Cardiovascular DiseasesBrand Brilinta (Generic)
Generic drugs, marketed without brand names, contain the exact same active ingredients used in their brand-name counterparts, but cost significantly less. The drugs are required to meet US Food and Drug Administration (FDA) standards for safety, purity and effectiveness.
Brilinta®
After suffering from a heart attack or severe chest pain (angina), patients can take Brilinta® to prevent the formation of blood clots in order to reduce their likelihood of experiencing a stroke or other significant heart issues in the future.
Brilinta® (ticagrelor) is an antiplatelet medication used to reduce the risk of cardiovascular events, such as heart attacks and strokes, in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI). Developed by AstraZeneca, Brilinta® was approved by the U.S. Food and Drug Administration (FDA) in 2011 and has since become a key therapeutic option in the management of cardiovascular diseases. This article provides an in-depth exploration of Brilinta®, including its mechanism of action, clinical indications, pharmacokinetics, safety profile, and place in therapy.
Mechanism of Action
Brilinta® belongs to a class of drugs known as P2Y12 platelet inhibitors. It works by reversibly binding to the P2Y12 adenosine diphosphate (ADP) receptor on platelets, preventing ADP from activating the receptor. ADP is a key mediator in the platelet aggregation process, which is essential for blood clot formation. By inhibiting this pathway, Brilinta® reduces the likelihood of thrombus formation in arteries, thereby decreasing the risk of cardiovascular events.
Unlike clopidogrel, another P2Y12 inhibitor, ticagrelor does not require metabolic activation and has a faster onset of action. Additionally, its binding to the P2Y12 receptor is reversible, allowing for quicker restoration of platelet function after discontinuation compared to irreversible inhibitors like clopidogrel.
Clinical Indications
Brilinta® is primarily indicated for the following conditions:
Acute Coronary Syndrome (ACS):
Brilinta® is used in patients with ACS, including unstable angina, non-ST-elevation myocardial infarction (NSTEMI), and ST-elevation myocardial infarction (STEMI).
It is typically administered in combination with low-dose aspirin to provide dual antiplatelet therapy (DAPT), which has been shown to significantly reduce the risk of recurrent cardiovascular events.
Secondary Prevention of Cardiovascular Events:
In patients with a history of myocardial infarction, Brilinta® is used to prevent further cardiovascular events, such as heart attacks or strokes.
The PEGASUS-TIMI 54 trial demonstrated the efficacy of ticagrelor in reducing the risk of major adverse cardiovascular events (MACE) in this patient population.
Coronary Artery Disease (CAD):
Brilinta® may also be used in patients with coronary artery disease who are at high risk for ischemic events.
Pharmacokinetics and Dosage
Absorption: Ticagrelor is rapidly absorbed after oral administration, with peak plasma concentrations achieved within 1.5 to 3 hours.
Metabolism: It is primarily metabolized by the liver via the cytochrome P450 3A4 (CYP3A4) enzyme system. The active metabolite, AR-C124910XX, contributes to its antiplatelet effects.
Elimination: The half-life of ticagrelor is approximately 7 to 9 hours, and it is excreted mainly in the feces and, to a lesser extent, in the urine.
Dosage Recommendations:
For ACS: An initial loading dose of 180 mg is followed by a maintenance dose of 90 mg twice daily.
For secondary prevention: A lower maintenance dose of 60 mg twice daily may be used.
Efficacy and Clinical Trials
The efficacy of Brilinta® has been demonstrated in several landmark clinical trials:
PLATO Trial (Platelet Inhibition and Patient Outcomes):
This pivotal trial compared ticagrelor with clopidogrel in patients with ACS.
Ticagrelor significantly reduced the composite endpoint of cardiovascular death, myocardial infarction, and stroke without increasing the risk of major bleeding.
PEGASUS-TIMI 54 Trial:
This study evaluated the long-term use of ticagrelor in patients with a history of myocardial infarction.
Ticagrelor reduced the risk of MACE but was associated with a higher risk of bleeding compared to placebo.
THEMIS Trial:
This trial investigated the use of ticagrelor in patients with type 2 diabetes and stable coronary artery disease.
Ticagrelor reduced ischemic events but increased bleeding risk, highlighting the need for careful patient selection.
Safety Profile and Adverse Effects
While Brilinta® is effective in reducing cardiovascular events, it is not without risks. Common adverse effects include:
Bleeding: The most significant risk associated with Brilinta® is bleeding, including life-threatening and fatal bleeding events. Patients should be closely monitored for signs of bleeding.
Dyspnea: Ticagrelor has been associated with dyspnea (shortness of breath), which is usually mild to moderate and resolves without discontinuation of therapy.
Bradycardia: Some patients may experience slow heart rate, particularly during the initial phase of treatment.
Other Side Effects: Headache, dizziness, and gastrointestinal symptoms (e.g., nausea, diarrhea) have also been reported.
Contraindications:
Brilinta® is contraindicated in patients with active pathological bleeding, a history of intracranial hemorrhage, or severe hepatic impairment.
It should be used with caution in patients taking strong CYP3A4 inhibitors or inducers, as these can affect ticagrelor levels.
Drug Interactions
Brilinta® has several important drug interactions:
CYP3A4 Inhibitors: Drugs like ketoconazole, clarithromycin, and ritonavir can increase ticagrelor levels, raising the risk of bleeding.
CYP3A4 Inducers: Medications such as rifampin and phenytoin can decrease ticagrelor levels, reducing its efficacy.
Aspirin: High-dose aspirin (>100 mg daily) may diminish the effectiveness of ticagrelor. Therefore, low-dose aspirin is recommended for concomitant use.
Place in Therapy
Brilinta® has established itself as a valuable option in the management of ACS and secondary prevention of cardiovascular events. Its rapid onset of action, reversible binding, and proven efficacy in reducing ischemic events make it a preferred choice in many clinical scenarios. However, its use must be balanced against the risk of bleeding, and careful patient selection is essential.
Compared to other P2Y12 inhibitors, such as clopidogrel and prasugrel, Brilinta® offers unique advantages, including faster onset and reversibility. However, the choice of antiplatelet therapy should be individualized based on patient characteristics, bleeding risk, and comorbidities.
Conclusion
Brilinta® (ticagrelor) represents a significant advancement in antiplatelet therapy, offering robust protection against cardiovascular events in high-risk patients. Its unique pharmacological profile, demonstrated efficacy in clinical trials, and manageable safety profile make it a cornerstone in the treatment of ACS and secondary prevention of cardiovascular disease. However, like all medications, it requires careful consideration of risks and benefits, and its use should be guided by evidence-based guidelines and clinical judgment. As research continues, Brilinta® is likely to remain a key player in the fight against cardiovascular disease.
Ticagrelor is an acronym for what?
Ticagrelor works to reduce the risk of blood clots by reducing the likelihood that platelets in your blood may clump together and attach to one another. Some diseases that affect the heart or blood vessels might lead to the formation of an unwelcome blood clot.
Ticagrelor is prescribed to patients who have suffered a heart attack or an episode of significant chest pain in order to reduce the likelihood that they would experience a stroke or develop major cardiac issues in the future (angina).
Moreover, this medicine guide does not include all of the possible applications for ticagrelor.
Information That Is Vital
If you have severe liver illness, any current bleeding (including a bleeding stomach ulcer), or a history of bleeding in the brain, you should not use ticagrelor. Ticagrelor can increase the risk of bleeding in the brain. Do not take this medication in the days leading up to your heart bypass operation (coronary artery bypass graft, or CABG).
In order to prevent excessive bleeding during surgery or dental procedures, it is possible that you will be required to temporarily discontinue the use of ticagrelor. Even if you see indications of bleeding, you should not stop taking ticagrelor before consulting with your primary care physician first. It is possible that if you stop taking ticagrelor, your chance of having a heart attack or stroke will increase.
It is possible that ticagrelor will make you bleed more readily, which can have serious consequences or even be fatal. Steer clear of any actions that can raise your chances of getting cut or bleeding out.
If you have bleeding that will not stop, either consult your primary care physician or go to the nearest hospital emergency room. There is a possibility that you are bleeding internally, such as in your stomach or intestines. If this occurs, get medical attention immediately. If you have stools that are black or bloody, urine that is red or pink, or if you cough up blood or vomit that looks like coffee grounds, you should contact your doctor as soon as possible. There is a possibility that you are experiencing bleeding in your digestive tract.
If you use ticagrelor together with a number of other medications�including certain over-the-counter medicines and herbal products�possible it's that you might have severe adverse health effects. It is critical that you inform your physician about any and all medications that you have used in the recent past.
Before beginning to use this medication
You should not use ticagrelor if you have an allergy to it, severe liver illness, any current bleeding, stomach ulcers or bleeding, or a history of bleeding in the brain. Furthermore, ticagrelor should be avoided if you are pregnant or breastfeeding (such as from a head injury).
Please refrain from using this medication in the 5 days leading up to your heart bypass operation (coronary artery bypass graft, or CABG).
Tell your doctor if you have any of the following conditions so that he or she can determine whether or not ticagrelor is safe for you to take: liver disease; a serious heart condition such as "sick sinus syndrome" or "AV block" (unless you have a pacemaker); asthma, COPD (chronic obstructive pulmonary disorder) or another breathing problem; a history of stomach ulcers or colon polyps; a history of stroke; or a history of bleeding or blood
It is possible that taking ticagrelor will make you more prone to bleeding, particularly if you have recently undergone surgery or been injured in a bleeding incident; a disease that affects the blood vessels in your brain; a history of stroke; a history of bleeding problems; a history of stomach or intestinal bleeding; or if you are 65 or older.
It is unknown whether or not this medication may cause harm to an unborn child if it is used during pregnancy. Inform your physician if you are pregnant or if you want to become pregnant in the near future.
It is unknown whether ticagrelor is excreted into breast milk or whether it might cause damage to a breastfeeding infant. When you are taking this medication, you should not breastfeed your child.
How exactly am I supposed to take ticagrelor?
Always make sure to follow all of the instructions on the label of your medication. Do not use this medication in greater or lower doses than indicated, nor for a longer period of time than specified.
Aspirin is recommended to be used concurrently with ticagrelor. Take the prescribed amount of aspirin, but be sure to listen to your physician's recommendations.
Take only the amount of aspirin that has been recommended by your healthcare provider. Ticagrelor's efficacy may be diminished if the patient takes an excessive amount of aspirin.
Ticagrelor can be taken either with food or on an empty stomach. Always remember to take your medication at the same time each day.
Since it prevents your blood from coagulating (clotting), ticagrelor can make it easier for you to bleed, even from a very slight injury. This can be a problem if you need surgery. If you have any bleeding that won't stop, either consult your primary care physician or go to the nearest hospital emergency room.
It is imperative that any physician, dentist, surgeon, or other medical professional who treats you be aware that you are currently taking ticagrelor. In order to minimize severe bleeding during surgery or dental work, it is possible that you will be required to discontinue use of the medication for a period of time prior to these procedures. In accordance with your physician's recommendations, you should resume taking ticagrelor as soon as humanly feasible.
Even if you see indications of bleeding, you should not stop taking ticagrelor before consulting with your primary care physician first. Ticagrelor should be used on a consistent basis to achieve the best results. It is important that you have the prescription for your medicine renewed before you run out completely. It is possible that if you stop taking ticagrelor, your chance of having a heart attack or stroke will increase.
Keep at room temperature and away from heat and moisture when storing.
What can I expect if I forget to take a dose?
When you realize you missed a dosage, take it as soon as you can. If it is almost time for your next scheduled dosage, you should skip the dose that you missed. It is not necessary to take additional medication in order to make up for a missed dosage.
While I am taking ticagrelor, what should I try not to do?
Do not take any nonsteroidal anti-inflammatory medicines (NSAIDs) while you are taking ticagrelor unless specifically instructed to do so by your physician. Ibuprofen (Advil and Motrin), naproxen (Aleve), celecoxib (Celebrex), diclofenac, indomethacin, and meloxicam are all examples of nonsteroidal anti-inflammatory drugs (NSAIDs).
Steer clear of any actions that can raise your chances of getting cut or bleeding out. While shaving or cleaning your teeth, take additional precautions to avoid cutting yourself and bleeding.
Avoid consuming alcohol. It may raise the likelihood that you may experience bleeding in either your stomach or intestines.
Before taking any drug for a cold, allergy, discomfort, or sleep issue, make sure to consult with a doctor or pharmacist. Aspirin, also known by its abbreviation ASA, can be included in a variety of different combination medications. Using some drugs at the same time might result in you receiving an excessive amount of aspirin, which can raise your risk of bleeding if taken unchecked. Examine the product's label to see whether or not it includes aspirin or ASA.
Ticagrelor side effects
Seek immediate medical attention if you experience any of the following symptoms of an allergic reaction: hives, difficulty breathing, and swelling of the face, lips, tongue, or neck are all symptoms of anaphylaxis.
Red or pink urine; pale skin, weakness, fever, or jaundice (yellowing of the skin or eyes); signs of stomach bleeding including bloody or tarry stools, coughing up blood; a nosebleed or other bleeding that will not stop; shortness of breath or a lightheaded feeling (like you might pass out), even with mild exertion or while lying down; easy bruising; unusual bleeding (nose, mouth, vagina, or rectum); purple or red pinpoint spots under your skin
Headaches, lightheadedness, coughing, nausea, and diarrhea are some of common adverse reactions that may occur.
This list of potential adverse effects is not exhaustive; additional symptoms may also surface.
To what extent may other medications interact with ticagrelor?
Ticagrelor can interact with a wide variety of medications. This does not include all of the conceivable combinations of factors. Imatinib; lovastatin (Advicor, Altoprev, Mevacor), or simvastatin (Zocor, Simcor, Vytorin, Juvisync); nefazodone; St. John's wort; an antibiotic � clarithromycin, telithromycin; antifungal medicine � itraconazole, ketoconazole, posaconazole, voriconazole; heart or blood pressure
This list is not exhaustive, and it is possible for ticagrelor to interact with a wide variety of other medications. This include both prescription and over-the-counter medications, in addition to herbal and vitamin supplements. Provide any healthcare practitioner who is treating you with a list of all the medications you are currently taking.
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try out a different kind and see if it was a better fit for my needs. Which it was!
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crossed my mind how much cheaper the generic versions were. When I started browsing the
items I couldn’t believe the price difference! This is my go to shop right now.
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always bought it in store. I spoke to one of their support reps and they were really nice
and helped to explain how it works and made me feel much more comfortable with my order!
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and it definitely won’t be my last! They had all the items I needed in one place and the
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