Probenecid Pharmacology


About Probenecid
Uricosuric, Antigout .
Mechanism of Action of Probenecid
Probenecid is a uricosuric agent. It increases the uric acid excretion by inhibiting the tubular reabsorption of uric acid and results in a decreased serum level of uric acid.
Antibiotic therapy adjunct: Probenecid is a competitive inhibitor of the secretion of weak organic acids such as Penicillins and some of the cephalosporin antibiotics, at the proximal and distal renal tubules. It thereby increases blood concentrations of these antibiotics, increases their elimination half-life, and prolongs their duration of action
Pharmacokinets of Probenecid
Absorption: It is completely absorbed after oral administration.
Distribution: Probenecid is widely distributed throughout the body
Metabolism: It is metabolised to active metabolite in the liver
Excretion: Probenecid and its active metabolites are excreted mainly in the urine. Probenecid is actively reabsorbed.
Onset of Action for Probenecid
Within 60 minutes
Duration of Action for Probenecid
1 day
Half Life of Probenecid
3 - 12 hours
Side Effects of Probenecid
1. Nausea
2. Vomiting
3. Headache
4. Dizziness
5. Anorexia
6. Sore gums
7. Urinary frequency
8. Renal colic
9. Nephrotic syndrome
10. Anaemia
11. Dermatitis
12. Pruritis
13. Flushing
14. Fever

Contra-indications of Probenecid
1. Hypersensitivity to Probenecid
2. Uric acid kidney stones
3. Blood dyscrasias
4. Acute gout
Special Precautions while taking Probenecid
1. Renal impairment
2. Peptic ulcer
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Below 2 years: contraindicated
NEONATES: contraindicated
Indications for Probenecid
1. Gout
2. Gouty arthritis
3. Along with antibiotics (Stimulate the action of some antibiotics)
Interactions for Probenecid
Acyclovir: Increased bioavailability of acyclovir may occur.
Allopurinol: Co-administration may increase uric acid lowering effect.
Barbiturate: Efficacy of thiopentone enhanced.
Benzodiazepines: More rapid or more prolonged benzodiazepine effect may occur.
Clofibrate: Increase in serum concentration of clofibric acid may occur.
Dapsone: Increased accumulation of dapsone may occur.
Methotrexate: Enhanced efficacy & toxicity of methotrexate.
NSAIDs: Increased plasma levels and toxicity of NSAID.
Penicillamine: Efficacy of penicillamine attenuated.
Sulfonylureas: Increased half-life of sulfonylureas.
Zidovudine: Bioavailability of zidovudine increased.
Salicylates: May result in inhibition of uricosuric effect.
Lab. Tests: False diagnosis of glycosuria. False high determination of theophylline by using Schack and Waxler technique. Probenecid may inhibit renal clearance of phenoelulonphtha-lein (PSP), 17 ketosteroids and sulfo-bromophthalein (BSP).

Typical Dosage for Probenecid
Gout: Initial dose: 500mg / day in 2 divided doses for 1 week followed by 1g /day if needed dosage can be increased by 500 mg/day every 1 month up to 2- 3 g/day.
Adjunct to penicillin or cephalosporin therapy: 2 g / day in 4 divided doses.
Gonorrhoea, uncomplicated: 1 g (as a single dose) 30 min before IM Penicillin and along with oral penicillin.
Neurosyphilis: 2g / day in 4 divided doses with penicillin G procaine aqueous
Pelvic inflammatory disease: 1 g (as a single dose) along with Cefoxitin,

Adjunct to penicillin or cephalosporin therapy: Pediatric, 2-14 years, initial: 25 mg/kg /day followed by 40mg/kg/day in 4 divided doses.
For children 50 kg or more: give adult dosage
Schedule of Probenecid
Storage Requirements for Probenecid
Store at room temperature. Protect from heat and light. Keep out of the reach of children
Effects of Missed Dosage of Probenecid
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Probenecid
Give supportive measures and symptomatic treatment. Drug can be removed from the body by inducing emesis and by gastric lavage. Seizure can be controlled by intravenous administration of Phenobarbital and Phenytoin.

Home Delivery for Probenecid in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including probenecid.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for probenecid and other medicines and health products. Home delivery services for probenecid may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take probenecid only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for probenecid before they complete the sale. You can get this information while placing the order for probenecid with the pharmacy.

Probenecid is a generic medicine name and there are several brands available for it. Some of the brands for probenecid might be better known than probenecid itself. If the pharmacy that's willing to deliver medicines to your home doesn't have probenecid in stock, you can ask for one of the branded alternatives for probenecid.