Probenecid ( *** ) - @ Agents for Gout
Drug Name:Probenecid ( *** ) - @ Agents for Gout
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Interaction with Food
Pregnancy and lactation
Drug Interaction:
Interacting drugs-summary
Probenecid +
Acyclovir
decreased acyclovir clearance and increased bioavailabilty following
IV use may occur
Allopurinol
beneficial interaction. Coadministration may increase uric acid lowering
effect
Barbiturates
anesthesia produced by thiopental extended or acheived
at lower rate
Benzodiapine
a more rapid onset or prolonged benzodiapine effect occur
Clofibrate
acculmulation of clofibric acid (active metabolite of clofibrate ) occur
leading to higher steady-state serum concentrations
Dapsone
probenecid reduces urinary excretion of dapsone metabolites
increasing plasma concentrations
Dyphylline
increased half-life and decreased clearance of dyphylline occur.
Beneficial in extending the dyphylline dosing interval
Methotrexate
methrotrexate plasma levels, therapeutic effects and toxicity
enhanced
NSAIDs
NSAIDs plasma levels increased, and toxicity enhanced
Penicillamine
pharmocolgical effect of Penicillamine attenuated
Zidovudine
increased zidovudine bioavailabilty ; cutaneous eruptions accompanied
by systemic symptoms including malaise, myalgia or fever have occured
Sulfonylureas
hypoglycemic effect of the sulfonylureas enhanced
due to various mechanisms
Zidovudine
increased zidovudine bioavailability, cutaneous eruptions accompanied
by systemic symtpoms including malaise, myalgia, or fever have
occurred
Salicylates +Probenecid
coadmin. may inhibit the urocosuric action of either drug alone
Indication:
Gouty arthiritis
Adverse Reaction:
Headache, anorexia, nausea, vomiting, urinary frequency, hypersensitivity reactions, nephrotic syndrome, hepatic necrosis, aplastic anemia, exacerbation of gout, uric acid stones with without haematuria, renal colic or costovertebral pain.
Contra-Indications:
Hypersens to probenecid,children below 2 years of age, blood dyscrasias, uric acid kidney
stones. Do not start therapy until an acute gouty attack has subsided.
Special precautions:
Haematuria, renal colic, costovetebral pain and formation of urate stones associated with use in gouty patients may be prevented by alkalisation of urine and liberal fluid intake. Monitor acid balance.
Alkilinization of urine- hematuria,renal colic, costovertebral pain and formation of urate stones associated with use in gouty patients may be prevented by alkalization of urine and liberal fliud intake. Monitor acid-base balance.
Peptic ulcer history- use with caution.
Warnings-
Exacerbation of gout- following therapy with probenecid may occur, in such cases , colchicine or other appropiate therapy is advisable.
Hypersensitivity- rarely severe allergic reactions and anaphylaxis have occured. Most of these occur within several hours of aftere readministration following prior use of the drug. The appearance of hypersentivity reactions requires cessation of therapy.
Pregnancy- use only when claerly needed and when potential benefits outweigh potentail hazards to the fetus.
Children- do not use in children < 2 years.
Dosages/ Overdosage Etc:
Indications:
Hyperuricemia associated with Gout, Gouty athiritis.
Dosage:
Adults- 0.25mg twice daily for a week followed by 0.5g twice daily. Thereafter, reduce dose in
case of gastric intolerance.
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. Avoid taking aspirin or other salicylates which may antagonize the effects of probenicid.
2. May cause GI upset, may be taken with food or antacids. If nausea, vomiting or loss of
appetite persists, notify physician
3. Drink plenty of water, at least 6 to 8 full glasses daily, to prevent development of kidney stones.
4.Allergies- tell your doctor if you have ever had any unusual or allergic reaction to probenecid.
Also tell your doctor if you are allergic to any other substances, such as foods, presevatives or dyes.
5.Pregnancy - probenecid has not been shown to cause birth defects or other problems in humans.
6.Breast feeding- probenecid has not been reported to cause problems in nursing babies
7. Children - studies on the effects of probenecid in patients with gout have been done only in adults. Gout is very rare in children.
8.Elderly- no specific information comparing use of probenecid in the elderly with use in other age groups.
9. Other medicines -
Aminoplastics - chance of serious side effects may be increased
Aspirin or other salicylates- these medicines amy keep the probenecid from working properly for treating gout
Heparin - probenecid may increase the effects of heparin which increases the chance of side effects
Indomethicin- or
Ketoprofen or
Methotrexate - probenecid may increase the blood levels of these medicines which increases the chance of side of side effects
Medicines for infection including tuberculosis- probenecid may increase the blood levels of many of these medicines
Nitrofurantoin- probenecid may keep nitrofurantoin from working properly
Zidovudine - probenecid increases the blood levels of zidovudine and may allow lower doses of zidovudine
to be used. Chances of side effects is also increased.
10. Other medical problems -
Tell your doctor if you have any other medical problems especially -
Blood disease or
Cancer or
Kidney disease or stones or
Stomach ulcer - chance of side efects may be increased
11. Missed dose -
If you miss a dose of this medicine, take it as soon as possible. however, if it is almost time for the next dose, skip the missed dose. Do not double doses.
12. Storage -
Keep out of reach of children. Store away from heat or direct sunlight. Do not store
the capsule in bathroom, near the kitchen sink, or in other damp places.
13. Outdated medicines -
Do not keep outdated medicine or medicine no longer needed. Be sure that any
discarded medicine is out of reach of children.
Pharmacology/ Pharmacokinetics:
Pharmacology:
A uricosuric acid and renal tubular blocking agent, probenecid inhibits the decreasing serum reabsorption of urate, thus increasing the urinary excertion of uric acid and decreasing serum uric acid levels.
Pharmacokinetics:
Probenicid is well absorbed after oral administration and produces peak plasma concentrations in 2 to 4 hours. The half life is dose dependent and varies from less than 5 to more than 8 hours. Probenecid is hydroxylated to active metabolites and is excreted in the urine primarily as metabolites
Interaction with Food:
Can be taken with food.
Pregnancy and lactation:
Pregnancy: Use only when clearly needed.
Children: Do not use in children below 2 years of age.
