Clopinol

Clopinol Uses, Dosage, Side Effects, Food Interaction and all others data.

(Clopinol) is an inhibitor of platelet aggregation. Lopirel (Clopinol) selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation.

Clopinol is a prodrug of a platelet inhibitor used to reduce the risk of myocardial infarction and stroke. It has a long duration of action as it is taken once daily and a large therapeutic window as it is given in doses of 75-300mg daily.

Trade Name Clopinol
Availability Prescription only
Generic Clopidogrel
Clopidogrel Other Names Clopidogrel, Clopidogrelum
Related Drugs aspirin, lisinopril, metoprolol, propranolol, Xarelto, Plavix, Brilinta, enoxaparin, rivaroxaban, pravastatin
Type Tablet
Formula C16H16ClNO2S
Weight Average: 321.822
Monoisotopic: 321.059027158
Protein binding

Both the active and inactive metabolites of clopidogrel are 98% protein bound in plasma. Studies in cows show clopidogrel 71-85.5% bound to serum albumin.

Groups Approved
Therapeutic Class Anti-platelet drugs
Manufacturer Knoll Healthcare Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Clopinol
Clopinol

Uses

(Clopinol) is used for the reduction of atherosclerotic events (myocardial infarction, ischaemic stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease.

Clopinol is also used to associated treatment for these conditions: Acute Coronary Syndrome (ACS), Acute Myocardial Infarction (AMI), Cardiovascular Events, Atherothrombotic events

How Clopinol works

Clopinol is metabolized to its active form by carboxylesterase-1. The active form is a platelet inhibitor that irreversibly binds to P2Y12 ADP receptors on platelets. This binding prevents ADP binding to P2Y12 receptors, activation of the glycoprotein GPIIb/IIIa complex, and platelet aggregation.

Dosage

Clopinol dosage

The recommended dose of Lopirel (Clopinol) is 75 mg once daily with or without food.

Side Effects

Generally Clopinol is well tolerated. However, a few common side effects i.e. Influenza-like symptoms, headache, upper respiratory tract infection, dizziness, muscle and back pain, and rash may occur.

Toxicity

A single dose of clopidogrel at 1500-2000mg/kg was lethal to mice and rats while 3000mg/kg was lethal to baboons. Symptoms of overdose include vomiting, breathing difficulty, gastrointestinal hemorrhage, and prostration. Clopinol is irreversibly bound to platelets for their lifetime, which is approximately 11 days. Overdoses of clopidogrel can be treated with platelet transfusions to restore clotting ability.

Precaution

As with other anti-platelet agents, Clopinol should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery, or other pathological conditions. Clopinol should be discontinued 7 days prior to surgery. Clopinol should be used with caution in hepatically impaired patients who may have bleeding diatheses.

Interaction

Concomitant use of Heparin, Warfarin and NSAIDs with Clopinol should be undertaken with caution. Clopinol potentiate the effect of Aspirin on collagen-induced platelet aggregation. The safety of chronic concomitant administration of Aspirin and Clopinol has not been established.

Food Interaction

  • Take with or without food.

Volume of Distribution

The apparent volume of distribution of clopidogrel is 39,240±33,520L.

Elimination Route

A 75mg oral dose of clopidogrel is 50% absorbed from the intestine. Clopinol can be taken with or without food. A meal decreases the AUC of the active metabolite by 57%. The active metabolite of clopidogrel reaches a maximum concentration after 30-60 minutes. Clopinol reached a Cmax of 2.04±2.0ng/mL in 1.40±1.07h.

The AUC for a 300mg oral dose of clopidogrel was 45.1±16.2ng*h/mL for poor metabolizers, 65.6±19.1ng*h/mL for intermediate metabolizers, and 104.3±57.3ng*h/mL for extensive metabolizers. The Cmax was 31.3±13ng/mL for poor metabolizers, 43.9±14ng/mL for intermediate metabolizers, and 60.8±34.3ng/mL for extensive metabolizers.

Half Life

That half life of clopidogrel is approximately 6 hours following a 75mg oral dose while the half life of the active metabolite is approximately 30 minutes.

Clearance

The clearance of a 75mg oral dose was 18,960±15,890L/h and for a 300mg oral dose was 16,980±10,410L/h.

Elimination Route

An oral dose of radiolabelled clopidogrel is excreted 50% in the urine and 46% in the feces over 5 days. The remainder of clopidogrel is irreversibly bound to platelets for their lifetime, or approximately 8-11 days.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies of Clopinol in pregnant women. However, Clopinol should be used during pregnancy only if clearly needed.

Lactation: Clopinol is not recommended for use while breast-feeding. It is not known for sure whether Clopinol is excreted in breast milk, although it is suspected that it is.

Contraindication

Clopinol is contraindicated in patients with a hypersensitivity to the drug substance or any component of the product, and those with active pathological bleeding such as peptic ulcer or intracranial hemorrhage.

Special Warning

Use in children: Safety and effectiveness of Clopinol in pediatric population have not been established.

Acute Overdose

In the event of over dosage no adverse effects were reported and no therapy was substituted.

Symptoms: Prolonged bleeding time and subsequent bleeding complications.

Management: May restore clotting ability with platelet transfusion.

Storage Condition

Store at 25° C.

Innovators Monograph

You find simplified version here Clopinol

Clopinol contains Clopidogrel see full prescribing information from innovator Clopinol Monograph, Clopinol MSDS, Clopinol FDA label

FAQ

What is Clopinol used for?

Clopinol is an antiplatelet medication used to reduce the risk of heart disease and stroke in those at high risk. It is also used together with aspirin in heart attacks and following the placement of a coronary artery stent. It prevents platelets from sticking together and forming a dangerous blood clot. Taking Clopinol helps prevent blood clots if you have an increased risk of having them.


How safe is Clopinol?

Clopinol is generally safe to take for a long time. In fact, it works best if you take it for many months or even years. If you're at risk of getting a stomach ulcer, your doctor may prescribe a medicine to help protect your stomach while you're taking Clopinol.

how does Clopinol work?

Clopinol slows the blood's clotting action by making platelets less sticky. Platelets are blood cells that stick together to block cuts and breaks in blood vessels. But if you're at risk of heart attack or stroke, platelets can stick together inside already narrowed blood vessels to form a clot.

What are the common side effects of Clopinol?

Common side effects of Clopinol are include:

  • excessive tiredness.
  • headache.
  • dizziness.
  • nausea.
  • vomiting.
  • stomach pain.
  • diarrhea.
  • nosebleed.

Is Clopinol safe during pregnancy?

Clopinol can be used throughout pregnancy. There may be another issue related to delivery, however. The patient in question is planning to have a repeat cesarean, and there is some evidence that Clopinol may cause more hemorrhagic complications of surgery.

Is Clopinol safe during breastfeeding?

The manufacturer reports that no adverse effects have been observed in breastfed infants with maternal Clopinol use during lactation in a small number of postmarketing cases.

Can I drink alcohol with Clopinol?

You can drink alcohol with Clopinol. But do not drink too much while taking this medicine.

When should be taken of Clopinol?

It is usually taken once a day with or without food. Take Clopinol at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.

Can I take Clopinol on an empty stomach?

You can be taken with or without food.

How long does Clopinol take to work?

Clopinol works within 2 hours of taking it.

How is Clopinol eliminated from the body?

An oral dose of radiolabelled Clopinol is excreted 50% in the urine and 46% in the feces over 5 days. The remainder of Clopinol is irreversibly bound to platelets for their lifetime, or approximately 8-11 days.

Is it safe to take Clopinol every other day?

Long term dual anti-platelet therapy with aspirin 81 mg daily and Clopinol 75 mg every other day beyond 12 months after PCI with DES may be a safe and efficacious cost-saving strategy to prevent VLST.

What is Clopinol half-life?

Oral dose of 75 mg, Clopinol has a half-life of approximately 6 hours.

Can I take Clopinol for a long time?

Clopinol oral tablet is used for long-term treatment. It comes with serious risks if you don't take it as prescribed. If you stop taking the drug or don't take it at all: You increase your risk of heart attack or stroke. These conditions can be fatal.

Who should not take Clopinol?

You should not use Clopinol if you have any active bleeding such as a stomach ulcer or bleeding in the brain.Clopinol increases your risk of bleeding, which can be severe or life-threatening. Call your doctor or seek emergency medical attention if you have bleeding that will not stop, if you have blood in your urine, black or bloody stools, or if you cough up blood or vomit that looks like coffee grounds.

What happens if I miss a dose?

Take Clopinol as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention.Overdose can cause excessive bleeding.

Can Clopinol cause heart attacks?

Clopinol may be at increased risk of serious problems like heart attacks or strokes.

Does Clopinol affect the kidneys?

In summary, among patients hospitalized with ACS and treated with Clopinol, lower levels of kidney function were associated with a greater risk of death, hospitalization for AMI, and major bleeding.

Does Clopinol affect sleep?

Clopinol are among the most prescribed drugs in cardiology and are not cited as causing insomnia or sleepiness.

Does Clopinol affect the liver?

Liver damage is a rare side effect of Clopinol.

Does Clopinol weaken immune system?

Clopinol may also cause weak immunosuppression that might contribute to risk of fatal infections.

*** Taking medicines without doctor's advice can cause long-term problems.
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