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Pathology (YCs): ID > cancer drugs > Flashcards

cancer drugs Flashcards

0
Q

What are the nitrogen mustards?

A

Nitrogen mustards:

  1. Mechloroethamine
  2. Cyclophosamide
  3. Ifofsamide
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1
Q

how do alkylating agents work and what are they?

A

akylating agents work by acetylating DNA (irreversible, covalent bond) and thus XL them and cause DNA damage. acts on both dividing and nondividing cells (cell cycle nonspecific)

  1. Nitrogen mustards
  2. Nitrosurea
  3. Triazenes
  4. Platinum analogs

TOX: BM TOX (NEUTROPENIA, THROMBOCYTOPENIA, ANEMIA)
mucosal tox, reproductive sys (male-sterility, females - amenorrhea), INC LEUKEMIA RISK, N+V

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2
Q

alkylating agent;;;nitrogen mustard:

mechloroethamine

A

TX: in combo with MOPP (Hodg), also used to tx cutaneous T-cell lymphoma

TOX: N+V, immunosupp (leucopenia, thrombocytopenia)

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3
Q

alkylating agent;;;nitrogen mustard

cyclophosamide and ifosfamide

A

TX: used in comb: CHOP (non-Hodg), CMF (BC), FAC (BC), FEC (BC): nonhodg, BC, ovarian, Lung, acute and chronic lymphocytic leukemia

-ifosfamide is converted in the P450 to active akylating agent, it is also used for sarcoma and testicular cancer
TOX: N+V, myelosuppression, HEMORRHAGIC CYSTITIS (b/c accumulation of acrolein (can be overcome by hydrating with MESNA)

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4
Q

alkylating agent;;;nitrosurea, list

A
  1. carmustine

2. lomustine

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5
Q

alkylating agent;;;nitrosurea

A

carmustine and lomustine
-both lipophilic
TX: brain tumors

TOX: renal tox, pul fibrosis, profound myelosuppression, severe N+V

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6
Q

alkylating agent;;;triazenes, list

A
  1. dacarbazine

2. temozolomide

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7
Q

alkylating agent;;;triazenes

A

Dacarbazine: IV, ABVD combo (Hodg, malig melanoma)
-prodrug, monoalkylators

Temozolomide: oral (good bioavailability), undergoes nonenzymatic conversion to methylhydrazine at physiological pH
-TX: malig gliomas, std tx in combo with radiation therapy

TOX: N+V, myelosuppression, FLU-LIKE SX (fever, fatigue)

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8
Q

alkylating agents;;;;platinum analogs

A
  1. cisplatin
  2. carboplatin
  3. oxaliplatin
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9
Q

platinum analogs

how they work

A
  • inorganic platinum derivatives
  • interacts with H20 to form the active cytotoxic form (+ charged, hydrated intermediate) –> covalently bind Gs in DNA –> intra and interstrand XLs
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10
Q

platinum analogs (what each of them tx)

A
  1. cisplatin - testicular, ovarian, cervical, bladder, HN, lung
    TOX: renal, ototox, severe N+V, peripheral motor and sensory neuropathy at high doses, mild/mod myelosuppression
  2. carboplatin: ovarian
    TOX: mild/mod myelosuppression
  3. oxaliplatin: gastric and colorectal (in combo with 5FU)
    TOX: COLD-INDUCED PERIPHERAL NEUROPATHY, (NEUROPENIA?)
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11
Q

how do metabolites work and what are they?

A
  • structural analogs of folic acid/purine/pyr bases, therefore inhibits enzymes required for puring/pyr nucleotide syn or compete with them for DNA/RNA syn
  • inhibits S phase (Cell cycle specific drugs / DNA syn inhibitors)
  1. folate analogs
  2. pyrimidine analogs
  3. purine analogs
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12
Q

antimetabolite;;;folate analogs and what they do

A
  1. methotrexate = antifolate = folic acid antagonist
    - blocks DHFR (DHFR normally converts dietary folate to tetrahydrofolate required for thymidine and purine biosynthesis)
    - use leucovorine rescue (N5-formyl-THF) to bypass the toxicity on other cells (normal cells have more carriers for leucovorine –> dec side effects)

TX: childhood acute lymphoblastic leukemia (ALL), choriocarcinoma (malig trophoblastic tumor)

  • {in combo therapy: burkitt’s lymphoma, breast, ovary, H+N, bladder carcinoma}
  • cannot penetrate CNS, therefore intrathecal administration for meningeal dz.
  • high concentrations tx osteosarcoma

TOX: BM (myelosuppression, spontaneous hemorrhage), GI tox (oral ulcers, stomatitis), renal (MTX crystalizes in urine and cause damage), liver (long term –> fibrosis/cirrhosis), defective oogenesis/spermatogenesis (abortions)

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13
Q

antimetabolite ;;; folate analogs

A

pemetrexed - considered a 2nd line therapy
-active form is polyglutamate form that inhibits THF-dependent enzymes (TS, DHFR)

TX: colon, pancreatic, mesothelioma, non SCLC, multitargeted folate analogs

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14
Q

antimetabolites ;;; pyrimidine analogs

A
  1. 5-FU
  2. capecitabine
  3. cytarabine (Ara-C)
  4. Gemcitabine
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15
Q

5FU

A

5-FU (pyr analog): a prodrug that req enzymatic conversion to become active: 5FdUMP (inhibits TS, prevents thymidine syn), 5FdUTP (incorp into RNA)

TX: IV bc GI tox, and rapid metabolic degradation in gut and liver
combos: breast, colorectal, gastric, HN, cervical, pancreatic
topical: TX BCC
TOX: HAND-FOOT SD, cardiac tox

16
Q

antimetabolite;;;pyrimidine analogs; capecitabine

A

capecitabine: new oral form, prodrug -> converted to 5’d-FdU

TX: met BC and colorectal cancer
TOX: HAND-FOOT Sd (sensitivity to palms and soles), CARDIAC TOX (ACUTE CP), anemia, thrombocytopenia, anorexia, N, mucosal ulcerations, stomatitis, diarrhea

17
Q

antimetabolite;;;pyrimidine analogs; cytarabine (ara-C)

A

Cytarabine (ara-C): S-phase specific pyrimidine antagonist
analog of 2-deoxycytidine but ribose is replaced by D-arabinose

1=deoxycytidine kinase
ara-C -1->ara-CMP –> ara-CTP (competes with dCTP for incorp into DNA by DNA poly –> premature DNA chain termination

MOST EFFECTIVE for acute myeloid leukemia (AML), useful for ALL, blast phase CML

TOX: severe myelosupp, GI tox

18
Q

antimetabolite;;;pyrimidine analogs; gemcitabine

A

gemcitabine: difluoro analog of deoxycytidine (dFdC)

gemcitabine -p–> dFdCMP –> dFdCDP –| ribonucleotide reductase (therefore deplete deoxyribonucleotide pool for DNA syn)
gemcitabine –p–>dFdCMP–>dFdCTP —> gets into DNA therefore terminates DNA syn

similar to cytarabine in that it also inhib dna syn
diff from cytarabine in that it is active throughout the whole cycle
MORE effective than cytarabine against solid tumors

TX: 1st line tx for pancreatic carcinoma, effective against nonSCLC, ovarian, bladder, esophageal, HN cancers

TOX: myelosupp, FLU-LIKE Sd

19
Q

what are the purine analogs

A
  1. 6-mecaptopurine
    - prodrug, metabolized by hypoxanthine-guanine phosphoribosyl transferase (HGPRT)

6MP —HGPRT–> 6TIMP
6MP –XO–> 6thiouric acid (allopurinol inhib XO)
6TIMP:
1. inhib the feedback inhib of p-ribosylamine syn (generated from PRPP (precursor to IMP)
2. inhib IMP (IMP makes AMP and XMP (GMP))
3. thio-GMP–>RNA (inhib DNA/RNA syn)

20
Q

what is 6mp used for and the tox, and mechanism of resistance

A

TX:

  • maintain remission in pts with ALL (acute lymphoblastic leukemia)
  • allopurinol + 6MP dec hyperuricemia in pts getting chemo. but since allopurinol inhib XO, 6MP builds up, therefore give lower dose of 6MP to avoid toxicities

TOX: BM supp, livetox with prolonged use
mechanism of resistance: dec HGPRT, dec drug tranport

21
Q

how do dna intercalating agents work?

A

aka antitumor ab’s from soil microbe streptomyces

-binds DNA: inhib DNA/RNA/both syn, cause DNA strand breaks, interfere w/ cell replication

22
Q

what are the DNA intercalating agents?

A
  1. Dactinomycin (aka Actinomycin D)
  2. Anthracyclines
  3. Bleomycin
23
Q

DNA intercalating agent ;;; actinomycinD

A

actinomycin D:
intercalates btwn GCs in DNA –> interferes w/ RNA poly –> cannot transx, cause single strand breaks

TX: pediatric tumors: Wilm’s tumor, rhabdomyosarcoma, Erwing’s sarcoma, advanced choriosarcoma in women

TOX: N+V, anorexia, hematopoietic supp with PANCYTOPENIA (WBC, RBC, platelets)

24
Q

what are the anthracyclines?

A
  1. daunorubicin
  2. doxyrubicin
  3. idarubicin
  4. epirubicin

they are all ANTIBIOTICS from streptomyces
ALL intercalate btwn DNA bps via HYDROXYL RADICALS

TOX: myelosupp, neutropenia, irrev dose-dep CARDIOTOXICITY (cardiomyopathy), stomatitis, GI disturbances, alopecia

25
Q

daunorubicin and idarubicin

A

AML

idarubicin also used in combo with Ara-C for CML

26
Q

doxorubicin

A

broad spectrum of use: sarcomas, breast and lung carcinomas, malignant lymphomas

27
Q

epirubicin

A

met BC and gastric cancer

28
Q

Bleomycin

A
  • mix of 2 copper chelating peptides from streptomyces
  • binds DNA and induces 1/ds DNA breaks after its oxidized and forms free radical

TX: testicular cancer (usually in combo with vinblastine / etoposide), SCC, lymphomas

TOX: min myelosupp and immunosupp
PUL TOX (PUL FIBROSIS)
CUTANEOUS TOX (hyperpig, hyperkeratosis, erythema)
hyperthermia, headache, N+V

29
Q

how do microtubule inhibitors work? and what are two of them?

A

microtubules are formed from tubulins poly/depoly

vinca alkaloids and taxanes –| mitosis by causing M arrest by interfering with microtubule function

30
Q

what are the vinca alkaloids? (they are natural plant alkaloids), how do resistance happen?

A

blocks tubulin POLYMERIZATION

  1. vinblastine: (w. bleomycin, cisplatin)
    TX: met testicular tumors
    part of ABVD for Hodg
    TOX: myelosupp, N+V
  2. vincristine: (w. glucocorticoids) –> childhood ALL
    TX: hodg, nonhodg
    TOX: dose limiting neurotoxicity (rel low tox in BM)

RESISTANCE:
via P-glycoprotein channels that pump the drug out

31
Q

what are the taxanes? (also plant alkaloids)

A
  1. paclitaxel (taxol)

2. docetaxel (taxotere) (more potent), yew trees

32
Q

what do the taxanes, paclitaxel and docetaxel, do?

A

prevent microtubule depoly (neccessary for chromo desegregation during mitosis), M phase arrest

TX: Met BC, ovarian, lung, HN tumors
docetaxel: hormone-refractory prostate cancer

TOX: neutropenia, peripheral neuropathy, hypersensitivity rxns

33
Q

what are the topoisomerase inhibitors? and want do they do in general?

A

topoisomerases (1-ssDNA, 2-dsDNA) breaks and reseals DNA during replication to relieve torsional stress.
-the drugs inhib the topo by preventing DNA resealing

  1. epipodophyllotoxins
  2. camptothecin analogs (natural from chinese plant)
34
Q

what are the epipodophyllotoxins?

A
  1. etoposide and teniposide
    both are podophyllotoxin derivative; semisynthetic
    both inhib topo2 –> DNA damage by stablizing the breaks induced by topo

etoposide: broad activity: testicular carcinoma, lung cancer, nonhodg
teniposide: ALL (Acute lymphoblastic leukemia)

TOX: dose-limiting myelosupp (neutropenia)
ORAL MUCOSITIS

35
Q

what are the camptothecin analogs and what do they do?

A

irinotecan and topotecan: synthetic camptothecin analogs (inc activity, dec tox)
both inhib topo 1 –> accumulation of DNA breaks

irinotecan: adv colorectal cancer, good for lung, ovarian, cervical, brain
topotecan: ovarian and SCLC

TOX: SEVERE neutropenia, SEVERE diarrhea

Pathology (YCs): ID (25 decks)

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