Drugs for Coagulation Disorders

Question 1

antipyretic, anti-inflammatory, ANTI-PLATELET, analgesic
prevents arterial thrombosis; used for inflammatory disorders
uncoupler of oxidative phosphorylation in ETC
SE: hypersensitivity

Answer 1

aspirin/acetylsalicylic acid/ASA

Question 2

toxic and lethal dose of ASA/aspirin

Answer 2

toxic dose: 150 mg/kg

lethal dose: 500 mg/kg

Question 3

acid-base disorder in aspirin intoxication

Answer 3

adults: respiratory alkalosis with HAGMA
children: HAGMA

Question 4

ASA intoxication in children

considered idiosyncratic

Answer 4

Reye Syndrome

Question 5

Samter Triad of ASA intoxication

Answer 5

asthma
aspirin sensitivity
nasal polyps

Question 6

GpIIb/IIIa inhibitor

prevents vessel restenosis, reinfarction, death

Answer 6

Abciximab

Eptifibatide, Tirofiban

Question 7

ADP inhibitor
reduces platelet aggregation
prevention and treatment of arterial thrombosis
has additive effects with aspirin

Answer 7

Clopidogrel
Ticlopidine (parent coumpound; has more GI and hema SE)
Prasugel

Question 8

PDE inhibitor
increases cAMP (which is an anti-aggregant)
for intermittent claudication

Answer 8

Dipyrimadole (has little or no benefit)

Cilostazol (contraindicated in heart failure)

Question 9

2 major types of anti-coagulants:
indirect thrombin inhibitors: ?
direct thrombin inhibitors: ?

Answer 9

indirect thrombin inhibitors: heparin, enoxaparin (LMWH), coumarin derivatives (warfarin)

direct thrombin inhibitors: lepirudin

Question 10

heparin antidote

Answer 10

protamine sulfate

Question 11

laboratory tests to evaluate coagulation pathways

Answer 11

intrinsic pathway: PTT

extrinsic pathway: PT

Question 12

indirect thrombin inhibitor; anticoagulant
activates antithrombin III
for deep venous thrombosis, pulmonary embolism, myocardial infarction
monitor with aPTT (N = 1.5 - 2.5)

Answer 12

heparin

Question 13

indirect thrombin inhibitor; anticoagulant
factor Xa selective
for deep venous thrombosis, pulmonary embolism, myocardial infarction
SE: less risk of thrombocytopenia
does NOT require aPTT monitoring
protamine sulfate is only partially effective in reversing effects

Answer 13

Enoxaparin

Dalteparin, Tinzaparin, Danaparoid, Fondaparinux

Question 14

direct thrombin inhibitor; anticoagulant
for heparin-induced thrombocytopenia
monitor effect with aPTT
NO REVERSAL AGENT EXISTS

Answer 14

Lepirudin

Desirudin, Bivalirudin, Argatroban, Dabigatran

Question 15

oral direct Factor Xa inhibitor

Answer 15

Rivaroxaban

Apixaban

Question 16

anticoagulant
for chronic anticoagulation EXCEPT in pregnancy
monitor effects with PT
NARROW THERAPEUTIC WINDOW
active ingredient in most rat poisons (racumin)

Answer 16

Warfarin
Dicumarol
Anisindione

SE: warfarin-induced skin necrosis (for protein C & S deficiencies)

Question 17

antidote for warfarin

Answer 17

Vit. K (slow) vs. FFP (fast)

Question 18

what is prothrombotic first before it works as an anticoagulant?

Answer 18

warfarin
requires elimination of preformed clotting factors (8-60 hrs)
hence heparin bypasses initial prothrombotic effect of warfarin (skin necrosis)

Question 19

what increases clearance and reduces anticoagulant effect?

Answer 19

cytochrome P450-inducers

Question 20

what reduces clearance and increases anticoagulant effect?

Answer 20

cytochrome P450-inhibitors

Question 21

cytochrome P450-inducers

Answer 21

Ethanol
Barbiturates
Phenytoin
Rifampicin
Griseofulvin
Carbamazepine
St. John's Wort/Smoking

Question 22

cytochrome P450-inhibitors

Answer 22

Isoniazid
Sulfonamides
Cimetidine
Ketoconazole
Erythromycin
Grapefruit juice
Ritonavir
Amiodarone
Quinidine

Question 23

antidote
chemical antagonist
partially reverses effects of LMWH

Answer 23

protamine sulfate

Question 24

tissue plasminogen activator analog
thrombolytic
for acute MI, ischemic stroke, pulmonary embolism
antidote: AMINOCAPROIC ACID

Answer 24

Alteplase
anistreplase, reteplase, streptokinase, tenecteplase, urokinase

loss of effectiveness (on 2nd use) and allergic reactions may be observed with STREPTOKINASE

Question 25

contraindication to thrombolysis

Answer 25

1. history of cerebrovascular hemorrhage at any time 2. non-hemorrhagic stroke or other cerebrovascular event within past year 3. marked hypertension (>180/110 mmHg) at any time during acute presentation 4. suspicion of aortic dissection 5. active internal bleeding (except menses)

Question 26

``` prothrombotic antiplasmin aminocaproic acid inhibits tPA CONTRAINDICATED IN DIC ```

Answer 26

Tranexamic Acid

Question 27

antidote prevention of hemorrhagic diathesis in newborns SE: severe infusion reaction (dyspnea, chest and back pain)

Answer 27

Vitamin K1 = Phytonadione Vitamin K2 = Menaquinone Vitamin L3 = Menadione --> SHOULD NEVER BE USED IN THERAPEUTICS (INEFFECTIVE)

Question 28

ADH agonist vasopressin V2 receptor agonist increases factor VIII activity of patients with mild hemophilia A or von Willebrand disease

Answer 28

Desmopressin | Vasopressin

Question 29

antiplasmin serine protease inhibitor for post-op or intra-op bleeding REMOVED IN 2007 FROM MARKET DUE TO MORTALITY

Answer 29

Aprotinin

Question 30

other drugs used for coagulation disorders

Answer 30

antihemophilic factor anti-inhibitor coagulant complex anti-thrombin III factor VIIa, VIII, IX complex