What is Probenecid? Instructions for use, synonyms, analogues and indications for the use of this medication will be indicated below.
Form, composition
What is probenecid? Instructions for use claims that this is an active substance that is part of many drugs. You can buy such medicines in any pharmacies at a very reasonable price. They can be in the form of tablets, capsules, and even powder for suspension.
Pharmacological action of a drug substance
How does the drug "Probenecid"? Instructions for use, reviews claim that this is an antigout agent that can suppress the reabsorption of uric acid in the renal tubules and significantly enhance its excretion.
According to experts, a significant increase in urinary acid excretion under the influence of the substance in question can lead to an increase in its release from tofus into the blood, which ultimately will cause the development of an acute attack of gout.
Also, the drug "Probenecid", the instructions for use of which are described below, often contributes to the delay in kidney excretion of other drugs, increasing their concentration in plasma. This allows you to use the drug in question as an additional medication during antibiotic therapy.
Kinetic characteristics
Is Probenecid absorbed? After oral administration, it is completely absorbed from the digestive tract. In this case, the peak concentration of probenecid in the blood is reached after three hours, and its binding to proteins is about 85-96%.
Where does the cleavage of the drug in question occur? According to the instructions, it is metabolized in the liver. In this case, the main acylglucuronide and other metabolites are formed.
Kidneycid is excreted by the kidneys through active secretion of the proximal tubules and glomerular filtration. About 75-86% of metabolites are found in the patientโs urine, and the rest is excreted unchanged (depending on the speed of the urine flow and its acidity).
Indications
What diseases does probenecid cure? Instructions for use states that such a tool is effective in the treatment of hyperuricemia in chronic gout, as well as hyperuricemia when using diuretics.
We can not say that as an additional tool, this medication is prescribed for antibiotic treatment with penicillins and cephalosporins.
Contraindications
In what cases is it prohibited to use Probenecid? Instructions for use indicate contraindications to the drug, such as:
- porphyria;
- acute gout attack;
- pregnancy period;
- urolithiasis (including the presence of urate stones);
- children's age up to two years;
- abnormalities in peripheral blood tests;
- hypersensitivity to probenecid;
- secondary hyperuricemia, which is caused by the use of chemotherapeutic agents or a tumor process.
Medication "Probenecid": instructions for use
Analogs of this tool will be listed below.
In chronic gout, the drug in question should be taken at a dose of 250 mg twice a day for one month. A week after the start of treatment, this amount can be increased exactly twice.
With insufficient therapeutic effect, the dosage can be increased every month by 500 mg. It should be remembered that the maximum dose of this medication is 2 g per day.
If within six months the patient did not experience acute attacks of gout, and the level of urate in the blood did not exceed the permissible level, then the indicated amount of the drug can be gradually reduced to the minimum effective (for example, by 500 mg every six months).
The dosage of probenecid in people receiving diuretics or pyrazinamide may be increased.
When carrying out antibiotic treatment with cephalosporins and penicillin preparations in adult patients, the medication in question is prescribed 500 mg four times a day.
In babies from the age of two years, the initial dose of the medication should be 25 mg per kg of weight, with a subsequent increase to 40 mg per kg. The time interval between doses of this medicine is 6 hours.
In the treatment of gonorrhea, the Probenecid drug is allowed to be used in a dosage of 1 g half an hour before parenteral administration of the antibiotic.
Side effects
What negative reactions can the Probenecid medication cause? The instructions attached to the drug indicate the following side effects:
- itching, anorexia, nephrotic syndrome, sore gums;
- headache, fever, dizziness;
- urticaria, nausea, increased urination, vomiting;
- leukopenia, Stevens-Johnson syndrome, liver necrosis, alopecia;
- anaphylactic shock, dermatitis, anemia, hot flashes;
- hemolytic anemia, exacerbation of gout, aplastic anemia.
Drug Interactions
According to the instructions, an active substance such as probenecid, can disrupt excretion and increase the concentration in the blood of such medicines as Captopril, Acyclovir, sulfonamide conjugates, Paracetamol, sulfonylurea derivatives, Naproxen, aminosalicylates, Methotrexate, Lorazepam, Meclofenamate, Rifampicin, Indomethacin, Zidovudine, and Ketoprofen.
It should also be noted that the drug in question reduces the concentration in the urine of penicillamine and nitrofurantoin, which helps to reduce their therapeutic effect in cystinuria and urinary tract infections, respectively.
The drug "Probenecid" causes an increase in the excretion of aminogippuric acid, phenylsulfontalein, 5-hydroxy-indolylacetic acid and sulfobromophthalein, as well as a decrease in the excretion of steroid hormone metabolites with urine.
Special information
What should I know before using medicines with probenecid? According to the instructions, such drugs are not recommended for use in secondary hyperuricemia, which is caused by a tumor process or the use of chemotherapeutic agents, since the substance does not reduce the synthesis of uric acid, but only increases its excretion by the renal system. Hyperuricosuria developing in this case may increase the risk of nephropathy.
With extreme caution, the drug in question should be prescribed to persons with peptic ulcer and in chronic renal failure. In the latter case, probenecid may be ineffective.
When using this medication for the treatment of chronic gout, an acute attack may develop, as well as increased growth of kidney stones.
In people with G6FD deficiency, hemolytic anemia may occur.
An overdose of probenecid causes CNS excitation, promotes the development of seizures, and can also lead to death due to respiratory failure.
It is necessary to avoid the simultaneous administration of probenecid with Ketorolac and salicylates.
People taking this drug need low dosages of Thiopental, which is intended for anesthesia.
With the parallel use of methotrexate and probenecid, the dose of the first should be reduced in order to reduce its side effects.
Against the background of taking this medication, a false-positive result of a urine test for glucose is possible.
Analogs, synonyms
How can I replace the drug "Probenecid"? Analogs of this tool can be purchased at any pharmacy. These include the following: Fitolizin, Citrokas, Uronefron, Uroholum, Baytach, Cyston, Cital, Fitolit, Urohol and others.
As for synonyms, such a drug as Santuril refers to them.
Reviews for gout
Unfortunately, there are not very many consumer reviews on the drug "Probenecid". However, there are plenty of reports on the action of Santuril. Patients claim that this medication works well in the treatment of hyperuricemia with chronic gout, as well as hyperuricemia with diuretics. It is also a good remedy for acute bacterial cystitis, nonspecific urethritis, postoperative urinary tract infections and other urological problems.
It is impossible not to say that the medication in question has its negative sides. Consumers include too many side effects and contraindications.