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Pharm II Test 4 > Chemo II Alkylating Agents > Flashcards

Chemo II Alkylating Agents Flashcards

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1
Q

Bifunctional Alkylating Agents- Bischloroethylamines- Available Drugs

A 
CYCLOPHOSPHAMIDE
Nitrogen Mustard
Chlorambucil
Melphalan
IFOSFAMIDE
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2
Q

Bifunctional Alkylating Agents- Bischloroethylamines- Mech of Action

A

must be activated by P-450- activated form is phosphoramide mustard

PHOSPHORAMIDE AMUSTARD BIFUNCTIONALLY ALKYLATED THE N7 POSITION OF GUANINE AND FORMS INTERSTRAND AND INTRASTRAND CROSSLINKS

Target= DNA

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3
Q

Bifunctional Alkylating Agents- Bischloroethylamines- Cell Cycle Specificity

A

No

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4
Q

Cyclophosphamide- Kinetics

A

metabolites excreted in urine

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5
Q

Cyclophosphamide- Clinical Use

A

breast cancer
non-Hodgkin’s lymphoma

help prevent hemorrhagic cystitis by early morning administration, drinking lots of water, and use of Mesna ( a uroprotective agent)

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6
Q

Cyclophosphamide, Nitrogen Mustard, Chlorambucil, Melphalan- Toxicities

A 
MYELOSUPPRESSION= LIMITING
nausea
vomiting 
hair loss
hemorrhagic cystitis

can produce a defect in free water clearance that can lead to hyponatremia

INCREASED CHANCE OF LEUKEMIA

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7
Q

Bifunctional Alkylating Agents- Bischloroethylamines- Resistance

A

enhanced cellular capacity for DNA repair

increased cellular concentrations of glutathione

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8
Q

Nitrogen Mustard- Clinical Use

A

Hodgkin’s Disease

Vesicant- extravasation leads to severe tissue damage

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9
Q

Chlorambucil, Melphalan- Clinical Use

A

chronic lymphocytic leukemia

multiple myeloma

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10
Q

Ifosfamide- Kinetics

A

excreted via urine

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11
Q

Ifosfamide- Toxicities

A 
URINARY TRACT TOXICITY= LIMITING
milder myelosuppression
lethargy
confusion
nausea
vomiting
hair loss

commonly causes hemorrhagic cystitis

DUE TO PROPENSITY FOR HEMORRHAGIC CYSTITIS IT IS ALWAYS COADMINISTERED WITH MESNA

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12
Q

Bifunctional Alkylating Agents- Nitrosoureas- Available Drugs

A

BCNU (Bischoloroethylnitrosourea)
CCNU
Streptozotocin

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13
Q

Bifunctional Alkylating Agents- Nitrosoureas- Mech of Action

A

non-enzymatic decomposition to active moieties

BIFUNCTIONAL ALKYLATION OF DNA AT N7 AND O6 OF GUANINE AND FORMS INTERSTRAND AND INTRASTRAND CROSSLINKS

target= DNA

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14
Q

Bifunctional Alkylating Agents- Nitrosoureas- Cell Cycle Specificity

A

No

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15
Q

Bifunctional Alkylating Agents- Nitrosoureas- Kinetics

A

LIPOPHILIC- CROSSES BBB

unstable in solution and rapidly cleared from plasma

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16
Q

Bifunctional Alkylating Agents- Nitrosoureas- Resistance

A

enhanced DNA repair capacity

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17
Q

BCNU (bischloroethylnitrosourea)- Clinical Use

A

BRAIN TUMORS

administered every 8 weeks IV

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18
Q

BCNU (bischloroethylnitrosourea)- Toxicities

A

MYELOSUPPRESSION (DOESN’T APPEAR UNTIL 4-6 WEEKS AFTER ADMINISTRATION)- LIMITING

CUMULATIVE PULMONARY TOXICITY

nausea, vomiting, hair loss

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19
Q

Streptozotocin- Clinical Use

A

pancreatic islet cell tumors

monofunctional

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20
Q

Streptozotocin- Toxicities

A

no myelosuppression

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21
Q

Bifunctional Alkylating Agents- Platinum Compounds- Available Drugs

A

Cisplatin (Cis-diaminedichloroplatinum)
Carboplatin
Oxaliplatin

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22
Q

Bifunctional Alkylating Agents- Platinum Compounds- Mech of Action

A

Activated by aquation in the presence of low Cl concentration

BIFUNCTIONAL ALKYLATION OF DNA AT N7 OF GUANINE AND ADENINE AND FORMS INTERSTRAND AND INTRASTRAND CROSSLINKS

target= DNA

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23
Q

Bifunctional Alkylating Agents- Platinum Compounds- Cell Cycle Specificity

A

No

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24
Q

Bifunctional Alkylating Agents- Platinum Compounds- Resistance

A

enhanced cellular capacity for DNA repair

increased cellular concentrations of glutathione

cross resistance between drugs

25
Q

Cisplatin (Cis-diaminedichloroplatinum)- Toxicities

A

RENAL TOXICITY (CAN PROTECT WITH SALINE/MANNITOL DIURESIS- CHLORURESIS PROTECTS TEH KIDNEY), REDUCE DOSE IN KIDNEY FAILURE- LIMITING

PTS W/ CARDIAC PROBLEMS MAY NOT BE ABLE TO TOLERATE THE DRUG WITH THE REQUIRED EXTRA HYDRATION- LIMITING

Intense nausea and vomiting
myelosuppression 
hypomagnesemia 
peripheral neuropathy 
8th cranial nerve damage
allergy
26
Q

Cisplatin (Cis-diaminedichloroplatinum)- Kinetics

A

Highly protein bound
Excretion by kidney

time to peak function is based on rate of aquation, = 6h

27
Q

Carboplatin- Clinical Use

A

TESTICULAR, OVARIAN, LUNG CANCER

Bladder, head, neck cancer

28
Q

Oxaliplatin- Toxicities

A

NEUROTOXICITY-LIMITING- COLD INDUCED, CUMULATIVE, MAY RESOLVE SOMEWHAT AFTER STOPPING DRUG

29
Q

Carboplatin- Kinetics

A

DOSE IS CALCULATED BY AUC

time to peak function is based on rate of aquation, = 12h

30
Q

Plant Alkyloids- Spindle Poisons- Mech of Action

A

BINDS DIMERIC FORM OF TUBULIN AND PREVENTS POLYMERIZATION OF TUBULIN AND THUS MICROTUBULE ASSEMBLY CAUSING DISSOLUTION OF MITOTIC SPINDLE

target= tubulin

31
Q

Carboplatin- Toxicities

A

LIMITING - MYELOSUPPRESSION

NOT RENAL TOXIC / DOES NOT REQUIRE EXTRA HYDRATION –> ALTERNATIVE TO CISPLATIN IN ORGAN DYSFUNCTION.

32
Q

Oxaliplatin- Clinical Use

A

GI MALIGNANCIES, ESPECIALLY COLORECTAL CANCER

33
Q

Plant Alkyloids- Spindle Poisons- Resistance

A

P-glycoprotien efflux pump (MDR)

34
Q

Plant Alkyloids- Spindle Poisons- Available Drugs

A

Vincristine
Vinblastine
Vinorelbine

35
Q

Vincristine- Clinical Use

A

LYMPHOBLASTIC LEUKEMIA
lymphoma
Hodgkin’s disease

36
Q

Plant Alkyloids- Spindle Poisons- Cell Cycle Specificity

A

M PHASE SPECIFIC

37
Q

Vinblastine- Toxicities

A

MYELOSUPPRESSION- LIMITING

No neurotoxicity

38
Q

Vincristine- Kinetics

A

EXCRETION IN BILE- PTS WITH ELEVATED BILIRUBIN REQUIRE DOSE ADJUSTMENT

39
Q

Paclitaxel (Taxol)- Kinetics

A

Tightly bound to protein

Biliary excretion

40
Q

Vincristine- Toxicities

A

SENSORY AND AUTONOMIC NEUROPATHIES
STIMULATION OF ADH RELEASE MAY CAUSE HYPONATREMIA

NO MYELOSUPPRESSION
little hair loss, nausea, and vomiting

do not exceed a single dose of >2mg= increased chance of neuropathies

41
Q

Plant Alkyloids- Tubulin Disassembly Inhibitors- Cell Cycle Specificity

A

M PHASE SPECIFIC

42
Q

Vinorelbine- Clinical Use

A

LUNG AND BREAST CANCER

43
Q

Paclitaxel (Taxol)- Toxicities

A 
MYELOSUPPRESSION- LIMITING
nausea
vomiting
stomatitis
peripheral sensory neuropathy

must be premedicated with steroids, diphenhydramine, and an H2 blocker to reduce chance of allergic reaction

44
Q

Plant Alkyloids- Tubulin Disassembly Inhibitors- Available Drugs

A

PACLITAXEL (TAXOL)

DOCETAXOL

45
Q

Plant Alkyloids- Tubulin Disassembly Inhibitors- Mech of Action

A

PREVENT TUBULIN DISASSEMBLY

Target= Tubulin

46
Q

Plant Alkyloids- Podophyllotoxin- Available Drugs

A

Etoposide (VP-16)

47
Q

Plant Alkyloids- Tubulin Disassembly Inhibitors- Resistance

A

tubulin mutations

MDR

48
Q

Docetaxol- Clinical Use

A

PROSTATE CANCER

49
Q

Paclitaxel (Taxol)- Clinical Use

A

OVARIAN CANCER

NON-SMALL CELL LUNG CANCER

50
Q

Etoposide (VP-16)- Kinetics

A

excretion in kidney and bile, thus reduce dose in kidney or hepatic problems

51
Q

Etoposide (VP-16)- Mech of Action

A

COMPLEX OF DRUG, DNA, AND TOPOISOMERASE II PRODUCES DNA STRAND BREAKAGE

target= Topoisomerase II

52
Q

Etoposide (VP-16)- Toxicities

A

LIMITING- MYELOSUPPRESSION

CAN INCREASE CHANCE OF LEUKEMIA

nausea
vomiting
hair loss
high rates of infusion associated with chest pain and hypotension

53
Q

Etoposide (VP-16)- Cell Cycle Specificity

A

LATE S-G2 PHASE BLOCK

54
Q

Cisplatin- Clinical Use

A

TESTICULAR, OVARIAN, LUNG CANCER

Bladder, head, neck cancer

55
Q

Etoposide (VP-16)- Clinical Use

A

TESTICULAR CANCER
SMALL CELL LUNG CANCER
LYMPHOMAS

56
Q

Etoposide (VP-16)- Resistance

A

Enhanced DNA repair
TOPO II mutations
MDR

57
Q

MESNA

A

DIMERIZES IN BLOOD AND IS INACTIVE

IN URINE IT BECOMES A MONOMER AND BINDS ALKYLATING AGENT METABOLITES

PREVENTS SIDE EFFECTS (HEMORRHAGIC CYSTITIS) IN HIGH DOSE ALKYLATING AGENTS

58
Q

Vinblastine- Clinical Use

A

LYMPHOBLASTIC LEUKEMIA
lymphoma
Hodgkin’s disease

59
Q

Vinblastine- Kinetics

A

EXCRETION IN BILE- PTS WITH ELEVATED BILIRUBIN REQUIRE DOSE ADJUSTMENT

Pharm II Test 4 (5 decks)

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