Explat
Explat Uses, Dosage, Side Effects, Food Interaction and all others data.
(Explat) is an inhibitor of platelet aggregation. Lopirel (Explat) 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.
Explat 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 | Explat |
| Availability | Prescription only |
| Generic | Clopidogrel |
| Clopidogrel Other Names | Clopidogrel, Clopidogrelum |
| Related Drugs | aspirin, lisinopril, metoprolol, propranolol, Xarelto, Plavix, Brilinta, enoxaparin, rivaroxaban, pravastatin |
| Weight | 75mg |
| 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 | Indus Pharma (pvt) Ltd, |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
(Explat) 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.
Explat is also used to associated treatment for these conditions: Acute Coronary Syndrome (ACS), Acute Myocardial Infarction (AMI), Cardiovascular Events, Atherothrombotic events
How Explat works
Explat 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
Explat dosage
The recommended dose of Lopirel (Explat) is 75 mg once daily with or without food.
Side Effects
Generally Explat 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. Explat 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, Explat should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery, or other pathological conditions. Explat should be discontinued 7 days prior to surgery. Explat should be used with caution in hepatically impaired patients who may have bleeding diatheses.
Interaction
Concomitant use of Heparin, Warfarin and NSAIDs with Explat should be undertaken with caution. Explat potentiate the effect of Aspirin on collagen-induced platelet aggregation. The safety of chronic concomitant administration of Aspirin and Explat has not been established.
Food Interaction
- Take with or without food.
Explat Drug Interaction
Moderate: aspirin, aspirin, aspirin, aspirin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acidsUnknown: ubiquinone, ubiquinone, rosuvastatin, rosuvastatin, metoprolol, metoprolol, metoprolol, metoprolol, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Explat Disease Interaction
Major: bleedingModerate: liver diseaseMinor: renal dysfunction
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. Explat 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. Explat 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 Explat in pregnant women. However, Explat should be used during pregnancy only if clearly needed.
Lactation: Explat is not recommended for use while breast-feeding. It is not known for sure whether Explat is excreted in breast milk, although it is suspected that it is.
Contraindication
Explat 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 Explat 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 Explat
Explat contains Clopidogrel see full prescribing information from innovator Explat Monograph, Explat MSDS, Explat FDA label
FAQ
What is Explat used for?
Explat 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 Explat helps prevent blood clots if you have an increased risk of having them.
How safe is Explat?
Explat 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 Explat.
how does Explat work?
Explat 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 Explat?
Common side effects of Explat are include:
- excessive tiredness.
- headache.
- dizziness.
- nausea.
- vomiting.
- stomach pain.
- diarrhea.
- nosebleed.
Is Explat safe during pregnancy?
Explat 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 Explat may cause more hemorrhagic complications of surgery.
Is Explat safe during breastfeeding?
The manufacturer reports that no adverse effects have been observed in breastfed infants with maternal Explat use during lactation in a small number of postmarketing cases.
Can I drink alcohol with Explat?
You can drink alcohol with Explat. But do not drink too much while taking this medicine.
When should be taken of Explat?
It is usually taken once a day with or without food. Take Explat 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 Explat on an empty stomach?
You can be taken with or without food.
How long does Explat take to work?
Explat works within 2 hours of taking it.
How is Explat eliminated from the body?
An oral dose of radiolabelled Explat is excreted 50% in the urine and 46% in the feces over 5 days. The remainder of Explat is irreversibly bound to platelets for their lifetime, or approximately 8-11 days.
Is it safe to take Explat every other day?
Long term dual anti-platelet therapy with aspirin 81 mg daily and Explat 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 Explat half-life?
Oral dose of 75 mg, Explat has a half-life of approximately 6 hours.
Can I take Explat for a long time?
Explat 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 Explat?
You should not use Explat if you have any active bleeding such as a stomach ulcer or bleeding in the brain.Explat 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 Explat 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 Explat cause heart attacks?
Explat may be at increased risk of serious problems like heart attacks or strokes.
Does Explat affect the kidneys?
In summary, among patients hospitalized with ACS and treated with Explat, lower levels of kidney function were associated with a greater risk of death, hospitalization for AMI, and major bleeding.
Does Explat affect sleep?
Explat are among the most prescribed drugs in cardiology and are not cited as causing insomnia or sleepiness.
Does Explat affect the liver?
Liver damage is a rare side effect of Explat.
Does Explat weaken immune system?
Explat may also cause weak immunosuppression that might contribute to risk of fatal infections.
