How to take Clopidogrel 75 mg: instructions and reviews

Clopidogrel is an antiaggregant drug.

The action of the drug is carried out due to the ability of the active substance to selectively inhibit the binding of adenosine diphosphate with receptors of platelets, as a result of which the activation of the glycoprotein IIb / IIIa complex is inhibited and the ability of platelets to aggregation.

On this page you will find all information about Clopidogrel: the full instructions for use for this medicine medium, average prices in pharmacies, complete and incomplete analogs of the drug, as well as reviews of people who have already applied Clopidogrel. Want to leave your opinion? Please write in the comments.

Clinical and pharmacological group

Antiaggregant.

Conditions of leave from pharmacies

It is released on prescription.

Price list

How much does Klopidogrel cost? The average price in pharmacies is at the level of220 rubles.

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Form of issue and composition

The tablets covered with a cover, pink color, biconcave. On the surface of the tablets, the roughness of the film coating is allowed.

• Active ingredient: clopidogrel - 75 mg in each tablet (in the form of clopidogrel hydrogen sulfite - 9, 75 mg).
• Excipients: mannitol, sodium croscarmellose, macrogol 4000, crospovidone, calcium stearate, silicon dioxide colloidal anhydrous, microcrystalline cellulose, hypromellose 2910, propylene glycol, titanium dioxide, carmuazine E-122, talc.

Pharmacological effect

Clopidogrel inhibits platelet aggregation and selectively inhibits the binding of adenosine diphosphate to receptors, localized on the walls of platelets, and induction of the GPIIb / IIIa complex, thus preventing gluing thrombocytes. Also, the substance blocks platelet aggregation, which is caused by other agonists, by stopping the stimulation of platelets by the released adenosine diphosphate.

The drug does not change the activity of phosphodiesterase, and it also provides an irreversible transformation adenosine diphosphate receptors on platelets, as a result of which they lose functionality until their natural death. The restoration of the physiological function takes place in the process of their regeneration, which takes about a week.

Indications for use

What helps? Clopidogrel is used to prevent thrombotic complications in patients with peripheral arterial occlusion, ischemic stroke or myocardial infarction.

In combination with acetylsalicylic acid, the drug is prescribed as a prophylaxis for thrombotic complications in acute coronary syndrome: without ST segment elevation (myocardial infarction myocardium without a Q wave, unstable angina), including those undergoing stenting; with an elevation of the ST segment, if it is possible to conduct a thrombolytic therapy.

Contraindications

The use of clopidogrel is contraindicated against the background of:

1. Acute bleeding, including intracranial hemorrhage or bleeding from peptic ulcers;
2. Severe hepatic insufficiency;
3. Hypersensitivity to the components of tablets.

Also, the medicine is not prescribed to nursing and pregnant women and children under 18 years of age.

Caution requires the simultaneous use of clopidogrel with warfarin, ASA, non-steroidal anti-inflammatory drugs (including COX-2 inhibitors), heparin and glycoprotein IIb / IIIa inhibitors, and the administration of when:

1. Inclination to bleeding;
2. Moderate hepatic impairment;
3. Chronic renal failure;
4. Pathological conditions that increase the risk of bleeding, including trauma and surgery.

Application in pregnancy and lactation

Pregnancy.In the absence of adequate clinical safety data, it is not recommended to take clopidogrel during pregnancy. Studies on the effect of clopidogrel on pregnancy carried out on animals showed no adverse effects on pregnancy, embryo / fetus development, labor and postnatal development.

Breast-feeding.It is not known whether clopidogrel penetrates into human breast milk. Animal studies have shown that the drug penetrates into breast milk. As a precaution, breastfeeding should be discontinued during treatment with clopidogrel. Since most drugs are excreted in breast milk, and because of the possibility of developing serious adverse reactions in infants on breastfeeding, the decision to discontinue the drug or stop breastfeeding should be taken, given the need for clopidogrel breastfeeding mother.

Reproductive function.In animal studies, the effect of clopidogrel on reproductive function was not revealed.

Instructions for use

The instructions for use indicate that the Clopidogrel tablets are taken orally, regardless of food intake.

• Adults and patients of advanced age are prescribed clopidogrel 75 mg once a day.

Treatment should start from the 1st day to the 35th day after myocardial infarction, from 7 days to 6 months after an ischemic stroke.

In acute coronary syndrome without ST segment elevation (unstable angina or myocardial infarction without Q-wave) treatment is started with a single dose of loading dose of 300 mg, and then continues at a dose of 75 mg 1 time / day (with ASK - 75-325 mg / day). Since the use of ASA in high doses is associated with a greater risk of bleeding, the recommended dose should not be more than 100 mg. The maximum favorable effect occurs after 3 months. The course of treatment is up to 1 year.

In acute coronary syndrome with ST segment elevation (acute myocardial infarction with ST segment elevation), 75 patients mg / day with the initial single dose loading in combination with ASA and thrombolytics (or without thrombolytics).

In patients with a genetically determined decrease in the activity of the isoenzyme CYP2C19, the effect of clopidogrel may be reduced. The optimal dosage regimen in these patients is not established.

• In patients over the age of 75, clopidogrel should be treated without the use of a loading dose. Combination therapy should be started as soon as possible after the development of symptoms and continue for at least 4 weeks.

The experience of using in patients with chronic renal failure or hepatic insufficiency of moderate degree is limited.

Due to the existing possibility of developing dizziness, during therapy it is recommended to use caution in managing motor transport and other potentially dangerous jobs requiring high concentration of attention and fast psychomotor reactions.

Side effects

Treatment with "Klopidogrel" medication can lead to undesirable consequences:

1. Cardiovascular system: sometimes - lowering blood pressure, vasculitis.
2. Blood coagulation system: infrequently - increased bleeding time.
3. Immune system: sometimes - anaphylactoid reactions, serum sickness.
4. Musculoskeletal system: sometimes - myalgia, arthralgia, arthritis, joint and muscle hemorrhages.
5. Sense organs: rarely - vertigo; infrequently - eye hemorrhage (in the tissue and retina of the eye, conjunctiva).
6. Urinary system: sometimes - increased levels of creatine in the blood, glomerulonephritis; infrequently - hematuria.
7. Respiratory system: sometimes - interstitial pneumonia, bronchospasm, bleeding from the respiratory tract (pulmonary hemorrhage, hemoptysis); often - epistaxis.
8. Subcutaneous tissues and skin: sometimes - angioedema, eczema, urticaria, flat lichen, erythematous rash, bullous dermatitis (Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis); infrequently - itching, rash, purpura.
9. Hemopoietic systems: sometimes - thrombotic thrombocytopenic purpura, agranulocytosis, aplastic anemia, pancytopenia, granulocytopenia, severe thrombocytopenia; rarely - neutropenia (including severe form); infrequently - eosinophilia, leukopenia.
10. Central nervous system: sometimes - confusion, hallucinations, taste disorders; infrequently - dizziness, headache, paresthesia, intracranial hemorrhage (there are reports of cases with lethal outcome).
11. Digestive system: sometimes - gastrointestinal hemorrhage and retroperitoneal bleeding with fatal outcome, hepatitis, colitis (including lymphocytic colitis or ulcerative colitis), pancreatitis, hepatic insufficiency in the stage of exacerbation, deviation from the norm of functional liver indicators, stomatitis; infrequent - attacks of nausea, bloating, constipation, vomiting, ulcer of duodenum and stomach; very often - diarrhea, indigestion, stomach ache.

Other: sometimes - fever; often - bleeding from the point of vascular puncture.

Overdose

The administration of the drug in doses exceeding the recommended dose is indicated by an increase in bleeding time with subsequent complications. In such situations, appropriate therapy will be required. In the case where rapid correction of the increased bleeding time is needed, transfusion of TM is necessary. There is no specific antidote.

special instructions

Simultaneous use with warfarin is not recommended, as this may increase the intensity of bleeding (except for special rare clinical situations).

During therapy, it is necessary to monitor the parameters of the hemostasis system, including the number of platelets, activated partial thromboplastin time, tests of the functional activity of platelets, and also regularly investigate the functional activity liver.

The drug should be used with caution in patients with an increased risk of bleeding during surgery, trauma, other pathological conditions, in the presence of diseases predisposing to the development of bleeding (especially the eye and gastrointestinal), as well as patients receiving acetylsalicylic acid, non-steroidal anti-inflammatory drugs (including COX-2 inhibitors), glycoprotein inhibitors IIb / IIIa or heparin.

To identify any signs of bleeding, including hidden, you should carefully monitor the condition of patients, especially during the first weeks of Clopidogrel application and / or after surgical operations or invasive procedures on the heart.

In surgical interventions, if antiplatelet effect is undesirable, Clopidogrel should be discontinued 7 days before surgery.

The drug extends the time of bleeding, so it is prescribed with caution to patients with diseases predisposing to the development of bleeding (especially, intraocular and gastrointestinal).

In the presence of severe functional disorders of the liver, you should consider the risk of hemorrhagic diathesis. The experience of using clopidogrel in patients with moderate functional impairment of the liver is limited, as a result of which such a drug is prescribed with caution.

In very rare cases, after taking clopidogrel (including its short-term use), thrombotic thrombocytopenic purpura, characterized by microangiopathic hemolytic anemia and thrombocytopenia in combination with neurologic symptoms, functional renal impairment or fever. Thrombotic thrombocytopenic purpura is a potentially life-threatening disease requiring immediate therapy, incl. with the use of plasmapheresis.

Drug Interactions

A number of clinical studies with clopidogrel and other, simultaneously prescribed with the aim of studying possible pharmacodynamic and pharmacokinetic interactions that showed that:

1. Antacids did not reduce the absorption of clopidogrel;
2. Simultaneous use of phenobarbital, cimetidine and estrogens had no significant effect on the pharmacodynamics of clopidogrel;
3. Pharmacokinetic indices of digoxin and theophylline did not change when they were combined with clopidogrel;
4. When clopidogrel was used together with atenolol, nifedipine, or both, clinically significant pharmacodynamic interaction was not observed;
5. Phenytoin and tolbutamide can be safely used concomitantly with clopidogrel (CAPRIE study), despite the fact that the data obtained from studies with microsomes of the human liver indicate that the carboxylic metabolite of clopidogrel can inhibit the activity of the 2S9 isoenzyme of the cytochrome P450 family, which can lead to increased plasma concentrations of certain drugs (phenytoin, tolbutamide and some NSAIDs), which are metabolized by the 2S9 isoenzyme of the cytochrome family. P450;
6. In clinical studies, there was no clinically significant adverse interaction with ACE inhibitors, diuretics, β-adrenoblockers, slow calcium channel blockers, lipid-lowering agents, coronary vasodilators, hypoglycemic means (including insulin), antiepileptic drugs, blockers of GPIIb / IIIa receptors and drugs for hormone replacement therapy.

With the simultaneous use of warfarin with clopidogrel, the intensity of bleeding may increase, so the use of this combination is not recommended.

The appointment of IIb / IIIa receptor blockers together with clopidogrel requires caution in patients who have increased risk of bleeding (with trauma and surgical interventions or other pathological states).

Acetylsalicylic acid does not alter the effect of clopidogrel, an inhibitor of ADP-induced aggregation thrombocytes, but clopidogrel potentiates the effect of acetylsalicylic acid on collagen-induced aggregation thrombocytes. However, simultaneous with clopidogrel, acetylsalicylic acid intake of 500 mg 2 times / day in for 1 day did not cause a significant increase in bleeding time caused by the admission clopidogrel. Between clopidogrel and acetylsalicylic acid, pharmacodynamic interaction is possible, which leads to an increased risk of bleeding. Therefore, when they are used simultaneously, care must be taken. Although in clinical trials, patients received combination therapy with clopidogrel and acetylsalicylic acid for up to one year.

According to the clinical trial conducted with the participation of healthy individuals, when taking clopidogrel, there was no need to change the dose of heparin and its anticoagulant effect did not change. With simultaneous application with heparin, there was no change in the antiplatelet effect of clopidogrel. Between clopidogrel and heparin, pharmacodynamic interaction is possible, which can increase the risk of bleeding, so the simultaneous use of these drugs requires caution.

The safety of the combined use of clopidogrel, fibrin-specific or fibrinospecific drugs and heparin was investigated in patients with acute myocardial infarction. The frequency of clinically significant bleeding was similar to that observed in the joint use of thrombolytic agents and heparin with acetylsalicylic acid.

In a clinical study conducted with the participation of healthy volunteers, the combined use of clopidogrel and naproxen increased latent blood loss through the gastrointestinal tract. However, due to the lack of research on the interaction of clopidogrel with other NSAIDs, at present It is not known whether there is an increased risk of gastrointestinal bleeding when taking clopidogrel together with other NSAIDs. Therefore, the appointment of NSAIDs, incl. inhibitors of COX-2, in combination with clopidogrel should be carried out with caution.

Reviews

We picked up some reviews of people taking the drug Clopidogrel:

1. Galina. For a year and two months, Coplanix-clopidogrel + acetylsalicylic acid was drunk after stenting (3 stents). The first three months the blood vessels bursted all over the body, bruised, there was even a puncture of the knee joint, they pumped out the blood that gathered in the knee joint. But this is all tolerable, the drug is excellent, with stenting and shunting without it, you can not do, if you care about blood vessels and your heart. No fatal outcome is even out of the question, no need to carry delirium, listen to your treating doctors and no one else! One single negative - the drug is very expensive, but life is more expensive! Health to all!
2. Lyudmila. The doctor prescribed to take clopidogrel for blood thinning. Spent 500 rubles. I read the instructions at home. Contraindications are more than good, in my opinion. Most likely I will not accept it, tk. there are problems with the gastrointestinal tract, nosebleeds, etc.
3. Marina. Clopidogrel buy her husband soon as a year. Last year he suffered a massive myocardial infarction. Since it takes the pill in the complex and it is recommended to take a long time, what effect is given specifically by clopidogrel, but for myself I learned something. It says, the side effects can be in the form of skin rashes. The problem of a dermatological nature is also there, with its different ointments, there is no complete healing.

Analogues

Analogues of Clopidogrel on active substance are medicines Cardutol, Agregal, Detromb, Klopilet, Trombeks, Plavix, Plogrel, Troken, Targetek, Plagril, Klopideks, Egitrombom, Tromborel.

In the presence of contraindications, one of the analogues of Clopidogrel may be used, which has a similar therapeutic effect. These include: Ilomedin, Agrenoks, Integrilin, Monafram, ReoPro, Tiklo, Aspicor, Persanthin, Coplavix, Aspirin, Ventavis, Cardiasc, Tiklid, Cardiomagnolo, Trombopol, Effient, Brilinta.

Before using analogues, consult your doctor.

Storage conditions and shelf life

Do not allow clopidogrel to enter children's hands, the storage temperature can not exceed 25 degrees. The drug is stored under these conditions for three years.

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