1. Macrolides(Erythromycin )
【Antibacterial activity 】
Erythromycin is bacteriostatic
It is effective against gram-positive organisms
It is active against some gram-negative organisms
Mycoplasma, Chlamydiae, Legionella are susceptible

2. Vancomycins 【Antibacterial activity 】 It is bactericidal agent
It is primarily active against gram-positive bacteria
(MRSA),but enterococci are resistant
3. Gram-negative bacilli are resistant to vancomycin

3. Aminoglycosides

4. 【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

5. Tetracyclines and Chloramphenicol
Section 1 Tetracyclines

6. 【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

7. 4. Vestibular problems: dizziness, nausea, vomiting
5. Pseudotumor cerebri: Benign intracranial
hypertension , headache , blurred vision
6. Superinfections: pseudomembranous enterocolitis
Vancomycin:

8. 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.

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

10. 【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

11. 【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

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

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

14. Artificial Synthetic
antibacterial drugs
Section I Quinolones

15. The second generation: The third generation: The fourth generation:
The first generation :
nalidixic acid, pipemidic acid
The second generation:
norfloxacin, ofloxacin, ciprofloxacin
The third generation:
sparfloxacin, levofloxacin, grepafloxacin
The fourth generation:
clinafloxacin, gatifloxacin.

16. Fluorequionlones:
The second generation
The third generation
The fourth generation

17. 【antibacterial action】
All of the quinolones are bactericidal
First generation only has active against some gram-negative bacteria
Second generation expend gram-negative bacteria spectrum
Third generation have active against gram-positive organisms, chlamydia, mycoplasma, Legionella and Bacillus tuberculosis
The fourth generation have active against anaerobic bacterium

18. Inhibit the replication of bacterial DNA
【Mechanism of action】
Inhibit the replication of bacterial DNA
interfering with the action of DNA gyrase:
gram-negative bacteria
interfering with the action of topoisomerase IV:
gram-positive bacteria

19. 【Clinical uses】 1. Genitourinary tract infections :
Urinary tract infections, prostatitis, cervicitis
2. Intestinal infection:
gastroenteritis, bacillary dysentery, diarrhea
3. Respiratory infection:
bronchitis, nasosinusitis ,pneumonia
4. Skeletal system infection:
medullitis and arthrosis

20. 【adverse effect】 Gastrointestinal discomfort:
poor appetite, nausea, vomiting, diarrhea
2. CNS problems:
dizziness, headache, insomnia, convulsion
3. Allergies：
angioneurotic edema，skin rash
Contraindications:
pregnancy, nursing mothers and children

21. 【drug resistance 】 1. Altered target:
modifications in the bacterial DNA gyrase
2. Decreased accumulation:
decreased number of porin proteins
increased energy-dependent efflux system

22. norfloxacin
This agent is effective against both gram-negative and gram-positive organisms in treating urinary tract infections and prostatitis, but not in systemic infections

23. ciprofloxacin
Ciprofloxacin is the most potent, used to treat many systemic infections with the exception of serious infections caused by MRSA, the enterococci and pneumococci. It is particularly useful in treating infections caused by gram-negative bacilli.

24. Ofloxacin
Ofloxacin is primarily used in the treatment of prostatitis. It may be used as alternative therapy in patients with gonorrhea. It has some benefit in the treatment of skin and lower respiratory tract infections.

25. Section II Sulfonamides
classification
oral, absorbable
oral, nonabsorbable
topical

26. 【Antibacterial action】
The sulfonamides are bacteriostatic;
These drugs inhibit both gram-positive and gram negative bacteria;
They have active against nocardia, Chlamydia trachomatis, and some protozoa;
They have no effective against mycoplasma, Rickett's organism, helicoid

27. 【Mechanism of action】 PABA + Pteridine Sulfonamides
Dihydropteroate
synthase
Sulfonamides
Dihydropteroic acid
Glutamate
Dihydrofolate
Dihydrofolate
reductase(DHFR)
Tetrahydrofolate
Purine、
pyrimidine nucleotide
precursor

28. 【Clinical uses 】 Systemic infections: oral and absorbable sulfonamides
2. Intestinal infection:
oral and nonabsorbable sulfonamides
3. Wound infection:
topical sulfonamides

29. 【adverse effect 】 1. Crystalluria: crystallura, hematuria, obstruction
adequate hydration and alkalinization of urine
2. Kernicterus:
sulfonamides displace bilirubin from binding sites on serum albumin
3. Hypersensitivity:
rashes, angioedema
4. Hemopoietic disturbances:
Hemolytic anemia, Granulocytopenia thrombocytopenia

30. Contraindications:
newborns and infants less than 2 months old as well as pregnant women

31. 【drug resistance 】 Increased PABA synthesis:
overcome the inhibition of the dihydropteroate synthetase by the sulfas
2. Altered enzyme:
decreased affinity for the sulfonamides
3. Decreased uptake:
decreased permeability of membrane

32. Oral, absorbable agents
Sulfisoxazole
Sulfamethoxazole
Sulfadiazine

33. Sulfisoxazole and sulfamethoxazole are used almost exclusively to treat urinary tract infections.
Sulfadiazine achieves high concentrations in cerebrospinal fluid, therefore it has preventative and therapeutic effective against Epidemic meningitis

34. Oral nonabsorbable agents
Sulfasalazine is widely used in ulcerative colitis, enteritis, and other inflammatory bowel disease.

35. Topical Agents
Sodium sulfacetamide
Mafenide acetate

36. Sodium sulfacetamide ophthalmic solution or ointment is effective treatment for bacterial conjunctivitis and as adjunctive therapy for trachoma.
Mafenide acetate is used topically to prevent bacterial colonization and infection of burn wounds.

37. Trimethoprim 1. The antibacterial spectrum is similar to that of
sulfamethoxazole
It inhibited dihydrofolate reductase
It is used alone in acute urinary tract infections and in the treatment of bacterial prostatitis
It induce megaloblastic anemia, leukopenia, and granulocytopenia
It altered dihydrofolate reductase, resulting in drug resistance

38. Co-trimoxazole Co-trimoxazole is combination of trimethoprim-
sulfamethoxazole
It shows greater antimicrobial activity than equivalent quantities of either drug used alone
It inhibits two sequential steps in the synthesis of tetrahydrofolic acid

39. pyrimidine nucleotide precursor
PABA + Pteridine
Dihydropteroate
synthase
sulfamethoxazole
Dihydropteroic acid
Glutamate
Dihydrofolate
Trimethoprim
(TMP)
Dihydrofolate
reductase(DHFR)
Tetrahydrofolate
Purine、
pyrimidine nucleotide
precursor

40. 4. Co-trimoxazole is used to treat upper respiratory infection, urinary tract infection， intestinal infection，typhoid fever
5. It is less frequently encountered than resistance to either of the drugs alone