MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Amicar® may be confused with amikacin, Amikin®, Omacor®
U.S. BRAND NAMES — Amicar®
PHARMACOLOGIC CATEGORY
Antifibrinolytic Agent
Antihemophilic Agent
Hemostatic Agent
Lysine Analog
DOSING: ADULTS
Acute bleeding syndrome: Oral, I.V.: Loading dose: 4-5 g during the first hour, followed by 1 g/hour for 8 hours (or 1.25 g/hour using oral solution) or until bleeding controlled (maximum daily dose: 30 g)
Control of bleeding in thrombocytopenia (unlabeled use):
Initial: I.V.: 100 mg/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours
Control of oral bleeding in congenital and acquired coagulation disorder (unlabeled use): Oral: 50-60 mg/kg every 4 hours
Prevention of dental procedure bleeding in patients on oral anticoagulant therapy (unlabeled use): Oral rinse: Hold 4 g/10 mL in mouth for 2 minutes then spit out. Repeat every 6 hours for 2 days after procedure (Souto, 1996). Concentration and frequency may vary by institution and product availability.
Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 10 g over 20-30 minutes prior to skin incision, followed by 1-2.5 g/hour (usual dose 2 g/hour) until the end of operation (may continue infusion for 4 hours after protamine reversal of heparin). May add 10 g to cardiopulmonary bypass circuit priming solution.
or
10 g over 20-30 minutes prior to skin incision, followed by 10 g after heparin administration then 10 g at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin
Traumatic hyphema (unlabeled use): Oral: 100 mg/kg/dose every 4 hours (maximum daily dose: 30 g)
DOSING: PEDIATRIC
(For additional information see "Aminocaproic acid: Pediatric drug information")
Acute bleeding syndrome (unlabeled use): Oral, I.V.: Loading dose: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour (I.V.) or 100 mg/kg (oral or I.V.) every 6 hours
Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 100 mg/kg given over 20-30 minutes after induction and prior to incision, 100 mg/kg during cardiopulmonary bypass, and 100 mg/kg after protamine reversal of heparin
Traumatic hyphema (unlabeled use): Oral: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — May accumulate in patients with decreased renal function.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (240 mL, 480 mL)
Syrup:
Amicar®: 1.25 g/5 mL (480 mL) [raspberry flavor]
Tablet [scored]: 500 mg
Amicar®: 500 mg, 1000 mg
DOSAGE FORMS: CONCISE
Injection, solution: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (480 mL)
Syrup:
Amicar®: 1.25 g/5 mL
Tablet [scored]: 500 mg
Amicar®: 500 mg, 1000 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Rapid I.V. injection (IVP) of undiluted solution is not recommended due to possible hypotension, bradycardia, and arrhythmia.
I.V.: Acute bleeding syndrome: Administer loading dose over 1 hour, followed by a continuous infusion
I.V.: Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): Administer loading dose over 20-30 minutes prior to skin incision, followed by a continuous infusion until the end of operation or as 2 additional bolus doses (over 20-30 minutes) given after heparin administration and at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin.
COMPATIBILITY — Stable in D5W, NS, Ringer's injection
USE — To enhance hemostasis when fibrinolysis contributes to bleeding (causes may include cardiac surgery, hematologic disorders, neoplastic disorders, abruption placentae, hepatic cirrhosis, and urinary fibrinolysis)
USE - UNLABELED / INVESTIGATIONAL — Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders; topical treatment (mouth rinse) of bleeding associated with dental procedures in patients on oral anticoagulant therapy; prevention of perioperative bleeding associated with cardiac surgery
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Arrhythmia, bradycardia, edema, hypotension, intracranial hypertension, peripheral ischemia, syncope, thrombosis
Central nervous system: Confusion, delirium, dizziness, fatigue, hallucinations, headache, malaise, seizure, stroke
Dermatologic: Rash, pruritus
Gastrointestinal: Abdominal pain, anorexia, cramps, diarrhea, GI irritation, nausea, vomiting
Genitourinary: Dry ejaculation
Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia
Local: Injection site necrosis, injection site pain, injectionsite reactions
Neuromuscular & skeletal: CPK increased, myalgia, myositis, myopathy, rhabdomyolysis (rare), weakness
Ophthalmic: Vision decreased, watery eyes
Otic: Tinnitus
Renal: BUN increased, intrarenal obstruction (glomerular capillary thrombosis), myoglobinuria (rare), renal failure (rare)
Respiratory: Dyspnea, nasal congestion, pulmonary embolism
Miscellaneous: Allergic reaction, anaphylactoid reaction, anaphylaxis
Postmarketing and/or case reports: Hepatic lesion, myocardial lesion
CONTRAINDICATIONS — Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Intrarenal obstruction: May occur secondary to glomerular capillary thrombosis or clots in the renal pelvis and ureters; do not use in hematuria of upper urinary tract origin unless possible benefits outweigh risks. Skeletal muscle weakness: Ranging from mild myalgias and fatigue to severe myopathy with rhabdomyolysis and acute renal failure has been reported with prolonged use. Monitor CPK; discontinue treatment with a rise in CPK.
Disease-related concerns: Renal impairment: Use with caution in patients with renal impairment; may accumulate.
Concurrent drug therapy issues: Blood products: Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes; may increase risk for thrombosis.
Dosage form specific issues: Benzyl alcohol: Injection contains benzyl alcohol which has been associated with "gasping syndrome" in neonates.
Other warnings/precautions: Appropriate use: Do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis. Inhibition of fibrinolysis may promote clotting or thrombosis; more likely due to the presence of DIC. I.V. administration: Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia; rapid injection of undiluted solution is not recommended.
DRUG INTERACTIONS
Anti-inhibitor Coagulant Complex: Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination
Factor IX: Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX. Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination
Factor IX Complex (Human): Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX Complex (Human). Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination
Fibrinogen Concentrate (Human): Antifibrinolytic Agents may enhance the adverse/toxic effect of Fibrinogen Concentrate (Human). Specifically, the risk for thrombosis may be increased. Fibrinogen Concentrate (Human) may enhance the adverse/toxic effect of Antifibrinolytic Agents. Specifically, the risk for thrombosis may be increased. Risk C: Monitor therapy
Tretinoin (Oral): May enhance the thrombogenic effect of Antifibrinolytic Agents. Risk C: Monitor therapy
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Animal reproductive studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)
Tablets (Amicar)
500 mg (30): $103.40
Tablets (Aminocaproic Acid)
500 mg (100): $177.59
MONITORING PARAMETERS — Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy), BUN, creatinine
INTERNATIONAL BRAND NAMES — Acepramin (HU); Acidum e-aminocapronicum (PL); Amicar (AE, AU, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Caproamin (ES, VE); Caproamin Fides (ES); Caprolest (NL); Caprolisin (IT); EAC (DE); Epsamon (CH); Epsicaprom (PT); Epsilon (FI); Hamostat (IN); Hemocaprol (ES); Hexalense (FR); Ipron (TW); Ipsilon (AR, BR, JP, PY, UY); Resplamin (JP); Syrop acidi e-aminocapronici (PL)
MECHANISM OF ACTION — Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).
PHARMACODYNAMICS / KINETICS
Onset of action: ~1-72 hours
Distribution: Widely through intravascular and extravascular compartments
Vd: Oral: 23 L, I.V.: 30 L
Metabolism: Minimally hepatic
Half-life elimination: ~2 hours
Time to peak: Oral: Within 2 hours
Excretion: Urine (65% as unchanged drug, 11% as metabolite)
PATIENT INFORMATION — Report any signs of bleeding; change positions slowly to minimize dizziness
Showing posts with label Aminocaproic acid. Show all posts
Showing posts with label Aminocaproic acid. Show all posts
Aminocaproic acid
MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Amicar® may be confused with amikacin, Amikin®, Omacor®
U.S. BRAND NAMES — Amicar®
PHARMACOLOGIC CATEGORY
Antifibrinolytic Agent
Antihemophilic Agent
Hemostatic Agent
Lysine Analog
DOSING: ADULTS
Acute bleeding syndrome: Oral, I.V.: Loading dose: 4-5 g during the first hour, followed by 1 g/hour for 8 hours (or 1.25 g/hour using oral solution) or until bleeding controlled (maximum daily dose: 30 g)
Control of bleeding in thrombocytopenia (unlabeled use):
Initial: I.V.: 100 mg/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours
Control of oral bleeding in congenital and acquired coagulation disorder (unlabeled use): Oral: 50-60 mg/kg every 4 hours
Prevention of dental procedure bleeding in patients on oral anticoagulant therapy (unlabeled use): Oral rinse: Hold 4 g/10 mL in mouth for 2 minutes then spit out. Repeat every 6 hours for 2 days after procedure (Souto, 1996). Concentration and frequency may vary by institution and product availability.
Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 10 g over 20-30 minutes prior to skin incision, followed by 1-2.5 g/hour (usual dose 2 g/hour) until the end of operation (may continue infusion for 4 hours after protamine reversal of heparin). May add 10 g to cardiopulmonary bypass circuit priming solution.
or
10 g over 20-30 minutes prior to skin incision, followed by 10 g after heparin administration then 10 g at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin
Traumatic hyphema (unlabeled use): Oral: 100 mg/kg/dose every 4 hours (maximum daily dose: 30 g)
DOSING: PEDIATRIC
(For additional information see "Aminocaproic acid: Pediatric drug information")
Acute bleeding syndrome (unlabeled use): Oral, I.V.: Loading dose: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour (I.V.) or 100 mg/kg (oral or I.V.) every 6 hours
Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 100 mg/kg given over 20-30 minutes after induction and prior to incision, 100 mg/kg during cardiopulmonary bypass, and 100 mg/kg after protamine reversal of heparin
Traumatic hyphema (unlabeled use): Oral: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — May accumulate in patients with decreased renal function.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (240 mL, 480 mL)
Syrup:
Amicar®: 1.25 g/5 mL (480 mL) [raspberry flavor]
Tablet [scored]: 500 mg
Amicar®: 500 mg, 1000 mg
DOSAGE FORMS: CONCISE
Injection, solution: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (480 mL)
Syrup:
Amicar®: 1.25 g/5 mL
Tablet [scored]: 500 mg
Amicar®: 500 mg, 1000 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Rapid I.V. injection (IVP) of undiluted solution is not recommended due to possible hypotension, bradycardia, and arrhythmia.
I.V.: Acute bleeding syndrome: Administer loading dose over 1 hour, followed by a continuous infusion
I.V.: Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): Administer loading dose over 20-30 minutes prior to skin incision, followed by a continuous infusion until the end of operation or as 2 additional bolus doses (over 20-30 minutes) given after heparin administration and at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin.
COMPATIBILITY — Stable in D5W, NS, Ringer's injection
USE — To enhance hemostasis when fibrinolysis contributes to bleeding (causes may include cardiac surgery, hematologic disorders, neoplastic disorders, abruption placentae, hepatic cirrhosis, and urinary fibrinolysis)
USE - UNLABELED / INVESTIGATIONAL — Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders; topical treatment (mouth rinse) of bleeding associated with dental procedures in patients on oral anticoagulant therapy; prevention of perioperative bleeding associated with cardiac surgery
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Arrhythmia, bradycardia, edema, hypotension, intracranial hypertension, peripheral ischemia, syncope, thrombosis
Central nervous system: Confusion, delirium, dizziness, fatigue, hallucinations, headache, malaise, seizure, stroke
Dermatologic: Rash, pruritus
Gastrointestinal: Abdominal pain, anorexia, cramps, diarrhea, GI irritation, nausea, vomiting
Genitourinary: Dry ejaculation
Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia
Local: Injection site necrosis, injection site pain, injectionsite reactions
Neuromuscular & skeletal: CPK increased, myalgia, myositis, myopathy, rhabdomyolysis (rare), weakness
Ophthalmic: Vision decreased, watery eyes
Otic: Tinnitus
Renal: BUN increased, intrarenal obstruction (glomerular capillary thrombosis), myoglobinuria (rare), renal failure (rare)
Respiratory: Dyspnea, nasal congestion, pulmonary embolism
Miscellaneous: Allergic reaction, anaphylactoid reaction, anaphylaxis
Postmarketing and/or case reports: Hepatic lesion, myocardial lesion
CONTRAINDICATIONS — Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Intrarenal obstruction: May occur secondary to glomerular capillary thrombosis or clots in the renal pelvis and ureters; do not use in hematuria of upper urinary tract origin unless possible benefits outweigh risks. Skeletal muscle weakness: Ranging from mild myalgias and fatigue to severe myopathy with rhabdomyolysis and acute renal failure has been reported with prolonged use. Monitor CPK; discontinue treatment with a rise in CPK.
Disease-related concerns: Renal impairment: Use with caution in patients with renal impairment; may accumulate.
Concurrent drug therapy issues: Blood products: Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes; may increase risk for thrombosis.
Dosage form specific issues: Benzyl alcohol: Injection contains benzyl alcohol which has been associated with "gasping syndrome" in neonates.
Other warnings/precautions: Appropriate use: Do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis. Inhibition of fibrinolysis may promote clotting or thrombosis; more likely due to the presence of DIC. I.V. administration: Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia; rapid injection of undiluted solution is not recommended.
DRUG INTERACTIONS
Anti-inhibitor Coagulant Complex: Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination
Factor IX: Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX. Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination
Factor IX Complex (Human): Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX Complex (Human). Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination
Fibrinogen Concentrate (Human): Antifibrinolytic Agents may enhance the adverse/toxic effect of Fibrinogen Concentrate (Human). Specifically, the risk for thrombosis may be increased. Fibrinogen Concentrate (Human) may enhance the adverse/toxic effect of Antifibrinolytic Agents. Specifically, the risk for thrombosis may be increased. Risk C: Monitor therapy
Tretinoin (Oral): May enhance the thrombogenic effect of Antifibrinolytic Agents. Risk C: Monitor therapy
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Animal reproductive studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)
Tablets (Amicar)
500 mg (30): $103.40
Tablets (Aminocaproic Acid)
500 mg (100): $177.59
MONITORING PARAMETERS — Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy), BUN, creatinine
INTERNATIONAL BRAND NAMES — Acepramin (HU); Acidum e-aminocapronicum (PL); Amicar (AE, AU, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Caproamin (ES, VE); Caproamin Fides (ES); Caprolest (NL); Caprolisin (IT); EAC (DE); Epsamon (CH); Epsicaprom (PT); Epsilon (FI); Hamostat (IN); Hemocaprol (ES); Hexalense (FR); Ipron (TW); Ipsilon (AR, BR, JP, PY, UY); Resplamin (JP); Syrop acidi e-aminocapronici (PL)
MECHANISM OF ACTION — Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).
PHARMACODYNAMICS / KINETICS
Onset of action: ~1-72 hours
Distribution: Widely through intravascular and extravascular compartments
Vd: Oral: 23 L, I.V.: 30 L
Metabolism: Minimally hepatic
Half-life elimination: ~2 hours
Time to peak: Oral: Within 2 hours
Excretion: Urine (65% as unchanged drug, 11% as metabolite)
PATIENT INFORMATION — Report any signs of bleeding; change positions slowly to minimize dizziness
Sound-alike/look-alike issues:
Amicar® may be confused with amikacin, Amikin®, Omacor®
U.S. BRAND NAMES — Amicar®
PHARMACOLOGIC CATEGORY
Antifibrinolytic Agent
Antihemophilic Agent
Hemostatic Agent
Lysine Analog
DOSING: ADULTS
Acute bleeding syndrome: Oral, I.V.: Loading dose: 4-5 g during the first hour, followed by 1 g/hour for 8 hours (or 1.25 g/hour using oral solution) or until bleeding controlled (maximum daily dose: 30 g)
Control of bleeding in thrombocytopenia (unlabeled use):
Initial: I.V.: 100 mg/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours
Control of oral bleeding in congenital and acquired coagulation disorder (unlabeled use): Oral: 50-60 mg/kg every 4 hours
Prevention of dental procedure bleeding in patients on oral anticoagulant therapy (unlabeled use): Oral rinse: Hold 4 g/10 mL in mouth for 2 minutes then spit out. Repeat every 6 hours for 2 days after procedure (Souto, 1996). Concentration and frequency may vary by institution and product availability.
Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 10 g over 20-30 minutes prior to skin incision, followed by 1-2.5 g/hour (usual dose 2 g/hour) until the end of operation (may continue infusion for 4 hours after protamine reversal of heparin). May add 10 g to cardiopulmonary bypass circuit priming solution.
or
10 g over 20-30 minutes prior to skin incision, followed by 10 g after heparin administration then 10 g at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin
Traumatic hyphema (unlabeled use): Oral: 100 mg/kg/dose every 4 hours (maximum daily dose: 30 g)
DOSING: PEDIATRIC
(For additional information see "Aminocaproic acid: Pediatric drug information")
Acute bleeding syndrome (unlabeled use): Oral, I.V.: Loading dose: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour (I.V.) or 100 mg/kg (oral or I.V.) every 6 hours
Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 100 mg/kg given over 20-30 minutes after induction and prior to incision, 100 mg/kg during cardiopulmonary bypass, and 100 mg/kg after protamine reversal of heparin
Traumatic hyphema (unlabeled use): Oral: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — May accumulate in patients with decreased renal function.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (240 mL, 480 mL)
Syrup:
Amicar®: 1.25 g/5 mL (480 mL) [raspberry flavor]
Tablet [scored]: 500 mg
Amicar®: 500 mg, 1000 mg
DOSAGE FORMS: CONCISE
Injection, solution: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (480 mL)
Syrup:
Amicar®: 1.25 g/5 mL
Tablet [scored]: 500 mg
Amicar®: 500 mg, 1000 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Rapid I.V. injection (IVP) of undiluted solution is not recommended due to possible hypotension, bradycardia, and arrhythmia.
I.V.: Acute bleeding syndrome: Administer loading dose over 1 hour, followed by a continuous infusion
I.V.: Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): Administer loading dose over 20-30 minutes prior to skin incision, followed by a continuous infusion until the end of operation or as 2 additional bolus doses (over 20-30 minutes) given after heparin administration and at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin.
COMPATIBILITY — Stable in D5W, NS, Ringer's injection
USE — To enhance hemostasis when fibrinolysis contributes to bleeding (causes may include cardiac surgery, hematologic disorders, neoplastic disorders, abruption placentae, hepatic cirrhosis, and urinary fibrinolysis)
USE - UNLABELED / INVESTIGATIONAL — Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders; topical treatment (mouth rinse) of bleeding associated with dental procedures in patients on oral anticoagulant therapy; prevention of perioperative bleeding associated with cardiac surgery
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Arrhythmia, bradycardia, edema, hypotension, intracranial hypertension, peripheral ischemia, syncope, thrombosis
Central nervous system: Confusion, delirium, dizziness, fatigue, hallucinations, headache, malaise, seizure, stroke
Dermatologic: Rash, pruritus
Gastrointestinal: Abdominal pain, anorexia, cramps, diarrhea, GI irritation, nausea, vomiting
Genitourinary: Dry ejaculation
Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia
Local: Injection site necrosis, injection site pain, injectionsite reactions
Neuromuscular & skeletal: CPK increased, myalgia, myositis, myopathy, rhabdomyolysis (rare), weakness
Ophthalmic: Vision decreased, watery eyes
Otic: Tinnitus
Renal: BUN increased, intrarenal obstruction (glomerular capillary thrombosis), myoglobinuria (rare), renal failure (rare)
Respiratory: Dyspnea, nasal congestion, pulmonary embolism
Miscellaneous: Allergic reaction, anaphylactoid reaction, anaphylaxis
Postmarketing and/or case reports: Hepatic lesion, myocardial lesion
CONTRAINDICATIONS — Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Intrarenal obstruction: May occur secondary to glomerular capillary thrombosis or clots in the renal pelvis and ureters; do not use in hematuria of upper urinary tract origin unless possible benefits outweigh risks. Skeletal muscle weakness: Ranging from mild myalgias and fatigue to severe myopathy with rhabdomyolysis and acute renal failure has been reported with prolonged use. Monitor CPK; discontinue treatment with a rise in CPK.
Disease-related concerns: Renal impairment: Use with caution in patients with renal impairment; may accumulate.
Concurrent drug therapy issues: Blood products: Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes; may increase risk for thrombosis.
Dosage form specific issues: Benzyl alcohol: Injection contains benzyl alcohol which has been associated with "gasping syndrome" in neonates.
Other warnings/precautions: Appropriate use: Do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis. Inhibition of fibrinolysis may promote clotting or thrombosis; more likely due to the presence of DIC. I.V. administration: Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia; rapid injection of undiluted solution is not recommended.
DRUG INTERACTIONS
Anti-inhibitor Coagulant Complex: Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination
Factor IX: Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX. Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination
Factor IX Complex (Human): Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX Complex (Human). Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination
Fibrinogen Concentrate (Human): Antifibrinolytic Agents may enhance the adverse/toxic effect of Fibrinogen Concentrate (Human). Specifically, the risk for thrombosis may be increased. Fibrinogen Concentrate (Human) may enhance the adverse/toxic effect of Antifibrinolytic Agents. Specifically, the risk for thrombosis may be increased. Risk C: Monitor therapy
Tretinoin (Oral): May enhance the thrombogenic effect of Antifibrinolytic Agents. Risk C: Monitor therapy
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Animal reproductive studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)
Tablets (Amicar)
500 mg (30): $103.40
Tablets (Aminocaproic Acid)
500 mg (100): $177.59
MONITORING PARAMETERS — Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy), BUN, creatinine
INTERNATIONAL BRAND NAMES — Acepramin (HU); Acidum e-aminocapronicum (PL); Amicar (AE, AU, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Caproamin (ES, VE); Caproamin Fides (ES); Caprolest (NL); Caprolisin (IT); EAC (DE); Epsamon (CH); Epsicaprom (PT); Epsilon (FI); Hamostat (IN); Hemocaprol (ES); Hexalense (FR); Ipron (TW); Ipsilon (AR, BR, JP, PY, UY); Resplamin (JP); Syrop acidi e-aminocapronici (PL)
MECHANISM OF ACTION — Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).
PHARMACODYNAMICS / KINETICS
Onset of action: ~1-72 hours
Distribution: Widely through intravascular and extravascular compartments
Vd: Oral: 23 L, I.V.: 30 L
Metabolism: Minimally hepatic
Half-life elimination: ~2 hours
Time to peak: Oral: Within 2 hours
Excretion: Urine (65% as unchanged drug, 11% as metabolite)
PATIENT INFORMATION — Report any signs of bleeding; change positions slowly to minimize dizziness
Aminocaproic acid
U.S. BRAND NAMES — Amicar®
PHARMACOLOGIC CATEGORY
Hemostatic Agent
DOSING: ADULTS
Acute bleeding syndrome: Oral, I.V.: 4-5 g during the first hour, followed by 1 g/hour for 8 hours or until bleeding controlled (maximum daily dose: 30 g)
Control bleeding in thrombocytopenia (unlabeled use):
Initial: I.V.: 0.1 g/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours
Control oral bleeding in congenital and acquired coagulation disorder (unlabeled use): Oral: 50-60 mg/kg every 4 hours
Traumatic hyphema (unlabeled use): Oral: 100 mg/kg/dose every 4 hours (maximum daily dose: 30 g)
DOSING: PEDIATRIC
(For additional information see "Aminocaproic acid: Pediatric drug information")
Acute bleeding syndrome (unlabeled use): Oral, I.V.: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour or 100 mg/kg (oral or I.V.) every 6 hours
Traumatic hyphema (unlabeled use): Oral: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — May accumulate in patients with decreased renal function.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: 250 mg/mL (20 mL)
Amicar®: 250 mg/mL (20 mL) [contains benzyl alcohol]
Solution, oral: 1.25 g/5 mL (240 mL, 480 mL)
Syrup:
Amicar®: 1.25 g/5 mL (480 mL) [raspberry flavor]
Tablet [scored]: 500 mg, 1000 mg
Amicar®: 500 mg, 1000 mg
DOSAGE FORMS: CONCISE
Injection, solution: 250 mg/mL (20 mL)
Amicar®: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (480 mL)
Syrup:
Amicar®: 1.25 g/5 mL
Tablet [scored]: 500 mg, 1000 mg
Amicar®: 500 mg, 1000 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — I.V.: May be administered over 30-60 minutes or by continuous infusion; rapid I.V. injection (IVP) should be avoided due to possible hypotension, bradycardia, and arrhythmia.
COMPATIBILITY — Stable in D5W, NS.
Compatibility when admixed: Compatible: Netilmicin.
USE — Treatment of excessive bleeding from fibrinolysis
USE - UNLABELED / INVESTIGATIONAL — Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Arrhythmia, bradycardia, hypotension, peripheral ischemia, syncope, thrombosis
Central nervous system: Confusion, delirium, dizziness, fatigue, hallucinations, headache, intracranial hypertension, malaise, seizure, stroke
Dermatologic: Rash, pruritus
Gastrointestinal: Abdominal pain, anorexia, cramps, diarrhea, GI irritation, nausea
Genitourinary: Dry ejaculation
Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia
Neuromuscular & skeletal: CPK increased, myalgia, myositis, myopathy, rhabdomyolysis (rare), weakness
Ophthalmic: Watery eyes, vision decreased
Otic: Tinnitus
Renal: Failure (rare), myoglobinuria (rare)
Respiratory: Dyspnea, nasal congestion, pulmonary embolism
CONTRAINDICATIONS — Hypersensitivity to aminocaproic acid or any component of the formulation; disseminated intravascular coagulation (without heparin); evidence of an intravascular clotting process
WARNINGS / PRECAUTIONS — Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia. Aminocaproic acid may accumulate in patients with decreased renal function. Intrarenal obstruction may occur secondary to glomerular capillary thrombosis or clots in the renal pelvis and ureters. Do not use in hematuria of upper urinary tract origin unless possible benefits outweigh risks. Use with caution in patients with cardiac, renal, or hepatic disease. Do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis. Inhibition of fibrinolysis may promote clotting or thrombosis; more likely due to the presence of DIC. Subsequently, use with great caution in patients with, or at risk for, veno-occlusive disease of the liver. Benzyl alcohol is used as a preservative in the injection, therefore, these products should not be used in the neonate. Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes.
DRUG INTERACTIONS — Increased toxic effect with oral contraceptives, estrogens.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproductive studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)
Tablets (Amicar)
500 mg (30): $78.37
MONITORING PARAMETERS — Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy)
REFERENCE RANGE — Therapeutic concentration: >130 mcg/mL (concentration necessary for inhibition of fibrinolysis)
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include acute renal failure, delirium, diarrhea, hepatic necrosis, nausea, seizures, transient hypotension, and thromboembolism. Aminocaproic acid may be removed by hemodialysis.
INTERNATIONAL BRAND NAMES — Acidum e-aminocapronicum (PL); Amicar (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Caproamin (VE); Caprolisin (IT); Hamostat (IN); Ipsilon (AR, BR, JP, PY, UY); Resplamin (JP); Syrop acidi e-aminocapronici (PL)
MECHANISM OF ACTION — Competitively inhibits activation of plasminogen to plasmin, also, a lesser antiplasmin effect
PHARMACODYNAMICS / KINETICS
Onset of action: ~1-72 hours
Distribution: Widely through intravascular and extravascular compartments
Vd: Oral: 23 L, I.V.: 30 L
Metabolism: Minimally hepatic
Half-life elimination: 2 hours
Time to peak: Oral: Within 2 hours
Excretion: Urine (65% as unchanged drug, 11% as metabolite)
PATIENT INFORMATION — Report any signs of bleeding; change positions slowly to minimize dizziness
PHARMACOLOGIC CATEGORY
Hemostatic Agent
DOSING: ADULTS
Acute bleeding syndrome: Oral, I.V.: 4-5 g during the first hour, followed by 1 g/hour for 8 hours or until bleeding controlled (maximum daily dose: 30 g)
Control bleeding in thrombocytopenia (unlabeled use):
Initial: I.V.: 0.1 g/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours
Control oral bleeding in congenital and acquired coagulation disorder (unlabeled use): Oral: 50-60 mg/kg every 4 hours
Traumatic hyphema (unlabeled use): Oral: 100 mg/kg/dose every 4 hours (maximum daily dose: 30 g)
DOSING: PEDIATRIC
(For additional information see "Aminocaproic acid: Pediatric drug information")
Acute bleeding syndrome (unlabeled use): Oral, I.V.: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour or 100 mg/kg (oral or I.V.) every 6 hours
Traumatic hyphema (unlabeled use): Oral: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — May accumulate in patients with decreased renal function.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: 250 mg/mL (20 mL)
Amicar®: 250 mg/mL (20 mL) [contains benzyl alcohol]
Solution, oral: 1.25 g/5 mL (240 mL, 480 mL)
Syrup:
Amicar®: 1.25 g/5 mL (480 mL) [raspberry flavor]
Tablet [scored]: 500 mg, 1000 mg
Amicar®: 500 mg, 1000 mg
DOSAGE FORMS: CONCISE
Injection, solution: 250 mg/mL (20 mL)
Amicar®: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (480 mL)
Syrup:
Amicar®: 1.25 g/5 mL
Tablet [scored]: 500 mg, 1000 mg
Amicar®: 500 mg, 1000 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — I.V.: May be administered over 30-60 minutes or by continuous infusion; rapid I.V. injection (IVP) should be avoided due to possible hypotension, bradycardia, and arrhythmia.
COMPATIBILITY — Stable in D5W, NS.
Compatibility when admixed: Compatible: Netilmicin.
USE — Treatment of excessive bleeding from fibrinolysis
USE - UNLABELED / INVESTIGATIONAL — Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Arrhythmia, bradycardia, hypotension, peripheral ischemia, syncope, thrombosis
Central nervous system: Confusion, delirium, dizziness, fatigue, hallucinations, headache, intracranial hypertension, malaise, seizure, stroke
Dermatologic: Rash, pruritus
Gastrointestinal: Abdominal pain, anorexia, cramps, diarrhea, GI irritation, nausea
Genitourinary: Dry ejaculation
Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia
Neuromuscular & skeletal: CPK increased, myalgia, myositis, myopathy, rhabdomyolysis (rare), weakness
Ophthalmic: Watery eyes, vision decreased
Otic: Tinnitus
Renal: Failure (rare), myoglobinuria (rare)
Respiratory: Dyspnea, nasal congestion, pulmonary embolism
CONTRAINDICATIONS — Hypersensitivity to aminocaproic acid or any component of the formulation; disseminated intravascular coagulation (without heparin); evidence of an intravascular clotting process
WARNINGS / PRECAUTIONS — Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia. Aminocaproic acid may accumulate in patients with decreased renal function. Intrarenal obstruction may occur secondary to glomerular capillary thrombosis or clots in the renal pelvis and ureters. Do not use in hematuria of upper urinary tract origin unless possible benefits outweigh risks. Use with caution in patients with cardiac, renal, or hepatic disease. Do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis. Inhibition of fibrinolysis may promote clotting or thrombosis; more likely due to the presence of DIC. Subsequently, use with great caution in patients with, or at risk for, veno-occlusive disease of the liver. Benzyl alcohol is used as a preservative in the injection, therefore, these products should not be used in the neonate. Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes.
DRUG INTERACTIONS — Increased toxic effect with oral contraceptives, estrogens.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproductive studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)
Tablets (Amicar)
500 mg (30): $78.37
MONITORING PARAMETERS — Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy)
REFERENCE RANGE — Therapeutic concentration: >130 mcg/mL (concentration necessary for inhibition of fibrinolysis)
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include acute renal failure, delirium, diarrhea, hepatic necrosis, nausea, seizures, transient hypotension, and thromboembolism. Aminocaproic acid may be removed by hemodialysis.
INTERNATIONAL BRAND NAMES — Acidum e-aminocapronicum (PL); Amicar (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Caproamin (VE); Caprolisin (IT); Hamostat (IN); Ipsilon (AR, BR, JP, PY, UY); Resplamin (JP); Syrop acidi e-aminocapronici (PL)
MECHANISM OF ACTION — Competitively inhibits activation of plasminogen to plasmin, also, a lesser antiplasmin effect
PHARMACODYNAMICS / KINETICS
Onset of action: ~1-72 hours
Distribution: Widely through intravascular and extravascular compartments
Vd: Oral: 23 L, I.V.: 30 L
Metabolism: Minimally hepatic
Half-life elimination: 2 hours
Time to peak: Oral: Within 2 hours
Excretion: Urine (65% as unchanged drug, 11% as metabolite)
PATIENT INFORMATION — Report any signs of bleeding; change positions slowly to minimize dizziness
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