Antibiotics in Dentistry Dr Mohammed Malik Afroz Format • • • • • • • • • • Introduction History Definition Classifications Antibiotics Problems that arise with use of antibiotics Principles of antibiotic selection Combinations of antibiotics Antibiotic prophylaxis Conclusion Introduction • • • • • Host , Environment & Organisms Normal oral flora- 300 types of bacteria Microorganisms breach the host defense ‘Antibiotics’ Mean – Kill or prevent Antibiotics are substances produced by various species of microorganisms (bacteria,fungi, actinomycetes) that supresses growth of other microorganisms and eventually may destroy them --Goodman & Gilman’s IXth edition Classifications Chemical structure: 1. Sulfonamides & related Sulfadizine, Sulfones, Paraaminosalicylic acid 2. Diaminopyrimidines: Trimethoprim , Pyrimethamine 3. Quinolones: Norfloxacin , Ciprofloxacin 4. β-lactum antibiotics: Penicillins, Cephalosporins 5. Tetracyclines: Doxycycline , Minocycline 6. Nitrobenzene derivatives Chloramphenicol 7. Aminoglycosides: Streptomycin , Gentamicin 8. Macrolide antibiotics: Erythromycin , Roxithromycin 9. Polypeptide antibiotics: Polymyxin-B , Bacitracin 10. Glycopeptides: Vancomycin 11. Oxazolidinone: Linezoid Classifications Chemical structure: 12. Nitrofuran derivatives: Nitrofurantoin 13. Nitroimidazoles: Metronidazole , Tinidazole 14. Nicotinic acid derivatives: Isoniazide , Pyrazinamide 15. Polyene antibiotics: Nystatin , Amphotericin-B 16. Azole derivatives: Miconazole , Clotrimazole 17. Others: Rifampin , Clindamycin , Lincomycin , Ethambutol , Griseofulvin Classification • Mechanism of action: Bacteria responsible for infections AEROBIC BACTERIA ANAEROBIC BACTERIA Gram-positive cocci • Streptococcus Viridans • hemolytic • Staphylococcus Gram-negative bacilli • Haemophilus influenza • Eischeria coli • Klebsiella • Eikenella corrodens Gram-positive cocci • Streptococcus • Peptostreptococcus Gram-negative bacilli • Porphyromonas • Prevotella • Fusobacterium • Bacteroids fragilis Beta – Lactum Antibiotics • • 1. 2. 3. 4. Most commonly used in dentistry Antibiotic in the group are: Penicillins Cephalosporins Monobactum Carbapenems Penicillins • Present source – Penicillium chrysogenum • Mechanism of action: inhibits synthesis of peptidoglycans – formation of cell wall deficient bacteria – lysis • • 1. 2. Spectrum of activity: Bactericidal Classification: Naturally occuring penicillins: Penicillin G , Penicillin V Semisynthetic penicillins: Short acting: Ampicillin,Amoxycillin,Amoxycillin with Clavulanic acid Long acting: Procaine penicillin Ampicillin • Semisynthetic aminopenicillin • Extended/broad spectrum • Spectrum of activity: Bactericidal • gram+ve cocci , bacilli , gram-ve bacilli • Many have developed resistance • Pharmacokinetics: • Absorption: well absorbed orally, causes Diarrhoea • Excretion : primary – kidneys enterohepatic circulation – bile & reabsorbed Ampicillin • Uses : • Dental infections – gram+ve , gram-ve & anaerobic bacteria • Medical: UTI, respiratory tract infections , bacillary dysentary , typhoid fever , cholysistitis Meningitis Gonorrhoea Subacute bacterial endocarditis • Dose: 0.5-2g oral/im/iv every 6 hours Children: 25 – 50 mg/kg/day AMPILIN, ROSCILLIN, BIOCILIN – 250,500 mg cap ; 125,250 mg/5ml dry syr ; 100 mg/ml pediatric drops ; 250,500mg & 1 g/vial inj Amoxicillin Similar to Ampicillin , except : • Good oral absorption – food does not interfere – higher & more sustained blood levels • Diarrhoea incidence is less • Most frequently used in dental infections Dose :250-500mg TDS for 5 days • 1st choice of drug for prophylaxis following dental surgery • Preferred for typhoid , bronchitis , UTI , SABE , gonorrhoea • Dose: 0.25 – 1g TDS oral/im AMOXYLIN , NOVAMOX: 250mg,500mg cap ; 125mg/5ml dry syr AMOXIL , MOX: 250mg,500mg cap ; 125mg/5ml dry syr ; 250mg, 500mg/vial inj Beta-Lactamase Inhibitor • Beta-Lactamase : family of enzymes produced by many gram+ve & gram-ve bacteria that inactivate beta-lactam antibiotics by opening the beta-lactum ring • Inhibitor of beta-lactamase enzyme are: 1. Clavulanic acid 2. Sulbactum Clavulanic acid • Mechanism of action: ‘Progressive’ inhibitor- binds with B-lactamase – inhibition increases with time. Pharmacokinetics: • Rapid oral absorption • Plasma t1/2 – 1hr & tissue distribution = amoxicillin • Coamoxiclav- combination of amoxicillin & clavulanic acid • Excreted by glomerular filteration Adverse effects: GI tolerance is poor in children Candida stomatitis/vaginitis ; rashes Clavulanic acid • Uses: • Coamoxiclav is indicated for: Dental infections by B-lactamase producing bacteria Skin , soft tissue infections, intra-abdominal & gynaecological sepsis , urinary , biliary & respiratory infections Gonorrhoea AUGMENTIN , ENHANCIN , AMONATE: Amoxicillin250mg+ clavulanic acid 125mg tab ;1-2 tab TDS AUGMENTIN: Amoxicillin1g + clavulanic acid 0.2g vial ; inject 1 vial deep im or iv 6-8 hourly – severe infections Cephalosporins • Semisynthetic B-Lactum antibiotic derived from ‘Cephalosporin-C’. Parenteral • First generation • Second generation • Third generation • Fourth generation Oral • Cephalothin • Cefazolin • • Cefamandole • Cefuroxime • Cephalexin • Cefadroxil • Cefotaxime • Ceftrioxone • Cefoperazone • Cefixime • Cefepime • Cefachlor • Cefuroxime axetil Cephalosporins • Mechanism of action: inhibition of bacterial cell wall synthesis but bind to different protein than penicillin • Spectrum of activity: Bactericidal Broad spectrum agents – therapuetically & prophylactically used in place of penicillin & erythromycin • Excreted rapidly by kidneys First generation Cephalosporins • Cephalothin – resistant to penicillinase – staphylococcal infections • Cefazolin – good tissue permeability – surgical prophylaxis • Cephalexin - most common alt – amoxicillin; minor oral infections – abscess / cellulitis; Pre , intra & post-operative – surgical procedure Not effective – anaerobic gram-ve organisms • Cefadroxil - good tissue permeability – alveolar bone. Sustained action • Cefazolin : Dose : 0.25g 8 hourly (mild) 1g 6 hourly i.m./i.v. (severe) • ALCIZON , ORIZOLIN 0.25 , 0.5 , 1g vial inj • Cephalexin :0.25-1g 6-8 hourly (25 -100mg/kg/day) • CEPHACILLIN – 250, 500mg cap • SPORIDEX , ALCEPHIN , CEPHAXIN – 250, 500mg cap 125mg/5ml dry syrup, 100mg/ml paediatric syrup • Cefadroxil: Dose: 0.5-1g BD • DROXYL 0.5-1g tab , 250mg/5ml syr • CEFADROX 0.5g cap , 125mg/5ml syr , 250mg kid tab • Cephalosporins • Uses: • Dental infections: • Alternative to penicillin 1st gen – cephalexin , cephadroxil gram+ve aerobic bacteria 2nd gen – cefaclor , cefuroxime axetil- oral anaerobes Cephalexin , cephadroxil – alt to amoxicillin for prophylaxis • Medical uses: • Respiratory , urinary , soft tissue infections – gram-ve organisms • Cefazolin-surgical prophylaxis • Gonorrhoea :ceftriaxone • Meningitis : 3rd gen • Typhoid ; alternate to ciprofloxacin • Nosocomial infections:3rd • Mixed aerobic-anaerobic inf in cancer pts …:3rd gen Cephalosporins • Adverse effects: • Hypersensitivity reactions • Nephrotoxicity : combination with other nephrotoxic drugs – avoided • Diarrhoea • Low WBC count • Causes Pain – site of injection • Causes Bleeding – in patients with hypo – prothrombinaemia – malnourished pts Thank You