Generality
Cilostazol is an active ingredient capable of inhibiting platelet aggregation and inducing vasodilation .
From the chemical point of view, cilostazol is a quinolone derivative and has specific therapeutic indications to facilitate gait without pain in patients with intermittent claudication . It is available as tablets for oral use that must be swallowed whole.
Medicinal products containing cilostazol can only be dispensed upon presentation of a repeatable prescription (RR).
Examples of Specialties Medicines containing Cilostazol
- Albaten®
- Cilostazol EG®
- Cilostazol Mylan®
- Cilostazol Sandoz®
- Fripass®
- Pletal®
Therapeutic indications
When is the use of Cilostazol indicated?
The use of cilostazol is indicated in the presence of intermittent claudication - a condition characterized by the perception of pain in the legs, difficulty walking and weakness - due to an insufficient supply of blood to the lower limbs (peripheral vasculopathy). Taking the drug reduces the pain during walking perceived by patients suffering from the aforementioned disorder.
Please note
The use of cilostazol is indicated only in patients in whom the intermittent claudication has not improved sufficiently after changing their habits and lifestyle (for example, abstaining from smoking, increasing physical activity, etc.). ).
To learn more: Claudicatio Intermittens »Warnings
Warnings and Precautions for the use of Cilostazol
Before taking cilostazol, you must inform your doctor if you suffer from any type of cardiovascular disease and / or if you suffer from blood pressure changes .
In any case, as a precautionary measure, before taking cilostazol-based medicines, it is advisable to inform the physician of your health conditions, making it aware of the possible presence of disorders or diseases of any kind, even if not of a cardiovascular nature.
Instead, during treatment with cilostazol, you must inform your doctor if:
- One must undergo any type of surgery, including dental surgery;
- Bruises and / or bleeding appear easily.
In the aforementioned cases, in fact, the doctor may decide to reduce the amount of active ingredient taken, or suspend the administration altogether.
Please note
Taking cilostazol can cause side effects that can negatively affect the ability to drive and / or use machinery (dizziness). For this reason, these activities should be avoided after taking the active ingredient in question.
Pharmacological Interactions
Interactions between Cilostazol and Other Drugs
Before starting treatment with cilostazol, you must inform your doctor if you are taking other drugs that can interfere with blood clotting or platelet aggregation (anticoagulant drugs, antiplatelet drugs, NSAIDs, etc.).
Furthermore, due to the drug interactions that may occur, it is necessary to inform the doctor if they are taking, or have recently been hired:
- Antibiotic drugs, in particular, macrolides (erythromycin, clarithromycin, etc.) and rifamycins (rifampicin);
- Antifungal drugs (eg, ketoconazole);
- Gastroprotective drugs (for example, omeprazole);
- Statins ;
- Ergot derivatives ;
- Antiepileptic drugs, such as phenytoin and carbamazepine;
- Cisapride ;
- Halofantrine ;
- Hypericum (also known as St. John's wort), its derivatives and products that contain it.
Finally, since cilostazol is able to increase the action of antihypertensive drugs, it is necessary to inform your doctor if you are taking:
- Beta-blocking drugs;
- ACE-inhibitors;
- Diuretics;
- Calcium channel blockers;
- Angiotensin II receptor antagonists.
However, before starting cilostazol therapy, you need to tell your doctor if you are taking, or have recently taken, any drugs or products of any kind, including non-prescription medicines (SOP ), OTC drugs, herbal and herbal products and homeopathic products.
Side effects
Side effects caused by the intake of Cilostazol
Like any other active ingredient, cilostazol can also cause side effects, although not all patients manifest them or manifest them in the same way. In fact, each person reacts subjectively to the administration of the drug manifesting side effects that are different in type and intensity, or not manifesting them at all.
However, below are some of the major side effects that can occur during treatment with cilostazol.
Blood disorders
Cilostazol treatment could lead to the appearance of:
- Anemia;
- Thrombocytopenia;
- Prolongation of bleeding time;
- Granulocytopenia or agranulocytosis;
- Leukopenia;
- pancytopenia;
- Hemorrhages in different organs and tissues;
- Bruising.
Nervous system disorders
During the intake of cilostazol may arise:
- dizziness;
- Headache;
- Insomnia;
- Hypoaesthesia;
- Paresis.
Cardiovascular disorders
The administration of cilostazol could give rise to several side effects of the cardiovascular system, among which we mention:
- Palpitations;
- Cardiac arrhythmias;
- Ventricular extrasystoles;
- Atrial fibrillation;
- Congestive heart failure;
- Syncope;
- Hot flashes;
- Hypertension.
Gastrointestinal disorders
Oral intake of cilostazol could cause:
- Nausea and vomit;
- Diarrhea;
- Flatulence;
- Abdominal pain;
- Dyspepsia;
- Gastritis.
Lung and airway disorders
Drug therapy with cilostazol could cause:
- Pharyngitis;
- Rhinitis;
- Cough;
- Dyspnoea;
- Pneumonia.
Skin and subcutaneous tissue disorders
With the administration of cilostazol may occur:
- Skin rash;
- Itch;
- Eczema;
- Urticaria;
- Stevens-Johnson syndrome or toxic epidermal necrolysis.
Other side effects
Other side effects that could occur during cilostazol therapy are:
- Allergic reactions, even serious, in sensitive individuals;
- Edema;
- Hyperglycemia and diabetes mellitus;
- Anorexia;
- States of anxiety;
- Conjunctivitis;
- Tinnitus;
- Changes in liver function, hepatitis and jaundice;
- Myalgia;
- Fever and chills;
- Malaise;
- Chest pain;
- Increased uricemia, blood urea and creatinemia.
Overdose
In the event of excessive doses of cilostazol, symptoms may arise such as: severe headache, diarrhea and tachycardia. Therefore, in the case of an overdose of cilostazol - ascertained or presumed to be - it is necessary to contact the doctor immediately or go to the nearest emergency room bringing with him the package of the medicinal product taken. There are no specific antidotes, therefore, the treatment is symptomatic and supportive. Emptying the stomach by inducing vomiting or gastric lavage may be useful.
Action mechanism
How does Cilostazol work?
Cilostazol carries out the anti-platelet and vasodilatory anti-aggregation action mainly through two mechanisms of action:
- Selective inhibition of phosphodiesterase 3A (PDE-3A): PDE-3A is the isoform of the enzyme phosphodiesterase type 3 most expressed at platelet level. It is responsible for the degradation of the AMPc (cyclic adenosine monophosphate, molecule with inhibitory action against aggregation and platelet degranulation) in AMP (adenosine monophosphate, a molecule that, instead, promotes platelet degranulation). With the inhibition of PDE-3A at the platelet level, therefore, there is an increase in the levels of AMPc which result in inhibition of platelet aggregation. Furthermore, the increase in cyclic AMP levels favors vasodilation.
- Inhibition of adenosine reuptake that, interacting with its receptors A1 and A2, causes an increase in the levels of AMPc. As stated above, the increase in the levels of the latter molecule favors both the inhibition of platelet degranulation and aggregation, and the dilation of blood vessels.
Thanks to the inhibition of platelet aggregation and the induction of vasodilation, cilostazol allows a better blood flow at the level of the lower limbs which we remember to be insufficient in the presence of intermittent claudication. In this way, therefore, cilostazol helps patients who suffer from this disorder to walk longer - traveling longer distances - without experiencing pain.
Use and Posology
How to take Cilostazol
Cilostazol is available as tablets for oral use . The tablets should be swallowed whole, with the help of a little water, at least 30 minutes before breakfast and dinner .
The dose of principle usually administered is 100 mg twice a day, in the morning and evening, to be taken as described above.
The duration of treatment could vary from 4 to 12 weeks. However, the exact dosage of the medicine will be established by the doctor for each patient.
Pregnancy and breastfeeding
Can Cilostazol be taken during pregnancy and during breastfeeding?
Since studies conducted in vivo showed that cilostazol has reproductive toxicity, its use is contraindicated during pregnancy .
Similarly, animal studies have shown that cilostazol can be excreted in breast milk. However, there is no confirmation that this also happens in humans. Therefore, as a precautionary measure, the use of the active ingredient during breastfeeding is not recommended .
For the reasons listed above, if the need arises to initiate a drug therapy based on cilostazol, pregnant women and breastfeeding mothers must necessarily inform the doctor of their condition.
Contraindications
When Cilostazol should not be used
The use of cilostazol is contraindicated in all the following cases:
- Known hypersensitivity to cilostazol itself and / or to one or more of the excipients contained in the medicinal product to be used;
- Patients who suffer - or who have suffered - from a variety of cardiovascular diseases or disorders, such as heart failure, heart disease, arrhythmias, heart attack and blood pressure changes;
- Patients suffering from liver and / or kidney diseases;
- Patients who suffer, or have suffered, from disorders or diseases capable of increasing the risk of bleeding (for example: stroke, gastrointestinal ulcers, eye disorders caused by diabetes, etc.);
- Taking drugs that increase the risk of bleeding (for example, antiplatelet drugs, anticoagulant drugs, NSAIDs, etc.);
- Pregnant.
