- Chemical substances produced by a 6. Bacitracin microorganism with the capacity to inhibit other 7. Metronidazole microorganisms - Destroy/kill the organism MINIMAL INHIBITORY MINIMAL LETHAL CONCENTRATION (MIC) CONCENTRATION (MLC)
NARROW SPECTRUM BROAD SPECTRUM - Is the lowest - Is the lowest
concentration of a concentration of drug - Effective against a - Destroy different kinds drug that inhibits that kills bacterial limited number of of organism bacterial growth growth pathogens 1. Ampicillin 1. Bacitracin 2. Cephalosporin 2. Clindamycin 3. Chloramphenicol 3. Dapsone 4. Ciprofloxacin THERAPEUTIC INDEX 4. Erythromycin 5. Rifampicin - Is the ratio of the toxic dose to the therapeutic 5. Gentamicin 6. Sulfonamines dose 6. Isoniazid 7. Trimethoprim - The higher the therapeutic index, the more 7. Polymyxin B 8. Tetracycline effective the chemotherapeutic agent 8. Vancomycin - (CARST) - (PIGBEDCV) QUALITIES OF A GOOD AMA KILL or INHIBIT pathogens CLASSIFICATION OF BROAD SPECTRUM Selective toxicity (cause NO damage to the host) a. Natural - Produced by bacteria or NON allergenic drugs fungi Stable 1. Ampoterecin B Remain in specific tissues of the body 2. Erythromycin, Kill pathogens before they mutate / resistant 3. Kanamycin 4. Neomycin 5. Nystatin ACTION OF ANTIMICROBIALS 6. Rifampicin 1. Inhibiting cell wall synthesis 7. Streptomycin 2. Inhibiting CHON synthesis 8. Tetracycline 3. Inhibiting N.A synthesis 9. Vancomycin 4. Destroying the cell membrane 10. Bacitracin 5. Inhibiting essential metabolites 11. Gentamicin 12. Polymyxin 13. Griseofulvin CELL WALL INHIBITORS 14. Penicillin 15. Cephalosphorin BACTERICIDAL b. Semi- - Chemically modified natural 1. Basitracin synthetic drugs with added extra 2. Cephalosporin drugs chemical groups 3. Ampicillin 1. Ampicillin, 4. Imipenem 2. Carbenicillin 5. Vancomycin 3. Methicillin 6. Isoniazid 4. Synthetic - Chemically produced drugs - acts only on growing cells (stati/cidal) drugs 1. Sulfonamides 7. Carbenicillin 2. Trimethoprim 8. Methicillin resembles D-alanyl-D- 3. Chloramphenicol PENICILIN 9. Penicillin alanineof the 4. Cifrofloxacin Beta lactamase resistant peptidoglycansubunits Broad spectrum penicillin 5. Isoniazid penicillin 1. Pen G inactivated by stomach 6. Dapsone 1. Cloxacilin 1. Amoxicillin acids, (parenterally) 2.2. Penicillin Dicloxacillin V 2. resistant acid Ampicillin(orally) 3. Mehcillin 3. Piperacillin 3.4. Penicillinase resistant penicillin BACTERIOSTATIC BACTERICIDAL Nafcillin 4. Carbenicillin 1. Methicillin AGENTS AGENTS 5. Oxacillin 5. Ticarcillin 2. Nafcillin 1. Chloramphenicol 1. Aminoglycosides Key points: 3. Oxacillin 2. Dapsone a. gentamicin 4. Cephalosporins Cell growths stops and death often follows 1. Cephalotin 3. Erythromycin b. amikacin Most selective antibiotics with high therapeutic 4. Clindamycin c. streptomycin index 2. Cefoxitin 5. Isoniazid 2. Beta-lactams 3. Ceftriazone Inhibits transpeptidation enzymes 6. Rifampicin a. ceftriazone 4. Cephalexine 7. Sulfonamides b. imipenem 5. Cefixime 8. Tetracyclines c. penicillin INHIBIT PROTEIN SYNTHESIS d. cefotaxime 30’S Ribosomes Inhibitors 6. Ribosomes 50’s Cefoperazone 3. Glycopeptides 5. Ampicillin acidInhibitors stable, effective for a. vancomycin 1. Tetracycline G+,1.G- Chloramphenicol- 4. Isoniazid 6. Vancomycin -BACTERIOSTATIC cup-shaped molecule BACTERIOSTATIC drug; teicoplanin drug 7. Carbenicillin Acid stable, Pseudomonas and Proteus 2. Aminoglycosides- 2. Macrolide DRUG RESISTANCE BACTERICIDAL a. Erythromycin – Intrinsic resistance Extrinsic resistance a. Streptomycin, BACTERIOSTATIC - Lack specific target - Cannot bind to bacterial Kanamycin Amikacin OR CIDAL site ( mycoplasma) cell ( mutation) Gentamicin b. Clindamycin- - Unable to reach its - Cannot pass through the b. Tobramycin BACTERIOSTATIC site of action cell membrane Neomycin/Netilmicin OR CIDAL ( ribosome) ( mutation-cell membrane c. Fusidic acid c. Lincomycin permeability) Key points: - Destroyed by the enzyme Binds with 30s subunit resulting to misreading of ( beta lactamase) mRNA and interferes with aminoacyl-tRNA binding PENICILLINASES and Binds with 50s subunit resulting to inhibition of CEPHALOSPORINASE peptidyl transferase and inhibits peptide chain 1) BETA lactam elongation INHIBITOR with BETA High dosage of tetracycline may lead to live and LACTAM antibiotic kidney damage and yellowing the teeth of children 2) CLAVULANIC ACID Chloramphenicol may cause temporary or with AMOXICILLIN permanent depression of bone marrow leading to ( AUGMENTIN) aplastic anemia and leukemia (toxic side effect) 3) SULBACTAM with Aminoglycosides Macrolide antibiotics AMPICILLIN 1. Gentamicin 1. erythromycin ( UNASYN) 2. Kanamycin 2. clindamycin - Pump out of the cell 3. Neomycin 3. azithromycin before it can damage or 4. streptomycin Chloramphenicol and kill cell ( MDR pump) 5. tobramycin erythromycin - they have cyclohexane - bind to 23s rRNA ring and may cause on the 50s deafness and loss of ribosomal unit balance (toxic)
INHIBIT NUCLEIC ACID SYNTHESIS
1. RIFAMPIN 2. MITOMYCIN 3. METRONIDAZOLE –disruption if DNA, for anaerobic 4. NOVOBIOCIN 5. NITROFURANTOIN 6. QUINOLONES and FLUROQUINOLONES a. CIPROFLOXACIN b. NALIDIXIC ACID c. NORFLOXACIN d. LEVOFLAXIN- - Interfere with the DNA gyrase and replication - Highly effective for enteric bacteria E.coli 7. BACTERICIDAL
Biochemistry & Genetics Important Concepts Q&as DR Kumar Ponnusamy & Jegathambigai RN, Biochemistry & Genetics, International Medical University (IMU) / AIMST University School of Medicine, Malaysia