4- (Dipropylsulfamoyl) benzoic acid
Probenecid is a white or almost white powder that is practically insoluble in water. The molecular weight of the agent = 285.4 grams per mole.
Previously, the substance was used to reduce the intensity of secretion of various antibacterial agents by the renal tubules (penicillin for example), now the medicine has been widely used in the treatment of gout and to reduce the harm from cidofovir. The tool is released in tablet form.
Pharmacodynamics and pharmacokinetics
The substance inhibits reabsorption uric acid in the renal tubules and accelerates its excretion. In addition, Probenecid tends to delay the excretion of other drugs through the kidneys, and thereby increase their plasma concentrations. Thus, the drug increases the effectiveness of antibiotics.
After taking the tablets, the substance is quickly absorbed. Its maximum plasma concentration is observed 3 hours after administration. The product has a fairly high degree of binding to blood plasma proteins - up to 95%. Metabolism occurs in the liver, the substance has a small amount of distribution in the body. The elimination half-life is from 2 to 6 hours. Probenecid is excreted by glomerular filtration and through the proximal channels of the kidneys.
Indications for use
The medicine is used:
- for treatmenthyperuricemia in chronic gout and while taking diuretics;
- as part of complex treatment antibiotics, penicillins and cephalosporins.
The tool can not be used:
- during acute attacks gout;
- with urolithiasis, especially in the presence of urate stones in the kidneys;
- patients with porphyria;
- pregnant women
- with a violation of the picture of peripheral blood;
- children under 2 years old;
- with secondary hyperuricemia (tumors, chemotherapy);
- at allergies per substance.
The following adverse reactions to Probenecid may occur:
- vomiting anorexia, nausea, pain in the gums, Stevens-Johnson syndrome, dermatitis;
- dizzinessfrequent urination headacheincreased body temperature hives and itching on the skin;
- anemia, leukopenia, hair loss, tidesaggravation gout;
- seldom - liver necrosis, anaphylactic reactions, aplastic anemia, nephrotic syndrome.
Probenecid, instructions for use (Method and dosage)
For the treatment of chronic gout 500 mg of the drug is prescribed per day, distributed in 2 doses. This regimen is observed for 4 weeks.
If the effectiveness of treatment is low, you can switch to large dosages, increasing the daily dose by 0.5 g per month. The maximum daily dosage should not exceed 2 grams.
Also, the daily dose can be reduced with a favorable course of the disease, the absence of acute attacks and stable laboratory parameters. Correction is carried out gradually, half a gram every half year. As a result, the patient takes a minimally effective dosage.
Probenecid during treatment antibiotics cephalosporin and penicillin row appoint 0.5 g, 4 doses / day. For children, the dose is adjusted, 25 mg per kg of the child’s weight, then increased to 40 mg per kg of weight. Tablets are taken every 6 hours.
If the weight of the child is more than 50 kg, then the transition to an adult dosage regimen is acceptable.
For treatment gonorrhea the medicine is used 1 gram half an hour before the injection of an antibiotic.
Taking large doses of the drug can lead to severe excitation of the central nervous system and even death. As a treatment for overdose, it is recommended to rinse the stomach and conduct symptomatic therapy.
The substance causes accelerated elimination phenolsulfophthalein, amino hippuric acid, sulfobromophthalein, 5-hydroxy-indolylacetic acid and metabolites of steroid hormones.
When taking Probenecid, plasma concentrations increase: acyclovir, captoprilderivatives sulfonylureas, lorazepam, rifampicin, aminosalicylates, paracetamol, zidovudine, indomethacinconjugates sulfonamides, ketoprofen, naproxen, meclofenamate, methotrexate.
Also, under the influence of the drug, the concentration decreases penicillamine and nitrofurantoin in urine, their therapeutic effect is reduced.
Dosage adjustment may be required during treatment. thiopental.
When combining the drug with methotrexate it is necessary to reduce the dosage of the latter in order to reduce the risk of adverse reactions.
The drug can not be prescribed for secondary hyperuricemiadue to swelling or conduction chemotherapy. The medicine does not reduce the intensity of synthesis uric acid, the risk of development will increase nephropathy.
With extreme caution, the medicine is used if available. stomach ulcers in the history of chronic kidney disease, the substance will be ineffective.
Chronic treatment gout may cause an acute attack goutthe growth or increase of kidney stones, renal colic, hematuria.
With caution Probenecid is prescribed for patients with deficiency glucose-6-phosphate dehydrogenase.
The medicine may cause a false positive reaction to glucose.
For children, the daily dosage is adjusted depending on the weight.
During pregnancy and lactation
This substance is known to cross the placental barrier. In this regard, it is not recommended for use during pregnancy. Lactation is recommended to stop.
Preparations that contain (Analogs of Probenecid)
Analogs: Probalan, Santuril, Probenecid Biocanol.
There are few reviews on the use of the drug. However, most of them talk about the relatively good tolerability of the drug, side effects from the gastrointestinal tract and allergic reactions occasionally occur.
Probenecid price, where to buy
Buy Probenecid in a pharmacy is quite difficult. The cost of drugs on the Internet on order differs depending on the manufacturer. The price of Probenecid is about 4,500 rubles for 30 tablets of 500 mg.