Drugs List

Therapeutic Indications

Uses

Atherothrombotic events post acute coronary syndromes: Prevention
Atherothrombotic events with history of myocardial infarction: Prevention

For prevention of atherothrombotic events in combination with aspirin in adults with:
Acute Coronary Syndromes (ACS).
History of myocardial infarction (MI) and a high risk of developing an atherothrombotic event.

Ticagrelor is indicated both for patients managed medically and those managed with percutaneous coronary intervention or a coronary artery by-pass graft.

Contraindications

Children under 18 years
Haemorrhage
Breastfeeding
History of cerebrovascular haemorrhage
Pregnancy
Renal dialysis
Severe hepatic impairment

Precautions and Warnings

Females of childbearing potential
Patients over 75 years
Predisposition to haemorrhage
Predisposition to syncope
Predisposition to trauma
Recent surgery
Recent trauma
Asthma
Bradycardia
Chronic obstructive pulmonary disease
Coagulopathy
Gastrointestinal haemorrhage
Gout
History of asthma
History of gastrointestinal bleeding
History of hyperuricaemia
Moderate hepatic impairment
Moderate renal impairment
Non paced second/third degree AV block
Non-paced sinus node dysfunction
Uric acid nephropathy

Advise ability to drive/operate machinery may be affected by side effects
Consider clinical assessment if central sleep apnoea is suspected
Monitor renal function one month after initiation then periodically
Advise on the need to report unusual bleeding
Advise patient that omitting dose may increase CV risk
Advise patient to contact their doctor if dyspnoea rapidly worsens
May prolong bleeding time
May affect results of some laboratory tests
Discontinue 5 days prior to surgery when antiplatelet effect not required
Advise patient not to take NSAIDs unless advised by clinician
Advise patient not to take St John's wort concurrently
Advise patient grapefruit products may increase plasma level
Female: Ensure adequate contraception during treatment
Advise patient of risk of bleeding
Advise patient to inform physician/dentist of their use of this medication

Lapses in treatment or premature discontinuation of treatment should be avoided. Patients with acute coronary syndromes who discontinue antiplatelet therapy prematurely could be at increased risk of cardiovascular death or myocardial infarction due to underlying disease.

Creatinine levels may increase during treatment with ticagrelor. Renal function should be checked after one month and thereafter according to routine medical practice, paying special attention to patients over 75 years old, those with moderate-severe renal impairment or those receiving concomitant medical treatment with an angiotensin receptor blocker.

In healthy volunteers suffering bleeding due to excessive dosing, the use of platelet transfusions was not beneficial in reversing the antiplatelet action of ticagrelor. Therefore, if bleeding occurs, other supportive measures should be taken.

Antifibrinolytic therapy and/or recombinant factor VIIa may increase haemostasis. Treatment with ticagrelor may be resumed after the cause of bleeding has been identified and controlled.

Pregnancy and Lactation

Pregnancy

Ticagrelor is contraindicated in pregnancy.

At the time of writing there is limited data on the use of ticagrelor in pregnancy. Studies in rats and rabbits have shown reproductive toxicity, with a slightly reduced body weight gain and reduced neonatal viability and birth weight with delayed growth. In female rats, ticagrelor at high dose showed an increased incidence of uterine tumours and hepatic adenomas (however this is considered by the manufacturer to be likely to be due to a rodent-specific mechanism). Minor developmental anomalies were seen in rats taking a maternally toxic dose. In rabbits, a slight delay in hepatic maturity and skeletal development was seen in foetuses from dams at high dose without showing maternal toxicity. Ticagrelor produced irregular cycles (mainly extended) in female rats but did not affect the overall fertility in male or female rats.

Lactation

Ticagrelor is contraindicated in breastfeeding.

At the time of writing, there is limited published information concerning the use of ticagrelor during breastfeeding. Animal studies have shown that ticagrelor and its active metabolites are excreted into the breast milk of rats. It is unknown if ticagrelor is excreted into human breast milk. A risk to newborns or infants cannot be excluded.

Side Effects

Abdominal pain
Angioedema
Atrioventricular block
Bradyarrhythmias
Cerebral haemorrhage
Cheyne-Stokes breathing
Confusion
Conjunctival haemorrhage
Constipation
Contusion
Diarrhoea
Dizziness
Dyspepsia
Dyspnoea
Ear haemorrhage
Ecchymosis
Epistaxis
Gastritis
Gastro-intestinal haemorrhage
Gingival bleeding
Gout
Gouty arthritis
Haemarthrosis
Haematoma
Haematospermia
Haematuria
Haemoptysis
Haemorrhage
Headache
Hypersensitivity reactions
Hyperuricaemia
Hypotension
Muscle haemorrhage
Nausea
Ocular haemorrhage
Paraesthesia
Petechiae
Postmenopausal bleeding
Pruritus
Pulmonary haemorrhage
Rash
Rectal haemorrhage
Retinal haemorrhage
Retroperitoneal bleeding
Serum creatinine increased
Skin/soft tissue haemorrhage
Sleep apnoea
Subcutaneous haemorrhage
Syncope
Thrombotic thrombocytopenic purpura
Tumour haemorrhage
Urinary tract bleeding
Vaginal haemorrhage
Vertigo
Vomiting
Wound haemorrhage

Presentation

Oral formulations of ticagrelor.

Drugs List

Therapeutic Indications

Uses

Atherothrombotic events post acute coronary syndromes: Prevention
Atherothrombotic events with history of myocardial infarction: Prevention

For prevention of atherothrombotic events in combination with aspirin in adults with:
Acute Coronary Syndromes (ACS).
History of myocardial infarction (MI) and a high risk of developing an atherothrombotic event.

Ticagrelor is indicated both for patients managed medically and those managed with percutaneous coronary intervention or a coronary artery by-pass graft.

Dosage

Adults

Additional Dosage Information

Contraindications

Children under 18 years
Haemorrhage
Breastfeeding
History of cerebrovascular haemorrhage
Pregnancy
Renal dialysis
Severe hepatic impairment

Precautions and Warnings

Females of childbearing potential
Patients over 75 years
Predisposition to haemorrhage
Predisposition to syncope
Predisposition to trauma
Recent surgery
Recent trauma
Asthma
Bradycardia
Chronic obstructive pulmonary disease
Coagulopathy
Gastrointestinal haemorrhage
Gout
History of asthma
History of gastrointestinal bleeding
History of hyperuricaemia
Moderate hepatic impairment
Moderate renal impairment
Non paced second/third degree AV block
Non-paced sinus node dysfunction
Uric acid nephropathy

Advise ability to drive/operate machinery may be affected by side effects
Consider clinical assessment if central sleep apnoea is suspected
Monitor renal function one month after initiation then periodically
Advise on the need to report unusual bleeding
Advise patient that omitting dose may increase CV risk
Advise patient to contact their doctor if dyspnoea rapidly worsens
May prolong bleeding time
May affect results of some laboratory tests
Discontinue 5 days prior to surgery when antiplatelet effect not required
Advise patient not to take NSAIDs unless advised by clinician
Advise patient not to take St John's wort concurrently
Advise patient grapefruit products may increase plasma level
Female: Ensure adequate contraception during treatment
Advise patient of risk of bleeding
Advise patient to inform physician/dentist of their use of this medication

Lapses in treatment or premature discontinuation of treatment should be avoided. Patients with acute coronary syndromes who discontinue antiplatelet therapy prematurely could be at increased risk of cardiovascular death or myocardial infarction due to underlying disease.

Creatinine levels may increase during treatment with ticagrelor. Renal function should be checked after one month and thereafter according to routine medical practice, paying special attention to patients over 75 years old, those with moderate-severe renal impairment or those receiving concomitant medical treatment with an angiotensin receptor blocker.

In healthy volunteers suffering bleeding due to excessive dosing, the use of platelet transfusions was not beneficial in reversing the antiplatelet action of ticagrelor. Therefore, if bleeding occurs, other supportive measures should be taken.

Antifibrinolytic therapy and/or recombinant factor VIIa may increase haemostasis. Treatment with ticagrelor may be resumed after the cause of bleeding has been identified and controlled.

Pregnancy and Lactation

Pregnancy

Ticagrelor is contraindicated in pregnancy.

At the time of writing there is limited data on the use of ticagrelor in pregnancy. Studies in rats and rabbits have shown reproductive toxicity, with a slightly reduced body weight gain and reduced neonatal viability and birth weight with delayed growth. In female rats, ticagrelor at high dose showed an increased incidence of uterine tumours and hepatic adenomas (however this is considered by the manufacturer to be likely to be due to a rodent-specific mechanism). Minor developmental anomalies were seen in rats taking a maternally toxic dose. In rabbits, a slight delay in hepatic maturity and skeletal development was seen in foetuses from dams at high dose without showing maternal toxicity. Ticagrelor produced irregular cycles (mainly extended) in female rats but did not affect the overall fertility in male or female rats.

Lactation

Ticagrelor is contraindicated in breastfeeding.

At the time of writing, there is limited published information concerning the use of ticagrelor during breastfeeding. Animal studies have shown that ticagrelor and its active metabolites are excreted into the breast milk of rats. It is unknown if ticagrelor is excreted into human breast milk. A risk to newborns or infants cannot be excluded.

Side Effects

Abdominal pain
Angioedema
Atrioventricular block
Bradyarrhythmias
Cerebral haemorrhage
Cheyne-Stokes breathing
Confusion
Conjunctival haemorrhage
Constipation
Contusion
Diarrhoea
Dizziness
Dyspepsia
Dyspnoea
Ear haemorrhage
Ecchymosis
Epistaxis
Gastritis
Gastro-intestinal haemorrhage
Gingival bleeding
Gout
Gouty arthritis
Haemarthrosis
Haematoma
Haematospermia
Haematuria
Haemoptysis
Haemorrhage
Headache
Hypersensitivity reactions
Hyperuricaemia
Hypotension
Muscle haemorrhage
Nausea
Ocular haemorrhage
Paraesthesia
Petechiae
Postmenopausal bleeding
Pruritus
Pulmonary haemorrhage
Rash
Rectal haemorrhage
Retinal haemorrhage
Retroperitoneal bleeding
Serum creatinine increased
Skin/soft tissue haemorrhage
Sleep apnoea
Subcutaneous haemorrhage
Syncope
Thrombotic thrombocytopenic purpura
Tumour haemorrhage
Urinary tract bleeding
Vaginal haemorrhage
Vertigo
Vomiting
Wound haemorrhage

Effects on Laboratory Tests

Treatment with ticagrelor may cause false negative results in platelet function tests for heparin induced thrombocytopenia (HIT).

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: April 2016

Reference Sources

Summary of Product Characteristics: Brilique 60mg film coated tablets. AstraZeneca UK Ltd. Revised November 2022.
Summary of Product Characteristics: Brilique 90mg film coated tablets. AstraZeneca UK Ltd. Revised November 2022.
Summary of Product Characteristics: Brilique 90mg Orodispersible Tablets. AstraZeneca UK Ltd. Revised November 2022.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 14 September 2022.