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Apurina

Apurina - General Information

The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Apurina has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.

 

Pharmacology of Apurina

Apurina is a uricosuric and renal tubular blocking agent and is used in combination with colchicine to treat chronic gouty arthritis when complicated by frequent, recurrent acute attacks of gout. It inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits.

 

Apurina for patients

 

Apurina Interactions

When probenecid is used to elevate plasma concentrations of penicillin, or other beta-lactams, or when such drugs are given to patients taking probenecid therapeutically, high plasma concentrations of the other drug may increase the incidence of adverse reactions associated with that drug. In the case of penicillin, or other beta-lactams, psychic disturbances have been reported.

The use of salicylates antagonizes the uricosuric action of probenecid . The uricosuric action of probenecid is also antagonized by pyrazinamide.

Probenecid produces an insignificant increase in free sulfonamide plasma concentrations but a significant increase in total sulfonamide plasma levels. Since probenecid decreases the renal excretion of conjugated sulfonamides, plasma concentrations of the latter should be determined from time to time when a sulfonamide and probenecid and colchicine are co-administered for prolonged periods. Probenecid may prolong or enhance the action of oral sulfonylureas and thereby increase the risk of hypoglycemia.

It has been reported that patients receiving probenecid require significantly less thiopental for induction of anesthesia. In addition, ketamine and thiopental anesthesia were significantly prolonged in rats receiving probenecid.

The concomitant administration of probenecid increases the mean plasma elimination half-life of a number of drugs which can lead to increased plasma concentrations. These include agents such as indomethacin, acetaminophen, naproxen, ketoprofen, meclofenamate, lorazepam, and rifampin. Although the clinical significance of this observation has not been established, a lower dosage of the drug may be required to produce a therapeutic effect, and increases in dosage of the drug in question should be made cautiously and in small increments when probenecid is being co-administrated. Although specific instances of toxicity due to this potential interaction have not been observed to date, physicians should be alert to this possibility.

Probenecid given concomitantly with sulindac had only a slight effect on plasma sulfide levels, while plasma levels of sulindac and sulfone were increased. Sulindac was shown to produce a modest reduction in the uricosuric action of probenecid, which probably is not significant under most circumstances.

In animals and in humans, probenecid has been reported to increase plasma concentrations of methotrexate.

Falsely high readings for theophylline have been reported in an in vitro study, using the Schack and Waxler technique, when therapeutic concentrations of theophylline and probenecid were added to human plasma.

 

Apurina Contraindications

Hypersensitivity to this product or to probenecid or colchicine.

Probenecid and colchicine tablets are contraindicated in children under 2 years of age.

Not recommended in persons with known blood dyscrasias or uric acid kidney stones.

Therapy with probenecid and colchicine should not be started until an acute gouty attack has subsided.

Pregnancy

Probenecid crosses the placental barrier and appears in cord blood. Colchicine can arrest cell division in animals and plants. In certain species of animal under certain conditions, colchicine has produced teratogenic effects. The possibility of such effects in humans also has been reported. Because of the colchicine component, probenecid and colchicine is contraindicated in pregnant patients. The use of any drug in women of childbearing potential requires that the anticipated benefit be weighed against the possible hazards.

 

Additional information about Apurina

Apurina Indication: For the treatment of gout and high levels of uric acid in the blood
Mechanism Of Action: Apurina inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels.
Drug Interactions: Methotrexate Apurina increases the effect and toxicity of methotrexate
Aspirin The salicylate decreases the uricosuric effect of probenecid
Bismuth Subsalicylate The salicylate decreases the uricosuric effect of probenecid
Salsalate The salicylate decreases the uricosuric effect of probenecid
Zidovudine Rash, malaise, myalgia
Trisalicylate-choline The salicylate decreases the uricosuric effect of probenecid
Valganciclovir Apurina increases the effect and toxicity of ganciclovir/valganciclovir
Salicylate-magnesium The salicylate decreases the uricosuric effect of probenecid
Salicylate-sodium The salicylate decreases the uricosuric effect of probenecid
Ganciclovir Apurina increases the effect and toxicity of ganciclovir/valganciclovir
Diflunisal Apurina increases toxicity of diflunisal
Indomethacin Apurina increases the effect/toxicity of indomethacin
Ketorolac Apurina increases toxicity of ketorolac
Cefaclor Apurina increases the antibiotic's level
Cefadroxil Apurina increases the antibiotic's level
Cefamandole Apurina increases the antibiotic's level
Cefazolin Apurina increases the antibiotic's level
Cefepime Apurina increases the antibiotic's level
Cefixime Apurina increases the antibiotic's level
Cefmetazole Apurina increases the antibiotic's level
Cefonicid Apurina increases the antibiotic's level
Cefotaxime Apurina increases the antibiotic's level
Cefotetan Apurina increases the antibiotic's level
Cefoxitin Apurina increases the antibiotic's level
Cefprozil Apurina increases the antibiotic's level
Cefuroxime Apurina increases the antibiotic's level
Ceftizoxime Apurina increases the antibiotic's level
Cephalexin Apurina increases the antibiotic's level
Cephaloglycin Apurina increases the antibiotic's level
Cephalothin Group Apurina increases the antibiotic's level
Cefradine Apurina increases the antibiotic's level
Loracarbef Apurina increases the antibiotic's level
Moxalactam Derivative Apurina increases the antibiotic's level
Food Interactions: Not Available
Generic Name: Probenecid
Synonyms: Not Available
Drug Category: Uricosuric Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Probenecid: Apurina; Benecid; Benemid; Benuryl; Col-Probenecid; Colbenemid; Polycillin-PRB; Probalan; Probampacin; Probecid; Proben; Proben-C; Probenecid Acid; Probenemid; Probexin; Prolongine; Synergid R; Tubophan; Uricosid;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: 75-95%
Biotransformation: Not Available
Half Life: 6-12 hours
Dosage Forms of Apurina: Tablet Oral
Chemical IUPAC Name: 4-(dipropylsulfamoyl)benzoic acid
Chemical Formula: C13H19NO4S
Probenecid on Wikipedia: http://en.wikipedia.org/wiki/Probenecid
Organisms Affected: Humans and other mammals