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Heme/Lymph 1 > Drugs Used to Prevent or Treat Thromboembolic Disorders > Flashcards

Drugs Used to Prevent or Treat Thromboembolic Disorders Flashcards

1
Q

Antiplatelet and coag vs. thrombolytics

A

Antiplatelet and coag - inhibit formation of clots

Thombolytics - lyse clots

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2
Q

Antidepressants and platelets

A

Increased serotonin release so can lead to risk of bleeding

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3
Q

Aspirin MOA

A 
Irreversible inhibitor (of mostly COX1)
COX1 constitutive in platelets 
INhibits TXA2 formation
No TXA2 can stimulate TP receptor 
Inhibits platelet aggregation for the life of the platelet
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4
Q

Other NSAIDs

A

Are reversible…may compete with aspirin and decrease its effectiveness

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5
Q

Uses of aspirin and route of delivery

A

Oral
Acutely in patients (MI or PCI)
Prophylaxis to prevent primary or secondary CV events

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6
Q

Other aspirin uses

A

Antipyretic
Analgesic
Anti-inflammatory

All at higher doses

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7
Q

Aspirin adverse effects and contraindications

A

Profound bleeding and bruising
Increased risk of heartburn and PUD due to inhibited gastric PG synthesis (less at lower dose)

Hypersensitivity of ASA or asthma

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8
Q

Aspirin PK

A

Half life short

Therapeutic effect 7-10 days

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9
Q

Clopidogrel MOA and use

A

Prodrug
Irreversible antagonist of ADP receptor P2Y12
Prevents ADP induced decrease in cAMP and thus prevents aggregation

similar to aspirin use

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10
Q

Clopidogrel metabolism and PK

A 
CYP2C19 metabolized...2 steps 
Don't use with CYP2C19 inhibitors (omeprazole)
Therapeutic is 7-10 days 
Oral 
Genetic variation of CYP2C19
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11
Q

Adverse effects of clopidogrel

A

Bruising and bleeding

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12
Q

Vorapaxar MOA and therapeutic use

A

Antagonist of protease activated receptor 1 (PAR1) thus prevents platelet activation by thrombin via this receptor

Only in patients with history of peripheral artery dz or previous MI…use with aspirin and/or clopidogrel

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13
Q

Vorapaxar adverse effects, contraindicated, and drug interactions

A

Increased bleeding

Patients with history of hemorrhage or TIA (transient ischemic attacks)

NSAIDs, SSRIs, SSNIs, and strong CYP3A4 modifeiers

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14
Q

Abciximab MOA and route

A

IV
GP2B/3A antagonist block platelet aggregation by preventing fibrinogen from binding platelets and consolidating platelet plug
Prevents platelet adhesion and aggregation by ANY stimulus
Prevents prothrombin from binding to platelets —– decreases thrombin formed—-anticoagulant
Monoclonal AB

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15
Q

Uses of abciximab

A

Emergency tx of acute coronary syndromes
During PCI
Crisis situations

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16
Q

Adverse effects and PK of abciximab

A

Bleeding

Half life of about 30 minutes
Gp2b/3a bound for 18-24 hours
PLatlet function back in 48 hours

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17
Q

Heparin route and MOA

A

IV, SC

Complex with AT and increases activity
Inactivates factors 2, 9, and 10 as suicide substrate

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18
Q

How to monitor heparin

A

Anti-10a assay (or aPTT) and platleet count…alters intrinsic pathway

19
Q

Heparin advewrse affects

A

Bleeding
HIT
Heparin sensitivyt
Osteoporosis

20
Q

Antidote for heparin

A

Protamine sulfate

21
Q

Enoxaparin MOA and route

A

Complexes with AT3 and increases activity…only inactivates 10a
IV, SC

22
Q

Fondaparinux MOA and route (with PK)

A

Only SC
Accelerates activity of AT3 against F10
More predicatble with 17 hour halflife

23
Q

Adverse effects of heparin and derivitives

A

Bleeding problems…patient education…less with fondaparinux

24
Q

Monitoring of heparin and derivatives

A

Heparin - must be monitored by Anti 10a (.3-.7 is goal)

Others - Anti 10a if needed

25
Q

PK of heparin and deriviates

A

Hep and LMWH - SC or IV
Fonda - only SC
Hep and LMWH - given IV at hospital for acute conditions due to rapid onset
All good for SC for long term outpatient use
Heparin is dose dependent (1/2 = 30-150 min)
Enox - 3-6 hr
Fonda - 17hr

DO NOT CROSS PLACENTA SO SAFE FOR PREG

26
Q

Use of heprain and deriv

A

Usually initial short term rx and transition to oral meds

Can also use with antiplatelet therapy in more urgent situations

27
Q

Bivalirudin MOA and route

A

Direct irreversible inhibitor of thrombin
IV infusion
T1/2 = 25 minutes

28
Q

Bivalirudin uses

A

Patients who need heparin but have HIT

Microvascular surgery to reattach digits

29
Q

Warfarin route and MOA

A

Oral
Antagonist of VKOR…inhibits synthesis of factors 2,7,9,10 and protein C and S
Onset of action is 8-12 days with full effect in 3 days

Alters both intrinsic and extrinsic pathways

30
Q

Warfarin uses

A

Tx of thrombosis/embolisms

Metal prosthetic valves

31
Q

Warfarin PK

A

Oral
99% plasma protein bound
CYP metabolized
therapeutic half life long

32
Q

Warfarin adverse effects

A

Bleeding
NOT GOOD WITH PREG
Warfarin induced skin necrosis - use heparin brdige to prevent
Purple toe syndrome

33
Q

Warfarin antidotes

A

Vit K1
FFP
Prothrombin complex
F7a

34
Q

Dabigatran etexilate advantages

A

Direct action on thrombin (rapid effect)
Prodrug activated by plasma esterases, NOT CYP
More effective with less drug interactions and little impact on anything but clotting

35
Q

MOA of dabigatran and route

A

Prodrug
Competitive inhibitor of thrombin activity on both fibrinogen and platelets decrasing both platelet and coag activity

Oral

36
Q

Dabigatran uses

A

Prevent strokes

DVT and PE

37
Q

Dabigatran adverse effect, antidote, and PK

A

Bleeding

Idarucizumab

Prodrug cleaved by esterases

Dose adjustment needed in renal dz and in combination with drugs that compete for the P glycoprotein efflux transporter which transports active drug into renal tubular fluid

38
Q

Rivaroxaban route, MOA, uses, PK

A

Oral

Directly inhibits factor 10a (not through AT3 like LMWH)

Same uses as dabigatran

Oral, once a day

39
Q

Rivaroxaban warnings and antidotie

A

Bleeding, monitor renal function

Andexanet alpha

40
Q

Alteplase MOA and PK

A

Binds to clot bound fibrin and converts plasminogen to plasmin which degrades fibrin

Recombinant tPA

IV only with short half life

41
Q

When to use alteplase

A

Acute stroke
MI
PE
DVT

42
Q

Adverse effects of alteplase

A

Lyse all physiologic thrombi as well

43
Q

Contraindications of alteplase

A

Surgery, trauma within 10 days
Serious GI bleeding in last 3 months
Hypertension
Activebleeding or threat

44
Q

Antidoes for fibrinolytic therapy

A

Epsilon aminocaproic acid - PO, IV…inhibits fibrinolysis

Tranxenamic acid - topical, PO…inhibits plasminogen activity…can also be used as rinse to reduce bleeding

Heme/Lymph 1 (14 decks)

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