Clopinol Ap
Clopinol Ap Uses, Dosage, Side Effects, Food Interaction and all others data.
(Clopidogrel) is an inhibitor of platelet aggregation. Lopirel (Clopidogrel) 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.
Clopidogrel 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 Ap |
| Generic | Clopidogrel + Acetylsalicylic acid / Acetyl Salicylic Acid |
| Weight | 150mg, 75mg |
| Type | Capsule, Tablet |
| Therapeutic Class | |
| Manufacturer | Knoll Healthcare Pvt Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
(Clopidogrel) 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 Ap is also used to associated treatment for these conditions: Acute Coronary Syndrome (ACS), Acute Myocardial Infarction (AMI), Cardiovascular Events, Atherothrombotic events
How Clopinol Ap works
Clopidogrel 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 Ap dosage
The recommended dose of Lopirel (Clopidogrel) is 75 mg once daily with or without food.
Side Effects
Generally Clopidogrel 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. Clopidogrel 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, Clopidogrel should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery, or other pathological conditions. Clopidogrel should be discontinued 7 days prior to surgery. Clopidogrel should be used with caution in hepatically impaired patients who may have bleeding diatheses.
Interaction
Concomitant use of Heparin, Warfarin and NSAIDs with Clopidogrel should be undertaken with caution. Clopidogrel potentiate the effect of Aspirin on collagen-induced platelet aggregation. The safety of chronic concomitant administration of Aspirin and Clopidogrel has not been established.
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. Clopidogrel 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. Clopidogrel 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 Clopidogrel in pregnant women. However, Clopidogrel should be used during pregnancy only if clearly needed.
Lactation: Clopidogrel is not recommended for use while breast-feeding. It is not known for sure whether Clopidogrel is excreted in breast milk, although it is suspected that it is.
Contraindication
Clopidogrel 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 Clopidogrel 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.
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