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Principles of Antidotal Action
PHAR340
20
Pharmacology
Undergraduate 3
12/06/2012

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Term
Chelating agents
Definition
Antidote complexes with poison rendering it inactive
Complex formed with heavy metal is readily excreted
Term
Dimercapol (BAL)
Definition
Arsenic binds to –SH groups in dimercaprol to form a stable 5-6 membered ring
Less toxic, though dimercapol tends to cause hypertension
Hydroxyl group increases solubility and excretion
Antidote complexes with poison rendering it inactive
Term
Calcium disodium edetate (Ca-EDTA)
Definition
Lead has a higher affinity for EDTA than calcium
Dimercapol, penicillamine, DMSA are also effective for lead poisoning
Free EDTA may deplete Ca2+ stores in the body
Antidote complexes with poison rendering it inactive
Term
Penicillamine
Definition
Treatment for lead and copper poisoning
Antidote complexes with poison rendering it inactive
Term
Deferoxamine
Definition
Treatment for iron poisoning
Antidote complexes with poison rendering it inactive
Term
Pralidoxine
Definition
Anticholinergic
Treatment for organophosphate poisoning (AChE inhibitor)
2-PAM removes organophosphorus molecule from Ache
Antidote complexes with poison rendering it inactive
Term
Nitrite
Definition
Hemoglobin (Fe2+) → Methemoglobin (Fe3+)
Treatment for cyanide poisoning
Not potent, rare but rapid cause of death
Increase availability of Fe3+ for CN- binding
Reactivate cytochrome oxidase
Susceptible to nitrite poisoning
Antidote complexes with poison rendering it inactive
Term
Protamine
Definition
Treatment for heparin (anticoagulant) poisoning
Antidote complexes with poison rendering it inactive
Term
Antitoxins
Definition
Treatment for toxins
Antidote complexes with poison rendering it inactive
Term
Thiosulfate
Definition
Sulfur donor to accelerate the detoxification reaction
CN- → CNS- via transsulfurase
Administer in combination with nitrite
Antidote accelerates metabolic conversion of poison to non-toxic product
Term
Ethanol
Definition
Blocks metabolic conversion of methanol to toxic formaldehyde
Administer base to neutralize acid
Ethanol has a higher affinity for ADH and ALDH than methanol
Antidote blocks metabolic conversion of poison
Term
Chloride supplement
Definition
Treatment for bromide poisoning
Administration of chloride will increase overall halide excretion
Antidote accelerates excretion of poison
Term
Calcium salts
Definition
Treatment for 90Sr
Antidote accelerates excretion of poison
Term
Hyperbaric oxygen
Definition
Treatment for CO poisoning
Reduced number of binding sites for O2 and lesser O2 release in the tissues
O2 cam compete with CO for the binding site in heme
Antidote competes with poison for essential receptors
Term
Edrophonium
Definition
Treatment for tubocurarine poisoning: non-depolarizing nicotinic blocking agent
AChE inhibitor increase [Ach] which competes for the receptor
Antidote competes with poison for essential receptors
Term
Atropine
Definition
Treatment for AChE inhibitor e.g. organophosphates, nerve gas
Blocks muscarinic receptor
Prevention of bronchoconstriction and hypersecretion of fluids
Administered in combination with pralidoxime to block nicotinic receptors at ganglia and neuromuscular junction
Artificial respiration may also be required
Antidote blocks receptors responsible for toxic effect
Term
Methylene blue
Definition
Treatment for methemoglobinemia from nitrite poisoning
metHb is a lethal vasodilator but used to treat cyanide poisoning
Increases rate of reduction of methhemoglobin to hemoglobin
HbFe3+ → HbFe2+ via methemoglobin reductase
Acts as an intermediate electron acceptor between NADPH and metHb
Antidote restores normal function by repairing or by-passing effect
of the poison
Term
K+ salts, anti-dysrhythmics
Definition
Treatment for digitalis poisoning
Digitalis is used to treat CHF but may cause arrhythmias
Antidote restores normal function by repairing or by-passing effect
of the poison
Term
Thymidine
Definition
Treatment for 5-fluorouacil overdose (anti-cancer drug)
Anti-cancer drugs resemble DNA subunits and can prevent DNA synthesis and division of cancer cells
However, some regular cells are also in a constant dividing state
Administer nucleotides to combat anti-cancer drug poisoning
Antidote restores normal function by repairing or by-passing effect
of the poison
Term
Purines
Definition
Treatment for 6-mercaptopurine overdose (anti-cancer drug)
Anti-cancer drugs resemble DNA subunits and can prevent DNA synthesis and division of cancer cells
However, some regular cells are also in a constant dividing state
Administer nucleotides to combat anti-cancer drug poisoning
Antidote restores normal function by repairing or by-passing effect
of the poison
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