Metal ions are used in medicine for both diagnostic and treatment purposes. Some metals like technetium, gadolinium, and iron are used in medical imaging techniques like MRI. Platinum compounds like cisplatin are commonly used to treat cancers by binding to DNA and interfering with cell division. While effective, metals can cause side effects if levels become unbalanced or toxicity occurs from treatment. Precise application of metal ions exploits their properties for medical benefit.
4.18.24 Movement Legacies, Reflection, and Review.pptx
Metal Ions in Medicine and Diagnosis
1. Metal Ions In Medicine
SAKHARKAR MOHD ANZAR
MSC-I
SEM-II
INORGANIC CHEMISTRY
Ramniranjan Jhunhunwala college
2/12/2013 By Mohd Anzar Sakharkar 1
2. Metal Ions in Medicine
Metals in medicine are used in organic
systems for diagnostic and treatment
purposes.
Inorganic elements are also essential for
organic life as cofactors in enzymes
called Metalloproteins.
When metals are scarce or high
quantities, equilibrium is set out of balance
and must be returned to its natural state.
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3. Metals in diagnosis
Metal ions are often used for diagnostic
medical imaging.
Metal complexes can be used either for
radioisotope imaging (from their emitted
radiation), for example, in magnetic resonance
imaging (MRI).
2/12/2013 By Mohd Anzar Structure
Sakharkar 3
4. Examples of metals used for
diagnosis:Tc is the most commonly used
Technetium:
radioisotope agent for imaging purposes. It has a
short half-life, emits only γ ray photons, and does
not emit β or α particles and thus is particularly
suitable as an imaging radioisotope.
Gadolinium(III), Iron(III), Manganese(II): For MRI
imaging paramagnetic metals are needed for
contrast imaging. Gd(III), Fe(III), and Mn(II) are all
paramagnetic metals that are able to alter the
tissue relaxation times and produce a contrast
image.
Cobalt(III): Co(III) is used with the compound
bleomycin, which is an antibiotic, to be selectively
be taken up by tumor cells. The use of Co results
in the best blood-to-tumor distribution ratio, but its
half-life is too long to be conducive for imaging
purposes 2/12/2013 By Mohd Anzar Sakharkar 4
5. Metals in treatment
Metals have been used in treatments since ancient
times.
Sodium vanadate has been used since the early 20th
century to treat rheumatoid arthritis.
Recently metals have been used to treat cancer, by
specifically attacking cancer cells and interacting
directly with DNA. The positive charge on most metals
can interact with the negative charge of the phosphate
backbone of DNA.
Some drugs developed that include metals interact
directly with other metals already present in protein
active sites, while other drugs can use metals to
interact with amino acids with the highest reduction
potential.
Cisplatin, a platinum Anzar Sakharkar complex.
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coordination 5
6. Examples of Metals used in
treatment
Platinum: Platinum based compounds have been shown to
specifically effect head and neck tumors.
Gold: Gold salt complexes have been used to
treat rheumatoid arthritis.
Zinc: Zinc can be used topically to heal wounds. Zn2+ can be
used to treat the herpes virus.
Silver: Silver has been used to prevent infection at the burn
site for burn wound patients.
Tungsten: Tungsten polyoxoanions can be used to treat AIDS.
Platinum, Titanium, Vandium, Iron: cis DDP (cis-
diaminedichoroplatinum), titanium, vanadium, and iron have
been shown to react with DNA specifically in tumor cells to
treat patients with cancer.
Gold, Silver, Copper: Phosphine ligand compounds containing
gold, silver, and copper have anti-cancer properties.
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7. Cisplatin
Cisplatin, cisplatinum, or cis-
diamminedichloroplatinum(II)
(CDDP) is a chemotherapy drug. It
was the first member of a class of
platinum-containing anti-cancer drugs.
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8. Cisplatin is administered intravenously as
short-term infusion in normal saline for
treatment of solid malignancies.
It is used to treat various types of cancers,
including sarcomas, some carcinomas (e.g.
small cell lung cancer, and ovarian cancer),
lymphomas, and germ cell tumors.
Cisplatin is particularly effective against
testicular cancer; the cure rate was improved
from 10% to 85%
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9. Mechanism of action
Following administration, one of the chloride ligands is
slowly displaced by water in a process termed
aquation.
The aqua ligand in the resulting [PtCl(H2O)(NH3)2]+ is
itself easily displaced, allowing the platinum atom to
bind to bases.
Of the bases on DNA, guanine is preferred.
Subsequent to formation of [PtCl(guanine-
DNA)(NH3)2]+, cross-linking can occur via displacement
of the other chloride ligand, typically by another
guanine.
The damaged DNA elicits DNA repair mechanisms,
which in turn activate apoptosis when repair proves
impossible.
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10. DNA binding
Cisplatin binds to DNA and causes a
critical structural change in the DNA –
a bend of 45 degrees.
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11. Cisplatin resistance
Cisplatin combination chemotherapy is the
cornerstone of treatment of many cancers.
Initial platinum responsiveness is high but the
majority of cancer patients will eventually
relapse with cisplatin-resistant disease.
Oxaliplatin is active in highly cisplatin-resistant
cancer cells in the laboratory; however, there
is little evidence for its activity in the clinical
treatment of patients with cisplatin-resistant
cancer
The drug paclitaxel may be useful in the
treatment of cisplatin-resistant cancer; the
mechanism for this activity is unknown.
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12. Carboplatin
Carboplatin, or cis-Diammine(1,1-
cyclobutanedicarboxylato)platinum
(II) is a chemotherapy drug used
against some forms of cancer (mainly
ovarian carcinoma, lung, head and
neck cancers)
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14. Side effects
Nephrotoxicity (kidney damage) is a major
concern. The dose is reduced when the
patient's creatinine clearance (a measure
of renal function) is reduced.
Myelotoxicity: This agent can also cause
profound bone marrow suppression.[15]
Hemolytic anemia can be developed after
several courses of cisplatin. It is
suggested that an antibody reacting with a
cisplatin-red-cell membrane is responsible
for hemolysis.[16] 2/12/2013 By Mohd Anzar Sakharkar 14
15. Neurotoxicity (nerve damage) can be
anticipated by performing nerve conduction
studies before and after treatment.
Nausea and vomiting: cisplatin is one of the
most emetogenic chemotherapy agents.
Ototoxicity (hearing loss): there is at present
no effective treatment to prevent this side
effect, which may be severe.
Electrolyte disturbance: Cisplatin can cause
hypomagnesaemia, hypokalaemia and
hypocalcaemia. The hypocalcaemia seems
to occur in those with low serum magnesium
secondary to cisplatin, so it is not primarily
due to the Cisplatin.
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