Pharmacology 6-8 Anticancer Agents

Question 1

Antimetabolites. Antimetabolites are ___ and ___ analogs and inhibit DNA synthesis. These are ___ cell cycle specific.

Answer 1

Antimetabolites are PURINE and PYRIMIDINE analogs and inhibit DNA synthesis. These are HIGHLY cell cycle specific.

Question 2

Antimetabolites. Methotrexate is a ___ acid analog and inhibits DHFR. As a result, the metabolically active form of folate, ___, is not generated and conversion of dUMP to dTMP cannot occur.

Answer 2

Methotrexate is a FOLIC acid analog and inhibits DHFR. As a result, the metabolically active form of folate, MTHF, is not generated and conversion of dUMP to dTMP cannot occur.

Question 3

Antimetabolites. 5-Flurouracil inhibits thymidylate synthase and prevents the conversion of ___ to ___.

Answer 3

5-Flurouracil inhibits thymidylate synthase and prevents the conversion of dUMP to dTMP.

Question 4

Antimetabolites. Hydroxyurea inhibits ribonucleotide reductase and inhibits conversion of ___ to ___.

Answer 4

Hydroxyurea inhibits ribonucleotide reductase and inhibits the conversion of dUMP to dTMP.

Question 5

Taxanes. Taxane drugs bind to microtubules and inhibit their ___ into tubulin. This prevents the cell from completing mitosis.

Answer 5

Taxane drugs bind to microtubules and inhibit their DEPOLYMERIZATION into tubulin. This prevents the cell from completing mitosis and dividing into two daughter cells.

Question 6

Taxanes. PaclitaXel and Docetaxel are taxane medications. These are given ___ and may irritate ___ and ___ membranes.

Answer 6

Paclitazel and Docetaxel are taxane medications. These are given IV and may irate SKIN and MUCOUS membranes.

Question 7

Taxanes. ___ is used to treat breast cancer and hormone refractory prostate cancer.

Answer 7

DOXETAXEL is used to treat breast cancer and hormone refractory prostate cancer.

Question 8

Taxanes. ___ is associated with neurotoxicity. ___ is associated with fluid retention.

Answer 8

PACILTAXEL is associated with neurotoxicity. DOCETAXEL is associated with fluid retention.

Question 9

Vinca Alkaloids. These medications include vinblastine and vincristine. Bind to ___ and prevent cells from making the ___ spindles.

Answer 9

Binds to TUBULIN and prevents cells from making the MITOTIC spindle.

Question 10

Vinca Alkaloids. Vinblastine and Vincristine are given ___. If administered intrathecally, ___ occurs.

Answer 10

Vinblastine and Vincristine are given IV. If administered intrathecally, DEATH occurs.

Question 11

Vinca Alkaloids. ___ is associated with neurotoxicity. ___ is associated with bone marrow suppression.

Answer 11

VINCRISTINE is associated with neurotoxicity. VINBLASTINE is associated with bone marrow suppression.

Question 12

Podophyllotoxin. Etoposide and teniposide are glucosides. These are used as ___ solutions as treatment for genital warts.

Answer 12

These are used as TOPICAL solutions as treatment for genital warts.

Question 13

Podophyllotoxin. Etoposide blocks the ___ and ___ phase of the cell cycle. Used primarily for __ cancer that hasn’t responded to other treatment plans. ___ is a common side affect.

Answer 13

Etoposide blocks the G1 and S2 phase of the cell cycle. Used primarily for TESTICULAR cancer that hasn’t responded to other treatment plans. HYPOTENSION is a common side effect.

Question 14

Antitumor antibiotics. These are derived from ___ species and cause ___ necrosis.

Answer 14

These are derived from STREPTOMYCES species and cause TISSUE necrosis.

Question 15

Antitumor antibiotics. Bleomycine is dosed based upon ____ area and ___ fibrosis is a side effect.

Answer 15

Bleomycine is dosed based upon SURFACE area and PULMONARY fibrosis is a side effect.

Question 16

Alkylating agents. These medications are developed and ___ gas and attach a alkyl group to the number seven nitrogen atom of the ___ ring.

Answer 16

These medications are developed from MUSTARD base and attach an alkyl group to the number seven nitrogen atom of the PURINE ring.

Question 17

Alkylating agents. Form ___ bonds to DNA. Specifically, the __ residue is attacked.

Answer 17

Form COVALENT bonds to DNA. Specifically, the GUANINE residue is attacked.

Question 18

Alkylating agents. Cyclophosphamide is metabolized by the ___ system into aldophoshamide.

Answer 18

Cyclophosphamide is metabolized by the P-450 system system into aldophoshamide.

Question 19

Alkylating agents. ___ juice is an CYP3A4 inhibitor and ___ the activation of cyclophosphamide.

Answer 19

GRAPEFRUIT juice is an CYP3A4 inhibitor and DECREASES the activation of cyclophosphamide.

Question 20

Anthracyclines inhibit ___ which generates ___ causing membrane damage and breaks within the DNA. Doxorubin is an example of an anthracycline.

Answer 20

Anthracycline inhibit DNA TOPOISOMERASE which generates FREE RADICALS causing membrane damage and breaks within the DNA. Doxorubin is an example of an anthracycline.

Question 21

Cisplatin enters the cell by passive diffusion and the ___ residue reacts with the N7 guanine causing ___ strands of cellular DNA. A side effect includes ___.

Answer 21

Cisplatin enters the cell by passive diffusion and the CHLORIDE residue reacts with the N7 guanine causing CROSS LINKING strands of cellular DNA. A side effect includes NEPHROTOXICITY.