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ANTIMICROBIAL DRUGS-2

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ANTIMICROBIAL DRUGS-2 Presented by: Sarbeel Al Mosddar Drugs that act on 50S subunit Chloramphenicol Antimicrobial Activity: Toxicity: MACROLIDES erythromycin ... – PowerPoint PPT presentation

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Title: ANTIMICROBIAL DRUGS-2


1
  • ANTIMICROBIAL DRUGS-2
  • Presented by
  • Sarbeel Al Mosddar

2
Drugs that act on 50S subunit
  • Chloramphenicol

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  • Antimicrobial Activity

Chloramphenicol has a wide spectrum of
antimicrobial activity
bacteriostatic.
Some strains of H influenzae, N meningitidis, and
bacteroides chloramphenicol bactericidal..
It is not active against chlamydia
The drug is commonly used as a topical
antimicrobial
5
  • Toxicity

Gastrointestinal disturbances
Gray baby syndrome
Aplastic anemia
6
MACROLIDES
  • erythromycin, azithromycin, and clarithromycin)

chlamydia, mycoplasma, legionella, gram-positive
cocci,
and some gram-negative organisms.
Azithrornycin has a similar spectrum of activity
but is more active against H influenzae,
Adverse effects include gastrointestinal
irritation (common),
skin rashes,
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CLINDAMYCIN
  • inhibit bacterial protein synthesis via a
    mechanism similar to that of the macrolides,

treatment of severe infec tions due to certain
anaerobes such as bacteroides.
prophylaxis of endocarditis in valvular disease
patients who are penicillin-allergic.
toxicity of clindamycin includes gastrointestinal
irrita tion, skin rashes, neutropenia
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LINEZOLID
  • drug-resis tant gram-positive cocci, including
    strains resistant to beta-lactams and vancomycin
  • - resistant Enterococcusfaecium).

Linezolid binds to a unique site on the 50S
ribosomal sub unit,
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Telithromycin
  • Ketolide group
  • Similar in structure and action to macrolide
  • Gram-positive and gram -negative bacteria
  • Treatment of community acquired pneumonia

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STREPTOGRAMIN S
  • Quinupristin-dalfopristin a combination of two
    streptogramins, is bactericidal

penicillin-resistant pneumococci,
methicillin-resistant) and vancomycin-resistant
staphylococci
resistant Entero coccus faecium.
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Inhibition of nucleic acid synthesis
  • Inhibition of precursor

Sulfonamides
active against gram-positive and gram-negative
bacteria.
nocardia. Shigella.Escherichia Selective action
in blocking folic acid synthesis
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Trimethoprim
  • Trimethoprim is a selective inhibitor of
    bacterial dihydrofolate reductase

dihydrofolate reductase is four to five orders of
magnitude
mammalian enzyme.
Trimethoprim plus sulfamethoxazole
22
Inhibition of DNA synthesis
  • Quinolones
  • Bactericidal
  • Inhibit DNA GYRASE

ciprofloxacin, ofloxacin, levofloxacin,
lomefloxacin, and sparfloxacin.
Fluoroquinolones are effective in the treatment
of infections
urogenital and gastrointestinal tracts caused by
gram-negative
respiratory tract, skin, and soft tissue
infections,
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Flucytosine
  • pyrimidine antimetabolite

Flucytosine is accumulated in fungal cells by the
action of a membrane permease
converted by cytosine deaminase to 5-FU, an
inhibitor of
thymidylate synthase
The antifungal spectrum of 5-FC is narrow
Cryptococcus neofor roans and possibly systemic
candidal infections.
25
Inhibition of mRNA synthesis
  • Rifampin

bactericidal against M tuberculo sis.
The drug inhibits DNA-dependent RNA polymerase
InTP rifampin is always used in combination with
other drugs.
prophylaxis against tuberculosis in
1NH-intolerant patients
26
Alternation of bacterial cell membrane
  • Polymyxins
  • Polypeptid
  • Polymyxin E most clinically useful
  • AGAINST gram-negative bacteria
  • Cationic detergent for phospholipids in plasma
    membrane

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daptomycin
  • Lipopeptide that disrupt the cell membrane of
    gram positive bacteria

29
Alternation of fungal cell membrane
  • Amphotericin B

Amphotericin B is the most important of the drugs
in treatment
of systemic mycoses
widest antifungal spectrum
the drug of choice for most systemic infections
caused by
aspergillus, Candida albicans, cryptococcus,
bind to ergosterol, a sterol specific to fungal
cell membranes, and cause the formation of
artificial pores
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  • Amphotericin B decreases the glomemlar filtration
    rate

tubular acidosis with magnesium and potassium
wasting.
Anemia
Liposomal formulations of amphotericin B have
reduced nephrotoxic effects,
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  • Nystatin
  • Only used topically for infection caused by
    Candidad
  • Azole

The azoles used for systemic mycoses
The azoles interfere with fungal cell membrane
permeability
hibiting the synthesis of ergosterol.
These drugs act at the step of 14c-demethylation
of lanosterol , which is catalyzed by a
cytochrome P450 isozyme.
Adverse effects of the azoles include vomiting,
diarrhea, rash,
34
Ketoconazole
  • narrow antifungal spectrum

backup drug for systemic infections caused by
certain blastomyces,
coccidioides, and histoplasma.
commonly for chronic mucocutaneous candidiasis
Fluconazole
Fluconazole is a drug of choice in esophageal and
oropharyngeal can didiasis
35
Additional drug mechanisms
  • Antibacterial activity
  • Isoniazid

the single most important drug used in
tuberculosis
inhibition of enzymes required for the synthesis
of mycolic acid
Neurotoxic effects are common and include
peripheral neuritis, restlessness, muscle
twitching, and insomnia.
administration of pyridoxine.
hepatotoxic
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Metronidazole
activity against protozoa and bacteria.
metronidazole is the drag of choice in
trichomoniasis
treatment of in- testinal amebiasis and amebic
hepatic abscess. HAVE 2 mechanismes of
action Electron sink Inhibit DNAsynthysis
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Ethambutol
  • Bacteriostatic

Ethambutol inhibits arabinosyl transferases
involved in the synthesis of arabinogalactan, a
component of mycobacterial cell walls.
The only use of ethambutol is in tuberculosis,
The most common adverse effects are
dose-dependent visual disturbances,
40
Antifungal activity
Griseofulvin Treatment of hair and nail
infection Bind to tubulin

41
  • Chemoprophylaxis
  • probiotics

42
  • Thanks for listening
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