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
No information provided.
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: http://en.wikipedia.org/wiki/Sulfinpyrazone
Organisms Affected: Humans and other mammals