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 states 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 are available in the form of tablets, capsules and even powder for suspension.
Pharmacological action of a medicinal substance
How does Probenecid work? Instructions for use, reviews claim that this is an anti-gout agent that can suppress the reabsorption of uric acid in the renal tubules and significantly increase its excretion.
According to experts, a significant increase in the excretion of uric acid under the influence of the substance in question can lead to an increase in the process of its release from tophi into the blood, which ultimately causes the development of an acute attack of gout.
Also, the drug "Probenecid", instructions for use of which are described below, often helps to delay the excretion of other drugs by the kidneys, increasing their concentration in plasma. This allows you to use the agent in question as an additional medication during antibiotic therapy.
Kinetic characteristics
Is Probenecid absorbed? After oral administration, it is completely absorbed from the gastrointestinal tract. At the same time, the peak concentration of probenecid in the blood is reached after three hours, and its protein binding is about 85-96%.
Where does the drug in question break down? According to the instructions, it is metabolized in the liver. This forms the main acylglucuronide and other metabolites.
Probenecid is excreted by the kidneys through active secretion of the proximal tubules and glomerular filtration. About 75-86% of metabolites are found in the patient's urine, and the rest is excreted unchanged (depending on the rate of urine flow and its acidity).
Indications
What diseases does Probenecid treat? Instructions for use states that such a remedy effectively manifests itself in the treatment of hyperuricemia in chronic gout, as well as hyperuricemia when using diuretics.
It is impossible not to say that as an additional remedy this medication is prescribed for antibiotic treatment with penicillins and cephalosporins.
Contraindications
In what cases is it prohibiteduse "Probenecid"? Instructions for use indicate such contraindications of the drug as:
- porphyria;
- Acute gout attack;
- pregnancy period;
- urolithiasis (including the presence of urate stones);
- children under two years of age;
- abnormalities in peripheral blood tests;
- hypersensitivity to probenecid;
- secondary hyperuricemia, which is due to the use of chemotherapeutic agents or a tumor process.
Medication "Probenecid": instructions for use
Analogues of this tool will be listed below.
For 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 exactly doubled.
If the therapeutic effect is insufficient, 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.
During an antibiotictreatment with cephalosporins and penicillin preparations in adult patients, the medication in question is prescribed 500 mg four times a day.
In children aged two years, the initial dose of the drug should be 25 mg per kg of body weight, followed by an increase to 40 mg per kg. The interval between doses of this medicine is 6 hours.
In the treatment of gonorrhea, Probenecid is allowed to be used at a dosage of 1 g half an hour before the parenteral administration of the antibiotic.
Side effects
What negative reactions can Probenecid cause? The instructions that come with the drug indicate the following side effects:
- pruritus, anorexia, nephrotic syndrome, sore gums;
- headache, fever, dizziness;
- urticaria, nausea, frequent urination, vomiting;
- leukopenia, Stevens-Johnson syndrome, liver necrosis, alopecia;
- anaphylactic shock, dermatitis, anemia, hot flashes;
- hemolytic anemia, exacerbation of gout, aplastic anemia.
Drug interaction
According to the instructions, such an active substance as probenecid can disrupt the excretion and increase the concentration in the blood of drugs such 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 of penicillamine and nitrofurantoin in the urine, which helps to reduce their therapeutic effect in cystinuria and urinary tract infections, respectively.
The drug Probenecid causes an increase in the excretion of aminohyppuric acid, phenylsulfonthalein, 5-hydroxy-indoleacetic acid and sulfobromphthalein, 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 mentioned substance does not reduce the synthesis of uric acid, but only increases its excretion by the renal system. The resulting hyperuricosuria may increase the risk of nephropathy.
With extreme caution, the drug in question should be prescribed to persons with peptic ulcer disease and chronic renal failure. In the latter case, probenecid may be ineffective.
Using this medication to treat chronic gout may cause an acute attack of gout and increase the growth of kidney stones.
Hemolytic anemia can occur in people with G6PD deficiency.
Overdose of probenecid causes CNS excitation, contributes to the development of seizures, and can also lead toto death due to respiratory failure.
It is necessary to avoid the simultaneous use of probenecid with Ketorolac and salicylates.
People taking this drug need low doses of Thiopental, an anesthetic drug.
When using methotrexate and probenecid in parallel, the dose of the former should be reduced in order to reduce its side effects.
A false-positive urinalysis for glucose may occur while taking this medication.
Analogs, synonyms
What can replace the drug "Probenecid"? Analogues of this tool can be purchased at any pharmacy. These include the following: Fitolizin, Citrokas, Uronefron, Uroholum, Baitach, Cyston, Cital, Fitolit, Urochol and others.
As for synonyms, they include a drug such as Santuril.
Reviews about the antigout remedy
Unfortunately, there are not very many consumer reviews about Probenecid. However, there are plenty of reports about the action of Santuril. Patients claim that this medication works well in the treatment of hyperuricemia in chronic gout, as well as hyperuricemia when using 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 also has negative sides. Consumers tothey carry too many side effects and contraindications.
