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Sulfonamides Trimethoprim and Quinolones
Sulfonamides Trimethoprim and Quinolones
trimethoprim and
Quinolones
By
S. Bohlooli, PhD
School of Medicine, Ardabil University of Medical
Sciences
Antifolate drugs
Sulfonamides
Trimethoprim
Trimethoprim & Sulfamethoxazole
mixture
Sulfonamides: chemistry
Sulfonamides: mechanism
of action
Inhibition of
dihydropetroate
synthase
Sulfonamides:
antimicrobial activity
Sulfonamides: resistance
Overproduction of PABA
Low affinity dihydropetroate
synthase
Loss of permeability to
sulfonamides
Sulfonamides:
pharmacokinetics
Oral absorbable
Short
Medium
Long
Oral,
nonabsorbable
topical
Serum protein
bind
20 ~ 90%
Excreted into
urine
Sulfisoxazole, sulfamethoxazole
Sulfadiazine: toxoplasmosis
Sulfadoxine: long acting, in a combination for
treatment of malaria
Topical agents
Sulfacetamide: ophthalemic
Mafenide & silver sulfadiazine: topically
Sulfonamides: adverse
reactions
Hematopoietic disturbance
Trimethoprim: chemistry
Trimethoprim: resistance
Trimethoprim:
pharmacokinetics
Clinical use
Oral trimethoprim
Oral trimethoprim-sulfamethoxazole
Intravenous trimethoprim-sulfamethoxazole
Adverse effects
Megaloblastic anemia
Leukopenia, granulocytopenia
Can be prevented by folinic acid
The AIDS patients have high
frequency of unwanted reactions
Fluoroquinolones
Nalidixic acid and cinoxacin
Fluoroquinolones:
chemistry
Fluoroquinolones:
chemistry-2
Fluoroquinolones:
antibacterial activity
Fluoroquinolones:
resistance
Change in permeability
Loss of affinity
Fluoroquinolones:
pharmacokinetics
Pharmacokinetic Properties of
Fluoroquinolones
Fluoroquinolones: clinical
uses
Bacterial diarrhea
Fluoroquinolones: adverse
effects