Brilinta

Brilinta Uses, Dosage, Side Effects, Food Interaction and all others data.

Brilinta is a selective adenosine diphosphate (ADP) receptor antagonist acting on the P2Y12 ADP-receptor that can prevent ADP-mediated platelet activation and aggregation. Brilinta reversibly interacts with the platelet P2Y12 ADP-receptor.Brilinta does not interact with the ADP binding site itself, but interacts with platelet P2Y12 ADP-receptor to prevent signal transduction.Thus it prevents platelet activation & aggregation.

Brilinta is a P2Y12 receptor antagonist that inhibits the formation of thromboses to reduce the risk of myocardial infarction and ischemic stroke. It has a moderate duration of action as it is given twice daily, and a wide therapeutic index as high single doses are well tolerated. Patients should be counselled regarding the risk of bleeding, dyspnea, and bradyarrhythmias.

Trade Name Brilinta
Availability Prescription only
Generic Ticagrelor
Ticagrelor Other Names Ticagrelor
Related Drugs Brilinta, Praluent, Repatha, amlodipine, aspirin, lisinopril, metoprolol, propranolol, Xarelto, clopidogrel
Weight 90mg, , 60mg
Type Tablet, Film Coated, Oral Tablet
Formula C23H28F2N6O4S
Weight Average: 522.568
Monoisotopic: 522.186080514
Protein binding

Ticagrelor and its active metabolite ate >99% protein bound in plasma, particularly albumin.

Groups Approved
Therapeutic Class Anti-platelet drugs
Manufacturer Astrazeneca Pharma India Ltd, Ziska Pharmaceuticals Ltd
Available Country India, Bangladesh, Canada, Australia, Saudi Arabia, United States,
Last Updated: September 19, 2023 at 7:00 am
Brilinta
Brilinta

Uses

Brilinta is used for the prevention of atherothrombotic events in adult patients with Acute Coronary Syndromes (unstable angina, non ST elevation Myocardial Infarction [NSTEMI] or ST elevation Myocardial Infarction [STEMI]); including patients managed medically, and those who are managed with percutaneous coronary intervention (PCI) or coronary artery by-pass grafting (CABG).

Brilinta is also used to associated treatment for these conditions: Cardiovascular Mortality, Myocardial Infarction, Myocardial Infarction First, Stent Thrombosis, Stroke

How Brilinta works

Brilinta 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.

Dosage

Brilinta dosage

Brilinta treatment should be initiated with a single 180 mg loading dose (two tablets of 90 mg) and then continued at 90 mg twice daily. Patients taking Brilinta should also take aspirin daily, unless specifically contraindicated. Following an initial dose of aspirin (usually 325 mg), Brilinta should be used with a maintenance dose of aspirin of 75-100 mg. Maintenance dose of Aspirin above 100 mg decreased the efficacy of Brilinta. So, maintenance dose of aspirin above 100 mg should be avoided.

A patient who misses a dose of Brilinta should take only one 90 mg tablet (the next dose) at its scheduled time. Patients treated with Clopidogrel can be directly switched to Brilinta if needed. Switching from prasugrel to ticagrelor has not been investigated.

Treatment is recommended for up to 12 months unless discontinuation of Brilinta is clinically indicated. Brilinta can be administered with or without food.

Side Effects

Dyspnea,bleeding,headache,cough,dizziness,nausea,atrial fibrillation, hypertension, non-cardiac chest pain, diarrhea, back pain, hypotension, fatigue, chest pain.

Toxicity

Patients experiencing an overdose may present with bleeding, nausea, vomiting, diarrhea, and ventricular pauses. Overdose can be managed through symptomatic and supportive treatment, including ECG monitoring. Dialysis is not expected to remove ticagrelor from the blood due to it being highly protein bound.

Precaution

General Risk of Bleeding: Drugs that inhibit platelet function including Brilinta increase the risk of bleeding.

Concomitant Aspirin Maintenance Dose: Use of Brilinta with maintenance doses of aspirin above 100 mg decreased the effectiveness of Brilinta. Therefore, after the initial loading dose of aspirin (usually 325 mg), use Brilinta with a maintenance dose of aspirin of 75-100 mg.

Moderate Hepatic Impairment: Brilinta has not been studied in patients with moderate hepatic impairment.

Discontinuation of Brilinta: Discontinuation of Brilinta will increase the risk of myocardial infarction, stent thrombosis, and death.

Interaction

CYP3A inhibitors: Avoid use of strong inhibitors of CYP3A (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir and telithromycin).

CYP3A inducers: Avoid use with potent inducers of CYP3A (e.g., rifampin, dexamethasone, phenytoin,carbamazepine and phenobarbital).

Aspirin: Use of Brilinta with aspirin maintenance doses above 100 mg reduced the effectiveness ofBrilinta.

Simvastatin, Lovastatin: Brilinta will result in higher serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4. Avoid simvastatin and lovastatin doses greater than 40 mg.

Digoxin: Because of inhibition of the P-glycoprotein transporter, monitor digoxin levels with initiation of or any change in ticagrelor therapy.

Other Concomitant Therapy: Brilinta can be administered with unfractionated or low-molecular-weight heparin, GPIIb/llla inhibitors, proton pump inhibitors, beta-blockers, angiotensin converting enzyme inhibitors, and angiotensin receptor blockers.

Food Interaction

  • Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of ticagrelor, which may increase its serum concentration.
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Herbs with antiplatelet activity may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of ticagrelor and may reduce its serum concentration.
  • Take with or without food.

Volume of Distribution

The steady state volume of distribution of ticagrelor is 88 L.

Elimination Route

Brilinta is 36% orally bioavailable. A single 200mg oral dose of ticagrelor reaches a Cmax of 923ng/mL, with a Tmax of 1.5 hours and an AUC of 6675ng*h/mL. The active metabolite of ticagrelor reaches a Cmax of 264ng/mL, with a Tmax of 3.0 hours and an AUC of 2538ng*h/mL.

Half Life

Brilinta has a plasma half life of approximately 8 hours, while the active metabolite has a plasma half life of approximately 12 hours.

Clearance

The renal clearance of ticagrelor is 0.00584L/h.

Elimination Route

A radiolabelled dose of ticagrelor is 57.8% recovered in feces and 26.5% recovered in urine. Less than 1% of the dose is recovered as the unmetabolized parent drug. The active metabolite AC-C124910XX makes up 21.7% of the recovery in the feces. The metabolite AR-C133913XX makes up 9.2% of the recovery in the urine and 2.7% of the recovery in the feces. Other minor metabolites are predominantly recovered in the urine.

Pregnancy & Breastfeeding use

Pregnancy category C. There are no or limited amount of data from the use of Brilinta in pregnant women.Brilinta is not recommended during pregnancy.

Nursing mothers: Available pharmacodynamic/toxicological data in animals have shown excretion of Brilinta and its active metabolites in milk. A risk to newborns/infants cannot be excluded. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from ticagrelor therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the women.

Contraindication

Brilinta is contraindicated in case of-

  • Hypersensitivity to Brilinta or to any of the excipients
  • Active pathological bleeding (peptic ulcer)
  • History of intracranial haemorrhage
  • Moderate to severe hepatic impairment
  • Co-administration of Brilinta with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, nefazodone, ritonavir, and atazanavir)

Special Warning

Pediatric Use: The safety and effectiveness of Brilinta in pediatric patients have not been established.

Geriatric Use: No overall differences in safety or effectiveness were observed in geriatric patients.

Hepatic Impairment: Brilinta has not been studied in the patients with moderate or severe hepatic impairment. Brilinta 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.

Acute Overdose

There is currently no known antidote to reverse the effects ofBrilinta and it is not expected to be dialysable.Treatment of overdose should follow local standard medical practice.The expected effect of excessive ticagrelor dosing is prolonged duration of bleeding risk associated with platelet inhibition. If bleeding occurs appropriate supportive measures should be taken.

Storage Condition

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

Innovators Monograph

You find simplified version here Brilinta

Brilinta contains Ticagrelor see full prescribing information from innovator Brilinta Monograph, Brilinta MSDS, Brilinta FDA label

FAQ

What Brilinta is used for?

Brilinta usue to makes your blood flow through your veins more easily. This means your blood will be less likely to make a dangerous blood clot. Taking Brilinta can help prevent blood clots if you have an increased risk of having them.

How safe is Brilinta?

This meta-analysis suggests that Brilinta was more effective, but less safe than clopidogrel and prasugrel in patients with ACS.

What are the common side effect of Brilinta?

More common side effects are include:

  • Back pain
  • bleeding gums
  • blurred vision
  • chest pain, tightness, or discomfort
  • confusion
  • cough
  • coughing up blood
  • difficult or trouble breathing
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • fast, slow, or irregular heartbeat
  • headache
  • increased menstrual flow or vaginal bleeding
  • lightheadedness, dizziness, or fainting
  • loss of consciousness
  • nausea or vomiting
  • nervousness
  • nosebleeds
  • paralysis
  • pounding in the ears
  • prolonged bleeding from cuts
  • red or black, tarry stools
  • red or dark brown urine
  • sweating
  • unusual bleeding or bruising
  • unusual tiredness or weakness

How long does Brilinta stay in your system?

The mean half-life is approximately 7 hours for Brilinta and 9 hours for the active metabolite.

Is Brilinta safe in pregnancy?

Brilinta is not recommended during pregnancy or if you're trying to get pregnant.

Is Brilinta safe during breastfeeding?

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Can I drink alcohol with Brilinta?

You can drink alcohol with Brilinta. But do not drink too much as it can irritate your stomach. You may need to stop taking Brilinta for a short time before having surgery or dental treatment.

Is there any food or drink Interactions with Brilinta?

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. 

How quickly does Brilinta work?

Brilinta works within 30 minutes of taking your first dose of two 90mg tablets.

What are the benefits of Brilinta?

Benefits of Brilinta can help reduce the risk of a first heart attack or stroke in high-risk patients with coronary artery disease, the most common type of heart disease.

What happens if I miss a dose?

If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

When should I stop using Brilinta?

If you are having surgery, your doctor may instruct you to stop taking Brilinta 5 days before your procedure.

Can Brilinta cause gout?

Brilinta can increase the level of uric acid in your blood and cause a flare up of gout.

Can Brilinta cause Anaemia?

A not negligible proportion of patients treated with Brilinta met criteria for anemia.

What happens when I stop taking Brilinta?

If you stop taking Brilinta, you'll have an increased risk of a heart attack, stroke, and death.

Is Brilinta blood thinner?

Is a blood-thinner used to reduce cardiovascular death and heart attack in patients with acute coronary syndromes.

*** Taking medicines without doctor's advice can cause long-term problems.
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