Core pharmacology

Class Group

AntiFibrinolytic

Introduction

Synthetic Lysine Derivative Antifibrinolytic

Indications Uses

1. Trauma
2. Elective Arthroplasty
3. Hemophilia
4. Obstetric surgery
5. Menorrhagia
6. Recent evidence to suggest possible role in mild to moderate TBI

Presentation

PO and IV
500mg tablet, 1g IV

Mechanism of action

Reversibly inhibits lysine binding sites on plasminogen → Inhibits conversion of plasminogen to plasmin, thereby preventing the breakdown of fibrin

Adverse Effects Toxicity

1. Abdominal pain, especially on rapid bolus
2. Possible risk of increased VTE (exact risk is controversial)
3. Delayed seizures

Absorption

BA 50%

Protein binding

<3L PB

Volume of distribution

Vd- 9-12L, crosses into all tissues

Metabolism

Minimally metabolized

Excretion

95% unchanged in urine

Half-life

T1/2 90min-3 hours