Febuxostat
Febuxostat Uses, Dosage, Side Effects, Food Interaction and all others data.
Febuxostat is a histamine H2-receptor antagonist. Febuxostat completely inhibits the action of histamine on H2-receptors of parietal cell. It inhibits basal, overnight and pentagastrin stimulated gastric acid secretion. The H2-receptor antagonist activity of Febuxostat is slowly reversible, since the drug dissociates slowly from H2-receptor.
Febuxostat decreases the production of gastric acid, suppresses acid concentration and pepsin content, and decreases the volume of gastric secretion. Febuxostat inhibits both basal and nocturnal gastric acid secretion, as well as acid secretion stimulated by food, caffeine, insulin, and pentagastrin.
Febuxostat has a dose-dependent therapeutic action, with the highest dose having the most extended duration of action and the highest inhibitory effect on gastric acid secretion. Following oral administration, the onset of action is within one hour, and the peak effect is reached within 1-3 hours. The duration of effect is about 10-12 hours.
| Trade Name | Febuxostat |
| Availability | Rx and/or OTC |
| Generic | Famotidine |
| Famotidine Other Names | Famotidina, Famotidine, Famotidinum |
| Related Drugs | omeprazole, pantoprazole, Nexium, Pepcid, Protonix, esomeprazole, sucralfate, Prilosec, ranitidine, lansoprazole |
| Weight | 40mg, , 80mg |
| Type | Tablet, Oral Tablet |
| Formula | C8H15N7O2S3 |
| Weight | Average: 337.445 Monoisotopic: 337.044934829 |
| Protein binding | The protein binding of famotidine is about 15 to 22%. |
| Groups | Approved |
| Therapeutic Class | H2 receptor antagonist |
| Manufacturer | Popular Pharmaceuticals Ltd, Rivopharm Uk Ltd, Micro Labs Limited |
| Available Country | Bangladesh, United Kingdom, United States, India, Nigeria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Febuxostat is used for-
- Short term treatment of active duodenal ulcer and benign gastric ulcer
- Maintenance therapy for prevention of relapses of duodenal ulceration
- Gastro-oesophageal reflux disease
- Zollinger Ellison Syndrome
Febuxostat is also used to associated treatment for these conditions: Chronic Back Pain, Duodenal Ulcer, Erosive Esophagitis, Extra-Articular Rheumatism, Gastritis, Heartburn, Helicobacter Pylori Infection, Multiple Endocrine Neoplasia, Muscle Spasms, Nonspecific Pain Post Traumatic Injury, Osteoarthritis (OA), Postoperative pain, Stress Ulcers, Zollinger-Ellison Syndrome, Active Gastric ulcer, Acute Duodenal Ulcers, Gastrointestinal ulceration, Pathological hypersecretory conditions, Symptomatic non-erosive gastroesphageal reflux disease
How Febuxostat works
Histamine acts as a local hormone that stimulates the acid output by parietal cells via a paracrine mechanism. Neuroendocrine cells called enterochromaffin-like (ECL) cells lie close to the parietal cells and regulate the basal secretion of histamine. Histamine release is also promoted from stimulation by acetylcholine and gastrin, a peptide hormone. Gastrin (G) cells release gastrin, which works on CCK2 receptors on ECL cells. This action promotes the release of histamine from ECL cells. Upon release, histamine acts on H2 receptors expressed on the basolateral membrane of parietal cells, leading to increased intracellular cAMP levels and activated proton pumps on parietal cells. Proton pump releases more protons into the stomach, thereby increasing the secretion of acid. In conditions that are associated with acid hypersecretion such as ulcers, there is a loss of regulation of acid secretion. Febuxostat works on H2 receptors and blocks the actions of histamine.
Dosage
Febuxostat dosage
Duodenal ulcer: 40 mg at night for 4 to 8 weeks
Benign gastric ulcer: 40 mg at night for 4 to 8 weeks; Maintenance therapy: 20 mg at night for preventing the recurrences of duodenal ulceration
Gastro-oesophageal reflux disease: 20 mg twice daily for 6 to 12 weeks
Zollinger Ellison syndrome: The recommended starting dose is 20 mg every six hours. Dosage should then be adjusted to individual response. Doses up to 160 mg every six hours have been administered to some patients without the development of significant adverse effects.
Dosage can be administered irrespective of meals. Antacids may be given concomitantly if needed.
Side Effects
Febuxostat is generally well tolerated and side effects are uncommon. Dizziness, headache, constipation and diarrhoea have been reported rarely. Other side effects reported less frequently include dry mouth, nausea and/or vomiting, rash, abdominal discomfort, anorexia and fatigue.
Toxicity
The oral LD50 is 4049 mg/kg in rats and 4686 mg/kg in mice. The subcutaneous LD50 is 800 mg/kg in rats and mice. The lowest published toxic dose (TDLo) in man following oral administration is 4 mg/kg/7D.
Symptoms of overdose resemble the adverse events seen with the use of recommended doses, and they should be responded with supportive and symptomatic treatment. Any unabsorbed drug should be removed from the gastrointestinal tract, and the patient should be monitored accordingly. The use of hemodialysis to eliminate the drug from the systemic circulation is effective, but the experience of using hemodialysis in response to famotidine overdose is limited in clinical settings.
Precaution
Dosage reduction should be considered or interval between doses should be prolonged if creatinine clearance falls to or below 30 ml/min.
Interaction
Febuxostat does not interact with the cytochrome P450 linked drug metabolising enzyme system. So, no interactions have been found in man with Warfarin, Theophylline, Phenytoin, Diazepam, Propranolol, Aminopyrine or antipyrine.
Food Interaction
- Avoid excessive or chronic alcohol consumption. Alcohol increases the risk of gastric irritation.
- Limit caffeine intake. Caffeine and other acidic beverages increases the risk of gastric irritation.
- Take with or without food. Food slightly increases bioavailability, but not to a clinically significant extent.
Febuxostat Drug Interaction
Minor: cyanocobalamin, cyanocobalaminUnknown: aspirin, aspirin, diphenhydramine, diphenhydramine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, metoprolol, metoprolol, metoprolol, metoprolol, acetaminophen, acetaminophen, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, cetirizine, cetirizine
Febuxostat Disease Interaction
Volume of Distribution
The steady-state volume of distribution ranges from 1.0 to 1.3 L/kg. Febuxostat is found in breast milk; however, it is found in breast milk at the lowest concentrations compared to other H2 receptor antagonists.
Elimination Route
Following oral administration, the absorption of famotidine is dose-dependent and incomplete. The oral bioavailability ranges from 40-50%, and the Cmax is reached in 1-4 hours post-dosing. While the bioavailability can be slightly increased with the intake of food and decreased by antacids, there is no clinical significance.
Half Life
The elimination half-life is about 2 to 4 hours. The half-life is expected to increase nonlinearly in patients with decreased renal function.
Clearance
Renal clearance is 250-450 mL/min, indicating some tubular excretion. Because the renal clearance rate exceeds the glomerular filtration rate, famotidine is thought to be mainly eliminated via both glomerular filtration and renal tubular secretion.
Elimination Route
About 65-70% of the total administered dose of famotidine undergoes renal elimination, and 30-35% of the dose is cleared by metabolism. Following intravenous administration, about 70% of the drug is eliminated in the urine as an unchanged drug.
Pregnancy & Breastfeeding use
Pregnancy: There are no adequate, well controlled studies on Febuxostat in pregnancy, but it is known to cross the placenta and should be prescribed only if clearly needed.
Lactation: It is not known whether Febuxostat is secreted into human milk, nursing mothers should either stop nursing or stop taking the drug.
Contraindication
There are no known contraindication to Febuxostat. If any evidence of hypersensitivity appear, the therapy should be discontinued and consultation with physician is required.
Storage Condition
Tablet: Store between 15-30° C. Concentrate for injection: Store between 2-8° C.
Innovators Monograph
You find simplified version here Febuxostat
Febuxostat contains Famotidine see full prescribing information from innovator Febuxostat Monograph, Febuxostat MSDS, Febuxostat FDA label
FAQ
What is Febuxostat used for?
Febuxostat is used to treat stomach ulcers, erosive esophagitis, and gastroesophageal reflux disease.is a histamine H₂ receptor antagonist medication that decreases stomach acid production. It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger-Ellison syndrome.
How does Febuxostat work?
Febuxostat works by decreasing the amount of acid produced by the stomach.
What are the common side effects of Febuxostat?
Common side effects of Febuxostat are include:
- Anxiety.
- blistering, peeling, or loosening of the skin.
- blood in the urine or stools.
- bloody, black, or tarry stools.
- difficulty breathing.
- discouragement.
- fast, irregular, pounding, or racing heartbeat or pulse.
- feeling sad or empty.
Is Febuxostat safe during pregnancy?
Use is recommended only if clearly needed and the benefit outweighs the risk.Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.
Is Febuxostat safe during breastfeeding?
Febuxostat doses in breastmilk result in infant dosages that are lower than those used in newborn infants. Febuxostat would not be expected to cause any adverse effects in breastfed infants. No special precautions are required.
Can I drink alcohol with Febuxostat?
Avoid drinking alcohol. It can increase the risk of damage to your stomach. Avoid taking other stomach acid reducers unless your doctor has told you to.
How should I take Febuxostat?
Febuxostat can be taken with or without food. To prevent heartburn and acid indigestion, take Febuxostat 15-60 minutes before eating food or drinking beverages that can cause indigestion.
How often should I use Febuxostat?
Do not take more than 2 tablets in 24 hours unless directed by your doctor. Adults 20 milligrams every 6 hours. Your doctor may adjust your dose as needed. Children use and dose must be determined by your doctor.
Is it better to take Febuxostat in the morning or at night?
If you are taking this Febuxostat once daily, it is usually taken right before bedtime.
How long does it take Febuxostat to take effect?
The effect of Febuxostat can be felt within one hour and can last up to 12 hours depending on the dose taken.
What is the half life of Febuxostat?
The plasma half-life is about 3 hours both after oral single doses and during repeated administration.
Can I take Febuxostat for a long time?
Febuxostat in 24 hours and do not take over-the-counter Febuxostat for longer than 2 weeks unless your doctor tells you that you should.
Who should not take Febuxostat?
Do not self-medicate with Febuxostat if you are over the age of 40 and this is the first time you have had heartburn or indigestion; have a family history of gastric cancer; have coughing spells; use NSAIDs anti-inflammatories; have difficulty or pain when swallowing; already take other.
Does Febuxostatc affect blood pressure?
Febuxostat demonstrated cardiac function improvements, including a slight decrease in both systolic and diastolic blood pressure.
Does Febuxostat cause joint pain?
Febuxostat can causes joint pain also with other side effects.
Can Febuxostat cause blurry vision?
transient and mild blurred vision has been reported,
Can Febuxostat cause heart problems?
Febuxostat not associated with increased cardiovascular risk.
What happens if I miss a dose of Febuxostat?
Take the medicine 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 happen if I take too much Febuxostat?
If you take too much you could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug can include: agitation, confusion.
What happen If I stop taking Febuxostat?
If you stop taking the drug suddenly or don't take it at all: Your acid reflux, heartburn, or ulcer symptoms may not get better or may get worse.
