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Pharm CH 34
Disorders of Coagulation
20
Pharmacology
Professional
05/30/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Heparin
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Indirect Thrombin Inhibitors (act through antithrombin)

 

Binds to & enhances anti-thrombin, which then inhibits clotting factors (IIa, IXa, Xa). Heparin is then released for renewed binding to more anti-thrombin.

bleeding, loss of hair (reversible alopecia), osteoporosis, mineralocorticoid deficiency,

heparin-induced thrombocytopenia (systemic hypercoagulable state), allergic reactions

CI: bleeding issues (hemophilia, hypertension), infective endocarditis, active TB, visceral carcinoma, advanced hepatic/renal disease

 

Term

Enoxaparin

and other low molecular weight "parin"s

Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Indirect Thrombin Inhibitors (act through antithrombin)

 

Inhibit activated factor X but have less effect on thrombin than HMW

 

Equal efficacy but increased bioavailability = less frequent dosing requirements

Osteoporosis, thrombocytopenia

thromboembolism

 

Term
Fondaparinux
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Indirect Thrombin Inhibitors (act through antithrombin)

 

Binds antithrombin with high specific affinity resulting in efficient inactivation of factor Xa

 

Does not cross-react with heparin-induced thrombocytopenia (HIT) antibodies in most people

Thromboembolism

 

Long half-life (1/day dosage)

 

Term

Epirudin

and other "rudin"s

Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Direct Thrombin Inhibitors (Bind directly to thrombin)

 

Bivalent DTIs that bind at both the catalytic or active site of thrombin as well as at a substrate recognition site

 

Excreted by kidney

 

Up to 40% of patients who receive long-term infusions develop antibody against thrombin-lepirudin complex

Rx: HIT, coronary angioplasty

in patients w. HIT

 

CI: renal insufficiency

Preferred for patients with hepatic insufficiency

 

Term
Argatroban
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Direct Thrombin Inhibitors (Bind directly to thrombin)

 

Small molecules that bind only at the thrombin active site

 

Clearance by liver

 

Rx: HIT, coronary angioplasty

in patients w. HIT

 

CI: hepatic insufficiency

Preferred for patients with renal insufficiency

 

Term
Warfarin
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Coumarin Anticoagulants

 

Blocks the γ-carboxylation of glutamate residues in prothrombin and factors VII, IX, and X as well as anticoagulant proteins C and S.  => incomplete coagulation factor molecules that are biologically inactive.

Protein carboxylation is coupled to oxidation of vitamin K.  Warfarin prevents reductive metabolism of the inactive vitamin K back to its active form.

CI: pregnancy (crosses placenta

and can cause hemorrhage or

abnormal bone formation in fetus)

 

Drug Interactions:

Synergistic effects with aspirin pyrazolones, metronidazole & trimethoprim

 

Competitive antagonism with

barbiturates & rifampin

By interfering with the

synthesis of clotting factors,

coumarin anticoagulants take

longer until the onset of effects.

 

Term
Streptokinase
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Fibrinolytic Drugs (Catalyze plasminogen → plasmin )

 

Protein synthesized by streptococci that combines with the proactivator plasminogen forming an enzymatic complex that catalyzes conversion of plasminogen to plasmin

Patients with antistreptococcal antibodies can develop fever, allergic reactions, and resistance

↑ bleeding risk in ischemic stroke

Pulmonary embolism

Deep venous thrombosis

Ascending thrombophlebitis Peripheral vascular disease

Acute MI

Term
Urokinase
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Fibrinolytic Drugs (Catalyze plasminogen → plasmin )

 

Enzyme synthesized by the kidney that directly converts plasminogen to active plasmin

 

Term
Tissue Plasminogen Activator
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

Fibrinolytic Drugs (Catalyze plasminogen → plasmin )

 

Activates plasminogen  that is bound to fibrin, which (theoretically) confines fibrinolysis to formed thrombi and avoids systemic activation

 

“ + acute ischemic stroke

Term
Drotrecogin
Definition

CH 34 Drugs Used in Disorders of Coagulation

Anticoagulant Drugs

 

recombinant form of activated protein C, which inhibits factors Va and VIIIa; anti-thrombotic, anti-inflammatory, and profibrinolytic properties

bleeding

Sever sepsis or septic shock

(but efficacy is now questionable)

 

Term
Clopidogrel
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

Irreversibly block the ADP receptor on platelets, inhibiting ADP induced platelet aggregation

hemorrhage, leukopenia, purpura

Agranulocytosis,

blood dyscrasias

Clopidogrel has ↓ neutropenia

Prevention of vascular events among patients with transient ischemic attacks, strokes, and angina pectoris

 

 

Term
Ticlopidine
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

Irreversibly block the ADP receptor on platelets, inhibiting ADP induced platelet aggregation

hemorrhage, leukopenia, purpura

Agranulocytosis,

blood dyscrasias

Clopidogrel has ↓ neutropenia

Prevention of vascular events among patients with transient ischemic attacks, strokes, and angina pectoris

 

Term
Abciximab
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

Inhibits glycoprotein IIb/IIIa receptor. This glycoprotein acts as the final common pathway for platelet aggregation. It is normally activated by fibronectin,

vitronectin, fibrinogen & vWF

Thrombocytopenia

Percutaneous coronary

interventions, acute coronary

syndrome

 

Term
Eptifibatide
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

Inhibits glycoprotein IIb/IIIa receptor

 

Thrombocytopenia

Percutaneous coronary interventions, acute coronary

syndrome

 

Term
Tirofiban
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

Inhibits glycoprotein IIb/IIIa receptor

 

Thrombocytopenia

Percutaneous coronary interventions, acute coronary

syndrome

 

Term
Dipyridamole
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

Vasodilator; ↓ platelet function by inhibiting adenosine uptake and cGMP phosphodiesterase activity

Little or no beneficial effect on its own

prevent cerebrovascular ischemia (w/aspirin), thromboembolis with prosthetic heart valves (w/ warfarin)

 

Term
Cilostazol
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

Phosphodiesterase inhibitor that promotes vasodilation and inhibition of platelet aggregation

 

Rx: intermittent claudication

(leg cramp w/ exercise d/t

arterial obstruction)

 

Term
Anagrelide
Definition

CH 34 Drugs Used in Disorders of Coagulation

Antiplatelet Agents

 

cAMP-PDE-III inhibitor that inhibits megakaryocyte maturation into platelets

Hepatic toxicity, CVA, hemorrhage

Essential thrombocytosis (overproduction of platelets); chronic myeloid leukemia

 

Term
Aminocaproic acid
Definition

CH 34 Drugs Used in Disorders of Coagulation

Fibrinolytic Inhibitors

 

Inhibits fibrinolysis by inhibiting

plasminogen activation

 

Rx: adjunctive therapy in

hemophilia, or as a prophylaxis

for re-bleeding from

intracranial aneurysms

 

Term
Aprotinin
Definition

CH 34 Drugs Used in Disorders of Coagulation

Fibrinolytic Inhibitors

 

Serine protease inhibitor that inhibits fibrinolysis by free plasmin. Inhibits the

plasmin-streptokinase complex

↑ risk of renal failure, heart attack, and stroke

Reduce bleeding from surgery

 

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