Heme

Question 1

Heparin

Answer 1

1) immediate anticoag for PE, ACS, MI, DVT (pregnancy safe)
2) Anti-thrombin: antithrombin cofactor –> decr thrombin* + decr factor Xa
3) toxicity: bleeding, HIT, osteoporosis, Rx interactions; protamine sulfate antidote (pos charge molec that binds neg charge heparin)
4) short 1/2 life

Question 2

Enoxaparin

Answer 2

1) immediate anticoag for PE, ACS, MI, DVT (pregnancy safe)
2) LMWH antithrombin: act more on factor Xa
3) toxicity but less risk than heparin: bleeding, HIT, osteoporosis, Rx interactions; no antidote
4) compared to heparin: better bioavail, 2~4x longer 1/2 life; sub-Q; no need to monitor

Question 3

Dalteparin

Answer 3

1) immediate anticoag for PE, ACS, MI, DVT (pregnancy safe)
2) LMWH antithrombin: act more on factor Xa
3) toxicity but less risk than heparin: bleeding, HIT, osteoporosis, Rx interactions; no antidote
4) compared to heparin: better bioavail, 2~4x longer 1/2 life; sub-Q; no need to monitor

Question 4

Argatroban

Answer 4

1) immediate anticoag for pts w/ HIT
2) directly inhibits thrombin
4) deriv of hirudin (leeches)

Question 5

Bivalirudin

Answer 5

1) immediate anticoag for pts w/ HIT
2) directly inhibits thrombin
4) deriv of hirudin (leeches)

Question 6

Warfarin (Coumadin)

Answer 6

1) chronic anticoag: post STEMI, VTE prophylaxis, prevent stroke in afib (teratogenic)
2) antiplt: interfere w/ nl syn + gamma-carboxylation of vit-K clotting factors on their glutamic residues (1972: X, IX, VII, II) + proteins C, S (by blocking Epoxide Reductase)
3) bleeding, teratogenic, skin/tissue necrosis*, Rx interactions; give vit K for OD, give FFP for severe OD
4) cyt P450 metabolized; incr PT (extrinsic path); long 1/2 life; follow PT/INR; PO

Question 7

Alteplase (tPA)

Answer 7

1) early MI, early ischemic stroke, direct thrombolysis of severe PE
2) thrombolytic: aid plasminogen –> plasmin to cleave thrombin + fibrin clots
3) bleeding (contraindicate in active bleed, intracranial bleed hx, recent sx, known bleed diathese, severe HTN); tx toxicity w/ aminocaproic acid (inhibits fibrinolysis)
4) incr PT, PTT; no change in plt ct

Question 8

Reteplase (rPA)

Answer 8

1) early MI, early ischemic stroke, direct thrombolysis of severe PE
2) thrombolytic: aid plasminogen –> plasmin to cleave thrombin + fibrin clots
3) bleeding (contraindicate in active bleed, intracranial bleed hx, recent sx, known bleed diathese, severe HTN); tx toxicity w/ aminocaproic acid (inhibits fibrinolysis)
4) incr PT, PTT; no change in plt ct

Question 9

Tenecteplase (TNK-tPA)

Answer 9

1) early MI, early ischemic stroke, direct thrombolysis of severe PE
2) thrombolytic: aid plasminogen –> plasmin to cleave thrombin + fibrin clots
3) bleeding (contraindicate in active bleed, intracranial bleed hx, recent sx, known bleed diathese, severe HTN); tx toxicity w/ aminocaproic acid (inhibits fibrinolysis)
4) incr PT, PTT; no change in plt ct

Question 10

Aspirin (ASA)

Answer 10

1) antipyretic, analgesic, anti-infl, anti-plt (decr aggregation)
2) irreversibly inhibits COX-1 (and -2) via covalent acetylation –> decr TxA2 + prostaglandins
3) gastric ulcer, tinnitus (CN VIII); chronic use: acute renal failure, interstitial nephritis, upper GI bleed; Reye’s syn in kids w/ viral infct; OD: respir alkalosis + met acidosis
4) plts can’t syn new COX so effect lasts until new plts made; incr bleeding time; no effect on PT, PTT

Question 11

Clopidogrel

Answer 11

1) ACS, coronary stenting, decr incidence + recurr of thrombotic stroke
2) ADP R inhibitor: inhibit plt aggregation by irreversibly blocking ADP R; inhibit fibrinogen binding via Gp IIb/IIIa

Question 12

Ticlopidine

Answer 12

1) ACS, coronary stenting, decr incidence + recurr of thrombotic stroke
2) ADP R inhibitor: inhibit plt aggregation by irreversibly blocking ADP R; inhibit fibrinogen binding via Gp IIb/IIIa
3) neutropenia (unique)

Question 13

Prasugrel

Answer 13

1) ACS, coronary stenting, decr incidence + recurr of thrombotic stroke
2) ADP R inhibitor: inhibit plt aggregation by irreversibly blocking ADP R; inhibit fibrinogen binding via Gp IIb/IIIa

Question 14

Ticagrelor

Answer 14

1) ACS, coronary stenting, decr incidence + recurr of thrombotic stroke2) ADP R inhibitor: inhibit plt aggregation by irreversibly blocking ADP R; inhibit fibrinogen binding via Gp IIb/IIIa3) N/A4) N/A

Question 15

Cilostazol

Answer 15

1) intermittent claudication, coronary vasodilation, prevent stroke/TIAs (w/ ASA), angina prophylaxis
2) PDE III inhibitor –> incr cAMP in plts –> inhibit plt aggregation; vasodilator
3) nausea, HA, facial flush, hypotension, ab pain

(cAMP usually decreases Ca and inhibits PLT granule release)

Question 16

Dipyridamole

Answer 16

1) intermittent claudication, coronary vasodilation, prevent stroke/TIAs (w/ ASA), angina prophylaxis
2) PDE III inhibitor –> incr cAMP in plts –> inhibit plt aggregation; vasodilator
3) nausea, HA, facial flush, hypotension, ab pain

Question 17

Abciximab

Answer 17

1) unstable angina, PTCA (percutaneous transluminal coronary angioplasty)
2) Gp IIb/IIIa inhibitor: bind R on activated plts –> prevent aggregation
3) bleeding, thrombocytopenia
4) made from monoclonal ab Fab fragments (unique)

Question 18

Eptifibatide

Answer 18

1) unstable angina, PTCA
2) Gp IIb/IIIa inhibitor: bind R on activated plts –> prevent aggregation
3) bleeding, thrombocytopenia

Question 19

Tirofiban

Answer 19

1) unstable angina, PTCA
2) Gp IIb/IIIa inhibitor: bind R on activated plts –> prevent aggregation
3) bleeding, thrombocytopenia

Question 20

Dimercaprol, EDTA

Answer 20

use for Lead poisoning in adults

Question 21

Succimer

Answer 21

used to chelate lead in children “it SUCks to be a kid who ate lead”

Question 22

Eculizumab

Answer 22

Rx for Paroxysmal Nocturnal Hemoglobinuria; terminal complement inhibitor

Question 23

Argatroban

Answer 23

Direct thrombin inhibitor, binds to the thrombin active site

Question 24

Abixaban, Rivaroxaban

Answer 24

Direct factor 10a inhibitor.

For tx and prophylaxis of DVT, PE, stroke prophylaxis in A-fib. Oral agents.