Second-generation cephalosporin

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Chapter: Medicinal Chemistry : Antibiotics

Second-generation cephalosporin : i. Cefaclor ii. Cefuroxime (Zinacef, Kefurox) iii. Cefoxitin iv. Cefamandole (Mandol, Kefadol) v. Cefonicid


Cephalosporins - Synthesis and Drug Profile

Second-generation cephalosporin

 

i. Cefaclor


Properties and uses: Cefaclor is a white or slightly yellow powder, slightly soluble in water, practically insoluble in methanol and methylene chloride. It has chloro group at C-3 position, and hence, stable in acid and achieves sufficient oral absorption. Used in the treatment of upper respiratory tract infections caused by Streptococcus pneumoniae and Haemophilus influenzae.

Dose: The dose orally for adults is 250–500 mg every 8 h.

Assay: It is assayed by adopting liquid chromatography technique.

Dosage forms: Cefaclor capsules B.P., Cefaclor oral suspension B.P., Prolonged-release Cefaclor tablets B.P.

Synthesis


 

ii. Cefuroxime (Zinacef, Kefurox)


Synthesis


Properties and uses: Cefiroxime sodium is a white hygroscopic powder, freely soluble in water, and very slightly soluble in ethanol. It has excellent activity against all gonococci, hence, is used to treat gonorrhoea. It may be used to treat lower respiratory tract infections caused by H. influenza and Para influenzae, Klebsiella spp. E.coli, Staphylococcus pneumoniae, and pyrogens.

Assay: It is assayed by adopting liquid chromatography technique.

Dose: The dose is 1.5 g (IM) as a single dose and also available as powder for injection in strengths of 0.75 and 1.5 g.

Dosage forms: Cefuroxime sodium injection I.P., Cefuroxime injection B.P.

 

iii. Cefoxitin


Synthesis


Properties and uses: Cefoxitin sodium is a white hygroscopic powder, soluble in water and sparingly soluble in alcohol. It is not the drug of choice for any infection, but it is an alternative drug for intra-abdominal infections, colorectal surgery, appendectomy, and ruptured viscus because it is active against most enteric anaerobes, including Bacteroides fragilis. It is approved for use in the treatment of bone and joint infections caused by Staphylococcus aureus, gynecological and intra-abdominal infections by Bacteroides spp.

Assay: It is assayed by adopting liquid chromatography technique.

Dosage forms: Cefoxitin injection B.P.

 

iv. Cefamandole (Mandol, Kefadol)


Synthesis


Properties and uses: Cefamandole nafate is a white powder, soluble in water, and sparingly soluble in methanol. It is the first compound of second-generation cephalosporin marketed in the United States. Cefamandole nafate is very unstable in solution and hydrolyzes rapidly to release cefamandole and formate. There is no loss of potency; however, these solutions are stored for 24 h at room temperature or up to 96 h by refrigeration.

Assay: It is assayed by adopting liquid chromatography technique.

Dose: IV dose is 0.5–2 g every 4 to 6 h, also available as injection in strengh of 0.5 and 1 mg/10ml.

 

v. Cefonicid


Synthesis


Properties and uses: Cefonicid is a second-generation cephalosporin that is structurally similar to cefamandole, except that it contains a methane sulphonic acid group attached to the N-1 position of the tetrazole ring. Used in the treatment of bacterial infections.

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