- March 15, 2022
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Brand Name :
Brilinta
Synonyms :
ticagrelor
Class :
Antiplatelet Agents, Platelet aggregation inhibitors
Dosage Forms & Strengths
Tablet
60mg
90mg
Loading dose (following ACS event): 180 mg orally, single dose
The maintenance dose (for 1st 12 months after diagnosis): 90 mg orally two times
The maintenance dose (after 12 months from diagnosis): 60 mg orally two times
Also, continue with aspirin 75-100 mg
Loading dose (following ACS event): 180 mg orally, single dose
The maintenance dose (for 1st 12 months after diagnosis): 90 mg orally two times
The maintenance dose (after 12 months from diagnosis): 60 mg orally two times
Also, continue with aspirin 75-100 mg
coronary artery atherosclerosis
60
mg
oraly
twice a day
Also, continue with aspirin 75-100 mg
Loading dose: 180 mg orally, single dose
Maintenance dose: 90 mg orally two times 30 days
Also, continue with aspirin with a loading dose (300-325 mg) and 75-100 mg for maintenance dose
CAD without a history of MI or stroke:
60
mg
Orally
twice a day
Tablet
provide together with a daily 75-100 mg aspirin maintenance dosage
Note:
Among individuals with coronary artery disease (CAD) who are at high risk for such events, to lower risk of first MI or stroke
The effectiveness was established in patients with type 2 diabetes mellitus, while use is not restricted to this situation (T2DM)
Use instead that precise dose for all Acute Coronary Syndrome patients.
Refer adult dosing
may have an increased anticoagulant effect when combined with heparin
morphine (Systemic): they may decrease the antiplatelet effect of Antiplatelet Agents (P2Y12 Inhibitors)
may enhance the serum concentration when combined
caplacizumab: they may increase the toxic effect of Antiplatelet agents
The GI absorption inhibition caused by codeine results in a decrease in the level or effectiveness of ticagrelor
CYP3A enhancers (strong) may decrease plasma concentrations of the active metabolite(s) of ticagrelor
may increase the antiplatelet effect
may enhance the risk of adverse effect of thrombolytic agents
may enhance the adverse/toxic effect of anticoagulants
may enhance the adverse/toxic effect of anticoagulants
may enhance the adverse/toxic effect of anticoagulants
may enhance the adverse/toxic effect of anticoagulants
may enhance the adverse/toxic effect of anticoagulants
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
choline magnesium trisalicylate
may have an increasingly adverse effect when combined with salicylates
ticagrelor: they may diminish serum concentrations of CYP3A4 Inducers
ticagrelor: they may diminish serum concentrations of CYP3A4 Inducers
ticagrelor: they may diminish serum concentrations of CYP3A4 Inducers
ticagrelor: they may diminish serum concentrations of CYP3A4 Inducers
ticagrelor: they may diminish serum concentrations of CYP3A4 Inducers
It may enhance the risk of adverse reactions when combined with P2Y12 inhibitors
It may enhance the risk of adverse reactions when combined with P2Y12 inhibitors
It may enhance the risk of adverse reactions when combined with P2Y12 inhibitors
It may enhance the risk of adverse reactions when combined with P2Y12 inhibitors
nafcillin will decrease the effect of action of ticagrelor by affecting enzyme CYP3A4 metabolism.
the effect of ticagrelor is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
it may increase the antiplatelet effect of other antiplatelets agents
may increase the anti-platelet effect
may increase the antiplatelet effect of antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may increase the antiplatelet effect of other antiplatelet agents
may have an increasingly adverse effect when combined with Cephalothin
may have an increasingly adverse effect when combined with Deoxycholic Acid
may increase the antiplatelet effect of nonsteroidal anti-inflammatory agents
may have an increased adverse effect when combined with ibritumomab tiuxetan
other antiplatelet agents increase the effect of anticoagulating agents
other antiplatelet agents increase the effect of anticoagulating agents
other antiplatelet agents increase the effect of anticoagulating agents
other antiplatelet agents increase the effect of anticoagulating agents
other antiplatelet agents increase the effect of anticoagulating agents
other antiplatelet agents increase the toxicity of apixaban
antiplatelet agents increase the effect of thrombolytic agents
it increases the effect of antiplatelet agents
antiplatelet agents increase the toxicity of obinutuzumab
they increase the efficacy of antiplatelet agents
it increases the efficacy of antiplatelet agents
it increases the efficacy of antiplatelet agents
it increases the toxicity of antiplatelet agents
it increases the effect of antiplatelet agents
other antiplatelet agents increase the anticoagulative effect of rivaroxaban
it increases the toxicity of antiplatelet agents
lipid emulsion (plant oil-based)
lipid emulsion: they may increase the toxic effect of antiplatelet agents
prostacyclin: they may increase the antiplatelet effect of antiplatelet agents
prostacyclin: they may increase the antiplatelet effect of antiplatelet agents
prostacyclin: they may increase the antiplatelet effect of antiplatelet agents
l-methylfolate-pyridoxal 5′-phosphate-methylcobalamine
multivitamins: they may increase the antiplatelet effect of antiplatelet agents
dasatinib: they may increase the anticoagulant effect antiplatelet properties
naftazone : they may increase the antiplatelet effect of antiplatelet agents
porfimer: they may increase the toxic effect of antiplatelet agents
other antiplatelet agents increase the anticoagulative effect of enoxaparin
Actions and Spectrum:
Actions:
Spectrum:
Adverse drug reactions:
Frequency Defined
>10%
Dyspnea
1-10%:
ECG abnormality
Hemorrhage
Dizziness
Increased serum creatinine
Nausea
Gout
Frequency not defined
Increased uric acid
Post-marketing:
AV block
Black Box Warning:
The black box warning for ticagrelor states that it may cause bleeding, which can be serious and sometimes lead to death. The warning also states that ticagrelor should not be used in patients who have a history of bleeding or a high risk of bleeding, such as those with a history of stroke or intracranial hemorrhage.
Contraindication / Caution:
Contraindications:
Cautions:
Pregnancy warnings:
AU TGA pregnancy category: B1
US FDA pregnancy category: C
Lactation:
Excreted into human milk is unknown
Pregnancy Categories:
Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.
Category B: No evidence shown of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a result in humans must take care of potential risks in pregnant women
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
ticagrelor is a medication used to prevent blood clots in individuals who have had a heart attack or stroke. It belongs to a class of drugs known as P2Y12 inhibitors, which work by blocking the activity of the P2Y12 receptor on platelets (a type of blood cell involved in clotting).
Pharmacodynamics:
ticagrelor works by inhibiting the P2Y12 receptor on platelets, which prevents the activation of the platelets and reduces the formation of clots. This results in a decrease in the formation of thrombi (blood clots) and an increase in the formation of fibrin (a protein that helps in the formation of blood clots).
Pharmacokinetics:
Absorption
It is rapidly absorbed following oral administration, with a mean peak plasma concentration (Cmax) of approximately 1.8 ng/mL achieved within 2-3 hours. The oral bioavailability of ticagrelor is approximately 90%.
Distribution
It is highly protein bound (over 99%) to plasma proteins, primarily to albumin. The volume of distribution of ticagrelor is approximately 140 L
Metabolism
It is metabolized by cytochrome P450 (CYP) enzymes, primarily by CYP3A4
Elimination and excretion
The elimination half-life of ticagrelor is approximately 12 hours. Ticagrelor and its active metabolite are primarily eliminated in the feces (approximately 84% of the dose) with minimal excretion in the urine (less than 2% of the dose).
Administration:
Oral administration
ticagrelor is a medication used to prevent blood clots in patients with acute coronary syndrome (ACS) or a history of heart attack or stroke. It is typically administered as an oral tablet, taken twice daily with or without food.
The usual starting dose of ticagrelor is 180 mg (two 90 mg tablets) taken once a day, followed by 90 mg (one 90 mg tablet) taken twice a day, starting the day after the first dose. The dosage may be adjusted based on the patient’s response to the medication and potential side effects.
It is important to note that ticagrelor should not be used in patients with severe liver or kidney dysfunction and should be used with caution in patients with a history of bleeding or a higher risk of bleeding. Patients should also inform their healthcare provider if they are taking any other medications that may interact with ticagrelor, such as blood thinners or non-steroidal anti-inflammatory drugs (NSAIDs)
Patient Information Leaflet
Generic Name: ticagrelor
Why do we use ticagrelor?
ticagrelor is a medication used to prevent blood clots in people with acute coronary syndrome (ACS) such as heart attack and unstable angina, as well as in people who have had a procedure called a percutaneous coronary intervention (PCI), such as angioplasty or stenting. It works by inhibiting a protein called P2Y12, which is involved in the formation of blood clots. By blocking this protein, ticagrelor helps to prevent clots from forming and reduces the risk of further cardiac events. ticagrelor is usually taken twice a day in combination with aspirin
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