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Pharmacology > Pharmacology: Heme/Onc > Flashcards

Pharmacology: Heme/Onc Flashcards

1
Q

Heparin

What lab value do you monitor?

A

Anti-coagulant; binds and enhances anti-thrombin III activity (induces conformational change that allows ATIII to rapidly inhibit thrombin [IIa], Xa, IXa, VIIa)
- Rapid effect
- Does not work on thrombin already bound to fibrin
- Monitor PTT
SE: excessive bleeding, HIT, osteoporosis, hypersensitivity, use low doses to decr risk from thrombosis from reduced levels of ATIII

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2
Q

Protamine sulfate

A

Reverses heparin action

- positively charged drug that binds negatively charged heparin

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3
Q

Enoxaparin

Monitor labs?

A

Anticoagulant; LMWH

  • More Xa effects
  • No labs to monitor
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4
Q

Lepirudin

A

Anticoagulant; direct thrombin inhibitor

Alternative for anticoaguation in HIT

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5
Q

Bivalirudin

A

Anticoagulant; direct thrombin inhibitor

Alternative for anticoaguation in HIT

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6
Q

Warfarin (Coumadin)

A

Anticoagulant; inhibits epoxide reductase (gamma-carboxylation of Vit K dependent clotting factors)
- Cyt P450 metabolism
- Long half-life
SEs: bleeding, teratogenic, drug-drug reactions, skin/tissue necrosis! (From pro-thrombotic state when anti-coag PC/PS initially decreases before clotting factors)

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7
Q

Fondaparinux

A

Synthetic pentasaccharide, selective Factor Xa inhibitor (NOT thrombin)

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8
Q

Streptokinase

A

Thrombolytic
Complexes with plasminogen and the resulting complex activates plasminogen to plasmin conversion
- Early MI, early ischemic stroke
SEs: Bleeding! (Don’t use in active bleeding, ICH, recent surgery, bleeding d/o, severe hypertension

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9
Q

Urokinase

A

Thrombolytic

Directly activates plasminogen to plasmin

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10
Q

tPA

A

Thrombolytic

Directly activates plasminogen to plasmin

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11
Q

Alteplase

A

Another name for tPA!
Thrombolytic
Directly activates plasminogen to plasmin

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12
Q

Anisoylated plasminogen streptokinase activator complex (APSAC)

A

Thrombolytic, already activated complex

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13
Q

Aminocaproic acid

A

Inhibits fibrinolysis by preventing plasminogen activation

SE: intravascular thrombosis

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14
Q

Tranexamic acid

A

Inhibits fibrinolysis by preventing plasminogen activation

SE: intravascular thrombosis

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15
Q

Aspirin

What does the BT, PT, PTT look like?

A

Anti-platelet (low dose), anti-pyretic and analgesic (med dose), anti-inflammatory (high dose)
- Acetylates and irreversibly inhibits COX-1 and -2
- Prevents AA –> TXA2 conversion (which normally mediates plt aggregation) and AA –> PGs
- Increases BT
- No effect on PT/PTT
SEs:
- GI: gastric ulcers, bleeding
- Renal: RF, AIN
- Hyperventilation, tinnitus (CN VIII)
- Reye’s syndrome in kids (rash, encephalitis, fatty liver)

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16
Q

Clopidogrel

A

Anti-platelet

Irreversible blockade of ADP receptors, prevent gpIIb/IIIa expression decr fibrinogen binding

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17
Q

Ticlopidine

A

Anti-platelet
Irreversible blockade of ADP receptors, prevent gpIIb/IIIa expression decr fibrinogen binding
SE: Neutropenia!

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18
Q

Clopidogrel vs. ticlopidine

A

Ticlopidine can cause neutropenia

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19
Q

Cilostazol

A

PDE III inhibitor (which normally degrade cAMP), increases cAMP and prevents platelet aggregation
Uses: intermittent claudication, coronary vasodilation, prevent stroke/TIA with ASA, ppx angina
SEs: nausea, HA, facial flushing, hypotension,abdominal pain

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20
Q

Dipyridamole

A

PDE III inhibitor (which normally degrade cAMP), increases cAMP and prevents platelet aggregation
Uses: same as cilostazol, also used in pharmacologic stress testing

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21
Q

Abiciximab

A

Antiplatelet

Monoclonal antibody against gp IIb/IIIa on activated platelets

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22
Q

Eptifibaride

A

Antiplatelet

Peptide inhibitor of gp IIb/IIIa

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23
Q

Tirofiban

A

Antiplatelet

Non-peptide inhibitor of gp IIb/IIIa

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24
Q

Hirudin

A

Direct thrombin inibitor

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25
Q

Argatroban

A

Direct thrombin inibitor

26
Q

Methotrexate

A

Antimetabolite

  • Folic acid analog, inhibits dihydrofolate reductase leading to decreased formation of dTMP and decreased DNA and protein synthesis
  • SEs: myelosuppression (leucovorin rescue), macrovesicular fatty liver change, mucositis, teratogenic
27
Q

5-fluorouracil

A

Antimetabolite

  • Pyrimidine analog, bioactivated to 5F-dUMP, which covalently complexes folic acid. Complex inhibitis thymidylate synthase
  • Synergistic with MTX
  • SEs: myelosuppression, not reversible with leucovorin; photosensitivity
28
Q

6-mercaptopurine

A

Antimetabolite

  • Leukemia/lymphoma, but NOT CLL or Hodgkin’s
  • XO metabolism, increased toxicity with allopurinol
29
Q

6-thioguanine

A

Antimetabolite

  • ALL
  • Ok with allopurinol
30
Q

Cytarabine (ara-C)

A

Antimetabolite

- Pyrimidine analog

31
Q
  1. Leucovorin

2. Allopurinol

A
  1. Myelosuppression by MTX can be rescued via leucovorin, but not with 5-FU
  2. 6-MP should not be used with allopurionol (metabolized by XO), but 6-TG is ok
32
Q

What other things can MTX be used for (other than leukemia/lymphoma)?

A
  1. Other cancers: choriocarcinoma, sarcomas (e.g. osteosarcoma)
  2. Noncancers: abortion, ectopic pregnancy, RA, psoriasis
33
Q

Dactinomycin

What is is used for?

A

Antitumor antibiotic
- DNA intercalation
Childhood tumors!! (Ewing’s, Wilms)

34
Q

Doxorubicin

A

Antitumor antibiotic

- FR generation, non-covalent DNA intercalation leading to DNA breaks and decreased replication

35
Q

Daunorubicin

A

Antitumor antibiotic

- FR generation, non-covalent DNA intercalation leading to DNA breaks and decreased replication

36
Q

Dexrazoxane

A

Iron chelating agent

Prevent cardiotoxicity with doxo/daunorubicin therapy

37
Q

Bleomycin

A

Antitumor antibiotic

- FR generation, non-covalent DNA intercalation leading to DNA breaks and decreased replication

38
Q

Etoposide (VP-16)

A

Antitumor antibiotic
Inhibits topoisomerase II, increases DNA degradation
- For small cell carcinoma of lung and prostate, testicular carcinoma
SEs: myelosuppresion, alopecia, GI irritation

39
Q

Teniposide

A

Antitumor antibiotic
Inhibits topoisomerase II, increases DNA degradation
- For small cell carcinoma of lung and prostate, testicular carcinoma
SEs: myelosuppresion, alopecia, GI irritation

40
Q

Cyclophosphamide

A

Alkylating agent

  • Covalently cross-link (interstrand) DNA at guanine N-7
  • Requires liver bioactivation
41
Q

Ifosfamide

A

Alkylating agent

  • Covalently cross-link (interstrand) DNA at guanine N-7
  • Requires liver bioactivation
42
Q

Mesna

A

For ppx of hemorrhagic cystitis by cyclophosphamide and ifosfamide

43
Q

Carmustine

A

Nitrosourea/alkylating agent
- Requires bioactivation
- Can cross BBB, use for brain tumors! (GBM)
SEs: CNS toxicity–dizziness, ataxia

44
Q

Lomustine

A

Nitrosourea/alkylating agent
- Requires bioactivation
- Can cross BBB, use for brain tumors! (GBM)
SEs: CNS toxicity–dizziness, ataxia

45
Q

Semustine

A

Nitrosourea/alkylating agent
- Requires bioactivation
- Can cross BBB, use for brain tumors! (GBM)
SEs: CNS toxicity–dizziness, ataxia

46
Q

Streptozocin

A

Nitrosourea/alkylating agent
- Requires bioactivation
- Can cross BBB, use for brain tumors! (GBM)
SEs: CNS toxicity–dizziness, ataxia

47
Q

Busulfan

A

Alkylating agent
- CML
SEs: pulmonary fibrosis, hyperpigmentation

48
Q

Vincristine

A

Microtubule inhibitor
- Bind tubulin in M phase and inhibit microtubule polymerization
- Mitotic spindle cannot form
SE: Neurotoxic (areflexia, peripheral neuritis), paralytic ileus

49
Q

Vinblastine

A

Microtubule inhibitor
- Bind tubulin in M phase and inhibit microtubule polymerization
- Mitotic spindle cannot form
SE: Myelosuppression

50
Q

Paclitaxel

A

Microtubule inhibitor
- Hyperstabilizes polymerized microtubules in M-phase so that mitotic spindle cannot form
- Ovarian and breast cancers
SEs; Myelosuppression and hypersensitivity

51
Q

Cisplatin

A

Cross-links DNA

- SEs: Nephrotoxicity, ototoxicity

52
Q

Carboplatin

A

Cross-links DNA

- SEs: Nephrotoxicity, ototoxicity

53
Q

Amifostine

A

FR scavenger

Use to prevent nephrotoxicity with -platin chemotherapy

54
Q

Choride diuresis

A

A method of forced diuresis to enhance excretion of drugs in urine
Used to prevent nephrotoxicity with -platin chemotherapy
e.g. AlCl.. makes urine more acidic

55
Q

Hydroxyurea

A

Inhibits ribonucleotide reductase and decreases DNA snythesis in S phase
Also increases HbF in SCD
- SEs: myelosuppression, GI upset

56
Q

Prednisone

A

May trigger apoptosis

57
Q

Tamoxifen

A

SERM

58
Q

Raloxifen

A

SERM

59
Q

Trastuzumab

A

aka Herceptin
Monoclonal ab against HER-2 (erb-b2), a tyrosine kinase
- SE: cardiotoxic

60
Q

Imatinib

A

aka Gleevec
For CML, bcr-abl tyr kinase inhibitor
- SE: fluid retention

61
Q

Rituximab

A

Monoclonal ab against CD20 in B cells

- Used for nHL, RA

Pharmacology (15 decks)

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