Cefalexin + Probenecid Pharmacology

Cefalexin + Probenecid

About Cefalexin + Probenecid
N/A
Mechanism of Action of Cefalexin + Probenecid
N/A
Pharmacokinets of Cefalexin + Probenecid
N/A
Onset of Action for Cefalexin + Probenecid
N/A
Duration of Action for Cefalexin + Probenecid
N/A
Half Life of Cefalexin + Probenecid
N/A
Side Effects of Cefalexin + Probenecid
N/A
Contra-indications of Cefalexin + Probenecid
N/A
Special Precautions while taking Cefalexin + Probenecid
N/A
Pregnancy Related Information
Contraindicated; since Probenecid is contraindicated in pregnancy, the combination generic cannot be used in pregnancy.
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution;Caphalexin and Probenecid are used with caution in breast feeding mother. So the combination generic is used with caution breast feeding
Children Related Information
N/A
Indications for Cefalexin + Probenecid
It is a combination of first generation Cephalexin and antigout drug Probenecid which is used to augment the action of Cephalexin.
1.Respiratory tract infections
2.Gonorrhea
3.Dental infections
4.Skin & soft tissue infections
5.Urinary tract infections
Interactions for Cefalexin + Probenecid
N/A
Typical Dosage for Cefalexin + Probenecid
Adults: 1 tablet to be taken 2 times daily.Each tablet contains Cephalexin 250mg + Probenecid 250mg or Cephalexin 500mg + Probenecid 500mg
Schedule of Cefalexin + Probenecid
N/A
Storage Requirements for Cefalexin + Probenecid
N/A
Effects of Missed Dosage of Cefalexin + Probenecid
N/A
Effects of Overdose of Cefalexin + Probenecid
N/A

Cefalexin

About Cefalexin
A first-generation cephalosporin antibiotic.
Mechanism of Action of Cefalexin
Cephalexin is a 1st generation cephalosporin which exerts its bactericidal action against both gram positive & gram negative organisms by inhibiting bacterial cell wall synthesis. Cephalexin 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 Cephalexin

Pharmacokinets of Cefalexin
Absorption: well absorbed orally, food delays absorption, Distribution: widely distributed, Metabolism: not metabolized, Excretion: excreted mainly through urine; & small amount is excreted in breast milk
Onset of Action for Cefalexin
Within 1hour
Duration of Action for Cefalexin
Up to 12 hours
Half Life of Cefalexin
N/A
Side Effects of Cefalexin
1.Nausea
2.Vomiting
3.Diarrhea
4.Gastritis
5.Super infections
6.Candidiasis
7.Rash & hypersensitivity reactions
8.Joint pain
9.Vaginitis
10.Neutropenia
11.Tthrombocytopenia
12.Headache
13.Dizziness
14.Hallucinations
15.Nephritis
16.Elevated liver enzymes
Contra-indications of Cefalexin
1.Hypersensitivity to cephalosporins
2.Porphyria
3.Neuromuscular disorders.
Special Precautions while taking Cefalexin
1.Renal impairment
2.Those allergic to penicillins
3. Neuromuscular disorders

Pregnancy Related Information
May be used
Old Age Related Information
May be used
Breast Feeding Related Information
Use with caution
Children Related Information
May be used
Indications for Cefalexin
1.Respiratory tract infections
2.Urinary tract infections
3.Surgical prophylaxis
4.Skin infections`
5.Joint & bone infections
6.Otitis media`
7.Reproductive tract infections`
Interactions for Cefalexin
Probenecid: Excretion of cephalexin reduced.
Aminoglycosides: Enhance half-life and potentiate nephrotoxicity.
Typical Dosage for Cefalexin
Adults: 0 .25 to 1gm orally three times daily or four times daily
Children: 25 to 100mg/kg/day orally four times daily
Infections caused by susceptible organisms:
Adults: 0.25 to 1gm orally four times daily
Children: 25 to 50mg/kg/day orally four times daily
Otitismedia:
Adults: 0.25 to 1gm orally four times daily
Children:75 to 100 mg/kg/day four times daily
Schedule of Cefalexin
H
Storage Requirements for Cefalexin
Store in a cool place.
Effects of Missed Dosage of Cefalexin
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 Cefalexin
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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