Aminocaproic acid - instructions for use, dose, side effects, contraindications

Aminocaproic acid refers to the synthetic analogues of lysine. It inhibits fibrinolysis, competitively saturating the lysine-binding receptors, through which plasminogen (plasmin) binds to fibrinogen (fibrin). The drug also inhibits biogenic polypeptides - kinins (inhibits the activating action of streptokinase, urokinase, tissue kinases for fibrinolysis), neutralizes the effects of kallikrein, trypsin and hyaluronidase, reduces the permeability of capillaries. Aminocaproic acid has anti-allergic effect, enhances detoxifying function of the liver, inhibits antibody formation.

Pharmacokinetics:

With intravenous administration, the effect is manifested after 15-20 minutes. Absorption - high, C_m_Oh - 2 hours, half-life (T_1/2) -4 hours. It is excreted by the kidneys - 40-60% unchanged. If there is a violation of the excretory function of the kidneys, delayed excretion of aminocaproic acid occurs, and as a result, its concentration in the blood sharply increases.

Indications:

Bleeding (hyperfibrinolysis, hypo- and afibrinogenemia), bleeding during surgical interventions and pathological conditions, accompanied by increased fibrinolytic activity of the blood (with neurosurgical, intracavitary, thoracic, gynecological and urological operations, including prostate gland, lungs, pancreas; tonsillectomy, after dental interventions, in operations using the device of artificial circulation). Diseases of internal organs with hemorrhagic syndrome. Premature detachment of the placenta, prolonged retention in the uterine cavity of the dead fetus, complicated abortion. Prevention of secondary hypofibrinogenemia in massive transfusions of canned blood.

Contraindications:

Hypersensitivity to the drug, a tendency to thrombosis and thromboembolic diseases, hypercoagulability (thrombosis, thromboembolism), coagulopathy due to diffuse intravascular coagulation, impaired cerebral circulation, pregnancy.

Carefully:

Hypotension, bleeding from the upper urinary tract (due to the risk intrarenal obstruction due to thrombosis of glomerular capillaries or formation of clots within the lumen of the renal pelvis and ureter; application in this case is only possible if the expected benefit outweighs the potential risk), subarachnoid hemorrhage, hepatic insufficiency , impaired renal function.

Pregnancy and lactation:

The use of the drug during pregnancy is contraindicated. Data on the use of aminocaproic acid in pregnant women are limited. In animal studies, fertility disorders and a teratogenic effect were detected with aminocaproic acid.

There are no data on excretion of aminocaproic acid in breast milk, and therefore, the period of treatment should abandon breastfeeding.

Dosing and Administration:

Intravenously, drip. When the need to achieve a rapid effect (acute gipofibrinogenemia) was added to 100 ml of a 5% solution at a rate of 50-60 drops per minute for 15-30 minutes. During the first hour is administered at a dose of 5.4 g of (80-100 ml), and then, if necessary, 1 g (20 ml) every hour for about 8 hours or until the bleeding stops.In the case of continuing or repeated bleeding, an infusion of 5% aminocaproic acid solution is repeated every 4 hours.

Children, at the rate of 100 mg / kg - in 1 hour, then 33 mg / kg / h; the maximum daily dose is 18 g / m body surface. The daily dose for adults is 5-30 g. The daily dose for children under 1 year is 3 g; 2-6 years - 3-6 g; 7-10 years - 6-9 g, from 10 years - as for adults. In acute blood loss: children under 1 year - 6 g, 2-4 years - 6-9 g, 5-8 years - 9-12 g, 9-10 years - 18 g. Duration of treatment - 3-14 days.

Side effects:

The most frequently reported occurrence of dizziness, lower blood pressure (including orthostatic arterial hypotension) and headache.

Cases of myopathy and randomisation were usually reversible after discontinuation of treatment, but creatine phosphokinase (CK) should be monitored in patients receiving long-term aminocaproic acid treatment and discontinuing treatment if the CK is increased.

System of organs	Often (≥1/100 <1/10)	Infrequently (≥1/1,000 <1/100)	Rarely (≥1/10,000 <1/1,000)	Very rarely (<1 / 10,000)	Frequency unknown
Blood and lymphatic system		agranulocytosis, coagulation disorders			leukopenia, thrombocytopenia
The immune system		allergic and anaphylactic reactions			maculopapular rashes
Nervous system	dizziness			confusion, convulsions, delirium, hallucinations, increased intracranial pressure, impaired cerebral circulation, fainting
The organs of sight			decreased visual acuity, lacrimation
Hearing organs	noise in ears
Cardiovascular system	lowering of blood pressure	bradycardia	peripheral tissue ischemia		thrombosis, subendocardial hemorrhage
Respiratory system and thoracic organs	nasal congestion	dyspnea	pulmonary embolism		inflammation of the upper respiratory tract
Gastrointestinal tract	abdominal pain, diarrhea, nausea, vomiting
Skin and subcutaneous tissue		itching, rash
Musculoskeletal and connective tissue		muscle weakness, myalgia	increased activity of CK, myositis		acute myopathy, randomisation, myoglobinuria
Kidneys and urinary tract					acute renal failure, increased blood urea nitrogen, renal colic, impaired renal function
Genital organs					Dry ejaculation
General disorders and disorders at the site of administration	headache, general weakness; pain and necrosis at the site of administration	edema

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

Symptoms: lowering of blood pressure, convulsions, acute renal failure.

Treatment: discontinuation of the drug, symptomatic therapy.

Aminocaproic acid is excreted in hemodialysis and peritoneal dialysis.

Interaction:

You can combine with the introduction of hydrolysates, a solution of glucose (dextrose), anti-shock solutions. In acute fibrinolysis, fibrinogen should additionally be administered in an average daily dose of 2-4 g (maximum dose of 8 g).

Do not mix aminocaproic acid with solutions containing levulose, penicillin, and blood products.

Decrease in efficacy with simultaneous reception of anticoagulants of direct and indirect action, antiplatelet agents.

Simultaneous use of aminocaproic acid with concentrates prothrombin complex, preparations of coagulation factor IX and estrogens may increase the risk of thrombosis.

Aminocaproic acid inhibits the action of plasminogen activators and, to a lesser extent, plasmin activity.

Special instructions:

When prescribing a drug, it is required to establish a source of bleeding and to control fibrinolytic activity of blood and concentration fibrinogen in the blood.It is necessary to control the coagulogram, especially in ischemic heart disease, after myocardial infarction, in pathological processes in the liver.

It is not recommended to use aminocaproic acid in women to prevent increased bleeding in childbirth due to an increased risk of thrombosis in the postpartum period.

With rapid administration, it is possible to develop arterial hypotension, bradycardia, and heart rhythm disturbances.

In rare cases, after long-term use, the lesion of skeletal muscles with necrosis of muscle fibers is described. Clinical manifestations can range from mild myalgia and muscle weakness to severe proximal myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure. It is necessary to monitor CK in patients who have undergone long-term treatment. The use of aminocaproic acid should be discontinued if there is an increase in CK. When there is myopathy, it is necessary to consider the possibility of myocardial damage.

The use of aminocaproic acid may alter the results of studies of platelet function.

Effect on the ability to drive transp. cf. and fur:

Data are not available due to the exclusive use of the drug in a hospital setting.

Form release / dosage:

Solution for infusions 5%.

Packaging:

100, 250, 500 or 1000 ml in polymeric containers of infusion solutions for polyvinyl chloride single use sterile KPIR two ports. Each container is placed in a bag of polyethylene or polyethylene-polyamide films (double sterile vacuum packaging).

Containers in the bags are placed in a box made of corrugated cardboard strips: 50, 75 pieces (100 ml) at 24, 36 pieces (250 ml) at 12, 18 pieces (500 ml) for 6, 9 pieces (1000 ml ). The box with bags put instructions for medical use the drug and guidance on the use of infusion solutions in polymeric containers rate of 1 piece of 6 containers (for hospitals).

Storage conditions:

In the dark place at a temperature of 0 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:For hospitals

Registration number:LP-002616

Date of registration:05.09.2014

Expiration Date:05.09.2019

The owner of the registration certificate:PLANT MEDSINTEZ, LLC PLANT MEDSINTEZ, LLC Russia

Manufacturer: & nbsp

PLANT MEDSINTEZ, LLC Russia

Information update date: & nbsp07.08.2017

Illustrated instructions

Instructions

Aminocaproic acid (Aminocaproic acid)