aminocaproic acid (Amicar)

Introduction

Tradename: Amicar.

Indications

• life-threatening hemorrhage secondary to fibrinolysis resulting from trauma
  • systemic fibrinolysis
  • urinary fibrinolysis
• hemorrhage due to platelet defects
  • Bernard Soulier disease
  • Glanzmann's thrombasthenia
  • Wiskott-Aldrich syndrome
  • gray platelet syndrome
  • granule storage pool defects
  • uremia
  • liver disease
• hemorrhagic telangiectasia
• hemophilia
• surgical hemostatis

Contraindications

• disseminated intravascular coagulation (DIC)
• hematuria

pregnancy category = d

safety in lactation = ?

Dosage

• adults:
  • 5 g PO/IV over 1 hour, then 1-1.25 g/hr for 8 hours, or until bleeding stops
  • max 30 g/day
• children:
  • 10 mg/kg or 3 g/m2 during 1st hour
  • infusion at 33 mg/kg/hr or 1 g/m2/hr
  • max: 18 g/m2/24 hours

Injection: 250 & 500 mg/mL (20 mL).

Syrup: 1.25 g/5 mL

Pharmacokinetics

• peak effects occur within 2 hours of oral dose
• therapeutic effects occur within 1-72 hours of administration

elimination via kidney

1/2life = 1-2 hours

protein binding = <5 %

elimination by hemodialysis = +

Adverse effects

• not common (1-10%)
  • hypotension, bradycardia, arrhythmia, dizziness, headache, malaise, fatigue, rash, GI irritation, nausea, cramps, diarrhea, impaired platelet function, elevated serum transaminases, myopathy, weakness, tinnitus, nasal congestion
• uncommon (< 1%)
  • convulsions, rhabdomyolysis (rare), renal failure, disorder of ejaculation
• other
  • may induce thrombosis if used during abdominal surgery

Drug interactions

• hypercoagulaton may result from use of estrogens in combination

Laboratory

• specimen:
  • serum, plasma (heparin, EDTA)
  • collect at trough concentration
• methods: HPLC, GLC

Mechanism of action

• inhibits conversion of plasminogen to plasmin

More general terms

• fibrinolytic inhibitor

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=564