Drug Interaction:
Itraconazole, voriconazole, saquinavir, nelfinavir, indinavir, rifampicin, phenytoin
telithromycin, carbamazepine, phenobarbital, and other CYP3A4 inhibitors
Ergot alkaloids, statins, and other CYP3A4 substrates.
NSAIDs, anticoagulants, fibronolytics, and other agents that alter hemostatis
Verapramil, dilitiazem, cyclosporin, and other strong P-gp substrates
Indication:
BRILINTA (ticagrelor) tablets, for oral use
Initial U.S. Approval: 2011
WARNING:
(A) BLEEDING RISK, and (B) ASPIRIN DOSE AND
BRILINTA EFFECTIVENESS
See full prescribing information for complete boxed warning.
BLEEDING RISK
BRILINTA, like other antiplatelet agents, can cause significant,
sometimes fatal bleeding
Do not use BRILINTA in patients with active pathological
bleeding or a history of intracranial hemorrhage
Do not start BRILINTA in patients undergoing urgent coronary
artery bypass graft surgery (CABG)
If possible, manage bleeding without discontinuing BRILINTA.
Stopping BRILINTA increases the risk of subsequent
cardiovascular events
ASPIRIN DOSE AND BRILINTA EFFECTIVENESS
Maintenance doses of aspirin above 100 mg reduce the effectiveness of BRILINTA
and should be avoided
Drug Name- Brilinta
Active Ingredient - Ticagrelor
To reduce cardiovascular death and heart attack in patients with
acute coronary syndromes(ACS)
Indication-
Reduce cardiovascular death and heart attack in patients with
acute coronary syndrome(ACS)
Approved by FDA on 20-7-2011 (Ref- FDA approved List- 2011)
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Ticagrelor Tablets 03-05-2012
For the Prevention of Thrombiotic events (Cardiovascular Death,
Myocardial Infraction and Stroke) in patients with Acute Coronary
Syndromes(ACS), Unstable Angina, Non ST elevation Myocardial
Infraction(STEM) including Patients Managed medically, and those who are
managed with Percutaneous Coronary Intravention (PCI) or Coronary Artery
By-Pass Grafting (CABG)
Adverse Reaction:
Headache, dyspnoea, epistaxis, nausea, diarrhoea, g-i haemorrhage,
subcutaneous or dermal bleeding, bruising,
Cardiac failure, Chest pain,
Increased serum uric acid, creatinine, atrial fibrillation, bradycardia,
Fatigue fever, odema, back pain, dizziness, cough, confusion,
Rash, anio-edema,
Hyper or hypotension
Contra-Indications:
Active bleeding, history of intracranial haemorrhage,
Moderate to severe hepatic impairment dialysis, uric acid nephropathy
Concurrent admin of ketoconazole, ritonavir, clarithromycin, nefazodone, atazanavir
Lactation, pregnancy.
Ensure contraception in women.
Special Precautions-
Bleeding, diathesis, surgery (discontinue 5 days prior)
Sick sinus syndrome without a pace maker
2nd or 3rd degee AV block, bradycaria-related syncope
Other risk factors of bradycadic events,
History of asthma, COPD
Hyperuricemia, gouty arthiritis.
Moderate to severe renal impairment
Monitor renal function after 1 month and as needed thereafter
Dosages/ Overdosage Etc:
Indication-
Reduce cardiovascular death and heart attack in patients with
acute coronary syndrome(ACS)
Dosage-
A loading dose of 180mg then 90mg twice daily for upto 12 months
INDICATIONS AND USAGE
BRILINTA is a P2Y12 platelet inhibitor indicated to reduce the rate of
cardiovascular death, myocardial infarction, and stroke in patients with acute coronary
syndrome (ACS) or a history of myocardial infarction (MI).
For at least the first 12 months following ACS, it is superior to clopidogrel.
BRILINTA also reduces the rate of stent thrombosis in patients who have been
stented for treatment of ACS.
DOSAGE AND ADMINISTRATION
Initiate treatment with 180 mg oral loading dose following an ACS event.
Continue treatment with 90 mg twice daily during the first year after an ACS
event. After one year, administer 60 mg twice daily.
Use BRILINTA with a daily maintenance dose of aspirin of 75-100 mg.
DOSAGE FORMS AND STRENGTHS
60 mg and 90 mg tablets
Patient Information:
PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Medication Guide)
Advise patients daily doses of aspirin should not exceed 100 mg and to avoid taking
any other medications that contain aspirin.
Advise patients that they:
- Will bleed and bruise more easily
- Will take longer than usual to stop bleeding
- Should report any unanticipated, prolonged or excessive bleeding, or blood in their
stool or urine.
-Advise patients to contact their doctor if they experience unexpected shortness
of breath, especially if severe.
-Advise patients to inform physicians and dentists that they are taking BRILINTA before
any surgery or dental procedure.
Pharmacology/ Pharmacokinetics:
1 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
2. Pharmacokinetics
Ticagrelor demonstrates dose proportional pharmacokinetics, which are similar in patients
and healthy volunteers.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1 Pregnancy
Pregnancy Category C:
There are no adequate and well-controlled studies of BRILINTA use in pregnant women.
In animal studies, ticagrelor caused structural abnormalities at maternal doses
about 5 to 7 times the maximum recommended human dose (MRHD) based
on body surface area. BRILINTA should be used during pregnancy only if the
potential benefit justifies the potential risk to the fetus.
2. Nursing Mothers
It is not known whether ticagrelor or its active metabolites are excreted in human milk.
Ticagrelor is excreted in rat milk. Because many drugs are excreted in human milk,
and because of the potential for serious adverse reactions in nursing infants from
BRILINTA, a decision should be made whether to discontinue nursing or to
discontinue BRILINTA.
3. Pediatric Use
The safety and effectiveness of BRILINTA in pediatric patients have not been established.
4. Geriatric Use
In PLATO and PEGASUS, about half of patients in each study were .65 years of age
and about 15% were .75 years of age. No overall differences in safety or effectiveness
were observed between elderly and younger patients
Manufacturer Details