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Semestre 6: bloque 3 > Pharmacology week 2 > Flashcards

Pharmacology week 2 Flashcards

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1
Q

Antiplatelet use of aspirin

A

Inducer of platelet aggregation and vasoconstrictor

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2
Q

Mechanism of action of aspirin

A

Blocks production of TxA by acetylating a serine residue near active sites of platelet COX1

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3
Q

Thienopyridine prodrug

A

Clopidogrel

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4
Q

Mechanism of action of clopidogrel

A

Irreversible inhibitor of P2Y12

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5
Q

Polymorphism that affects metabolic activation of clopidogrel

A

CYP2C19

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6
Q

FDA indications for clopidogrel

A

Reduce rate of stroke, myocardial infarction, ischemic stroke, established peripheral artery disease, acute coronary syndrome

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7
Q

Adverse effects of clopidogrel

A

Increases risk of bleeding

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8
Q

Drug interactions of clopidogrel

A

CYP2C19 inhibition by PPIs: reduces conversion to active metabolite of clopidogrel
CYP2C19 inducers and opioids: decreases exposure to clopidogrel
Anticoagulants, NSAIDs, antidepressants: increases risk of bleeding

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9
Q

Adverse effect of glycoprotein IIb/IIIa inhibitors

A

Bleeding

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10
Q

Therapeutic use of glycoprotein IIb/IIIa inhibitors

A

Px undergoing percutaneous coronary intervention

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11
Q

Fab fragment of humanized monoclonal antibody directed vs aIIIbB3 receptor

A

Abciximab

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12
Q

Cyclic peptide inhibitor of fibrinogen binding site on aIIIbB3

A

Eptifibatide

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13
Q

Nonpeptide, small molecule inhibitor of aIIIbB3

A

Tirofiban

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14
Q

Mechanism of action of heparin

A

Activates antithrombin → inhibits factor IIa (thrombin) and factor Xa (both part of common coagulation cascade)

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15
Q

Anticoagulant of choice for pregnant women

A

Heparin

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16
Q

How is therapy with heparin monitored

A

Measuring aPPT (increased)

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17
Q

Adverse effect of heparin

A

Heparin induced thrombocytopenia due to anti PF4

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18
Q

Role of platelet factor 4 in heparin

A

Binds to heparin and prevents it from interacting with antithrombin
Limit activity of heparin in vicinity of platelet-rich thrombi

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19
Q

Antidote for heparin induced hemorrhage

A

IV protamine sulfate infusion

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20
Q

Contraindications for heparin

A

Px with creatinine <30 mL/min

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21
Q

Low molecular weight heparin drugs

A

Enoxaparin and nadroparin

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22
Q

Clinical use of enoxaparin

A

Out-of-hospital management of px with deep vein thrombosis or pulmonary embolism

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23
Q

True or false: enoxaparin and fondaparinux have shorter lives than heparin

A

False: they have longer half lives as well as lower affinity to PF4

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24
Q

Synthetic drug with similar characteristics to heparin

A

Fondaparinux

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25
Target factor for fondaparinux
Factor Xa
26
What is the main difference between warfarin and acenocoumarol
Acenocoumarol has a shorter half live
27
Mechanism of action of warfarin
Inhibition of vitamin K epoxide reductase (VKOR)
28
Coagulation factors affected by warfarin
Factors II, VII, IX, X and proteins C and S
29
True or false: Warfarin has no effect on activity of fully y-carboxylated factors already in circulation
True: this is why it has a delayed onset of action (4-5 days)
30
How are vitamin K dependent factors activated
Glu residues are y-carboxylated to form the Ca-binding Gla domain
31
Hypersensitivity variants of warfarin
Variants to CYP2C9: affect pharmacokinetics Variants to VKORC1: affect pharmacodynamics
32
Adverse effects of warfarin
Bleeding Birth defects Skin necrosis Purple toe syndrome Fatal calciphylaxis
33
Examples of direct oral Xa factor inhibitors
Rivaroxaban, apixaban, edoxaban, betrixaban
34
Mechanism of action of direct oral Xa factor inhibitors
Inhibit free and clot-associated factor Xa → reduced thrombin generation
35
Bioavailability of rivaroxaban, apixaban, edoxaban
Rivaroxaban → 80% bioavailability Apixaban → 50% bioavailability Edoxaban → 62% bioavailability
36
Therapeutic uses of direct oral Xa factor inhibitors
Stroke prevention in px with atrial fibrillation and tx of acute deep vein thrombosis or pulmonary embolism
37
Contraindications for direct oral Xa factor inhibitors
Contraindicated in px with mechanical heart valves Should be avoided in px with antiphospholipid sx
38
Drug interactions with direct oral Xa factor inhibitors
Substrates for P-glycoprotein
39
Tissue plasminogen activators
Alteplase Streptokinase Tenecteplase
40
Mechanism of action of alteplase
When bound to fibrin, alteplase activates fibrin-bound plasminogen several 100x more rapidly than it activates plasminogen in circulation
41
Therapeutic uses of alteplase
Acute myocardial infarction Acute ischemic stroke Life-threatening pulmonary embolism
42
Difference between alteplase and tenecteplase
Tenecteplase has longer plasma half lives than alteplase and is more resistant to inhibition by PAI-1
43
Contraindications for the use of alteplase
Prior intracranial hemorrhage Known structural cerebral vascular lesion Malignant intracranial neoplasm Ischemic stroke within 3 months Suspected aortic dissection
44
Inhibitors of fibrinolysis
Aminocaproic acid and tranexamic acid
45
Mechanism of action of aminocaproic acid and tranexamic acid
Competes for binding sites of plasminogen and plasmin → blocks interaction with fibrin → inhibits fibrinolysis
46
Therapeutic use of aminocaproic acid
IV: reduce bleeding after prostatic cx Oral: reduce bleeding after tooth extractions in px with hemophilia
47
Therapeutic uses of tranexamic acid
IV: trauma resuscitation, px with massive hemorrhage, women with postpartum hemorrhage and to reduce operative bleeding in px undergoing hip or knee arthroplasty or cardiac cx
48
Mechanism of action of aprotinin
Inhibit serine proteases (plasmin, kallikrein, trypsin) → reduced fibrinolysis and intrinsic pathway activation, decreased preservation of platelet function, decreased inflammation (kallikrein)
49
Contraindications for aprotinin use
Do not give to px with DIC
50
Where is vitamin K found
Phytonadione (K1) → plants Menaquinones (K2) → gram (+) bacteria
51
Only natural vitamin K available for therapeutic use
Phytonadione (vitamin K1)
52
Pharmacological actions of phytonadione
Promote biosynthesis of factors II, VII, IX, X and anticoagulant proteins C and S
53
Major clinical manifestation of vitamin K deficiency
Bleeding
54
Adverse effects of Menadione (vitamin K2)
Hemolytic anemia and kernicterus in neonates
55
Therapeutic uses of phytonadione
Correct bleeding tendency or hemorrhage associated with its deficiency
56
Why is hypopothrombinemia of the newborn caused
Healthy newborn infants have decreased plasma concentrations of vitamin-K dependent factors for few days after birth
57
Enhances expression of multiple hypoxia-induced genes like vascular endothelial growth factor and erythropoietin
HIF (hypoxia-inducible factor)
58
Where is erythropoietin produced
Peritubular interstitial cells of kidney
59
Pharmacological drug nearly identical to erythropoietin
Epoetin alfa
60
Erythropoiesis-stimulating peptide for tx of anemia due to chronic kidney disease
Peginesatide
61
Therapeutic use of epoetin alfa
Anemias
62
FDA black box warning for epoetin alfa
Should not be used to increase Hb concentrations >11 g/dL --> heart risks
63
Fun fact! Competitive athletes have used epoetin alfa as blood doping to improve their performance
.
64
Mechanism of action of methenolone
Androgen receptor binding → promote protein synthesis, muscle growth, erythropoiesis and nitrogen retention
65
Therapeutic uses of methenolone
Tx of catabolic states: chronic illness, surgery, trauma Muscle-wasting diseases Support in long-term corticosteroid therapy Osteoporosis
66
Adverse effects of methenolone use
Androgenic → acne, oily skin, hair loss, voice deepening or hirsutism in women, suppressing natural testosterone production Low HDL and high LDL
67
Treatment of choice for iron deficiency
Ferrous sulfate (oral administration)
68
Adverse effects of ferrous sulfate
Heartburn, nausea, upper gastric discomfort, diarrhea, constipation
69
Treatment for iron poisoning
Deferoxamine
70
Oral iron chelators for tx of px with thalassemia with iron overload
Deferiprone and deferasirox
71
Indications for parenteral iron administration
Iron malabsorption, oral iron intolerance, routine supplement to total parenteral nutrition, px receiving erythropoietin
72
Parenteral iron with lowest anaphylaxis risk
Iron sucrose
73
Parenteral iron with highest anaphylaxis risk
Iron dextran
74
What is the source of vitamin B12
Moo that grow in soil or intestinal lumen of animals that synthesize vitamin
75
Types of preparations of vitamin B12
Cyanocobalamin or hydroxocobalamin
76
Metabolic functions of vitamin B12
Methionine synthase Methylmalonyl-CoA mutase Folate regeneration
77
Where is vitamin B12 absorbed
Ileum
78
Role of transcobalamin
Transport vitamin B12 to tissues
79
Recommended daily intake of vitamin B12
2.4 ug
80
Causes of megaloblastic anemia
Vitamin B12 or folate deficiency
81
What does the Schilling test evaluate
Measure absorption of vitamin B12
82
Complications of vitamin B12 deficiency
Peripheral neuropathy
83
Treatment of choice for vitamin B12 deficiency
Cyanocobalamin IM or subcutaneous 100 mg every 4 weeks NEVER IV!!
84
Common pharmaceutical form of folic acid
Pteroylglutamic acid
85
Folic acid roles in metabolism
Conversion homocysteine to methionine Conversion serine to glycine Synthesis of thymidylate Histidine metabolism Synthesis of purines
86
Source of folic acid
Food sources → fresh green vegetables, liver, yeast, some fruit
87
Recommended daily intake of folic acid
400 ug
88
Sensitive marker of folic acid deficiency
Serum homocysteine

Semestre 6: bloque 3 (6 decks)

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