Generality
Ticagrelor is an active ingredient with an anti-platelet aggregation action.
Its use, therefore, is indicated in all those cases in which it is necessary to prevent blood clotting in order to avoid the appearance of cardiovascular events in patients at risk.
Usually, ticagrelor is administered orally in association with another active ingredient with an anti-platelet aggregation action: acetylsalicylic acid . The dosage of drug to be administered may vary depending on the reason why it is necessary to hinder platelet aggregation.
Examples of Medicinal Specialties Containing Ticagrelor
- Brilique®
Therapeutic indications
When is the use of Ticagrelor indicated?
The use of ticagrelor is indicated to decrease the possibility of the onset of heart attack, stroke or other fatal cardiovascular events caused by the formation of blood clots in patients who, in the past, have had a heart attack or who have suffered from angina unstable .
Warnings
Warnings and precautions for the use of Ticagrelor
Before starting the ticagrelor treatment, it is advisable to inform your doctor if you are in one or more of the following conditions:
- One must undergo surgery . In such a condition, in fact, ticagrelor-based therapy should be suspended in good time in order to avoid an increased risk of bleeding and bleeding during the surgical procedure. Indicatively, the suspension of the drug should take place 5 days before the execution of the intervention; in any case, the doctor will provide the correct information on the matter.
- You are exposed to a greater risk of bleeding / haemorrhage due to recent surgical interventions (including dental ones), the presence of coagulation disorders, the presence of serious wounds, the presence of gastric ulcer or polyps of the colon and rectum.
- You suffer from bradycardia .
- You suffer from asthma, breathing difficulties or other disorders and lung diseases .
- There are high levels of uricemia (uric acid in the blood).
- You suffer from disorders or liver diseases .
However, as a precautionary measure, before taking ticagrelor-based medicines, it is always a good idea to inform your doctor of your health conditions and of the possible presence of any type of disorder or illness.
Pharmacological Interactions
Interactions of Ticagrelor with Other Drugs
Before taking ticagrelor, you must tell your doctor if you are taking other medicines that may increase your risk of bleeding, such as:
- Oral anticoagulants, such as warfarin;
- Fibrinolytic drugs (alteplasi, streptokinase, etc.);
- Non-steroidal anti - inflammatory drugs (NSAIDs), such as, for example, naproxen and ibuprofen;
- Antifungal drugs like ketoconazole;
- The alkaloids and ergot derivatives used in the treatment of headaches;
- Antibiotics like clarithromycin;
- Cisapride (active ingredient used against dyspeptic disorders);
- Antidepressants such as nefazodone and selective serotonin reuptake inhibitors (SSRIs), such as sertraline, citalopram and paroxetine;
- Antivirals such as atazanavir and ritonavir.
Also, because of the drug interactions that could occur, it is equally important to tell your doctor if you are taking:
- Antiarrhythmic drugs, such as diltiazem and quinidine;
- Antihypertensive drugs (verapamil and beta-blockers);
- Digitalis glycosides such as digoxin;
- Antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, etc.);
- Statins, such as atorvastatin and lovastatin, in particular, at dosages above 40 mg a day;
- Immunosuppressants such as cyclosporine;
- Opioid drugs;
- Rifampicin (an antibiotic belonging to the rifamycin group).
In any case, before starting ticagrelor therapy, you need to tell your doctor if you are taking - or if you have recently been - drugs or products of any kind, including medicines without a prescription (SOP ), OTC drugs, herbal and herbal products and homeopathic products.
Side effects
Side Effects Caused by the Assumption of Ticagrelor
Like all drugs, ticagrelor can also cause several side effects, although not all patients manifest them or manifest them in the same way. In fact, each individual reacts differently and subjectively to the administration of the drug.
However, the main side effects that could occur during ticagrelor therapy are listed below.
Bleeding and Bleeding
Since ticagrelor is a platelet antiplatelet, it is possible that its intake carries a greater risk of bleeding and bleeding .
In particular, ticagrelor can cause:
- Gastrointestinal hemorrhage;
- Retroperitoneal hemorrhage;
- Intracranial hemorrhage;
- Respiratory tract bleeding;
- Muscle bleeding;
- Urinary tract bleeding;
- Ocular hemorrhage;
- otorrhagia;
- Subcutaneous bleeding;
- Reproductive system bleeding.
The risk of bleeding and bleeding is particularly pronounced in the presence of tumors, other blood diseases, gastric pathologies (for example, ulcer), trauma, etc.
Gastrointestinal disorders
Treatment with ticagrelor may cause the appearance of:
- Nausea;
- Diarrhea or constipation;
- Dyspepsia.
Nervous system disorders
During ticagrelor therapy, the following may occur:
- Headache;
- dizziness;
- Syncope;
Skin and subcutaneous tissue disorders
Taking ticagrelor could result in rashes and itching.
Other side effects
Other possible side effects of taking ticagrelor consist of:
- Allergic reactions in sensitive individuals;
- Dyspnoea;
- Dizziness;
- Hyperuricemia, gout and gouty arthritis;
- Hypotension;
- Confusion;
- Increased blood creatinine levels.
Overdose
In the event of an overdose of ticagrelor, it is possible to develop one or more of the aforementioned side effects. All this is associated with a significant increase in the risk of bleeding and bleeding. Therefore, if you take an overdose of ticagrelor - suspected or ascertained to be - you must immediately go to the emergency room bringing the packaging of the medicine you are using.
Action mechanism
How does Ticagrelor work?
Ticagrelor exerts its antiplatelet action through selective and reversible binding with the P2Y12 receptor located on the platelets. In fact, when this receptor is activated by the link with its endogenous substrate - ADP (adenosine diphosphate) - there is a considerable increase in platelet aggregation induced by the inhibition of adenylate cyclase and the consequent decrease in levels of cyclic AMP (compound that, in contrast to ADP, inhibits platelet aggregation).
Ticagrelor binds to the P2Y12 receptor and prevents activation and signal transduction induced by ADP, with consequent inhibition of platelet aggregation .
Please note
The ticagrelor does not hinder the binding of ADP with P2Y12, but prevents the latter from being activated when the bond with its endogenous substrate (the ADP, in fact) occurs.
Method of use and Posology
How to take ticagrelor
Ticagrelor is available in pharmaceutical formulations suitable for oral administration, such as coated tablets - containing 60 mg or 90 mg of active ingredient - and orodispersible tablets - containing 90 mg of active ingredient.
The coated tablets should be swallowed whole with a little water; while the orodispersible tablets must be dissolved slowly in the mouth .
The ticagrelor can be taken, indifferently, far or near meals, but it is advisable to take the drug all the days (as long as the doctor says) at the same time .
The dosage of the active ingredient indicated to prevent the formation of clots in each patient must be established by the doctor. However, the dosage is usually as follows:
- Tablets containing 60 mg of ticagrelor : they are used to prevent the formation of clots in patients who have had a heart attack for over a year . The usual administered dose is two tablets per day, to be taken in the morning and evening.
- Tablets containing 90 mg of ticagrelor : they are used to prevent the formation of clots both in patients who have had a heart attack and in patients who have suffered from unstable angina. Usually, an initial attack dose is administered first and then given a maintenance dose:
- Initial attack dose : two tablets to be taken at once, for a total of 180 mg of ticagrelor.
- Usual maintenance dose : one 90 mg tablet to be taken twice a day, up to 12 months or for the period prescribed by the doctor.
Patients with Swallowing Difficulties
Patients who struggle to swallow the ticagrelor-coated tablet whole and cannot take the orodispersible tablets, can pulverize it and suspend it in half a glass of water, stirring quickly and drinking immediately. After that, it is recommended to refill the glass and drink again, so as to be sure that you have taken all the powdered tablet.
Combination with acetylsalicylic acid
Usually, ticagrelor is administered in combination with another antiplatelet agent, acetylsalicylic acid . Generally, the dose of this active ingredient usually administered ranges from 75 mg to 150 mg a day. However, the exact dosage of both active ingredients - ticagrelor and acetylsalicylic acid - will be established by the doctor on an individual basis for each patient.
Pregnancy and breastfeeding
Can Ticagrelor be taken during pregnancy and during breastfeeding?
The use of ticagrelor is not recommended in pregnant women and breastfeeding mothers, as it has shown reproductive toxicity and because it is excreted in breast milk . Therefore, this category of patients, if the need arises to take the active ingredient in question, must necessarily inform the doctor of their condition before the start of treatment.
In addition, fertile women receiving ticagrelor should use appropriate contraceptive methods to avoid pregnancies.
Contraindications
When the Ticagrelor should not be used
Ticagrelor administration is contraindicated in all the following cases:
- Known hypersensitivity to the same ticagrelor or to any of the excipients contained in the medicinal product to be used;
- In patients with bleeding or bleeding in progress ;
- In patients who suffered from stroke caused by bleeding in the brain;
- In patients suffering from severe liver disorders and diseases ;
- In patients on medication, such as: ketoconazole (antifungal), clarithromycin (antibiotic), nefazodone (antidepressant), ritonavir and atazanavir (antiviral);
- In pregnancy and during breastfeeding .
Also, remember that the use of ticagrelor is recommended only in adults, therefore, it should not be used in children and adolescents under 18 years of age .
