Formulary
Ticagrelor: Indications, Dosing, Side Effects and Interactions
Ticagrelor is a P2Y 12 receptor antagonist that prevents ADP-mediated P2Y 12 dependent platelet activation and aggregation.
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Ticagrelor: Indications, Dosing, Side Effects and Interactions
Ticagrelor is a P2Y 12 receptor antagonist that prevents ADP-mediated P2Y 12 dependent platelet activation and aggregation.
Drug action
Ticagrelor is a P2Y 12 receptor antagonist that prevents ADP-mediated P2Y 12 dependent platelet activation and aggregation.
Indications and dose
**Prevention of atherothrombotic events in patients with acute coronary syndrome [in combination with aspirin]**
- **Adult** (By Mouth): 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]**
- **Adult** (By Mouth): 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.
**Transient ischaemic attack [in patients with a low risk of bleeding],Minor ischaemic stroke [in patients with a low risk of bleeding]**
- **Adult** (By Mouth): Initially 180 mg for 1 dose, to be started within 24 hours of onset of symptoms, then 90 mg twice daily, to be combined with aspirin for the first 30 days.
Cautions
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)
Contraindications
Active bleeding; history of intracranial haemorrhage
Side effects
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
Interactions
**Severe interactions:**
- These increases are not considered clinically significant.
- However, no evidence of clinically significant adverse reactions was observed in the PLATO trial after concomitant administration with one or more medicinal products known to induce bradycardia (e.g.
**Other interactions (41):**
- Ticagrelor is primarily a CYP3A4 substrate and a mild inhibitor of CYP3A4.
- Ticagrelor is also a P-glycoprotein (P-gp) substrate and a weak P-gp inhibitor and may increase the exposure of P-gp substrates.
- Ticagrelor is a breast cancer resistance protein (BCRP) inhibitor.
- Effects of medicinal and other products on ticagrelor CYP3A4 inhibitors Strong CYP3A4 inhibitors - Co-administration of ketoconazole with ticagrelor increased the ticagrelor C max and AUC equal to...
- There was no effect of ticagrelor on diltiazem plasma levels.
- Other moderate CYP3A4 inhibitors (e.g.
Pregnancy
Manufacturer advises avoid-toxicity in animal studies.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises caution in moderate impairment (limited information available); avoid in severe impairment (no information available).
Medicinal forms
Tablet,Tablet
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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