chemotherapy Flashcards

1
Q

what are the 4 main therapeutic agents used in chemotherapy?

A

alkylating agents
antimetabolites
cytotoxic antibodies
plant derivatives

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2
Q

what do alkylating agents do to cause conformational changes in DNA?

A

they form covalent bonds with nucleophilic substances in the cell and cross link DNA which prevents DNA polymerase accessing to replicate the DNA

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3
Q

how exactly is the DNA changed by alkylating agents?

A

modifies guanine so it mispairs with Thymine which causes the cell to undergo apoptosis

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4
Q

what type of alkylating agent is cyclophosphamide?

A

a nitrogen mustard

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5
Q

what enzyme in the liver activates cyclophosphamide?

A

p450 enzymes

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6
Q

what is the cytotoxic product of nitrogen mustards?

A

phosphor amide mustartd

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7
Q

what is the toxic by-product of the activation of nitrogen mustards which is counteracted by mesna?

A

acrolein

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8
Q

which alkylating agent is used in chronic granulocyte leukaemia to prevent formation of granulocytes and platelets in low dosage and RBCs in high dosage?

A

Busulphan (an alkylsulphonate)

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9
Q

which type of alkylating agent is used to treat brain tumours because of its lipid soluble properties which allow it to cross the blood-brain barrier?

A

nitrosoureas (eg lomustine and carmustine)

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10
Q

what class of alkylating agent is a water soluble complex?

A

platinum based compounds (e.g. cisplatin)

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11
Q

what are the three classes of antimetabolite chemotherapy drugs?

A

antifolates
antipyrimidines
antipurines

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12
Q

what is an example of the drug which is a competitive inhibitor of the folate pathway and is giving orally usually?

A

methotrexate

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13
Q

what are two examples of antipyrimides which mimic the structure of pyrimidines and inhibit DNA polymerase?

A

Fluorouracil (5-FU) gemcitabine (and its analogue cytarabine)

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14
Q

what are some examples of antipurines which act as fraudulent nucleotides and inhibit DNA polymerase?

A

mercaptopurine, thioguanin, fludarabine

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15
Q

what are the four different cytotoxic antibiotic classes?

A

anthracyclines
dactinomycin
bleomycin
mitomycin

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16
Q

what is the mechanism of action of anthracyclines?

A

bind to DNA and prevents DNA and RNA synthesis by stabilising the DNA - topoisomerase II complex

17
Q

what is the most common example of an anthracycline drug?

A

doxorubicin

18
Q

what is the mechanism of action of dactinomycin drugs?

A

binds in the minor groove of DNA and prevents the movement of RNA polymerase and therefore prevents transcription

19
Q

what is the mechanism of action of belomycins?

A

these are a group of metal-chelating gycopeptide antibiotics that degrade preformed DNA, causing chain fragmentation and release of free bases (most effective at G2 stage but also active against non-dividing cells)

20
Q

what is the mechanism of action of Mitomycin?

A

functions as a bifunctional alkylating agent, alkylating preferentially at O6 of guanine - cross links DNA and may also degrade DNA through generation of free radicals

21
Q

what is the main mechanism of action of plant derivative chemotherapy drugs?

A

they are spindle poisons which affect microtubule function and prevent mitotic spindle formation

22
Q

what are the four different classes of plant derivative chemotherapy drugs?

A

vinca alkaloids
taxanes
camptothecins
etoposide

23
Q

what is the mechanism of action of vinca alkaloids?

A

bind tubular and prevent polymerisation into microtubules

24
Q

what are some examples of vinca alkaloids?

A

vincristine and vinblastine

25
Q

what is the mechanism of action of taxanes?

A

stabilise microtubules

26
Q

what are some examples of taxanes?

A

paclitaxel (taxol)

docetaxel

27
Q

what is the mechanism of action of camptothecins?

A

bind to and inhibit topoisomerase 1

28
Q

what is an example of a camptothecin?

A

irinotecan

29
Q

what is the mechanism of action of etoposide?

A

inhibits mitochondrial function, nucleoside transport and topoisomerase II