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Year 2 Unit 2 > Drugs To Treat Clotting Disorders > Flashcards

Drugs To Treat Clotting Disorders Flashcards

1
Q

Drugs that decrease clotting

A

Anticoagulants
Antiplatelet drugs
Thrombocytes

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2
Q

Systemic coagulants

A 
Vitamin K
Replacement factors 
Aminocaproic acid (Fibrinogen conc., prothrombin complex conc.)
Tranexamic acid
DOAC antidotes
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3
Q

DOACs and their antidotes

A

Direct oral anticoagulants:

  • Dabigatran (direct thrombin inhibitor)
  • -> idarucizumab (Praxbind)
  • rivaroxoban, apixaban, edoxaban (direct Xa inhibitors)
  • Warfarin toxicity
  • ->vit k
  • Heparin
  • -> protamine sulfate
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4
Q

Anticoagulants

A

Inhibit formation of arterial and venous fibrin clots

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5
Q

Vitamin E Epoxide Reductase Inhibitor

A

Warfarin

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6
Q

Indirect Thrombin Inhibitors

A

Heparin (unfractionated)

LMWH

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7
Q

Low Molecular Weight Heparin

A

Enoxaparin
Dalteparin
Tinzaparin (off market in 2011)

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8
Q

Direct Thrombin Inhibitors (DTI)

A

Dabigatran
Argobatran
Bivalirudin
Desirudin

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9
Q

Direct Xa inhibitors

A

-all oral
Rivaroxoban
Apixaban
Edoxaban

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10
Q

Indirect Xa inhibitors

A

-antithrombin II or III mediated inhibition of Xa
Fondaparinux (injectable)
Indraparinux (longer acting, withdrawn from market)

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11
Q

Antiplatelet agents

A

Inhibition of platelet aggregation

Important in pathological artery occlusion

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12
Q

COX inhibitors

A

Aspirin

Others exist but none indicated by FDA for clotting disorders

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13
Q

Platelet P2Y12 receptor antagonists

ADP inhibitors

A 
Cangrelor 
Clopidogrel 
Prasugrel 
Ticagrelor 
Ticlopidine HCl
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14
Q

PDE/Adenosine uptake inhibitors

A

Dipyridamole

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15
Q

Glycoprotein IIb/IIIa inhibitors

A

Abciximab
Eptifibatide
Tirofiban HCl

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16
Q

Thrombolytics

A

Tx of arterial or venous thrombi (after formed)

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17
Q

Plasminogen activators

A

Alteplase recombinant
Reteplase recombinant
Tenecteplase recombinant

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18
Q

Thrombolytic enzyme

A

Urokinase

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19
Q

Human protein C

A

Protein C Conc. (Human)

- used in severe congenital protein C deficiency

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20
Q

Common coagulation studies

A

PT, aPTT, INR
Used to diagnose coagulation abnormalities or monitor effectiveness of anticoagulantion therapy
- when used to assess drug therapy, achieving a value outside the reference range is therapeutically desirable

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21
Q

aPTT

A

Activated patient thromboplastin time

  • measures the intrinsic clotting system
    • Factors VII, IX, XI, and XII, and factors in common pathway (II, X, V)
  • used to monitor unfractionated heparin therapy
  • reference range 20-39s
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22
Q

PT

A

Prothrombin Time

  • directly measures activity of clotting factors VII and X, prothrombin (Factor II), and Fibrinogen
  • reference range 10-14s
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23
Q

International Normalized Ratio

A
  • Recommended method to monitor anticoagulant therapy
  • Variable sensitivity of thromboplastin reagents to decreases in specific clotting factors causes a lack of reliability when used at onset of warfarin therapy and in screening for a coagulopathy
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24
Q

ACT

A

Activated Clotting Time

  • used before, during, after medical procedures that require blood clotting to be suppressed
  • measures the immediate effect of heparin but not the level of heparin
  • sometimes DTI
  • “bedside coagulation monitoring”
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25
Q

How is warfarin supplied

A

Oral tablets

-iv discontinued and off market

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26
Q

Warfarin mech of action

A

Vitamin k Reductase inhibitor, leads to depletion of vit k dependent clotting factors
- II (60h), VII (6h), IX (24h), X (40h), protein C, protein S

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27
Q

Bridge therapy

A
  • Administration of short acting anticoagulant (LMWH, Unfractionated Heparin) while long acting anticoagulant (warfarin) is withheld before surgery
  • Subsequently given after surgery as well until long acting anticoagulant is in target therapeutic range
  • also applies to new start long acting anticoagulant therapy
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28
Q

Indications for warfarin

A
  • MI: STEMI, afib, CHADS2>/=2, mechanical valve, VTE, hypercoagulable disorder
  • Thromboembolic complications prevention and/or tx assoc. w afib and/or cardiac valve replacement
  • Venous Thrombosis/PE
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29
Q

Warfarin Dosing

A
  • 3 ranges of expected MD depending on combination of VKORC1 and CYP2C9 genotype
  • traditional means of coumadinization where pt takes 2-5mg daily
  • LD of 10mg for 2 days sometimes used, but not recommended for elderly or pts recovering from Heparin induced thrombocytopenia (HIT)
  • css in ~5 days
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30
Q

Warfarin Absorption

A

Completely absorbed after oral admin. W peak conc. Generally attained within first 4 hours

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31
Q

Warfarin Distribution

A
  • relatively small - 0.14L/kg
  • dist. Phase lasting 6 to 12h after oral admin. of aq soln.
  • ~99% bound to plasma proteins
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32
Q

Warfarin Metabolism

A
  • Metabolized by CYP450 enzymes to hydroxylated metabolites and by reductases to warfarin alcohols
  • inhibits VKOR, which reduces regen. Of vit k from vit k Epoxide
  • polymorphs in VKORC1 gene associated w variable warfarin dose requirements
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33
Q

Warfarin Excretion

A
  • terminal half life @ ~1 week
  • effective half life ranges from 20-60h, mean 40h
  • urinary excretion as metabolites
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34
Q

Warfarin duration of therapy

A

Indication dependent

  • indefinitely: afib, >2 documented DVTs or PE
  • 3 months: ant. MI w LV thrombus, high risk for LV thrombus, bioprosthetic valves in mitral position
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35
Q

Warfarin for the elderly

A

Lower initiation and MD recommended

“Start low and go slow”

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36
Q

Warfarin w renal impairments

A

No dosage adjustment necessary

Incr. risk of bleeding complications

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37
Q

Warfarin w hepatic impairment

A

Response to oral anticoagulants may be markedly enhanced in obstructive jaundice, hepatitis, cirrhosis
INR should be monitored closely

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38
Q

Warfarin w Asian patients

A

May require lower initiation and MD

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39
Q

Warfarin monitoring

A
  • Daily INR monitoring until pt in therapeutic range
  • periodic INR monitoring during maintenance (every 1-4 weeks), plus after exchange of products, when other meds are initiated, discontinued, or taken irregularly
  • PT, hct, INR, consider genotyping prior to therapy
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40
Q

Warfarin common ADRs

A
  • minor and major bleeding episodes
  • dermatological rxns
  • hypersensitivity
  • chills, vasculitis
  • tracheal/ tracheobronchial calcification
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41
Q

Warfarin antidote

A

Vit K injection (phytonadione)

  • indicated in coagulation disorders due to faulty factor II, VII, IX, X formation when caused by vit k deficiency or interference w vit k activity
    • anticoagulant induced prothrombin deficiency, hemorrhagic diseases of the newborn, hypoprothrombinemia
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42
Q

Warfarin food interactions

A
  • Anticoagulant effects may be decreased if taken with foods rich in vit k
  • vit E may increase warfarin effect
  • Cranberry juice may increase warfarin effect
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43
Q

Warfarin contraindications

A
  • pregnancy, hemorrhagic tendencies, malignant hypertension, known hypersensitivity
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44
Q

Warfarin Use in pregnancy

A

Category D: contraindicated except in pregnant women with mechanical heart valves at high risk of thromboembolism

  • risk of teratogenicity
  • crosses the placenta, concentrations in fetal plasma similar to maternal, teratogenic effects may include Coumadin embryopathy
  • LMWH generally used if necessary
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45
Q

An I coagulant/DTIs

A 
Unfractionated heparin (UFH, high molecular weight)
LMWHs: enoxaparin (lovenox), Dalteparin (fragmin), tinzeparin (off market)
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46
Q

UFH supply

A

Injection of widely varied strengths

  • used for anticoagulation
  • used to maintain latency of IV devices
  • not to be used for systemic anticoagulant therapy (heparin lock flush soln.)
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47
Q

UFH mechanism of action

A
  • binds to antithrombin III via its pentasaccharide sequence
    • inhibits factor Xa, which normally activate thrombin
  • large enough to simultaneously bind antithrombin and thrombin III
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48
Q

LMWH mechanism of action

A

Pentasaccharide sequence bind antithrombin III, potentiating factor Xa inhibition
- cannot simultaneously bind thrombin

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49
Q

Fondaparinux mechanism of action

A

Classified as an indirect Xa inhibitor

- synthetic pentasaccharide which accelerates only factor Xa inhibition by potentiating of antithrombin III

50
Q

UFH indications

A
  • prophylaxis and tx of thromboembolic disorders
  • off label: interstitial cystitis, STEMI as adjuncts to fibrinolytic tx
  • unstable angina and non STEMI
  • Anticoagulant during percutaneous coronary intervention
  • following DVT, PE, superficial vein thrombosis, pts w afib undergoing cardioversion, nonbacterial thrombotic endocarditis and systemic or pulmonary emboli, cerebral venous sinus thrombosis, acute arterial emboli or thrombosis
51
Q

UHF administration

A
  • can be given SC, by cont. iv, by heparin lock
  • do not give IM
  • CVCs must be flushed w heparin soln when inserted, daily, and after blood withdrawal or transfusion, and after infusion w injectable cap
52
Q

UFH absorption

A

Oral, rectal: erratic at best

Subcutaneous: also erratic, but acceptable for prophylaxis

53
Q

UFH metabolism

A

Hepatic, may be partially metabolized in the reticuloendothelial system

54
Q

UFH excretion

A

Urine (small amts as unchanged drug)

Half life eliminate: short and affected by various conditions

55
Q

UFH time to onset

A

IV: immediate
SC: ~20-30m

56
Q

UFH special pops

A

Renal function impairment: half life may be increased
Hepatic function impairment: half life may be incr. or decr.
Elderly: plasma levels may be higher

57
Q

UFH monitoring

A
  • aPTT/ antifactor Xa activity levels, ACT when high dose heparin w procedures where clotting is suppressed
  • platelet counts when HIT risk
58
Q

Common UFH ADRs

A
  • Heparin Induced thrombocytopenia (HIT)
  • Hypersensitivity
  • Local rxns: erythema, hematoma, irritation, pain, ulceration
  • Misc.: cutaneous necrosis, delayed transient alone is, osteoporosis
  • elevations of ALT and AST
59
Q

Heparin Induced Thrombocytopenia

A

Drug induced immunologic rxn

  • incidence of 1-2%
  • leading complication is thromboembolism
  • type 1: presents 2d post admin, then platelet count normalizes
  • type2: 4-10d and can cause life threatening thrombotic event
  • skin lesions, chills, fever, dispensing and chest pain after IV
  • Probability det. by 4 Ts
60
Q

Management of HIT

A
  • discontinue heparin, replace w anticoagulant that doesn’t cause HIT (bivalirudin, argatroban, fondaparinux)
  • renal insuff.–> argatroban
  • hepatic impairment –> fondaparinux
  • both–> low dose argatroban or bivalirudin
61
Q

Transition to warfarin post HIT

A
  • do not use as initial anticoagulant after HIT, may increase risk of gangrene by rapid lowering of protein C
  • should be started only after:
    • pt is antioagulated w alternative anticoagulant
    • platelet count of at least 150k/microL
  • min 5 days overlapping therapy
62
Q

UFH hypersensitivity

A

Heparin are porcine products

Fondaparinux is synthetic w lower risk of hypersensitivity

63
Q

UFH antidote

A

Protamine Sulfate

  • binds to long part of heparin molecules, neutralizes
    • only partially works on LMWHs
  • minimal dose should be used to avoid anticoagulant effects: 1mg for every 100 units heparin
64
Q

UFH in pregnancy

A

Category C: does not cross placenta. May be used for prevention and tx of TE in pregnancy, but LMWH is preferred

65
Q

LMWHs

A

Enoxaparin, Dalteparin

66
Q

LMWH metabolism/excretion

A
  • primarily metabolized in the liver by desulfurization and/depolymerization
  • total renal clearance of active and inactive enoxaparin fragments represents 40% of the dose, w 10% active fragments
67
Q

Dalteparin special pop

A

Pts w chronic renal insuff requiring hemodialysis–> expect greater accumulation

68
Q

Enoxaparin special pop

A
  • Renal insuff: antifactor Xa exposure @css marginally increased in mild and moderate renal insuff, significant in severe renal insuff.
  • elderly: antifactor Xa exposure 15% greater @ day 10 than day 1
  • weight: antifactor Xa exposure increased in low weight pts
69
Q

LMWH monitoring

A
  • periodic CBC incl. platelet count and hct or hgb
  • closely monitor Thrombocytopenia
  • no special blood clotting time monitoring needed
  • monitor for signs of bleeding in pts w low body weigh, risk for renal disfunction, pregnancy
  • monitor for thromboembolism in obese pts
70
Q

LMWH in pregnancy

A

Category B: does not cross placenta, fetal bleeding or teratogenicity not reported
- recommended over UFH for treatment of acute VTE in pregnancy

71
Q

LMWH and UFH interactions

A
  • avoid combination w other anticoagulants and antiplatelet agents, may enhance effect (apixaban, Dabigatran)
  • Other agents w antiplatelet properties: clopidogrel, NSAIDs, SSRIs
  • hormones can increase coagulopathy risk and diminish efficacy
  • vit E, herbals, supplements can increase risk of bleeding
72
Q

LMWH and UFH contraindications

A
  • hypersensitivity to LMWHs, heparin a, pork products, or any component of the formulation
  • active major bleeding
  • epidural or spinal hematoma so may occur in pts who are anticoagulated w LMWHs or heparinoids and are receiving neuraxial anesthesia or undergoing spinal puncture
73
Q

Direct Thrombin Inhibitors

A

Dabigatran (Pradaxa) - PO
Argatroban - IV
Bivalirudin (Angiomax) - IV
Desirudin (Ipravask) - SC

74
Q

Direct Factor Xa inhibitors

A

Rivaroxoban (Xarelto) - PO
Apixaban (Eliquis) - PO
Edoxaban (Savaysa) - PO

75
Q

Indirect Factor Xa inhibitors

A

Fondaparinux (Arixtra) - IV

  • accelerates only factor Xa inhibition by antithrombin
  • lower HIT risk compared to LMWHs,higher bleed risk
76
Q

DTI monitoring

A
  • monitor for symptoms of blood loss
  • aPTT is generally used, but dose response is not linear and reaches a plateau
  • INR increased by all DTIs (variably)
  • aPTT more than 2.5 may indicate over anticoagulation
  • monitor renal function
77
Q

DTI common ADRs

A
  • Bleeding is major adverse effect
  • hemorrhage may occur at virtually any site
    • risk dependent on multiple variables: intensity of anticoagulation, concurrent use of a glycoproteins IIb/IIIa inhibitor (bivalirudin), and pt susceptibility
78
Q

DTIs drug interactions

A

Dabigatran is a substrate of P-glycoprotein

G-protein inhibitors would decrease absorption

79
Q

DTIs contraindications

A
  • Hypersensitivity to active ingredients
  • active major bleeding
  • Mechanical prosthetic heart valve (Dabigatran only)
80
Q

DTIs in pregnancy

A 
Category B: argatroban, bivalirudin 
Category C: Dabigatran, Desirudin
Insufficient data to evaluate safety of DTIs in pregnancy
Avoid use of oral agents
Unknown if excreted in breast milk
81
Q

DTI antidote

A

Idarucizumab (Praxbind)

  • reversal of Dabigatran (Pradaxa)
  • Humanized monoclonal antibody fragment (Fab) derived whose target is Dabigatran
  • for use in urgent/ emergent life threatening bleeds
  • 5g IVx1, repeat if necessary
82
Q

Direct and Indirect Xa inhibitor monitoring

A
  • periodically monitor for blood loss, periodic cbc and stool occult tests recommended during tx
  • frequently monitor for neurological impairment, renal function prior to initiation and when clinically indicated (at least annually)
  • monitor hepatic function
  • antifactor Xa assay may be helpful in guiding clinical decisions
83
Q

Apixaban metabolism/ transport effects

A
  • Minor substrate of: BRCP, CYP1A2, CYP2C19, CYP2C8, CYP2C9
  • Major substrate of CYP3A4
  • substrate of P-glycoprotein
  • weak inhibitor of CYP2C19
84
Q

Edoxaban metabolism/transport effects

A

Substrate of P-glycoprotein

85
Q

Rivaroxoban metabolism/transport effects

A
  • Minor substrate of CYP2J2
  • Major substrate of CYP3A4
  • substrate of P-glycoprotein
86
Q

Direct and Indirect Xa inhibitor Drug-disease interactions

A
  • impaired renal function + rivaroxaban + drugs that are weak to moderate CYP3A4 and P-gp inhibitors may have increases in Rivaroxoban exposure
  • grapefruit juice may increase levels / effects of apixaban and rivaroxaban
87
Q

Direct and Indirect Xa inhibitor contraindications

A
  • hypersensitivity
  • active, major bleeding
  • Fondaparinux: severe renal impairment (
88
Q

Direct and Indirect Xa inhibitors in Pregnancy

A

Category B: apixaban, Fondaparinux
Category C: rivaroxaban, edoxaban
-may increase risk of pregnancy related hemorrhage
-anticoagulant effect cannot be easily monitored or reversed. Prompt clinical evaluation is warranted w any unexplained decrease in Hb, hct, BP, or fetal distress

89
Q

Direct and Indirect Xa inhibitor antidote

A

There are none

  • also not dialyzable
  • Protamine and vit k do not affect anticoagulant activity
  • Therapy for severe hemorrhage may include prothrombin complex (PCC), activated prothrombin complex concentrate (APCC) or recombinant factor VIIa
  • potential use of activated charcoal if ingestion of apixaban within 2-6h of presentation
90
Q

Antiplatelet agents

A
  • COX inhibitors
  • PDE/adenosine uptake inhibitors
  • aggregation inhibitors/ platelet P2Y12 receptor antagonists (ADP inhibitors)
  • aggregation inhibitors/ PDE III inhibitor
  • glycoproteins IIb/IIIa inhibitors
91
Q

COX inhibitors

A

Aspirin (PO) 75-500mg

92
Q

PDE/ adenosine uptake inhibitors

A

Dipyridamole (PO)

93
Q

ADP inhibitors (platelet P2Y12 receptor antagonists)

A
  • Cangrelor
  • Clopidogrel (Plavix)
  • Prasugrel (effient)
  • Ticragrelor (Brillinta)
  • Ticlopodine HCl (Ticlid)
94
Q

PDE III inhibitor

A

Cilostazol (pletal)

95
Q

Glycoprotein IIb/IIIa inhibitors

A
  • Abciximab (ReoPro) - IV
  • Eptifibatide (integrilin) - IV
  • Tirofiban HCl (Medicure) - IV
96
Q

Aspirin (ASA) indications

A
  • Prevention of recurrence of stroke, TIA, MI
  • Revascularization procedures
  • Acute coronary syndromes: do not use ext. release or enteric coated form
97
Q

Aspirin dosage (STEMI and unstable angina/ non-STEMI)

A

Initial: 162-325 mg on presentation
Maintenance: 81mg/d, same if taken w Ticagrelor
- doses over 150mg makes little difference in CV outcomes, but increases bleeding risk
Concomitant: in combination w clopidogrel or Ticagrelor (or w an IV GPIIb/IIIa inhibitor if invasive strategy for Unstable Angina/non-STEMI

98
Q

Aspirin onset of action

A

Immediate release: platelet inhibition within 1 hour

Enteric coated: delayed (but within 20 mins if chewed)

99
Q

Aspirin duration

A

IR: 4-6h

- platelet inhibition lasts lifetime of platelet be of irreversible inhibition of platelet COX1

100
Q

Aspirin Absorption

A

IR: rapidly absorbed in stomach and upper intestine
XR: dependent upon food, alcohol, and gastric pH

101
Q

Aspirin distribution

A

VD 10L, readily into most body fluids and tissues

Protein Binding: Concentration dependent, inverse to salicylate concentration

102
Q

Aspirin Metabolism

A

Hydrolysis to salicylate (active) by esterases in GI mucosa, RBCs, synovial fluid, and blood

  • metabolism of salicylate occurs primarily by hepatic conjugation
  • metabolic pathways are saturable
103
Q

Aspirin Excretion

A

Urine
Half life:
- parent drug: 15 to 20 minutes
- salicylates: 3h at lower doses, 5-6h after 1g, 10h with higher doses

104
Q

Aspirin contraindications

A
  • Hypersensitivity to NSAIDS
  • Allergic cross reactivity for salicylates
  • ADR
105
Q

Aspirin in pregnancy

A
  • salicylates cross placenta, can cause mortality, intrauterine growth retardation, salicylate intoxication, bleeding abnormalities, neonatal acidosis
  • use close to delivery may cause premature closure of ductus arteriosus
  • may be used in 2nd and third trimesters in women w prosthetic valves
106
Q

Aspirin interactions

A
  • Any drug that has anticoagulant effect - incr. bleed risk
  • NSAIDs suppress glomerular filtration, may cause toxicity in drugs that rely on renal excretion
  • NSAIDs can elevate BP an antagonize hypertensive meds
  • very sensitive to pH changes: Ammonium chloride and acetazolamide may increase. Serum conc. And Sodium bicarbonate alkalizer urine, leading to enhanced excretion
107
Q

Dipyridamole indications

A

Adjunct to Coumadin anticoagulants

Prevention of stroke or TIA

108
Q

Dipyrimadole absorption/distribution

A
  • 75 min to peak conc. After oral dose

- alpha half life of 40 mins, beta half life is 10h

109
Q

Dipyridamole metabolism and excretion

A

Metabolized in liver, conjugated as a glucuronide and excreted in bile

110
Q

Dipyridamole contraindications

A
  • hypersensitivity
  • elevation in hepatic enzymes
  • headache (has vasodilatory effect)
111
Q

Dipyridamole in pregnancy

A

Category B
Excreted in human milk
Not used in pregnancy much

112
Q

Dipyridamole drug interactions

A

Inhibits P-glycoprotein

113
Q

Dipyridamole monitoring

A

Signs and symptoms of bleeding

FDA doesn’t recommend any labs

114
Q

Dipyridamole fun facts

A

Not used much

Short acting might lead to increased risk of cardiac ischemia when used by patients using dipyridamole to prevent MI

115
Q

Cilostazol indications

A
  • Intermittent claudication

- - reduction of symptoms as indicated by walking distance

116
Q

Cilostazol distribution

A

Protein binding: Cilostazol 95-98%; active metabolites 66-97%

117
Q

Cilostazol metabolism

A

Hepatic
Major: CYP2C19, CYP3A4
Minor: CYP1A2, CYP2D6

118
Q

Cilostazol excretion

A

Urine (74%), feces (20%) as metabolites

Half life elimination: 11-13h

119
Q

Cilostazol onset

A

Effect on walking distance:2-4 weeks, may require up to 12 weeks

120
Q

Cilostazol special pops

A

Renal function impairment - increases metabolic concentrations and alters protein binding of parent drug
Dialysis- unlikely that it can be removed efficiently bc of protein binding
Smokers - decreases exposure by 20%

121
Q

Cilostazol monitoring

A

Periodic white blood cell and platelet counts

Year 2 Unit 2 (6 decks)

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