Chelation" root word,

"chele" Greek for the

claw of a lobster or crab. 
Chelating Agents[claw]
People exposed to heavy metals in
the environment-occupational
Metallic contamination of food and
water-Ind.pollutants
Metals leached from eating
utensils and cookware. Toys
Pesticides and therapeutic agents
Burning of fossil fuels containing
heavy metals*
Heavy metals combine with
reactive groups essential for normal
physiological functions.
“Heavy-metal antagonists possess
the common ability to form
complexes with heavy metals and
thereby prevent or reverse the
binding of metallic cations to body
ligands.”
Complex soluble & non toxic
These drugs are chelating agents.*
 An ideal chelating agent

High solubility in water: Distribution

Resistance to biotransformation. Th.efeciency
Reach sites of metal storage
Form nontoxic complexes with toxic metals
Retain chelating activity at the pH of body fluid
Ready excretion of the chelat
A low affinity for Ca2+ also is desirable
The most important property of a therapeutic
chelating agent is greater affinity for the metal
than that of the endogenous ligands*
 Dimercaprol[British anti-lewisite (BAL)]

 Developed as antidote to “Lewisite”.

 Chemistry: Oily fluid with a pungent, disagreeable
odor
 MOA: Formation of chelation complexes between its
sulfhydryl groups and metals.
 1:1 with metal not stable. 2:1 stable
 More effective in preventing inhibition of sulfhydryl
enzymes than in reactivating them.
Uses of BAL
I.m. not oral
As, Hg, Pb, Au, Bi, Ni, Poisoning
Adjuvant in Pb poisonong
Adjuant in Cu poisoning
C.I. in Fe, Cadmium
 ADE: rise BP, Tachycardia, vomiting, tingling,
inflammation of m.m.
2mg/kgx2d. OD 10 d. C.I.Organic or elemental
Succimir: Similar to BAL [Dimercatosuccinic
acid] *
Edetate Calcium Disodium (CaNa2EDTA)
 EthyleneDiamineTetraAcetic acid (EDTA) →
Na2EDTA →cation used to make a water-soluble
salt of EDTA →hypocalcemic tetany → “Edetate
calcium disodium (CaNa2EDTA)”

 Chelates Pb, Zn, Cd, Mn, Cu and some

radioactive metals
 Exchanges with Ca.
 Not orally absorbed
 i.m., Does not cross BBB*
[CaNa2EDTA] Uses:
 Lead poisoning- MOST IMP USE
 Not in Hg → Hg is bound in inaccessible regions.
 Chelation therapy with CaNa2EDTA for
atherosclerotic plaque → without therapeutic
rationale
ADE:
 NO TETANY
 Anaphylactoid reaction
 Acute febrile
 Tubular necrosis*
Penicillamine:

Isolated in 1953 from

the urine of patients
receiving penicillin.
Uses.
Cu, Hg, Zn, Pb poisoning.
Penicillamine uses contd…
Wilson’s disease[Hepatolenticular
degenaration] → Cerulospasmin is
deficient → cu accumulates in liver,
basal ganglion → life long therapy →
0.5g orally before food. [Trientine is
the alternate drug].
Cystin stones.
Scleroderma → increases soluble
collagen.
Rh.Arthritis.*
 Deferoxamine[Desferioxamine]

Isolated as the iron chelate from

Streptomyces pilosus
Poorly absorbed orally
i.v. for acute poisoning, i.m. for
chronic(e.g., thalassemia along with
blood)
Life saving-children
Does not affect Fe in Hb.*
ADE; histamine release,
allergic reactions, fall in B.P.,
urticaria.
Iron-BAL complex toxic
Deferiprone: orally
effective iron chelator, less
effective*
Others
Unithol: water soluble analog of
Dimercaprol
Deferasirox: orally effective
against Fe
Prussian blue: Against
radioactive Cesium “DIRTY
BOMB”*
Oxytocin is most effective in
stimulating the uterus during
A.  I trimester
B. II Month of pregnancy
C. II Trimester
D. III Trimester

 Ans: D
Oxytocin usually administered by
following route:

B. Orally
C. Intravenously
D. Sublingually
E. All of the above
 Ans: B
Oxytocin has a half life of

B. 4-6minutes
C. 40-60 minutes
D. 1-2hours
E. 90 minutes
 Ans: A
Overdose of oxytocin may result in

B. Water intoxication
C. Fetal anoxia
D. Rupture of the uterus
E. All of the above
 Ans: D
Which of the following IS NOT true
of Oxytocin
B. It is as potent as Vasopressin in antdiuretic
activity
C. It can not be given orally
D. It stimulates milk ejection reflex in humans
E. Has greatest pharmacological value in elective
induction of labour
 Ans: A
D.O.C to Lead poisoning is

C. BAL
D. Penicillamine
E. CaNa2Edetate
F. Deferoxamine
 Ans: C
Chelating agent that can reactivate
sulfahydryl groups is

B. CaNa2Edetate
C. Dimercaprol
D. Penicillamine
E. All of the above

 Ans: B
Chelating agent that produces tetany
unless given in Ca chelate form is

B. Na2Edetate
C. Dimercaprol
D. Penicillamine
E. Deferoxamine
 Ans: A.