreted in the milk. The use of Ticagrelor (BRILINTA) during breastfeeding is not recommended.
Adverse Reactions
In PLATO, patients on Ticagrelor (BRILINTA) had a higher incidence of discontinuation of study drug due to adverse events than patients on clopidogrel (7.4% for ticagrelor 90 mg twice daily vs. 5.4% for clopidogrel 75 mg once daily).
In PEGASUS, patients on Ticagrelor (BRILINTA) had a higher incidence of discontinuation of study drug due to adverse events compared to ASA therapy alone (16.1% for ticagrelor 60 mg twice daily with ASA vs. 8.5% for ASA therapy alone).
In THEMIS patients who had undergone PCI, discontinuation of study drug due to adverse events was 21.3% for Ticagrelor (BRILINTA) in combination with ASA vs. 13.0% for ASA alone.
The most commonly reported adverse drug reactions in patients treated with ticagrelor were bleeding and dyspnoea (see also Precautions).
Tabulated list of adverse drug reactions: Adverse drug reactions determined from clinical studies with Ticagrelor (BRILINTA) are listed by MedDRA System Organ Class (SOC) and frequency category in Table 4. Within each SOC and frequency category, adverse drug reactions are presented in order of decreasing seriousness.
Drug Interactions
Diltiazem (Moderate CYP3A4 inhibitors): Co-administration of Ticagrelor and diltiazem increased the Cmax of Ticagrelor by 69% and AUC by 174%, and decreased the active metabolite Cmax by 38% and AUC was unchanged. There was no effect of Ticagrelor on diltiazem plasma levels. Other moderate CYP3A4 inhibitors (e.g. amprenavir, aprepitant, erythromycin, fluconazole, and verapamil) can as well be co-administered with Ticagrelor (BRILINTA).
Rifampin and Other CYP3A Inducers: Co-administration of rifampin with Ticagrelor decreased Ticagrelor Cmax and AUC by 73% and 86%, respectively. The Cmax of the active metabolite was unchanged and the AUC was decreased by 46%, respectively. Other CYP3A4 inducers (e.g. phenytoin, carbamazepine and phenobarbital) would be expected to decrease the exposure to Ticagrelor as well and may result in reduced efficacy of Ticagrelor (BRILINTA).
Cyclosporine (PgP and CYP3A inhibitor): Co-administration of cyclosporine (600 mg) with ticagrelor increased ticagrelor Cmax and AUC equal to 2.3-fold and 2.8-fold, respectively. The AUC of the active metabolite was increased by 32% and Cmax was decreased by 15% in the presence of cyclosporine. There was no effect of ticagrelor on cyclosporine blood levels.
Others: Clinical pharmacology interaction studies showed that co-administration of Ticagrelor with heparin, enoxaparin, and aspirin did not have any effect on Ticagrelor or the active metabolite plasma levels. Co-administration of Ticagrelor and heparin had no effect on heparin based on activated partial thromboplastin time (aPTT) and activated coagulation time (ACT) assays. Co-administration of Ticagrelor and enoxaparin had no effect on enoxaparin based on factor Xa assay.
Delayed and decreased exposure to oral P2Y12 inhibitors, including ticagrelor and its active metabolite, has been reported in patients treated with morphine (approximately 35% reduction in ticagrelor). This interaction may be related to reduced gastrointestinal motility, and therefore apply to other opioids. The clinical relevance is unknown.
Caution For Usage
Instructions for use, handling and disposal: No special requirements.
Storage
Action
Pharmacology: Pharmacodynamics: Mechanism of action: Ticagrelor (BRILINTA) contains Ticagrelor, a member of the chemical class cyclopentyltriazolopyrimidines (CPTP), which is an oral, direct acting, selective, and reversibly binding P2Y12 receptor antagonist that prevents adenosine diphosphate (ADP)-mediated P2Y12 dependent platelet activation and aggregation. Ticagrelor does not prevent ADP binding, but when bound to the P2Y12 receptor prevents ADP-induced signal transduction. Since platelets participate in the initiation and/or evolution of thrombotic complications of atherosclerotic disease, inhibition of platelet function has been shown to reduce the risk of cardiovascular events such as CV death, MI, or stroke.
Ticagrelor has an additional mechanism of action, increasing local endogenous adenosine levels by inhibiting equilibrative nucleoside transporter-1 (ENT-1). Adenosine is formed locally at sites of hypoxia and tissue damage through degradation of released adenosine tri- and di-phosphate (ATP and ADP). As adenosine degradation is essentially restricted to the intracellular space, inhibition of ENT-1 by ticagrelor prolongs the half-life of adenosine and thereby increases its local extracellular concentration providing enhanced local adenosine responses. Ticagrelor has no clinically significant direct effect on adenosine receptors (A1, A2A, A2B, A3) and is not metabolised to adenosine. Adenosine has been documented to have a number of effects that include: vasodilation, cardioprotection, platelet inhibition, modulation of inflammation, and induction of dyspnoea, which may contribute to the clinical profile of ticagrelor.
Pharmacodynamic effects: Onset of action: The inhibition of platelet aggregation (IPA) by ticagrelor and clopidogrel was compared in a 6-week study examining both acute and chronic platelet inhibition effects in response to 20μM ADP as the platelet aggregation agonist in patients with stable coronary artery disease (CAD) on ASA. The onset was evaluated following a loading dose of 180 mg ticagrelor or 600 mg clopidogrel.
Ticagrelor (BRILINTA) demonstrates a rapid onset of pharmacological effect as demonstrated by a mean IPA for Ticagrelor (BRILINTA) at 0.5 hours after 180 mg loading dose of about 41%, with the maximum IPA effect of 87.9% to 89.6% by 2-4 hours post dose. 90% of patients had final extent IPA >70% by 2 hours post dose. The high IPA effect of Ticagrelor (BRILINTA) between 87%-89% was maintained between 2-8 hours.