CHELATING

AGENTS
• from the greek word “claw”

• First chelating agent: BAL (british

anti-lewiste)

CHELATION: organic molecules

which form stable complexes
with metal ions. Usually water
POISON ANTIDOTE COMMMENTS
Acetaminophen Acetylcystiene Given before 24 hours
ingestion activated
charcoal
Lead Calcium-EDTA Chelating agent

arsenic?/ other metals Dimercaprol Chelating agent

D- penicillamine
Lead, mercury, succiner Chelating agent
arsenic
Chelating agents
• Drugs that prevent or reverse
toxic effect of heavy metal on an
enzyme or other cellular target.

• Determined by number of
ligands groups. The greater the
number, the stable the metal
chelator complex.
DIMERCAPROL
• ( 2,3-dimercaptopropanol)
• Also known as BAL : prototype
• Given after Asenic exposure
• IM/ often painful
TOXICITY: contraindicated in
CHRONIC POISONING
(may redistribute mercury and
arsenic)
SUCCIMER
• (dimercaptosuccimic acid, DMSA)
• Water analog of dimercaprol
• Excreted in urine
• USA: oral prepartion available.
Other place is IV.
• Peaks at 3hours
• Half life: 2-4 hours
mech: binds to ammino acid
cystiene to form 1:1 and 1:2
mixed disulfide increasing
excretion.
ADV: G.I. Problem, rashes, n/v,
anorexia
EDTA
• (ethylene diaminetetraacetic acid)
• To prevent depletion of calcium,
preparation should only be CALCIUM
DISODIUM SALT.
• I.V. Infusion
• Contraindicated for anuria patient

2004: EDTA is FDA approved used to

uranium ,plutonium , americanium,
curium.
UNITHOL
• (dimercaptopropanesulfonic
acid)DMPS
• Water soluble to dimercaprol
• 1st used in Russia(1958)/ used in
USA (1994)

• Bioavailability: oral (50%)

peak:3-7 hr
• Used against mercury, arsenic,
lead.
TOXICITY: aqueous preparation
(50mg/kg in sterile water every 4
hours over 20 mins (slow I.V.)

Oral Unithol: alternative use for

succiner
• Adverse: limited to dermatologic
reaction
-urticaria
-Erythema multiform
-Steven – Johnson syndrome

Note: rapid infusion can cause

hypotension
PENICILLAMINE
• (D-dimethycystiene)
• White crystalline, water derivative
of penicillin
• Readily absorbed on GUT and
Metabolic degradation
Indication: copper poisoning (wilsons
dse)
severe rheumatoid
arthritis
Adv: hypersensitivity/nephrotoxicity
DEFEROXAMINE
• Isolated from STREP. PILOSUS

• Chelator of choice for iron poisoning

• Deferoxamine + hemodialysis
= tx for aluminum toxicity of renal
failure

• may increase iron absorption if given

orally

• Pathway is unknown
• Excreted in urine and causes
ORANGE-RED color.
ADV:
• Rapid I.V. = hypotension
• Idiosyncratic reaction
• Pulmonary comlication an
susceptibilty to infection ( seen
in long term use)
PRUSSIAN BLUE
• (ferric hexacyanoferate )
• Hydrated crystalline compund in
which Fe atoms are coordinated
with cyanide groups in a cubic
lattice structure.
MECH of ACTION: ion-exchange/
mechanical trapping on
adsorption to certain univalent
cations
• For cesium/ thallium
• Elimination via feces
INDICATION: 2003- FDA approved
treament for cesium
Dosage: 3g orally 3x/day
Serial monitoring/ fecal and urine
Contipation mmay occur
Reference
• Bertman G. Katzung (lange)

• John joseph fenton ( toxicology)

• Steven G. Gilbert (a small dose

of toxicology)
THANK YOU