Antidotes: Its Mechanism and

Therapeutic Uses
• An antidote is an agent which counteracts a
poison
• In the treatment of acute poisoning most patients
require only supportive and symptomatic
therapy.
• The active removal of poisons from the stomach:
>by gastric lavage or
>emesis induction
>reduce the absorption.
 Mechanism of Action of Antidotes

1) Complex formation
2) Metabolic conversion
3) Prevention of toxic metabolite formation
4) By changing the physio-chemical nature of
toxicant
5) Promotes return to normal function by
repairing a defect or enhancing a function
that corrects the effects of poison.
 Classification of Antidotes
1) Chemical Antidotes, change the chemical nature of poison;
example:
sodium thiosulphate which changes toxic cyanide to the non-toxic
thiocyanate-sodium
calcium edetate chelates agents used for heavy metal poison.
2) Physiological Antidotes, producing the effect opposite to that of
poison:
sodium nitrite converts hemoglobin into methemoglobin in order
to bind cyanide.
3) Mechanical Antidotes, prevent the absorption of poison into the
body. example: activated charcoal absorbs the poison prior to
absorption across intestinal wall.
Copper sulphate, magnesium sulphate and sodium
monohydrogen phosphate inactivate and precipitate the toxic
material as insoluble salts by chelation
 drug Antidotes
Paracetamol (acetaminophen) (N-acetylcysteine)

Anticoagulants, E.G., Warfarin (Vitamin K)

Opioids (Naloxone)

Iron (and other heavy metals) (Desferrioxamine, Deferasirox or Deferiprone)

Benzodiazepines (Flumazenil)

Methanol (Ethanol or Fomepizole)

Cyanide (Amyl Nitrite, NaNitrite & Na Thiosulfate)

Calcium Channel Blockers
(Verapamil, Diltiazem) (Calcium Gluconate)
Beta-Blockers
Propranolol, Sotalol) (Calcium Gluconate and/or Glucagon)

Isoniazid (Pyridoxine)
Atropine (Physostigmine)
 PARACETAMOL
• Acetylcysteine (N-acetylcysteine) is used as a mucolytic
and to treat paracetamol overdose.
Acetylcysteine splits disulfide bonds in muco-proteins
and thus lowers mucus Viscosity, resulting in a larger
volume of sputum. Acetylcysteine is also an antioxidant
andmay protect the lung from free radicals generated
by inflammatory cells activated by influenza virus
infection.
• Acetylcysteine is used intravenously as an antidote for
severe paracetamol poisoning, in which it acts as a
thiol donor
 vitamin K
• No clear mechanism of aldesleukin-induced
coagulopathy has been identified, and the
efficacy of prophylactic vitamin K has been
disputed
• aldesleukin may activate the coagulation and
fibrinolytic system
 FLUMAZENIL
• It binds selectively to a subset of Benzo-
diazepine receptors
 NALOXON
• naloxone, an effective opioid antidote
• Morphine reduces the rate of transient lower
esophageal sphincter relaxation in patients
with reflux disease, thus reducing the number
of reflux episodes; the effect was reversed by
naloxone