Dosing & Uses
Dosage Forms & Strengths
tablet
- 60mg
- 90mg
Acute Coronary Syndrome or History of MI
Indicated to reduce risk of cardiovascular death, MI, and stroke in patients with acute coronary syndrome (ACS) or history of MI
Also, reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS
For at least the first 12 months following ACS, it is superior to clopidogrel to lower risk of further major adverse cardiovascular events (MACE) (PLATO study)
Loading dose (following ACS event): 180 mg PO x 1 dose
Maintenance dose (for first year following ACS event): 90 mg PO BID
Maintenance dose (after 1 year of maintenance): 60 mg PO BID
Administer with daily maintenance dose of aspirin 75-100 mg; the use of aspirin above 100 mg decreases effectiveness of ticagrelor
Coronary Artery Disease
Indicated to reduce risk of a first MI or stroke in patients with coronary artery disease (CAD) who are at high risk for such events
While use is not limited to this setting, efficacy was established in patients with type 2 diabetes mellitus (T2DM)
CAD, but no prior stroke or MI: 60 mg PO BID
Administer with daily maintenance dose of aspirin 75-100 mg
For all patients with ACS, use that specific dosing instead
Acute Ischemic Stroke or TIA
Indicated to reduce risk of stroke in patients with acute ischemic stroke (NIH stroke scale score ≤5) or high-risk transient ischemic attack (TIA)
Loading dose: 180 mg PO x 1 dose
Maintenance dose: 90 mg PO BID for up to 30 days
Use with loading dose of aspirin (300-325 mg) and daily maintenance dose of 75-100 mg
Dosage Modifications
Renal impairment
- No dosage adjustment needed
-
End-stage renal disease
- Clinical efficacy and safety studies did not enroll patients with end-stage renal disease (ESRD) on dialysis
- Intermittent hemodialysis: No clinically significant difference in concentrations of ticagrelor and its metabolite and platelet inhibition are expected compared to those observed in patients with normal renal function
Hepatic impairment
- Mild: No dose adjustment required
- Moderate: Data are limited; caution advised
- Severe: Not studied; avoid use due to likely increase systemic exposure to ticagrelor
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (4)
- abrocitinib
abrocitinib and ticagrelor both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- flibanserin
ticagrelor will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of flibanserin with moderate or strong CYP3A4 inhibitors is contraindicated. Severe hypotension or syncope can occur.
- itraconazole
itraconazole increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated during and 2 weeks after itraconazole treatment.
- lomitapide
ticagrelor increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Increases lomitapide levels several folds.
Serious - Use Alternative (34)
- abametapir
abametapir will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.
- apalutamide
apalutamide will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- caplacizumab
caplacizumab, ticagrelor. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug.
- cobicistat
cobicistat will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cobimetinib
ticagrelor will increase the level or effect of cobimetinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concurrent short term (14 days or less) use of moderate CYP3A inhibitors is unavoidable for patients who are taking cobimetinib 60 mg, reduce the cobimetinib dose to 20 mg. After discontinuation of a moderate CYP3A inhibitor, resume cobimetinib 60 mg. Use an alternative to a moderate CYP3A inhibitor in patients who are taking a reduced dose of cobimetinib (40 or 20 mg daily).
- codeine
codeine will decrease the level or effect of ticagrelor by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Co-administration of opioid agonists delay and reduce absorption of ticagrelor and its active metabolite presumably by slowing gastric emptying; consider the use of a parenteral anti-platelet agent in acute coronary syndrome patients requiring co-administration of opioid agonists
- darunavir
darunavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- eliglustat
ticagrelor increases levels of eliglustat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Moderate CYP3A4 inhibitors are not recommended with eliglustat poor or intermediate metabolizers; reduce eliglustat dose from 84 mg BID to 84 mg once daily in extensive metabolizers .
- enzalutamide
enzalutamide will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fentanyl
ticagrelor will increase the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl intranasal
ticagrelor will increase the level or effect of fentanyl intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl transdermal
ticagrelor will increase the level or effect of fentanyl transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl transmucosal
ticagrelor will increase the level or effect of fentanyl transmucosal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fexinidazole
fexinidazole will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- hydromorphone
hydromorphone will decrease the level or effect of ticagrelor by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Co-administration of opioid agonists delay and reduce absorption of ticagrelor and its active metabolite presumably by slowing gastric emptying; consider the use of a parenteral anti-platelet agent in acute coronary syndrome patients requiring co-administration of opioid agonists C
- idelalisib
idelalisib will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- irinotecan liposomal
ticagrelor will increase the level or effect of irinotecan liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ivabradine
ticagrelor will increase the level or effect of ivabradine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of ivabradine with moderate CYP3A4 inhibitors.
- ivosidenib
ivosidenib will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- ketoconazole
ketoconazole increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- levoketoconazole
levoketoconazole increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- lonafarnib
ticagrelor will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of lonafarnib (a sensitive CYP3A substrate) with weak CYP3A inhibitors is unavoidable, reduce to, or continue lonafarnib at starting dose. Closely monitor for arrhythmias and events (eg, syncope, heart palpitations) since lonafarnib effect on QT interval is unknown.
- morphine
morphine will decrease the level or effect of ticagrelor by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Co-administration of opioid agonists delay and reduce absorption of ticagrelor and its active metabolite presumably by slowing gastric emptying; consider the use of a parenteral anti-platelet agent in acute coronary syndrome patients requiring co-administration of opioid agonists
- naloxegol
ticagrelor will increase the level or effect of naloxegol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministation of naloxegol with moderate CYP3A4 inhibitors is unavoidable, reduce naloxegol dose to 12.5 mg qDay
- olaparib
ticagrelor will increase the level or effect of olaparib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with moderate CYP3A inhibitors cannot be avoided, reduce olaparib dose to 200 mg (capsule) or 150 mg (tablet) PO BID. Do not substitute tablets with capsules.
- oxycodone
oxycodone will decrease the level or effect of ticagrelor by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Co-administration of opioid agonists delay and reduce absorption of ticagrelor and its active metabolite presumably by slowing gastric emptying; consider the use of a parenteral anti-platelet agent in acute coronary syndrome patients requiring co-administration of opioid agonists
- oxymorphone
oxymorphone will decrease the level or effect of ticagrelor by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Co-administration of opioid agonists delay and reduce absorption of ticagrelor and its active metabolite presumably by slowing gastric emptying; consider the use of a parenteral anti-platelet agent in acute coronary syndrome patients requiring co-administration of opioid agonists
- ribociclib
ribociclib will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rimegepant
ticagrelor will increase the level or effect of rimegepant by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- sotorasib
sotorasib will decrease the level or effect of ticagrelor by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
- topotecan
ticagrelor will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- tucatinib
tucatinib will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- venetoclax
ticagrelor will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- voxelotor
voxelotor will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (123)
- abciximab
ticagrelor, abciximab. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- acalabrutinib
acalabrutinib increases effects of ticagrelor by anticoagulation. Modify Therapy/Monitor Closely. Coadministration of acalabrutinib with antiplatelets or anticoagulants may further increase risk of hemorrhage. Monitor for signs of bleeding and consider the benefit-risk of withholding acalabrutinib for 3-7 days presurgery and postsurgery depending upon the type of surgery and the risk of bleeding.
- alteplase
ticagrelor, alteplase. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- anagrelide
ticagrelor, anagrelide. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- antithrombin alfa
ticagrelor, antithrombin alfa. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- antithrombin III
ticagrelor, antithrombin III. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- argatroban
ticagrelor, argatroban. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- aspirin
aspirin, ticagrelor. Other (see comment). Use Caution/Monitor. Comment: Maintenance doses of aspirin above 100 mg decreases effectiveness of ticagrelor. Therefore, after the initial loading dose of aspirin (usually 325 mg), use ticagrelor with a maintenance dose of aspirin of 75-100 mg.
- aspirin/citric acid/sodium bicarbonate
aspirin/citric acid/sodium bicarbonate, ticagrelor. Other (see comment). Use Caution/Monitor. Comment: Maintenance doses of aspirin above 100 mg decreases effectiveness of ticagrelor. Therefore, after the initial loading dose of aspirin (usually 325 mg), use ticagrelor with a maintenance dose of aspirin of 75-100 mg.
- atazanavir
atazanavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- atogepant
ticagrelor will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- avapritinib
ticagrelor will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- betrixaban
ticagrelor increases levels of betrixaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Decrease betrixaban dose to 80 mg PO once, then 40 mg PO qDay if coadministered with a P-gp inhibitor.
- bivalirudin
ticagrelor, bivalirudin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- bosentan
bosentan decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- brexpiprazole
ticagrelor will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.
- cabozantinib
ticagrelor will increase the level or effect of cabozantinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- carbamazepine
carbamazepine decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- cenobamate
cenobamate will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- ceritinib
ticagrelor increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- cilostazol
ticagrelor, cilostazol. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- citalopram
citalopram increases effects of ticagrelor by pharmacodynamic synergism. Use Caution/Monitor. Combination may increase risk of bleeding.
- clarithromycin
clarithromycin increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- clopidogrel
ticagrelor, clopidogrel. Either increases effects of the other by Other (see comment). Use Caution/Monitor. Comment: Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- conivaptan
conivaptan increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- crofelemer
crofelemer increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.
- dabigatran
ticagrelor, dabigatran. Either increases effects of the other by anticoagulation. Use Caution/Monitor. According to official packaging labeling, dose adjustment of oral dabigatran not required when coadministered with oral dose of ticagrelor.
ticagrelor will increase the level or effect of dabigatran by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Atrial fibrillation: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <30 mL/min. DVT/PE treatment: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <50 mL/min - dabrafenib
dabrafenib will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- dalteparin
ticagrelor, dalteparin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- defibrotide
defibrotide increases effects of ticagrelor by Other (see comment). Use Caution/Monitor. Comment: Defibrotide may enhance effects of platelet inhibitors.
- desirudin
ticagrelor, desirudin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- dexamethasone
dexamethasone decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- diclofenac
ticagrelor, diclofenac. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- digoxin
ticagrelor increases levels of digoxin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ticagrelor inhibits P-glycoprotein transporter. Monitor digoxin levels with initiation of or any change in ticagrelor therapy.
- dipyridamole
ticagrelor, dipyridamole. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- duvelisib
duvelisib will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.
- edoxaban
edoxaban, ticagrelor. Either increases toxicity of the other by anticoagulation. Modify Therapy/Monitor Closely. Both drugs have the potential to cause bleeding. The need for simultaneous use of platelet aggregation inhibitors with anticoagulants is common for patients with cardiovascular disease, but may result in increased bleeding; monitor closely. Promptly evaluate any signs or symptoms of blood loss.
- efavirenz
efavirenz decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- elagolix
elagolix will increase the level or effect of ticagrelor by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
elagolix decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed. - eliglustat
eliglustat increases levels of ticagrelor by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Monitor therapeutic drug concentrations, as indicated, or consider reducing the dosage of the P-gp substrate and titrate to clinical effect.
- enoxaparin
ticagrelor, enoxaparin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- eptifibatide
ticagrelor, eptifibatide. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- etodolac
ticagrelor, etodolac. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- etravirine
etravirine decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- fedratinib
fedratinib will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fenoprofen
ticagrelor, fenoprofen. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- finerenone
ticagrelor will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.
- fish oil
fish oil, ticagrelor. Other (see comment). Use Caution/Monitor. Comment: Patients taking fish oil and an anticoagulant or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding. .
- fish oil triglycerides
fish oil triglycerides will increase the level or effect of ticagrelor by anticoagulation. Use Caution/Monitor. Prolonged bleeding reported in patients taking antiplatelet agents or anticoagulants and oral omega-3 fatty acids. Periodically monitor bleeding time in patients receiving fish oil triglycerides and concomitant antiplatelet agents or anticoagulants.
- flurbiprofen
ticagrelor, flurbiprofen. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- fondaparinux
ticagrelor, fondaparinux. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- fosamprenavir
fosamprenavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- fosphenytoin
fosphenytoin decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- grapefruit
grapefruit will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- heparin
ticagrelor, heparin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- ibrutinib
ibrutinib will increase the level or effect of ticagrelor by anticoagulation. Use Caution/Monitor. Ibrutinib may increase the risk of hemorrhage in patients receiving antiplatelet or anticoagulant therapies and monitor for signs of bleeding.
- ibuprofen
ticagrelor, ibuprofen. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- ibuprofen IV
ticagrelor, ibuprofen IV. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- icosapent
icosapent, ticagrelor. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Icosapent may prolong bleeding time; monitor periodically if coadministered with other drugs that affect bleeding.
- iloperidone
iloperidone increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.
- imatinib
imatinib increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
imatinib, ticagrelor. Either increases toxicity of the other by Other (see comment). Modify Therapy/Monitor Closely. Comment: Imatinib may cause thrombocytopenia; bleeding risk increased when imatinib is coadministered with anticoagulants, NSAIDs, platelet inhibitors, and thrombolytic agents. - indinavir
indinavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- indomethacin
ticagrelor, indomethacin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- isavuconazonium sulfate
ticagrelor will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
istradefylline will increase the level or effect of ticagrelor by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates. - ketoprofen
ticagrelor, ketoprofen. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- ketorolac
ticagrelor, ketorolac. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- lemborexant
ticagrelor will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.
- lonafarnib
lonafarnib will increase the level or effect of ticagrelor by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.
- lopinavir
lopinavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- lorlatinib
lorlatinib will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lovastatin
ticagrelor increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid lovastatin doses greater than 40 mg.
- meclofenamate
ticagrelor, meclofenamate. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- mefenamic acid
ticagrelor, mefenamic acid. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- mefloquine
ticagrelor will increase the level or effect of mefloquine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- meloxicam
ticagrelor, meloxicam. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- midazolam intranasal
ticagrelor will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.
- mifepristone
mifepristone will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mitotane
mitotane decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.
- nabumetone
ticagrelor, nabumetone. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- nafcillin
nafcillin will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nefazodone
nefazodone increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- nelfinavir
nelfinavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- nevirapine
nevirapine decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- nicardipine
nicardipine increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- nintedanib
ticagrelor increases levels of nintedanib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. If nintedanib adverse effects occur, management may require interruption, dose reduction, or discontinuation of therapy .
- oxaprozin
ticagrelor, oxaprozin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- palbociclib
ticagrelor will increase the level or effect of palbociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- phenobarbital
phenobarbital decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- phenytoin
phenytoin decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- piroxicam
ticagrelor, piroxicam. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- posaconazole
posaconazole increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- prasugrel
ticagrelor, prasugrel. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- primidone
primidone decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- protein C concentrate
ticagrelor, protein C concentrate. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- reteplase
ticagrelor, reteplase. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- rifabutin
rifabutin decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- rifampin
rifampin decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- rifapentine
rifapentine decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- rifaximin
ticagrelor increases levels of rifaximin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ritonavir
ritonavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- rivaroxaban
ticagrelor, rivaroxaban. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- rucaparib
rucaparib will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- saquinavir
saquinavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- selumetinib
ticagrelor and selumetinib both increase anticoagulation. Modify Therapy/Monitor Closely. An increased risk of bleeding may occur in patients taking a vitamin-K antagonist or an antiplatelet agent with selumetinib. Monitor for bleeding and INR or PT in patients coadministered a vitamin-K antagonist or an antiplatelet agent with selumetinib.
- simvastatin
ticagrelor increases levels of simvastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid simvastatin doses greater than 40 mg.
- sonidegib
ticagrelor will increase the level or effect of sonidegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of sonidegib with moderate CYP3A4 inhibitors. If a moderate CYP3A inhibitor must be used, administer the moderate CYP3A inhibitor for <14 days and monitor closely for adverse reactions, particularly musculoskeletal adverse reactions.
- St John's Wort
St John's Wort decreases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid use of ticagrelor with potent CYP3A inducers.
- stiripentol
stiripentol, ticagrelor. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
- sulindac
ticagrelor, sulindac. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- suvorexant
ticagrelor will increase the level or effect of suvorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Decrease suvorexant starting dose to 5 mg HS if coadministered with moderate CYP3A4 inhibitors
- tazemetostat
tazemetostat will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
ticagrelor will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - tecovirimat
tecovirimat will decrease the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- tenecteplase
ticagrelor, tenecteplase. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- ticlopidine
ticagrelor, ticlopidine. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- tinidazole
ticagrelor will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tipranavir
tipranavir increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- tirofiban
ticagrelor, tirofiban. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.
- tofacitinib
ticagrelor increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- tolmetin
ticagrelor, tolmetin. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding with use of ticagrelor and chronic NSAID use. .
- tucatinib
tucatinib will increase the level or effect of ticagrelor by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
- voriconazole
voriconazole increases levels of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Ticagrelor is metabolized by CYP3A4/5. Avoid use with strong CYP3A inhibitors.
- warfarin
ticagrelor, warfarin. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Drugs with antiplatelet properties may increase anticoagulation effect of warfarin.
Minor (0)
Adverse Effects
>10%
Dyspnea (13.8%)
Bleeding (see specific data listed below)
1-10%
Dizziness (4.5%)
Nausea (4.3%)
Diarrhea (3.7%)
Ventricular pauses (6%)
Bleeding
Non-CABG related bleeds (PLATO trial)
- Total bleeds (major + minor) (7.7%)
-
Major bleeds
- Major bleeds (3.9%)
- Fatal/life-threatening (1.9%)
- Fatal (0.2%)
- Intracranial (fatal/life-threatening) (0.3%)
CABG related bleeds (PLATO trial)
- Total major bleeds (81.3%)
- Major bleeds when antiplatelet therapy stopped 5 days before CABG (75%)
- Fatal/life-threatening (43.8%)
- Fatal (0.8%)
Bleeding events (PEGASUS trial)
-
TIMI major
- TIMI major: 8 per 1000 patient years
- Fatal: 1 per 1000 patient years
- Intracranial hemorrhage: 2 per 1000 patient years
-
TIMI major or minor
- 11 per 1000 patient years
Bleeding events (THEMIS trial)
- TIMI major: 9 per 1000 patient years
- TIMI major or minor: 12 per 1000 patient years
- TIMI major or minor or requiring medical attention: 46 per 1000 patient years
- Fatal bleeding: 1 per 1000 patient years
- Intracranial hemorrhage: 3 per 1000 patient years
Postmarketing Reports
Immune system disorders: Hypersensitivity reactions including angioedema
Skin and subcutaneous tissue disorders: Rash
Blood and lymphatic system disorders: Thrombotic thrombocytopenic purpura (rare)
Respiratory disorders: Central sleep apnea, Cheyne-Stokes respiration
Warnings
Black Box Warnings
Bleeding risk
- Like other antiplatelet agents, can cause significant, sometimes fatal, bleeding
- Do not use with active pathological bleeding or a history of intracranial hemorrhage
- Do not start in patients planned to undergo urgent coronary artery bypass graft surgery (CABG); when possible, discontinue at least 5 days prior to any surgery
- Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures after starting ticagrelor
- If possible, manage bleeding without discontinuing; stopping ticagrelor increases risk of subsequent cardiovascular events
Aspirin dose and ticagrelor effectiveness
- Aspirin maintenance dose >100 mg reduces the effectiveness of ticagrelor and should be avoided
- After any initial loading dose, use with aspirin 75-100 mg/day
Contraindications
Hypersensitivity (eg, angioedema)
History of intracranial hemorrhage (ICH)
Active pathologic bleeding (eg, peptic ulcer, ICH)
Cautions
Inhibits platelet function, and thereby, increases bleeding risk; if possible, manage bleeding without discontinuing drug; stopping ticagrelor increases risk of subsequent cardiovascular events
Discontinuation of therapy will increase risk of myocardial infarction, stroke, and death in patients being treated for coronary artery disease; if drug must be temporarily discontinued (eg, to treat bleeding or for significant surgery), restart it as soon as possible; when possible, interrupt therapy for five days prior to surgery that has a major risk of bleeding and resume therapy as soon as hemostasis is achieved
Surgery: When possible, discontinue 5 days prior to surgery
Dyspnea reported; intensity described as usually mild-to-moderate and decreases/resolves during continued treatment; if dyspnea symptoms intolerable consider administering a different antiplatelet agent
Can cause ventricular pauses; bradyarrhythmias, including AV block reported; patients with history of sick sinus syndrome, 2nd or 3rd degree AV block, or bradycardia-related syncope who were not protected by a pacemaker were excluded from PLATO and PEGASUS and may be at increased risk of developing bradyarrhythmias with ticagrelor
Avoid use with severe hepatic impairment, which may increase ticagrelor serum levels
Reported to cause false-negative results in platelet functional tests (eg, HIPA assay for HIT)
Central sleep apnea (CSA) including Cheyne-Stokes respiration (CSR) reported in post-marketing setting, including recurrence or worsening of CSA/CSR following rechallenge; if central sleep apnea suspected, consider further clinical assessment
Drug interaction overview
- Ticagrelor is a CYP3A4 substrate and weak CYP3A4 inhibitor
- May cause false negative results in platelet functional tests (to include, but may not be limited to, the heparin-induced platelet aggregation [HIPA] assay) for patients with heparin-induced thrombocytopenia (HIT)
-
Simvastatin or lovastatin
- Ticagrelor increases serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4
- Avoid simvastatin and lovastatin doses >40 mg
-
Digoxin
- Ticagrelor inhibits the P-glycoprotein transporter
- Monitor digoxin levels with initiation of, or change in ticagrelor dose
-
Opioids
- As with other oral P2Y12 inhibitors, coadministration of opioid agonists delay and reduce the absorption of ticagrelor and its active metabolite presumably because of slowed gastric emptying
- Consider the use of a parenteral antiplatelet agent in ACS patients requiring coadministration of morphine or other opioid agonists
-
Strong CYP3A4 inhibitors
- Avoid coadministration
- Strong CYP3A inhibitors substantially increase ticagrelor exposure and therefore increase the risk of adverse effects (eg, dyspnea, bleeding)
-
Strong CYP3A4 inducers
- Avoid coadministration
- Strong CYP3A inducers substantially reduce ticagrelor exposure and efficacy
-
Aspirin
- Aspirin maintenance doses >100 mg/day reduces ticagrelor efficacy
Pregnancy & Lactation
Pregnancy
Available data from case reports on use in pregnant females have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
Animal data
- Drug given to pregnant rats and pregnant rabbits during organogenesis caused structural abnormalities in the offspring at maternal doses about 5 to 7 times maximum recommended human dose (MRHD) based on body surface area; when given to rats during late gestation and lactation, pup death and effects on pup growth were seen at ~10 times the MRHD
Lactation
There are no data on presence of drug or metabolites in human milk, effect on breastfed infants, or on milk production
Ticagrelor and its metabolites were present in rat milk at higher concentrations than in maternal plasma; when a drug is present in animal milk, it is likely that the drug will be present in human milk
Breastfeeding is not recommended during therapy
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation
Ticagrelor and its active metabolite are approximately equipotent
Patients can be transitioned from clopidogrel to ticagrelor without interruption of antiplatelet effect
Inhibition of platelet aggregation (IPA)
- Transitioning from clopidogrel to ticagrelor resulted in an absolute IPA increase of 26.4%
- Transitioning from ticagrelor to clopidogrel an absolute IPA decrease of 24.5%
Absorption
Bioavailability: 36%
Peak plasma time
Tablets: 1.5 hr (ticagrelor); 2.5 hr (AR-C124910XX [active])
Crushed tables administered via NG tube: 1 hr (ticagrelor); 2 hr (AR-C124910XX [active])
Distribution
Vd (steady-state): 88 L
Protein bound: >99% (ticagrelor and active metabolite)
Metabolism
Metabolized primaryly by CYP3A4 to form major active metabolite (AR-C124910XX); metabolized by CYP3A5 to a lesser extent
Systemic exposure to AR-C124910XX accounts for ~30-40%
Ticagrelor and its major active metabolite are weak P-gp substrates and inhibitors
Elimination
Half-life: 7 hr (ticagrelor); 9 hr (active metabolite)
Excretion
- Ticagrelor: Feces (58%); urine (26%)
- Active metabolite: Primarily by biliary excretion; urine (<1%)
Administration
Oral Administration
Do not administer with another oral P2Y12 platelet inhibitor
May administer with or without food
Missed dose: Skip missed dose and take next dose at its scheduled time; do not take 2 doses at the same time
Unable to swallow tablet whole
- Crush tablets, mix with water, and drink immediately
- Refill glass with water, stir, and drink contents to ensure complete dose is consumed
- May be administered via nasogastric (NG) tube (≥CH8)
- Important to flush NG tube through with water after administration of the mixture
Storage
Store at 25ºC (77ºF); excursions permitted to 15-30ºC (59-86ºF)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Brilinta oral - | 90 mg tablet |  | |
| Brilinta oral - | 60 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
ticagrelor oral
TICAGRELOR - ORAL
(tye-KA-grel-or)
COMMON BRAND NAME(S): Brilinta
WARNING: Ticagrelor may cause serious (sometimes fatal) bleeding. Before taking this medication, tell your doctor your medical history, especially about any bleeding problems. Also, before having any surgery, tell your doctor or dentist about all the products you use, especially ticagrelor. Your doctor or dentist will give you specific directions for when to stop taking this medication before your surgery. See also Precautions section.This medication is usually taken with low-dose aspirin, usually 75-100 milligrams once a day. Unless otherwise directed by your doctor, do not take more than 100 milligrams of aspirin daily. Doing so may make ticagrelor work less well. Ask your doctor or pharmacist for details.
USES: Ticagrelor is used along with low-dose aspirin to help prevent heart attack and stroke in people with a history of heart disease, stroke, or at increased risk for heart disease or stroke (for example, due to diabetes, history of transient ischemic attack-TIA). It may also prevent blood clots after certain heart surgeries (such as stent placement).Ticagrelor works by blocking platelets from sticking together and prevents them from forming harmful clots. It is an antiplatelet drug. It keeps blood flowing smoothly in your body.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking ticagrelor and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually twice daily. The dosage and length of treatment are based on your medical condition and response to treatment. Take a low-dose aspirin (usually 75-100 milligrams) once a day as directed by your doctor. Follow your doctor's directions carefully. See also Warning section.If you have trouble swallowing ticagrelor, you may crush the tablet. Mix the crushed tablet with water in a glass, then drink the mixture right away. Refill the glass with water, stir, and drink to make sure you take all of your dose.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.Do not increase your dose or take this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.Keep taking this medication even if you feel well. Do not stop taking this medication without consulting your doctor. If you stop taking this medication early, you may have a higher risk of getting a heart attack or stroke.
SIDE EFFECTS: Shortness of breath, headache, dizziness, nausea, and nosebleed may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Although unlikely, serious bleeding may occur. Tell your doctor right away if you have any serious side effects, including: easy bruising/bleeding, bleeding that is severe or that you cannot control (such as a severe nosebleed that you cannot stop), bloody/black stools, vomit with blood or that looks like coffee grounds, bloody/red/pink/dark urine.Tell your doctor right away if you have any serious side effects, including: interrupted breathing during sleep.Get medical help right away if you have any very serious side effects, including: fast/slow/irregular heartbeat, fainting, confusion, trouble speaking, vision changes, signs of a blood clotting problem (such as red/purple pinpoint-sized spots on the skin, fever).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking ticagrelor, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: bleeding problems (such as bleeding in the brain, hemophilia, ulcers, frequent nosebleeds), gout, liver disease, recent surgery, serious injury/trauma, heart rhythm problems (heart block or fast/slow/irregular heartbeat).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). This medicine can cause stomach bleeding. Daily use of alcohol while using this medicine may increase your risk for stomach bleeding.To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Your doctor or dentist may tell you to temporarily stop ticagrelor at least 5 days before surgery or a dental procedure. Carefully follow your doctor's or dentist's specific directions for when to stop or restart this medication.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: mifepristone, other drugs that can cause bleeding/bruising (including other antiplatelet drugs such as clopidogrel, NSAIDs such as ibuprofen/naproxen, "blood thinners" such as dabigatran/warfarin).Other medications can affect the removal of ticagrelor from your body, which may affect how ticagrelor works. Examples include dexamethasone, nefazodone, azole antifungals (such as itraconazole, ketoconazole), HIV protease inhibitors (such as atazanavir, ritonavir), macrolide antibiotics (such as clarithromycin), rifamycins (such as rifampin), drugs used to treat seizures (such as carbamazepine, phenytoin), telithromycin, among others.Check all prescription and nonprescription medicine labels carefully since many medications contain pain relievers/fever reducers (aspirin, NSAIDs such as ibuprofen or naproxen). These drugs are similar to ticagrelor and may increase your risk of side effects if taken together. However, if your doctor has directed you to take low-dose aspirin to prevent heart attack or stroke (usually at dosages of 75-100 milligrams a day), you should continue taking the aspirin unless your doctor instructs you otherwise. Ask your doctor or pharmacist for more details.This medication may interfere with certain lab tests (such as platelet functional tests), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe bleeding, nausea, vomiting, diarrhea, irregular heartbeat.
NOTES: Do not share this medication with others.Laboratory and/or medical tests (such as complete blood count) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Different brands of this medication have different storage needs. Check the product package for instructions on how to store your brand, or ask your pharmacist. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised February 2022. Copyright(c) 2022 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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