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Pharm Drug Table > Drug Table - Alkylating Agents > Flashcards

Drug Table - Alkylating Agents Flashcards

1
Q

Alkylating Agents Mechanism

A

Produce strong electrophiles through
carbonium or ethyleneimonium ion
intermediates, which covalently bond via
alkylation of nucleophilic moieties in DNA
(mostly N7 position of guanine); Cell Cycle
Non-Specific (CCNS)

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2
Q

Alkylating Agents Important Side Effects

A

Bone marrow, mucosal toxicity,
nausea and vomiting, toxic effects
on reproductive systems,
increased leukemia risk

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3
Q

Alkylating Agents Miscellaneous

A 
Resistance may occur due to:
decreased permeability or uptake;
increased rates of catabolism;
enhanced DNA repair; increased
glutathione production (inactivates
via conjugation)
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4
Q

List 11 Alkylating Agents

A 
Mechlorethamine (Mustargen)
Cyclophosphamide (Cytoxan)
Ifosfamide (Ifex)
Carmustine (Gliadel)
Lomustine (Ceenu)
Dacarbazine (DTIC)
Procarbazine (Matulane)
Temozolomide (Temodar)
Cisplatin (Platinol)
Carboplatin (Paraplatin)
Oxaliplatin (Eloxatin)
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5
Q

Mechlorethamine class

A

(Mustargen)

Nitrogen mustard

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6
Q

Mechlorethamine mechanism

A

Alkylating agent; spontaneous conversion to active metabolites in body fluids or
enzymatically converted in liver

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7
Q

Mechlorethamine Therapeutics

A

Hodgkin’s disease, topically for treatment of cutaneous T-cell lymphoma

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8
Q

Mechlorethamine “Other” side effects

A

Severe nausea and vomiting,
myelosuppression (leucopenia,
thrombocytopenia)

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9
Q

Mechlorethamine Misc

A

Don’t use much anymore due to sterility

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10
Q

Cyclophosphamide
(Cytoxan)
Class

A

Nitrogen mustard

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11
Q

Cyclophosphamide
(Cytoxan)
Mechanism

A

Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard

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12
Q

Cyclophosphamide
(Cytoxan)
Therapeutics

A

Most widely used alkylating agent (broad clinical spectrum); singly or in
combination for ALL, CLL, non-Hodgkin’s lymphoma, and breast, lung, and ovarian cancer

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13
Q

Cyclophosphamide
(Cytoxan)
Important Side Effects

A 
Hemorrhagic cystitis (bladder
irritation) due to acrolein (toxic
drug metabolite); adequate
hydration and administration of
MESNA (2-mercaptoethane
sulfonate) minimizes problem
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14
Q

Cyclophosphamide
(Cytoxan)
“Other” Side Effects

A

Nausea, vomiting,

myelosuppression

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15
Q

Cyclophosphamide
(Cytoxan)
Miscellaneous

A

Relatively long plasma half-life (7-15 hrs); taken orally

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16
Q

Difference between Ifosfamide and Cyclophosphamide

A

Therapeutics
Ifos is used for Sarcoma and testicular cancer
Cyclophosphamide is the most widely used

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17
Q

Carmustine (Gliadel)
Lomustine (Ceenu)
Class

A

Nitrosoureas

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18
Q

Carmustine (Gliadel)
Lomustine (Ceenu)
Mechanism

A

Alkylating agent

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19
Q

Carmustine (Gliadel)
Lomustine (Ceenu)
Therapeutics

A

Brain tumors (cross blood-brain barrier)

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20
Q

Carmustine (Gliadel)
Lomustine (Ceenu)
Imp Side Effects

A

Renal toxicity, pulmonary fibrosis

21
Q

Carmustine (Gliadel)
Lomustine (Ceenu)
Other side effects

A

Profound myelosuppression,

severe nausea and vomiting

22
Q

Dacarbazine (DTIC)

class

A

Triazenes

23
Q

Dacarbazine (DTIC)

Mechanism

A

Alkylating agent; prodrug activated by liver

cytochromes

24
Q

Dacarbazine (DTIC)

Therapeutics

A

Part of ABVD for Hodgkin’s disease; also, malignant melanoma

25
Q

Dacarbazine (DTIC)

“Other” Side Effects

A

Nausea and vomiting,
myelosuppression (neutropenia, thrombocytopenia), flu-like
symptoms (fever, fatigue)

26
Q

Dacarbazine (DTIC)

Miscellaneous

A

IV administration

27
Q

Procarbazine
(Matulane)
class

A

Triazenes

28
Q

Procarbazine
(Matulane)
Mechanism

A

Alkylating agent; forms free radicals

29
Q

Procarbazine
(Matulane)
Therapeutics

A

Hodgkin’s lymphoma

30
Q

Procarbazine
(Matulane)
Important side effects

A

May cause leukemia

31
Q

Temozolomide
(Temodar)
class

A

Triazenes

32
Q

Temozolomide
(Temodar)
Mechanism

A

Alkylating agent; nonenzymatic conversion

to methylhydrazine at physiologic pH

33
Q

Temozolomide
(Temodar)
Therapeutics

A

Malignant gliomas

34
Q

Temozolomide
(Temodar)
“Other” Side Effects

A

Nausea and vomiting,
myelosuppression (neutropenia,
thrombocytopenia), flu-like
symptoms (fever, fatigue)

35
Q

Temozolomide
(Temodar)
Miscellaneous

A

Taken orally

36
Q

Cisplatin (Platinol)

class

A

Platinum analogs

37
Q

Cisplatin (Platinol)

Mechanism

A

Alkylating agents that do not form
carbonium ion intermediates or formally
alkylate DNA; covalently bind nucleophilic
sites on DNA (e.g., guanine N7); converted
to active cytotoxic forms by reacting with
water to form (+)charged, hydrated
intermediates that react with DNA guanine,
forming inter- and intrastand cross-links

38
Q

Cisplatin (Platinol)

Therapeutics

A

Testicular, ovarian, cervical, and
bladder cancers; also useful in
treatment of head and neck cancer,
and lung carcinoma

39
Q

Cisplatin (Platinol)

Imp Side Effects

A

Nephrotoxicity, ototoxicity,
peripheral motor and sensory
neuropathy at high doses

40
Q

Cisplatin (Platinol)

Other side effects

A

Severe nausea and vomiting,
mild to moderate
myelosuppression

41
Q

Carboplatin
(Paraplatin)
Class

A

Platinum analogs

42
Q

Carboplatin
(Paraplatin)
Mechanism

A

Alkylating agents that do not form
carbonium ion intermediates or formally
alkylate DNA; covalently bind nucleophilic
sites on DNA (e.g., guanine N7); converted
to active cytotoxic forms by reacting with
water to form (+)charged, hydrated
intermediates that react with DNA guanine,
forming inter- and intrastand cross-links

43
Q

Carboplatin
(Paraplatin)
Therapeutics

A

Ovarian cancer

44
Q

Carboplatin
(Paraplatin)
Other side effects

A

Myelosuppression

thrombocytopenia

45
Q

Oxaliplatin (Eloxatin)

class

A

Platinum analogs

46
Q

Oxaliplatin (Eloxatin)

Mechanism

A

Alkylating agents that do not form
carbonium ion intermediates or formally
alkylate DNA; covalently bind nucleophilic
sites on DNA (e.g., guanine N7); converted
to active cytotoxic forms by reacting with
water to form (+)charged, hydrated
intermediates that react with DNA guanine,
forming inter- and intrastand cross-links

47
Q

Oxaliplatin (Eloxatin)

Therapeutics

A

Gastric and colorectal cancer

48
Q

Oxaliplatin (Eloxatin)

Imp Side effects

A

Peripheral sensory neuropathy

cold-induced

49
Q

Oxaliplatin (Eloxatin)

Other side effects

A

Neutropenia

Pharm Drug Table (11 decks)

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