𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 : 𝐁𝐞𝐭𝐚 𝐥𝐚𝐜𝐭𝐚𝐦 𝐀𝐧𝐭𝐢𝐛𝐢𝐨𝐭𝐢𝐜

In simple words, Cephalosporin is a large group of Antimicrobial drug, which kills the bacteria by inhibiting their cell-wall synthesis. They have beta lactam ring and known as Beta Lactam antibiotic.

𝐐. 𝐖𝐡𝐲 𝐚𝐫𝐞 𝐭𝐡𝐞𝐲 𝐜𝐚𝐥𝐥𝐞𝐝 “𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧”? 𝐖𝐡𝐲 𝐧𝐨𝐭 𝐀𝐁𝐂𝐃?
Because Historically, an Italian scientist named Giuseppe Brotzu discovered Cephalosporin (1945) by isolating a mixture of compounds from the mold Acremonium ( which was previously called Cephalosporium), Hence the name Cephalosporin.
Now most Cephalosporins are produced semi-synthetically.

𝐂𝐡𝐞𝐦𝐢𝐜𝐚𝐥 𝐬𝐭𝐫𝐮𝐜𝐭𝐮𝐫𝐞 𝐚𝐭 𝐚 𝐠𝐥𝐚𝐧𝐜𝐞 :
In a Cephalosporin there are,

• 2 Rings -Beta lactam ring
-Dihydrothiazine ring
• Acetyl side chain

𝐒𝐡𝐨𝐫𝐭-𝐜𝐮𝐭 𝐏𝐡𝐚𝐫𝐦𝐚𝐜𝐨𝐤𝐢𝐧𝐞𝐭𝐢𝐜𝐬 𝐚𝐧𝐝 𝐨𝐭𝐡𝐞𝐫 𝐏𝐫𝐨𝐩𝐞𝐫𝐭𝐢𝐞𝐬 :
• Route:
– Oral (as Cephalosporins are relatively acid stable)
– Parental ( IM or IV)
• Half-life: 1-2 hours
• Metabolism – in Liver
• Excretion- through Kidney (Probenecid can decrease⬇︎ excretion)
• Bactericidal in nature
• They are pregnancy Safe
• Well tolerated by Children and Neonates

𝐂𝐥𝐚𝐬𝐬𝐢𝐟𝐢𝐜𝐚𝐭𝐢𝐨𝐧:
According to spectrum of activity,

𝟏𝐬𝐭 𝐆𝐞𝐧𝐞𝐫𝐚𝐭𝐢𝐨𝐧 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 :
(more active against Gram+ve org.)
Cefazoline
Cefalexin
Cefalothin
Cefaloridin
Cefadroxil
Cephradin

𝟐𝐧𝐝 𝐆𝐞𝐧𝐞𝐫𝐚𝐭𝐢𝐨𝐧 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 :
(Intermediate spectrum, Extended Gram-ve coverage)
Cefuroxime
Cefoxitine
Cefprozil
Cefaclor
Cefomandole
Cefmetazol

𝟑𝐫𝐝 𝐆𝐞𝐧𝐞𝐫𝐚𝐭𝐢𝐨𝐧 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 :
(Extended spectrum, Extended Gram-ve coverage)
Ceftriaxone
Cefoperazone
Cefotaxime
Cefexime
Cefopodoxime
Ceftizoxime
Ceftazidime
Cefnidir
Ceftibuten
Moxalactam

𝟒𝐭𝐡 𝐆𝐞𝐧𝐞𝐫𝐚𝐭𝐢𝐨𝐧 𝐂𝐞𝐩𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 :
(Extended Gram-ve coverage, increased activity against Streptococci & MRSA)
Cefepime
Cefpirome

𝟓𝐭𝐡 𝐆𝐞𝐧𝐞𝐫𝐚𝐭𝐢𝐨𝐧 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 :
(Extended spectrum against MRSA)
Ceftaroline
Ceftibiprole

𝐌𝐞𝐜𝐡𝐚𝐧𝐢𝐬𝐦 𝐨𝐟 𝐚𝐜𝐭𝐢𝐨𝐧 :

They are bacterial cell-wall synthesis inhibitor.

𝐐. 𝐇𝐨𝐰 𝐝𝐨 𝐭𝐡𝐞𝐲 𝐝𝐨 𝐭𝐡𝐚𝐭?!

1. At first, Cephalosporin , cell-membrane এর Penicillin binding protein (PBP) নামে একটি specific receptor এর সাথে bind করে ➡︎ যা Transpeptidase enzyme কে কাজ করতে বাধা দেয় ➡︎So peptidoglycan synthesis হয়না ➡︎Cell membrane porous হয়ে এর permeability বেড়ে যায় ➡︎ hypertonic Internal Osmotic Pressure এর জন্য fluid cell এর ভিতরে যায় ➡︎Bacterial cell becomes swollen ➡︎ bacterial cell lysis ➡︎ Bactericidal Action
2. Also Cephalosporin activates the Autolytic enzymes of the cell wall➡︎ Peptidoglycans ভেঙ্গে যায় ➡︎ Bacterial lysis ➡︎ bactericidal action

𝐈𝐧𝐝𝐢𝐜𝐚𝐭𝐢𝐨𝐧𝐬 / 𝐂𝐨𝐦𝐦𝐨𝐧 𝐮𝐬𝐞𝐬 𝐨𝐟 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 :

1. Urinary tract infection
2. Respiratory tract infection
3. Skin and soft tissue infection
4. Meningitis
5. Septicemia
6. Gonorrhea
7. Penicillinase producing Staphylococcal infection
8. Enteric fever
9. Surgical prophylaxis
10. As alternative to Penicillin in Upper respiratory tract infection
11. Hospital acquired infections ( specially respiratory and other infections in ICU)

𝐀𝐝𝐯𝐚𝐧𝐭𝐚𝐠𝐞𝐬 𝐨𝐟 𝟑𝐫𝐝 𝐆𝐞𝐧𝐞𝐫𝐚𝐭𝐢𝐨𝐧 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 :

1. Extended spectrum of activity
2. Highly resistant against beta lactamase from gram –ve bacteria
3. Highly effective against wide range of serious infections ( bacterial meningitis, typhoid fever, complicated UTI, abdominal sepsis, septicemia )
4. Can enter into CNS ( can be used in Meningitis)

𝐀𝐝𝐯𝐚𝐧𝐭𝐚𝐠𝐞𝐬 𝐨𝐟 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧𝐬 𝐨𝐯𝐞𝐫 𝐧𝐚𝐭𝐮𝐫𝐚𝐥 𝐏𝐞𝐧𝐢𝐜𝐢𝐥𝐥𝐢𝐧 :

1. Broad spectrum of activity
2. More stable to beta lactamase enzyme
3. Less hypersensitivity reaction
4. Relativelty stable to temperature and pH

𝐏𝐚𝐭𝐡𝐨𝐠𝐞𝐧𝐬 / 𝐁𝐚𝐜𝐭𝐞𝐫𝐢𝐚 𝐭𝐡𝐚𝐭 𝐚𝐫𝐞 𝐍𝐎𝐓 𝐜𝐨𝐯𝐞𝐫𝐞𝐝 𝐛𝐲 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧𝐬:

Mnemonic –‘𝐀𝐭𝐲𝐩𝐢𝐜𝐚𝐥 𝐌𝐑 𝐜𝐚𝐧𝐧𝐨𝐭 𝐄𝐍𝐓𝐄𝐑 𝐭𝐡𝐞 𝐋𝐈𝐒𝐓’

𝐀𝐭𝐲𝐩𝐢𝐜𝐚𝐥 – (Atypical bacteria: wall less, live intracellularly)- Mycoplasma, Chlamydia
𝐌𝐑– MRSA (Methicillin Resistant Staphylococcus Aureus)
𝐄𝐍𝐓𝐄𝐑 – Enterococci
𝐋𝐈𝐒𝐓 – Listeria

𝐂𝐨𝐧𝐭𝐫𝐚𝐢𝐧𝐝𝐢𝐜𝐚𝐭𝐢𝐨𝐧𝐬 𝐚𝐧𝐝 𝐜𝐚𝐮𝐭𝐢𝐨𝐧𝐬 :

1. 𝐊𝐧𝐨𝐰𝐧 𝐚𝐥𝐥𝐞𝐫𝐠𝐲 𝐭𝐨 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 𝐚𝐧𝐝 𝐚𝐥𝐬𝐨 𝐏𝐞𝐧𝐢𝐜𝐢𝐥𝐥𝐢𝐧 as they show molecular similarity
2. 𝐇𝐞𝐩𝐚𝐭𝐢𝐜 𝐚𝐧𝐝 𝐫𝐞𝐧𝐚𝐥 𝐢𝐦𝐩𝐚𝐢𝐫𝐦𝐞𝐧𝐭 ( can interfere with the metabolism and excretion of the drug)
3. 𝐉𝐚𝐮𝐧𝐝𝐢𝐜𝐞𝐝 𝐧𝐞𝐨𝐧𝐚𝐭𝐞𝐬 ( as Cephalosporin eg. Ceftriaxone has the affinity for binding to Albumin by replacing Bilirubin , so there’s a risk of Bilirubin encephalopathy)
4. 𝐏𝐚𝐭𝐢𝐞𝐧𝐭 𝐬𝐡𝐨𝐮𝐥𝐝 𝐚𝐯𝐨𝐢𝐝 𝐚𝐥𝐜𝐨𝐡𝐨𝐥 𝐰𝐡𝐢𝐥𝐞 𝐨𝐧 𝟑𝐫𝐝 𝐠𝐞𝐧𝐞𝐫𝐚𝐭𝐢𝐨𝐧 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 to prevent Disulfiram like reactions
5. 𝐀𝐦𝐢𝐧𝐨𝐠𝐥𝐲𝐜𝐨𝐬𝐢𝐝𝐞𝐬 𝐬𝐡𝐨𝐮𝐥𝐝 𝐛𝐞 𝐚𝐯𝐨𝐢𝐝𝐞𝐝 𝐰𝐢𝐭𝐡 𝐂𝐞𝐩𝐡𝐚𝐥𝐨𝐬𝐩𝐨𝐫𝐢𝐧 because their combined effect can cause Acute tubular necrosis.

𝐀𝐝𝐯𝐞𝐫𝐬𝐞 𝐞𝐟𝐟𝐞𝐜𝐭𝐬 :

1. Hypersensitivity reaction like Steven-Johnson syndrome ( rashes, angioedema, urticaria, dermatitis) , anaphylaxis
2. GIT upset, Diarrhea
3. Nephrotoxicity, Renal failure
4. Superinfection
5. Bleeding tendency ( specially in cancer patient)
6. Intra-abdominal infection
7. Neutropenia
8. Pain at the site of injection
9. Coagulopathy, Thrombophlebitis may occur
10. Hepatitis
11. Pseudomembranous colitis (mostly 3rd generation Cephalosporins like Cefixime)
12. Cephalosporin induced disulfiram like reactions (by Cefoperazone )

Reference :
Berterm G. Katzung, Susan B. Masters, Anthony J.Trevor
Basic and Clinical Pharmacology 12th Edition, Page: 797.

Platform Academic Division:
Saimuma Rahman
Medical College for Women and Hospital
Session : 2019-20