Cefuroxime + Probenecid Pharmacology

Cefuroxime + Probenecid

About Cefuroxime + Probenecid
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Mechanism of Action of Cefuroxime + Probenecid
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Pharmacokinets of Cefuroxime + Probenecid
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Onset of Action for Cefuroxime + Probenecid
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Duration of Action for Cefuroxime + Probenecid
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Half Life of Cefuroxime + Probenecid
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Side Effects of Cefuroxime + Probenecid
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Contra-indications of Cefuroxime + Probenecid
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Special Precautions while taking Cefuroxime + Probenecid
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Cefuroxime + Probenecid
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Interactions for Cefuroxime + Probenecid
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Typical Dosage for Cefuroxime + Probenecid
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Schedule of Cefuroxime + Probenecid
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Storage Requirements for Cefuroxime + Probenecid
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Effects of Missed Dosage of Cefuroxime + Probenecid
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Effects of Overdose of Cefuroxime + Probenecid
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Cefuroxime

About Cefuroxime
Second Generation Cephalosporin antibiotic.
Mechanism of Action of Cefuroxime
Cefuroxime is a 2nd generation cephalosporin which exerts its bactericidal action against both gram positive & gram negative organisms by inhibiting bacterial cell wall synthesis. Cefuroxime inhibits transpeptidase & thus prevents cross linking of bacterial cell wall. Transpeptidase & associated proteins constitute various types of specific binding proteins which have affinity for cephalosporins like Cefuroxime

Pharmacokinets of Cefuroxime
Cefuroxime sodium is orally not well absorbed & should be given parenterally but Cefuroxime axetil is absorbed orally & food increases absorption rate. Distribution: widely distributed, & greater CSF penetration. Metabolism: Not metabolized, Excretion: Excreted mainly through urine & small amount is seen in breast milk.
Onset of Action for Cefuroxime
Within 1 hour
Duration of Action for Cefuroxime
12 hours
Half Life of Cefuroxime
N/A
Side Effects of Cefuroxime
1.Pain after I.M. injection & thrombophlebitis after I.V. injection.
2.Rashes & allergic manifestations
3.Vaginitis
4.Nephrotoxicity
5.Pseudo membranous colitis
6.Pruritus
7.Candidiasis
8.Glossitis
9.Nausea
10.Vomiting
11.Elevated liver enzymes
12.Neutropenia
13.Thrombocytopenia
14.Hemolytic anemia
Contra-indications of Cefuroxime
1.Hypersensitivity to Cefuroxime or other cephalosporins
2.Along with other nephrotoxic drugs
3.Along with oral anticoagulants
4.Pseudo membranous colitis
Special Precautions while taking Cefuroxime
1.Pseudomembranous colitis
2.Patients sensitive to Penicillin
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
May be used
Indications for Cefuroxime
1.Meningitis caused by H.influenzae, meningococci, pneumococci etc.
2.Gonorrhea
3.Pneumonia & Pulmonary infections
4.Infections caused by ampicillin resistant H. influenzae
5.Septicemia
6.Tonsillitis
7.Pharyngitis
8.Urinary tract infections
9.Otitis media
Interactions for Cefuroxime
Synergy with aminoglycosides.
Typical Dosage for Cefuroxime
Adults:
Oral dose: 0.25 to 0.5gm two times daily
Parenteral dose: 0.75 to 1.5gm I.M or I.V. thrice daily for 5 to 10 days.
Severe infections: 1.5gm I.M. or I.V. four times daily
Meningitis: 3gm I.M.or I.V. thrice daily
Tonsillitis, Pharyngitis, Urinary tract infections etc.: 125 to 500mg orally twice daily up to 10 days

Children:30 to 100mg/kg/day I.M or I.V. three times daily or four times daily
Meningitis: Initially 200 to 240mg/kg/day I.V. three times daily or four times daily & continue the therapy with 100mg/kg/day.
Tonsillitis, Pharyngitis, Urinary tract infections etc.:
Above 1`2 years:same as adult dose
Below 12 years: 0.125gm to 0.25gm orally twice daily for 10 days or :20mg/kg/day oral suspension twice daily for 10 days
Otitismedia: 30mg/kg/day orally twice daily
Schedule of Cefuroxime
H
Storage Requirements for Cefuroxime
Store in a cool place.
Effects of Missed Dosage of Cefuroxime
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 Cefuroxime
Symptoms of over dosage include neuromuscular disorders & some times seizure may get precipitated. Treatment includes removal of drug from the body by dialysis & supportive measures.

Probenecid

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
Contraindicated
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
Adult:
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,

Children:
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
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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.

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