Approved on.
Date of revision:
Tegretol Tablets Instructions
Please read the instructions carefully and use under the guidance of your physician
Warning: risk of bleeding
As with other antiplatelet drugs, Tegretol can cause significant and sometimes fatal bleeding.
Do not use Tegretol in patients with active pathologic bleeding or a history of intracranial hemorrhage Tegretol in patients with active pathologic bleeding or a history of intracranial hemorrhage.
Do not use tegretol in patients scheduled for emergency coronary artery bypass grafting ( CABG) in patients scheduled to receive tegretol. If possible, discontinue tegretol at least 7 days prior to any procedure.
If possible, treat bleeding without stopping tegretol. Perform treatment. Discontinuing tegretol increases the risk of subsequent cardiovascular events.
Warning: Aspirin Dose and Efficacy of Tegretol
Aspirin maintenance doses greater than 100 mg reduce the clinical efficacy of tegretol in reducing composite endpoint events and therefore a maintenance dose of aspirin of 75 to 100 mg/day after any initial dose is given.
[Drug Name]
Generic Name: Tegretol Tablets
English name: Ticagrelor Tablets
Hanyu Pinyin: Tigeruiluo Pian
[Ingredients
The active ingredient is Tegretol, whose chemical name is: (1S, 2S, 3R, 5S)-3-[7-{[(1R, 2S)-2-(3, 4-difluorophenyl)cyclopropyl]amino} -5-propylthio-3H[1,2,3]triazolo[4,5d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
Chemical structure formula.
Molecular formula: C23H28F2N6O 4S
Molecular weight: 522.57
[Properties]This product is a yellow film-coated tablet. After removing the coating, it appears white or off-white.
Tegretol in combination with aspirin in patients with acute coronary syndrome (ACS) or a history of myocardial infarction with at least one risk factor for atherosclerotic thrombotic events (see clinical trials PEGASUS Study) in patients with reduced incidence of cardiovascular death, myocardial infarction, and stroke.
Tigretol was more effective than clopidogrel for at least the first 12 months after the onset of ACS.
Tegretol was studied in combination with aspirin in patients with ACS. The results found that maintenance doses of aspirin greater than 100 mg reduced the clinical efficacy of tegretol in reducing composite endpoint events, and therefore, maintenance doses of aspirin should not exceed 100 mg daily.
[Specification]90 mg
[Dosage].
Orally. It can be taken before or after meals.
Unless clearly contraindicated, should be co-administered with aspirin. After the first dose of loading aspirin, the maintenance dose of aspirin is 75 to 100 mg once daily.
Patients with acute coronary syndrome.
Tegretol tablets are initiated at a single loading dose of 180 mg (90 mg x 2 tablets), followed by maintenance dosing of 1 tablet (90 mg) twice daily, with recommended maintenance therapy for 12 months. Unless there is a clinical indication to discontinue treatment with Tegretol tablets (see [Clinical Trials]).
Patients with a history of myocardial infarction.
Patients with a history of myocardial infarction of at least 1 year with at least one risk factor for atherosclerotic thrombotic events (see clinical trial PEGASUS Study) In patients with a history of myocardial infarction of at least 1 year and with at least one risk factor for atherosclerotic thrombotic events (see clinical trial PEGASUS Study), the recommended dose is 60 mg twice daily when the patient requires long-term therapy. In patients with ACS who are at high risk for atherosclerotic thrombotic events, continuous treatment with tegretol 60 mg twice daily may be initiated immediately after 1 year of treatment with tegretol 90 mg or other adenosine diphosphate (ADP) receptor inhibitors. Tegretol tablet therapy may also be initiated 2 years after myocardial infarction or within 1 year after discontinuation of a previously administered ADP receptor inhibitor. Data on the efficacy and safety of taking tegretol tablets for more than 3 years are limited.
Treatment should avoid missed doses as much as possible. If a patient misses a dose, one tablet should be taken at the scheduled next dose time (the patient’s next dose).
If replacing another antiplatelet agent with Tegretol, the first dose of Tegretol tablets should be given 24 hours after the last dose of the other antiplatelet agent.
For patients who are unable to swallow the tablets whole, the Tegretol tablets can be crushed into a fine powder and mixed with half a glass of water and taken immediately. Afterwards, wash the glass with another half glass of water and drink all the contents of the glass. This mixture can also be administered through a nasogastric tube (CH8 or larger size), but the tube must be flushed with water after administration.
Special Populations
Patients with children.
The safety and efficacy of Tegretol in children under 18 years of age have not been established and no study data are available.
Older patients:
No dose adjustment required.
Renal impairment.
Patients with renal impairment do not require dose adjustment (see [Pharmacokinetics]). No information is available on the use of Tegretol tablets in patients on renal dialysis, and Tegretol is not recommended for these patients.
Hepatic impairment.
Tegretol has not been studied in patients with severe hepatic impairment; therefore, tegretol tablets are contraindicated in patients with severe hepatic impairment. Data in patients with moderate hepatic impairment are limited and no dose adjustment is recommended, but tegretol should be administered with caution. No dose adjustment is required in patients with mild hepatic impairment.
[Adverse Reactions
The safety of tegretol was evaluated in two large phase 3 studies (PLATO and PEGASUS), which enrolled more than 39,000 patients. ,000+ patients.
The incidence of discontinuation due to adverse events was higher in patients treated with tegretol than with clopidogrel in the PLATO study (7.4% and 5.4%).In the PEGASUS study, compared with patients treated with aspirin monotherapy, patients receiving Patients treated with tegretol in combination with aspirin had a higher incidence of discontinuation due to adverse events (16.1% in the tegretol 60 mg in combination with aspirin group and 8.5% in the aspirin monotherapy group). The most commonly reported adverse reactions in patients treated with tegretol were bleeding and dyspnea (see [Caution]).
List of Adverse Reactions Summary
The following adverse reactions have been reported in clinical studies and post-marketing experience (Table 1).
Adverse reactions are listed according to the Medical Dictionary for Drug Administration (MedDRA) Systematic Organ Classification (SOC). Within each SOC, adverse drug reactions were ranked by frequency of occurrence, with frequency groupings defined as follows: very common (≥1/10), common (≥1/100, <1/10), occasional (≥1/1,000, <1/100), rare (≥1/10,000, <1/1000), very rare (<1/10,000), and unknown (cannot be estimated from available data).
Table 1. Adverse reactions categorized by frequency of occurrence and system organ classification (SOC)
System organ classificationVery commonCommonUnusualBenign, malignant, and tumors of unknown nature (including cysts and polyps) Tumor Bleedinga. /sup>Diseases of the blood and lymphatic systemBlood Disorders Bleedingb Immune System Disorders Allergies, including angioedemacMetabolic and nutritional disordersHigh uric acid bloodd Gout/Gouty Arthritis Psychiatric category Confusion of consciousnessAll types of neurological disorders dizziness, fainting, headache Intracranial hemorrhageOcular organ disease Eye BleedeEar and disorientation disorders GlareEar bleedingVascular disease Low blood pressure Respiratory, thoracic and mediastinal disordersHard to breatheRespiratory bleedingf Gastrointestinal Disorders Gastrointestinal bleedingg, diarrhea, nausea, indigestion, constipationRetroperitoneal hemorrhage Dermal and subcutaneous tissue disorders Subcutaneous or cutaneous bleeding h, rash, itching