1

Penicillins

- bactericidal
-
transpeptidase peptidoglycans

- penicillns

( penicillns-binding proteins,PBPs )
PBP1A,1B,2,3,4,5,6 PBPs

-

peptidoglycan

1. Pneumococci

2. Streptococci URI
endocarditis
3. Meningococci
4. Staphylococci penicillinases
()
5. Anaerobes periodontal
6. Gonococci 4
7. Spirochetes
8. Corynebacterium diphtheriae
9. Clostridium
10.

1.
Penicillin v
- 125 . 250 . 125 250 ./

2.
2.1 Aqueous crystalline Na or K salt Penicillin G
(
) 620 4-6
2.2 Penicillin G procaine suspension
24
3 -6 1-2
2.3Penicillin G benzathine suspension
4
6 -1.2
grA
betahemo lytic Streptococcus Syphilis

1. maculopapularrash
anaphylaxis
2.
thrombophlebitis

3. microflora

Cephalosporins

1. First generation cephalosporinase

( ) anaerobes
Ps.aeruginosa
2. Second generation cephalosporinase

Ps.aeruginosa
3. Third generation cephalosporinase

Ps.aeruginosa
4. Fourth generation Cefpirome
Cefepime

Cephalothin
Cefadroxil
1 Cefazolin
Cephalexin,
Cephapirin*
cefalexin
Cephradine *
Cephradine*
?

Cefamandole
Cefaclor
2 Cefoxitin
Cefuroxime axetil
Cefuroxime
Cefprozil
Cefonicid*
Loracarbef
Ceforanide*
Cefmetazole*
Cefotetan*

Cefotaxime
Cefdinir
3 Ceftriaxone
Cefixime
Cefoperazone
Cefpodoxime
Ceftazidime
proxetil
Ceftizoxime*
Ceftibuten
Moxalactam*
Cefditoren pivoxil

Cefepime
4 Cepirome

- Penicillins

- bactericidal bacteriostatic

1 First Second generation

- : Cefazolin t1/2

- : first generation

Cefmandole

(
K.pneumoniae H.influenzae )
- : Cefamandole
Cefoxitin
( E.coli K.pneumoniae )
-
Cefoxitin
2 Third generation
-
- PPNG type : Cefotaxime Ceftraxone
-
Cephalosporins 2 Aminoglycosides

1.
Penicillins
- Anaphylaxin
2.



Pseudomembranous colitis (
Clostridium difficile)
3. Cephaloridine

Aminoglycosides
4. Methylthiotetrazole side chain
Cefamandole,Moxalactam,Cefoperazone
prothrombin time
intestinal flora
5.
( disulfiramlike effect )
methylthiotetrazole side chain 4
6. Candida
Pseudomonas
7.


Cephalothin

Macrolides

Erythromycin

Erythromycin




Penicillins Mycoplasma
Haemophilus influenza

Ophthalmia Neonatorum

50S

bacteriostatic mature organism

bactericidal ( cell wall)

penicillin ( penicillinase-producing
organism)
Erythromycin,

Erythromycin Estollate [Ilosone] Erythromycin Stearate

[Erythrocin; Bristamycin] Dry syrup

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Erythromycin
Ethylsuccinate Erythromycin Gluceptate ;
Erythromycin Lactobionate

1-4 / 6
30-50 ./ 1 .. / 6

Erythromycin Stearate

Cholestatic hepatitis

Lincosamides
Lincomycin, Clindamycin
mechanism of action; same as macroliddes
clinical use;
- anaerobe , diabetic
food infection,
- ( clindamycin cream )

Chloramphenicals
Chloramphenical
inhibit proteins synthesis by binded 30s ribosome
clinical use;
- alternative in treatment bacyeria meningitis
- mellioidosis
- Anaerobe

- ricketsia
tetracycline
ADR;
- Allergic reaction ; rash, fever, anaphylaxis
- Grey baby syndrome; vomitting, abdominal distention,
cyanosis, hypothermia--- immature hepatic function of
neonates

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- Bone marrow suppression

Tetracyclines

Tetracycline
Tetracycline
3
1.Short-acting tetracycline hydrochloride
chlortetracycline oxytetracycline
2.Intermediate acting demeclocycline methacycline
3.Long acting doxycycline minocycline

Tetracyclines 30-S
subunit ribosome Mrna aminoacyl-tRNA
mRNA ribosome complex acceptor site ( A site)
Tetracyclines

rickettsiae, chlamydia
host
Tetracyclines
host Tetracyclines

Tetracyclines

amphotericin B polymyxin B

Tetracycline

Rickettsiae Chlamydia Mycoplasma Spirochetes
Tetracycline
Tetracycline
doxycycline minocycline
Tetracycline Streptococcs pneumoniae
S.pyogenes Tetracycline Streptococcs
Tetracycline Streptococcs
Tetracycline Tetracycline
, cephalosporin 1
Tetracycline Staphylococus aureus
Tetracycline minocycline
Tetracycline
Listeria monocytogenes

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Tetracycline

Tetracycline
Nesseria
N. gonorrhoeae N.meningitidis N. gonorrhoeae
PPNG Tetracycline
H. influenzae Tetracycline
Escherichia coli , Klebsiella
Tetracycline

Tetracycline
N. gonorrhoeae Tetracycline
mutation E.coli

species
Tetracycline

Tetracycline

Tetracycline
chlortetracycline
25-30 minocycline
98 Tetracycline pH pH
Tetracycline
Tetracycline

ferrous sulfate Tetracycline
Tetracycline
cimetidine
sodium bicarbonate
Tetracycline Tetracycline
Short-acting doxycycline
minocycline

Tetracycline
Tetracycline

aqueous
humor Tetracycline
Tetracycline

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Tetracyclines
Tetracyclines

1. rickettsiae Rocky mountain spotted

fever Brill.s disease (epidemictyphus) murine typhus scrub
typhus rickettsialpox Q fever
2. Mycoplasma pneumoniae
Tetracyclines Tetracyclines,demeclocycline
erythromycin
3. Chlamydia Lymphogranuloma venereum
Tetracyclines 500 . 4
2 doxycycline 100 . 2
2
2
4. Tetracyclines

anogemnitalia,pharynx

spectinomycin

Chlamydia trachomatis genital mycoplasma

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1.




Tetracyclines

2. Tetracyclines

normal flora

enterocolitis Clostridium
difficile staphylococci
Candida albican

3. Tetracyclines
Tetracyclines

2 4-6 doxycycline
Tetracyclines
4. Tetracyclines

demeclocycline doxycycline
Tetracyclines minocycline

5. Tetracyclines

2

6. Tetracyclines
azotemia doxycycline
Tetracyclines
urea nitrogen
(BUN)

Tetracyclines doxycycline
minocycline

Tetracyclines Fanconi
syndrome

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proximal tubule

7. Tetracyclines

Tetracyclines (fixed-drug eruption )

Minocycline
cranial nerve
8 vestibular

Aminoglycoside

30S subuit

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m-RNA (translation)

Aminoglycoside 30S subunit

(passive transport) (active

transport) Penicillins Cephalosporins
Aminoglycosides

Aminoglycosides

Pseudomonus aeruginosa

Streptomysim sulfate
15 25 // ( 2
12 ) 7-10
20-40 // ( 2
12 )
10-20 //
( 2 12 )

Aminoglycosides

1.

2. Aminoglycosides

Cephaloridine ,
Amphotericin B , Polymyxin B , Colistin , Vancomycin
Ethacrynic Furosemide
3. Aminoglycosides


4.
myasthenia gravis
5. Aminoglycosides

QUINOLONES

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Quinolones
E.coli, Salmonella, Shigella, Enterobacter,
Campylobacter Neisseria DNA
gyrase DNA

E.coli, Shigella,
salmonella, Campylobacter, Staphylococcal

Nitrofurantoin
50-100 4
1-2

Sulfonamides
Sulfadiazine , Cotrimoxazoles ( Sulfamethoxazole + trimethoprim )
clinical use;
-
-

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P. carinii
HIV
- Mellioidosis
- Toxoplasmosis

PABA
dihydropteroate synthetase hydrofolate synthetase

DNA , RNA

1.

2.
G6-PD

3.

4.


3-5
-

Nitroimidazoles
intestinal extra intestinal sites
asymptomatic intestinal amoebiasis

Metronidazole

Nitroimidazoles anaerobic
microaerophilic microorganism hypoxic cell nitro
group metonidazole electron transport

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protein flavoproteins ferredoxins

nitro reductase
flain radical nitro compound reduction
iron sulfur complexs eleetron
reduetion reduced nicotinamide
adenine dinucleotide phosphate ( NADPH) sulfide
reduced form
DNA
T.vaginalis Clostridium bifermentans
DNA antimicrobial
mutagenic effect

50 . 1
10 /.
8 10 volume of
distribution 1
10%


unchanged metronidazole metabolites

Metronidazole 250 . 500 .

BENZOYL METRONIDAZOLE

triochomoniasis
250 . 3
7
4 6
2 .


trichomonas
250 . 3 7

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