Zilt, 75 mg, film-coated tablets, 84 pcs., KRKA-Rus buy in Moscow at a low price

Compound

One tablet of the drug Zilt contains 97.8 milligrams of clopidogrel hydrogen sulfate .
When calculated in clopidogrel, one tablet of this medicine contains 75 milligrams of the active drug compound. In addition, Zilt contains such auxiliary components as: hydrogenated castor oil (4 mg), pregelatinized starch (12 mg), anhydrous lactose (108.1 mg), microcrystalline cellulose (30 mg), as well as 6000 macrogol ( 8 mg.).

The film shell of the tableted drug contains the following elements: propylene glycol (0.4 mg), hypromellose (5.6 mg), red iron oxide (0.04 mg), titanium dioxide (1.46 mg), as well as talc (0.5 mg.).

Pharmacodynamics and pharmacokinetics

The so-called prodrug compound clopidogrel, in its chemical structure, is an active metabolite and is an inhibitor of platelet aggregation . The drug compound selectively inhibits the binding of adenosine diphosphates (abbreviated as ADP , i.e. free nucleotide , the chemical composition of which contains phosphoric acid, ribose, and adenine ) with platelet receptors P2Y12 .

In addition, the drug affects ADP-mediated activation of GPIIb/IIIa (glycoprotein complex) , thereby inhibiting platelet aggregation . It is noteworthy that the process of platelet aggregation is irreversible and does not stop during their life cycle, which usually lasts from 7 to 10 days. This means that the restoration of platelet occurs simultaneously with their renewal.

Since the blockade of platelet activation is enhanced under the influence of ADP , platelet aggregation can also occur when induced other than ADP . When taking this drug, the effectiveness of ADP , which is produced in each active platelet, decreases. Noticeable inhibition of platelet aggregation can be observed already on the first day of taking the drug at a dosage of 75 mg.

After five days from the last dose of the drug, platelet aggregation , as well as the duration of bleeding, is restored to its previous level. The drug helps prevent the development of atherothrombotic in patients who suffer from atherosclerosis . Zilt is especially effective in cases of damage to peripheral, cerebral, and coronary arteries .

A single daily dose of Zilt (75 mg) is rapidly absorbed. The maximum blood level of clopidogrel is achieved after 45 minutes. The kidneys remove half of the drug from the body, the intestines remove the second half.

Pharmacological properties of the drug Zilt

By preventing the binding of ADP to receptors located on the surface of platelets and the activation of the GP IIb/IIIa complex, clopidogrel inhibits ADP-dependent platelet aggregation. Clopidogrel also inhibits platelet aggregation caused by other factors. The effect of clopidogrel persists throughout the life of platelets. With prolonged use of clopidogrel at a therapeutic dose (75 mg/day), a noticeable inhibition of platelet aggregation occurs already on the 1st day of treatment, then the antiplatelet effect gradually increases and reaches a maximum after 3–7 days of regular use of the drug. With prolonged use of clopidogrel at a therapeutic dose, the average level of inhibition of platelet aggregation is 40–60%. After cessation of treatment, the effect of clopidogrel on aggregation and bleeding duration disappears, usually after 5 days. After oral administration, clopidogrel is rapidly absorbed (the time to reach maximum plasma concentration is 0.7–0.8 hours). After 2 hours, the drug is no longer detectable in the blood plasma. Absorption is approximately 50% and does not depend on simultaneous food intake. The main part of clopidogrel and its main metabolite (98 and 94%, respectively) is reversibly bound to plasma proteins. Clopidogrel is a prodrug. Metabolized in the liver, the main metabolite is a pharmacologically inactive derivative of carboxylic acid. Its concentration in blood serum is 85% of the total amount of the drug. Maximum serum concentrations are achieved approximately 1 hour after administration. The active metabolite, a thiol derivative, is formed by the oxidation of clopidogrel to 2-oxoclopidogrel, followed by hydrolysis. This oxidation occurs with the participation of cytochrome P450. This active metabolite, which can be isolated in vitro , quickly and irreversibly binds to platelet receptors and inhibits their aggregation. It is not detected in blood serum. After a single or repeated dose, 50% of the administered dose of clopidogrel is excreted in the urine and 46% in the feces. The half-life of the main metabolite after a single or repeated dose of the drug is 8 hours.

Indications for use of Zilta

Indications for the use of Zilt are the following cases:

prevention atherothrombotic complications in patients who have recently suffered a myocardial infarction , as well as after a stroke ;
arterial diseases;
acute coronary syndrome .

It is worth noting that this drug is used in the treatment of two groups of patients suffering from coronary syndrome:

when raising the ST segment , i.e. in the case of a so-called acute heart attack ;
with unstable angina , as well as with a heart attack without a Q wave , when the ST segment does not rise .

In addition, Zylt is used in combination with acetylsalicylic acid in the thrombolytic therapeutic treatment of patients.

Contraindications

Zilt is contraindicated:

for hypersensitivity ;
in acute forms of bleeding, for example, intracranial hemorrhage;
in case of liver dysfunction;
for lactose intolerance ;
with lactase deficiency ;
during pregnancy and during breastfeeding ;
patients under 18 years of age.

The drug should be taken with caution in the first days after a heart attack . Since the active components included in Zilt increase bleeding, it should not be prescribed to patients after surgery , severe injuries , or other pathological conditions . The same rule should be followed for patients with impaired renal function, ulcers , and liver failure.

Side effects

When using the drug, it is extremely rare that such general and specific side effects may occur from the nervous, respiratory, muscular, cardiovascular and autonomic systems, as well as the hematopoietic organs, gastrointestinal tract and senses such as:

chest pain;
hernia;
dizziness;
syncope;
hyperesthesia;
heart failure;
paresthesia;
headache;
peripheral edema;
dispersion;
vomit;
gastritis or ulcer;
hepatitis;
diarrhea;
anemia;
agranulocytosis;
neutropenia;
taste disturbance;
purpura;
epistaxis;
stomach bleeding;
intracranial hemorrhage;
hemothorax;
arthralgia;
arthrosis;
dyspnea;
pneumonia;
rhinitis;
sinusitis;
arthritis;
cystitis;
cataract;
hives;
conjunctivitis;
dermatitis;
eczema;
skin rash;
bleeding in the urinary tract;
bronchitis and cough.

In addition, when taking the drug Zilt, isolated cases of side effects such as membranous nephropathy, angioedema, anaphylactic shock, uremic syndrome , and bronchospasm .

Side effects of the drug Zilt

General reactions : chest pain, increased fatigue, asthenia. From the nervous system : headache, dizziness, paresthesia, leg cramps, hypoesthesia, neuralgia, loss of consciousness. From the cardiovascular system : peripheral edema, hypertension (arterial hypertension), heart failure, tachycardia. From the gastrointestinal tract : abdominal pain, dyspepsia, diarrhea, nausea, constipation, vomiting, flatulence, impaired taste, perforation of a stomach ulcer, hemorrhagic gastritis, gastrointestinal bleeding. From the liver and biliary tract : increased activity of liver transaminases, hyperbilirubinemia, hepatitis, liver steatosis. From the blood system : thrombocytopenia, anemia (aplastic or hypochromic), agranulocytosis, granulocytopenia, leukocytosis, leukopenia, neutropenia. From the blood coagulation system : nosebleeds, gastrointestinal bleeding, hemarthrosis, bleeding from the urinary tract, hemoptysis, intracranial hemorrhage, retroperitoneal bleeding, bleeding from a postoperative wound, hemorrhage in the eye, hemothorax, pulmonary hemorrhage, allergic purpura, thrombocytopenic purpura. From the musculoskeletal system: back pain, arthritis, arthrosis. From the central nervous system: depression. From the respiratory system : inflammation of the upper respiratory tract, shortness of breath, rhinitis, bronchitis, cough, pneumonia, sinusitis. Skin : rash, itching, eczema, skin ulcers, bullous dermatitis, erythematous rash, maculopapular rash, urticaria. From the senses : cataracts, conjunctivitis. From the genitourinary system : urinary tract infection, cystitis, hypermenorrhea, isolated cases of hemolytic uremic syndrome and membranous nephropathy. Allergic reactions: isolated cases of hypersensitivity reactions (angioedema, bronchospasm, anaphylaxis).

Zilt tablets, instructions for use (Method and dosage)

In accordance with the instructions for use of Zilt, the medicine is taken regardless of food intake in a dosage depending on the severity of the disease, the patient’s health condition and the doctor’s recommendations.

When treating the consequences of heart attacks and strokes, Zylt is taken one tablet (75 mg) once a day. For angina pectoris, coronary syndrome ST segment a elevation and infarction without Q wave, treatment begins with a single dose of the drug in the so-called loading dose, which is equal to 300 mg. Subsequently, the patient takes 75 mg. medicine. The course of treatment with the drug can reach 12 months, and a positive effect is observed by the third month of taking Zilt.

Patients with ST segment elevation heart attack are also recommended to take a loading dose in combination with acetylsalicylic acid , and then take 75 mg. drug daily. It is worth emphasizing that when treating patients over 75 years of age, the initial loading dose is not used.

Zyllt®

Anticoagulants for oral administration:

simultaneous use of clopidogrel and oral anticoagulants may increase the intensity of bleeding, and therefore the use of this combination is not recommended.

The use of clopidogrel at a dose of 75 mg per day does not change the pharmacokinetics of warfarin (a CYP2C9 isoenzyme substrate) or the international normalized ratio (INR) in patients receiving long-term treatment with warfarin. However, simultaneous use with warfarin increases the risk of bleeding due to its independent additional effect on blood clotting. Therefore, caution should be exercised when using warfarin and clopidogrel simultaneously.

Glycoprotein IIb/IIIa inhibitors:

simultaneous use of clopidogrel and glycoprotein IIb/IIIa inhibitors requires caution in patients with an increased risk of bleeding (in case of trauma, surgery or other pathological conditions) (see section "Special instructions").

Acetylsalicylic acid:

Acetylsalicylic acid does not affect clopidogrel-induced inhibition of ADP-induced platelet aggregation, but clopidogrel potentiates the effect of acetylsalicylic acid on collagen-induced platelet aggregation. However, simultaneous administration of 500 mg of acetylsalicylic acid twice daily for one day does not significantly prolong the bleeding time caused by taking clopidogrel. The pharmacodynamic interaction between clopidogrel and acetylsalicylic acid may lead to an increased risk of bleeding. Given this, caution should be exercised when taking these drugs concomitantly, although in clinical studies, patients received combination therapy with clopidogrel and acetylsalicylic acid for one year.

Heparin:

According to a clinical study in healthy individuals, when taking clopidogrel, no change in the dose of heparin was required, and the anticoagulant effect of heparin did not change. Concomitant use of heparin had no effect on the suppression of platelet aggregation by clopidogrel. There may be a pharmacodynamic interaction between clopidogrel and heparin, leading to an increased risk of bleeding. Therefore, the simultaneous use of these drugs requires caution.

Thrombolytics:

The safety of simultaneous use of clopidogrel, fibrin-specific or fibrin-specific thrombolytics and heparin was assessed in patients with acute myocardial infarction. The incidence of clinically significant bleeding was comparable to that with the simultaneous use of thrombolytics, heparin and acetylsalicylic acid.

Nonsteroidal anti-inflammatory drugs (NSAIDs):

According to a clinical study involving healthy volunteers, the simultaneous use of clopidogrel and naproxen increased occult gastrointestinal bleeding. However, due to the lack of interaction studies with other NSAIDs at this time, it is not known whether the risk of gastrointestinal bleeding is increased when used together with other NSAIDs. Therefore, simultaneous therapy with NSAIDs, including COX-2 inhibitors, and clopidogrel should be carried out with caution (see section "Special Instructions").

CYP2C19 isoenzyme inhibitors:

Clopidogrel is metabolized to the formation of its active metabolite, partly under the influence of the CYP2C19 isoenzyme. Therefore, drugs that inhibit this isoenzyme may cause a decrease in the concentration of the active metabolite of clopidogrel. The clinical significance of this interaction is unknown. Concomitant use with strong or moderate inhibitors of the CYP2C19 isoenzyme should be avoided. Inhibitors of the CYP2C19 isoenzyme include: omeprazole and esomeprazole, fluvoxamine, fluoxetine, moclobemide, voriconazole, fluconazole, ticlopidine, ciprofloxacin, cimetidine, carbamazepine, oxcarbazepine and chloramphenicol.

Proton pump inhibitors: p

The use of omeprazole at a dose of 80 mg once daily simultaneously with clopidogrel or with a 12-hour break between taking the two drugs reduced the systemic exposure (AUC) of the active metabolite of clopidogrel by 45% (after taking a loading dose of clopidogrel) and 40% (after taking a maintenance dose). clopidogrel dose). A decrease in the AUC of the active metabolite of clopidogrel is associated with a decrease in the degree of inhibition of platelet aggregation (39% after taking a loading dose of clopidogrel and 21% after taking a maintenance dose of clopidogrel). A similar interaction between clopidogrel and esomeprazole is expected. Observational and clinical studies have reported conflicting data on cardiovascular clinical manifestations regarding this pharmacokinetic/pharmacodynamic interaction. Concomitant use with omeprazole or esomeprazole should be avoided.

Proton pump inhibitors with minimal inhibitory effects on the CYP2C19 isoenzyme include pantoprazole and lansoprazole. With simultaneous use of pantoprazole at a dose of 80 mg once daily, a decrease in the concentration of the active metabolite of clopidogrel in the blood plasma was observed by 20% (after taking a loading dose of clopidogrel) and by 14% (after taking a maintenance dose of clopidogrel). This was accompanied by a decrease in the degree of inhibition of platelet aggregation by an average of 15% and 11%, respectively. Therefore, the simultaneous use of clopidogrel with pantoprazole is possible.

Other medicines

When studying the pharmacodynamic and pharmacokinetic interactions of clopidogrel and other drugs, the following was revealed:

— with simultaneous use of clopidogrel with atenolol and/or nifedipine, no clinically significant pharmacodynamic interaction was detected;

- the pharmacodynamic activity of clopidogrel did not change significantly when used simultaneously with phenobarbital, cimetidine or estrogens;

— the pharmacokinetics of digoxin or theophylline did not change;

- antacids do not affect the degree of absorption of clopidogrel;

- Phenytoin and tolbutamide can be safely used concomitantly with clopidogrel. It is unlikely that clopidogrel can affect the metabolism of other drugs, such as phenytoin and tolbutamide, as well as NSAIDs, which are metabolized by the CYP2C9 isoenzyme;

- diuretics, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors, slow calcium channel blockers, lipid-lowering agents, coronary vasodilators, hypoglycemic agents (including insulin), antiepileptic drugs, hormone replacement therapy: not identified in clinical studies clinically significant adverse interactions.

Interaction

Zylt is not recommended to be taken together with thrombolytic drugs, as well as Warfarin and Heparin clopidogrel , which is part of the drug, increases the risk of bleeding . The drug affects the effectiveness of acetylsalicylic acid .

For this reason, continuous combined treatment with the two drugs listed above should be carried out for a maximum of 12 months. The risk of developing peptic ulcers increases when taking Zylt together with anti-inflammatory drugs that do not contain steroids .

When taking the drug with Tolbutamine and Phenytoin, it is possible to increase the level of CY2C9 (cytochrome P450 enzyme) in the blood; in addition, Zilt inhibits the activity of this enzyme .

Drug interactions Zilt

Due to the increased risk of bleeding, simultaneous use of clopidogrel and warfarin is not recommended. When clopidogrel is used concomitantly with heparin or other thrombolytic agents, the risk of bleeding may increase, so the combined use of these drugs requires caution. The simultaneous use of clopidogrel and NSAIDs increases the risk of ulcerogenic effects and the development of bleeding from ulcers, so the use of clopidogrel with NSAIDs requires caution. With simultaneous use of clopidogrel with atenolol, nifedipine, digoxin, phenobarbital, cimetidine, estrogens or theophylline, no clinically significant interaction was observed. There is data on the safety of simultaneous use of clopidogrel with phenytoin and tolbutamide. Antacids do not affect the absorption of clopidogrel.

special instructions

The drug increases the duration of bleeding , so it should be prescribed with extreme caution to patients at risk of bleeding, for example, after surgery, trauma and other pathological conditions. of hemostasis as activity and platelet should be monitored .

This drug does not affect the ability to drive vehicles, nor does it reduce the reaction when working with potentially dangerous mechanisms or devices.

Overdose of the drug Zilt, symptoms and treatment

One case of an intentional overdose of clopidogrel has been described, when a 34-year-old woman with suicidal intent took 1050 mg (14 tablets) of clopidogrel. There were no symptoms of overdose or complications noted, no special treatment was performed. After healthy volunteers took 600 mg of clopidogrel, no side effects (except for a 1.7-fold increase in bleeding time) were noted. There is no specific antidote. The effects of clopidogrel can be reversed by platelet transfusion.

Zilta's analogs

Level 4 ATC code matches:
Persantine

Aegitromb

Plavix

Coplavix

Chime

Cardiomagnyl

Polocard

Thrombo ACC

Brilinta

Magnicor

Plagril

Dipyridamole

Clopidogrel

Lopirel

CardiASK

Aspirin Cardio

Acecardole

Aspinat

Aspicor

The main analogues of the drug Zilt include the following drugs:

Aggregal;
Dethromb;
Cardutol;
Clopidex;
Clopylet;
Listab 75;
Deplatt-75;
Cardogrel;
Clopigrant;
Clopidogrel;
Lirta;
Plavix;
Targetek;
Lopirel;
Plagril;
Aegitromb;
Trocken;
Plogrel;
Trombex.

It is also noteworthy that the price of Zilt analogues is sometimes several times higher or, conversely, lower than the cost of the original drug.

Zylt or Plavix which is better?

Quite often the question of the effectiveness of both drugs is raised on forums. Some patients and doctors are of the opinion that Zylt is at least 10% less effective than Plavix. Others argue that both drugs have the same effect because they have an identical chemical composition, but Plavix costs almost twice as much as its competing analogue.

Zylta price, where to buy

The cost of the drug depends on the region, but on average the price of Zilt (75 mg, 14 tablets) is in the range of 550-600 rubles.

Online pharmacies in RussiaRussia
Online pharmacies in KazakhstanKazakhstan

ZdravCity

Zylt tablets p.p.o.
75 mg 84 pcs. Krka-Rus LLC RUB 1,753 order
Zylt tablets p.p.o. 75 mg 28 pcs. Krka-Rus LLC
960 rub. order

Pharmacy Dialogue

Zilt tablets 75 mg No. 84KRKA-RUS
RUB 1,947 order
Zilt tablets 75mg No. 28KRKA-RUS
RUB 1,036 order