Apo-Sulfinpyrazone: Full Drug Profile
Apo-Sulfinpyrazone - General Information
A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.
Pharmacology of Apo-Sulfinpyrazone
Apo-Sulfinpyrazone's pharmacologic activity is the potentiation of the urinary excretion of uric acid. It is useful for reducing the blood urate levels in patients with chronic tophaceous gout and acute intermittent gout, and for promoting the resorption of tophi.
Apo-Sulfinpyrazone for patients
Apo-Sulfinpyrazone Interactions
No information provided.
Apo-Sulfinpyrazone Contraindications
Patients with an active peptic ulcer or symptoms of gastrointestinal inflammation or ulceration should not receive the drug.
The drug is contraindicated in patients with a history or the presence of:
1. Hypersensitivity to phenylbutazone or other pyrazoles
2. Blood dyacrasias
Additional information about Apo-Sulfinpyrazone
Apo-Sulfinpyrazone Indication: For the treatment of gout and gouty arthritis. Mechanism Of Action: Apo-Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Apo-Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Apo-Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Apo-Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Apo-Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Apo-Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs). Drug Interactions: Not Available Food Interactions: Not Available Generic Name: Sulfinpyrazone Synonyms: Sulfinpyrazon; Sulfinpyrazine; Sulfoxyphenylpyrazolidine; Sulphinpyrazone; Usaf Ge-13; Diphenylpyrazone Drug Category: Uricosuric Agents Drug Type: Small Molecule; Approved Other Brand Names containing Sulfinpyrazone: Anturan; Anturane; Anturanil; Anturano; Anturen; Anturidin; Apo-Sulfinpyrazone; Enturan; Enturen; Novopyrazone; Absorption: Not Available Toxicity (Overdose): Symptoms of overdose include nausea, vomiting, diarrhea, epigastric pain, ataxia, labored respiration, convulsions, coma. Possible symptoms, seen after overdosage with other pyrazolone derivatives: anemia, jaundice, and ulceration. Protein Binding: 98-99% Biotransformation: Not Available Half Life: Approximately 4-6 hours Dosage Forms of Apo-Sulfinpyrazone: Tablet Oral Chemical IUPAC Name: 1,2-di(phenyl)-4-(2-phenylsulfinylethyl)pyrazolidine-3,5-dione Chemical Formula: C23H20N2O3S Sulfinpyrazone on Wikipedia: https://en.wikipedia.org/wiki/Sulfinpyrazone Organisms Affected: Humans and other mammals
