aminocaproic acid (Rx)

Frequency Not Defined

Confusion

Vision decrease

Vomiting

Headache

Convulsions

Malaise

Muscle weakness

Dizziness

Tinnitus

Nausea

Bradycardia

Thrombosis

Edema

Hypotension

Stroke

Syncope

Intracranial hypertension

Peripheral ischemia

Pulmonary embolism

Dyspnea

Congestion

Diarrhea

Abdominal pain

Leukopenia

Agranulocytosis

Coagulation disorder

Dry ejaculation

Injection site reactions (pain/necrosis)

Myopathy

Pruritus

Rash

Renal failure

Anaphylaxis

Contraindications

In presence of DIC without concomitant heparin

Evidence of active intravascular clotting process

Cautions

Use cautioni in renal/cardiac/hepatic impairment

In patients with upper urinary tract bleeding, therapy has been known to cause intrarenal obstruction in form of glomerular capillary thrombosis or clots in renal pelvis and ureters; for this reason, drug should not be used in hematuria of upper urinary tract origin, unless possible benefits outweigh risks

Avoid rapid IV administration

Therapy inhibits both action of plasminogen activators and to a lesser degree, plasmin activity; drug should not be administered without a definite diagnosis and/or laboratory finding indicative of hyperfibrinolysis (hyperplasminemia)

Preservative benzyl alcohol linked to fatal "Gasping Syndrome" in premature neonates

Skeletal muscle weakness with necrosis of muscle fibers reported following prolonged administration (rare); Clinical presentation may range from mild myalgias with weakness and fatigue to severe proximal myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure; muscle enzymes, especially creatine phosphokinase (CPK) are elevated; monitor CPK levels in patients on long-term therapy; stop therapy if rise in CPK noted; resolution follows discontinuation of therapy; however, syndrome may recur if therapy restarted

Inhibition of fibrinolysis may theoretically result in clotting or thrombosis; there is no definite evidence that therapy has been responsible for few reported cases of intravascular clotting which followed treatment; rather, it appears that intravascular clotting was most likely due to patient's preexisting clinical condition, eg, the presence of DIC; it has been postulated that extravascular clots formed in vivo may not undergo spontaneous Iysis as do normal clots

Therapy should not be administered with Factor IX Complex concentrates or Anti-Inhibitor Coagulant concentrates, as risk of thrombosis may increase

Reports have appeared in literature of increased incidence of certain neurological deficits,j including hydrocephalus, cerebral ischemia, or cerebral vasospasm associated with use of antifibrinolytic agents in treatment of subarachnoid hemorrhage (SAH); all of these events have also been described as part of the natural course of SAH, or as a consequence of diagnostic procedures such as angiography; drug relatedness remains unclear

Differentiate primary fibrinolysis from disseminated intravascular coagulation (DIC)

• When there is uncertainty as to whether cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (DIC), distinction must be made before administering therapy

• The following tests can be applied to differentiate the two conditions:

  • Platelet count is usually decreased in DIC but normal in primary fibrinolysis
  • Protamine paracoagulation test is positive in DIC; a precipitate forms when protamine sulfate is dropped into citrated plasma; the test is negative in presence of primary fibrinolysis
  • The euglobulin clot Iysis test is abnormal in primary fibrinolysis but normal in DIC

Pregnancy Category: C

Lactation: Not known whether excreted in breast milk, use caution

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Inhibits fibrinolysis through inhibition of plasminogen binding to fibrin and subsequent conversion to plasmin, which in turn inhibits fibrinolysis

Exhibits antiplasmin activity

Pharmacokinetics

Onset: 1-72 hr

Duration: 3-4 hr (after 1 dose)

Half-Life: 2 hr

Vd: 23 L (PO), 30 L (IV)

Metabolism: Liver

Metabolites: Adipic acid

Clearance: 169 mL/min

Time to peak: Within 2 hr (PO)

Excretion: urine (65%)

Dialyzable: HD: yes

IV Compatibilities

Solution: D5W, NS, Ringer's

Additive: netilmicin

Y-site: fenoldopam

IV Administration

Initial 5 g in 250 mL over 1 hr, each subsequent gram in 50-100 mL at 1 g/hr

Rapid injection undiluted into a vein is not recommended

Continue for about 8 hr or until bleeding has been controlled

Storage

Store between 15-30°C (59-86°F)

Do not freeze