Drugs Week 1

Question 1

Methotrexate

Answer 1

MOA: Inhibit DHFR and thus decreasing nucleotide synthesis and DNA replication.

CCS: S phase

Side effects: Bone marrow suppression, nausea, vomitting

Question 2

5 Fluorouracil

Answer 2

Inhibit Pyrimidine synthesis of Thiamine blocking DNA synthesis.

CCS: S phase

Side effects: Bone marrow suppression, nausea, vomitting

Question 3

ARA - C

Answer 3

Inhibit pyrimidine synthesizing enzymes.

CCS: S phase

Question 4

Fludarabine

Answer 4

Inhibits purine synthesizing enzymes

CCS: S phase

Question 5

Busulfan

Answer 5

DNA alkylating agent. Damages DNA.

CCNS

Question 6

Cyclophosphamide

Answer 6

DNA alkylating agent. Damages DNA

CCNS

Question 7

Temozolamide (TMZ)

Answer 7

DNA alkylating agent. Damages DNA.

Crosses BBB well. Small, Lipophilic, not effluxed.

Prodrug–> given orally.

First line for Glioblastoma, but extremely expensive with limited gains.

CCNS

Question 8

Carmustine (BCNU)

Answer 8

DNA alkylating agent. Damages DNA.

Some BBB crossing. Large, somewhat lipophilic, and efflux pumps somewhat effected

Can be implanted as a wafer into brain.

CCNS

Question 9

Doxorubicin

Answer 9

DNA intercalting agent. Damages DNA

CCNS

Question 10

Etoposide

Answer 10

Causes strand breaks during replication. Damages DNA

CCS: S phase

Question 11

Paclitaxel

Answer 11

Overstabilizes spindle formation. Interupts mitosis.

CCS: M phase

Question 12

Vincristine

Answer 12

Blocks spindle formation. Interupts mitosis.

Doesn’t cross BBB well. Large, lipophilic, and effluxed.

CCS: M phase.

Question 13

Amphotericin B

Answer 13

Systemic antifungal that binds erg11 and creates holes in membrane.

Must be given IV. Used for systemic fungal infections especially in the immunocompromised. Broad fungal spectrum.

Can cross BBB: Large, Lipophilic, and effluxed.
Side effects: severe nephrotoxicity