* Some most common
antidotes
Dr. Nasiara Karim
Assistant Professor
* 3. Antidotes
*An antidote is a substance which can counteract a form
of poisoning.
OR
*A substance used to treat poisoning which has a specific
action depending on poison.
Chemical antidotes
It neutralizes the poison by changing the chemical
nature of poison e.g. dimercaprol
Mechanical antidotes
It prevents the absorption of poison e.g. activated
charcoal
Physiological antidote
It counteract the effect of poison by producing opposite
physiological effects e.g. naloxone
Agent Indication
Activated charcoal with sorbitol Used for many oral toxins
Atropine Organophosphate and carbamate
insecticides, some mushrooms
Beta blocker Theophylline
Calcium chloride Calcium channel blockers
Chelators such as EDTA, dimercaprol, Heavy metal poisoning
Penicillamine
Cynaide antidote (Amyl nitrite, Cyanide poisoning
Sodium nitrite or thiosulphate)
Deferoxamine maleate Iron poisoning
Digoxin immune Fab antibody Digoxin poisoning
(Digiband, Digifab)
Diphenhydramine and Benztropine Extrapyramidial reactions associated
with antipsychotic (Chlorpromazine)
Flumazenil Benzodiazepines
Glucagon Beta blocker poisoning and calcium
channel blocker poisoning
100 % oxygen Carbon monoxide poisoning
Leucovorin Methotrexate
Naloxone hydrochloride Opioid poisoning
N-acetylcysteine Paracetamol
Pralidoxime hydrochloride Organophosphate insecticides
Protamine sulphate Heparin sulphate
Physostigmine sulphate Anticholinergic poisoning
Pyridoxine Isoniazid poisoning
Vitamin K Warfarin poisoning
Mechanism of action of some common
antidotes
CHARCOAL
Also known as Activated Charcoal
Mode of action
Activated charcoal binds to drugs and poisons, thereby reducing absorption
either by binding the substance before absorption in the GIT .
Indications
GI decontamination for drug or poison ingestion associated with significant
risk of toxicity.
Dosage
1 g/kg to a maximum of 50–100 g for each dose of activated charcoal.
Repeat doses may be required every 4–6 hours
* ACETYLCYSTEINE
Mode of action
It is a Precursor for glutathione synthesis.
Glutathione bind to reactive metabolite of Paracetamol (N-acetyl para
benzoquinone imines) (and other drugs) and conjugate them and prevent
hepatotoxicity.
* Repletion of glutathione also directly reduces oxidative cell injury.
Acetylcysteine may also improve hepatic perfusion in established liver injury due
to paracetamol or other insults.
Dosage & method of administration
Acetylcysteine is either given by the oral or parenteral route. Several
protocols are suggested according to patient’s criteria
Oral
•Loading dose 140mg/kg of the 10% or 20% solution diluted to 5% in
juice or soda.
•Maintenance dose: 70mg/kg every 4 hours for 17 doses [i.e. 72
hours], another option is to give 8 maintenance doses [i.e. 36 hours] if
liver function tests are normal.
Parental Dose
The initial dose is 150 mg/kg given in 200 ml of dextrose over 15
minutes, followed by 50 mg/kg in 500 ml of dextrose (5%) over 4 hours
and finally 100 mg/kg in 1000 ml dextrose is given over the next 16
hours.
CYANIDE KIT
CYANIDE KIT CONTAINS Sodium nitrite and Sodium thiosulphate
injectable solution and amyl nitrite (0.3
ml) crushable ampules for inhalation.
* They oxidize hemoglobin to methemoglobin, which binds the
cyanide to form nontoxic cyanmethemoglobin.
* Inhalation
of an ampule of amyl nitrite produces a
methemoglobin level of 5%.
* Intravenous administration of a single dose of sodium nitrite is
anticipated to produce a methemoglobin level of about 20-30%.
Dosage and method of administration
• Amyl Nitrite is administered by inhalation for up to 30
seconds every 2 to 3 minutes. Up to 6 ampules can be
used.
• Amyl nitrite is followed by infusion of 300 mg or 10
mg/kg IV sodium nitrate, over 2-5 minutes.
• Then inject 12.5 g sodium thiosulfate IV over 10 minutes
PRN; may repeat both injections at 1/2 original dose.
Antidotes should be administered in patients who are
clinically symptomatic (i.e., unstable vital signs, acidosis,
impaired consciousness, seizures, or coma).
Deferoxamine
Deferoxamine is produced by actinobacter Streptomyces
pilosus. It has medical application as chelating agent and
used to remove excess poison from body.
Mechanism of action
• Deferoxamine act by binding free iron in the blood stream and
enhancing its elimination in urine. By removing excess iron , the
agent reduces the damage to various organs and tissues such as
the liver.
• A recent study also shows that it speeds healing of nerve
damage.
Uses
• It is used to treat acute iron poisoning
• It is also used to treat hemochromatosis, a disease of iron
accumulation that can be either genetic or acquired.
• It is also used to treat aluminum toxicity in some patients
Dimercaprol
Was developed by British biochemists at Oxford
university during world war II. It was developed
secretly as antidote for Lewisite. Today it is used
medicinally in the treatment of arsenic, mercury
and lead and other toxic metal poisoning.
It has also been used in wilson disease, a genetic
disorder in which the body tends to retain copper.
Lewisite is an organoarsenic compound. It was
once manufactured in the U.S., Japan, and
Germany[2] for use as a chemical weapon, acting as
a vesicant (blister agent) and lung irritant.
Mechanism of action
Dimercaprol competes with the sulfhydral groups
for binding the metal ion which is then excreted in
urine.
Penicillamine
It is a metabolite of penicillin although it has no
antibiotic properties. The pharmceutical form is D-
penicillamine as L-penicillamine is toxic.
Indications
• Used as immunosuppressant in rheumatid arthritis. It
works by reducing the number of T-lymphocytes,
inhibiting macrophage function, decreasing IL-1 and
preventing collagen from cross linking.
• It is used as chelating agent
• Used in wilson disease as it binds copper and
enhance its elimination through urine.
• Also used in mercury poisoning
Naloxone
It is indicated in patients with opiates drugs such as
• Morphine
• Codeine
• Heroine
• Methadone
These drugs tend to produce extreme drowsiness
associated with respiratory compromise and hypoxia.
Mechanism of action
It acts as competitive antagonists at opioid receptors
Dose: 0.2-4 mg I/V bolus, repeat every 2-3 minute intervals untill
desired response is obtained.
Naloxone is usually diluted with sufficient amount of 5% dextrose
or normal saline to provide adequate fluid maintenance for the
patients.
