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ABC > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Aspirin: MOA

A

Nonselective COX inhibitor

In platelets, aspirin irreversibly acetylates COX-1, inhibiting COX-1 –> prevents TxA2 synthesis and associated platelet aggregation

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2
Q

Aspirin: differential effect in platelets vs endothelial cells

A

Platelets express COX-1 –> TxA2 synthesis (PROMOTES platelet aggregation)

  • Endothelial cells express COX-1 and COX-2 –> prostacyclin synthesis (INHIBITS platelet aggregation)

However, effect of aspirin in platelets lasts longer because platelets do not have a nucleus and cannot regenerate COX-1, thus tipping balance in favor of inhibited platelet aggregation

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3
Q

Aspirin: dose dependent effect

A

Low doses: anti-thrombotic

Higher doses: anti-inflammatory (3-5g/day)

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4
Q

Aspirin: adverse effects

A
  • Bleeding
  • GI upset and ulcers (COX-1 involved in production of stomach mucus)
  • Renal toxicity (prostaglandins involved in vasodilation of afferent arteriole and regulation of GFR)
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5
Q

Aspirin in kids after viral illness: consequence

A

Reye Syndrome: hepatic injury and encephalopathy in kids –> AVOID!!

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6
Q

Aspirin: indications

A

Arterial thrombosis: MI, stroke, peripheral artery disease, angina, atrial fibrillation, during and post PCI (percutaneous coronary intervention, aka stent)

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7
Q

Clopidogrel: MOA

A

Irreversible ADP receptor antagonist

Prodrug requiring CYP activation

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8
Q

Clopidogrel: indications

A

Pre-PCI: bolus given

After-PCI: clopidogrel + aspirin for one year

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9
Q

ADP receptor antagonists: name 3

A

“GREL’s”

1) Clopidogrel (irreversible, prodrug)
2) Prasugrel (irreversible, prodrug, faster kinetics)
3) Ticagrelor (reversible, NOT a prodrug)

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10
Q

GpIIb/IIIa inhibitors: name 3

A

Abciximab
Tirofiban
Eptifibitide

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11
Q

GpIIb/IIIa inhibitors: indications

A

During PCI (only IV), and after for 12-24 hours

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12
Q

Anticoagulants: indications

A

Both venous and arterial: PE, DVT, MI, acute coronary syndromes

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13
Q

Heparin: MOA

A

Catalyzes antithrombin-3 (AT3) inactivation of thrombin and factor Xa

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14
Q

Low molecular weight (LMW) heparin (enoxaparin): MOA

A

Catalyzes antithrombin-3 (AT3) inactivation of factor Xa (like fondaparinux)

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15
Q

Fondaparinux: MOA

A

Catalyzes antithrombin-3 (AT3) inactivation of factor Xa (like enoxaparin)

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16
Q

LMWH and fondaparinux: monitoring

A

None needed. Can use anti-Xa testing

Thrombin: rate limiting step, which comes AFTER Factor Xa

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17
Q

What reverses heparin activity?

A

Protamine

18
Q

Heparin: adverse effects

A

Heparin-induced thrombocytopenia: IgG antibody to heparin and platelet factor 4 activates platelets, leading to widespread platelet coagulation and thrombocytopenia

19
Q

Heparin: route

A

IV or SC

20
Q

LMW heparin: route

A

SC

21
Q

Thrombin inhibitors: name 3

A

Dabigatran (reversible)

“Rudins”: bivalirudin, desirudin

22
Q

Dabigatran: MOA

A

Thrombin inhibitor (antidote exists)

“DABigatran” –> II [arms]

23
Q

“Rudins”: MOA

A

Thrombin inhibitors

“RU” rhymes with TWO

24
Q

Rivaroxaban: MOA

A

Factor X inhibitor (no antidote)

RivaroXaBAN
“Ban” = X

25
Q

Unfractionated heparin: indications

A

Bypass surgeries

Dialysis

26
Q

Warfarin: MOA

A

Inhibition of epoxide reductase (normally activates Vit K in liver) –> inhibits vitamin K dependent gamma-carboxylation of Factors 10, 9, 7, 2, and Proteins C and S

“1972”

27
Q

Why is heparin bridge needed when administering warfarin?

A

Proteins C and S (“clot stoppers”) are first to be depleted after warfarin is administered –> there’s actually an increased risk of clotting and skin necrosis immediately after

28
Q

Reversal for warfarin

A

Vit K

Fresh frozen plasma (faster)

29
Q

Warfarin: route

A

Oral

30
Q

Oral anticoagulants

A

Warfarin
Dabigatran
Rivaroxaban

31
Q

PTT or PT for monitoring unfractionated heparin?

A

PTT

Heparin catalyzes AT3-mediated inactivation of thrombin and Factor Xa

32
Q

PTT or PT for monitoring warfarin?

A

PT

Factor 7 is Vit-K dependent

33
Q

PTT test: what does it measure?

A

Intrinsic pathway, common pathway
Rate-limiting step: Factor IIa (thrombin)

Two T’s: “IN” a relationship

34
Q

PT test: what does it measure?

A

Extrinsic pathway
Common pathway

Rate-limiting step: Factor VII (short half life)

Need to add tissue factor to sample to activate extrinsic pathway

35
Q

What is PT/INR?

A

PT times are standardized b/c of variability in added TF

INR = (PTtest/PTnl)^ISI

36
Q

Warfarin: adverse events

A

Bleeding
Teratogen
Skin and tissue necrosis
Early transient hypercoagulability

37
Q

Direct Factor Xa inhibitors

A

Rivaroxaban (Xarelto)

Apixaban (Eliquis)

38
Q

Thrombolytics: name 4

A

Streptokinase

Alteplase, reteplase, tenecteplase

39
Q

Thrombolytics: MOA

A

Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin
clots

“Clot busters”

40
Q

Thrombolytics: indications

A

STEMI
Stroke
PE

41
Q

Thrombolytics: contraindications

A

Active bleeding, Hx intracranial bleeding, recent surgery, stroke <6 mo

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