Heme Drugs Flashcards Preview

Pharmacology > Heme Drugs > Flashcards

Flashcards in Heme Drugs Deck (162):
1

Heparin (mechanism)

Activates antithrombin III --> decreases activity of thrombin (IIa) and factor Xa --> blood as site of action
Monitor PTT (intrinsic)

2

Heparin (antidote)

Protamine (chemical inactivation)

3

Heparin (use/placenta crossing)

Immediate anticoagulation for DVT, PE, MI
Can use during pregnancy (doesn't cross placenta)

4

Heparin (side effects)

Skin necrosis at injection site
HIT
Bleeding (duh)

5

Warfarin (mechanism)

Inhibits gamma carboxylation of vit K-dependent factors (II, VII, IX, X, C, S) --> liver as site of action
Monitor PT/INR (extrinsic)

6

Warfarin (use/placenta crossing)

Chronic anticoagulation
Crosses placenta so don't use in pregnant women

7

Warfarin (side effects)

Skin/tissue necrosis (usually seen first week of therapy -> due to protein C depletion b/c of its short HL -> so predisposition to this side effect w/ existing protein C and S deficiency)
Bleeding (duh)

8

Warfarin (antidotes)

Vit K
If severe, fresh frozen plasma

9

"-parin" (mechanism)

Enoxaparin, Dalteparin
LMW heparin: acts more on factor Xa (than II), longer HL, more bioavailable
Doesn't need to monitor labs like normal heparin

10

"-parin" (side effect)

No antidote like heparin

11

"-xaban" (mechanism)

Apixaban, rivaroxaban
Direct factor Xa inhibitor

12

"-xaban" (3 uses)

Tx/prophylaxis of DVT, PE, stroke

13

"-xaban" (side effect)

No antidote like heparin or warfarin

14

"-teplase" (mechanism)

Thrombolytics (fibrin-specific so only attaches to recently formed clot) -> aid conversion of plasminogen to plasmin --> plasmin cleaves thrombin and fibrin clots (so prolong both PT and PTT)
Alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA)

15

"-teplase" (3 uses)

Early MI
Early ischemic stroke (3-hr window)
Direct thrombolysis of severe PE

16

"-teplase" (side effects)

Verify that bleeding is not present before use!
Don't use in severe HTN
Accelerated idioventricular rhythm (AIVR) -> reperfusion arrhythmia that is benign and self-resolving

17

"-teplase" (3 antidotes)

Aminocaproic acid (inhibits fibrinolysis)
Fresh frozen plasma
Cryoprecipitate

18

Aspirin (mechanism)

Inhibits both COX-1 and 2 by covalent acetylation --> antiplatelet AGGREGATION is from the effects on COX-1 (COX-2 is not present on platelets but on endothelium)

19

Aspirin (side effects)

Gastric ulcers, tinnitus (VIII), renal failure w/ chronic use
Reye syndrome in children with viral infection
Overdose: resp alkalosis superimposed by metabolic acidosis

20

"-grel" (mechanism)

Clopidogrel, prasugrel
Irreversibly blocking ADP receptor --> inhibits platelet AGGREGATION
Prevents GP IIb/IIIa from binding to fibrinogen
Prodrug that needs to be activated by P450

21

"-grel" (3 uses)

Acute coronary syndrome
Coronary stenting
Reduces thrombotic stroke

22

"-grel" (2 side effects)

TTP/HUS

23

Ticlopidine (mechanism)

Irreversibly blocking ADP receptor --> inhibits platelet AGGREGATION
Prevents GP IIb/IIIa from binding to fibrinogen

24

Ticlopidine (3 uses and 3 side effects)

Only when can't tolerate aspirin or clopidogrel (1st line) -> for acute coronary syndrome, coronary stenting, reduces thrombotic stroke
Side effects: neutropenia (presenting as FEVER AND MOUTH ULCERS -> so monitor CBC biweekly for the first 3 months), TTP/HUS

25

Ticagrelor (mechanism)

Irreversibly blocking ADP receptor --> inhibits platelet AGGREGATION
Prevents GP IIb/IIIa from binding to fibrinogen

26

Ticagrelor (3 uses)

Acute coronary syndrome
Coronary stenting
Reduces thrombotic stroke

27

Ticagrelor (2 side effects)

TTP/HUS

28

Cilostazol (mechanism)

Phosphodiesterase III inhibitor --> increases cAMP inplatelets --> inhibits platelet aggregation
ALSO A DIRECT ARTERIAL VASODILATOR

29

Cilostazol (4 uses)

Intermittent claudication -> better than aspirin at peripheral arterial disease
Coronary vasodilation
Prevention of stroke/TIAs (combined w/ aspirin)
Angina prophylaxis

30

Cilostazol (5 side effects)

Flushing, abd pain, hypotension, nausea, headache

31

Dipyridamole (mechanism)

Phosphodiesterase III inhibitor --> increases cAMP inplatelets --> inhibits platelet aggregation
Vasodilator

32

Dipyridamole (4 uses)

Intermittent claudication
Coronary vasodilation
Prevention of stroke/TIAs (combined w/ aspirin)
Angina prophylaxis

33

Dipyridamole (5 side effects)

Flushing, abd pain, hypotension, nausea, headache

34

Abciximab (mechanism)

Monoclonal Ab Fab fragments, analog of fibrinogen
GP IIb/IIIa (integrin) inhibitor --> inhibits platelet aggregation

35

Abciximab (2 uses)

Unstable angina
Percutaneous transluminal coronary angioplasty

36

Abciximab (2 side effects)

Thrombocytopenia, bleeding

37

Eptifibatide (mechanism)

Analog of fibrinogen
GP IIb/IIIa (integrin) inhibitor --> inhibits platelet aggregation

38

Eptifibatide (2 uses)

Unstable angina
Percutaneous transluminal coronary angioplasty

39

Eptifibatide (2 side effects)

Thrombocytopenia, bleeding

40

Tirofiban (mechanism)

Analog of fibrinogen
GP IIb/IIIa (integrin) inhibitor --> inhibits platelet aggregation

41

Tirofiban (2 uses)

Unstable angina
Percutaneous transluminal coronary angioplasty

42

Tirofiban (2 side effects)

Thrombocytopenia, bleeding

43

Streptokinase (mechanism)

Binds free plasminogen to activate it (plasminogen doesn't have to be bound to fibrin clots) --> gets increased plasmin
Nonfibrin-specific (unlike "-teplase")

44

Streptokinase (3 uses)

Acute MI
Stroke
PE

45

Streptokinase (3 side effects)

Loses efficacy after initial administration (sensitized)
Allergic response
Bleeding (duh)

46

Methotrexate (mechanism)

Antimetabolite (S-phase specific) -> folic acid analog inhibiting DHF reductase (so decreases dTMP)
Converted to polyglutamate form after it gains access to cell to prevent movement out of cell

47

Methotrexate (3 categories of use)

Cancers: leukemias, lymphomas, choriocarcinoma, sarcoma
Abortion-related: abortion, ectopic pregnancy -> inhibits trophoblast division
Inflammation: RA, psoriasis, IBD

48

Methotrexate (4 side effects)

Myelosuppression (fixed w/ leucovorin rescue)
Hepatotoxicity (macrovesicular fatty change in liver)
Stomatitis (painful mouth ulcers) -> supplement w/ folic acid to prevent this
Teratogenic

49

5-fluorouracil (mechanism)

Antimetabolite (S-phase specific) - pyrimidine analog that interferes w/ folate metabolism -> inhibits thymidylate synthase (so decreases dTMP; reduced toxic effects in cells deficient in THF)

50

5-fluorouracil (3 uses)

Colon cancer
Pancreatic cancer
Basal cell carcinoma (topical)

51

5-fluorouracil (2 side effects)

Myelosuppression (not reversible w/ leucovorin!)
Photosensitivity

52

5-fluorouracil (antidote)

Uridine

53

Cytarabine (arabinofuranosyl cytidine) and gemcitabine (mechanism)

Antimetabolite (S-phase specific) - pyrimidine analog inhibiting DNA polymerase
Gemcitabine does the same thing but not S-phase specific and so more toxicity

54

Cytarabine (arabinofuranosyl cytidine) (2 uses)

Leukemias, lymphomas

55

Cytarabine (arabinofuranosyl cytidine) (side effect)

Pancytopenia (leukopenia, thrombocytopenia, megaloblastic anemia)

56

Azathioprine (mechanism)

Azathio"PURINE"
Antimetabolite (S-phase specific) - purine analog inhibiting de novo purine synthesis (thus also inhibits lymphocyte proliferation)
Activated by HGPRT

57

Azathioprine (2 categories of use)

Inflammatory: prevents organ rejection, RA, SLE, Crohn, glomerulonephritis
Cancer: leukemia

58

Azathioprine (4 side effects)

Bone marrow (pancytopenia), GI, liver
Increased toxicity w/ allopurinol (b/c its metabolism is mediated by xanthine oxidase)

59

6-mercaptopurine (mechanism)

Antimetabolite (S-phase specific) - purine analog inhibiting de novo purine synthesis
Activated by HGPRT

60

6-mercaptopurine (2 categories of use)

Inflammatory: prevents organ rejection, RA, IBD
Cancer: leukemia

61

6-mercaptopurine (4 side effects)

Bone marrow, GI, liver (abd pain, cirrhosis, cholestasis, jaundice)
Increased toxicity w/ allopurinol (b/c its metabolism is mediated by xanthine oxidase)

62

6-thioguanine (mechanism)

Antimetabolite (S-phase specific) - purine analog inhibiting de novo purine synthesis
Activated by HGPRT

63

6-thioguanine (2 categories of use)

Inflammatory: prevents organ rejection, RA, IBD
Cancer: leukemia

64

6-thioguanine (3 side effects)

Bone marrow, GI, liver

65

Dactinomycin (actinomycin D) (mechanism)

Antitumor antibiotics - intercalates in DNA

66

Dactinomycin (actinomycin D) (3 uses)

Children tumors: Wilm tumor, Ewing sarcoma, rhabdomyosarcoma

67

Dactinomycin (actinomycin D) (side effect)

Myelosuppression

68

Doxorubicin (adriamycin) and daunorubicin (mechanism)

Antitumor antibiotics - generates free radicals and breaks DNA (interrupts "proper base pairing and H bond formation")

69

Doxorubicin (adriamycin) and daunorubicin (3 uses)

Solid tumors, leukemias, lymphomas

70

Doxorubicin (adriamycin) and daunorubicin (3 side effects)

Cardiotoxicity (dilated cardiomyopathy; prevented by dexrazoxane which is iron-chelating agent) (think of D being the shape of heart)
Myelosuppression
Alopecia

71

Bleomycin (mechanism)

Antitumor antibiotics - generates free radicals and breaks DNA
G2 phase specific

72

Bleomycin (2 uses)

Testicular cancer
Hodgkin lymphoma

73

Bleomycin (4 side effects)

Pulmonary fibrosis (think of B being the shape of lungs)
Skin changes
Mucositis
Myelosuppression (minimal)

74

Cyclophosphamide (mechanism)

Alkylating agent - covalently X-linked (interstrand) at guanine N-7
Requires activation by liver P450

75

Cyclophosphamide (4 uses)

Solid tumors
Leukemia
Lymphomas
Some brain cancers

76

Cyclophosphamide (2 side effects)

Hemorrhagic cystitis: prevented by Mesna (binds metabolite acrolein in bladder) (think of C and Y being a bladder and urethra respectively)
Myelosuppression

77

Ifosfamide (mechanism)

Alkylating agent - covalently X-linked (interstrand) at guanine N-7
Requires activation by liver

78

Ifosfamide (4 uses)

Solid tumors
Leukemia
Lymphomas
Some brain cancers

79

Ifosfamide (2 side effects)

Hemorrhagic cystitis (C=C): prevented by Mesna (binds metabolite acrolein in bladder)
Myelosuppression

80

"-mustine" (mechanism and CNS penetration)

Nitrosoureas: carmustine, lomustine, semustine
Alkylating agent - X-links DNA
Requires bioactivation
Crosses BBB

81

"-mustine" (use)

Brain tumors (incl glioblastoma multiforme)

82

"-mustine" (side effect)

CNS toxicity (convulsions, dizziness, ataxia)

83

Streptozocin (mechanism and CNS penetration)

Nitrosourea too
Alkylating agent - X-links DNA
Requires bioactivation
Crosses BBB

84

Streptozocin (use)

Brain tumors (incl glioblastoma multiforme)

85

Streptozocin (side effect)

CNS toxicity (convulsions, dizziness, ataxia)

86

Busulfan (mechanism)

Alkylating agent - X-links DNA

87

Busulfan (2 uses)

CML
Ablate bone marrow before transplantation

88

Busulfan (3 side effects)

Severe myelosuppression
Pulmonary fibrosis
Hyperpigmentation

89

"Vin-" (mechanism)

Vincristine, vinblastine
Inhibits microtubule formation (M-phase specific)

90

"Vin-" (3 uses)

Solid tumors
Leukemias
Lymphomas

91

"Vin-" (3 side effects)

Vincristine: neurotoxicity (think of V being arms and legs and representing peripheral neuropathy), paralytic ileus
Vinblastine: myelosuppression

92

Paclitaxel and other taxols (mechanism)

Inhibits microtubule disassembly (M-phase specific) so anaphase can't occur

93

Paclitaxel and other taxols (2 uses)

Ovarian and breast carcinomas
Elution of coronary artery stents -> inhibits intimal hyperplasia -> prevents thrombosis and restenosis

94

Paclitaxel and other taxols (3 side effects)

Myelosuppression
Alopecia
Hypersensitivity

95

"-platin" (mechanism)

Cisplatin, carboplatin
X-link DNA

96

"-platin" (4 uses)

Testicular, bladder, ovary, lung carcinomas

97

"-platin" (2 side effects)

Nephrotoxicity (prevents w/ amifostine, which is a free radical scavenger, and chloride diuresis) (think of C for cysplatin and carboplatin being the shape of kidneys)
Acoustic nerve damage (think of C as ears)

98

"-poside" (mechanism)

Etoposide, teniposide
Inhibits topoisomerase II (S and G2 phase)

99

"-poside" (3 uses)

Solid tumors (esp testicular and small cell lung cancer)
Leukemias
Lymphomas

100

"-poside" (3 side effects)

Myelosuppression
GI irritation
Alopecia

101

"-tecan" (mechanism)

Irinotecan, topotecan
Inhibits topoisomerase I

102

"-tecan" (3 uses)

Colon cancer (irinotecan)
Ovarian cancer (topotecan)
Small cell lung cancer (topotecan)

103

"-tecan" (2 side effects)

Severe myelosuppression
Diarrhea

104

Hydroxyurea (mechanism)

Inhibits ribonucleotide reductase (S-phase specific)

105

Hydroxyurea (3 uses)

Melanoma
Myeloproliferative disorders: CML, PV (2nd line after phlebotomy)
Sickle cell disease (to increase HbF)

106

Hydroxyurea (2 side effects)

Bone marrow suppression
GI upset

107

"Predni-" (mechanism)

Prednisone, prednisolone
Glucocorticoids, trigger apoptosis (work on nondividing cells as well)

108

"Predni-" (2 categories of use)

Cancer (in combination regimen): CLL, non-Hodgkin lymphomas
Immunosuppression

109

"Predni-" (side effect)

Cushing-like sx (incl psychosis and peptic ulcers)

110

Trastuzumab (mechanism)

Monoclonal Ab against HER-2 (c-erbB2)

111

Trastuzumab (2 uses)

HER-2 positive breast cancer and gastric cancer

112

Trastuzumab (side effect)

Cardiotoxicity ("HEARTceptin" for Herceptin)

113

Imatinib (mechanism and 2 uses)

Tyrosine kinase inhibitor of bcr-abl (CML) and c-kit (GI stromal tumors)

114

Imatinib (side effect)

Fluid retention

115

Rituximab (mechanism)

Monoclonal Ab against CD20

116

Rituximab (3 uses)

Non-Hodgkin lymphoma (follicular lymphoma)
RA (w/ methotrexate)
ITP

117

Rituximab (side effect)

Increased risk of progressive multifocal leukoencephalopathy

118

Vemurafenib (mechanism)

Inhibits B-Raf kinase w/ V600E mutation

119

Vemurafenib (use)

Metastatic melanoma

120

Bevacizumab (mechanism)

Monoclonal Ab against VEGF (so inhibits angiogenesis)

121

Bevacizumab (4use)

Colorectal cancer
Metastatic renal cell carcinoma
Recurrent GBM
Metastatic NSCLC

122

Bevacizumab (2 side effects)

Hemorrhage
Impaired wound healing

123

Cyclosporin (mechanism)

Calcineurin inhibitor (binds cyclophilin and blocks T cell activation by preventing IL-2 TRANSCRIPTION)

124

Cyclosporin (3 uses)

Transplant rejection prophylaxis
Psoriasis
RA

125

Cyclosporin (side effects)

Nephrotoxicity
HTN, HLD, hyperglycemia
Tremor
Hirsutism (difference from tacrolimus)
Gingival hyperplasia (difference from tacrolimus)

126

Tacrolimus (mechanism)

Calcineurin inhibitor (binds FKBP and blocks T cell activation by preventing IL-2 TRANSCRIPTION)

127

Tacrolimus (use)

Transplant rejection prophylaxis

128

Tacrolimus (side effects)

Nephrotoxicity
HTN, HLD, hyperglycemia
Tremor
Increased risk of DM and neurotoxicity (difference from cyclosporin)

129

Sirolimus (Rapamycin) (mechanism)

mTOR inhibitor (binds FKBP like tacrolimus, blocks T cell activation and B cell differentiation by preventing IL-2 SIGNAL TRANSDUCTION)

130

Sirolimus (Rapamycin) (use)

Kidney transplant rejection prophylaxis

131

Sirolimus (Rapamycin) (side effects)

Not nephrotoxic (like tacrolimus)
Blood counts go down: anemia, thrombocytopenia, leukopenia
Insulin resistance, HLD

132

Basiliximab (mechanism)

Monoclonal Ab blocking IL-2R

133

Basiliximab (use)

Kidney transplant rejection prophylaxis

134

Basiliximab (3 side effects)

Edema
HTN
Tremor

135

Glucocorticoids (mechanism)

Inhibits NF-KB (suppresses both B and T fx by decreasing transcription of cytokines)

136

Glucocorticoids (2 uses)

Transplant rejection phophylaxis
Other autoimmune disorders and inflammation

137

Epoetin alfa (mechanism and use)

Erythropoietin
For anemia esp in renal failure

138

Oprelvekin (mechanism and use)

IL-11
For thrombocytopenia

139

Filgrastim (mechanism and use)

GC-SF
For recovery of bone marrow

140

Sargramostim (mechanism and use)

GMC-SF
For recovery of bone marrow

141

Aldesleukin (mechanism and 2 uses)

IL-2
For renal cell carcinoma, metastatic melanoma

142

Alemtuzumab (mechanism and use)

Ab against CD52 -> directly cytotoxic thru complement fixation and Ab-dependent, cell-mediated cytotoxicity
For CLL

143

Cetuximab (mechanism and 4 uses)

Ab against EGFR
For stage IV colorectal cancer, head and neck cancer, pancreatic cancer, NSCLC

144

Infliximab (mechanism and 4 uses)

Ab against TNF-a
For IBD, RA, ankylosing spondylitis, psoriasis

145

Adalimumab (mechanism and 4 uses)

Ab against TNF-a
For IBD, RA, ankylosing spondylitis, psoriasis

146

Natalizumab (mechanism)

Ab against alpha4-integrin (leukocyte adhesion impaired)

147

Natalizumab (2 uses)

MS, Crohn

148

Natalizumab (side effect)

Risk of PML in pts w/ JC virus

149

Denosumab (mechanism and use)

Ab against RANKL
For osteoporosis (inhibits osteoclast maturation by mimicking osteoprotegrin)

150

Omalizumab (mechanism and use)

Ab against IgE
For allergic asthma (prevents it from binding to FceRI)

151

Vemurafenib (mechanism and use)

BRAF kinase inhibitor
For melanoma w/ BRAF V600E mutation

152

Dexrazoxane (mechanism and use)

Iron-chelating agent
Used to prevent doxorubicin cardiotoxicity

153

OKT3 (mechanism and use)

Anti-CD3 (so anti T cells)
Used to reduce acute rejection of liver, heart, kidney

154

Argatroban (mechanism and use)

Direct thrombin inhibitor
Anti-clotting in pt that you can't use heparin or warfarin on (for fear of skin necrosis or HIT)

155

Bivalirudin and other hirudin derivatives (mechanism and use)

Direct thrombin inhibitor
Anti-clotting in pt that you can't use heparin or warfarin on (for fear of skin necrosis)

156

Aminocaproic acid (mechanism and 2 uses)

Blocks activation of plasminogen
Used as anidote for thrombolytics, and for disorder of fibrinolysis (radical prostatectomy and cirrhosis of liver)

157

Cladribine (2-CDA) (mechanism and use)

Purine analog resistant to degradation by adenosine deaminase
Penetrates CNS well, excreted in urine unchanged
DOC for hairy cell leukemia

158

Desmopressin acetate (DDAVP) (mechanism and 2 uses)

Stimulates endothelial cells (so release factor VIII and vWF)
Use in vWF disease and mild-moderate hemophilia A

159

Bortezomib (mechanism and 2 uses)

Proteasome inhibitor
For MM and Waldenstrom macroglobulinemia

160

Gardos channel blockers (mechanism and use)

Ca2+-dependent K+ channel blocker
Prevent intracellular dehydration -> reduces polymerization in sickle cell

161

Fludarabine (mechanism and use)

Deamination-resistant purine nucleotide analog
For CLL

162

Lepirudin (mechanism and use)

Direct thrombin inhibitor
Anti-clotting in pt that you can't use heparin or warfarin on (for fear of skin necrosis or HIT)