Heme - FA Pharm p427 - 436 Flashcards

1
Q

MoA of Heparin

A

Activates antithrombin, which dec action of IIa (thrombin) and factor Xa.

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

Why is Heparin safe for use in pregnancy?

A

Doesn’t cross placenta

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

How do you test for Heparin fxn?

A

PTT

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

name 3 low molecular weight heparins? MoA?

A

enoxaparin, dalteparin, fondaparinux

Acts predominantly on FXa

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

5 clinical applications of heparin?

A
  1. immediate anticoagulant for PE 2. acute coronary syndrome 3. MI 4. DVT 5. for pregnancy (does not cross placenta)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what are the 5 characteristics of fondaparinux?

A
  1. act more on factor Xa 2. better bioavailability 3. 2-4 times longer half life 4. can be administered subcutaneously without lab monitoring 5. not easily reversible
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

In HIT, what is the pathomech?

A

development of IgG antibodies against heparin bound platelet factor 4 (PF4).

Antibody-heparin-PF4 complex activates platelets –> thrombosis and thrombocytopenia.

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

Ex of direct thrombin inhibitors

A

Bivalirudin, Argatroban, Dabigatran

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

When do we use direct thrombin inhibitors

A

Venous thromboembolism, atrial fibrillation. Can be used in HIT, when heparin is BAD for the patient

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

How to reverse dabigatran?

What if not avail?

A

idarucizumab to reverse dabigatran

Consider PCC and/or antifibrinolytics (eg, tranexamic acid) if no reversal agent available.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what is heparin bridging?

A

heparin is used when starting warfarin which causes transient hypercoagulable state.

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

initial heparin therapy with warfarin reduces risk of

A

recurrent venous thromboembolism and skin/tissue necrosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

in warfarin toxicity, what causes the skin/tissue necrosis?

A

small vessel microthromboses

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

what gene polymorphism can affect the efficacy of warfarin?

A

VKORC1 (vit K epxoide reductase complex)

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

DOC for DVT/PE prophylaxis?

A

apixaban, rivaroxaban

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

treatment for CLL?

A

anti-CD52 (alemtuzumab)

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

treatment for hairy cell leukemia

A

cladribine (adenosine analog, 2CDA), pentostatin

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

explain the mech of thrombolytics

A

directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibirn clots

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

what are the 3 clinical applications for thrombolytics?

A
  1. early MI 2. early ischemic stroke 3. direct thrombolysis of severe PE
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what are the 5 contraindications with thrombolytics?

A
  1. active bleeding 2. hx of intracranial bleeding 3. recent surgery 4. known bleeding diatheses (hypocoagulable) 5. severe HPT
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

what is the antidote for thrombolytics?

A
aminocaproic acid (antifibrinolytics)
platelet transfusions

FFP/PCC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Common side effect of ADP receptor blockers?

What SE is unique to Ticlopidine?

A

TTP

neutropenia

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

monoclonal Ab against GP IIb/IIIa?

A

AbCIXimab (2 times 3 = six)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Name other GpIIb/IIIa (-)’rs

A

Eptifibatide
Tirofiban
Lomifiban
Orbofiban

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Uses of GpIIb/IIIa (-)’rs

A

unstable angina
percutaneous coronary intervention

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

MoA of Cilostazol/Dipyridamole

A

Inc cAMP in platelets –> (-)’n of platelet aggregation

vasodilate ( by (-) Myosin light chain kinase)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Uses of Cilostazol/Dipyridamole

A

1) Intermittent claudication (Periph vascular disease) 2) Prevention of Stroke/transient ischemic attacks

Dipyridamole - also used for cardiac stress testing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

SE of Cilostazol/Dipyridamole

A

Nausea, headache, facial flushing, hypotension, abdominal pain.

29
Q

What is the only G2 phase antineoplastic drug and its MOA?

A

Bleomycin: (+) free radicals, causes DNA strand breakage in tumor cells

30
Q

Adverse effects of Bleomycin

A

pulmonary fibrosis, skin hyperpigmentation

31
Q

Drugs that cause pulmonary fibrosis

A

Methotrexate,
Nitrofurantoin,
Bleomycin,
Busulfan,
Amiodarone

32
Q

List 4 drugs that inhibit nucleotide synthesis and their mechanism -

A

MTX, 5-FU:
dec thymidine synthesis
6-MP:
dec de novo purine synthesis

Hydroxyurea:
inhibits ribonucleotide
reductase

33
Q

4 cancer drugs that (-) microtubule formation

A

Paclitaxel
Vinblastine
Vincristine
Eribulin - breast cancer rx

34
Q

Name the antineoplastic drug which causes BMS with megaloblastic anemia, and the cancer against it is used? MoA?

A

Cytarabrine used for AML and lymphomas

pyrimidine analogue - DNA chain termination, (-) DNA polymerase

35
Q

Name the antineoplastic drug which causes pancytopenia, and the cancer against it is used? MoA?

A

Cytarabrine used for AML and lymphomas

pyrimidine analogue - DNA chain termination, (-) DNA polymerase

36
Q

Name the cancer drug and its metabolite which is contraindicated in gout therapy? Why?

A

Azathioprine gets metabolized into 6-Mercaptopurine and both are metabolized by Xanthin oxidase. Allopurinol/ Febuxostat increase 6-MP levels leading to GI and liver tox

37
Q

Name the cancer drug and MOA that treats abnormal B cells with hair like projections which stain for tartarate resistant acid phosphatase?

A

Cladribine (2-CDA) is a purine analog which inhibits DNA polymerase and causes DNA strand breakage

DOC for Hairy Cell Leukemia

38
Q

T5-FU can be used topically for ____ cancer? MOA please

A

5 Fluorouracil used for Basal cell carcinoma

MOA: 5FU acts as a pyrimidine analog and inhibits thymidylate synthase by converting into a suicide inhibitor 5F-dUMP

39
Q

Indication (4) of methotrexate and MOA?

A

MOA: MTX inhibits Dihydrofolate Reductase which indirectly inhibits Thymidylate Synthase

1) MTX treats cancers such as ALL, lymphoma, choricarcinoma,sarcomas
2) Ectopic pregnancy/ Abortion(w/ PGE2 analog)
3) Psoriatic & Rheumatoid Arthritis
4) Tx for Vasculitis
5) IBD

40
Q

How to recover from the BMS due to MTX? How is this different from 5-FU?

A

MTX inhibits folate production which can be replenished by leucovorin (Folate analog)

BUT 5-FU forms suicide inhibitor 5F-dUMP (covalent bond with folic acid) and can’t be replenished by leucovorin

41
Q

This anticancer drug is used for many childhood cancers. Name drug, MOA, and 3 cancers it treats?

A

Actinomycin D (dactinomycin): intercalates in DNA , (-) RNA synthesis

Cancers

Tx for: 1) Wilms tumor 2) Ewing sarcoma 3) Rhabdomyosarcoma

42
Q

This antineoplastic has adverse effects to the heart?Name the drug, the toxicity it causes, and the antidote to it?

A

Doxorubicin/Danorubicin leads to Dilated Cardiomyopathy (DCM)

Cardiotoxicity can be prevented by DEXRAZOXANE (Iron chelator)

43
Q

MoA of doxo/daunorubicin?

A

Generate free radicals.
Intercalate in DNA –> breaks in DNA –> dec replication.
Interferes with topoisomerase II
enzyme.

44
Q

Name 3 cancer drugs that cause pulmonary fibrosis

A

MTX, Busulfan, Bleomycin

45
Q

Myelosuppression is a detrimental side effect of antineoplastic therapy. This famous Hodgkin’s Disease drug causes very little bone marrow suppression?

A

Bleomycin

46
Q

This alkylating agent has a specific site of cross linking DNA, and require activation? Name the drug, site of crosslinking, and where is it activated?

A

Cyclophosphamide: crosslinks DNA on the Guanine at the N-7 position. It needs to be bioactivated by the liver.

47
Q

A 55 yr old lymphoma pt is started on an alkylating agent. A week later he starts complaining of blood in his urine? Name the Dx, and the metabolite of this drug that caused it? How could this have been prevented?

A

The pt has hemorrhagic cystitis caused by the Cyclophosphamide. Cyclophosphamide gets converted into the toxic metabolite Acrolyn and could have been prevented by administering Mesna

48
Q

Which anticancer drug can cross BBB and is therefore useful to treat CNS tumors? MoA?

A

Nitrosoureas (carmustine, lomustine) can pass the BBB. - cross links DNA

Can be used for CNS tumors such as Glioblastoma multiforme

49
Q

These drugs hyperstabilize polymerized microtubules in M phase - Which cancers are they used for?

A

Taxanes like paclitaxel are indicated for ovarian and breast tumors

50
Q

These drugs inhibit microtubule polymerization. Name the two antineoplastics and the cancers they are used for?

A

Solid tumors, leukemias,
Hodgkin and non-Hodgkin
lymphomas.

51
Q

How can the Platin caused nephrotoxicity be prevented?

A

Chloride saline diuresis w/ administeration of Amifostine (free radical scavenger)

52
Q

The (-tecan) group of drugs mingle with the unwinding of the DNA in tumor cells causing cell cycle arrest. Name the topisomerase inhibited, and two examples with the cancers they treat?

A

Topoisomerase I is inhibited 1) Irinotecan treats Colon Cancer 2) Topotecan treats Ovarian and sm CC of the lung

53
Q

MOA of the topside drugs and indications

A

Etoposide inhibits topoisomerase II

Etwoposide

Used in Tx of: 1) Testicular cancer 2) Sm CC of Lung 3) Leukemia/Lymphoma

54
Q

This S phase specific antineoplastic drug can be beneficial to Sickle Cell patients? Name the drug and how does it help them?

A

Hydroxyurea inhibits Ribonucelotide Reductase

Used in Myeloproliferative disorders - CML, PCV

Promotes formation of HbF molecules in SCA pts who are suffering from crisis symptoms of dactylitis

55
Q

What are the 2 most commonly used glucocorticoids in cancer chemotherapy?

A

Prednisone, prednisolone

56
Q

Diabetic retinopathy is treated with what Monoclonal antibody?

A

Bevacizumab -> anti- VEGF

57
Q

Tx of Adenocarcinoma of the lung and MOA?

A

Erlotinib: EGFR tyrosine kinase inhibitor

any non small cell lung cancer

58
Q

Rituximab inhibits which CD?

A

CD20

Rituximab = Re2Ximab XX = 20 in latin

59
Q

Pt that has been treated with BCR-ABL mutation presents with edema, what was the Tx?

A

Imatinib, dasatinib - Fluid retention.

60
Q

What drug would you use to treat a 68 year old female with breast ca?

A

Not a SERM, used primarily in pre-menopausal women ( estrogen levels)

In post menopausal women, we tend to use aromatase inhibitors - anastrozole, letrozole and exemestane

61
Q

HER-2 (c-erbB2) is what kind of receptor?

A

tyrosine kinase receptor

62
Q

Which Tx blocks the binding of estrogen to ER ⊕ cells?

A

(SERMs)—receptor antagonists in breast

63
Q

Tx and MOA that treats Metastatic melanoma?

Given with what other class of rx?

A

Vemurafenib/Dabrafenib

Small molecule inhibitor of BRAF oncogene ⊕ melanoma

VEmuRAF-enib is for V600Emutated
BRAF inhibition.

With MEK inhibitors - Trametinib

64
Q

Pt undergoing Tx for B-cell neoplastic presents with nonenhancing areas of demyelination on MRI. What was the Tx that caused this?

A

Rituximab due to developement of progressive multifocal leukoencephalopathy

(Natalizumab also)

65
Q

Toxicity of Herceptin?

A

Cardiotoxicity

(Brand name of Trastuzumab)

66
Q

SE: of EGFR tyrosine kinase inhibitor?

A

rash, photosen.

67
Q

(SERMs)—receptor antagonists of the breast causes an incr risk of endometrial cancer?

A

Tamoxifen

68
Q

This drugs SE are similar to a dz that is caused by shistosomiasis?

A

CYclophosphamide–> hemorrhagic cystitis

69
Q

Pt in chemotherapy acquires hearing loss, what was the Tx?

A

Cisplatin/Carboplatin