8-Kefpod 06
8-Kefpod 06
8-Kefpod 06
Cephalosporin (1)
-lactum antibiotics containing 7aminocephalosporanic acid nucleus Classification: Based on antibacterial activity 1st generation- good activity against gram positive & relatively modest activity against gram negative
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Cephalosporin (2)
2nd generation- increased activity against gram negative 3rd generation- increased spectrum of activity against gram negative, but less active against gram positive than 1st generation 4th generation- extended spectrum of activity against gram positive & negative
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Cephalosporin (3)
Generation Example Cephalexin Cephalothin Cefuroxime Cefaclor Cefotaxime* Ceftriaxone Cefpodoxime proxetil* Cefepime Cefpirome
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Spectrum Mostly gram positive Few gram negative Covers most gram negative Increased spectrum for gram negative Less active against gram positive Extended spectrum of activity
First
Second
Third
Fourth
Cefpodoxime proxetil
CH2OCH 3
Methoxymethyl group improves the antibacterials activity against gram+ve bacteria and increases the GI stability.
Cefpodoxime proxetil
3rd generation, extended spectrum, semisynthetic, oral cephalosporins Prodrug- active metabolite is cefpodoxime Active against wide spectrum of gram positive & gram negative organisms Stable against many -lactamases producing organisms
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Mechanism of Action
Inhibition of bacterial cell wall synthesis
Binds to PBPs & inhibits transpeptidation reaction involved in final step in synthesis of bacterial cell wall Also binds to the inhibitor of murein hydrolase which causes lysis of bacterial cell
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Staphylococcus saphrophyticus
Streptococcus pneumoniae (excluding penicillinresistant) Streptococcus pyogenes
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Cefixime
(MIC90 mcg/mL)
Cefaclor
(MIC90 mcg/mL)
Gram Positive Organisms Staph. aureus Strep. pyogenes Strep. pneumoniae Strep. agalactae H. influenzae 2 0.02 0.02 >0.12 0.25 32 0.13 0.13 0.28 0.25 8 0.25 0.25 32 16
M. catarrhalis
K. pneumoniae
0.125
0.125
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0.06
0.5
1
8
Pharmacokinetics
Rapidly absorbed from GIT & de-esterified to its active metabolite, cefpodoxime Bioavailability 50% Cmax = 1.4 mcg/mL (100 mg) 2.3 mcg/mL (200 mg) 3.9 mcg/mL (400 mg) T1/2 = 2.09 to 2.84 Plasma Protein Binding = 21-29% Food enhances absorption
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Pharmacokinetics
Distribution: Skin-blister fluid: 200 mg BD for 5 days-mean maximum concentration 1.6 mcg/mL Tonsil tissue: 100 mg single dose-0.24 mcg/mL at 4 hrs & 0.09 mcg/mL at 7 hrs (exceed MIC90 for S. pyogenes) Lung tissue: 200 mg single oral dose- 0.63 mcg/mL at 3 hrs; 0.52 mcg/mL at 6 hrs & 0.19 at 12 hrs (exceed MIC90 for S. pneumoniae & H. influenzae)
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Pharmacokinetics
Metabolism: Minimal metabolism of cefpodoxime Most drug excreted in urine as intact (29-33%) & metabolites Renal Failure: Elimination reduced in sever renal impairment (Creatinine clearance <50
mL/min)
Hepatic Failure: No dosage adjustment is recommended Elderly Patients: Do not require dosage adjustment if normal renal function
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Indications (1)
Treatment of infections caused by susceptible strains of microorganisms Acute otitis media Pharyngitis & Tonsillitis Community-acquired pneumonia Acute bacterial exacerbation of chronic bronchitis (AECB)
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Indications (2)
Acute, uncomplicated urethral & cervical gonorrhea Acute, uncomplicated ano-rectal infections in women Uncomplicated skin & skin structure infections (SSTIs) Acute maxillary sinusitis Uncomplicated urinary tract infections
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Contraindications
Patients with known allergy to cefpodoxime or cephalosporin group Warnings: Allergy to penicillin group of antibiotics H/O severe antibacterial associated diarrhea
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Precautions
Renal insufficiency Prolonged use Pregnancy & Lactation: Pregnancy category B Use only if clearly indicated Paediatric: Safety & efficacy not established in infants <2 months of age Elderly: No dose adjustment in patients with normal renal function
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Drug Interactions
Antacids: High doses decreases absorption of cefpodoxime Probenecid: Decrease renal excretion of cefpodoxime
Adverse Reactions
Well tolerated in various clinical trials using recommended dosage range (100400 mg BD)
Most were transient & mild to moderate in severity in clinical trials Diarrhea Nausea & Vomiting Abdominal pain
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Dosage
Tablets administered with food to enhance absorption Suspension may be given without regard food Adult & Adolescents (>12 yrs) 100-400 mg BD for 5-14 days Children (2 months to <12 yrs) 5 mg/kg / dose BD (Max:200 mg/dose) for 5-10 days
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Dosage Schedule
Children (2 months to <12 yrs)
Type of Infection Total daily dose (mg/kg/day) Frequency (mg/kg) Duration (Days)
5-10
10
5-10 14 10
Uncomplicated gonorrhea
SSTI Acute maxillary sinusitis Ucomplicated UTI
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Hospital-acquired pneumonia
Pneumonia caused by Gram-negative bacilli Sepsis of unknown origin Sepsis caused by Gram-negative bacilli Pyelonephritis Arthritis caused by Gram-negative bacilli
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J of Antimicrobial Chemotherapy1994;33:169-171
Clinical Trial
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Drug intervention :
Cefpodoxime in 396 patients-5mg/kg Cefixime in 380 patients,-4 mg/kg
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MIC (mcg/mL )
H. influenza M. catarrhalis S. pneumoniae
Cefpodoxime
0.06-0.12 0.12-0.25 0.03
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Cefixime
0.06 0.12 0.25
Cefixime
Cure
Improvement
61.3%
35.7%
43%
43.8%
Clinical success
Failure
97.0%
3.0% Bacterial out come
86.8%
13.2%
Eradication Failure
93.4% 6.6%
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82.9% 17.1%
Cefpodoxime cefixime
Good
Fair
Poor
Good
Fair
Poor
Cefpodoxime Dose
Clinical cure Bacterial eradication
Ceftriaxone
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Drug intervention:
Cefpodoxime proxetil -10mg/kg BD for 10 days Amoxicillin/clavulanate -40mg/10mg per kg TID for 10 days
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Clinical efficacy for Cefpodoxime proxetil b.i.d. is Equivalent to Amoxicillin/Clavulanate t.i.d. in AOM
Adverse events
40% 35% 30% 25% 20% 15% 10% 5% 0%
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Conclusion
Cefpodoxime proxetil is well tolerated Superior alternative to other third generation cephalosporins Expanded spectrum of activity First line antimicrobial in pediatric patients of LRTIs
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