Cephalosporins

β-lactum drugs.

Sturcture is almost like penicillin.

Source:Cepahlosporium(Fungus).

Classification:

Generation	Examples	Dose	Clinical use	Active against
First generation	Oral ·         Cephradine ·         Cefalexin ·         Cefradoxil Cephazolin(IV/IM)	500mg, 6hourly 0.5-2gm, 8hourly	UTI,Cellulitis, Tonsilitis,soft tissue  infection,Otitis. *Surgical prophylaxis, *Kelbsiella pneumonia *Staphylococcus infection	Gram(+)ve organisms, E.coli, Kelbsiella, Proteus
Second generation	Oral: ·         Cefuroxime, ·         Cefaclor. Parentral: ·         Cefamandol, ·         Cefoxitin.		*Sinusitis *Peritonotis. *Otitis. *Lower respiratory tract infection. *Community acquired pneumonia	Gram(+)ve organisms and H.influenza,K.pneumonia-which produce β-lactamase enzymes
Third generation	Oral ·         Cefixime ·         Cefodoxime ·         Ceftibuten Parental ·         Cefotaxime ·         Ceftriaxone ·         Moxalactum ·         Cefoperazone.	inj.125mg oral 400mg	*Gonorrhoea( caused by  N.gonorrhoea, resistent to penicillin) *UTI. *Meningitis. *Sepsis of unknown cause. *Enteric fever.	gram(+)ve & some gram(-)ve. Also pseudomonas *If meningitis caused by pseudomonas-3rd generation + Aminoglycosides
Fourth generation	Parental ·         Cefepime			*Enterobacter-resistence to 3rd generation. *P.aeruginose. *S.aurius. *H.influenzae. *S.Pneumoniae.

                           

Advantage of 3rd generation cephalosporins:

1)      Expanded gram negative coverage.

2)      Can reach the CNS effectively.

Adverse effects of cephalosporine:

[A]Allergy:Fever,skin rashes,granulocytopenia,hemolytic anaemia,anphylaxis.

[B]Nephrotoxicity:Interstial nephritis,acute tubular necrosis.

[C]Superinfection.

[D]Local infection:Pain,fever,local oedema.

Adverse effects of 3rd/4th generation cephalosporines:

a)      Hypersensitivity:

·         Rash.

·         Fever.

·         Pruritus.

·         Anaphylaxis.

b)      Gastro-intestinal:

·         Nausea.

·         Vomiting.

·         Diarrhoea.

·         Abdominal pain.

c)       CNS:

·         Headache.

·         Dizziness.

·         Paraesthesia.

d)      Genito-urinary:

·         Candidiasis.

·         Vaginitis.

e)      Others:

·         Leucopenia.

·         Neutropenia.

·         Thrombocytopenia.

Drugs that are effective against stapphylococcal infection:

1)      Flucloxacillin.

2)      Cephalosporins.

3)      Carbapenems.

4)      Macrolids-Erythromycin.