Cefadroxil + Probenecid Pharmacology

Cefadroxil + Probenecid

About Cefadroxil + Probenecid
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Mechanism of Action of Cefadroxil + Probenecid
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Pharmacokinets of Cefadroxil + Probenecid
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Onset of Action for Cefadroxil + Probenecid
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Duration of Action for Cefadroxil + Probenecid
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Half Life of Cefadroxil + Probenecid
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Side Effects of Cefadroxil + Probenecid
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Contra-indications of Cefadroxil + Probenecid
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Special Precautions while taking Cefadroxil + 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 Cefadroxil + Probenecid
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Interactions for Cefadroxil + Probenecid
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Typical Dosage for Cefadroxil + Probenecid
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Schedule of Cefadroxil + Probenecid
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Storage Requirements for Cefadroxil + Probenecid
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Effects of Missed Dosage of Cefadroxil + Probenecid
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Effects of Overdose of Cefadroxil + Probenecid
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Cefadroxil

About Cefadroxil
First Generation Cephalosporin, para-hydroxy derivative of cefalexin, Oral broad-spectrum antibiotic
Mechanism of Action of Cefadroxil
Cefadroxil is a 1st generation cephalosporin which exerts its bactericidal action against both gram positive & gram negative organisms by inhibiting bacterial cell wall synthesis. Cefadroxil 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 Cefadroxil

Pharmacokinets of Cefadroxil
Absorption: well absorbed orally, Distribution: widely distributed, Metabolism: not metabolized, Excretion: excreted mainly through urine; & small amount is excreted in breast milk.
Onset of Action for Cefadroxil
Within one hour
Duration of Action for Cefadroxil
Up to16 hours
Half Life of Cefadroxil
N/A
Side Effects of Cefadroxil
1.Nausea
2.Vomiting
3.Diarrhea
4.Gastritis
5.Super infection
6.Candidiasis
7.Rash
8.Hypersensitivity reactions
9.Angioedema
10.Vaginitis
11.Neutropenia
12.Thrombocytopenia
13.Headache
14.Dizziness
15.Hallucinations
16.Nephritis
17.Elevated liver enzymes.
Contra-indications of Cefadroxil
1.Hypersensitivity to cephalosporins
2.Porphyria
3.Neuromuscular disorders.
Special Precautions while taking Cefadroxil
1.Renal impairment
2.Patient allergic to penicillins
3.Neuromuscular disorders
Pregnancy Related Information
Use with caution.
Old Age Related Information
May be used.
Breast Feeding Related Information
Use with caution.
Children Related Information
May be used.
Indications for Cefadroxil
1. Urinay tract infections
2. Tonsillitis & Pharyngitis
3. Skin &soft tissue infections
4. Otitis media.
Interactions for Cefadroxil
Aminoglycosides (Gentamycin, Tobramycin): Nephrotoxicity of aminoglycosides potentiated.
Oral anticoagulants: Hypoprothrombinaemic effect potentiated, bleeding complications may occur.
Bacteriostatic Agents like Chloramphenicol: Decrease efficacy of Cefadroxil.
Probenecid: Slows tubular excretion and this enhances efficacy.
Frusemide & Ethacrynic Acid: Potentiate Nephrotoxicity of Cefadroxil.
Urine Glucose: False positive with Benedicts solution and Fehlings solution.
Direct Coomb?s Test: False positive.
Urinary 17-Ketosteroid values: Falsely elevated values.

Typical Dosage for Cefadroxil
Adults:500mg to 1gm 12 hourly
Children:30mg/kg/day two times daily
Schedule of Cefadroxil
H
Storage Requirements for Cefadroxil
Store in a cool place.

Effects of Missed Dosage of Cefadroxil
Take the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose.
Effects of Overdose of Cefadroxil
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
N/A
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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