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