Antidotes

ANTIDOTES
Dr. E. B. Theodory, (MD)

VIHAS
• According to WHO
• “Antidote was defined as a therapeutic substance used to counteract
the toxic action(s) of a specified xenobiotic.”
• Antidotes reduce the overall burden of health service in managing of

poisoning cases
Classifications of antidotes
According to mode of Action:
• Physical
• Chemical
• Physiological/pharmacological
According to Site of Action:
1. Interacts with the poison to form a non toxic complex that can be
excreted:e.g. Chelators
2. Accelerates the detoxification of the poison e.g. Nacetylcystine,
thiosulfate
3. Decrease the rate of conversion of poison into toxic metabolite
e.g.Ethanol, Fomepizole
4. Compete the poison for certain receptors.:e.g. Nalaxone
5. Block the receptor through which the toxic effect of the poison is
mediated e.g.Atropine
6. Bypass the effect of Poison:O2 in the treatment of CO and cyanide
toxicity
7. Antibodies to the poison : digiband and antivenoms
Physical Antidote:
• Agent use to interfere with poison through physical properties, not

change their nature
a) Adsorbing: The main example is activated charcol
b) Coating: A mixture of egg & milk make a coat over the mucosa.
c) Dissolving: 10% alcohol or glycine for carbolic acid
CHARCOL:
(Universal Antidote)
• Produced by heating pulverized carbonaceous substances sawdust,

peat, or coconut shells
• Activation: Hot air to erode the internal surfaces of the product and
thereby increase its adsorptive surface area.
• Adsorption results from weak intermolecular forces
• AC can prevent systemic absorption of drugs when given within 1-2 h
of ingestion
How is activated charcoal used
as an antidote?
• As an antidote, activated charcoal is mainly known both for its use in
drug overdoses and chemical poisonings.
• Charcoal acts to purify and cleanse the body due to its amazing ability
to attract poisons to itself.
• Charcoal has a wide range of absorption.
• Heavy metals, viruses, bacterial and fungal toxins, etc. are all
absorbed effectively.
• Activated charcoal often absorbs more than its own weight of
injurious materials.
How does charcoal work?
• Internally as an antidote and remedy, charcoal works by binding drugs
and poisons within the gastrointestinal tract.
• This allows their transfer out of the body in a harmless form.
• Charcoal absorbs like a sponge, and renders poisons harmless.
• It can do varied tasks because of it’s amazing ability to attract other
substances to its surface and hold on to them until they exit the body.
How does charcoal work with
drug or aspirin poisoning
• The most common drug poisoning is from aspirin.
• Charcoal should be given within the first 30 minutes of an overdose.
• Powdered charcoal reaches its maximum rate of absorption rapidly,
within one minute.
• The sooner it is given the better the chances of successful treatment.
• Charcoal given after one hour of fast absorbing drugs, like aspirin, are
usually only about 10 percent effective.
Charcoal Effect
Common side effects of Charcoal
• Antidote:
Black Stools (severe)
Diarrhea (Less severe)
Vomiting (Less severe)
Rare side effects of Charcoal
• Antidote:
Stomach Cramps (severe)
Swelling of the Abdomen (less severe)
Chemical Antidote:
• Interact specifically with a toxicant, or neutralize the toxicant. e.g.

metal chelators combine with metals to form complexes that can then
be eliminated by the kidneys
• Mainly act by two mechanisms:
Complex Formation:
• Antidote make complex with the toxicant making it unavailable to
cross the membrane or to interact with receptors
• Dimercaprol and dimercaptosuccinic acid are sulfohydral compounds
that bind metal such as arsenic acid ,lead.
• Sp. Binding agents like EDTA, defroxamine and D-pencillamine act by
chelation of metal forming more water soluble complex
• Antivenins and antibodies against digitoxin are immunologicaly
genrated agents that bind specifically to the toxin or venom
Metabolic conversion:
• Detoxification to less toxic product
• Nitrite interact with hemoglobin and cyanide to form
cyanomethamoglobin which is less toxic than cyanide and interfare
with the cyanide access to cytochrome oxidase system.
Cyanide Effect
Common side effects of cyanide antidote
• intravenous:
Abnormal Heart Rhythm (Severe)
Abnormally Low Blood Pressure (Severe)
Coma (Severe)
Confuse (Less severe)
Fast Heartbeat (Less Severe)
Headache (Less severe)
Rare side effect of cyanide Antidotes:
Increased Risk of Bleeding (Severe)
Excessive Sweating(Less Severe)
Feeling Weak(Less Severe)
Rapid Breathing(Less Severe)
Taste Problems(Less Severe)
Dimercaprol Effect:
• Common side effects of Dimercaprol:
Weakness.
Headache.
fever (especially in children).
pain or a hard lump(swelling) where the medicine was
injected.
Throwing up.
Pharmacological antidote:
• Counteract the effects of a poison by producing the opposite

pharmacological effects, e.g., ACHE inhibitors atropine
• Pharmacologic antidotes may neutralize or antagonize the effects of a
toxicant.
• This type of antidote may act by following 5 mechanism.
3. By competing with the Toxicant’s action at a receptor site:
a) Antagonism:
• Competitive antagonism:
Naloxone/Naltrexone: Opioid dependence, longer action and affinity for
mu receptor.
Flumenazil: Antagonist for Benzodiazepine
Atropine: organophosphate, carbamate and other
parasympathomimetic antidote.
• It is also used to correct bradycardia caused by morphine, digitalis, beta
blockers etc
b) Non Competitive Antagonism:
• Calcium gluconate:
Used for Calcium channel blocker especialy Verapamil
Black widow spider bite
Lead colic
Oxalic acid
• Paralidoxime :ChE activator act by breaking Alkyl phosphate ChE bond. It is used
in organophosphate toxicity.
• Diacetyl Monoxyime(DAM): action same as PAM but with more BBB penetration.
• Physostigmine: Counteract the anticholinergic effect
4. By blocking receptors responsible for the toxic effect :
• The physiologic effect induced by a toxin is prevented by an antidote,
although the toxicant is unchanged and may still be active.
Example:
• Atropine blocks the physiologic effect of acetylcholine at cholinergic
synapse and neuromuscular junction ,and in organophosphate toxicity
5. By aiding in the restoration of normal function:
• The antidote promotes return to normal function by repairing a defect or
enhancing a function that correct the effect of poison.
Example:
• Methylene blue:
In nitrite poisoning, methylene blue interact with reduced NADPH to reduce
the ferric iron of methemoglobin back to ferrous ion in hemoglobin, which can
again transport oxygen
• Acetylcysteine :
Acetylcysteien supplies the precursor amino acids for glutathione, which
serves as biologic antioxident against acetaminphen toxicosis
• Poison is harmful substance which when comes in contact with a
living being produces abnormal effects on health
Sources –chemical toxins, insecticides, pesticides, micro-organisms
and snake venoms,
Major drugs involved in poisoning
• Paracetamol.
• Aspirin.
• Benzodiazepines.
• SSRIs.
• Anticonvulsants.
• Other analgesics including NSAIDs.
Poisoning substances other than
drugs
• Petroleum distillates.
• Nature toxins as mushrooms.
• Industrial chemicals.
• Toiletries.
• Household products.
• Agrochemicals.
Antidotes in most common use in
clinical toxicology
• Paracetamol: N-acetyl Cysteine
• Opioid: Naloxone.
• Iron: Desferroxamine
• Heparin- Protamine Sulphate
• Cyanide- Sodium Nitrate, Sodium
Thiosulphate
• Theophylline, Caffine- Esmolol
• Atropine – Physostigmine
• Curare Poisoning – Neostigmine
• Arsenic- Dimercaprol
Antidotes
• Lead –calcium disodium edetate
• Streptokinase, fibrinolytics- epsilon amino caproic acid
• Insulin- glucose
• Digilatis –digoxin specific antibody fragments
• Methanol –ethanol, fomepizole
• Carbon monoxide-oxygen
• Nitrates- methylene blue
• Warfarin- vitamin K1 oxide
THE END

Antidotes

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ANTIDOTES

Dr. E. B. Theodory, (MD)

• Antidotes reduce the overall burden of health service in managing of

• Agent use to interfere with poison through physical properties, not

• Produced by heating pulverized carbonaceous substances sawdust,

• Interact specifically with a toxicant, or neutralize the toxicant. e.g.

• Counteract the effects of a poison by producing the opposite

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