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