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ANTIBIOTICS
1S Y E D T A N V E E R S H A H Z A D
CLASSIFICATION OF ANTIBIOTICS
CHEMICAL STRUCTURE
SPECTRUM OF ACTIVITY
MECHANISM OF ACTION
2S Y E D T A N V E E R S H A H Z A D
MECHANISM OF ACTION
3S Y E D T A N V E E R S H A H Z A D
INHIBITORS OF CELL WALL SYNTHESIS
4S Y E D T A N V E E R S H A H Z A D
BETA LACTAM ANTIBIOTICS
PENICILLINS
CEPHALOSPORINS
CARBAPENEMS
MONOBACTAMS
5S Y E D T A N V E E R S H A H Z A D1/20/2018
PENICLLINS
DERIVED FROM THE FUNGUS PENICILLIUM
THERAPEUTIC CONCENTRATION IN MOST
TISSUES
POOR CSF PENETRATION
RENAL EXCRETION
SIDE EFFECTS: HYPERSENSITIVITY, NEPHRITIS,
NERUOTOXICITY, PLATELET DYSFUNCTION
6S Y E D T A N V E E R S H A H Z A D
ANTISTAPHYLOCOCCAL PENICILLINS
METHICILLIN
NAFCILLIN
OXACILLIN
DICLOXACILLIN
7S Y E D T A N V E E R S H A H Z A D
AMINOPENICILLINS
AMOXICILLIN +/- CLAVULANATE
AMPICILLIN +/- SULBACTAM
8S Y E D T A N V E E R S H A H Z A D
ANTIPSEUDOMONAL PENICILLINS
CARBENICILLIN
TICARCILLIN +/- CLAVULANATE
PIPERACILLIN +/- TAZOBACTAM
9S Y E D T A N V E E R S H A H Z A D
CEPHALOSPORINS
 STRUCTURALLY SIMILAR TO
PENICILLINS
 THERAPEUTIC
CONCENTRATION IN MANY
TISSUES, 3RD AND 4TH
GENERATION INTO CSF
 RENAL EXCRETION
 SIDE EFFECTS
 ALLERGY
 ANTI-VITAMIN K
10
S Y E D T A N V E E R S H A H Z A D1/20/2018
11
S Y E D T A N V E E R S H A H Z A D
MONOBACTAMS
AZTREONAM
 SINGLE BETA LACTAM RING
 NARROW SPECTRUM: GRAM-
NEGATIVE AEROBES
 ENTEROBACTERIACEA
 PSEUDOMONAS
 GIVEN IV/IM
 RENAL EXCRETION
 LITTLE CROSS-REACTIVITY WITH
OTHER BETA LACTAMS
 SIDE EFFECTS: PHLEBITIS, RASH,
ELEVATED LFT’S
12S Y E D T A N V E E R S H A H Z A D1/20/2018
CARBAPENEMS
MEROPENEM/IMIPENEM
 BROAD SPECTRUM
 ACTIVE AGAINST MRSA
 GIVEN IV
 PENETRATES CSF
 RENAL METABOLISM AND
EXCRETION
 ADDITION OF CILASTIN
 SIDE EFFECTS: GI UPSET,
EOSINOPHILIA, NEUTROPENIA,
LOWERING OF SEIZURE
THRESHOLD
13S Y E D T A N V E E R S H A H Z A D1/20/2018
VANCOMYCIN
TRICYCLIC GLYCOPEPTIDE
INHIBITS SYNTHESIS OF PHOSPHOLIPIDS AND
CROSS-LINKING OF PEPTIDOGLYCANS
ACTIVITY AGAINST GRAM-POSITIVE ORGANISMS
USEFUL FOR BETA LACTAM RESISTANT
INFECTIONS
WIDELY DISTRIBUTED, PENETRATES CSF
RENAL ELIMINATION, FOLLOWS CREATININE CL.
SIDE EFFECTS: PHLEBITIS, RED MAN SYNDROME,
OTOTOXICITY, NEPHROTOXICITY
14S Y E D T A N V E E R S H A H Z A D
PROTEIN SYNTHESIS INHIBITORS
HUMAN RIBOSOME
 80S
40S
60S
BACTERIAL RIBOSOME
 70S
30S
50S
15S Y E D T A N V E E R S H A H Z A D1/20/2018
TETRACYCLINES
ISOLATED FROM STREPTOMYCES AUREOFACIENS
REVERSIBLY BIND 30S RIBOSOMAL SUBUNIT
PENETRATE SINUS MUCOSA, SALIVA AND TEARS
METABOLIZED IN LIVER-->EXCRETED IN BILE-->
REABSORBED-->ELIMINATED IN URINE
SIDE EFFECTS: GI UPSET, HEPATOTOXICITY,
PHOTOSENSITIVITY, BONY DEPOSITION
CONTRAINDICATED IN PREGNANT OR BREAST
FEEDING WOMEN, CHILDREN UNDER 8 Y/O
16S Y E D T A N V E E R S H A H Z A D
TETRACYCLINES
17S Y E D T A N V E E R S H A H Z A D
AMINOGLYCOSIDES
DERIVED FROM STREPTOMYCES AND
MICORMONOSPORA
IRREVERSIBLE BINDING TO 30S SUBUNIT
ACTIVELY TRANSPORTED INTO BACTERIAL CELLS
VARIABLE TISSUE PENETRATION, UNRELIABLE CSF
LEVELS
CONCENTRATE WITHIN PERILYMPH
RENAL ELIMINATION
NEPHROTOXICITY, OTOTOXICITY, NEUROTOXICITY
18S Y E D T A N V E E R S H A H Z A D
AMINOGLYCOSIDES
19
S Y E D T A N V E E R S H A H Z A D
MACROLIDES
MACROCYCLIC LACTONE STRUCTURE
IRREVERSIBLE BINDING TO 50S SUBUNIT
THERAPEUTIC CONCENTRATIONS IN
OROPHARYNGEAL AND RESPIRATORY
SECRETIONS
NO CSF PENETRATION
METABOLIZED IN LIVER, EXCRETED IN FECES
AND URINE
SIDE EFFECTS: GI UPSET, OTOTOXICITY,
HEPATOTOXICITY
20S Y E D T A N V E E R S H A H Z A D
CHLORAMPHENICOL
ISOLATED FROM STREPTOMYCES
REVERSIBLE BINDING TO 50S SUBUNIT
BROAD SPECTRUM OF ACTIVITY
INDICATED FOR SEVERE ANAEROBIC INFECTIONS OR
UNRESPONSIVE LIFE-THREATENING INFECTIONS
WIDELY DISTRIBUTED, ENTERS CSF
METABOLIZED IN LIVER (INHIBITS P-450), ELIMINATED IN
URINE
TOXICITIES: REVERSIBLE ANEMIA, HEMOLYTIC ANEMIA,
APLASTIC ANEMIA, GRAY BABY SYNDROME
21S Y E D T A N V E E R S H A H Z A D
CLINDAMYCIN
SEMISYNTHETIC DERIVATIVE OF LINCOMYCIN
IRREVERSIBLE BINDING TO 50S SUBUNIT
COVERS ANAEROBES AND GRAM + AEROBES
WIDELY USEFUL FOR HEAD AND NECK INFECTIONS
PENETRATES SALIVA, SPUTUM, PLEURAL FLUID, AND
BONE, BUT NOT CSF
METABOLIZED IN LIVER-->REABSORBED-->ELIMINATED IN
URINE
SIDE EFFECTS: RASH, NEUTROPENIA /
THROMBOCYTOPENIA, PSEUDOMEMBRANOUS COLITIS
22S Y E D T A N V E E R S H A H Z A D
INHIBITORS OF METABOLISM
SULFONAMIDES
TRIMETHOPRIM
INTERFERE WITH THE
PRODUCTION OF FOLIC
ACID COENZYMES THAT
ARE REQUIRED FOR
PURINE AND PYRIMIDINE
SYNTHESIS
23S Y E D T A N V E E R S H A H Z A D1/20/2018
SULFONAMIDES
DERIVED FROM PRONTOSIL
COMPETITVE ANTAGONIST OF PABA
WIDE DISTRIBUTION, PENETRATE CSF,
CROSS PLACENTA
METABOLIZED IN LIVER,ELIMINATED IN
URINE.
SIDE EFFECTS: RASH, ANGIOEDEMA,
STEVENS-JOHNSON SYNDROME,
KERNICTERUS
AVOID IN PREGNANCY AND INFANTS
24S Y E D T A N V E E R S H A H Z A D1/20/2018
SULFONAMIDES
25
S Y E D T A N V E E R S H A H Z A D
TRIMETHOPRIM
INHIBITS DIHYDROFOLATE REDUCTASE
1000X HIGHER AFFINITY FOR BACTERIAL ENZYME
THAN HUMAN ENZYME
SIMILAR SPECTRUM AND PHARMACOKINETIC
PROFILE AS SULFAS
SIDE EFFECTS: FOLATE DEFICIENCY ANEMIA,
LEUKOPENIA, GRANULOCYTOPENIA
26S Y E D T A N V E E R S H A H Z A D
INHIBITORS OF NUCLEIC ACID
FUNCTION/SYNTHESIS
FLUOROQUINOLONES
 BIND BACTERIA DNA GYRASE (TOPOISOMERASE II)
 CONCENTRATE IN SINUS AND MIDDLE EAR MUCOSA,
PENETRATE CARTILAGE AND BONE
 PARTIALLY METABOLIZED IN LIVER-->GI OR RENAL
EXCRETION
 SIDE EFFECTS: NAUSEA, DIZZINESS, PHOTOTOXICITY,
NEPHROTOXICITY
 AVOID IN PREGNANT OR NURSING WOMEN
 ? USE IN CHILDREN--POSSIBLE EFFECT ON ARTICULAR
CARTILAGE
27S Y E D T A N V E E R S H A H Z A D
FLUOROQUINOLONES
28
S Y E D T A N V E E R S H A H Z A D
ANTIMYCOBACTERIAL THERAPY
MUST ADDRESS TWO DISTINCT POPULATIONS
OF TUBERCLE BACILLI
FIRST-LINE TREATMENT: REGIMENS OF 3-4
DRUGS FOR 6 MONTHS TO 2 YEARS
SECOND-LINE THERAPY: RESERVED FOR
MULTI-DRUG RESISTANT ORGANISMS OR
UNRESPONSIVE INFECTION
29S Y E D T A N V E E R S H A H Z A D
ISONIAZIDE
RIFAMPIN
PYRAZINAMIDE
ETHAMBUTOL
STREPTOMYCIN
ISONIAZIDE
 MOST POTENT DRUG
 INHIBITS FORMATION OF OUTER
MYCOLIC ACID
 WIDELY DISTRIBUTES AND
PENETRATES CSF
 METABOLIZED IN LIVER, EXCRETED IN
URINE, SALIVA, AND SPUTUM
 SIDE EFFECTS: HYPERSENSITIVITY,
NERUOPATHY, HEPATOTOXICITY
30
FIRST-LINE AGENTS
S Y E D T A N V E E R S H A H Z A D
PROPHYLACTIC ANTIBIOTICS
COVER BACTERIAL FLORA INVOLVED IN THE
SURGICAL FIELD
ADMINISTER WITHIN 2 HOURS BEFORE OR 3
HOURS AFTER SURGERY HAS BEGUN
MAINTAIN THERAPEUTIC BLOOD LEVEL DURING
LENGTHY PROCEDURES
CONTINUE PROPHYLAXIS FOR THE 24 HOUR
PERIOD SURROUNDING SURGERY
31S Y E D T A N V E E R S H A H Z A D

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Antibiotics

  • 1. ANTIBIOTICS 1S Y E D T A N V E E R S H A H Z A D
  • 2. CLASSIFICATION OF ANTIBIOTICS CHEMICAL STRUCTURE SPECTRUM OF ACTIVITY MECHANISM OF ACTION 2S Y E D T A N V E E R S H A H Z A D
  • 3. MECHANISM OF ACTION 3S Y E D T A N V E E R S H A H Z A D
  • 4. INHIBITORS OF CELL WALL SYNTHESIS 4S Y E D T A N V E E R S H A H Z A D
  • 6. PENICLLINS DERIVED FROM THE FUNGUS PENICILLIUM THERAPEUTIC CONCENTRATION IN MOST TISSUES POOR CSF PENETRATION RENAL EXCRETION SIDE EFFECTS: HYPERSENSITIVITY, NEPHRITIS, NERUOTOXICITY, PLATELET DYSFUNCTION 6S Y E D T A N V E E R S H A H Z A D
  • 8. AMINOPENICILLINS AMOXICILLIN +/- CLAVULANATE AMPICILLIN +/- SULBACTAM 8S Y E D T A N V E E R S H A H Z A D
  • 9. ANTIPSEUDOMONAL PENICILLINS CARBENICILLIN TICARCILLIN +/- CLAVULANATE PIPERACILLIN +/- TAZOBACTAM 9S Y E D T A N V E E R S H A H Z A D
  • 10. CEPHALOSPORINS  STRUCTURALLY SIMILAR TO PENICILLINS  THERAPEUTIC CONCENTRATION IN MANY TISSUES, 3RD AND 4TH GENERATION INTO CSF  RENAL EXCRETION  SIDE EFFECTS  ALLERGY  ANTI-VITAMIN K 10 S Y E D T A N V E E R S H A H Z A D1/20/2018
  • 11. 11 S Y E D T A N V E E R S H A H Z A D
  • 12. MONOBACTAMS AZTREONAM  SINGLE BETA LACTAM RING  NARROW SPECTRUM: GRAM- NEGATIVE AEROBES  ENTEROBACTERIACEA  PSEUDOMONAS  GIVEN IV/IM  RENAL EXCRETION  LITTLE CROSS-REACTIVITY WITH OTHER BETA LACTAMS  SIDE EFFECTS: PHLEBITIS, RASH, ELEVATED LFT’S 12S Y E D T A N V E E R S H A H Z A D1/20/2018
  • 13. CARBAPENEMS MEROPENEM/IMIPENEM  BROAD SPECTRUM  ACTIVE AGAINST MRSA  GIVEN IV  PENETRATES CSF  RENAL METABOLISM AND EXCRETION  ADDITION OF CILASTIN  SIDE EFFECTS: GI UPSET, EOSINOPHILIA, NEUTROPENIA, LOWERING OF SEIZURE THRESHOLD 13S Y E D T A N V E E R S H A H Z A D1/20/2018
  • 14. VANCOMYCIN TRICYCLIC GLYCOPEPTIDE INHIBITS SYNTHESIS OF PHOSPHOLIPIDS AND CROSS-LINKING OF PEPTIDOGLYCANS ACTIVITY AGAINST GRAM-POSITIVE ORGANISMS USEFUL FOR BETA LACTAM RESISTANT INFECTIONS WIDELY DISTRIBUTED, PENETRATES CSF RENAL ELIMINATION, FOLLOWS CREATININE CL. SIDE EFFECTS: PHLEBITIS, RED MAN SYNDROME, OTOTOXICITY, NEPHROTOXICITY 14S Y E D T A N V E E R S H A H Z A D
  • 15. PROTEIN SYNTHESIS INHIBITORS HUMAN RIBOSOME  80S 40S 60S BACTERIAL RIBOSOME  70S 30S 50S 15S Y E D T A N V E E R S H A H Z A D1/20/2018
  • 16. TETRACYCLINES ISOLATED FROM STREPTOMYCES AUREOFACIENS REVERSIBLY BIND 30S RIBOSOMAL SUBUNIT PENETRATE SINUS MUCOSA, SALIVA AND TEARS METABOLIZED IN LIVER-->EXCRETED IN BILE--> REABSORBED-->ELIMINATED IN URINE SIDE EFFECTS: GI UPSET, HEPATOTOXICITY, PHOTOSENSITIVITY, BONY DEPOSITION CONTRAINDICATED IN PREGNANT OR BREAST FEEDING WOMEN, CHILDREN UNDER 8 Y/O 16S Y E D T A N V E E R S H A H Z A D
  • 17. TETRACYCLINES 17S Y E D T A N V E E R S H A H Z A D
  • 18. AMINOGLYCOSIDES DERIVED FROM STREPTOMYCES AND MICORMONOSPORA IRREVERSIBLE BINDING TO 30S SUBUNIT ACTIVELY TRANSPORTED INTO BACTERIAL CELLS VARIABLE TISSUE PENETRATION, UNRELIABLE CSF LEVELS CONCENTRATE WITHIN PERILYMPH RENAL ELIMINATION NEPHROTOXICITY, OTOTOXICITY, NEUROTOXICITY 18S Y E D T A N V E E R S H A H Z A D
  • 19. AMINOGLYCOSIDES 19 S Y E D T A N V E E R S H A H Z A D
  • 20. MACROLIDES MACROCYCLIC LACTONE STRUCTURE IRREVERSIBLE BINDING TO 50S SUBUNIT THERAPEUTIC CONCENTRATIONS IN OROPHARYNGEAL AND RESPIRATORY SECRETIONS NO CSF PENETRATION METABOLIZED IN LIVER, EXCRETED IN FECES AND URINE SIDE EFFECTS: GI UPSET, OTOTOXICITY, HEPATOTOXICITY 20S Y E D T A N V E E R S H A H Z A D
  • 21. CHLORAMPHENICOL ISOLATED FROM STREPTOMYCES REVERSIBLE BINDING TO 50S SUBUNIT BROAD SPECTRUM OF ACTIVITY INDICATED FOR SEVERE ANAEROBIC INFECTIONS OR UNRESPONSIVE LIFE-THREATENING INFECTIONS WIDELY DISTRIBUTED, ENTERS CSF METABOLIZED IN LIVER (INHIBITS P-450), ELIMINATED IN URINE TOXICITIES: REVERSIBLE ANEMIA, HEMOLYTIC ANEMIA, APLASTIC ANEMIA, GRAY BABY SYNDROME 21S Y E D T A N V E E R S H A H Z A D
  • 22. CLINDAMYCIN SEMISYNTHETIC DERIVATIVE OF LINCOMYCIN IRREVERSIBLE BINDING TO 50S SUBUNIT COVERS ANAEROBES AND GRAM + AEROBES WIDELY USEFUL FOR HEAD AND NECK INFECTIONS PENETRATES SALIVA, SPUTUM, PLEURAL FLUID, AND BONE, BUT NOT CSF METABOLIZED IN LIVER-->REABSORBED-->ELIMINATED IN URINE SIDE EFFECTS: RASH, NEUTROPENIA / THROMBOCYTOPENIA, PSEUDOMEMBRANOUS COLITIS 22S Y E D T A N V E E R S H A H Z A D
  • 23. INHIBITORS OF METABOLISM SULFONAMIDES TRIMETHOPRIM INTERFERE WITH THE PRODUCTION OF FOLIC ACID COENZYMES THAT ARE REQUIRED FOR PURINE AND PYRIMIDINE SYNTHESIS 23S Y E D T A N V E E R S H A H Z A D1/20/2018
  • 24. SULFONAMIDES DERIVED FROM PRONTOSIL COMPETITVE ANTAGONIST OF PABA WIDE DISTRIBUTION, PENETRATE CSF, CROSS PLACENTA METABOLIZED IN LIVER,ELIMINATED IN URINE. SIDE EFFECTS: RASH, ANGIOEDEMA, STEVENS-JOHNSON SYNDROME, KERNICTERUS AVOID IN PREGNANCY AND INFANTS 24S Y E D T A N V E E R S H A H Z A D1/20/2018
  • 25. SULFONAMIDES 25 S Y E D T A N V E E R S H A H Z A D
  • 26. TRIMETHOPRIM INHIBITS DIHYDROFOLATE REDUCTASE 1000X HIGHER AFFINITY FOR BACTERIAL ENZYME THAN HUMAN ENZYME SIMILAR SPECTRUM AND PHARMACOKINETIC PROFILE AS SULFAS SIDE EFFECTS: FOLATE DEFICIENCY ANEMIA, LEUKOPENIA, GRANULOCYTOPENIA 26S Y E D T A N V E E R S H A H Z A D
  • 27. INHIBITORS OF NUCLEIC ACID FUNCTION/SYNTHESIS FLUOROQUINOLONES  BIND BACTERIA DNA GYRASE (TOPOISOMERASE II)  CONCENTRATE IN SINUS AND MIDDLE EAR MUCOSA, PENETRATE CARTILAGE AND BONE  PARTIALLY METABOLIZED IN LIVER-->GI OR RENAL EXCRETION  SIDE EFFECTS: NAUSEA, DIZZINESS, PHOTOTOXICITY, NEPHROTOXICITY  AVOID IN PREGNANT OR NURSING WOMEN  ? USE IN CHILDREN--POSSIBLE EFFECT ON ARTICULAR CARTILAGE 27S Y E D T A N V E E R S H A H Z A D
  • 28. FLUOROQUINOLONES 28 S Y E D T A N V E E R S H A H Z A D
  • 29. ANTIMYCOBACTERIAL THERAPY MUST ADDRESS TWO DISTINCT POPULATIONS OF TUBERCLE BACILLI FIRST-LINE TREATMENT: REGIMENS OF 3-4 DRUGS FOR 6 MONTHS TO 2 YEARS SECOND-LINE THERAPY: RESERVED FOR MULTI-DRUG RESISTANT ORGANISMS OR UNRESPONSIVE INFECTION 29S Y E D T A N V E E R S H A H Z A D
  • 30. ISONIAZIDE RIFAMPIN PYRAZINAMIDE ETHAMBUTOL STREPTOMYCIN ISONIAZIDE  MOST POTENT DRUG  INHIBITS FORMATION OF OUTER MYCOLIC ACID  WIDELY DISTRIBUTES AND PENETRATES CSF  METABOLIZED IN LIVER, EXCRETED IN URINE, SALIVA, AND SPUTUM  SIDE EFFECTS: HYPERSENSITIVITY, NERUOPATHY, HEPATOTOXICITY 30 FIRST-LINE AGENTS S Y E D T A N V E E R S H A H Z A D
  • 31. PROPHYLACTIC ANTIBIOTICS COVER BACTERIAL FLORA INVOLVED IN THE SURGICAL FIELD ADMINISTER WITHIN 2 HOURS BEFORE OR 3 HOURS AFTER SURGERY HAS BEGUN MAINTAIN THERAPEUTIC BLOOD LEVEL DURING LENGTHY PROCEDURES CONTINUE PROPHYLAXIS FOR THE 24 HOUR PERIOD SURROUNDING SURGERY 31S Y E D T A N V E E R S H A H Z A D