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(CHEPHALOSPORIN), 1960s
Active to Gam+ve
Weak to Gram-ve, semi…
CHEPHALOSPORIN
3' Generation
Cefpodoxime //
PROXETIL
- Oral active ester prodrug of Cefpodoxime
- Highly active to:
- Enterobacteriaceae
- Streptococci
- inhibits Staphylococcal aureus
- Indications: Respiratory, Urinary, Skin, Soft tissue infections
Ceftriaxone
- Longer duration action - Half-life: 8hrs - Once or twice dose per day
- Good CSF penetration
- Excrete equally in urine and bile
- High efficacy & wide ranges:
- Bacteria meningitis - especially children
- Dose: 4g - 2g iv // child 75-100mg/kg OD 7-10days
- Multi-resistant typhoid fever
- Dose: 4g iv daily x2days - 2g/day // child 75mg/kg till 2days after fever subsides
- Complicated urinary tract infections
- Abdominal sepsis & Septicemias
- Gonnorhoea, PPNG - single dose 250mg im
- Adverse effects:- Hypoprothrombineamia & Bleeding
Cefizoxime
- Similar to Cefotaxime
- not metabolized
- Excreted by kidney at slower rate
- Half-life: 1.5-2hrs
- Dose: 5-1g 8-12hrly im/iv
Ceftazidime
- Indications:
- Pseudonomas - highly active
- Febrile neutropenic patients with: Hematological malignancy, Burns, etc
- Resistant typhoid - 20mg/kg/day
- Dose: 0.5-2g im/iv QID, Child 30mg/kg/day
- Adverse effects:
- Neutropenia
- Thrombocytopenia
- Rise in plasma transaminases
- Rise in blood urea
Cefoperazone
- Stronger activity against Pseudonomas
- Indications:
- Severe urinary infections
- Biliary infections
- Respiratory infections
- Skin soft tissue infections
- Meningitis
- Septicaemias
- Dose: 1-2g im/iv 12hrly
Cefixime
- Orally active
- Longer acting - Half-life: 3hrs
- Indications:
- Respiratory infections
- Urinary infections
- Biliary infections
- Dose: 200-400mg BD
- Side effects:
Cefotaxime
- Prototype drug
- Prominent indications:
- Meningitis of Gram-ve bacilli
- Life-threatening, resistant, hospital-acquired infections
- Septicemias
- Infections in immuno-compromised
- PPNG urethritis - single dose therapy:
- Cefotaxime 1g im + Probenecid oral
- Dose: 1-2g 6-12hrly im/iv - Children: 20-100mg/kg/day
Cefdinir
- Active against B-lactamase producing organisms
- Against respiratory pathogens - Gram+ve cocci
- Indications:
- Pneumonia
- Acute exacerbations of chronic bronchitis
- ENT - "Otorhinolaryngology"
- Skin infections
- Dose: 300mg BD
Cefibuten
- Against: Gram+ve & Gram-ve bacteria
- Stable to B-lactamase
- Indications: UTI, RTI, GIT infections
- Dose: 200mg BD or 400mg OD
4' Generation
Cefepime
- Highly resistant to B-lactamases
- Active against:
- P. aeruginosa
- Staph. aureus
- High potency
- Extended Spectrum
- Effective for // Indications:
- Hospital-acquired pneumonia
- Febrile neutropenia
- Bacteraemia
- Septicaemia
- Dose: 1-2g iv 8-12hrly
Cefpirone
- Treat serious and resistant hospital-acquired infections: Septicaemias & Lower RTIs
- Zwitter ion character - better penetration thru porin channels of Gram-ve bac.
- Resistant to B-lactamase
- Inhibits type I B-lactamsase producing Enterobacteriaceae
- More potent against Gram+ve
- Dose: 1-2g im/iv 12hourly
2' Generation
Cefoxitin
- Uses:
1) Serratia
2) Indole positve proteus
3) B. fragilis
4) Gram-ve bac - highly resistant to B-lactamases
5) Anaerobes
6) Mixed obsteric/surgical infections
7) Lung abscess
- Dose: 1-2g im/iv every 6-8hr
Cefuroxime axetil
- Ester form
- Effective orally, but incomplete absorption
- Activity depends on hydrolyses & release of Cefuroxime
- Dose: 250-500mg BD
Cefuroxime
- resistant to Gram-ve B-lactamase
- High activity:
- PPNG - single dose therapy
- Ampicillin-resistant H. influenza
- Meningitis caused by: H. influenza, Meningococci, Pneumococci
Cefaclor
- Oral route
- more active compared to 1st generation
- Against:
- H. influenza
- E. coli
- Proteus mirabillis
- Anaerobes in oral cavity
1' Generation
Cephalexin
- Similar to Cefazolin
- Orally effective
- Less active against H. influenza
- Dose: 0.25-1g 6-8hrly
- Children - 25-100mg/kg/day
Cephradine
- Orally active, but causes diarrhea
- Available for paranteral
- Dose: 0.25-1g 6-16hrly oral/im/iv
Cefazolin
- Active against most PnG sensitive:
- Streptococci
- Gonococci
- Meningococci
- More active: Klebsiella & E. coli
- Used for surgical prophylaxis
- Dose:
- Mild - 0.25g 8hourly im/iv
- Severe - 1g 6hourly im/iv
Cefadroxil
- Close congener of Cephalexin
- Dose: 0.5-1g BD
Adverse effects
- Generally well-tolerated but more toxic than Penicillin
- Pain after IM injection
- Thrombophlebitis on IV injection
- Diarrhea - alteration of gut ecology or irritation effects
- Hypersensitivity reactions
- 10% ppl who allergy to Penicillin show cross reactivity with Cephalosporin
- Nephrotoxicity
- Bleeding - Hypoprothrombinaemia
- Neutropenic & Thrombocytopenia - Ceftazidine
- Disulfram-like interaction with alcohol - Cefoperazone
Uses
- Respiratory, Urinary, Soft tissue infections
- Penicillinase-producing Staphylococcal infections
- Septicaemias - in combination with Aminoglycosides
- Surgical prophylaxis
- Meningitis:
- H. influenza
- Enterobacteriaceae
- Pseudonomas meningitis - Best treat by Ceftazidime + Gentamicin
- Gonorrhoea - PPNG
- Chancroid
- Typhoid - Ceftriaxone & Cefoperazone are fatest acting
- Mixed aerobic-anaerobic infections
- Hospital-acquired infections resistant to common antibiotics
- Dental infections
- 1960s
- Active to Gam+ve
- Weak to Gram-ve
- semi-synthetic antibiotics
- derived from Cephalosporin-C
- obtained from fungus Cephalosporium
- Bactericidal
- same MOA as Penicillin
- More active to Gram-ve
- Some are active to Anaerobes
- Highly resistant to Gram-ve B-lactamase
- Less active: Anaerobes & Gram+ve cocci
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