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Anticholinesterase Insecticides

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Anticholinesterase Insecticides
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posted:
11/16/2011
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Anticholinesterase

Insecticides

• Organophosphates

• Carbamates

• Variable toxicity

• Toxicity usually occurs from misuse

of products or improper storage

Mechanism of Action



Inhibition of acetylcholinesterase

Signs of Toxicity

• Muscarinic

• Salivation, lacrimation, urination,

diarrhea, miosis, dyspnea, bradycardia

• Nicotinic

• Muscle fasciculations beginning with

face, generalized tremors, weakness

• CNS

• Respiratory depression, clonic-tonic

seizures

Diagnosing Toxicity

• Clinical signs

• Decreased AChE activity (Blood,

Brain)

• Test dose of atropine

• Chemical analysis for specific

compounds

Treatment of Anti-Esterase

Toxicity

• Atropine sulfate for muscarinic

signs, dose to effect; will not stop

nicotinic signs

• Oximes can reactivate AChE before

aging

• Diazepam or barbiturates for

seizures

Ethylene Glycol

• Major ingredient in normal antifreeze

• Toxicity usually in small animals

• Exposure most common in Spring

and Fall

• Animals often “like” ethylene glycol

Mechanism of Action

• Ethylene glycol acts like ethanol,

producing early signs of

“drunkeness”

• Metabolism to glycolic acid causes

acidosis

• Metabolism to oxalic acid which

combines with calcium to form

insoluble crystals

Signs of Toxicity

• 3 stages of intoxication

• Stage I (30 minutes-3 hours)

• “drunkeness”, ataxia, depression. Often not

observed

• Stage II (12-24 hours)

• Tachypnea, tachycardia (or bradycardia)

• Often not observed

• Stage III (12-72 hours)

• Oliguric renal failure. Prognosis is poor

here.

Diagnosing Toxicity

• Acidosis

• Anion and osmolal gap

• Crystalluria

• Crystals in kidney and urine.

• Clinical sign.

Oxalate Crystals

Granular appearance.

Oxalate Crystals

Treatment of Ethylene

Glycol Toxicity

• Traditional treatment is ethanol and

bicarbonate

• Ethanol is competitive inhibitor of

Alcohol Dehydrogenase (ADH) which is

initial 1st step in EG metabolism. 3hours

• Bicarbonate used to correct acidosis.

Good for CNS signs.

• 4-methylpyrazole and Antizol® are ADH

inhibitors that can replace ethanol

Acetaminophen

• Present in many OTC pain and cold

remedies (Tylenol)

• Metabolized extensively by the liver

by Glucuronidation, sulfation.

• Activated by P450 to reactive

compound detoxified by GSH

• When GSH is depleted, toxicity

occurs

Signs of Toxicity

• Methemoglobinemia, ( brown blood)

Heinz body formation in cats

• Cyanosis, dyspnea.

• Facial and paw edema *

• Anorexia, vomiting

• Humans and dogs develop hepatic

necrosis in overdoses.

Acetaminophen

Facial Edema

Acetaminophen

Hepatic Necrosis

Acetaminophen

Hepatic Necrosis

Treatment of APAP

Toxicity

• GI Decontamination, emesis

,charcoal

• N-acetylcysteine (Mucomyst®) to

replenish and substitute for GSH

• Ascorbic acid used to treat

methemoglobinemia in cats,

methylene blue in other animals

Methylxanthines

• Caffeine, theobromine, theophylline.

• Usually a problem with dogs due to

eating habits.

• Found in chocolate, coffee,

medications

• Unsweetened baking chocolate is

especially toxic; as little as 0.2 oz/kg

may kill a dog

Mechanism of Action

• Antagonist of adenosine receptors;

causes CNS stimulation,

vasoconstriction, and tachycardia

• Prevents Ca++ reuptake

• Inhibits phosphodiesterase

Signs of Toxicity

• GI… Vomiting, diarrhea

• Hyperactivity

• Tachycardia, PVC, hypertension

• Ataxia

• Tremors, seizures

• Coma

Treating Methyl-Xanthine

Toxicity

• Monitor EKG

• Treat tachyarrhytmias with lidocaine

(not in cats) or metoprolol

• Treat seizures with diazepam or

barbiturates

Anticoagulant Rodenticides

• First generation compounds

• Warfarin

• Short-half life (15 hours), low potency,

required multiple feeding.

• Second generation compounds

• Brodifacoum, bromodialone, diphacinone

• Long half-life (15-20 days); high potency (one

feeding)

• 0.25 mg/kg often toxic

Anticoagulants

• Usually a problem in small animals.

• If cat or wild animal eat rat who has been

poisoned. They will be poisoned as well.

• Large animals can develop similar

problems from moldy sweet clover

Mechanism of Action

• Inhibits vitamin K epoxide reductase.

• Results in depletion of vitamin K

dependent clotting factors (II, VII, IX,

X).

Signs of Toxicity

• Delayed onset as clotting factors are

consumed (3-5 days).

• Initial signs are often depression,

anorexia, and anemia.

• Pale mucosa, dyspnea, nosebleeds, and

bloody feces.

• Abdominal pain.

• Hemorrhage and hematoma. (carful when

you give an injection).

Diagnosing Toxicity

• Increased prothrombin (PT) time

• Increased activated partial

thromboplastin time (APTT or PTT)

• Chemical analysis

Treatment of Anti-Coagulant

Toxicity

• Vitamin K1 administration (giving

oral is more effective than injectable

V.K )

• Therapy should be continued for 10-

14 days with warfarin; 21-30 days for

second generation compounds.

• Transfusion.

Strychnine

• Alkaloid used as pesticide to control

gophers, moles, rats, and coyotes

• Controlled in most states

• Still commonly used as a malicious

poison

• All species are sensitive but dogs are

most commonly poisoned.

Mechanism of Action

• Competitive inhibitor of glycine at

postsynaptic neurons

• Glycine NT is inhibitory so result is

disinhibition (stimulation)

Signs of Toxicity

• Initial signs are anxiety and stiffness

• “Grinning” muscle pull back around the teeeth.

• Violent tetanic seizures usually initiated by

sudden noise or light , normal between seizure

• Saw horse stance

• Persistent rigid extensions of all limbs (extensor

muscle are stronger so they dominate).

• Apnea due to rigidity of muscle.

Treating Strychnine

Toxicity

• Control seizures with pentobarbital

(as much as anesthesia level to be

effective) or Methocarbamol

(Robaxin), muscle relaxing.

• Prevent asphyxiation

• May require intubation and

respiratory support.

Metaldehyde



•Slug and snail baits

•Generally 3.5%

metaldehyde

•Ingestion of 1-4 oz of bait

will cause toxicity in

average dog

•Toxicity is most common

in dogs

Mechanism of Action

• Metaldehyde is hydrolyzed to

acetaldehyde by gastric acids

• Further metabolism of acetaldehyde

to acidic products thought to

account to acidosis

• Exact mechanism is unknown

Signs of Toxicity

• Initial signs are anxiety, nystagmus

• Progresses to salivation, vomiting,

ataxia, seizures, hyperthermia

• Profound acidosis.

• “Formaldehyde”-like smell

Treating Metaldehyde

Toxicity

• Control seizures with diazepam or

barbiturates

• GI decontamination

• Treat acidosis with fluids and

bicarbonate

• Treat hyperthermia . Ice packs.

Cholecalciferol

• Vitamin D3

• Used as a rodenticide

and psoriasis

treatment

• Usually sold as a bait

preparation

• Toxicity occurs at

doses above 0.5mg/kg

Mechanism of Action

• Metabolized to 1,25-

dihydroxycholecalciferol

• Increases serum Ca by increasing GI

absorption, decreasing renal

excretion, and stimulating bone

resortpion

Signs of Toxicity

• Vomiting, diarrhea

• Polydipsia, polyuria, radio-opaque

kidneys

• Elevated serum Ca (>11.5 mg/dl),

BUN, and creatinine

• Mineralization of soft tissues.

Tissue Mineralization

Tissue Mineralization

Treating Vit D Toxicity

• IV saline and furosemide (excretion)

• Cortisone (work opposit of PTH )

• Calcitonin immediate reverse

• Low Ca diet and avoid sunlight

• Continue treatment until Ca

stabilizes in normal range (up to 2

weeks).

Lead Toxicosis

• Affects large and small animals;

waterfowl.

• Sources include old paint, motor oil,

grease, batteries, lead shot and

fishing sinkers.

• Toxicity usually results from acute

oral exposures to lead.

Mechanism of Action

• Multiple actions, many based on the

reaction of Pb with –SH groups of

key enzymes and effects on calcium

regulation (important to CNS).

• Lead inhibits delta-aminolevulinic

acid dehydratase and heme

synthetase, both involved in heme

synthesis (blood signs)

Signs of Lead

Poisoning

• Lead causes a mixture of neurologic,

GI, and hematopoietic signs

• Neurologic signs include blindness,

seizures, ataxia, head-pressing,

“roaring”-horses.

• GI signs include anorexia, vomiting,

constipation then diarrhea (often

bloody), colic

Signs of Lead Poisoning

• Hematopoietic signs include

regenerative anemia with nucleated

RBCs,

• Basophilic stippling of RBCs (dogs).

• Increased zinc protoporphyrin

(dogs),

• elevated plasma porphyrins (cattle)

might florence if hold under black

light.

Diagnosing Lead Poisoning

• Clinical signs

• Whole blood lead levels of 0.6part

per million (ppm) or greater

• Decreased serum d-ALAD activity,

increased urine d-ALA

Treating Lead Toxicity

• GI decontamination using a cathartic

or surgical removal of large objects

• Chelation therapy with Ca-EDTA,

DMSA (Succimer) (more effective but

not approved for vet use),

• d-Penicillamine

• Thiamine may improve symptoms in

cattle

• Control seizures with barbiturates.

Oxalate Containing Plants

• Many members of the Areaceae family of

plants contain preformed Ca-oxalate

crystals that cause mechanical injury

(needle shape ) to the mouth resulting in

pain, salivation, vomiting, dyspnea

(mostly cats)

• Dieffenbachia, Caladium, Philodendron,

Calla lily

Oxalate Containing

Plants

• Plants containing soluble oxalates

produce hypocalcemia and renal injury

due to precipitation of Ca-oxalate crystals

• Examples are Rhubarb, Beets, Lamb’s

quarters

• Detoxification with limewater (calcium

hydroxide) and supportive treatment of

hypocalcemia and nephrosis.

Nitrates

• Sources are plants and fertilizer

• Ruminants are most susceptible due

to conversion of nitrate to nitrite in

rumen

• Nitrite oxidizes hemoglobin to

methemoglobin

Signs of Nitrate Toxicity

• Methemoglobinemia, “chocolate”

brown blood

• Brownish cast to membranes

• Cyanosis, dyspnea

• Tachycardia

Treating Nitrate

Toxicity

• Convert methemoglobin to

oxyhemoglobin with methylene blue

(except cats) (ascorbic acid) .

• Avoid overdosing as methylene blue

can cause methemoglobinemia

• Avoid stressing animals

Cyanide

• Released from cyanogenic glycosides

found in some plants (wild cherry and

other Prunus spp., Sudan and Johnson

grass, arrowgrass) ruminant most

susceptible.

• Acts by inhibiting cytochrome oxidase

which inhibits oxidative phosphorylation

Signs of Cyanide Poisoning

• Initial signs are salivation and

tachypnea

• Progress to dyspnea, weakness,

seizures, tachycardia

• Death in 20-120 minutes

• *Cherry-red blood that clots slowly*

(over oxygenated)

Treating Cyanide

Toxicity

• Cyanide binds tightly to Fe(III)

• Convert hemoglobin to

methemoglobin with sodium nitrite

• Promote detoxification of cyanide

with sodium thiosulfate.

Other Sources of

Information

• American Board of Veterinary

Toxicolgy

– www.abvt.org

• ExToxNet

– http://ace.orst.edu/info/extoxnet/


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