Alkylating Agents Flashcards

1
Q

MoA of Busulfan

A

Cross-links DNA

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2
Q

What is used to ablate patient’s bone marrow before bone marrow transplantation?

A

Busulfan

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3
Q

Use of Busulfan

A

CML

ablating bone marrow before BM transplant

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4
Q

Tox of Busulfan

A

Severe Myelosuppression (in almost all cases)
Pulmonary Fibrosis
Hyperpigmentation

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5
Q

MoA of Cyclophosphamide, Ifosfamide

A

Cross-links DNA

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6
Q

Where do Cyclophosphamide and Ifosfamide cross-link DNA at?

A

cross-links DNA at Guanine N-7

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7
Q

What must happen to Cyclophosphamide and Ifosfamide before they work?

A

bioactivation in the liver

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8
Q

Clinical Use Cyclophosphamide, Ifosfamide

A

solid tumors
leukemias/lymphomas
Vasculitides

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9
Q

Tox of Cyclophosphamide, Ifosfamide

A

Myelosuppression

Hemorrhagic Cystitis

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10
Q

How do you prevent Cyclophosphamide, Ifosfamide Hemorrhagic Cystitis?

A

Mesna

N-Acetylcysteine

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11
Q

How does Mesna work?

A

Mesna prevents Cyclophosphamide induced Hemorrhagic Cystitis by a thiol group binding to toxic metabolites

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12
Q

What are the Nitrosureas? (4)

A

Carmustine
Lomustine
Semustine
Streptozocin

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13
Q

MoA of Nitrosureas

A

cross-link DNA

crosses BBB

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14
Q

What must happen to Nitrosureas before they work?

A

Require Bioactivation

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15
Q

Use of Nitrosureas

A

Brain Tumors

Glioblastoma Multiforme

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16
Q

Tox of Nitrosureas

A

CNS Tox

Convulsions, Dizziness, Ataxia