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Pharm II Test 4 > Chemo II Alkylating Agents > Flashcards

Chemo II Alkylating Agents Flashcards

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
Cisplatin (Cis-diaminedichloroplatinum)- Toxicities
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
Cisplatin (Cis-diaminedichloroplatinum)- Kinetics
Highly protein bound Excretion by kidney time to peak function is based on rate of aquation, = 6h
27
Carboplatin- Clinical Use
TESTICULAR, OVARIAN, LUNG CANCER Bladder, head, neck cancer
28
Oxaliplatin- Toxicities
NEUROTOXICITY-LIMITING- COLD INDUCED, CUMULATIVE, MAY RESOLVE SOMEWHAT AFTER STOPPING DRUG
29
Carboplatin- Kinetics
DOSE IS CALCULATED BY AUC time to peak function is based on rate of aquation, = 12h
30
Plant Alkyloids- Spindle Poisons- Mech of Action
BINDS DIMERIC FORM OF TUBULIN AND PREVENTS POLYMERIZATION OF TUBULIN AND THUS MICROTUBULE ASSEMBLY CAUSING DISSOLUTION OF MITOTIC SPINDLE target= tubulin
31
Carboplatin- Toxicities
LIMITING - MYELOSUPPRESSION NOT RENAL TOXIC / DOES NOT REQUIRE EXTRA HYDRATION --> ALTERNATIVE TO CISPLATIN IN ORGAN DYSFUNCTION.
32
Oxaliplatin- Clinical Use
GI MALIGNANCIES, ESPECIALLY COLORECTAL CANCER
33
Plant Alkyloids- Spindle Poisons- Resistance
P-glycoprotien efflux pump (MDR)
34
Plant Alkyloids- Spindle Poisons- Available Drugs
Vincristine Vinblastine Vinorelbine
35
Vincristine- Clinical Use
LYMPHOBLASTIC LEUKEMIA lymphoma Hodgkin's disease
36
Plant Alkyloids- Spindle Poisons- Cell Cycle Specificity
M PHASE SPECIFIC
37
Vinblastine- Toxicities
MYELOSUPPRESSION- LIMITING No neurotoxicity
38
Vincristine- Kinetics
EXCRETION IN BILE- PTS WITH ELEVATED BILIRUBIN REQUIRE DOSE ADJUSTMENT
39
Paclitaxel (Taxol)- Kinetics
Tightly bound to protein | Biliary excretion
40
Vincristine- Toxicities
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
Plant Alkyloids- Tubulin Disassembly Inhibitors- Cell Cycle Specificity
M PHASE SPECIFIC
42
Vinorelbine- Clinical Use
LUNG AND BREAST CANCER
43
Paclitaxel (Taxol)- Toxicities
``` 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
Plant Alkyloids- Tubulin Disassembly Inhibitors- Available Drugs
PACLITAXEL (TAXOL) | DOCETAXOL
45
Plant Alkyloids- Tubulin Disassembly Inhibitors- Mech of Action
PREVENT TUBULIN DISASSEMBLY | Target= Tubulin
46
Plant Alkyloids- Podophyllotoxin- Available Drugs
Etoposide (VP-16)
47
Plant Alkyloids- Tubulin Disassembly Inhibitors- Resistance
tubulin mutations | MDR
48
Docetaxol- Clinical Use
PROSTATE CANCER
49
Paclitaxel (Taxol)- Clinical Use
OVARIAN CANCER | NON-SMALL CELL LUNG CANCER
50
Etoposide (VP-16)- Kinetics
excretion in kidney and bile, thus reduce dose in kidney or hepatic problems
51
Etoposide (VP-16)- Mech of Action
COMPLEX OF DRUG, DNA, AND TOPOISOMERASE II PRODUCES DNA STRAND BREAKAGE target= Topoisomerase II
52
Etoposide (VP-16)- Toxicities
LIMITING- MYELOSUPPRESSION CAN INCREASE CHANCE OF LEUKEMIA nausea vomiting hair loss high rates of infusion associated with chest pain and hypotension
53
Etoposide (VP-16)- Cell Cycle Specificity
LATE S-G2 PHASE BLOCK
54
Cisplatin- Clinical Use
TESTICULAR, OVARIAN, LUNG CANCER Bladder, head, neck cancer
55
Etoposide (VP-16)- Clinical Use
**TESTICULAR CANCER** SMALL CELL LUNG CANCER LYMPHOMAS
56
Etoposide (VP-16)- Resistance
Enhanced DNA repair TOPO II mutations MDR
57
MESNA
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
Vinblastine- Clinical Use
LYMPHOBLASTIC LEUKEMIA lymphoma Hodgkin's disease
59
Vinblastine- Kinetics
EXCRETION IN BILE- PTS WITH ELEVATED BILIRUBIN REQUIRE DOSE ADJUSTMENT

Pharm II Test 4 (5 decks)

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