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MCC > Quiz 2 drugs > Flashcards

Quiz 2 drugs Flashcards

1
Q

Why is mesna necessary with Cyclophosphamide administration?

A

it is a prodrug activated with multiple active forms, one of which is converted to acrolein (cytotoxic and damages bladder), and mesna binds acrolein

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2
Q

What is the PK of cyclophosphamide?

A

Metabolized by CYP P450 enzymes to active/inactive metabolites, 80% renal elimination

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3
Q

What is the acute/delayed toxicity of cyclophosphamide?

A

A: N/V (high dose)
D: BM toxicity, mucositis, azoospermia, ovarian failure, secondary cancers, alopecia, hemorrhagic cystitis and SIADH

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4
Q

What is the generic/brand name of the principle Platinum drug (alkylating-like) used for MCC?

A

Cisplatin (Platinol)

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5
Q

What is the MoA of Cisplatin?

A

Forms primarily intrastrand cross links (also interstrand and mono) as well as binds to nuclear and cytoplasmic proteins

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6
Q

What is the dosage and administration of Cisplatin?

A

IV

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7
Q

What are the acute/delayed toxicities of Cisplatin?

A

A: N/V (high dose)
D: Nephrotoxicity, peripheral sensory neuropathy, ototoxicity, nerve dysfunction

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8
Q

What is the principle drug used as a folic acid analog?

A

Methotrexate

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9
Q

What is the MoA of Methotrexate?

A

Inhibits DHFR and prevents conversion of FA to THF, the methyl-donor for thymidylate synthase. Also affects nucleotide synthesis minor mechanisms

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10
Q

What is the dosage and admin of MTX?

A

PO, IV, IT (high dose MTX with leucovorin after)

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11
Q

What is the relevant PK of MTX?

A

Renal elimination, dose with urinary alkalinization and hyper-hydration

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12
Q

What is the acute/delayed toxicity of MTX?

A

A: N/V (scales with dose)
D: myelosuppression, mucositis, nephrotoxicity, hepatotoxicity, pneumonitis

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13
Q

What are significant drug interactions for MTX?

A

Salicylates, sulfonamides, probenecid, penicillin, NSAIDs

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14
Q

What is the generic/brand name of the principle Nitrogen mustard used in MCC?

A

Cyclophosphamide (cytoxan)

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15
Q

What is the MoA of Cyclophosphamide?

A

It forms primarly intERstrand DNA crosslinks (also intRA and mono) resulting in inhibition of DNA synthesis and function

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16
Q

What are the dosage and admin of Cyclophosphamide?

A

D: IV, PO
A: High dose with mesna

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17
Q

What antidote can be given for MTX adminstration?

A

carboxypeptidase G2

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18
Q

What two fluorinated Pyrimidine analogs are used to treat cancer in MCC?

A

Fluorouracil “5-FU” and Capecitabine (Xeloda)

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19
Q

What is the MoA of the fluorinated pyrimidine analogs used in MCC?

A

Suicide inhibition of Thymidylate synthase; incorporation of F-UTP into RNA, FdUTP into DNA

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20
Q

What are the doseage and admin of 5-FU and Capecitabine?

A

5- IV
C-PO, with food b.i.d.

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21
Q

What are the PK of 5-FU and Capecitabine?

A

Extensive liver processing

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22
Q

What is the acute/delayed toxicity for 5-FU and Capecitabine?

A

A: N/V (low)
D: HFS, Myelosuppression, diarrhea, and coronary vasospasm

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23
Q

What are the significant drug interactions of Capecitabine?

A

CYP2C9 inhibitors (Warfarin)

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24
Q

What antidote could be given for a fluorinated pyrimidine analog?

A

Uridine triacetate

25
Q

What is the principal Cytidine pyrimidine analog used in MCC?

A

Cytarabine “Ara-C”

26
Q

What is the MoA of Cytarabine?

A

Ara-C inhibits DNA chain elongation, synthesis and repair; inhibits ribonucleotide reductase, reduced formation of dNTPs; cytarabine triphosphate incorporated into DNA

27
Q

What is the dosage and admin of Cytarabine?

A

IV, SQ, IT

28
Q

What are the notable PK of Cytarabine?

A

Renal elimination, good BBB penetration

29
Q

What is the acute/delayed toxicity of Cytarabine?

A

A: N/V (follows dose)
D: myelosuppression, GI, cerebellar toxicity, ocular conjunctivitis, rash

30
Q

What other notable actions are taken during Cytarabine treatment?

A

neurological exam before each dose
steroid eye drops during use

31
Q

Which two chemotherapy drugs have the best BBB penetration? What drug family are they in?

A

Methotrexate and Cytarabine; Antimetabolites

32
Q

Which of the chemotherapy drugs are prodrugs?

A

Cyclophosphamide, Cytarabine,…

33
Q

What specific drugs are principally used in MCC as Vitamin K antagonists?

A

Warfarin

34
Q

What is the MoA of Warfarin?

A

Warfarin inhibits Vit K epoxide reductase; causing decreased Factors II, VII, IX, X as well as proteins C and S

35
Q

Which anticoagulant drugs are metabolized by CYP enzymes?

A

Wafarin- CYP2C9
Direct Factors Xa inhibitors- CYP3A4/5 also a P-gp substrate

36
Q

Which anticoagulant medication is preferred to treat DIC?

A

unfractionated heparin

37
Q

Which anticoagulants require monitoring?

A

Warfarin- PT/INR
Heparin- aPTT/anti-Xa
Direct FXa inhibitor- monitor renal/hepatic funciton
Thrombin inhibitor- monitor renal function

38
Q

Which anticoagulant drugs have a HIT risk?

A

Unf. heparin and LMWHs

39
Q

Which anticoagulants are contraindicated in pregnancy?

A

Warfarin

40
Q

Which anticoagulants are preferred for A-fib in a pt with prosthetic valves? Without?

A

Warfarin; DOACs (rivaroxaban, apixaban, edoxaban, dibigatran)

41
Q

Which anticoagulants are preferred for prophylaxis in THA and TKA?

A

DOACs

42
Q

What is the CrCl cutoff for edoxaban treatment?

A

Excluded in pts with CrCl>95

43
Q

Which anticoagulants are more largely hepatically cleared?

A

apixaban

44
Q

Which is the protocol for reversal of Warfarin treatment?

A

PT complex concentrate, FFP, Vit K (depending on bleeding and INR)

45
Q

What is the protocol for reversal of unfractionated heparin treatment?

A

Protamine

46
Q

What is the protocol for reversal of LMWHs?

A

partial reversal with protamine

47
Q

What is the protocol for reversal of fondaparinux?

A

None

48
Q

What is the protocol for reversal of Direct Factor Xa inhibitors?

A

andexanet alfa (only for rivaroxaban and apixaban)

49
Q

What is the protocol for reversal of Dabigatran?

A

idarucizumab

50
Q

What is the protocol for reversal of bivalirudin and argatroban?

A

None

51
Q

What is the MoA of Heparin?

A

Potentiation of antithrombin -> inhibition of Xa and IIa

52
Q

What is the difference in MoA between heparin, LMWHs and Synthetic heparin derivatives?

A

They all potentiate AT; LMWHs have less effect on IIa than Heparin, Fondaparinux only inhibits Xa

53
Q

What medications in MCC are principally used as LMWHs?

A

dalteparin, enoxaparin, tinzaparin

54
Q

What medications in MCC are principally used as a synthetic heparin derivative?

A

fondaparinux

55
Q

What medications in MCC are principally used as thrombin inhibitors?

A

bivalirudin, argatroban, dabigatran (also a DOAC)

56
Q

What is the MoA of aspirin?

A

irreversible inhibition of COX-1 -> inhibiton of TxA2 synthesis, imparing platelet aggregation

57
Q

What are the generic names of the thienopyridine drugs used in MCC?

A

clopidogrel and prasugrel

58
Q

What is the MoA of the pro-drugs, clopidogrel and prasugrel

A

Irreversible inhibition of platelet ADP receptors

MCC (10 decks)

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