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Clopidogrel

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2019-09-19
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Clinical Pharmacology

Antiplatelet. Clopidogrel is a prodrug, one of the active metabolites of which is an inhibitor of platelet aggregation. The active metabolite of clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to the P2Y12 platelet receptor and the subsequent ADP-mediated activation of the GPIIb / IIIa complex, leading to the suppression of platelet aggregation. Due to irreversible binding, platelets remain insensitive to stimulation of ADP for the remainder of their life (approximately 7-10 days), and restoration of the normal function of platelets occurs at a rate corresponding to the rate of platelet renewal. Platelet aggregation, caused by agonists other than ADP, is also inhibited due to the blockade of enhanced activation of platelets released by ADP. Since the formation of an active metabolite occurs with the help of isoenzymes of the P450 system, some of which may differ in polymorphism or may be inhibited by other drugs, not all patients can adequately suppress platelets.

Clopidogrel is able to prevent the development of atherothrombosis in any localization of atherosclerotic vascular lesions, in particular in cases of cerebral, coronary or peripheral arteries.

With daily use of clopidogrel in a dose of 75 mg from the first day of administration, a significant suppression of ADP-induced platelet aggregation is noted, which gradually increases over 3-7 days and then goes to a constant level (when an equilibrium state is reached). In equilibrium, platelet aggregation is suppressed on average by 40-60%. After discontinuation of clopidogrel, platelet aggregation and bleeding time gradually return to the initial level on average within 5 days.

Indications

Prevention of atherothrombotic events in patients after myocardial infarction (with prescription from several days to 35 days), ischemic stroke (with prescription from 7 days to 6 months) or having diagnosed peripheral arterial occlusive disease.

Prevention of atherothrombotic events (in combination with acetylsalicylic acid) in patients with acute coronary syndrome:

- without ST segment elevation (unstable angina or myocardial infarction without a Q wave), including patients who underwent stenting for percutaneous coronary intervention;

- With the rise of the ST segment (acute myocardial infarction) with medical treatment and the possibility of thrombolysis.

Composition

1 tab. - clopidogrel (in the form of hydrogensulfate or bisulfate) 75 mg.
Excipients: lactose monohydrate (milk sugar) - 38.4 mg, microcrystalline cellulose - 129.48 mg, croscarmellose sodium (primelloza) - 12 mg, colloidal silicon dioxide (aerosil) - 3.12 mg, sodium stearyl fumarate - 2 mg.

The composition of the shell: Opadry II - 8 mg (polyvinyl alcohol, partially hydrolyzed - 3.52 mg, talc - 1.6 mg, titanium dioxide (E171) - 1.5336 mg, macrogol (polyethylene glycol 3350) - 0.988 mg, soy lecithin (E322) - 0.28 mg, dye-based aluminum lacquer azorubine - 0.0408 mg, crimson-based aluminum lacquer dye [Ponso 4R] - 0.0328 mg, aluminum lacquer based on indigo carmine dye - 0.0048 mg).

Clopidogrel is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Clopidogrel-SZ pills
Plavix Sanofi-aventis France pills
Clopidogrel-SZ North Star Russia pills
Clopidogrel Izvarino Pharma Russia pills
Deplatt-75 Torrent India pills
Clopidex Belupo Croatia pills
Plagril Dr. Reddy`s India pills
Clopidogrel-Teva Teva Israel, Israel, Russia pills
Zylt Krka dd Novo mesto AO Slovenia pills
Lopirel Actavis Ltd Iceland pills
Clopidogrel Canonpharma Russia pills
Egitromb Egis Hungary pills

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Clopidogrel

Dosage and Administration

Adults and elderly patients with normal activity of isoenzyme CYP2C19

Clopidogrel-SZ should be taken orally, regardless of the meal.

Myocardial infarction, ischemic stroke and diagnosed peripheral arterial occlusive disease

The drug is taken at 75 mg 1 time / day.

In patients with myocardial infarction (MI), treatment can be started from the first days to 35 days of MI, and in patients with ischemic stroke (AI), from 7 days to 6 months after AI.

Acute coronary syndrome without ST segment elevation (unstable stenocardia, myocardial infarction without Q wave)

Treatment with Clopidogrel-SZ should begin with a single dose of a loading dose of 300 mg, and then continued at a dose of 75 mg 1 time / day (in combination with acetylsalicylic acid as an antiplatelet agent at doses of 75-325 mg / day). Since the use of acetylsalicylic acid in higher doses is associated with an increased risk of bleeding, the dose of acetylsalicylic acid recommended for this indication should not exceed 100 mg. The maximum therapeutic effect is observed by the third month of treatment. The course of treatment is up to 1 year.

Acute coronary syndrome with ST segment elevation (acute myocardial infarction with ST segment elevation)

Clopidogrel is prescribed in a dose of 75 mg 1 time / day with an initial single dose of a loading dose in combination with acetylsalicylic acid as an antiplatelet agent and thrombolytic agents (or without thrombolytic agents). Combination therapy is started as soon as possible after the onset of symptoms and continues for at least 4 weeks. In patients over the age of 75, treatment with Clopidogrel-SZ should be started without taking a loading dose.

Patients with a genetically determined reduction in the function of the isoenzyme CYP2C19

The weakening of metabolism using CYP2C19 isoenzyme can lead to a decrease in the antiplatelet effect of clopidogrel. The optimal dosing regimen for patients with a weakened metabolism using the CYP2C19 isoenzyme has not yet been established.

After repeated administration of the drug Clopidogrel-SZ at a dose of 75 mg / day inpatients with severe kidney damage (CC from 5 to 15 ml / min) Inhibition of ADP-induced platelet aggregation (25%) was lower compared to that in healthy volunteers, however, the lengthening of bleeding time was similar to that in healthy volunteers who received Clopidogrel-SZ at a dose of 75 mg / day. In addition, all patients had good tolerability.

After taking clopidogrel-SZ in the dose of 75 mg daily for 10 dayspatients with severe liver damageinhibition of ADP-induced platelet aggregation was similar to that in healthy volunteers. The average bleeding time was also comparable in both groups.

The prevalence of alleles of the CYP2C19 isoenzyme genes, which are responsible for the intermediate and reduced metabolism of clopidogrel to its active metabolite, differs among members of different ethnic groups. Only limited data are available for representatives of the Mongoloid race to assess the effect of the CYP2C19 isoenzyme genotype on clinical outcomes.

Adverse reactions

Classification of the incidence of side effects (WHO): often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10 000 and <1/1000), very rarely (<1/10 000).

From the central and peripheral nervous system: infrequently - headache, dizziness and paresthesia; rarely - vertigo; very rarely - a violation of taste.

Mental disorders: very rarely - confusion, hallucinations.

Since the cardiovascular system: very rarely - vasculitis, marked reduction in blood pressure, intracranial hemorrhage, eye hemorrhages (conjunctival, in the tissue and retina), hematoma, nosebleeds, bleeding from the respiratory tract, gastrointestinal bleeding, retroperitoneal hemorrhage outcome, hemorrhages in the muscles and joints, hematuria.

On the part of the respiratory system: very rarely - bronchospasm, interstitial pneumonitis.

On the part of the digestive system: often - diarrhea, abdominal pain, dyspepsia; infrequently - gastric and duodenal ulcers, gastritis, vomiting, nausea, constipation, flatulence; very rarely - pancreatitis, colitis (including ulcerative or lymphocytic colitis), stomatitis, acute liver failure, hepatitis.

On the part of the urinary system: very rarely - glomerulonephritis.

On the part of the blood coagulation system: infrequently - prolonged bleeding time.

From the hematopoietic system: infrequently - thrombocytopenia, leukopenia, neutropenia and eosinophilia; very rarely - thrombocytopenic thrombohemolytic purpura, severe thrombocytopenia (platelet count ≤ 30 × 109/ l), agranulocytosis, granulocytopenia, aplastic anemia (pancytopenia), anemia.

From the skin and subcutaneous tissues: infrequently - skin rash and itching; very rarely - angioedema, urticaria, erythematous rash (associated with clopidogrel or acetylsalicylic acid); very rarely - bullous dermatitis (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), eczema and lichen planus.

On the part of the musculoskeletal system: very rarely - arthralgia, arthritis, myalgia.

On the part of the immune system: very rarely - anaphylactoid reactions, serum sickness.

From the laboratory parameters: very rarely - changes in liver function tests, an increase in serum creatinine concentration.

Other: very rarely - fever.

Contraindications

- severe liver failure;

- acute bleeding (for example, bleeding from a peptic ulcer or intracranial hemorrhage);

- rare hereditary lactose intolerance, lactase deficiency and glucose-galactose malabsorption;

- pregnancy;

- lactation period;

- children's and teenage age till 18 years (safety and efficiency of use are not established);

- Hypersensitivity to clopidogrel or any of the excipients of the drug.

Carefully:

- moderate hepatic impairment, in which a predisposition to bleeding is possible (limited clinical experience of use);

- renal failure (limited clinical experience of use);

- trauma, surgery;

- Diseases in which there is a predisposition to the development of bleeding (especially gastrointestinal or intraocular);

- simultaneous administration of nonsteroidal anti-inflammatory drugs, incl. selective COX-2 inhibitors;

- simultaneous use of warfarin, heparin, glycoprotein IIb / IIIa inhibitors;

- in patients with a genetically determined decrease in the function of the isoenzyme CYP2C19 in recommended doses (there are literature data indicating that patients with a genetically determined decrease in the function of the isoenzyme CYP2C19 are exposed to a lower systemic exposure to the active metabolite of clopidogrel and have a less pronounced effect of the drug, in addition they may there is a higher incidence of cardiovascular complications after myocardial infarction compared with patients with normal function of the isoenzyme CYP2C19).

Drug interactions

Warfarin

Simultaneous use with clopidogrel can increase the intensity of bleeding, so the use of this combination is not recommended.

IIb / IIIa receptor blockers

The use of IIb / IIIa receptor blockers in conjunction with clopidogrel requires caution in patients who have an increased risk of bleeding (for injuries and surgical interventions or other pathological conditions).

Acetylsalicylic acid

Acetylsalicylic acid does not alter the effect of clopidogrel, which inhibits ADP-induced platelet aggregation, but clopidogrel potentiates the effect of acetylsalicylic acid on collagen-induced platelet aggregation.However, the simultaneous use of acetylsalicylic acid as an antipyretic with 500 mg of clopidogrel 2 times a day for 1 day did not cause a significant increase in the bleeding time caused by the use of clopidogrel. Between clopidogrel and acetylsalicylic acid pharmacodynamic interaction is possible, which leads to increased risk of bleeding. Therefore, with their simultaneous use, caution should be exercised, although in clinical studies, patients received combination therapy with clopidogrel and acetylsalicylic acid for up to one year.

Heparin

According to a clinical study conducted with the participation of healthy volunteers, taking clopidogrel did not require a change in the dose of heparin and its anticoagulant effect did not change. The simultaneous use of heparin did not alter the antiplatelet effect of clopidogrel. Between clopidogrel and heparin, pharmacodynamic interaction is possible, which may increase the risk of bleeding, therefore the simultaneous use of these drugs requires caution.

Thrombolytic

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

NSAIDs

In a clinical study conducted with the participation of healthy volunteers, the simultaneous 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, it is currently unknown if there is an increased risk of gastrointestinal bleeding when taking clopidogrel along with other NSAIDs. Therefore, the appointment of NSAIDs, incl. selective inhibitors of COX-2, in combination with clopidogrel should be carried out with caution.

Other combination therapy

Since Clopidogrel is metabolized before the formation of its active metabolite using CYP2C19 isoenzyme, the use of drugs that inhibit this system can lead to a decrease in the concentration of the active metabolite of clopidogrel and a decrease in its clinical efficacy. Simultaneous administration of drugs inhibiting CYP2C19 isoenzyme (for example, omeprazole) is not recommended.

A number of clinical studies were conducted with clopidogrel and other concomitantly prescribed drugs in order to study possible pharmacodynamic and pharmacokinetic interactions, which showed that:

- when using clopidogrel together with atenolol, nifedipine or with both drugs at the same time, no clinically significant pharmacodynamic interaction was observed;

- simultaneous use of phenobarbital, cimetidine and estrogen had no significant effect on clopidogrel pharmacodynamics;

- pharmacokinetic indices of digoxin and theophylline did not change when they were applied simultaneously with clopidogrel;

- antiacid means did not reduce clopidogrel absorption;

- Phenytoin and tolbutamide can be safely applied simultaneously with clopidogrel, despite the fact that data obtained from human liver microsome studies suggest that the carboxyl metabolite of clopidogrel may inhibit the activity of the CYP2C9 isoenzyme, which can lead to an increase in plasma concentrations drugs (phenytoin, tolbutamide and some NSAIDs) that are metabolized by the isoenzyme CYP2C9;

- ACE inhibitors, diuretics, beta-blockers, slow calcium channel blockers, hypoglycemic agents (includinginsulin), lipid-lowering drugs, anti-epileptic drugs, HRT and GP IIb / IIIa receptor blockers — in clinical studies, no clinically significant undesirable interactions were found.

Pregnancy and Lactation

As a precautionary measure, it is not recommended to use clopidogrel during pregnancy due to the lack of clinical data on its use in pregnant women, although animal studies have not revealed either direct or indirect adverse effects on the course of pregnancy, embryonic development, childbirth and postnatal development.

Breastfeeding in the case of treatment with clopidogrel should be discontinued, because studies on rats have shown that clopidogrel and / or its metabolites are excreted in breast milk. Whether clopidogrel penetrates human breast milk is unknown.

Special instructions

In the treatment with Clopidogrel-SZ, especially during the first weeks of therapy and / or after invasive cardiac procedures / surgery, it is necessary to carefully monitor patients to exclude signs of bleeding, including and hidden.

Due to the risk of bleeding and hematological undesirable effects, if clinical symptoms that are suspicious of bleeding occur during the treatment, a clinical blood test should be urgently performed, the APTT, platelet count, indicators of the functional activity of platelets and other necessary studies should be determined.

Clopidogrel-SZ, as well as other antiplatelet drugs, should be used with caution in patients with an increased risk of bleeding associated with injuries, surgical interventions or other pathological conditions, as well as in patients receiving acetylsalicylic acid, NSAIDs, including COX-2 inhibitors, heparin or glycoprotein IIb / IIIa inhibitors.

The combined use of clopidogrel with warfarin can increase the intensity of bleeding, therefore, with the exception of special rare clinical situations (such as the presence of a floating thrombus in the left ventricle, stenting in patients with atrial fibrillation), the combined use of clopidogrel and warfarin is not recommended.

If the patient has a planned surgical intervention, and there is no need for an antiplatelet effect, then 7 days before the operation, the use of the drug Clopidogrel-SZ should be stopped.

Clopidogrel prolongs bleeding time and should be used with caution in patients with diseases that predispose to the development of bleeding (especially gastrointestinal and intraocular).

Patients should be warned that when using the drug Clopidogrel-SZ (alone or in combination with acetylsalicylic acid), it may take longer to stop the bleeding, and also that if they develop unusual (by localization or duration) bleeding should report this to your doctor. Before any forthcoming surgery and before the start of taking any new drug, patients should be informed to the doctor (including the dentist) about taking the drug Clopidogrel-SZ.

Very rarely, after the use of the drug Clopidogrel-SZ (sometimes even briefly) there have been cases of thrombocytopenic thrombohemolytic purpura (THP), which is characterized by thrombocytopenia and microangiopathic hemolytic anemia, accompanied by neurological disorders, impaired kidney function and fever. TBD is a potentially life-threatening condition that requires immediate treatment, including plasmapheresis.

During treatment, it is necessary to control the functional activity of the liver. In severe liver dysfunction, the risk of hemorrhagic diathesis should be kept in mind.

The use of the drug Clopidogrel-SZ is not recommended for acute stroke with a prescription of less than 7 days (since there are no data on its use in this state).

Clopidogrel-SZ should not be taken in patients with rare hereditary galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome.

Influence on ability to drive motor transport and control mechanisms

Clopidogrel-SZ does not have a significant impact on the ability to drive vehicles or work with machinery.

Overdosage

Symptoms: lengthening of bleeding time with subsequent complications in the form of bleeding.

Treatment: stop bleeding, platelet transfusions. The antidote is unknown.

  • Brand name: Clopidogrel-SZ
  • Active ingredient: Clopidogrel
  • Dosage form: pills, film coated from pink to dark pink, round, biconvex.
  • Manufacturer: Canonpharma

Studies and clinical trials of Clopidogrel (Click to expand)

  1. Combination therapy with clopidogrel and aspirin after coronary stenting
  2. Highly Efficient Chemoenzymatic Synthesis of Methyl (R)-o-Chloromandelate, a Key Intermediate for Clopidogrel, via Asymmetric Reduction with Recombinant Escherichia coli
  3. Immune heparin-induced thrombocytopenia can occur in patients receiving clopidogrel and aspirin
  4. Clopidogrel-associated thrombotic thrombocytopenic purpura presenting with coronary artery thrombosis
  5. Laboratory evaluation of clopidogrel responsiveness by platelet function and genetic methods
  6. Randomized clinical trial of the antiplatelet effects of aspirin–clopidogrel combination versus aspirin alone after lower limb angioplasty
  7. Clopidogrel: review of bioanalytical methods, pharmacokinetics/pharmacodynamics, and update on recent trends in drug–drug interaction studies
  8. Clopidogrel: review of bioanalytical methods, pharmacokinetics/pharmacodynamics, and update on recent trends in drug-drug interaction studies
  9. Sensitivity enhancement and matrix effect evaluation during summation of multiple transition pairs—case studies of clopidogrel and ramiprilat
  10. Influence of number of calibration standards within a defined range on pharmacokinetic disposition—case studies with omeprazole and clopidogrel carboxylic acid
  11. Validated HPLC method for determination of carboxylic acid metabolite of clopidogrel in human plasma and its application to a pharmacokinetic study
  12. Interaction study of aspirin or clopidogrel on pharmacokinetics of donepezil hydrochloride in rats by HPLC-fluorescence detection
  13. Determination of clopidogrel in human plasma by liquid chromatography/tandem mass spectrometry: application to a clinical pharmacokinetic study
  14. Clopidogrel therapy in patients undergoing coronary stenting: Value of a high-loading-dose regimen
  15. Impact of angina class on inhibition of platelet aggregation following clopidogrel loading in patients undergoing coronary intervention: Do we need more aggressive dosing regimens in unstable angina?
  16. Late stent thrombosis (> 1 year) following clopidogrel withdrawal after brachytherapy treatment: Need to assess aspirin resistance?
  17. Clopidogrel-associated autoimmune thrombocytopenic purpura
  18. Efficacy of clopidogrel in the treatment of post-ASD closure migraines
  19. Clopidogrel resistance
  20. Closure devices and vascular complications among percutaneous coronary intervention patients receiving enoxaparin, glycoprotein IIb/IIIa inhibitors, and clopidogrel
  21. Clopidogrel (Plavix) desensitization: A case series
  22. What is the best measure of thrombotic risks—pretreatment platelet aggregation, clopidogrel responsiveness, or posttreatment platelet aggregation?
  23. Clopidogrel (Plavix) desensitization protocol

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