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Protein Synthesis Inhibitors

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Presentation on theme: "Protein Synthesis Inhibitors"— Presentation transcript:

1 Protein Synthesis Inhibitors
Tetracyclines Macrolides Chloramphenicol Aminoglycosides Clindamycin Streptogramins Alan M. Reynared, Ph.D.

2 QUICK REVIEW - Protein Synthesis

3 Tetracyclines - Structure
Excretion R1 R2 R3 R4 mg/hr tetracycline (Achromycin) H OH CH3 H chlortetracycline (Aureomycin) H OH CH3 Cl oxytetracycline (Terramycin) OH OH CH3 H demethylchlortetracycline (Declomycin) H OH H Cl doxycycline (Vibramycin) OH CH3 H H minocycline (Minocin) H H H N(CH3) 9

4 Tetracyclines - Uses Gram- Bacteria Other Organisms
 Helicobacter pylori (duodenal ulcer)  Borrelia recurrentis (Lyme disease, relapsing fever) Other Organisms  Mycoplasma pneumoniae  acne

5 Tetracycline - Mechanism
 Inhibits protein synthesis  Static  Chelates divalent cations -- Ca++, Mg++

6 Tetracycline - Adverse Effects
 headache, nausea, vomiting  discoloration of bones and teeth  photosensitivity  liver damage  superinfection

7 Superinfection A new infection appearing during treatment
for a primary infection The organism will be resistant to the antibiotic used for the primary infection Organisms causing superinfection Staphylococcus aureus - enterocolitis Candida albicans - vagina, mouth Clostridium difficile - pseudomembranous colitis Risk factors in hospital > 6 days 6 > age > 60 broad spectrum antibiotic

8 Tetracylines  Administration Oral administration but interference by
food, Ca++, Mg++  Excretion renal, fecal enterohepatic

9 Chloramphenicol - structure/features
 Broad Spectrum  Inexpensive  Oral administration  Virtually non-toxic

10 Chloramphenicol - uses/toxicity
 Haemophilus influenzae (meningitis)  Typhus  Rocky Mountain Spotted Fever  eye infections Adverse Effects  superinfection  aplastic anemia

11 Chloramphenicol - mechanism
 Inhibits protein synthesis  Static

12 Macrolides - structure / names
erythromycin azithromycin clarithromycin

13 Macrolides - uses whooping cough pharyngitis
Community-acquired pneumonia Penicillin-allergic patients staphylococcus streptococcus pneumococcus

14 Macrolides - mechanism
 Inhibits protein synthesis  Static

15 Macrolides - toxicity / drug interactions
 nausea, vomiting, diarrhea  cholestatic hepatitis (esp. estolate) Drug Interactions  inhibit P450 system

16 Macrolides Administration  erythromycin destroyed by gastric acid
- enteric coated tablets - erythromycin stearate - erythromycin estolate  food decreases absorption of all macrolides

17 Aminoglycosides - structure / names
streptomycin gentamicin kanamycin tobramycin neomycin netilmicin paromomycin amikacin spectinomycin

18 Aminoglycosides - uses
Amikacin  serious Gram-negative infections  endocarditis (+ a penicillin or cephalosporin) Streptomycin  plague (Yersinia pestis)  tuleremia (Francisella tulerensis)  tuberculosis (Mycobacterium tuberculosis)

19 Aminoglycosides - mechanism
 inhibits protein synthesis  ribosomal binding is very tight  cidal  at high doses  bacterial cell permeability

20 Aminglycosides - adverse effects
- deafness - vertigo - kidney damage

21 Aminoglycosides - spectinomycin
Use Reserve drug for gonorrhea

22 Clindamycin USES  Staphylococcus aureus  Streptococcus pyogenes
 Bacteroides fragilis  Clostridium tetani

23 Clindamycin - mechanism
 Inhibits protein synthesis  static

24 Clindamycin - adverse effects
superinfection pseudomembranous colitis (ulcerative colitis) Clostridium difficile

25 Streptogramins Synercid  synergistic combination quinupristin
dalfopristin  activity against staphylococci streptococci vancomycin-resistant enterococci (VRE)

26 Drug Resistance Types of resistance Mechanisms of resistance
chromosomal plasmid-mediated Mechanisms of resistance enzymatic destruction of drug altered target of drug decreased influx of drug increased efflux of drug

27 Drug Resistance Multiple Drug Resistance Transmissible Drug Resistance
epidemic of dysentary in Tokyo Multiple Drug Resistance streptomycin 10-8 tetracycline 10-8 chloramphenicol 10-8 sulfisoxazole 10-8 all four 10-32 Transmissible Drug Resistance patient excreting MDR S. dysenteriae and E. coli

28 Drug Resistance Bacterial Conjugation

29 Drug Resistance Plasmid specifying resistance to 2 antibiotics

30 Drug Resistance MDR spread rapidly all over the world

31 Drug Resistance Increase in resistance with increased
production of antibiotics

32 Drug Resistance - specific antibiotics
penicillin -lactamase altered penicillin-binding protein aminoglycosides acetylation AcCoA + AG AcAG + CoA phosphorylation ATP + AG P-Ag + ADP adenylylation ATP + AG AMP-Ag + PPi

33 Drug Resistance - specific antibiotics
chloramphenicol acetylation AcCoA + CM AcCM + CoA erythromycin altered ribosome tetracycline active efflux of drug

34 Drug Resistance - aminoglycosides

35 Sulfonamides Gerhard Domagk, V.P., I. G. Farbenindustrie

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