aminocaproic acid, Amicar

 Indications

Management of acute, life-threatening hemorrhage due

to systemic hyperfibrinolysis or urinary fibrinolysis.

Unlabeled Use: Prevention of recurrent subarachnoid hemorrhage. Prevention of bleeding following oral A

surgery in hemophiliacs. Management of severe hemorrhage

caused by thrombolytic agents.

Action

Inhibits activation of plasminogen. Therapeutic Effects:

Inhibition of fibrinolysis. Stabilization of clot

formation.

Pharmacokinetics

Absorption: Rapidly absorbed following oral administration.

Distribution: Widely distributed.

Metabolism and Excretion: Mostly eliminated

unchanged by the kidneys.

Half-life: Unknown.

TIME/ACTION PROFILE (peak blood levels)

ROUTE ONSET PEAK DURATION

PO unknown 2 hr N/A

IV unknown 2 hr N/A

Contraindications/Precautions

Contraindicated in: Active intravascular clotting.

Use Cautiously in: Upper urinary tract bleeding;

Cardiac, renal, or liver disease (dosage reduction may

be required); Disseminated intravascular coagulation

(should be used concurrently with heparin); OB, Lactation:

Safety not established; Pedi: Do not use products

containing benzyl alcohol with neonates.

Adverse Reactions/Side Effects

CNS: dizziness, malaise. EENT: nasal stuffiness, tinnitus.

CV: arrhythmias, hypotension (IV only). GI: anorexia,

bloating, cramping, diarrhea, nausea. GU: diuresis,

renal failure. MS: myopathy.

Interactions

Drug-Drug: Concurrent use with estrogens, conjugated

may result in a hypercoagulable state. Concurrent

use with clotting factors mayqrisk of thromboses.

Route/Dosage

Acute Bleeding Syndromes due to Elevated

Fibrinolytic Activity

PO (Adults): 5 g 1st hr, followed by 1–1.25 g q hr for

8 hr or until hemorrhage is controlled; or 6 g over 24

hr after prostate surgery (not 30 g/day).

IV (Adults): 4–5 g over 1st hr, followed by 1 g/hr for

8 hr or until hemorrhage is controlled; or 6 g over 24

hr after prostate surgery (not 30 g/day).

PO, IV (Children): 100 mg/kg or 3 g/m2 over 1st hr,

followed by continuous infusion of 33.3 mg/kg/hr; or 1

g/m2/hr (total dose not 18 g/m2/24 hr). 

Subarachnoid Hemorrhage

PO (Adults): To follow IV—3 g q 2 hr (36 g/day). If

no surgery is performed, continue for 21 days after

bleeding stops, then decrease to 2 g q 2 hr (24 g/day)

for 3 days, then 1 g q 2 hr (12 g/day) for 3 days.

IV (Adults): 36 g/day for 10 days followed by PO.

Prevention of Bleeding Following Oral

Surgery in Hemophiliacs

PO (Adults): 75 mg/kg (up to 6 g) immediately after

procedure, then q 6 hr for 7–10 days; syrup may also

be used as an oral rinse of 1.25 g (5 mL) 4 times a day

for 7–10 days.

IV, PO (Children): Also for epistaxis—50–100 mg/

kg/dose administered IV every 6 hr for 2–3 days starting

4 hr before the procedure. After completion of IV

therapy, aminocaproic acid should be given as 50–100

mg/kg/dose orally every 6 hr for 5–7 days.

Availability

Tablets: 500 mg, 1000 mg. Syrup (raspberry flavor):

1.25 g/5 mL. Injection: 250 mg/mL.