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Antibacterials

Antibiotics are the substances produced by microorganisms, which suppress the growth of or kill other microorganisms at very low concentrations. 


Mechanism of action 

Spectrum 

Mechanism of resistance 

Adverse effects

Penicillin

Bactericidal 

Inhibit TRANSPEPTIDASE so that crosslinking of bacterial cellwall is lost.

Narrow spectrum 

Gram positive and few gram negative and anaerobic bacteria

Tolerance 

Penicillinase production 

Local irritation

Hypersensitivity

JARISCH HERSCHEIMER REACTION in syphilis patients

Super infection 

Hemolytic anemia 

Cephalosporin

Bactericidal 

Inhibit cellwall synthesis

Mixed spectrum 

I gen: gram positive.

II gen: gram negative, few gram positive bacteria 

III, IV, V gen: gram negative, enterpbacteriaceae, Pseudomonas, weakly gram positive 

Increased efflux

Impermeability to antibiotics 

Elaboration of beta lactamase

Pain

Diarrhea

Nephrotoxicity 

Neutropenia, thrombocytopenia 

Disulfiram like reaction


Tetracycline

Bacteriostatic 

Binds with 30s ribosomes, inhibits protein synthesis 

Broad Spectrum 

Gram positive, gram negative bacteria 

Rickettsia 

Mycoplasma 

Actinomycetes

Spirochetes

Protozoans like E. histolytica

Pumping out the tetracyclines 

Ribosomal protection 

Enzymatic inactivation 

Renal damage 

Anti anabolic effect

Phototoxicity

Diabetes insipidus

Hepatic damage

Fanconi syndrome

Vestibular toxicity

Chloramphenicol

Bacteriostatic 

Binds with 50s ribosomes,

inhibit protein synthesis 

Broad spectrum 

Gram positive, gram negative bacteria 

Spirochetes 

Rickettsia

Mycoplasma 

Salmonella etc

Inactivation by Acetyl transferase enzyme 

Bone marrow suppression 

Hypersensitivity 

Super infection 

Gray baby syndrome 

Macrolide

Bacteriostatic but at high dose, bactericidal 

Inhibit protein synthesis 

Narrow spectrum 

Gram positive bacteria 

Increased efflux 

Erythromycin esterase production 

Ribosomal protection 

Cross resistance 

Motilin receptor agonist - diarrhea 

Allergy 

CVS: QT prolongation, ventricular arrhythmia

Reversible ototoxicity

Sulfonamide

Bacteriostatic 

Competitively inhibit union of PABA with pteridine leading to inhibitioj of folic acid synthesis 

Narrow spectrum 

Strep. pyogenes

H. influenza

V. cholerae

H. ducreyi

Adapt alternative mechanism for folate synthesis 

Increased PABA synthesis 

Aplastic anemia

Bilirubin displacement 

Crystalluria, hematuria

Rashes

SLE

Hemolytic in G6PD deficiency 

Cotrimoxazole

Bactericidal 

Fixed dose of TRIMETHOPRIM and SULFAMETHOXAZOLE in the ratio of 1:5

S typhi

Sulfonamide resistant strains of Staph. aureus

Kelbsiella, Enterobacter

Yersinia

P. jiroveci

Gonococci

Meningococci etc.

Alternative pathway of folate mechanism

Plasmid mediated acquisition of DHFRase

Nausea, vomitting 

Stomatitis

Headache 

Folate def.

C/I in pregnancy, renal disease

Fluoroquinolone

Bactericidal 

Inhibit DNA gyrase, topoisomerase IV - inhibiting DNA replication

Wide range of organisms

Due to chromosomal mutation 

Reduced affinity for fluorosquinolones 

GI Distress

Headache, dizziness

Seizures

C/I pregnancy, tendonitis in adults


Aminoglycoside

Bactericidal 

Bind to 30s and 50s ribosomes and freeze initiation

Narrow spectrum 

Ribosomal protection 

Mutation 

Decreased efficiency of transport mechanism (not seen in amikacin, netilmycin)

Nephrotoxicity 

Allergy 

Neurotoxic 

Ototoxic


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