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Metabolism Inhibitors
VM 607 Final
24
Veterinary Medicine
Professional
02/28/2012

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Term
Sulfonomides Group
Definition
Sulfamethoxazole
Sulfadiazine
Sulfadimethoxine
Term
Sulfonomides Mechanism of Action
Definition
penetrate bacteria
compete with PABA to inhibit folic acid synthesis in bacteria
Term
Sulfonomides Activity
Definition
bacteriostatic
time-dependent
decreased by pus or necrotic tissues
Term
Sulfonomides Spectrum of Action
Definition
Gram + and Gram -
broad spectrum
aerobes only
mainly extracellular bacteria
some protozoa
Term
Sulfonomides Combinations
Definition
additive or synergistic activity with diaminopyrimidines
Term
Sulfonomides Pharmacokinetics
Definition
partial oral absorptions
extracellular distribution
good penetration in fluids (CSF and prostatic secretions)
liver metabolism
mixed liver and renal elimination
Term
Sulfonomides Adverse Effects
Definition
dose-dependent adverse effects
inhibits thyroid function in dogs (reversible)
avoid using in hypothyroid dogs or adjust T4 drugs accordingly

Keratoconjunctivitis sicca is rare in dogs
monitor tear production and avoid in dogs with chronic eye disease

very rare urinary disturbances

cytopenia (NOT dose-depedent) in combined diaminopyrimidine and sulfonamide
immune-mediated cytopenia due to sulfonamide
Term
Sulfonomides Allergic Reactions
Definition
rare in dogs
less frequent than B-lactam allergies
Term
Sulfonomides Clinical Usage
Definition
use carefully in dogs with hypothyroidism or with eye disease
don't use in Dobermans/Doberman pinchers unless it is life-threatening
usually used in combination with diaminopyrimidines
off-label use BANNED in lactating dairy cattle
Term
Diaminopyrimidines Group
Definition
end in -oprim
Trimethoprim
Ormetoprim
Term
Diaminopyrimidines Mechanism of Action
Definition
prevents activation of folic acid to folinic acid
this inhibits RNA and DNA synthesis
Term
Diaminopyrimidines Activity
Definition
bacteriostatic
time-dependent
more active that sulfas on their own
Term
Diaminopyrimidines Spectrum of Action
Definition
Gram + and Gram -
broad spectrum
aerobic bacteria only
extracellular and intracellular bacteria
wider spectrum for protozoa
Term
Diaminopyrimidines Pharmacokinetics
Definition
well absorbed orally
distributes extracellularly and intracellularly
good penetration in fluids and deep tissues
liver metabolism and excretion
Term
Diaminopyrimidines Adverse Effects
Definition
dose-dependent side effects due to folate deficiency
blood cytopenia when used at high doses and/or for long periods of longs (reversible)
avoid in pregnant animals
can supplement with folic acid
Term
Potentiated Sulfonamides Group
Definition
combined sulfonamides and diaminopyrimidines
Sulfamethoxale-Trimethoprim
Sulfadimethoxine-Ormetoprim
Sulfadiazine-Trimethoprim
Term
Reason for Potentiated Sulfonamides
Definition
sequential mechanism of action in folic acid synthesis pathway
combination potentially bactericidal even though the drugs separately are bacteriostatic
extension of spectrum to intracellular microbes
extension of tissue penetration
Term
Potentiated Sulfonamides Activity
Definition
bacteriostatic separately
bactericidal with certain bacteria and once certain concentrations are reached
time-dependent
Term
Nitrofurans Mechanism of Action
Definition
go after energy production pathway
deprives bacteria from key energy production pathway
also damages DNA
Term
Nitrofurans Group
Definition
Nitrofurantoin
Term
Nitrofurans Action
Definition
bacteriostatic or bacteriocidal
can go after 4 quadrants
Gram +, Gram -, anaerobic, aerobic, protozoa
Term
Nitrofurans Pharmacokinetics
Definition
extracellular distribution
mainly renal excretion very quickly
get concentrated in urine in active form
Term
Nitrofurans Adverse Effects
Definition
dose-dependent toxicity
common drug allergy
Term
Nitrofurans Clinical Usage
Definition
locally for otitis, keratitis
systemically for UTIs with multi-resistant bacteria
BANNED in food animals
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