Study your flashcards anywhere!

Download the official Cram app for free >

  • Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

How to study your flashcards.

Right/Left arrow keys: Navigate between flashcards.right arrow keyleft arrow key

Up/Down arrow keys: Flip the card between the front and back.down keyup key

H key: Show hint (3rd side).h key

A key: Read text to speech.a key

image

Play button

image

Play button

image

Progress

1/65

Click to flip

65 Cards in this Set

  • Front
  • Back
Pt tx w chemo for Hodgkins develops symptoms of symptoms of schizophrenia - which drug?
–vincristine, nitrogen mustard, prednisone, combination or another drug?
Answer=prednisone
(==>CNS toxicity=psychosis)

NOT THE ANSWER:
-vincristine=neurotoxicity (areflexia, peripheral neuritis) limits useflness
-nitrogen mustards=alkylate DNA (Rx=M2C2: mechlorethamine, melphalan, cyclophosphamide, chlorambucil)
cancer cells lacking HGPRT are resistant to wht Rx?
*6-mercaptoPURINE (6-MP)
*6-thioguanine (6-TP)
[guanine is a PURINE]

(antimetabolites; thus S-phase specific)

*HGPRT (purine salvage pathway) converts these drugs into their active forms, which inhibit purine synthesis
==>inhibit DNA/RNA syn
cyclophosphamide
(cell cycle non-specific <== alkylating agent)

Tx:
-non-Hodgkins lymphoma
-ovarian and breast carcinomas

MOA:
*activated by CYP450 (thus must have working liver)
*alkylating agent
*covalently X-links DNA strand at guanine N-7

S/E:
-myelogenous (granulocytic) leukemia
-acute hemorrhagic cystitis (urinary bladder)==>prevent with mesna

(Alkylating agents):
-moderate BM depression
-large doses==>severe BM depression with:
*leukopenia
*thrombocytopenia
*bleeding


-allopurinol prolongs half-life of cyclophosphamide (MOA is unknwon)
-Thus, when person is taking allopurinol, must reduce cyclophosphamide dose to 25% of nl.
pt tx with chemo with cyclophosphamide. pt also tx with drug for gout. what Rx incr toxicity of cyclophosphamide?
-allopurinol
-Cyclophosphamide is metabolized by xanthine oxidase, which is inhibited by allopurinol.
-Thus, if you take allopurinol
==>less xanthine oxidase
==>can't eliminate cyclophosphamide
==>cyclophosphamide toxicity:
-myelongeous (grnaulocytic) leukemia
-acute hemorrhagic cystitis

*Thus, when person is taking allopurinol, must reduce cyclophosphamide dose to 25% of nl.
pt taking azathioprine and drug for gout. what should you do?
azathioprine is metabolized to 6-mercaptopurine, which is metabolized by xanthine oxidase. Sice allopurinol inhibits xanthine oxidase, can't elim 6-MP.
*Thus, when person is taking allopurinol, must reduce azathioprine dose to 25% of nl.
pt taking 6-mercaptopurine and drug for gout. what should you do?
(drug for gout=allopurinol, which inhibits xanthine oxidase)

azathioprine is metabolized to 6-mercaptopurine, which is metabolized by xanthine oxidase. Since allopurinol inhibits xanthine oxidase, can't elim 6-MP.
*Thus, when person is taking allopurinol, must reduce azathioprine dose to 25% of nl.
allopurinol
Tx: prevent hyperuricemia after tx of hematologic cancers

MOA: inhibits xanthine oxidase to prevent formation of urice acid

S/E:
-inhibits the metabolism of 6-mercaptopurine (6-MP) by xanthine oxidase
==>reduce dose of 6-MP to 25% of normal dose in patients on allopurinol

-need to reduce dose of immunosuppressive drug azathioprine by 25% of normal when given to a patient taking allopurinol because azathioprine is metabolized to 6-MP
paclitaxel
Tx: ovarian and breast CA

*M phase cell cycle specific

MOA: binds microtubules and hyperstabilizes them
==>microtubules cannot be broken down during anaphase
==>mitotic arrest

S/E:
-peripheral neuropathy
-BM dep
Dactinomycin (Actinomycin D)
*cell cycle non-specific (<==antibiotics like dactinoMYCIN, doxorubICIN, bleoMYCIN)

mneum: "ACTinomycin used in kids b/c kids ACT out
==>thus Tx:
*Wilm’s tumor
*rhabdomyosarcoma
*Ewing’s sarcoma

“You must BIND G (Greg) and C (Charles) tightly, or else those kids will act out."


MOA: binds tightly to ds DNA b/w G and C pairs
==>inhibits all DNA-dependent RNA-synthesis, esp mRNA synthesis

S/E:
BM depression
doxorubicin
*cell cycle non-specific (<==antibiotics like dactinoMYCIN, doxorubICIN/daunorubICIN, bleoMYCIN)

=anthracycline AB
(doxoRUBICIN & daunoRUBICIN)

MOA: intercalates into DNA==>
inhibits DNA syn

S/E:
forms free radicals
==>cardiotoxicity ("RUBI": heart is red)
-red urine (not hematuria) [doxoRUBIcin=red)
-BM dep
daunorubicin
cell cycle non-specific (<==antibiotic)

=anthracycline AB
(doxoRUBICIN & daunoRUBICIN)

Tx:
Hodgins
sarcomas

MOA: intercalates into DNA==>
inhibits DNA syn

S/E:
forms free radicals
==>cardiotoxicity ("RUBI": heart is red)
methotrexate
-Tx?
-etc
*S phase specific (antimetabolite)

Tx:
*leukemia
*sarcoma

-forms polyglutamate adduct, which is imp for duration of action

MOA: inhibits DHFR==>can't regen THF
==>inhibits synthesis of thymidylate, purines, and the AA's serine and methionine
==>inh syn of DNA, RNA, & proteins

-Resistance to methotrexate d/t:
-altered DHFR
-incr DHFR
-decr drug transport
-decr polyglutamate formation

S/E:
-BM depression==>use leucovorin for BM rescue
Clinical: A patient tx w methotrexate develops bone marrow depression. How to tx?
leucovorin (=folinic acid) rescues BM. nl cells take up leucovorin (rescuing them), but tumor clels cannot
5-fluorouracil
*S cycle specific (antimetabolite)

Tx: colon cancer

mneum: "put your FU-TS in a dUMP (colon: you take a dUMP out of your colon)

MOA: 5-FU converted to 5-dUMP
==>inhibit thymidylate synthetase
==>no dTMP
==>no thymidine for DNA syn
==>cell death

*no leucovorin rescue!

S/E:
-oral & GI ulceration (mneum: use "flour"ide on your teeth (oral))
pt on chemo has cough w crackles, X-ray shows diffuse basilar infiltrates, drug =?
bleomycin (Bleomycin "blasts" the lung)

G2 specific

MOA: forms free radicals
==>DNA fragmentation (breaks, gaps, "Bleomycin BLASTS DNA into fragments")
==>cells accumulate in G2 and do not proceed to M

S/E:
-pulm fibrosis ("bleomycin blasts the lung")
-little BM toxicity!
Drug w antiestrogenic effects for tx of breast cancer = ?
tamoxifen
carmustine
*cell cycle non-specific (<==alkylating agents)

carMUSTIne & loMUSTIne (nitrosureas)

mneum: "as you sit inside your car while it runs, the CAR's MUSTIness (fumes like CO) cross your BBB
==>kill brain tumors, but gives you CNS toxicity (ataxia, dizziness)

MOA:
*cross-links DNA via alkylation
*requires bioactivation
lomustine
*cell cycle non-specific (<==alkylating agents)

carMUSTIne & loMUSTIne (nitrosureas)

mneum: "as you sit inside your car while it runs, the CAR's MUSTIness (fumes like CO) cross your BBB
==>kill brain tumors, but gives you CNS toxicity (ataxia, dizziness)

MOA:
*cross-links DNA via alkylation
*requires bioactivation
what type of receptors must be present to Tx breast cancer w/leuprolide and goserelin?
must have estrogen receptors in tumor tissue

GnRH analogs (leuprolide & goserelin) given in continuous manner
==>inhibit release of LH/FSH from pit
==>decr LH
==>decr estrogen synthesis by ovaries
==>less stimulation of tumor
cisplatin
*cell cycle non-specific (<==alkylating agents, ~cyclophosphamide)

Tx: testicular and lung CA

MOA (~cyclophosphamde)

hydrolyze Cl groups
==>forms intra- and interstrand cross links at N7 of guanine
==>replacement of Cl with water forms the active drug

S/E:
*nephrotoxicity==>loss of Mg++, Ca++, K++, and phosphate
*decr nephrotoxicity by inducing Cl diuresis (since Cl- stabilizes the drug's platin complex)
*acoustic nerve dysfunction
prednisone:

-which cancers does it Tx?
-MOA?
prednisone

Tx: CLL, Hodgkin's

MOA: apoptosis in non-dividing cells
radiation and alkylating agnets

-how incr tumor cell death
-incr tumor cell death by incr dose antimetabolites

-incr tumor cell death by incr exposure time, not hte dose
what are the alkylating agents?

-what S/E?
A. ALKYLATING AGENTS=
1. Nitrogen mustards; mneum: "C2M2"=
-cyclophosphamide
-CHLORambucil
-meCHLORethamine
-melphalan

2. nitrosureas (carMUSTine, loMUSTine)

3. busulfan

4. cisPLATIN, carboPLATIN


S/E of Alkylating agents:
-moderate BM depression
-large doses==>severe BM depression with:
*leukopenia
*thrombocytopenia==>bleeding
large doses of this Rx causes severe BM depression with:
*leukopenia
*thrombocytopenia
*bleeding
A. ALKYLATING AGENTS=
1. Nitrogen mustards; mneum: "C2M2"=
-cyclophosphamide
-CHLORambucil
-meCHLORethamine
-melphalan

2. nitrosureas (carMUSTine, loMUSTine)

3. busulfan

4. cisPLATIN, carboPLATIN
S/E:
-pulm fibrosis
-hyperpigmentation
-adrenal insufficiency
busulfan (Tx CML)

(adrenal insufficiency
==>decr cort
==>incr ACTH
==>hyperpigmentation)
S/E hemorrhagic cystitis
cyclophosphamide, tx with mesna
S/E:
renal damage
acoustic nerve damage
cisplatin

"ciSPLATin (and carboPLATIN make your kidney & ears go SPLAT"
S/E:
acoustic nerve damage
cisplatin
S/E:
renal damage
cisplatin

S/E:
*acoustic nerve damage

*renal damage
==>incr excretion of Ca, Mg, K, phosphate

~Can decr renal damage from CispLatin via Cl diuresis (Cl stabilizes the drug's platin complex)
S/E procarbazine
CNS depression
S/E:
CNS depression
procarbazine
S/E:
psychosis
glucocorticoids (prednisone)
S/E: oral and GI ulceration
5-fluorouracil (5-FU)

imagine a foot (FU-TS) violently kicking your oral and GI mucosa, creating ulcers
S/E: pulm fibrosis
bleomycin,
busulfan

"bleomycin & busulfan blast the lungs"
S/E: BM depression
A. Hydroxyurea (S phase specific)


B. etoposide (S & G2 phase specific)


C. paclitaxel (taxol) (M phase specific)


D. ALKYLATING AGENTS (cell cycle non-specific)
1. Nitrogen mustards; mneum: "C2M2"=
-CYCLOPHOSPHAMIDE
-CHLORambucil
-meCHLORethamine
-melphalan

2. nitrosureas (carMUSTine, loMUSTine) [~cyclophosphamide)

3. busulfan

4. cisPLATIN, carboPLATIN


E. ANTIBIOTICS (cell cycle non-specific):

-dactinomycin
-doxorubicin/daunorubicin
S/E:
-cardiac toxicity
doxoRUBIcin/daunoRUBIcin (heart is red)
S/E:
-red urine (not hematuria)
doxoRUBICin
S/E of vincristine
areflexia
peripheral neuritis
musc weakness
paralytic ileus
alopecia

("Vincristine is more subtle. She doesn't blast the BM like vinblastine does.")
S/E of vinblastine
-BM depression
-loss of reflexes
-areflexia

(Jeff: "vinBLASTine BLASTS the BM & reflexes (the explosion behind her as she walks to her Porsche)
S/E: incr risk of endometrial cancer
tamoxifen
S/E: menopausal Sx
tamoxifen
S/E of tamoxifen
-incr risk of endometrial cancer
-menopausal Sx
what is the S-phase specific drug that inhibits DNA poly
cytarabin (C-ara)

MOA: C-ara is incorporated as ara-CTP and thus inhibits DNA elongation

*cytarabine (via deoxycytidine kinase)
==>AraCMP
==>AraCTP
G1-phase specific drugs
none

[G1 phase synthesizes compounds needed to synthesize DNA in S phase, which comes right after G1]
S-phase specific drugs
block in S phase
="antimetabolites"
=prevent DNA replic and repair

1. hydroxyurea (inhibit ribonucleotide reductase)
2. 5-FU [fluorouracil] (inhibit thymidylate synthase)
3. 6-MP [mercaptopurine] & 6-TP (inhibit purine synthesis)
4. methotrexate (inhibit DHF-R)
5. cytarabine [Ara-C] (prevents DNA elongation by incorporating AraCTP)
G2-phase specific drugs
block G2= block synthesis of molecules req for mitosis

1. bleomycin
-form free radicals
==>"blasts" DNA into fragments
==>DNA fragmentation


2. eTOPOside:
-stabilizes bond b/w TOPOII and DNA
==>inhibits TopoII
==>DNA breaks remain
==>cannot proceed to mitosis

[TopoI and TopoII unwind the ds DNA to repair it)]
M-phase specific drugs
1. vincristine/vinblastine:

bind tubulin
==>cannot assemble microtubules
==>mitotic filaments cannot form

2. paclitaxel & other taxols:

hyperpolymerizes microtubules
==>microtubules cannot break down during anaphase
==>stops mitosis
cell cycle specific drugs
S phase specific:
1. hydroxyurea
2. 5-FU
3. 6-MP, 6-TP
4. methotrexate
5. cytarabine [Ara-C]

G2 phase-specific:
1. bleomycin
2. etoposide

M phase-specific:
1. vincristine/vinblastine
2. paclitaxel (and other taxols)
cell cycle non-specific
A. ALKYLATING AGENTS=
1. Nitrogen mustards; mneum: "C2M2"=
-cyclophosphamide
-CHLORambucil
-meCHLORethamine
-melphalan

2. nitrosureas (carMUSTine, loMUSTine)

3. busulfan

4. cisPLATIN, carboPLATIN

B. ANTIBIOTICS
-dactinoMYCIN
-plicaMYCIN
-doxoRUBICIN/daunoRUBICIN
(exception: bleoMYCIN=G2 phase specific)

C. glucocorticoids

D. dacarbazine/procarbazine

Cell cycle non-specific Rx:
-can work at any phase of cell cycle, incl Go
-cells are more sensitive in late G1-S phases b/c polynucleotides are more susceptible to alkylation in unpaired state than in helical form
-toxicity usu occurs when cells enter S phase and progression thru cell cycle is blocked
-ex. doxorubicin-intercalates into DNA
==>DNA strand scission (single and double strand breaks) via inhibition of TopoII (cells die in G2)
Tx:
-non-Hodgkins lymphoma
-ovarian and breast carcinomas
cyclophosphamide
Tx: prevent hyperuricemia after tx of hematologic cancers
allopurinol
Tx: Wilm's tumor
Dactinomycin (Actinomycin D)

mneum: "ACTinomycin used in kids b/c kids ACT out. You must BIND G (Greg) and C (Charles) tightly, or else those kids will act out."

*cell cycle non-specific (<==antibiotics like dactinoMYCIN, doxorubICIN, bleoMYCIN)

MOA: binds tightly to ds DNA b/w G and C pairs
==>inhibits all DNA-dependent RNA-synthesis, esp mRNA synthesis

S/E:
BM depression
Tx:
Hodgkins
Doxorubicin/daunorubicin

Tx:
Hodgkins
sarcomas
Tx:
sarcomas
Doxorubicin/daunorubicin

Tx:
Hodgkins
sarcomas
Tx:
*leukemia
Methotrexate

*S phase specific (antimetabolite)

Tx:
*leukemia
*sarcoma

-forms polyglutamate adduct, which is imp for duration of action

MOA: inhibits DHFR==>can't regen THF
==>inhibits synthesis of thymidylate, purines, and the AA's serine and methionine
==>inh syn of DNA, RNA, & proteins

-Resistance to methotrexate d/t:
-altered DHFR
-incr DHFR
-decr drug transport
-decr polyglutamate formation

S/E:
-BM depression==>use leucovorin for BM rescue
Tx: sarcoma
1. Doxorubicin/daunorubicin

Tx:
Hodgkins
sarcomas

Or

2. Methotrexate

*S phase specific (antimetabolite)

Tx:
*leukemia
*sarcoma

-forms polyglutamate adduct, which is imp for duration of action

MOA: inhibits DHFR==>can't regen THF
==>inhibits synthesis of thymidylate, purines, and the AA's serine and methionine
==>inh syn of DNA, RNA, & proteins

-Resistance to methotrexate d/t:
-altered DHFR
-incr DHFR
-decr drug transport
-decr polyglutamate formation

S/E:
-BM depression==>use leucovorin for BM rescue
Tx: colon cancer
5-flourouracil

*S cycle specific (antimetabolite)

Tx: colon cancer

mneum: "put your FU-TS in a dUMP (colon: you take a dUMP out of your colon)

MOA: 5-FU converted to 5-dUMP
==>inhibit thymidylate synthetase
==>no dTMP
==>no thymidine for DNA syn
==>cell death

*no leucovorin rescue!

S/E:
-oral & GI ulceration (mneum: use "flour"ide on your teeth (oral))
Tx: testicular CA
Cisplatin

*cell cycle non-specific (<==alkylating agents, ~cyclophosphamide)

Tx: testicular and lung CA

MOA (~cyclophosphamde)

hydrolyze Cl groups
==>forms intra- and interstrand cross links at N7 of guanine
==>replacement of Cl with water forms the active drug

S/E:
*nephrotoxicity==>loss of Mg++, Ca++, K++, and phosphate
*decr nephrotoxicity by inducing Cl diuresis (since Cl- stabilizes the drug's platin complex)

*acoustic nerve dysfunction:

"ciSPLATin (and carboPLATin) make your kidneys and ears go SPLAT"
Tx: lung CA
Cisplatin

*cell cycle non-specific (<==alkylating agents, ~cyclophosphamide)

Tx: testicular and lung CA

MOA (~cyclophosphamde)

hydrolyze Cl groups
==>forms intra- and interstrand cross links at N7 of guanine
==>replacement of Cl with water forms the active drug

S/E:
*nephrotoxicity==>loss of Mg++, Ca++, K++, and phosphate
*decr nephrotoxicity by inducing Cl diuresis (since Cl- stabilizes the drug's platin complex)
*acoustic nerve dysfunction
Tx: CLL
prednisone (the PREsiDent's SON, George W. Bush, wants to win votes of the rich elderly so he cures elderly people's leukemia (CLL, >60 y/o) & lymphoma (Hodgkin's lymphoma [vs. Non-Hodgkins which AIDS pts get b/c he doesn't want to help them])

Tx: CLL, Hodgkin's

MOA: apoptosis in non-dividing cells
Tx: Hodgkins
Doxorubicin/daunorubicin:
Tx:
Hodgkins
sarcomas


or

Prednisone

Tx: CLL, Hodgkin's

MOA: apoptosis in non-dividing cells
Tx CML
Imatinib (Gleevec):
Philadelphia chromosone brc-abl tyrosine kinase inhibitor

or

busulfan (Tx CML)

(adrenal insufficiency
==>decr cort
==>incr ACTH
==>hyperpigmentation

[mneum: hyperpigmented spots that smell like rotten eggs--sulfur (bulSULFan)]

S/E:
-pulm fibrosis
-hyperpigmentation
-adrenal insufficiency
Tx rhabdomyosarcoma
Dactinomycin (Actinomycin D)

mneum: "ACTinomycin used in kids b/c kids ACT out
==>thus Tx:
*Wilm’s tumor
*rhabdomyosarcoma
*Ewing’s sarcoma

“You must BIND G (Greg) and C (Charles) tightly, or else those kids will act out."

*cell cycle non-specific (<==antibiotics like dactinoMYCIN, doxorubICIN, bleoMYCIN)

MOA: binds tightly to ds DNA b/w G and C pairs
==>inhibits all DNA-dependent RNA-synthesis, esp mRNA synthesis

S/E:
BM depression
Tx Ewing's sarcoma
Dactinomycin (Actinomycin D)

mneum: "ACTinomycin used in kids b/c kids ACT out
==>thus Tx:
*Wilm’s tumor
*rhabdomyosarcoma
*Ewing’s sarcoma

“You must BIND G (Greg) and C (Charles) tightly, or else those kids will act out."

*cell cycle non-specific (<==antibiotics like dactinoMYCIN, doxorubICIN, bleoMYCIN)

MOA: binds tightly to ds DNA b/w G and C pairs
==>inhibits all DNA-dependent RNA-synthesis, esp mRNA synthesis

S/E:
BM depression
what anti-cancer drug must be activated to a ribonucleotide before it's active?
6-mercaptopurine

activated by HGPRTase