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Pharmacology > non - receptor mediated pharmacology (prodrugs and antiparacitic drugs) > Flashcards

non - receptor mediated pharmacology (prodrugs and antiparacitic drugs) Flashcards

1
Q

what is the parasite that causes malaria called?

A

P. Falciparium

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2
Q

how does P.Falciuparium cause malaria?

A

It digests the hosts Hb in the RBCs to give free soluble harm and Ferriprotoporphyrin (FP IX)

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3
Q

what is FPIX?

A

it is excreted by the parasite and converted in the parasites lysosome to non-toxic product hemazoin

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4
Q

what converts FPIX to hemazoin?

A

the enzyme Heme polymerase in the parasites lysosome

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5
Q

where would you find chloroquine?

A

it concentrates in acidic environments such as lysosomes - where it is protonated

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6
Q

what does chloroquine do? Result?

A

inhibits Heme polymerase

  • FPIX builds up (toxic)
  • chloroquine-haem complex forms - toxic free radical
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7
Q

what are the 5 targets for antimalarial drugs?

A

cytosolic compartment, mitochondria, apicoplast, digestive vacuole, membranes

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8
Q

how would antimalarial drugs target the cytosolic compartment? examples.

A

inhibit or antagonise folic acid metabolism - dihydrosulfate reductase inhibitors

  • sulfadoxine, dapsone
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9
Q

how would antimalarial drugs target the mitochondria? examples

A

block electron transport energy production -

hydroxynapthquinolones (pyridines)

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10
Q

how would antimalarial drugs target the apicoplast? examples

A

block the protein synthesis machinery

tetracyclines - doxycycline and azithromycin

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11
Q

how would antimalarial drugs target the digestive vacuole? examples

A

inhibit the detoxification system

  • quinolones (end in quine)
  • aryl amino alcohols (lumefantrine)
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12
Q

how would antimalarial drugs target the membranes

A

inhibition of Ca2+ dependent ATPase

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13
Q

what is chelation therapy?

A

chelating metals, binding them together os they are easily excretable

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14
Q

name 5 WHO essential medicines

A

dimercaprol, dimercaptosuccinic acid, penicillamine, EDTA, deferoximine

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15
Q

what does dimercperol chelate?

A

acute lead, arsenic, mercury poisoning

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16
Q

what does dimercaptosuccinic acid chelate?

A

acute lead, arsenic, mercury poisoning

17
Q

what does penicillamine chelate?

A

wilsons disease - chelation of copper

also a disease modifying anti-rheumatic drug;
non-receptor mediated

18
Q

what does EDTA chelate?

A

acute lead poisoning

19
Q

what does deferoximine chelate?

A

iron poising - dietary supplement

20
Q

what is iron overload called?

A

haemachromatosis

21
Q

what is a prodrug?

A

A compound that undergoes ‘biotransformation’ before exhibiting pharmacological effects

22
Q

who won the nobel prize in 2000 for discovering a use for the prodrug L-DOPA

A

arvid carlsson

parkinsons disease

23
Q

how does L-DOPA help to treat parkinson disease?

A

it crosses the BBB and increases the amount of dopamine in the substantial nigra

24
Q

why is L-DOPA not an effective treatment

A

massiv doses (g) are required because of peripheral DOPA decarboxylase (DDC)

25
Q

what does carbidopa do?

A

inhibits DDC so dopamine isn’t formed from L-DOPA

26
Q

what is prodrug codine metabolised by?

A

CYP2D6

27
Q

mesalazine clinical use

A

rheumatoid atheritis and IBS

28
Q

mesalazine prodrug

A

azoreduction of the drug by gut bacteria to 5-ASD and sulfapyridine

29
Q

sulfasalazine prodrug

A

reduction to sulfapyridine and mesalazine

30
Q

what does CPA stand for

A

cyclophosphamide

31
Q

what are the clinical uses for cyclophosphamide?

A

cancer, autoimmune disease (one of the most potent immunosuppressants)

32
Q

how is the prodrug cyclophosphamide metabolised and bioactivated?

A

CPA is metabolised in the liver by cytochrome P450 to 4-OH-CPA (carbinolamnie) which alkylated guanidine residues in DNA.

33
Q

what do alkylating agents do?

A

Causes intra-strand breaks on O7 and N7 on adjacent guanines

34
Q

what have alkylating agents done as a treatment

A

Revolutionised the treatment of solid tumours of the testes and ovaries

Pharmacology (18 decks)

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