Esloric 100 mg Tablet
Esloric 100 mg Tablet Uses, Dosage, Side Effects, Food Interaction and all others data.
Esloric 100 mg Tablet is a xanthine oxidase inhibitor which is administered orally. It acts on purine catabolism without disrupting the biosynthesis of purine. It reduces the production of uric acid by inhibiting the biochemical reactions immediately preceding its formation. Esloric 100 mg Tablet is a structural analogue of the natural purine base, hypoxanthine. It is an inhibitor of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and xanthine to uric acid, the end product of purine metabolism
Esloric 100 mg Tablet decreases the production of uric acid by stopping the biochemical reactions that precede its formation . This process decreases urate and relieves the symptoms of gout, which may include painful tophi, joint pain, inflammation, redness, decreased range of motion, and swelling .
| Trade Name | Esloric 100 mg Tablet |
| Availability | Prescription only |
| Generic | Allopurinol |
| Allopurinol Other Names | 4-HPP, Allopurinol, Allopurinolum, Alopurinol |
| Related Drugs | sodium bicarbonate, febuxostat, Zyloprim, probenecid, Uloric, Krystexxa, rasburicase, Elitek, Aloprim |
| Weight | 100 mg |
| Type | Tablet |
| Formula | C5H4N4O |
| Weight | Average: 136.1115 Monoisotopic: 136.03851077 |
| Protein binding | Allopurinol and oxypurinol are only negligibly bound to plasma proteins . |
| Groups | Approved |
| Therapeutic Class | Drugs used in Gout |
| Manufacturer | Square Pharmaceuticals Ltd. |
| Available Country | Bangladesh |
| Last Updated: | September 24, 2024 at 5:38 am |
Uses
Esloric 100 mg Tablet is used for prevention and treatment of high blood uric acid level and gout, prevents deposition of urate crystal in kidney, serous membranes of liver, heart, air sac and joints of poultry.
Esloric 100 mg Tablet is also used to associated treatment for these conditions: Hyperuricemia, Primary Gout, Recurrent calcium oxalate calculi, Secondary gout, Calcium oxalate calculi Renal Calculi
How Esloric 100 mg Tablet works
Esloric 100 mg Tablet is a structural analog of the natural purine base, hypoxanthine. After ingestion, allopurinol is metabolized to its active metabolite, oxypurinol (alloxanthine) in the liver , which acts as an inhibitor of xanthine oxidase enzyme .
Esloric 100 mg Tablet and its active metabolite inhibit xanthine oxidase, the enzyme that converts hypoxanthine to xanthine and xanthine to uric acid. Inhibition of this enzyme is responsible for the effects of allopurinol. This drug increases the reutilization of hypoxanthine and xanthine for nucleotide and nucleic acid synthesis by a process that involves the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase). This process results in an increased nucleotide concentration, which causes feedback inhibition of de novo purine synthesis. The end result is decreased urine and serum uric acid concentrations , which decreases the incidence of gout symptoms.
Accompanying the reduction of serum uric acid by allopurinol is an increase in the serum and urine concentrations of hypoxanthine and xanthine (due to inhibition of xanthine oxidase). In the absence of allopurinol, regular urinary excretion of oxypurines almost entirely occurs in the form of uric acid. After the ingestion of allopurinol, the contents of excreted urine are hypoxanthine, xanthine, and uric acid. Because each substance has its own individual solubility, the concentration of uric acid in plasma is decreased without exposing the renal tissues to a high load of uric acid, thereby decreasing the risk of crystalluria. By lowering the uric acid concentration in the plasma below its limits of solubility, allopurinol encourages the dissolution of gout tophi. Although the levels of hypoxanthine and xanthine are found to be increased after allopurinol ingestion, the risk of deposition in renal tissues is less than that of uric acid, as they become more soluble and are rapidly excreted by the kidney .
Dosage
Esloric 100 mg Tablet dosage
Poultry- 25 mg/kg body or 2.5 gm/liter water for 3-5 days, or as directed by registered veterinarian.
Side Effects
The most frequent adverse reaction to Esloric 100 mg Tablet is skin rash such as, pruritic maculopapular skin eruptions, sometimes scaly or exfoliative.
Toxicity
Oral TDLO (rat): 10 mg/kg; Oral LD50 (mouse): 78 mg/kg; Oral TDLO (mouse): 100 mg/kg
Use in pregnancy
Reproductive studies have been completed using rats and rabbit models at doses up to twenty times the normal human dose ( about 5 mg/kg per day), and it was concluded that fertility was not impaired and there was no fetal harm. There is a published report of a study in pregnant mice administered 50 or 100 mg/kg allopurinol intraperitoneally on gestation days 10 or 13. There were increased numbers of dead fetuses in dams administered 100 mg/kg allopurinol, however, death did not occur in those given 50 mg/kg. There were higher numbers of external malformations in fetuses at both doses of allopurinol on gestation day 10 and higher numbers of skeletal malformations in fetuses at both doses on gestation day 13. Despite the above findings, there are no adequate or well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if it is absolutely required .
Use in nursing
Both allopurinol and the metabolite oxipurinol have been found in the milk of a mother who was receiving allopurinol. Since the effect of allopurinol on the nursing infant is unknown, it is advisable to exercise caution when allopurinol is taken by a nursing woman .
Mutagenicity and carcinogenicity
Cytogenic studies demonstrate that allopurinol does not induce chromosomal abnormalities in human blood cells in vitro at concentrations up to 100 g/mL and in vivo at doses up to 60 mg/day for an average duration of 40 months. Esloric 100 mg Tablet does not form nitroso compounds (which may be carcinogenic) or affect lymphocyte transformation in vitro. Evidence suggests that allopurinol does not have deleterious effects on DNA at any stage of the cell cycle and was not found to be mutagenic. No evidence of carcinogenicity has been observed in mice treated with allopurinol for up to a 2 year period .
Precaution
Before you use discuss with your doctor if you are allergic to it or its ingredients.
Interaction
Anticoagulant: Esloric 100 mg Tablet prolongs the half life of the anticoagulant, dicumarol.
Diuretic: Concomitant use of Esloric 100 mg Tablet and thiazide diuretics may contribute to the enhancement of Esloric 100 mg Tablet toxicity.
Cytotoxic agent: Enhanced bone marrow suppression by cyclophosphamide and other cytotoxic agent has been reported among patients with neoplastic disease.
Food Interaction
- Avoid alcohol.
- Take with a full glass of water.
- Take with food.
Esloric 100 mg Tablet Drug Interaction
Unknown: aspirin, aspirin, aspirin, aspirin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, furosemide, furosemide, atorvastatin, atorvastatin, metoprolol, metoprolol, metoprolol, metoprolol, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Esloric 100 mg Tablet Disease Interaction
Moderate: bone marrow suppression, dehydration, liver disease, renal dysfunction
Volume of Distribution
Esloric 100 mg Tablet and oxypurinol are both substrates for the enzyme xanthine oxidase, which is present in the cytoplasm of endothelial cells of capillaries, including sinusoids, with the highest activity demonstrated in the liver and intestinal lining. Tissue concentrations of allopurinol have not yet been reported in humans, however, it is probable that allopurinol and the metabolite oxypurinol would be measured in the highest concentrations in the abovementioned tissues. In animals, allopurinol concentrations are found to reach the highest levels in the blood, liver, intestine and heart, and lowest in the brain and lung tissues .
Elimination Route
This drug is about 90% absorbed from the gastrointestinal tract. Peak plasma levels normally occur at 1.5 hours and 4.5 hours post-dose for allopurinol and oxipurinol respectively. Following one oral dose of 300 mg of allopurinol, maximum plasma levels of about 3 mcg/mL of allopurinol and 6.5 mcg/mL of oxipurinol were measured .
Half Life
The plasma half-life of allopurinol is 1-2 hours, due to its rapid renal clearance .
Clearance
Since allopurinol and its metabolites are mainly eliminated by the kidney, accumulation of this drug can occur in patients with renal dysfunction or failure, and the dose of allopurinol should, therefore, be reduced. With a creatinine clearance of 10 to 20 mL/min, a daily dosage of 200 mg of allopurinol is suitable. When the creatinine clearance is less than 10 mL/min, the daily dosage should not be higher than 100 mg. With severe renal impairment (creatinine clearance measured at less than 3 mL/min) a longer interval between doses may be required .
Elimination Route
Approximately 80% of orally ingested allopurinol is found excreted in the urine as various metabolites . About 20% of ingested allopurinol is excreted in the feces .
Pregnancy & Breastfeeding use
Sufficient clinical data is not available. This drug should be used during pregnancy only if clearly indicated. Esloric 100 mg Tablet has been found in breast milk, caution should be exercised when Esloric 100 mg Tablet is administered to a lactating mother.
Contraindication
Patients who have developed a severe reaction to allopurinol should not be restarted the drug. Esloric 100 mg Tablet should be withdrawn immediately when a skin rash or other evidence or sensitivity occurs. Dosage reduction should be considered in the presence of severe hepatic or renal disorder.
Acute Overdose
Over dosage may cause diarrhea, abdominal pain and neurotoxicity.
Interaction with other Medicine
Anticoagulant: Esloric 100 mg Tablet prolongs the half life of the anticoagulant, dicumarol.
Diuretic: Concomitant use of Esloric 100 mg Tablet and thiazide diuretics may contribute to the enhancement of Esloric 100 mg Tablet toxicity.
Cytotoxic agent: Enhanced bone marrow suppression by cyclophosphamide and other cytotoxic agent has been reported among patients with neoplastic disease.
Storage Condition
Protect from light & keep in a cool and dry place. Keep out of reach of children.
Innovators Monograph
You find simplified version here Esloric 100 mg Tablet
Esloric 100 mg Tablet contains Allopurinol see full prescribing information from innovator Esloric 100 mg Tablet Monograph, Esloric 100 mg Tablet MSDS, Esloric 100 mg Tablet FDA label
FAQ
What is Esloric 100 mg Tablet used for?
Esloric 100 mg Tablet is a medication used to decrease high blood uric acid levels. It is specifically used to prevent gout, prevent specific types of kidney stones and for the high uric acid levels that can occur with chemotherapy.
How safe is Esloric 100 mg Tablet?
Esloric 100 mg Tablet is considered very safe to take for a long period of time. There are unlikely to be any long-term effects.
How does Esloric 100 mg Tablet work?
Esloric 100 mg Tablet works by reducing the amount of uric acid made by body cells.
What are the common side effects of Esloric 100 mg Tablet?
The more common side effects of Esloric 100 mg Tablet can include:
- skin rash.
- diarrhea.
- nausea.
- changes in your liver function test results.
- gout flare-up (if you have gout)
Is Esloric 100 mg Tablet safe during pregnancy?
Limited data available on use of this Esloric 100 mg Tablet in pregnant women to inform a drug-related risk.
This Esloric 100 mg Tablet should only be used during pregnancy when there is no safe alternative and when the disease itself carries risks for the mother or child.
Is Esloric 100 mg Tablet safe during breastfeeding?
If Esloric 100 mg Tablet is required by the mother, it is not a reason to discontinue breastfeeding, but exclusively breastfed infants should be monitored if this Esloric 100 mg Tablet is used, including observation for allergic reactions (such as rash) and periodic CBC and differential blood counts.
Can I drink alcohol with Esloric 100 mg Tablet?
Yes, you can drink alcohol while taking Esloric 100 mg Tablet. But drinking alcohol increases the level of uric acid in your blood and can trigger an attack of gout. If you feel safe, you can drink alcohol in moderation.
Can I drive after taking Esloric 100 mg Tablet?
Esloric 100 mg Tablet oral tablet may cause drowsiness. You shouldn't drive, use machinery, or do other tasks that require alertness until you know how Esloric 100 mg Tablet affects you. It can also cause other side effects.
Should Esloric 100 mg Tablet be taken daily?
Esloric 100 mg Tablet should be taken every day to prevent a gout attack.
How many time can I take Esloric 100 mg Tablet daily?
taken once a day or in divided doses.
When should be best taken of Esloric 100 mg Tablet ?
It is usually taken once or twice a day, preferably after a meal. To help you remember to take Esloric 100 mg Tablet, take it around the same time every day.
How long does Esloric 100 mg Tablet take to work?
Esloric 100 mg Tablet can take 2-3 months to become fully effective. It does not have any effect during a gout attack, although you should continue to take it regularly every day even if this happens.
What is the half life of Esloric 100 mg Tablet?
Esloric 100 mg Tablet has a plasma half-life of about 1 to 2 hours.
How long should I take Esloric 100 mg Tablet?
For gout attacks – treatment is usually only for a few days. For FMF – treatment is usually long term. You may need to take it for the rest of your life. Talk to your doctor if you're not sure how long you need to take this medicine for.
Can I take Esloric 100 mg Tablet for long-term?
Esloric 100 mg Tablet is considered very safe to take for a long period of time.
Can Esloric 100 mg Tablet affects my liver?
Esloric 100 mg Tablet is a rare but well known cause of acute liver injury that has features of a hypersensitivity reaction and can be severe and even fatal.
Who should not take Esloric 100 mg Tablet?
You should not use this Esloric 100 mg Tablet if you have ever had a serious allergic reaction to Esloric 100 mg Tablet. Stop taking the medicine and call your doctor at once if you have any signs of skin rash (no matter how mild), painful urination, blood in your urine, burning in your eyes, or swelling in your face or throat.
What happens if I miss a dose?
Take the Esloric 100 mg Tablet oral dose 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. Call your doctor for instructions if you miss an injection.
What happen If I stop taking Esloric 100 mg Tablet?
If you stop Esloric 100 mg Tablet treatment suddenly, there is a high risk that gout may get worse or you will get serious side effects. Only stop taking Esloric 100 mg Tablet if a doctor tells you to. A doctor will help you to reduce your dose slowly so you do not get serious side effects.
Does Esloric 100 mg Tablet affect my heart?
Esloric 100 mg Tablet had no effect on heart rate variability, mean heart rate or dysrhythmias in our cohort of heart failure patients.
Can Esloric 100 mg Tablet affect my kidneys?
Esloric 100 mg Tablet does not cause worsening renal function and may have protective affects for the kidney.
Can Esloric 100 mg Tablet affects my liver?
Esloric 100 mg Tablet often used to prevent painful gout attacks, can cause liver injury within days to weeks of the start of treatment. Esloric 100 mg Tablet may cause changes in liver function test results and liver failure.
Will Esloric 100 mg Tablet affect my fertility?
There's no firm evidence to suggest that taking Esloric 100 mg Tablet will reduce fertility in either men or women.
