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Pharm-antiprotozoals
pharm
45
Veterinary Medicine
Undergraduate 3
05/25/2012

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Term
name 6 anticoccidiostats
Definition
sulphonamides
amprolium
4-hydroxyquinolone
ionophores
benzeneacetonitiriles
halofugirone
Term
other antiprotozoals =
Definition
imidocarb
clindamycin
metronidazole
Term
why are coccidiostats mainly used as prophylactics?
Definition
-most are coccidiostats = decr ability to attack coccidia
-only affect invading sporozoites, NOT adults (once past sporozoite stage = coccidiostats are ineffective)
-dx of coccidial infection only possible late in infection - past point of tx
Term
admin of anticoccidials =
Definition
tend to be in water/feed
Term
sulphonamides largley used in...
Definition
....poultry, although less now due to R
...cattle and sheep
Term
sulphonamides have what effects?
Definition
antibacterial and antiprotozoal
Term
at low dose sulphonamides =
Definition
coccidiostatic
Term
at high dose sulphonamides =
Definition
coccidiocidal
Term
mech of sulphonamide =
Definition
competitive inhibitor of DHPS = block folate synth
Term
sulphonamide action is against...
Definition
...IC sporozoan para (as v low folate levels here, so none to take in and cant produce any cus of the drugs effects)
Term
sulphonamide synergises with what to make it coccidiocidal?
Definition
trimethoprim (inhibits DHFR)
Term
Amprolium is an analogue of...
Definition
...thiamine
Term
mech of amprolium =
Definition
thiamine analogue = selective inhibiton of protozoal thiamine pump (pumps thiamine into cell) = blocks thiamine transporter =disrupts coccidias CHO metab
Term
thiamine otherwise known as...
Definition
...vit B
Term
thiamine req for...
Definition
...CHO metab in protozoa
Term
deficiency of thiamine in host =
Definition
supression of coccidial infection/not susuceptible to coccidial infection
Term
spectrum of activity of amprolium =
Definition
confined to eimeria
Term
R and potnecy of amprolium =
Definition
little R development and mediocre efficacy
Term
amprolium often used as...
Definition
...prophylactic tx in chickens and cattle in conjunction with sulphonamides (To improve efficacy)
Term
site of action of 4-hydroxyquinolone =
Definition
unknown

possibly cytochrome O (specific metabolic enzyme of eimeria = block oxidation and therfore block mitochondrial resp)
Term
toxicity of 4-hydroxyquinolone?
Definition
relatively non-toxic as no effect on avian or mammalian mitochondria :)

and porr gut absorption = decr toxicity
Term
4-hydroxyquinolone used for...
Definition
....prophylactic tx of chickens, cattle and sheep
Term
4-hydroxyquinolones spectrum of activity =
Definition
limited to eimeria
Term
4-hydroxyquinolones activity =
Definition
coccidiostat
Term
most commonly used coccidiostat in poultry =
Definition
ionophores
Term
2 examples of ionophores
Definition
monensin
salinomysin
Term
mech of ionophore =
Definition
make cell mb perm to inorganic cations and form a complex with inorganic cations

exchange Na+ for K+ = disrupt ion balance = decr K+ in cell (K+ vital for metabolic activities)
Term
ionophore toxicity?
Definition
high - act on mammalian and avian cells as much as protozoa :(

Only usuable due to poor gut absorption
Term
ionophores can be used as what in cattle?
Definition
growth promoters - alter rumen flora, when admin orally, in favour of energy rich proprionate over acetate = incr FCR

BANNED
Term
ionophores are highly toxic to what sp?
Definition
horses LD50 =nearly 100x lower than for cattle when given orally
Term
why are horses much more susceptible to ionophore toxicity compared to cattle?
Definition
horses are monogastric = rapid absorption of drug = heart stops v rapidly due to ionic balance

Ruminants absorb alot of drug in ruminal flora
Term
why are horses much more susceptible to ionophore toxicity compared to cattle?
Definition
horses are monogastric = rapid absorption of drug = heart stops v rapidly due to ionic balance

Ruminants absorb alot of drug in ruminal flora
Term
host cells susceptible to ionophores =
Definition
mm and neurone = effect heart
Term
ionophores given in ...
Definition
...poultry feed
Term
if horses eat poultry feed containing ionophore, monensin =
Definition
will die
Term
halofuginone controls...
Definition
...cryptosporidosis in calfs
Term
Imidocard use =
Definition
restricted to use in cattle with babesia (red water fever)
Term
Imidocarbs TI =
Definition
low :(
Term
mech of Imidocarb =
Definition
unclear
Term
Clindamycine useful in tx of...
Definition
...anaerobic infections (many protozoa are anaerobic) and toxoplasmosis in cats
Term
clindamycins action =
Definition
targets protein synth of bacteria and protozoa
Term
metronidazole is useful for tx of...
Definition
...anaerobic bacterial and protozoal infections
Term
metronidazole is effective against..
Definition
...Giarda and Trichomonas in doga (anaerobic protozoa)
Term
mech of metronidazole =
Definition
prodrug - req reduction in anaerobic enviro to active form = free radical= binds to DNA and proteins and destroys them

therefore drug is inhibites/doesnt work in aerobic enviro
Term
protozoa R to metronidazole use...
Definition
...a mutant pyrivate oxidase which doesnt accept metronidazole as its cofactor
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