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PM2A: Molecules and medicines > Heavy metals, Chelating metals: Medicinal Inorganic Chemistry 2 > Flashcards

Heavy metals, Chelating metals: Medicinal Inorganic Chemistry 2 Flashcards

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1
Q

Define what is heavy metal poisoning?

A

Toxic accumulation of heavy metals in soft tissue of the body

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2
Q

Describe what a heavy metal is and give some examples?

A
  1. Chemical that have a specific gravity (density) of 5 times more than water
  2. Examples: Lead, mercury, arsenic and cadmium
  3. Examples in body: zinc, copper, chromium, iron and manganese
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3
Q

Describe how sources of heavy metal enter the body, the problems it can have and contact sources?

A
  1. Enter via food sources, water, air or absorption through skin
  2. Competes with essential minerals like zinc, calcium, copper, magnesium: interferes with organ system
  3. Contact sources:
    - Industrial work
    - Pharmaceutical manufacturing
    - Agriculture
    - Children playing in contaminated soil
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4
Q

What are the causes and symptoms of heavy metal poisoning?

A
  1. Depends on the type of metal ingested and the concentration of it
  2. Symptoms typically: nausea, vomiting, diarrhoea, stomach pain, headache, sweating and metallic taste in mouth
  3. Impairment of cognitive features and motor skills
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5
Q

What are the main metals involved in heavy metal poisoning?

A

Transition metals:

  • Cr
  • Mn
  • Fe
  • Cu
  • Zn
  • Cd
  • Hg
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6
Q

How do you diagnose and detect different common heavy metal poisonings?

A
  1. Blood and urine tests
  2. Hair and tissue analysis
  3. X-rays
  4. Lead poisoning: have to do a blood test
  5. Mercury poisoning: blood and urine test
  6. Arsenic poisoning: Rapidly cleared from blood, in the urine (48 hours after seafood)
    - detected in abdomen via x rays
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7
Q

How do you treat heavy metal poisoning and give example of them?

A
  1. Chelating agent specific to the metal
  2. Oral, intravenous or intramuscular application
  3. Requires hospitalisation as the treatment can be painful
  4. Intravenous fluids necessary for shock, anaemia and kidney failure
  5. Calcium disodium edetate
  6. Penicillamine
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8
Q

Explain the action of chelation therapy in treating heavy metal poisoning?

A
  1. Chelating agents bind to the metal in the body
  2. Formation of a complex
  3. Complex is then filtered through the blood stream
  4. Kidneys filter the blood and the compounds
  5. Excretion of urine gets rid of it
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9
Q

Describe what chelation is?

A
  1. The binding of a polydentate ligand onto a metal ion- can form more than one co-ordinate bond to bind to the central co-ordination complex
  2. Polydentate ligands are known as chealtors or chealating ions
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10
Q

Define what chelation is?

A

Formation of two or more co-ordinate bonds between a polydentate ligand and a single atom

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11
Q

What does it mean when the denticity is equal to one and two?

A
  1. Monodentate ligand- formed 1 co-ordinate bond from ligand to metal
  2. Polydentate ligand- formed 2 co-ordinate bond from ligand to metal
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12
Q

Describe what EDTA is and how it works?

A
  1. The lead chelating agent that’s a synthetic amino acid
  2. Uncomfortable side effects
  3. Widely used to sequester di and tivalent metal ions
  4. Binds to metals via 4 carboxylate groups and two amine groups
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13
Q

What are the clinical uses of EDTA?

A
  1. Acute hypercalcemia- irreversibly collates to calcium to prevent blood from clotting
  2. Mercury poisoning
  3. Lead poisoning
  4. Measuring GFR alongside chromium (Cr-EDTA)
  5. Anti-coagulant for blood samples (K2-EDTA)
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14
Q

Describe Dimercaprol mechanism of action?

A

Acts on sulfhydryl residues on metabolic enzymes to create the chelate effect which inhibits enzyme activity

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15
Q

Describe the clinical uses of Dimercaprol?

A
  1. Arsenic poisoning
  2. Mercury poisoning
  3. Lead poisoning
  4. Wilsons disease: genetic disease where body retains copper
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16
Q

What are the disadvantages of using Dimercaprol?

A
  1. It’s poisonous by itself
  2. Has to be administered intramuscularly which is painful
  3. Can concentrate arsenic in some organs
  4. Narrow therapeutic range
  5. Multiple side effects
17
Q

Describe what penicillamine is and what its pharmaceutical form is known as?

A
  1. The alpha-amino counterpart of penicillin

2. Pharmaceutical form: D-penicillamine

18
Q

What are the medical uses of penicillamine?

A
  1. Immunosuppression in rheumatoid arthritis
  2. Used in Wilsons Disease to bind to the copper and newly formed complex is excreted in urine
  3. Used as 2nd treatment option for arsenic poisoning
  4. Cystinuria- used against the formation of cystine stones to create a mixed disulphide which is more soluble than cystine
19
Q

What are the common side effects associated with penicillamine?

A
  1. Bone marrow suppression
  2. Anorexia
  3. Diarrhoea
  4. Vomiting
20
Q

Explain the clinical use of DMSA?

A
  1. Number one use in the USA for mercury, lead and arsenic poisoning
  2. Can cross the blood brain barrier and be used against heavy metals stored there
  3. di-thiol with less side effects that EDTA and BSL
21
Q

Describe the clinical uses of DMPS?

A
  1. Used for mercury poisoning as the di-thiol prolongs the survival time
  2. Decreasing urinary mercury concentration
22
Q

Describe the clinical uses of ALA?

A
  1. Lipoic acid- used as a common supplement
  2. Compound is transformed in the body to di-thiol which is used in arsenic and mercury poisoning
  3. Treatment of Mercury poisoning as it can cross BBB and cell membrane
  4. Not clinically as effective as DMSA and DMPS for mercury poisoning however

PM2A: Molecules and medicines (22 decks)

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