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Toxicology Semmelweis > TOX 4- Pharmacology of chelators > Flashcards

TOX 4- Pharmacology of chelators Flashcards

1
Q

chelators

A
  1. DIMERCAPROL (2,3-dimercaptopropanol, BAL, dithiol chelator)
  2. SUCCIMER (dimercaptosuccinic acid, DMSA)- water soluble forms of dimercaprol
  3. DMPS (dimercaptopropan-sulfonic acid) - water soluble forms of dimercaprol
  4. PENICILLAMINE (d-dimethylcysteine) - water soluble derivative of penicillin, orally administered
  5. EDTA CALCIUM DISODIUM (ethylenediaminetetraacetic acid, EDTA)
  6. DEFEROXAMINE
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2
Q

mechanism of action- DIMERCAPROL (2,3-dimercaptopropanol, BAL, dithiol chelator)

A
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3
Q

DIMERCAPROL Pharmacokinetic characteristic

A
  • not stabile in water, dispensed in peanut oil, given always im. !!!
  • good permeability
  • advantage - binds intracellular located cations
  • disadvantage – promotes their infiltration from extracellular compartment into the tissues - excretion by kidney (6-8 hours)
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4
Q

DIMERCAPROL

A
  • not stabile in water, dispensed in peanut oil, given always im. !!!
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5
Q

adv and disadv of dimercaprol

A

good permeability

  • advantage - binds intracellular located cations
  • disadvantage – promotes their infiltration from extracellular compartment into the tissues - excretion by kidney (6-8 hours)
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6
Q

dimercaprol excretion by

A
  • excretion by kidney (6-8 hours)
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7
Q

Therapeutical indication dimercaprol

A
  1. acute arsenic
  2. inorganic mercury,
  3. gold,
  4. bismuth,
  5. antimony
  6. severe lead intoxication (together with NaCaEDTA)
  7. Special indication: encephalopathy induced by inorganic lead or bismuth
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8
Q

Adverse effects- dimercaprol

A
  • nausea,
  • vomiting,
  • hypertension,
  • tachycardia,
  • fever pain,
  • hematoma on the site if injection (thrombocytopenia, increased prothrombin time)
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9
Q

Special Indication of dimercaprol

A

lead or bismuth induced encephalopathy

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10
Q

SUCCIMER (dimercaptosuccinic acid, DMSA)

DMPS (dimercaptopropan-sulfonic acid)

Pharmacokinetic characteristic

A
  • Water soluble forms of dimercaprol
  • oral administration (DMPS also parenterally) -
  • disadvantage moderate intracellular distribution
  • advantage less adverse effect - faster excretion
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11
Q

water soluble forms of dimercaprol

A

SUCCIMER (dimercaptosuccinic acid, DMSA)

DMPS (dimercaptopropan-sulfonic acid)

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12
Q

how is SUCCIMER (dimercaptosuccinic acid, DMSA) administered

A

oral administration only

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13
Q

how is DMPS (dimercaptopropan-sulfonic acid) administered

A
  1. oral administration and
  2. parenterally (DMPS only)
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14
Q

SUCCIMER (dimercaptosuccinic acid, DMSA)

DMPS (dimercaptopropan-sulfonic acid)

adv and disadv

A

disadvantage moderate intracellular distribution

advantage less adverse effect - faster excretion

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15
Q

SUCCIMER (dimercaptosuccinic acid, DMSA) DMPS (dimercaptopropan-sulfonic acid) used for

A

for

  1. acute arsenic and mercury (effective only for some hours after intoxication),
  2. lead poisoning but not in encephalopathy
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16
Q

SUCCIMER (dimercaptosuccinic acid, DMSA) DMPS (dimercaptopropan-sulfonic acid) adverse effects

A

– better tolerated than dimercaprol

  • nausea, vomiting, diarrhea,
  • mild/moderate neutropenia
17
Q

PENICILLAMINE (d-dimethylcysteine) chelator administration

A

water soluble derivative of penicillin, orally administered

18
Q

PENICILLAMINE (d-dimethylcysteine) used for

A

Used for

  1. copper intoxication (Wilson’s disease)
  2. rheumatoid arthritis
19
Q

adverse effects of penicillamine

A
  1. hypersensitive reactions in case of long-term treatment
  2. autoimmune reactions
  3. B6 vitamin depletion
20
Q

EDTA CALCIUM DISODIUM (ethylenediaminetetraacetic acid, EDTA) used for

A

Used for lead poisoning (binds other cations as well)

21
Q

Pharmacokinetic characteristic EDTA calcium disodium

A

- no absorption from the GI

– administration - slow iv. infusion for 5 days

  • distribution only in the extracellular compartment
  • fast excretion by kidney (glomerular filtration)
22
Q

EDTA administration

A

administration - slow iv. infusion for 5 days

23
Q

EDTA distributes only in

A
  • distribution only in the extracellular compartment
  • fast excretion by kidney (glomerular filtration)
24
Q

EDTA Ca disodium excreted by

A

fast excretion by kidney (glomerular filtration)

25
Q

adverse effects of EDTA

A

Adverse effects nephrotoxicity (rarely)

26
Q

DEFEROXAMINE used for

A

Used for

  1. iron poisoning
  2. hemosiderosis,
  3. thalassemia
  4. Aluminum toxicity in kidney failure
27
Q

Pharmacokinetic characteristic - deferoxamine

A
  • no absorption from the GI – administration iv. or im.
  • excretion by kidney and partly by the bile
28
Q

deferoxamine administration

A
  • no absorption from the GI – administration
  1. iv. or
  2. im.
29
Q

Excretion of deferoxamine

A
  • excretion by
  1. kidney and
  2. partly by the bile
30
Q

Adverse effects deferoxamine

A
  1. idiosyncratic reactions
  2. acute respiratory distress syndrome
  3. neurotoxicity

Toxicology Semmelweis (20 decks)

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