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aminocaproic acid (Amicar)

Tradename: Amicar. Indications: 1) life-threatening hemorrhage secondary to fibrinolysis resulting from trauma a) systemic fibrinolysis b) urinary fibrinolysis 2) hemorrhage due to platelet defects [4] - Bernard Soulier disease - Glanzmann's thrombasthenia - Wiskott-Aldrich syndrome - gray platelet syndrome - granule storage pool defects - uremia - liver disease [4] 3) hemorrhagic telangiectasia 4) hemophilia 5) surgical hemostatis Contraindications: 1) disseminated intravascular coagulation (DIC) 2) hematuria Dosage: 1) 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 2) 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: 1) peak effects occur within 2 hours of oral dose 2) therapeutic effects occur within 1-72 hours of administration Adverse effects: 1) 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 2) uncommon (< 1%) - convulsions, rhabdomyolysis (rare), renal failure, disorder of ejaculation 3) other - may induce thrombosis if used during abdominal surgery [4] Drug interactions: - hypercoagulaton may result from use of estrogens in combination Laboratory: 1) specimen: a) serum, plasma (heparin, EDTA) b) collect at trough concentration 2) methods: HPLC, GLC Mechanism of action: - inhibits conversion of plasminogen to plasmin

General

fibrinolytic inhibitor

Properties

MISC-INFO: elimination route KIDNEY 1/2life 1-2 HOURS therapeutic-range 100-400 UG/ML protein-binding <5% elimination by hemodialysis + pregnancy-category D safety in lactation ?

Database Correlations

PUBCHEM cid=564

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Medical Knowledge Self Assessment Program (MKSAP) 11, 17. American College of Physicians, Philadelphia 1998, 2015
  5. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
  6. Deprecated Reference