Platelet Aggregation Inhibitor Ticagrelor(274693-27-5) for sale
Ticagrelor(274693-27-5) is a platelet aggregation inhibitor, It keeps the platelets in your blood from coagulating (clotting) to prevent unwanted blood clots. Visit: http://www.aasraw.com/products/ticagrelor-powder/
Ticagrelor(274693-27-5) is a platelet aggregation inhibitor, It keeps the platelets in your blood from coagulating (clotting) to prevent unwanted blood clots. Visit: http://www.aasraw.com/products/ticagrelor-powder/
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<strong>Platelet</strong> <strong>Aggregation</strong> <strong>Inhibitor</strong> <strong>Ticagrelor</strong>(<strong><strong>27</strong>4693</strong>-<strong>27</strong>-5)<br />
For Sale<br />
<strong>Platelet</strong> <strong>Aggregation</strong> <strong>Inhibitor</strong> <strong>Ticagrelor</strong>(<strong><strong>27</strong>4693</strong>-<strong>27</strong>-5) For Sale.......................................................1<br />
1. <strong>Ticagrelor</strong>(<strong><strong>27</strong>4693</strong>-<strong>27</strong>-5)..................................................................................................................1<br />
2. <strong>Ticagrelor</strong> Brand Name: Brilinta................................................................................................2<br />
3. <strong>Ticagrelor</strong>: Mechanism Of Action....................................................................................................3<br />
4. How does ticagrelor(Brilinta) work?............................................................................................... 5<br />
5. <strong>Ticagrelor</strong>--Clinical Trials..................................................................................................................5<br />
(1) Clinical efficacy of <strong>Ticagrelor</strong>................................................................................................. 5<br />
(2) Conclusion..............................................................................................................................6<br />
6. What is the drug ticagrelor used <strong>for</strong>?............................................................................................. 9<br />
7. How to take <strong>Ticagrelor</strong>(Brilinta) reasonably?................................................................................. 9<br />
(1) <strong>Ticagrelor</strong>(Brilinta) dosing in<strong>for</strong>mation................................................................................. 9<br />
(2) How is this <strong>Ticagrelor</strong> best taken?.......................................................................................11<br />
(3) How should I take ticagrelor (Brilinta)?...............................................................................13<br />
(4) What should I avoid while taking ticagrelor(Brilinta)?........................................................14<br />
8. <strong>Ticagrelor</strong> Side Effects................................................................................................................... 14<br />
9. What other drugs will affect ticagrelor?....................................................................................... 16<br />
10. What should I know about storage and disposal of this medication?....................................... 17<br />
11. What is the most important in<strong>for</strong>mation I should know about ticagrelor (Brilinta)?................18<br />
12. Where can I get more in<strong>for</strong>mation?............................................................................................20<br />
1. <strong>Ticagrelor</strong>(<strong><strong>27</strong>4693</strong>-<strong>27</strong>-5)<br />
<strong>Ticagrelor</strong> (trade name Brilinta in the US, Brilique and Possia in the EU) is a<br />
platelet aggregation inhibitor produced by AstraZeneca. Unlike clopidogrel,<br />
ticagrelor is not a prodrug and does not require metabolic<br />
activation. <strong>Ticagrelor</strong> is used along with aspirin to prevent serious or<br />
life-threatening problems with the heart and blood vessels in people who<br />
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have had a heart attack or severe chest pain. It is also used to prevent blood<br />
clots from <strong>for</strong>ming in people with coronary stents (metal tubes surgically<br />
placed in clogged blood vessels to improve blood flow) who have had a heart<br />
attack or severe chest pain. <strong>Ticagrelor</strong> is in a class of medications called<br />
antiplatelet medications. It works by preventing platelets (a type of blood cell)<br />
from collecting and <strong>for</strong>ming clots that may cause a heart attack or stroke.<br />
2. <strong>Ticagrelor</strong> Brand Name: Brilinta<br />
<strong>Ticagrelor</strong> is a crystalline powder with an aqueous solubility of approximately<br />
10 mcg/mL at room temperature.<br />
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Brilinta tablets <strong>for</strong> oral administration contain 90 mg of ticagrelor and the<br />
following ingredients: mannitol, dibasic calcium phosphate, sodium starch<br />
glycolate, hydroxypropyl cellulose, magnesium stearate, hydroxypropyl<br />
methylcellulose, titanium dioxide, talc, polyethylene glycol 400, and ferric<br />
oxide yellow.<br />
3. <strong>Ticagrelor</strong>: Mechanism Of Action<br />
<strong>Ticagrelor</strong>(Brilinta), a member of the new chemical class<br />
cyclopentyltriazolopyrimidines (CPTP), which is a oral, direct acting, selective<br />
and reversibly binding P2Y12 receptor antagonist that prevents adenosine<br />
diphosphate (ADP)-mediated P2Y12 platelet activation and aggregation.<br />
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<strong>Ticagrelor</strong> does not prevent ADP binding, but when bound to the P2Y12<br />
receptor prevents ADP-induced signal transduction.<br />
Since platelets participate in the initiation and/or evolution of thrombotic<br />
complications of atherosclerotic disease, inhibition of platelet function has<br />
been shown to reduce the risk of cardiovascular events such as death,<br />
myocardial infarction or stroke.<br />
<strong>Ticagrelor</strong> has an additional mechanism of action, increasing local<br />
endogenous adenosine levels by inhibiting equilibrative nucleoside<br />
transporter-1 (ENT-1). Adenosine is <strong>for</strong>med locally at sites of hypoxia and<br />
tissue damage through degradation of released adenosine tri- and<br />
di-phosphate (ATP and ADP). As adenosine degradation is essentially<br />
restricted to the intracellular space, inhibition of ENT-1 by ticagrelor prolongs<br />
the half-life of adenosine and thereby increases its local extracellular<br />
concentration providing enhanced local adenosine responses. <strong>Ticagrelor</strong> has<br />
no clinically significant direct effect on adenosine receptors (A1, A2A, A2B, A3)<br />
and is not metabolised to adenosine. Adenosine has been documented to<br />
have a number of effects that include: vasodilation, cardioprotection, platelet<br />
inhibition, modulation of inflammation and induction of dyspnoea, which<br />
may contribute to the clinical profile of ticagrelor.<br />
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4. How does ticagrelor(Brilinta) work?<br />
<strong>Ticagrelor</strong>(Brilinta)reversibly inhibits the platelet adenosine diphosphate (ADP)<br />
P2Y12 receptors which results in rapid inhibition of platelet activation and<br />
aggregation. Clopidogrel also acts on these receptors, however, because it is<br />
a “prodrug”, the trans<strong>for</strong>mation to the active metabolite tends to result in<br />
slower and less consistent inhibition of platelets than with<br />
ticagrelor(Brilinta).3, 5 The trans<strong>for</strong>mation of clopidogrel to its active<br />
metabolite requires the enzyme CYP2C19. Approximately 30–40% of people<br />
of M ā ori, Pacific and Asian ethnicity have reduced function CYP2C19<br />
polymorphisms, compared to 15% of Europeans. Although it is not yet<br />
proven, ticagrelor(Brilinta) may be of particular benefit, compared with<br />
clopidogrel, <strong>for</strong> people in these ethnic groups (Māori, Pacific and Asian).<br />
5. <strong>Ticagrelor</strong>--Clinical Trials<br />
(1) Clinical efficacy of <strong>Ticagrelor</strong><br />
The efficacy and safety of ticagrelor have been evaluated by <strong>Platelet</strong><br />
inhibition and Patient Outcomes (PLATO) phase-III trial. The PLATO trial was<br />
per<strong>for</strong>med in patients with either non-ST elevation or ST-elevation ACS. A<br />
total of 18,624 patients were randomly assigned to receive either ticagrelor<br />
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(180 mg loading dose, 90 mg twice daily thereafter) or clopidrogel (300-600<br />
mg loading dose, 75 mg thereafter) along with aspirin (75-100 mg per day)<br />
<strong>for</strong> 12 months. The primary efficacy outcome was the death from<br />
cardiovascular causes.<br />
Myocardial infarction or stroke was significantly<br />
reduced among patients who received ticagrelor compared with those who<br />
took clopidrogel (9.8% versus 11.7%; hazard ratio (HR) 0.84, P < 0.001).<br />
However, one group of patients enrolled in United States fared worse with<br />
ticagrelor as compared of clopidrogel (hazard ratio 1.<strong>27</strong> as compared to<br />
hazard ratio <strong>for</strong> non US patients: 0.81). PLATO data showed that aspirin<br />
dosage was ≥300 mg in this subgroup of patients and that might be reason<br />
<strong>for</strong> this type of response.<br />
(2) Conclusion<br />
In view of the overall health impact of ACS, as well as its significant economic<br />
burden, P&T decision makers need to identify optimal treatment approaches<br />
to this debilitating and potentially fatal disorder.<br />
<strong>Ticagrelor</strong>(Brilinta) is the first cyclopentyltriazolopyridine in a new class of<br />
antiplatelets. <strong>Ticagrelor</strong> interacts with the P2Y12 ADP receptor, which is<br />
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approved <strong>for</strong> the reduction of thrombotic cardiovascular events in patients<br />
with ACS. <strong>Ticagrelor</strong> is not a prodrug and does not require metabolic<br />
activation to inhibit the P2Y12 receptor; however, hepatic metabolism is<br />
needed to produce its active metabolite.<br />
In the pivotal phase-3 PLATO trial, <strong>Ticagrelor</strong>(Brilinta) significantly reduced<br />
the rate of first occurrence of the study ’ s composite end point of<br />
cardiovascular death, nonfatal MI (excluding silent MI), or stroke versus<br />
clopidogrel. <strong>Ticagrelor</strong> also reduced the secondary end points of<br />
cardiovascular death and MI individually, with no difference in stroke versus<br />
clopidogrel.<br />
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<strong>Ticagrelor</strong>(Brilinta) has been studied in ACS in combination with aspirin.<br />
Maintenance doses of aspirin above 100 mg decreased the effectiveness of<br />
<strong>Ticagrelor</strong>. Maintenance doses of aspirin above 100 mg should be avoided.<br />
Like other antiplatelet agents, <strong>Ticagrelor</strong> can cause significant, sometimes<br />
fatal, bleeding. <strong>Ticagrelor</strong> should not be used in patients with active<br />
pathological bleeding or a history of intracranial hemorrhage. <strong>Ticagrelor</strong><br />
should not be started in patients planned to undergo urgent CABG surgery.<br />
When possible, discontinue <strong>Ticagrelor</strong> at least 5 days prior to any surgery.<br />
Suspect bleeding in any patient who is hypotensive and has recently<br />
undergone coronary angiography, PCI, CABG, or other surgical procedures in<br />
the setting of <strong>Ticagrelor</strong>. If possible, manage bleeding without discontinuing<br />
<strong>Ticagrelor</strong>. Stopping <strong>Ticagrelor</strong> increases the risk of subsequent<br />
cardiovascular events.<br />
<strong>Ticagrelor</strong>(Brilinta) is contraindicated in patients with a history of intracraial<br />
hemorrhage and active pathological bleeding, such as peptic ulcer. <strong>Ticagrelor</strong><br />
is also contraindicated in patients with severe hepatic impairment because of<br />
a probable increase in exposure. <strong>Ticagrelor</strong> has not been studied in these<br />
patients. Severe hepatic impairment increases the risk of bleeding because of<br />
reduced synthesis of coagulation proteins.<br />
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The clinical use of <strong>Ticagrelor</strong> is supported by a Risk Evaluation and Mitigation<br />
Strategy (REMS) initiative, which is designed to in<strong>for</strong>m health care<br />
professionals and patients about the risks associated with <strong>Ticagrelor</strong>,<br />
particularly the risk of bleeding, and about the need to ensure that the<br />
maintenance dose of aspirin, co-administered with <strong>Ticagrelor</strong>, does not<br />
exceed 100 mg.<br />
6. What is the drug ticagrelor used <strong>for</strong>?<br />
♦ <strong>Ticagrelor</strong> use: It is used to lower the chance of heart attack, stroke, and<br />
death in some people.<br />
♦ <strong>Ticagrelor</strong> use: It is used to lower the chance of blockage of a stent after a<br />
stent is placed in the heart.<br />
♦ <strong>Ticagrelor</strong> use: It may be given to you <strong>for</strong> other reasons. Talk with the<br />
doctor.<br />
7. How to take <strong>Ticagrelor</strong>(Brilinta) reasonably?<br />
(1) <strong>Ticagrelor</strong>(Brilinta) dosing in<strong>for</strong>mation<br />
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Usual Adult Dose <strong>for</strong> Acute Coronary Syndrome:<br />
Following an acute coronary syndrome (ACS) event:<br />
Loading dose: 180 mg orally once<br />
Maintenance dose: 90 mg orally twice a day <strong>for</strong> 1 year<br />
Maintenance dose after 1 year: 60 mg orally twice a day<br />
Comments:<br />
-This drug should be taken in conjunction with a daily maintenance dose of<br />
aspirin 75 to 100 mg orally once a day.<br />
-For at least the first 12 months following ACS, this drug is superior to<br />
clopidogrel.<br />
Uses:<br />
-To reduce the rate of cardiovascular death, myocardial infarction, and stroke<br />
in patients with acute coronary syndrome (ACS) or a history of myocardial<br />
infarction.<br />
-To reduce the rate of stent thrombosis in patients who have been stented<br />
<strong>for</strong> treatment of ACS.<br />
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Usual Adult Dose <strong>for</strong> Prevention of Atherothrombotic Events:<br />
Following an acute coronary syndrome (ACS) event:<br />
Loading dose: 180 mg orally once<br />
Maintenance dose: 90 mg orally twice a day <strong>for</strong> 1 year<br />
Maintenance dose after 1 year: 60 mg orally twice a day<br />
Comments:<br />
-This drug should be taken in conjunction with a daily maintenance dose of<br />
aspirin 75 to 100 mg orally once a day.<br />
-For at least the first 12 months following ACS, this drug is superior to<br />
clopidogrel.<br />
Uses:<br />
-To reduce the rate of cardiovascular death, myocardial infarction, and stroke<br />
in patients with acute coronary syndrome (ACS) or a history of myocardial<br />
infarction.<br />
-To reduce the rate of stent thrombosis in patients who have been stented<br />
<strong>for</strong> treatment of ACS.<br />
(2) How is this <strong>Ticagrelor</strong> best taken?<br />
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Use ticagrelor as ordered by your doctor. Read all in<strong>for</strong>mation given to you.<br />
Follow all instructions closely.<br />
♦ Take ticagrelor at the same time of day.<br />
♦ Take with or without food.<br />
♦ If you cannot swallow the tablet whole, the tablet can be crushed and<br />
mixed with water.<br />
♦ Drink right away after mixing. Refill the glass with water, stir, and drink.<br />
♦Those who have feeding tubes may use the tablet. Crush the tablet and mix<br />
it with water.<br />
♦ Flush the feeding tube after ticagrelor is given.<br />
♦ To gain the most benefit, do not miss doses.<br />
♦ Keep taking ticagrelor as you have been told by your doctor or other health<br />
care provider, even if you feel well.<br />
What do I do if I miss a ticagrelor dose?<br />
♦ Skip the missed ticagrelor dose and go back to your normal time.<br />
♦ Do not take 2 ticagrelor doses at the same time or extra doses.<br />
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(3) How should I take ticagrelor (Brilinta)?<br />
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Take exactly as prescribed by your doctor. Do not take in larger or smaller<br />
amounts or <strong>for</strong> longer than recommended. Follow the directions on your<br />
prescription label.<br />
<strong>Ticagrelor</strong> should be taken together with aspirin. Follow your doctor's<br />
instructions about how much aspirin you should take. <strong>Ticagrelor</strong> can be taken<br />
with or without food. Take the medicine at the same time each day.<br />
Because ticagrelor keeps your blood from coagulating (clotting) to prevent<br />
unwanted blood clots, this medicine can also make it easier <strong>for</strong> you to bleed,<br />
even from a minor injury. Contact your doctor or seek emergency medical<br />
attention if you have any bleeding that will not stop.<br />
If you need surgery or dental work, tell the surgeon or dentist ahead of time<br />
that you are using ticagrelor. You may need to stop using the medicine <strong>for</strong> at<br />
least 5 days be<strong>for</strong>e having surgery, to prevent excessive bleeding. Follow your<br />
doctor's instructions and start taking ticagrelor again as soon as possible.<br />
Do not stop taking ticagrelor without first talking to your doctor, even if you<br />
have signs of bleeding. Use ticagrelor regularly to get the most benefit. Get<br />
your prescription refilled be<strong>for</strong>e you run out of medicine completely.<br />
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Stopping ticagrelor may increase your risk of a heart attack or stroke. Store at<br />
room temperature away from moisture and heat.<br />
(4) What should I avoid while taking ticagrelor(Brilinta)?<br />
Drinking alcohol while taking aspirin can increase your risk of stomach<br />
bleeding.<br />
Avoid activities that may increase your risk of bleeding or injury. Use extra<br />
care to prevent bleeding while shaving or brushing your teeth.<br />
While taking ticagrelor with aspirin, avoid using medicines <strong>for</strong> pain, fever,<br />
swelling, or cold/flu symptoms. They may contain ingredients similar to<br />
aspirin (such as salicylates, ibuprofen, ketoprofen, or naproxen). Taking<br />
certain products together can cause you to get too much aspirin which can<br />
increase your risk of bleeding.<br />
8. <strong>Ticagrelor</strong> Side Effects<br />
WARNING/CAUTION: Even though it may be rare, some people may have<br />
very bad and sometimes deadly ticagrelor side effects when taking ticagrelor.<br />
Tell your doctor or get medical help right away if you have any of the<br />
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following signs or symptoms that may be related to a very bad ticagrelor side<br />
effect:<br />
♦ Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered,<br />
or peeling skin with or without fever; wheezing; tightness in the chest or<br />
throat; trouble breathing, swallowing, or talking; unusual hoarseness; or<br />
swelling of the mouth, face, lips, tongue, or throat.<br />
♦ Signs of bleeding like throwing up blood or throw up that looks like coffee<br />
grounds; coughing up blood; blood in the urine; black, red, or tarry stools;<br />
bleeding from the gums; vaginal bleeding that is not normal; bruises without<br />
a reason or that get bigger; or any bleeding that is very bad or that you<br />
cannot stop.<br />
♦ Weakness on 1 side of the body, trouble speaking or thinking, change in<br />
balance, drooping on one side of the face, or blurred eyesight.<br />
♦ Very bad headache.<br />
♦ Shortness of breath.<br />
♦ Slow heartbeat.<br />
♦ A heartbeat that does not feel normal.<br />
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9. What other drugs will affect ticagrelor?<br />
Sometimes it is not safe to use certain medications at the same time. Some<br />
drugs can affect your blood levels of other drugs you take, which may<br />
increase side effects or make the medications less effective.<br />
Tell your doctor about all your current medicines. Many drugs can interact<br />
with ticagrelor, especially:<br />
♦ antifungal medicine;<br />
♦ antiviral medicine to treat HIV or AIDS;<br />
♦ a blood thinner;<br />
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♦ cholesterol medication;<br />
♦ heart or blood pressure medication;<br />
♦ opioid medication;<br />
♦ seizure medicine; or<br />
♦ tuberculosis medicine.<br />
10. What should I know about storage and disposal of this medication?<br />
Keep this medication in the container it came in, tightly closed, and out of<br />
reach of children. Store it at room temperature and away from excess heat<br />
and moisture (not in the bathroom).<br />
Unneeded medications should be disposed of in special ways to ensure that<br />
pets, children, and other people cannot consume them. However, you should<br />
not flush this medication down the toilet. Instead, the best way to dispose of<br />
your medication is through a medicine take-back program. Talk to your<br />
pharmacist or contact your local garbage/recycling department to learn<br />
about take-back programs in your community. See the FDA's Safe Disposal of<br />
Medicines website <strong>for</strong> more in<strong>for</strong>mation if you do not have access to a<br />
take-back program.<br />
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It is important to keep all medication out of sight and reach of children as<br />
many containers (such as weekly pill minders and those <strong>for</strong> eye drops, creams,<br />
patches, and inhalers) are not child-resistant and young children can open<br />
them easily. To protect young children from poisoning, always lock safety<br />
caps and immediately place the medication in a safe location – one that is<br />
up and away and out of their sight and reach.<br />
11. What is the most important in<strong>for</strong>mation I should know about<br />
ticagrelor (Brilinta)?<br />
<strong>Ticagrelor</strong> keeps your blood from coagulating (clotting) to prevent unwanted<br />
blood clots that can occur with certain heart or blood vessel conditions.<br />
Because of this drug action, ticagrelor can make it easier <strong>for</strong> you to bleed,<br />
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even from a minor injury. Contact your doctor or seek emergency medical<br />
attention if you have bleeding that will not stop.<br />
You may also have bleeding on the inside of your body, such as in your<br />
stomach or intestines. Call your doctor at once if you have black or bloody<br />
stools, or if you cough up blood or vomit that looks like coffee grounds.<br />
These could be signs of bleeding in your digestive tract.<br />
While you are taking ticagrelor, do not take aspirin or other NSAIDs<br />
(non-steroidal anti-inflammatory drugs) without your doctor's advice. NSAIDs<br />
include ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn, Naprelan,<br />
Treximet), celecoxib (Celebrex), diclofenac (Cataflam, Voltaren), indomethacin<br />
(Indocin), meloxicam (Mobic), and others.<br />
<strong>Ticagrelor</strong> may cause you to bleed more easily, especially if you have: a<br />
history of bleeding problems, surgery or a medical emergency, a disease<br />
affecting the blood vessels in your brain, a history of stomach or intestinal<br />
bleeding, or if you are 65 or older.<br />
Many drugs (including some over-the-counter medicines and herbal<br />
products) can interact with ticagrelor. It is very important to tell your doctor<br />
about all medicines you have recently used. Ask your doctor be<strong>for</strong>e taking<br />
any medicine <strong>for</strong> pain, arthritis, fever, or swelling. These medicines may affect<br />
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blood clotting and may also increase your risk of stomach bleeding. Any<br />
doctor, dentist, surgeon, or other medical care provider who treats you<br />
should know that you are taking ticagrelor.<br />
12. Where can I get more in<strong>for</strong>mation?<br />
Remember, keep this and all other medicines out of the reach of children,<br />
never share your medicines with others, and use this medication only <strong>for</strong> the<br />
indication prescribed.<br />
Every ef<strong>for</strong>t has been made to ensure that the in<strong>for</strong>mation provided<br />
by AASraw up-to-date, and complete, but no guarantee is made to that<br />
effect. Drug in<strong>for</strong>mation contained herein may be time sensitive.<br />
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and consumers in the United States and there<strong>for</strong>e AASraw does not warrant<br />
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accessed by clicking on this link. Join <strong>Platelet</strong> <strong>Aggregation</strong><br />
<strong>Inhibitor</strong> <strong>Ticagrelor</strong>(<strong><strong>27</strong>4693</strong>-<strong>27</strong>-5) <strong>for</strong> <strong>sale</strong>--AASraw.<br />
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