Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm Drug Table > Drug Table - Antimetabolites > Flashcards

Drug Table - Antimetabolites Flashcards

1
Q

Antimetabolites in general

A

Structural analogs of folic acid or of the
purine/pyramidine bases found in DNA; act
in S-phase (cell cycle specific)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Antimetabolites list

A 
Methotrexate (Trexall)
Pemetrexed (Alimta)
5-Fluorouracil (5-FU, Carac)
Cytarabine (AraC, Depocyt)
Gemcitabine (dFdC, Gemzar)
6-Mercaptopurine (Purinethol)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Methotrexate (Trexall) class

A

Folate analogs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Methotrexate (Trexall) mech

A 
Inhibits dihydrofolate reductase (DHFR),
which converts dietary folate to
tetrahydrofolate (THF) needed for thymidine
and purine synthesis; given orally or
intrathecally
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Methotrexate (Trexall) Therapeutics

A 
Childhood ALL and choriocarcinoma;
combination therapy for Burkitt's
lymphoma and carcinomas of breast,
ovary, head and neck, and bladder;
administered intrathecally for
meningeal leukemia and meningeal
metastases of tumors (can't cross
BBB); high-dose for osteosarcoma
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Methotrexate (Trexall) Imp Side effects

A 
Renal toxicity (crystallization in
urine at high doses), hepatotoxicity
(long-term, fibrosis/cirrhosis),
reproductive (defective oogenesis
or spermatogenesis, abortion)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Methotrexate (Trexall) Other side effects

A 
Bone marrow
(myelosuppression,
spontaneous hemorrhage); GI
toxicity (oral ulceration,
stomatitis)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Methotrexate (Trexall) Misc

A

Can use leucovorin to prevent toxic
effects of MTX, as healthy cells can
take it up a lot better than tumor cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Pemetrexed (Alimta) class

A

Folate analogs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Pemetrexed (Alimta) Mech

A 
Polyglutamate forms that inhibit THFdependent
enzymes (e.g., DHFR, TS);
metabolized to polyglutamate forms that
inhibit THF-dependent enzymes (e.g.,
DHFR, thymidylate synthase (TS))
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Pemetrexed (Alimta) Therapeutics

A

Colon cancer, mesothelioma, non-small

cell lung cancer, pancreatic cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

5-Fluorouracil (5-FU, Carac) class

A

Pyramidine analogs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

5-Fluorouracil (5-FU, Carac) Mech

A

5-FU is converted to active metabolites: 5-
FdUMP inhibits TS; 5-FdUTP incorporates
into RNA & interferes with RNA function;
prodrug [capesitabine] ribosylated and phophosrylated into
5-FdUMP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

5-Fluorouracil (5-FU, Carac) Therapeutics

A

Combination therapy for breast,
colorectal, gastric, head and neck,
cervical and pancreatic cancer;
topically for basal cell carcinoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

5-Fluorouracil (5-FU, Carac) Imp Side Effects

A

Hand-foot syndrome (erythema,
sensitivity of palms and soles),
cardiac toxicity (acute chest pains)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

5-Fluorouracil (5-FU, Carac) Other side effects

A

Anorexia and nausea; mucosal
ulcerations, stomatitis, diarrhea;
thrombocytopenia and anemia

17
Q

5-Fluorouracil (5-FU, Carac) Misc

A

Leucovorin can potentiate effects of
5-FU; must be given IV (GI toxicity
and rapid degradation + metabolism
in gut and liver)

18
Q

Cytarabine (AraC, Depocyt) Class

A

Pyramidine

analogs

19
Q

Cytarabine (AraC, Depocyt) Mech

A

Ara-C converted by deoxycytidine kinase to
Ara-CMP –> Ara-CTP; terminates DNA
synthesis as Ara-CTP

20
Q

Cytarabine (AraC, Depocyt) Therapeutics

A

AML (most effective treatment), ALL

and blast phase CML

21
Q

Cytarabine (AraC, Depocyt) Other side effects

A

Severe myelosuppression
(leucopenia, thrombocytopenia,
anemia), GI tract toxicity
(ulceration, stomatitis, diarrhea)

22
Q

Gemcitabine (dFdC, Gemzar) class

A

Pyramidine

analogs

23
Q

Gemcitabine (dFdC, Gemzar) Mech

A

Converted to active metabolites: dFdCDP
inhibits ribonucleotide reductase (lowers
deoxyribonucleotide); dFdCTP incorporates
into DNA, terminating DNA synthesis

24
Q

Gemcitabine (dFdC, Gemzar) Therapeutics

A

Pancreatic cancer; effective against
non-small cell lung cancer, ovarian,
bladder, esophageal, and head and
neck cancer

25
Q

Gemcitabine (dFdC, Gemzar) Other side effects

A

Myelosuppression (leucopenia,

thrombocytopenia, anemia), flulike

26
Q

Gemcitabine (dFdC, Gemzar) Misc

A

More effective against solid tumors

than cytarabine

27
Q

6-Mercaptopurine (Purinethol) Class

A

Purine analogs

antimetabolites

28
Q

6-Mercaptopurine (Purinethol) Mech

A

Prodrug metabolized by hypoxanthineguanine
phosphoribosyl transferase
(HGPRT) to 6-thioinosinic acid (TIMP);
TIMP inhibits first step of de novo purine
base synthesis and the formation of AMP
and xanthinylic acid from inosinic acid,
reducing purine levels. As well, TIMP is
converted to thio-guanine ribonucleotides,
inhibiting DNA and RNA synthesis

29
Q

6-Mercaptopurine (Purinethol) Therapeutics

A

Maintain remission in acute ALL

30
Q

6-Mercaptopurine (Purinethol) Imp side effects

A

Hepatotoxicity in prolonged use

31
Q

6-Mercaptopurine (Purinethol) Other side effects

A

Bone marrow suppression

32
Q

6-Mercaptopurine (Purinethol) Misc

A 
Drug interaction with allopurinol (for
gout), which inhibits xanthine
oxidase; decrease 6-MP dose to
avoid drug accumulation and
toxicities

Pharm Drug Table (11 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions