Drug reference
Ticagrelor is a P2Y12 receptor antagonist that prevents ADP-mediated P2Y12 dependent platelet activation and aggregation. Fibrinolytic drugs act as thrombolytics by activating plasminogen to form plasmin, which degrades fibrin and so breaks up thrombi.
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Prevention of atherothrombotic events in patients with acute coronary syndrome [in combination with aspirin] ▶BY MOUTH ▶Adult: Initially 180 mg for 1 dose, then 90 mg twice daily usually for up to 12 months Prevention of atherothrombotic events in patients with a history of myocardial infarction and a high risk of an atherothrombotic event [in combination with aspirin] ▶BY MOUTH ▶Adult: 60 mg twice daily, extended treatment may be started without interruption after the initial 12-month therapy for acute coronary syndrome. Treatment may also be initiated up to 2 years from the myocardial infarction, or within 1 year after stopping previous ADP receptor inhibitor treatment. There are limited data on the efficacy and safety of extended treatment beyond 3 years
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Active bleeding. history of intracranial haemorrhage Acute pancreatitis. aneurysm. aortic dissection. arteriovenous malformation. bacterial endocarditis. bleeding diatheses. coagulation defects. coma. heavy vaginal bleeding. history of cerebrovascular disease (especially recent events or with any residual disability). neoplasm with risk of haemorrhage. oesophageal varices. pericarditis. recent gastro-intestinal ulceration. recent haemorrhage. recent surgery (including dental extraction). recent trauma. severe hypertension
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Asthma. bradycardia (unless pacemaker fitted) . chronic obstructive pulmonary disease. discontinue 5 days before elective surgery if antiplatelet effect not desirable. history of hyperuricaemia. patients at increased risk of bleeding (e.g. from recent trauma, surgery, gastro- intestinal bleeding, or coagulation disorders). second- or third-degree AV block (unless pacemaker fitted). sick sinus syndrome (unless pacemaker fitted) Conditions in which thrombolysis might give rise to embolic complications such as enlarged left atrium with atrial fibrillation (risk of dissolution of clot and subsequent embolisation). elderly. external chest compression. hypertension. risk of bleeding (including that from venepuncture or invasive procedures)
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NICE decisions ▶Ticagrelor for the treatment of acute coronary syndromes (October 2011) NICE TA236 Ticagrelor, in combination with low-dose aspirin, is recommended for up to 12 months as a treatment option in adults with acute coronary syndromes, that is, people: . with ST-segment elevation myocardial infarction— defined as ST elevation or new left bundle branch block on electrocardiogram—that cardiologists intend to treat with primary percutaneous coronary intervention, or . with non-ST-segment elevation myocardial infarction (NSTEMI), or . admitted to hospital with unstable angina—defined as ST or T wave changes on electrocardiogram suggestive of ischaemia plus one of the characteristics defined below. Before ticagrelor is continued beyond the initial treatment, the diagnosis of unstable angina should first be confirmed, ideally by a cardiologist. Characteristics to be used in defining treatment with ticagrelor for unstable angina are: . age 60 years or older; . previous myocardial infarction or previous coronary artery bypass grafting; . coronary artery disease with stenosis of 50% or more in at least two vessels; . previous ischaemic stroke; . previous transient ischaemic attack, carotid stenosis of at least 50%, or cerebral revascularisation; . diabetes mellitus; . peripheral arterial disease, or . chronic renal dysfunction (creatinine clearance less than 60 mL/minute/1.73 m2). www.nice.org.uk/guidance/ta236 ▶Ticagrelor for preventing atherothrombotic events after myocardial infarction (December 2016) NICE TA420 Ticagrelor, in combination with aspirin, is recommended within its marketing authorisation as an option for preventing atherothrombotic events in adults who had a myocardial infarction and who are at high risk of a further event. Treatment should be stopped when clinically indicated or at a maximum of 3 years. www.nice.org.uk/guidance/ta420
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→Appendix 1: ticagrelor
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▶Common or very common Constipation. diarrhoea. dizziness. dyspepsia. dyspnoea. gout. gouty arthritis. haemorrhage. headache. hyperuricaemia. hypotension. nausea. skin reactions. syncope. vertigo ▶Uncommon Angioedema. confusion. intracranial haemorrhage. tumour haemorrhage ▶Frequency not known Thrombotic thrombocytopenic purpura ▶Common or very common Anaphylactic reaction. angina pectoris. cardiac arrest. cardiogenic shock. chills. CNS haemorrhage. ecchymosis. fever. haemorrhage. haemorrhagic stroke. heart failure. hypotension. Cardiovascular system ischaemia recurrent (when used in myocardial infarction). nausea. pericarditis. pulmonary oedema. vomiting ▶Uncommon Aphasia. mitral valve incompetence. myocardial rupture. pericardial disorders. reperfusion arrhythmia (when used in myocardial infarction). seizure SIDE-EFFECTS, FURTHER INFORMATION Serious bleeding calls for discontinuation of the thrombolytic and may require administration of coagulation factors and antifibrinolytic drugs.
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Manufacturer advises avoid—toxicity in animal studies. Thrombolytic drugs can possibly lead to premature separation of the placenta in the first 18 weeks of pregnancy. There is also a risk of maternal haemorrhage throughout pregnancy and post-partum, and also a theoretical risk of fetal haemorrhage throughout pregnancy.
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Manufacturer advises avoid—present in milk in animal studies.
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Manufacturer advises caution in moderate impairment (limited information available); avoid in severe impairment (no information available). Manufacturers advise avoid in severe impairment. eiiii F 229
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Manufacturer advises monitor renal function 1 month after initiation in patients with acute coronary syndrome.
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There can be variation in the licensing of Cardiovascular system different medicines containing the same drug. Orodispersible tablet ▶Brilique (AstraZeneca UK Ltd) Ticagrelor 90 mg Brilique 90mg orodispersible tablets sugar-free | 56 tablet P £54.60 DT = £54.60 Tablet ▶Brilique (AstraZeneca UK Ltd) Ticagrelor 60 mg Brilique 60mg tablets | 56 tablet P £54.60 DT = £54.60 Ticagrelor 90 mg Brilique 90mg tablets | 56 tablet P £54.60 DT = £54.60 ANTITHROMBOTIC DRUGS › TISSUE PLASMINOGEN ACTIVATORS Fibrinolytic drugs Overview The value of thrombolytic drugs for the treatment of myocardial infarction has been established. Streptokinase p. 230 and alteplase p. 230 have been shown to reduce mortality. Reteplase and tenecteplase p. 231 are also licensed for acute myocardial infarction. Thrombolytic drugs are indicated for any patient with acute myocardial infarction for whom the benefit is likely to outweigh the risk of treatment. Trials have shown that the benefit is greatest in those with ECG changes that include ST segment elevation (especially in those with anterior infarction) and in patients with bundle branch block. Patients should not be denied thrombolytic treatment on account of age alone because mortality in the elderly is high and the reduction in mortality is the same as in younger patients. Alteplase should be given within 6–12 hours of symptom onset, reteplase and streptokinase within 12 hours of symptom onset, but ideally all should be given within 1 hour; use after 12 hours requires specialist advice. Tenecteplase should be given as early as possible and usually within 6 hours of symptom onset. Alteplase, streptokinase and urokinase p. 148 can be used for other thromboembolic disorders such as deep-vein thrombosis and pulmonary embolism. Alteplase is also used for acute ischaemic stroke. Urokinase is also licensed to restore the patency of occluded intravenous catheters and cannulas blocked with fibrin clots. Fibrinolytics f
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Initially 180 mg for 1 dose, then 90 mg twice
First-line fragment. Read the complete Indications and Dose section above.
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60 mg twice daily, extended treatment may be
First-line fragment. Read the complete Indications and Dose section above.
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