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(UNI) Chemotherapy & Selective Toxicity (3rd Year) > Alkylating Agents > Flashcards

Alkylating Agents Flashcards

1
Q

What is the largest class of anticancer drugs?

A

Alkylating agents.

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2
Q

Alkylating agents follow the same general mechanism, explain this mechanism.

A

They all follow the same general mechanism; they are all electrophilic molecules that covalently modify nucleophilic molecules in cells. DNA is the most important adduct (N7 and O6 of Guanine) for anticancer properties.

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3
Q

What are the two types of alkylating agents?

A

Monofunctional and bifunctional.

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4
Q

Describe monofunctional alkylating agents.

A

Alkylating agents that cause single strand DNA breaks.

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5
Q

Describe bifunctional alkylating agents.

A

Alkylating agents that inhibit DNA replication and transcription by cross-linking DNA.

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6
Q

Give the subtypes of alkylating agents.

A
  • Nitrogen mustards.
  • Nitroso-ureas.
  • CIS Platinum Compounds.
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7
Q

Give some examples of nitrogen mustards.

A

Mechlorethamine (Mustargen), Chlorambucil (Leukeran), Cyclophosphamide (Cytoxan).

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8
Q

What is mustargen used to treat?

A

This is used for Hodgkin’s/other lymphomas and chronic leukemias.

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9
Q

Mustargen is used as part of which combination therapy/regimen?

A

The MOPP regimen.

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10
Q

What drugs does the MOPP regimen include?

A

Mechlorethamine, vinvristine (Oncovin), procarbazine, prednisolone.

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11
Q

Which drug is the prototype for the mustards (alkylating agents)?

A

Mustargen.

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12
Q

What percentage response rate is seen in patients treated with mustargen?

A

80%.

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13
Q

What percentage cure rate is seen in patients treated with mustargen?

A

50%.

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14
Q

What are the toxic effects of mustargen?

A

Its toxicity profile includes nausea and vomiting. The effects of dose limiting toxicity (DLT) are bone marrow suppression affecting white blood cells (esp. granulocytes).

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15
Q

When is the max bone marrow suppression seen with mustargen seen clinically? When is recovery seen?

A

10-12 days. Around 42 days.

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16
Q

What is the half life of mustargen?

A

Less than 30 minutes.

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17
Q

How is mustargen administered?

A

In a free-flowing catheter.

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18
Q

What are some analogues of mustargen?

A
  • Chlorambucil (Leukeran).

* Melphalan (Alkeran) – Used in myeloma (longer half-life, PO).

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19
Q

What is chlorambucil used for?

A

This drug is used for the treatment of chronic lymphocytic leukaemia and malignant lymphomas.

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20
Q

What is the main side effect of chlorambucil?

A

It can lead to cumulative bone marrow toxicity.

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21
Q

What type of electrophilic reaction do the mustards undergo?

A

SN2.

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22
Q

What is cyclophosphamide used to treat?

A

Cyclophosphamide is a prodrug used for the treatment of malignant lymphomas and various carcinomas.

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23
Q

Which single drug is the most widely used alkylating agent?

A

Cyclophosphamide.

24
Q

Which drugs are included in the CMF anticancer regimen?

A

Cyclophosphamide, methotrexate, flurouricil.

25
Q

How does the CMF regimen increase 7 year survival rates?

A

31% to 49%.

26
Q

Cyclophosphamide has a better toxocity profile than mustargen, what specifically is seen in this regard?

A

Better bone marrow recovery seen.

27
Q

How long does cyclophosphamide treatment last at a time?

A

10-12 days.

28
Q

How long after treatment with cyclophosphamide is taken for recovery?

A

21 days.

29
Q

How is cyclophoisphamide administered?

A

Parenterally.

30
Q

Cells resistant to cyclophosphamide may contain which chemical compound?

A

Aldehyde oxidase.

31
Q

Give some examples of nitrosoureas.

A
  • Bis-chloro-nitrosourea (Carmustine, BCNU).

* Chloroethylcyclohexylnitrosourea (Lomustine, CCNU).

32
Q

What are BCNU and CCNU used to treat?

A

BCNU and CCNU are both used for brain tumours, Hodgkin’s disease, and melanoma.

33
Q

What properties of BCNU and CCNU make them viable for the treatment of brain tumours?

A

They are lipid soluble which makes them CNS active and a possible drug for treating brain tumours as they can pass the BBB.

34
Q

What is the mode of action for the nitrosoureas such as BCNU and CCNU?

A

There method of action includes the alkylation of the O6 of Guanine (comparatively, the alkylation by mustards is the N7 of guanine).

35
Q

Why should care be taken when treating women with nitrosoureas?

A

Care should be taken with pregnant women or women planning on becoming pregnant as these drugs are teratogenic.

36
Q

What type of electrophilic reaction do the nitrosoureas undergo?

A

SN1.

37
Q

BCNU is used in the treatment of glioblastome. With surgery and radiation treatment, how long can this increase lifespan?

A

20 weeks to 50 weeks.

38
Q

BCNU has a high toxicity, therefor how long should treatment last?

A

A max length of 28 days.

39
Q

How long does recovery from the toxic effects of BCNU take?

A

42 days?

40
Q

How is BCNU administered?

A

By injection.

41
Q

What is the common name for BCNU?

A

Carmustin.

42
Q

Why may haematological toxicity persist with the use of BCNU?

A

BCNU is very lipophilic and has low ionisation at physiological pH, this gives a risk of haematological toxicity persisting due to storage in the liver.

43
Q

How is CCNU given?

A

Orally.

44
Q

What is a new non-nitrosourea which is used frequently in the treatment of glioblastoma?

A

Temozolomide (Temodar).

45
Q

What is glioblastoma?

A

Glioblastoma, also known as glioblastoma multiforme (GBM), is the most aggressive cancer that begins within the brain. Initially, signs and symptoms of glioblastoma are non-specific. They may include headaches, personality changes, nausea, and symptoms similar to those of a stroke.

46
Q

At what dose is temozolomide administered?

A

200mg/m^2 daily for 5 days.

47
Q

What is the active metabolite of temozolomide?

A

MTIC.

48
Q

What is the lead structure for the cis-platinum compounds?

A

Cisplatin.

49
Q

In what type of therapy is cisplatin most commonly used?

A

Combination therapy.

50
Q

In combination therapy, which cis-platinum compound is the first line treatment for colon cancer?

A

Cisplatin.

51
Q

What is the common name for cisplatin?

A

Platinol.

52
Q

What is the percentage cure rate for cisplatin when used in testicular cancer?

A

85%.

53
Q

What is the toxicity profile of cisplatin?

A

Its toxicity profile shows nephrotoxicity and hearing loss at the high end of doses.

54
Q

Give some analogues of cisplatin.

A
  • Carboplatin (Parbaplatin).

* Oxaliplatin (Eloxatin).

55
Q

Where do nitrosoureas alkylate cytosine?

A

3’N.

(UNI) Chemotherapy & Selective Toxicity (3rd Year) (18 decks)

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