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Antibiotics

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  • 1. ANTIBIOTICS Dr shabeel pn ROYAL DENTAL COLLEGE
  • 2. INTRODUCTION
    • GREATEST CONTRIBUTION OF 20 TH CENTURY TO THERAPEUTICS
    • MORE IMPORTANT IN DEVELOPING COUNTRIES – INFECTIOUS DISEASES
    • MINIMAL EFFECT ON RECIPIENT
    • MOST FREQUENTLY USED AS WELL AS MISUSED DRUGS
    • CHEMOTHERAPY
  • 3. HISTORY OF CHEMOTHERAPY
    • PRE-EHRLICH ERA:
    • BEFORE 1981, EMPIRICAL USAGE
    • CINCHONA, MERCURY, CHAULMOOGRA OIL
    • PERIOD OF EHRLICH:
    • FATHER OF CHEMOTHERAPY
    • DYES - “MAGIC BULLETS”
    • METHYLENE BLUE(MALARIA),
    • TRYPTAN RED
    • MODERN ERA:
    • AFTER 1935
  • 4. MODERN ERA
    • DOMAGK 1935
    • EFFICIENCY OF ‘PRONTOSIL’(SULFONAMIDE DYE)
    • SULFAPYRIDINE 1 ST MARKETTED IN 1938
    • ANTIBIOSIS –PASTEUR 1877
    • -GROWTH OFANTHRAX BACILLI IN URINE
    • INHIBITTED BY AIRBORNE BACERIA
    • FLEMMING 1929 : PENICILLIN- STAPH
    • CHAIN, ABRAHAM & FLOREY 1941
  • 5. DEFINITION
    • “A CHEMICAL SUBSTANCE PRODUCED BY MICRO ORGANISMS, HAVING THE PROPERTY OF INHIBITING THE GROWTH OF OR DESTROYING OTHER MICRO ORGANISMS IN HIGH DILUTION”
    • EXCLUDES NATURAL SUBSTANCES LIKE ANTIBODIES AND ETHANOL, LACTIC ACID , HYDROGEN PEROXIDE……
  • 6. CLASSIFICATION
    • TYPE OF ACTION
    • 1. PRIMARILY BACTERIOSTATIC:
    • TETRACYCLINES, CHLORAMPHENICOL
    • ERYTHROMYCIN, ETHAMBUTOL
    • 2. PRIMARILY BACTERICIDAL:
    • PENICILLINS, AMINOGLYCOSIDES
    • POLYPEPTIDES, CEPHALOSPORINS
    • VANCOMYCIN, CIPROFLOXACIN
  • 7. CLASSIFICATION
    • SPECTRUM OF ACTIVITY
    • 1. BROAD SPECTRUM
    • TETRACYCLINES, CHLORAMPHENICOL
    • 2. NARROW SPECTRUM
    • PENICILLIN G, STREPTOMYCIN, ERYTHROMYCIN
  • 8. CLASSIFICATION
    • BETA-LACTAM ANTIBIOTICS: PENICILLINS, CEPHALOSPORINS, CARBAPENEMS
    • AMINOGLYCOSIDE ANTIBIOTICS: STREPTOMYCIN, GENTAMYCIN, KANAMYCIN, AMIKACIN
    • TETRACYCLINES: TETRACYCLINE, DOXYCYCLINE, MINOCYCLINE, OXYTETRACYCLINE
    • QUINOLONES: CIPROFLOXACIN, NORFLOXACIN, OFLOXACIN
    • MACROLIDES: ERYTHROMYCIN, AZITHROMYCIN, ROXITHRMYCIN, CLARITHROMYCIN
    • NITROIMIDAZOLES: METRONIDAZOLE, TINIDAZOLE
  • 9. CLASSIFICATION
    • INHIBIT CELL WALL SYNTHESIS: PENICILLIN, CEPHALOSPORIN, VANCOMYCIN, BACITRACIN
    • CAUSE LEAKAGE FROM MEMBRANES: AMPHOTERICIN B, NYSTATIN
    • INHIBIT PROTEIN SYNTHESIS: TETRCYCLINES, ERYTHROMYCIN, CHLORAMPHENICOL
    • CAUSE MISREADING OF m-RNA CODE: STREPTOMYCIN, GENTAMYCIN
    • INHIBIT DNA-GYRASE: CIPROFLOXACIN
    • INTERFERE WITH DNA FUNCTION: RIFAMPIN, METRONIDAZOLE
    • INTERFERE WITH DNA SYNTHESIS: IDOXURIDINE
    • INTERFERE WITH INTERMEDIARY METABOLISM: TRIMETHOPRIM, ETHAMBUTOL
  • 10. PENICILLINS
    • NATURAL PENICILLINS: PENICILLIN G, PROCAINE P
    • BENZATHINE P
    • ACID RESISTANT PENICILLINS: PHENOXYMETHYL P, PHENOXYETHYL P
    • PENICILLINASE RESISTANT PENICILLNS: METHICILLIN, NAFCILLIN, CLOXACILLIN
    • EXTENDED SPECTRUM PENICILLINS: CARBOXY P, UREIDO P, AMINO P
    • PENICILLINS WITH BETA-LACTAMASE INHIBITORS:
  • 11. AMOXICILLIN
    • SEMISYNTHETIC, EXTENDED SPECTRUM
    • AMINO PENICILLIN
    • NO RESISTANCE TO PENICILLINASE OR OTHER BETA-LACTAMASES
    • MORE ACTIVE THAN NATURAL ONE
    • MANY GRAM –VE MICROBES (E. COLI, PROTEUS, H. INFLUENZA, SALMONELLA, SHIGELLA) ALSO
    • ORAL ABSORPTION IS BETTER; FOOD DOES NOT INTERFERE
    • MORE SUSTAINED BLOOD LEVELS
    • LESS CHANCE OF DIARRHOEA COMPARED TO AMPICILLIN
  • 12. AMOXICILLIN
    • USES:
    • -ACUTE INFECTIONS
    • -RESPIRATORY, URINARY TRACT
    • INFECTIONS
    • - MENINGITIS
    • -GONORRHOEA
    • - TYPHOID FEVER
    • - SUBACUTE BACTERIAL ENDOCARDITIS
    • -CHOLECYSTITIS
    • - SEPTICAEMIAS AND MIXED INFECTIONS
  • 13. BETA LACTAMASE INHIBITORS
    • CLAVULANIC ACID:
    • - STREPTOMYCES CLAVULIGEROUS
    • - INHIBITS WIDE VARIETY OF B-LACTAMASES
    • - REVERSIBLE INITIALLY, LATER COVALENT
    • - ‘SUICIDE INHIBITOR’, INACTIVATED AFTER BINDING
    • SULBACTUM
    • - SEMISYNTHETIC BETA LACTAMASE INHIBITOR
    • - SIMILAR TO CLAVULANIC ACID IN ACTIVITY & STRUCTURE
    • - ORAL ABSORPTION IS INCONSISTENT, SO GIVEN
    • PARENTARALLY
  • 14. DOSAGE
    • ORAL
    • ADULT: 250-500mg Q8H (TRIHYDRATE)
    • CHILD: 125-250mg Q8H
    • PARENTARAL
    • ADULT: 500mg IM (SODIUM)
    • OR SLOW IV INJECTION EVERY 8 HRS
    • CHILD: 50-100mg/kg BODY WEIGHT
  • 15. COMMERCIAL PRODUCTS
    • BLUMOX - 6.5Rs/500mg Cap
    • IMOX - 6.3Rs/500mg Cap
    • ARISTOMOX- 5.7/Cap
    • - I.8/125mg Tab
    • BIG MOX - 3.0/250mg Cap
    • INMOX - 3.5/250mg Tab
    • - 6.5/500mg Cap
    • INMOX-KID- 2.0/125mg Tab
  • 16. CHOICE OF ANTIBIOTIC
    • HOST RELATED FACTORS
    • PATHOGEN RELATED FACTORS
    • DRUG RELATED FACTORS
  • 17. HOST FACTORS
    • AGE: CHLORAMPHENIOL NOT IN NEWBORN(LIVER ENZ)
    • TETRACYCLINES – CHILDREN BELOW 6
    • ACCUMILATE IN DEVELOPING TEETH
    • IMMUNOCOMPETENCY STATUS
    • BACTEROSTATIC OR BACTERICIDAL
    • PREGNANCY: RISK TO FETUS
    • ALLERGY:
    • LOCAL FACTORS: PUS, NECROTIC MATERIAL
    • HEMATOMA
  • 18. PATHOGEN FACTORS
    • EVALUATION OF ETIOLOGY:
    • NOT NON-SPECIFIC ANTIPYRETICS
    • NOT FOR VIRAL DISEASES LIKE COLD
    • BACTERIOLOGICAL EXAMINATION:
    • CULTURE & SENSITIVITY
    • CHANCE OF DRUG RESISTANCE
    • IF MANY STRAINS, MORE CHANCE
  • 19. DRUG FACTORS
    • NATURE:
    • BACTERICIDAL PREFFERED
    • BACTEROSTATIC NOT EFFECTIVE IN THE
    • ABSENCE OF INFLAMATION
    • SPECTRUM
    • DEFINITIVE THERAPY- NARROW
    • EMPIRICAL THERAPY - BROAD
    • RELATIVE TOXICITY
    • ROUTE OF ADMINISTRATION
    • SENSITIVITY
    • EVIDENCE OF CLINICAL EFFICACY
    • COST
  • 20. PREGNANCY SAFETY INDEX
    • SAFELY PRESCRIBING DRUGS IN PREGNANCY BASED ON US FDA
    • DO NOT IMPLY AN INCREASING PROGRESSION OF RISK FROM A – X
    • BASED ON THE RISK OF REPRODUCTIVE AND DEVELOPMENTAL ADVERSE EFFECTS AND RISK vs. BENEFIT CONSIDERATIONS
    • DRUGS IN DIFFERENT CATEGORIES MAY HAVE SIMILAR RISK, BUT CATEGORIZED DIFFERENTLY
  • 21. CATEGORY - A
    • CONTROLLED STUDIES IN WOMEN FAIL TO DEMONSTRATE A RISK TO THE FOETUS IN 1 ST TRIMESTER(NO EVIDENCE OF RISK IN OTHER TRIMESTERS) AND POSSIBILITY OF FETAL HARM REMAINS REMOTE
    • ASCORBIC ACID, BETACAROTENE -IN PROPER DOSE
  • 22. CATEGORY - B
    • EITHER ANIMAL- REPRODUCTION STUDIES HAVE NOT DEMONSTRATED A FETAL RISK BUT THERE ARE NO CONTROLLED STUDIES IN PREG. WOMEN
    • OR
    • ANIMAL-REPRODUCTION STUDIES HAVE SHOWN AN ADVERSE EFFECT (OTHER THAN DECREASE IN FERTILITY)THAT WAS NOT CONFIRMED IN CONTROL STUDIES IN WOMEN IN THE 1 ST TRIMESTER
    • AMOXICILLIN, AMPICILLIN, AMPHOTERICIN B
  • 23. CATEGORY - C
    • EITHER STUDIES IN ANIMALS HAVE REVEALED ADVERSE EFFECTS ON THE FETUS(TERATOGENIC OR EMBROCIDAL OR OTHERS) AND THERE ARE NO CONTROLLED STUDIES IN WOMEN
    • OR
    • STUDIES IN WOMEN AND ANIMALS ARE NOT AVAILABLE
    • (DRUGS SHOULD BE GIVEN ONLY IF POTENTIAL BENEFIT JUSTIFIES THE POTENTIAL RISK TO THE FETUS)
    • CYCLOSPORIN, CIPROFLOXACIN, CLARYTHROMYCIN
  • 24. CATEGORY - D
    • THERE IS POSITIVE EVIDENCE OF HUMAN FETAL RISK, BUT THE BENEFITS FROM USE IN PREGNANT WOMEN MAY BE ACCEPTABLE DESPITE THE RISK.
    • LIFE THREATENING CONDITION – SAFER DRUGS CAN NOT BE USED OR INEFFECTVE
    • AMIKACIN, CHLORTETRACYCLINE, BLEOMYCIN
  • 25. CATEGORY - X
    • STUDIES IN ANIMALS OR HUMAN BEINGS HAVE DEMONSTRATED FETAL ABNORMALITIES OR THERE IS EVIDENCE OF FETAL RISK BASED ON HUMAN EXPERIENCE OR BOTH, AND THE RISK OF USE OF DRUG IN PREGNANT WOMEN CLEARLY OUTWEIGHS ANY POSSIBLE BENEFIT. THE DRUG IS CONTRAINDICATED IN WOMEN WHO ARE OR MAY BECOME PREGNANT
    • TRIAZOLAM, TESTOSTERONE, THALIDOMIDE
  • 26. ANTIBOTIC PROPHYLAXIS
  • 27.  
  • 28.  
  • 29. REFERENCES
    • ESSENTIALS OF MEDICAL PHARMACOLOGY
    • K D TRIPATHI
    • PHARMACOLOGY & PHARMACOTHERAPEUTICS
    • R S SATOSKAR
    • PRINCIPLES OF DENTAL PHARMACOLOGY
    • NARESH KUMAR KHANNA
    • CURRENT INDEX OF MEDICAL SPECIALITIES
    • INTERNET
  • 30. THANK YOU