Anticoagulants Flashcards Preview

Pharma > Anticoagulants > Flashcards

Flashcards in Anticoagulants Deck (20)
1

heparin sulfate

Indirect Thrombin Inhibitor

Catalyzes antithrombin activity

Linear polysaccharide so has to be give parenterally

Pentasaccharid structure is active

Binds antithrombin, causes conformational change that results in activation through increase in flexibility of REACTIVE SITE LOOP

Inhibits
IIA
IXA
XA

Source: Extracted from poricne/bovine sources
Mixture of smaller molecular weight fragments

Can be toned down to low molecular weight heparin (<7,000 MW)

INDICATION:
- DVT or PE
- Useful in prophylaxis of venous thrombosis and in cases of DIC

Toxicity:
Bleeding, allergy, thrombosis, and osteoporosis

Heparin induced thrombocytopenia (systemic hypercoaguable state that occurs in UFH for a 7 days

Never administer IM (hematoma)

Requires close monitoring (PTT)

Reversal initiated by protamine sulfate

Removed from blood by:
- Saturable: Reticuloendothelial system
- Non-Saturable: RENAL

2

rivaroxaban

Anticoagulant

New

Oral administer

Factor Xa Inhibitor

No monitoring needed

Short half-life

NO GOOD REVERSAL

Maximum inh. of factor Xa occurs four hours after dose

Once daily dose

Liver, Renal, and Fecal biliary clearance

3

warfarin

Anticoagulant

Blocks vitamin K dependent factors
II, VII, IX, X, Factor C and s

Inhibits vitamin K metabolism, disrupts POSTTRANSLATIONAL gamma-carboxylation of glutamate residues

Partially inhibits synthesis, not degradation
- Makes it depend on factor half life for effectiveness

Increased INR: 2 to 3

Patients who start warfarin are put on heparin for "warfarization

Due to levels of protein C and S dropping faster than proclotting factors

Toxicity:
- bleeding
- skin necrosis
- teratogenesis
- thrombosis

Interacts with numerous other drugs, diets, disease states

Cleared by:
- Kidney
- Liver

Reversal
- Vit K
- Fresh-frozen plasma
- Recombinant factor VIIa

4

protamine sulfate

Heparin antagonist

Highly cationic peptide that binds heparin to form a stable ion pair inhibiting function

5

menadione

Warfarin antidote

Vitamin K

6

dalteparin

Low molecular weight heparin

Enhances antithrombin activity on Factor X

Use cautiously in patients with renal insufficiency

Available for prophylaxis and treatment,

Do not require laboratory monitoring

Neutralize via protamine but is incomplete, does not work on fondaparinux

Metabolism: Kidney

7

enoxaparin

Low molecular weight heparin

Enhances antithrombin activity on Factor X

Use cautiously in patients with renal insufficiency

Available for prophylaxis and treatment,

Do not require laboratory monitoring

Neutralize via protamine but is incomplete, does not work on fondaparinux

Metabolism: Kidney

8

Fondaparinux

Just pentasaccharide

Enhances antithrombin activity on Factor X

Use cautiously in patients with renal insufficiency

Available for prophylaxis and treatment,

Do not require laboratory monitoring

Neutralize via protamine but is incomplete, does not work on fondaparinux

Metabolism: Kidney

9

argatroban

Direct Thrombin Inhibitor

Parenteral

Hepatic clearance

Small molecule

IV only due to short half life

10

bivalirudin

Direct Thrombin Inhibitor

Parenteral

Hepatic clearance

20% renal clearance

20 amino acid peptide

11

lepirudin

Direct Thrombin Inhibitor

Parenteral

Renal clearance

65 aa protein

12

tissue plasminogen activator

Fibrinolytic Drug

Indications:
- Massive venous thrombosis
- Pulmonary emboli
- Acute MI

Human

Non-allergenic

Shortest half life

13

streptokinase

Fibrinolytic Drug

Indications:
- Massive venous thrombosis
- Pulmonary emboli
- Acute MI

Streptococcus

Allergic Reactions

Long half life

14

Urokinase

Fibrinolytic Drug

Indications:
- Massive venous thrombosis
- Pulmonary emboli
- Acute MI

Human

Non-allergic

Short half life

15

abciximab

Antiplatelet Drug

Chimeric monoclonal antibody

Target platelet IIb/IIIa receptor complex
- Functions as receptor for fibrinogen and vitronectin and Von Willebrand Factor

Administer Parenterally

16

aspirin

Antiplatelet Drug

Inhibit synthesis of thromboxane A2 by irreversible acetylation of COX

Most commonly used antiplatelet drug

Cardiovascular indications
- Reduce TIA
- Prevent stroke
- Primary and secondary prevention of MI
- Prevention coronary restenosis following MI/fibrinolytic therapy or bypass grafting

Side Effects:
- Excessive bleeding

17

clopidogrel

Antiplatelet Drug

Thienopyridine derivative that reduce platelet aggregation by Irreversibly blocking P2Y12 receptor on platelets

No effect on prostaglandin metabolism

Standard for patients undergoing coronary stent

Useful in patients who cannot tolerate aspirin

Fewer adverse effects and requries less dosing than ticolpidine and is therefore preferred

Activated by: CYP2C19
- Genetic variability in this populaiton

18

prasugrel

Antiplatelet Drug

Thienopyridine derivative that reduce platelet aggregation by Irreversibly blocking P2Y12 receptor on platelets

No effect on prostaglandin metabolism

Standard for patients undergoing coronary stent

Useful in patients who cannot tolerate aspirin

Fewer adverse effects and requries less dosing than ticolpidine and is therefore preferred

Prasugerel decreases platelet aggregation more rapidly and consistently

Effective in MOST INDIVIDUALS

Activation through HYDROLYSIS NOT OXIDATION

19

ticlopidine

Antiplatelet Drug

Thienopyridine derivative that reduce platelet aggregation by Irreversibly blocking P2Y12 receptor on platelets

No effect on prostaglandin metabolism

Standard for patients undergoing coronary stent

Useful in patients who cannot tolerate aspirin

Adverse Effect:
- Nausea
- Dyspepsia
- Diarrhea
- Hemorrhage
- Leukopenia (1%)

20

tirofiban

Antiplatelet Drug

IIb/IIIa inhibitor

Target receptor complex which functions as receptor for fibrinogen, vWF, and vitronectin

Smaller molecule with similary properties to eptifibatide

Administer parenterally