Brainscape's Knowledge GenomeTM

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


See full index

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

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

Bifunctional Alkylating Agents- Bischloroethylamines- Cell Cycle Specificity

A

No

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

Cyclophosphamide- Kinetics

A

metabolites excreted in urine

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

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Bifunctional Alkylating Agents- Bischloroethylamines- Resistance

A

enhanced cellular capacity for DNA repair

increased cellular concentrations of glutathione

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Nitrogen Mustard- Clinical Use

A

Hodgkin’s Disease

Vesicant- extravasation leads to severe tissue damage

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

Chlorambucil, Melphalan- Clinical Use

A

chronic lymphocytic leukemia

multiple myeloma

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

Ifosfamide- Kinetics

A

excreted via urine

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

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

Bifunctional Alkylating Agents- Nitrosoureas- Available Drugs

A

BCNU (Bischoloroethylnitrosourea)
CCNU
Streptozotocin

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

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

Bifunctional Alkylating Agents- Nitrosoureas- Cell Cycle Specificity

A

No

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

Bifunctional Alkylating Agents- Nitrosoureas- Kinetics

A

LIPOPHILIC- CROSSES BBB

unstable in solution and rapidly cleared from plasma

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

Bifunctional Alkylating Agents- Nitrosoureas- Resistance

A

enhanced DNA repair capacity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

BCNU (bischloroethylnitrosourea)- Clinical Use

A

BRAIN TUMORS

administered every 8 weeks IV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

BCNU (bischloroethylnitrosourea)- Toxicities

A

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

CUMULATIVE PULMONARY TOXICITY

nausea, vomiting, hair loss

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Streptozotocin- Clinical Use

A

pancreatic islet cell tumors

monofunctional

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Streptozotocin- Toxicities

A

no myelosuppression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Bifunctional Alkylating Agents- Platinum Compounds- Available Drugs

A

Cisplatin (Cis-diaminedichloroplatinum)
Carboplatin
Oxaliplatin

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Bifunctional Alkylating Agents- Platinum Compounds- Cell Cycle Specificity

A

No

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

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