1. Gram-positive bacilli
β－Lactam Antibiotics
Penicillins
【 Antibacterial activity 】
Gram-positive coccus
Gram-negative coccus
Gram-positive bacilli
Helicoids

2. Semisynthetic penicillin
Penicillinase-resistant penicillin( Oxacillin )
(1) They kill penicillinase-producing staphylococci
(2) They can’t kill Methicillin-resistant strains of
Staphylococcus aureus (MRSA)

3. Extended spectrum penicillins (Ampicillin) Antipseudomonal penicillins
They are more effective against gram-negative bacilli
They can not kill pseudomonas aeruginosa
Antipseudomonal penicillins
Carbenicillin
Piperacillin

4. Cephalosporins Feature
First
Second
Third G＋
＋＋＋ ＋＋ ＋ G－
Pseudomonas aeruginosa －
anaerobes
nephrotoxic
＋＋＋

5. Other β-lactams antibiotics
Carbapenems
Imipenem + cilastatin
β-lactamase inhibitors
Clavulanic acid + Amoxicillin

6. Chapter 37
Macrolides
Lincomycins
Polypeptide antibiotics

7. Macrolides
Erythromycin
Clarithromycin
Azithromycin

8. 一、Erythromycin 【Pharmacokinetics】
Erythromycin base is destroyed by gastric acid
It distributes well to all body fluids including prostatic fluid ,but it does not enter the cerebrospinal fluid (CSF)
Erythromycin is extensively metabolized and is excreted in the bile, and only 5% is excreted in the urine.

9. 【Antibacterial activity 】
Erythromycin is bacteriostatic
It is effective against gram-positive organisms
It is active against some gram-negative organisms
Mycoplasma, Chlamydozoan, Legionella and campylobacteria are susceptible.

10. Inhibit protein synthesis
【Mechanism of action】 P A
Inhibit protein synthesis
Erythromycin(50S) P A P A
translocase

11. 【Clinical uses】 Gram-positive coccus infection
staphylococci: bouton (boil)
streptococci: pharyngitis, febris rubra
streptococcus pneumoniae: pneumonia genuina
2. Corynebacterium diphtheriae
3. Chlamydial infections
urethral, endocervical, rectal, epididymal, urogenital
4. Mycoplasmal pneumonia
5. Legionella pneumonia

12. Contraindications: hepatic dysfunction
【Adverse effect】
1. Gastrointestinal effects
Anorexia, nausea, vomiting, and diarrhea
2. Cholestatic jaundice
estolate form of erythromycin
3. Ototoxicity
Transient deafness
Contraindications: hepatic dysfunction

13. methylation of an adenine of the 23S bacterial ribosomal RNA
【Drug resistance】
1. Reduced permeability of the cell membrane
or active efflux
2. Modification of the ribosomal binding site
3. Production of esterases that hydrolyze macrolides
methylation of an adenine of the 23S bacterial ribosomal RNA

14. 二、Clarithromycin
Its activity against Chlamydia, Legionella and Ureaplasma is higher than that of erythromycin.
It has lower frequency of gastrointestinal intolerance

15. 三、 Azithromycin
Azithromycin is more active against Haemophilus influenzae and Chlamydia than erythromycin
It is less active against streptococci and staphylococci
It is now used for urethritis caused by Chlamydia trachomatis.
It is rapidly absorbed and well tolerated orally.

16. Section 2 Lincomycins  
Lincomycin
Clindamycin

17. 【 Antibacterial action and Clinical uses 】
1. Clindamycin is significantly effective against
anaerobic bacteria
2. It is employed primarily in the treatment of
infections caused by anaerobic bacteria
3. Enterococci and clostridium difficile are resistant
4. It distributes well into bone, so treats medullitis
5. It does not penetrate into cerebrospinal fluid ,
not use to treat Epidemic meningitis alone

18. vancomycin metronidazole
【Adverse effect 】
vancomycin metronidazole
Fatal pseudomembranous colitis
Impaired liver function

19. Section 3 Polypeptide antibiotics
Vancomycins
polymyxins

20. 一、Vancomycin 【Antibacterial activity 】 It is bactericidal agent
It is primarily active against gram-positive bacteria
(MRSA and MRSE),but enterococci are resistant
3. All species of gram-negative bacilli and mycobacteria are resistant to vancomycin

21. 【Mechanism of action】
Vancomycin

22. 【Clinical use and Adverse effect 】
1. Gram-positive bacteria infections:
pneumonia, empyema, endocarditis, osteomyelitis,
and soft-tissue abscesses, MRSA infection
2. Fatal pseudomembranous colitis due to Clostridium
difficile or staphylococci
3. Adverse effects: ototoxicity, nephrotoxicity , "red
man syndrome

23. 二、Polymyxins
They are bactericidal agent, active against gram-negative bacilli
2. They increased permeability of the bacterial membrane resulting bacterial cell death
3. They are available for external otitis, corneal ulcers caused by Pseudomonas
4. Adverse effects: nephrotoxicity, neurotoxicity, hypersensitive reaction

24. Chapter 38 Aminoglycosides
Streptomycin
Neomycin
Kanamycin
Amikacin
Gentamicin
Tobramycin

25. Antibacterial spectrum :
【Antibacterial activity】
Antibacterial spectrum :
All aminoglycosides are bactericidal
They are effective against aerobic gram-negative bacilli
They are ineffective against anaerobic organisms

26. 【Mechanism of action】 interfere with the initiation complex
Decoding P A
interfere with the initiation complex
nonfunctional or toxic protein synthesis
aminoglycosides(30S,A)
breakup of polysomes into nonfunctional monosomes P A P A

27. 【Pharmacokinetics 】 Aminoglycosides must be given parenterally
High concentrations accumulate in the renal cortex and in the endolymph and perilymph of the inner ear
All may accumulate in fetal plasma and amniotic fluid.
All are rapidly excreted into the urine

28. 【Clinical uses】
Aminoglycosides are mostly used to treat infection caused by gram-negative bacteria
Penicillin combination with aminoglycoside is used for treatment of enterococcal endocarditis , streptococcal and staphylococcal endocarditis

29. dizziness, visual extinction, ocular tremor, nausea, vomiting, ataxia.
【Adverse effect】
dizziness, visual extinction, ocular tremor, nausea, vomiting, ataxia.
Ototoxicity ：
vestibular dysfunction
Injury of cochlear auditory nerve
Nephrotoxicity:
3. Neuromuscular paralysis:
4. Allergic reactions:
ear noises
hearing diminution permanent deafness

30. 【Drug resistance】
Synthesis of enzymes that modify and inactivate aminoglycoside antibiotics.
Altered target site
Decreased uptake of drug

31. Chapter 39 Tetracyclines and Chloramphenicol
Section 1 Tetracyclines
Tetracycline
Doxycycline
Demeclocycline
Minocycline

32. 【Antibacterial activity】
Tetracyclines are broad spectrum bacteriostatic
antibiotics
2. They are active against many gram-positive and gram-negative bacteria
3. They are also active against Rickett's organism, helicoid, mycoplasma and Chlamydia

33. 【Mechanism of action】 P A
Tetracyclines
(30S,A)
tetracyclines enter microorganism by passive diffusion and an energy-dependent process of active transport.
tetracyclines bind reversibly to the 30S subunit of the bacterial ribosome

34. 【Pharmacokinetics】 Tetracyclines are adequately but incompletely
absorbed after oral ingestion
2. Tetracyclines cross the placental barrier and concentrate in fetal bones and dentition
3. Tetracyclines are metabolized in liver and then are excreted from kidney, except doxycycline

35. 【Clinical uses】
Rickettsial infection: fever, chill, ache in bones and joints
Chlamydiae infection: pneumonia , urethritis, trachelitis, ophthalmia and trachoma
Mycoplasma infection: mycoplasmal pneumonia
Spirochetal infection: lyme disease
Bacterial infection: cholera

36. 【Adverse effect 】 Gastric discomfort: Nausea, vomiting, and diarrhea
Bony structures and Teeth :discoloration and hypoplasia of the teeth and a temporary stunting of growth
Fatal hepatotoxicity: in pregnant women
Phototoxicity: severe sunburn

37. 4. Vestibular problems: dizziness, nausea, vomiting
5. Pseudotumor cerebri: Benign intracranial
hypertension , headache , blurred vision
6. Superinfections: pseudomembranous enterocolitis caused by Clostridium difficile.
7. Contraindications: renally-impaired patients ,
pregnant or breast-feeding women, or in children
\under 8 years of age.

38. 【Drug resistance】 Decreased intracellular accumulation
production of protected proteins that interfere with tetracycline binding to the ribosome
Enzymatic inactivation of tetracyclines

39. Section 2 Chloramphenicol
【 Antibacterial action】
Chloramphenicol is either bacteriostatic or bactericidal
It is active against both aerobic and anaerobic gram-positive and gram-negative organisms
It has effective against rickettsiae, helicoids, Chlamydia and mycoplasma.

40. 【Mechanism of action】 Chloramphenicol(50S,A) Peptidyl transferase P A

41. 【pharmacokinetics】
Chloramphenicol may be administered either intravenously or orally
It penetrate blood-brain barrier, placental barrier, blood-ocular barrier
It is inactivated by conjugation with glucuronic acid in liver, secreted by the renal tubule

42. 【Clinical uses】 Bacterial meningitis: meningococcal meningitis
Rickettsial infections: typhus or Rocky Mountain spotted fever
Eye infection: outer eye infection, intraocular infection, eyeball infection
Anaerobic infection: peritoneal abscess, pelvic inflammation and peritonitis

43. 【Adverse effect】 Bone marrow depression Aplastic anemia
Gray baby syndrome:
poor feeding, depressed breathing,
cardiovascular collapse, cyanosis

44. 【Drug resistance 】 Produce inactivator： acetyl coenzyme A transferase
Membrane permeability is decreased, chloramphenicol penetrate the organism less