What is Clopidogrel? Investigation of side effects and uses of clopidogrel

Clopidogrel is a well-known antiplatelet drug that is used as one of the main tools in preventing the formation of blood clots and closing blood vessels. This drug thins the blood by inhibiting the function of platelets and minimizes the possibility of blockage of blood vessels. As a result, for people who are at risk of developing cardiovascular diseases, this drug is proposed as an important treatment choice. In this article, we intend to do a more detailed analysis of the drug clopidogrel and its uses in the prevention of cardiovascular diseases.

Clopidogrel dosage forms

Clopidogrel is available in tablet form of 75 mg and 300 mg, which is prescribed by the doctor depending on the type of disease. Other similar drugs from the family of clopidogrel include Osix 75 mg tablets, Zyllt 75 mg tablets and clopidogrel 75 mg tablets. This drug is produced and marketed in Iran under the license of Obedi Company.

Uses of clopidogrel tablets

Clopidogrel is used to prevent heart attacks and strokes in people with heart disease (recent heart attack), recent stroke, or circulatory disease (peripheral vascular disease). It is also used with aspirin to treat new or worsening chest pain (new heart attack). This drug is used for unstable angina and to keep blood vessels open and prevent blood clotting after certain procedures (such as cardiac stenting).

Some of the most important uses of this drug are acute coronary syndrome, heart attack, stroke or recently developed peripheral arterial disease, coronary artery disease, embolic heart attack, carotid artery stenting, etc.

Uses of clopidogrel tablets in adults

1. Acute coronary syndrome
2. heart attack
3. Recent stroke or peripheral arterial disease
4. Coronary Artery Disease
5. embolic heart attack
6. Carotid artery stenting

Pharmacological effects and mechanism of action of clopidogrel drug

The mechanism of action of clopidogrel is to inhibit the adenosine diphosphate (ADP)-induced pathway for platelet aggregation. This drug is metabolized in the liver by hepatic CYP450 enzymes (in vitro by CYP3A4, CYP2C19 [عمدتاً]others) to produce active metabolite and also by esterase to produce inactive metabolite.

thiol (active); Further activation of the thiol metabolite via hydrolysis is required via paraoxonase-1 (PON-1). Allelic variations of PON-1 may inhibit activation and increase the risk of stent thrombosis. Finally, this drug is excreted through urine (50%) and feces (46%).

Dosage of clopidogrel

Take this medication orally with or without food as directed by your doctor, usually once a day. Take clopidogrel tablets as prescribed by your doctor to get the most out of it. The dose and length of treatment is based on your medical condition and your response to treatment. If you are taking this medicine to prevent blood clots after stent implantation or other procedures, you should take it along with aspirin for several months to years after the procedure (depending on the procedure and type of stent) as directed by your doctor. Consult your doctor for more details and risks of premature discontinuation.

Dosage of clopidogrel tablets in acute coronary syndrome

1. Dosage in myocardial infarction without fragments and unstable angina: the loading dose is 300 mg, and starting the treatment without the loading dose delays the antiplatelet effect for several days. After loading dose, 75 mg/day PO for up to 12 months.
2. In some patients, more than 12 months may be prescribed if used together with aspirin (75-100 mg per day).
3. Long-term combination therapy with aspirin after stent placement depends on how the patient tolerates long-term dual antiplatelet therapy (DAPT), whether the patient has stable coronary artery disease, and risk factors (eg, TIA or stroke). ) is prescribed.
4. The dosage for people younger than 75 years is 300 mg and then 75 mg for 14 days to 12 months (if there is no bleeding). In case of simultaneous treatment with aspirin, 325-75 mg per day should be prescribed with or without thrombolytics.
5. In people over 75 years old, there is no loading dose and 75 mg is prescribed for 14 days to 12 months (if there is no bleeding).

Dosage of clopidogrel tablets in adults

1. For the treatment of recent myocardial infarction, stroke, or peripheral arterial disease, 75 mg daily without a loading dose; It is recommended as an alternative to aspirin or at the same time as aspirin.
2. The recommended dosage for coronary artery disease is 75 mg per day.
3. Carotid artery stenting, 300 mg plus aspirin 325-81 mg for 1 dose daily before carotid artery stenting (CAS), then 75 mg daily plus aspirin 325-81 mg daily for at least 30 days To be consumed after CAS.

Time to take clopidogrel tablets

If the disease improves and you feel better, do not stop taking this medicine without consulting your doctor. Also, avoid eating grapefruit (a type of fruit) or drinking grapefruit juice while using this medicine. Grapefruit can increase the possibility of side effects of this drug. If you still have symptoms like a heart attack or a new stroke after taking the medicine (such as pain in the chest, jaw, left arm, shortness of breath, unusual sweating, weakness on one side of the body, difficulty speaking, sudden changes in vision, confusion, etc.) See a doctor.

Precautions

Before taking clopidogrel, if you are allergic to it or other similar antiplatelet drugs (thinopyridines such as prasugrel), avoid taking the drug. Before taking the drug, inform the doctor of your medical history, such as bleeding conditions (stomach ulcer, bleeding in the brain or eyes), recent surgery, serious injury or trauma, liver disease, bleeding disease (such as hemophilia), etc.

This product may contain inactive ingredients that can cause allergic reactions or sensitivities. To reduce the chance of cuts, bruises, or injury, use caution with sharp objects such as razors and avoid activities such as contact sports.

1. Use with caution in patients with bleeding or platelet disorders.
2. Early termination increases the risk of cardiovascular events. Discontinue 5 days before surgery that has a high risk of bleeding.
3. Use caution in patients with atrial fibrillation, carefully assess bleeding risk.
4. There is a risk of bleeding with potentially fatal consequences, liver or kidney failure in patients.
5. Allergic cross-reaction including rash, angioedema, or hematologic reaction has been reported among thienopyridines (eg, ticlopidine, prasugrel). Before taking the drug, evaluate the patient for history of hypersensitivity.
6. Early discontinuation of therapy may lead to stent thrombosis with fatal and non-fatal myocardial infarction. The duration of treatment should be determined based on the type of stent placed.
7. P2Y12 inhibitors (thinopyridines), including clopidogrel, inhibit platelet aggregation during the platelet lifetime (7-10 days). Because the half-life of the active metabolite of clopidogrel is short, it may be possible to restore homeostasis by administering exogenous platelets. However, platelet transfusions within 4 hours of a loading dose or 2 hours after a maintenance dose are less effective.
8. It increases the risk of major bleeding in patients with lacunar stroke.

Clopidogrel contraindications

1. Hypersensitivity
2. Pregnant women (only with doctor’s prescription)
3. Active pathological bleeding (eg peptic ulcer, intracranial bleeding)

Clopidogrel side effects

Easy bleeding or bruising, discomfort or stomach pain, diarrhea and constipation are some of the side effects of clopidogrel tablets. If any of these effects persist or worsen, tell your doctor or pharmacist right away. Some serious side effects of this drug include severe stomach or abdominal pain, uncontrolled bleeding from the gums or nose, bloody or black stools, confusion, fever, severe pale skin, purple spots on the skin, fainting, fast heartbeat, sudden severe headache. , unusual weakness or fatigue, vomiting with blood or that looks like coffee grounds, difficulty speaking, changes in vision, seizures, yellowing of the eyes and skin, bloody urine (red, pink, and dark), signs of kidney problems (such as changes in the amount of urine) . If any of these occur, see a doctor.

1. Upper respiratory tract infection
2. Chest pain
3. Headache
4. Influenza syndrome
5. Arthralgia
6. the pain
7. dizziness
8. diarrhea
9. rush
10. rhinitis
11. depression
12. UTI

Clopidogrel drug interactions

Before going to the doctor, patients should prepare a list of their chemical and herbal medicines and show it to the doctor. According to the drugs you use, the doctor should prescribe drugs that do not cause interactions and side effects. Some medicines can affect how clopidogrel is removed from your body, which may affect how it works. Certain acid reducing drugs (proton pump inhibitors/PPI such as omeprazole, esomeprazole), cimetidine, etravirine, felbamate, fluconazole, fluoxetine, fluvoxamine, ketoconazole, rifampin, ticlopidine, voriconazole are among these.

1. Class X drug interactions (avoidance): rimepanet, pazopanib, topotecan, urokinase, amodiaquine
2. Decreased effects of clopidogrel by drugs: calcium channel blockers, cangrelor, strong and moderate CYP2C19 inhibitors, erythromycin (systemic), omeprazole, etravirine, fentanyl, fluvoxamine, grapefruit juice, lansoprazole, omeprazole, pantoprazole, ritonavir, amiodarone
3. Increased effects of drugs by clopidogrel: drugs with anti-platelet properties, alplizib, ombitasvir, paritapravir, ritonavir, dasabuvir, ozanimod, paclitaxel (common dosage form and protein-bound dosage form), pazopanib, pioglitazone, repaglinide, rimagpent, bemiparin, bupropion, cephalothin , cladribine, collagenase (systemic), dabigatran etexilate, dabrafenib, dasabuvir, deoxycholic acid, desloratadine

Taking clopidogrel tablets (ibuprofen) during pregnancy and breastfeeding

Available data from two decades of case reports and post-marketing surveillance have not identified any drug-related risk for birth defects or miscarriage. There are only risks for pregnant women and the fetus in connection with myocardial infarction and stroke. Myocardial infarction and stroke are medical emergencies that should not be withheld from pregnant women due to potential concerns about the effects of clopidogrel on the fetus. Delay treatment with this medicine 5 to 7 days before delivery. Because this product increases the risk of bleeding during childbirth, which can be dangerous.

The effect of clopidogrel on breastfeeding

There is no information on the presence of the drug in human milk or its effects on milk production. In a small number of post-marketing cases, no adverse effects on breastfed infants were observed. When a drug is present in animal milk (animal tests), it is likely that the drug is also present in human milk. Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for treatment and any possible adverse effects on the infant from medication or the mother’s underlying disease.

Storage conditions for clopidogrel tablets

Clopidogrel tablets should be stored at room temperature away from light and moisture. Different medicines should also be kept out of the reach of children and animals.

The last words of clopidogrel tablets

Clopidogrel has been approved as one of the key tools in the prevention of cardiovascular diseases. This drug offers people who are at risk of developing these types of diseases an important opportunity to improve their heart health. The drug introduced in the online pharmacy magazine Positive Green has side effects such as upper respiratory tract infection, chest pain, headache, influenza syndrome, arthralgia, diarrhea, dizziness and pain, etc., which should be taken with caution and in the right amount with a doctor’s prescription.

Site source: Medscape