Sulfinpyrazone ( ** )- @ pyrazolidone der. Agents for Gout
Drug Interaction:
Interacting drugs - summary
Sulfinpyrazone +
Acetoaminophen
risk of acetoaminophen hepatoxicity may be increased.
the therapeutic effects of acetoaminophen may be reduced.
Anticoagulant
anticoagulant activity of warfarin will be enhanced, hemorrhage
could occur.
Theophylline
plasma theophylline clearance may be increased, thus lowering
plasma levels
Tolbutamide
decreased clearance and increased half-life of tolbutamide may
occur: hypoglycemia may result.
Verapramil
increased clearance and decreased bioavailabilty of verapramil
may occur
Sulfinpyrazone
Niacin
sulfinpyrazones uricosuric effect may be reduced.
Salicylates
sulfipyrazones uricosuric effect may be suppressed.
Sulfonylureas
hypoglycemic effect of the sulfonylureas may be enhanced
due to various mechanisms ( eg decreased hepatic
metabolism, inhibition of renal excretion, displacement from
protein binding sites,decreased blood glucose or
alteration of carbohydrate metabolism
Betablockers
bioavailability and plasma levels of certain beta blockers may be
decreased by these agents, possibly resulting in decreased
pharmacologic effect
Indication:
Chronic and intermittant gouty arthritis
Adverse Reaction:
Most frequent- Upper GI disturbances. Administer with food,milk,antacids; despite this precaution, the drug may aggravate or reactivate peptic ulcer.
Less frequent- Rash,rare blood dyscrasias, bronchoconstriction in patients with aspirin-induced asthma.
Contra-Indications:
Active peptic ulcer or symptoms of GI inflammation or ulceration,hypersen to phentyl butazone,or other pyrazoles; blood dyscrasias.
Special precautions:
Keep patients under close medical supervision; perform periodic blood counts.
Administer with care,healed peptic ulcer. Alkalisation of urine, may precipitate gouty arthiritis,urolithiasis and renal colic.
Monitoring- keep patients under close medicalsupervision , perform periodic blood counts
Healed peptic ulcer- administer with care.
Alkalizaton of urine- adequate fliud intake and alkaliozation of theurine are recommended
Warnings-
Renal function impairment- periodically assess renal function. Renal failure has occured,but a cause and effect relationship has not always been clearly established
Pregnancy- use only when clearly needed and when the potential benefits outweigh the potential hazards to the fetus.
Dosages/ Overdosage Etc:
Indications:
Chronic and intermittant gouty arthritis
Dosage:
Initial- 200 to 400 mg daily in 2 divide doses,with meals or milk.; gradually increasing when
necessary to full maintenance dosage in 1 week.
Maintenance- 400 mg daily, given in 2 divided doses; may increase to 800 mg daily or reduce to as low as 200 mg daily after blood urate level has been controlled.
Overdosage-
Symptoms
Nausea, vomiting, diasrrhea,epigastric pain, ataxia, laboured respiration, convulsions, coma. Possible symptoms seen with other pyrozolidine derivatives, anemia, jaundice, ulceration.
Treatment
1. No specific antidote
2. Treatment includes usual supportive measures.
Missed dose-
1. If you miss a dose of this medicine, take it as soon as possible.
2. However, if it is almost time for next dose, skip the missed dose and go back to your regular dosing schedule.
3. Do not double doses.
Patient Information:
1.May cause GI upset; take with food,milk or antacids
2 Avoid aspirin and other products containing salicylates which may antagonise
the action of sulfinylpyrazone.
3. Drink at least 10 to 12 glasses ( 8 ounzes each ) of fluid daily
Ref - USP PDI Vol II 17th Edition (1997)
SULFINPYRAZONE - SYSTEMIC
1.Allergies-
Tell your doctor if you have ever had any unusual or allergic reaction to
sulfinpyrazone or to aspirin, oxyphenbutazone or other anti-inflammatory
analgesics. Also tell your healthcare care professional if you are allergic
to any other substances such as foods. preservatives or dyes.
2.Pregnancy-
Sulfinpyrazole has not shown to cause problems in humans.
3. Breast-feeding-
It is not known whether sulfinpyrazone passes into breast milk.
4.Children-
There is no specific information comparing use of sulfinpyrazone in children
with use in other age groups.
5.Older adults-
There is no specific information comparing use of sulfinpyrazone in the elderly
with use in other age groups.
6. Other medicines-
When you are taking sulfinpyrazone it is especially important to tell your doctor
if you are using any other medicines.
7. Other medical problems-
The presence of other medical problems may affect the use of sulfinpyrazone.
Make sure you tell your doctor if you have any other medical problems
Pharmacology/ Pharmacokinetics:
Pharmacology:
Sulfinylpyrazone,a pyrazolidone is a potent uricsuric which also has antithrombitic and platelet inhibitory effects.
Pharmacokinetics:
Well absorbed after oral administration. The plasma half-life is about 2.2 to 3 hours. About one-half of the administerd dosage appears in the urine unchanged.
Interaction with Food:
Not significant
Pregnancy and lactation:
Pregnancy-
Use only when clearly needed and when the potential benefits outweigh the potenntial hazards to the fetus.