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Antiprotozoals
Hsu
56
Pharmacology
Professional
11/01/2011

Additional Pharmacology Flashcards

 


 

Cards

Term

 

 

Coccidosis pathogens

Definition

Eimeria

Isospora

 

Affects growth of animal-young animals more seriously than adults (7-14 day old pigs, calves, puppies)

 

Treatment and prevention difficult

Term

 

 

 Anticoccidials in mammals

Definition

Decoquinate

Na+, H+-ionophores: monensin, lasalocid

Amprolium

Antifolates

Triazine derivatives: Idiclazuril (Clinacox), ponazuril (Marquis)

Term

Decoquinate

(Deccox)

Definition

Coccidistat (not -cidal)

Effective vs. sporozoites

decreased electron transport

 

ADM: 0.5 mg/kg/d in cattle feed for about 4 weeks

PK: Poor absorption after oral dosing

No preslaughter withdrawal

Adverse effects: None

 

Term
Ionophores: monensin, lasalocid
Definition

Isolated from Steptomyces spp.

Anticoccial activity vs all coccidia

(1st generation trophozoites, merozoites)

Growth promotant in ruminants


MOA: increased Na+, H+ entry->

1. Disrupts mictochondria

2. Disrupts Golgi

3. Increased osmolarity

4. decreased pH

Term

Ionophores

ADM

Definition
0.3-1 mg/kg/d in cattle feed for prevention
Term

Ionophores

PK

Definition

no information in mammals

in chickens monensin t1/2=2 hours, lasalocid t1/2=11 h

 

No preslaughter withdrawal

Do not use in calves

Can be used in lactating cows

Term
Ionophores adverse effects
Definition

increased Na+ entry=cell death

increased Na+ entry=increased Ca2+ entry into cells

increased myocardial contractility

increased Catecholamine release

degeneration of myocardium

monensin > lasalocid (horses!!!)

 

Mix thoroughly! Protect workers!

Term
Amprolium (Corid)
Definition

Quaternary compound

thiamine antagonist

coccidia are 50X more sensitive than animal cells

Effective vs 1st generation trophozoites, schizonts

 

Drug resistance: drug combination

Term

Amprolium

 

ADM

Definition
5 mg/kg/d in cattle feed for prevention
Term

Amprolium

 

PK

Definition

Poor absorption after oral administation

 

no preslaughter withdrawal

Term

Amprolium

 

Adverse effects

Definition
none at therapeutic doses
Term
Antifolates
Definition

Sulfonamides and dihydrofolate reductase inhibitors

Longest history for outbreak treatment and prevention

Peak activity vs 2nd generation schizonts

 

Sulfadimethoxine, sulfaquinoxaline, sulfamethazine

Ormetoprim, trimethoprim, pyrimethamine, methotrexate

Sulfadimethoxine+ormetoprim (Primor, Rofenaid)

ADM: 55 mg/kg (d1), then 27.5 mg/kg/d

Term

Diclazuril

 

(Clinacox, Protazil)

Definition

Diclazuril is approved for EPM and avian coccidiosis

 

For prevention and treatment of coccidiosis

Effective vs. coccidia in very young animals (stops oocyst shedding very soon after treatment is initiated)

 

Term

 

Diclazuril

 

MOA

Definition

effective vs. schizonts and gametes

inhibits nuclear division

Term

Diclazuril

 

ADM

Definition

Feed additive: 0.2% Clinacox; 1.56% Protazil

 

25 mg/kg PO, can redose 15 d later

Term

Diclazuril

 

PK

Definition

Protazil in horses is extralabel

 

Oral bioavailability: 5%

 

After oral dosing, Tp=8-24 h

 

B=43-65 h about 2 days

Term

Diclazuril

 

adverse effects

Definition
Safe when used as directed
Term
Ponazuril
Definition

Extra-label for coccidiosis

Active metabolite of toltrazuril (sulfone)

 

Used for EPM, toxoplasmosis

 

5x's less potent than diclazuril

 

Ponazuril past-Marquis paste=1 ml=150 mg ponazuril

1ml ponazuril +2 mlH2O->50 mg/ml

Term

Ponazuril

 

ADM

Definition

15-30 mg/kg, PO

may repeat after 10 days

Term

Ponazuril

 

PK

Definition
Beta=4.5 d in horses
Term

Ponazuril

 

Adverse effects

Definition

GI disturbances

Hypersensitivity

Term

3 anticoccidial drugs used for prevention

(not outbreak treatment)

Definition

Decoquinate

Ionophores

Amprolium

Term
3 Anticoccidial drugs used for prevention and outbreak treatment
Definition

Antifolates

Diclazuril

Ponazuril

Term
Anticoccidial drugs used on a single dose bases
Definition

Diclazuril (can redose after 15 days)

 

Ponazuril (can redose after 10 days)

 

Term
Why should diclazuril and ponazuril be used more frequently than other drugs?
Definition

 

They are much newer (less resistance) and work on latter part of the lifecycle

 

Term
Which anticoccidial has least residue problems?
Definition
Amprolium-no GI absorption
Term

Which group of anticoccidial drugs is most toxic to animals?

 

Definition
Ionophores-affect myocardium
Term
Equine Protozoal Myeloencephalitis (EPM)
Definition

Most important equine protozoal disease in US

Sarcocystis neurona infects opossum (definitive host)

Small mammals are intermediate host

Horse is aberrant, dead-end host

Infected by ingestion of sporocysts in contaminated feed/water

Schizonts in CNS

Clinical signs: head tilt, ataxia, muscle weakness, atrophy, urinary incontinence, constipation (stroke-like)

Term
Treatment of EPM
Definition

Tx on long term basis

1. Trimethoprim-sulfadiazine, pyrimethamine-sulfadizine (Rebalance), PO, daily for over 30 days

2. Ponazuril (Marquis) PO 5 mg/kg/d for 28-56 days

3. Diclazuril (Protazil) PO 1 mg/kg/d 28 days

4. Anti-inflammatories: flunixin, phenylbutazone, glucocorticoid, DMSO

Physical therapy following chemotherapy

Term

Ponazuril Paste (Marquis) vs EPM

 

spectrum

Definition

treatment of coccidiosis, EPM, toxoplasmosis, neosporosis

broad spectrum, cross BBB

Term

Ponazuril paste vs EPM

 

MOA

Definition
vs. schizonts by inhibiting nuclear division
Term

Ponazuril paste vs EPM

 

ADM

Definition

5 mg/kg/d, PO, 4 wk

after a grain meal

Term

Ponazuril paste vs EPM

 

PK

Definition

Tp=18d

 

B=4.5 d (after multiple doses)

Term

Ponazuril vs EPM

 

adverse effects

Definition

blisters on nose and mouth

skin rash and hives

GI disturbances

colic

seizures

Do not use in sick/debilitated animals due to other disorders

 

Relapse in 5-30% cases

Term

Diclazuril (Protazil) vs EPM

 

formulation

Definition

pellets as feed additive

 

similar to ponazuril, more potent

Term

Diclazuril vs EPM

 

ADM

Definition
1 mg/kg/d, PO, 4 wk, mix in grain meal
Term

Diclazuril vs EPM

 

PK

Definition

Tp=18 h

B=43 h

Term

Diclazuril vs EPM

 

adverse effects

Definition

similar to ponazuril

 

blisters on nose and mouth, skin rash and hives, GI disturbances, colic, seizures

Term
Metronidazole (Broad Spectrum)
Definition

Nitroimidazoles: dimetridazole, ipronidazole, metronidazole

 

Metranidazole is a human drug

 

For giardiasis, histomoniasis, babesiosis, trichomoniasis, amebiasis

Term

Metronidazole

 

MOA

Definition

disruption of helical structure of DNA by active metabolite

(Ferrodoxin-linked M)

Term

Metronidazole (Flagyl)

 

ADM

Definition
10-30 mg/kg after food, bid or tid for 5-7 days
Term

Metronidazole

 

PK

Definition

GI absorption, 50-100%

 

Tp=1 h, widely distributed

 

excreted in urine in 24 hours: 50% metranidazole, 50% metabolites

Oxidation followed by conjugation: excreted in urine in 24 h

B=3-5 h

Term

Metronidazole

 

adverse effects

Definition

GI disturbances

CNS disturbances

Mutagenicity, cardiogenicity

Neutropenia

Term
Benzimidazoles
Definition

Albendazole and fenbendazole-against giardiasis

 

Anti-infective with broadest spectrum

Term

Benzimidazoles

 

ADM

Definition
25 mg/kg, bid for 2 d; after food
Term

Benzimidazoles

 

Adverse effects-albendazole

Definition

may be toxic to liver, bone marrow

teratogen

Term

Control of cryptosporidiosis

 

3 drugs

Definition

Paromomycin (Humatin)

 

Nitrozoxanide (Alinia)-in humas

25 mg/kg, PO, bid, food, 7-28 d

 

Azithromycin (Zithromax)

15 mg/kg, bid, 14 d

Term
Paromomycin for cryptosporidiosis
Definition

an aminoglycoside for extra-label use, very expensive

 

potential to prevent and treat cryptosporidiosis (125 mg/kg, PO, bid, 5 d)

No PK given for animals

minimal systemic absorption when given PO

 

Adverse effects: vomiting, diarrhea, colic, nephrotoxic, deafness

Term

 

Babesiosis

 

characteristics

Definition

Protozoans that parasitize RBC's, cause anemia

endemic in southern states-Florida, Texas

Sporadic cases in horses in Indiana, Wisconsin, Minnesota

Ticks-vectors

direct animal to animal transmission can occur

 

Tx with Imidocarb (Imizol)

Term

Imidocarb (Imizol)

 

MOA

Definition
binds DNA of babesia and denatures it
Term

Imidocarb

 

ADM

Definition

IM or SC

in dogs, 6.6 mg/kg, repeat dose in 2 weeks

in horses, for b. caballi: 2 mg/kg x 2d

for B. equi, 4 mg/kg, q 72 h x 4

 

Do not use in food animals

Term

Imidocarb

 

PK

Definition

readily absorbed from injection site

 

B=3.5 h

 

Excreted in urine and feces as parent compound

Term

Imidocarb

 

Adverse effects

 

Definition

Injection pain and inflammation 1-7 d

 

Stimulation of parasympathetic NS, SLUDD (decreased AChE)

Teratogenicity and carcinogenicity

 

Precautions: No cholinergic stimulants

don't use in pregnant animals

Should use with atropine

Term

Toxoplasmosis and Neosporosis

 

Definition

Neosporosis->encephalomyelitis in dogs, abortion in cattle

Vertical transmission in dogs and cattle

Pharmacological control in dogs only

 

 

Term
Anti-Toxoplasmosis and Anti-Neosporosis Drugs
Definition

Trimethoprim-sulfadiazine->15 mg/kg, bid 4 wks

 

Pyrimethamine (0.25-0.5 mg/kg)+sulfadiazine (30 mg/kg), bid, 4 wk

 

Clindamycin->10-20 mg/kg, PO, IM, bid for 3-6 wk

*preferred treatment

 

Ponazuril 7.5-15 mg/kg/d for 4 wk

Term
Coccidia lifecycle
Definition
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