Aspartic acid. Experience of using the oral form of L-ornithine-L-aspartate for hyperammonemia in patients with chronic liver diseases at the pre-cirrhotic stage. Mechanism of action of l-ornithine aspartate

Included in the preparations

ATX:

A.05.B.A.06 Ornithine oxoglurate

Pharmacodynamics:

Ornithine acts as a catalyst for the enzymes carbamoylphosphate synthetase and ornithine carbamoyltransferase, and is also the basis for the synthesis of urea. In addition, the drug reduces the level of ammonia in the body due to tylation of ammonium groups in synthesis urea (in the ornithine Krebs urine cycle).

The drug also promotes the production growth hormone and insulin, improves protein metabolism.

Reduces the concentration of ammonia in the blood plasma, promotes normalization acid-base state body and the production of insulin and growth hormone. Improves protein metabolism in diseases that require parenteral nutrition.

Pharmacokinetics:

When ornithine is taken orally, aspartate dissociates into its constituent components (and aspartate), which are absorbed into the small intestine by active transport through the intestinal epithelium.

It is excreted in urine through the urea cycle.

Indications:

Spicy and chronic diseases liver (hepatitis, liver cirrhosis, hepatic encephalopathy (latent and severe), including in the composition complex therapy in case of impaired consciousness (precoma or coma), which is accompanied by hyperammonemia.

Hyperammonemia.

Dynamic study of pituitary gland function.

As a corrective additive to parenteral nutrition preparations for patients with protein deficiency.

IV.E40-E46.E46 Protein-energy malnutrition, unspecified

XI.K70-K77.K72 Liver failure, not classified elsewhere

IV.E70-E90.E72.2 Disorders of the urea cycle

XI.K70-K77.K74 Fibrosis and cirrhosis of the liver

XI.K70-K77.K76.9 Liver disease, unspecified

Contraindications:

Expressed renal failure(creatinine concentration more than 3 mg per 100 ml).

Hypersensitivity.

Lactation.

Childhood up to 18 years old.

Carefully:

Pregnancy.

Pregnancy and lactation:

If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.

Directions for use and dosage:

Inside, intravenously, intramuscularly.

Orally: after meals, 3 g of granulate, previously dissolved in 200 ml of liquid, 2-3 times a day.

Intramuscularly: 2-6 g per day, 1-2 times a day.

Intravenous drip: dose, duration and frequency of infusions, duration of treatment are determined individually, usually 20 g per day (pre-diluted in 500 ml infusion solution, maximum speed infusion - 5 g per hour or 40 drops per minute); it is possible to increase the dose to 40 g per day.

Intravenously in a stream of 2-4 g 1-2 times a day.

Side effects:

Skin reactions.

Nausea.

Vomit.

Overdose:

Symptoms: increased severity of dose-dependent side effects. Treatment: the drug should be stopped, gastric lavage, activated carbon, symptomatic treatment.

Interaction:

Preparation f pharmaceutically incompatible(R solutions cannot be mixed in one syringe)with vitamin K, benzathine benzylpenicillin, diazepam, meprobamate, phenobarbital, rifampicin, ethionamide.

Special instructions:

If nausea or vomiting occurs, the rate of administration should be optimized.

When using a certain dosage form Ornithine should be used in accordance with specific indications.

The course of treatment can be repeated every 2-3 months.

When administering the drug in high doses, the concentration of urea in the blood plasma and urine should be monitored.

Impact on the ability to drive vehicles and operate machinery

The drug may cause a slowdown in the speed of psychomotor reactions and impaired concentration.

Instructions

Rp: Sol. Ornithini aspartat 5.0 - 10 ml
D.t.d.N. 5 in amp.
S. According to the scheme.

pharmachologic effect

Hypoammonemic agent. Reduces increased level ammonia in the body, in particular in liver diseases. The action is associated with participation in the ornithine cycle of Krebs urea formation (the formation of urea from ammonia). Promotes the production of insulin and growth hormone. Improves protein metabolism in diseases requiring parenteral nutrition.
Ornithine aspartate in the body dissociates into the amino acids ornithine and aspartate, which are absorbed in the small intestine by active transport through the intestinal epithelium. Excreted in urine.

Mode of application

For adults: Inside. Dissolve the contents of 1-2 packets of Hepa-Merz in large quantities liquid (in particular a glass of water or juice) and take during or after meals up to 3 times a day.
IV. Often the dosage is up to 4 ampoules (40 ml) per day. In case of precoma or coma, administer up to 8 ampoules (80 ml) over 24 hours, depending on the severity of the condition. Before administration, add the contents of the ampoule to 500 ml of solution, but do not dissolve more than 6 ampoules in 500 ml infusion solution.
The highest rate of administration of L-ornithine-L-aspartate is 5 g/h (which corresponds to the contents of 1 ampoule).
The period of treatment with Hepa-Merz is determined by the doctor depending on clinical condition patient.

Indications

Treatment of patients with concomitant diseases and complications caused by impaired detoxification function of the liver (in particular in liver cirrhosis) with symptoms of latent or severe hepatic encephalopathy
- especially disturbances of consciousness (precoma, coma).

Contraindications

Acute and chronic liver diseases accompanied by hyperammonemia. Hepatic encephalopathy.
- For dynamic study of the function of the pituitary gland.
- As a corrective additive to drugs for parenteral nutrition in patients with protein deficiency.
- Expressed disorders renal function (serum creatinine content more than 3 mg/100 ml).
- If nausea or vomiting occurs, the rate of administration should be optimized.
- When using a particular dosage form of ornithine, compliance with the specific indications must be observed.
- Impact on the ability to drive vehicles and operate machinery
- Ornithine can cause disturbances in concentration and speed of psychomotor reactions.

Side effects

From the gastrointestinal tract: rarely (>1/10,000,<1/1000) — тошнота, рвота, боль в желудке, метеоризм, диарея.
- From the musculoskeletal system: very rarely (<1/10 000) — боль в суставах.
- These adverse reactions are often short-lived and do not require discontinuation of the drug. They disappear when the dosage or rate of administration of the drug is reduced.
- Allergic reactions are possible.

Release form

Gran. 3 g/5 g package 5 g, No. 30, No. 50, No. 100
Ornithine aspartate 3 g/5 g.
Other ingredients: anhydrous citric acid, sodium saccharin, sodium cyclamate, povidone 25, fructose, lemon flavor, orange flavor, yellow-orange dye S (E110).

Conc. d/r-ra d/inf. 5 g amp. 10 ml, no. 10
Ornithine aspartate 0.5 g/ml.
Other ingredients: water for injection.

ATTENTION!

The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to provide healthcare workers with additional information about certain medications, thereby increasing their level of professionalism. Use of the drug " Ornithine aspartate“mandatorily requires consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.

2,5-diaminopentanoic acid

Chemical properties

Ornithine – diaminovaleric acid . Structural formula of the chemical compound: NH2CH2CH2CH2CH(NH2)COOH. In peptide sequences, the substance is designated Orn. The drug is present in free form in living organisms and is a component of some.

If carbon monoxide 4 is split off from a molecule of diaminovaleric acid (the reaction occurs during the process of decay of a corpse), then putrescine – one of the main components of cadaveric poison. L-ornithine (L-ornithine) is an optical isomer of this substance. It was first synthesized from shark liver tissue in 1937. The amino acid is colorless crystals that are easily soluble in water and alcohol, and sparingly soluble in ether. Molecular mass of chemical compound = 132.2 grams per mole. About 50 tons of this lek are produced annually in the world. facilities.

In the composition of various drugs, the substance is most often found in the form ketoglutarate or aspartate .

pharmachologic effect

Hepatoprotective , detoxification , hypoazotemic .

Pharmacodynamics and pharmacokinetics

Ornithine takes part in synthesis processes urea (V ornithine cycle ), promotes the utilization of ammonium groups, reduces the concentration ammonia in blood. Thanks to this drug, the body's acid-base balance is normalized and growth hormone is produced.

If you use the medicine for diseases that require parenteral nutrition, it significantly improves protein metabolism.

After taking the drug orally ornithine aspartate dissociates into aspartate And ornithine , which are quickly and completely absorbed in the small intestine using active transport reactions through epithelial tissues. The medicine is excreted through the kidneys with urine during the urea cycle.

Indications for use

The drug is prescribed:

  • at hyperammonemia ;
  • patients with or;
  • with latent or pronounced hepatic encephalopathy ;
  • as part of complex treatment of disorders of consciousness ( precoms i) due to hepatic encephalopathy ;
  • as an additive to parenteral nutrition for patients with protein deficiency;
  • for diagnostics, dynamic study of work.

Contraindications

L-ornithine contraindicated for use:

  • for this substance;
  • patients with severe renal failure ( creatinine more than 3 mg per 100 ml).

Side effects

Ornithine is well tolerated. Rarely, allergic skin rashes, vomiting, nausea may occur. If allergies occur, it is recommended to consult a doctor.

Ornithine, instructions for use (Method and dosage)

The drug is prescribed intravenously, orally or intramuscularly.

Intravenously, the medicine is prescribed as infusions. The dosage regimen, frequency and duration of infusion depend on various parameters and are determined by the attending physician individually. Typically 20 grams of the substance are dissolved in 500 ml infusion solution . The maximum speed at which the medicine can be administered is 5 grams per hour. The maximum daily dosage is 40 g.

Overdose

There is no information about an overdose of the drug.

Interaction

Ornithine is not pharmaceutically compatible with benzylpenicillin benzathine , , , And ethionamide .

The medicine should not be mixed in the same syringe with and benzathine benzylpenicillin .

Terms of sale

No recipe needed.

special instructions

If vomiting or nausea occurs during intravenous administration of the drug, it is recommended to reduce the infusion rate.

It is necessary to strictly observe the compliance of the specific dosage form of the drug with the indications for use.

During pregnancy and lactation

Only the attending physician can prescribe medicine to pregnant women according to direct indications. It is recommended to stop breastfeeding, as the drug is excreted in milk.

Drugs containing (Analogs)

Level 4 ATX code matches:

Structural analogues of this substance: , Ornilatex , Larnamine , Ornitsetil . Also lek. the product is included in: solution for infusion Aminoplasmal Hepa , Aminoplasmal E , .

Aspartic acid is a non-essential acidic amino acid. This endogenous substance plays an important role for the proper functioning of the nervous and endocrine systems, and also promotes the production of certain hormones (growth hormone, testosterone, progesterone). Contained in proteins, it acts on the body as an stimulating neurotransmitter of the central nervous system. In addition, it is used as dietary supplements, an antibacterial agent, and is part of detergents. Brought out in 1868 from asparagus.

general characteristics

Natural aspartic acid with the formula C4H7NO4 is colorless crystals with a high melting point. Another name for the substance is aminosuccinic acid.

All amino acids used by humans for protein synthesis (except ) have 2 forms. And only the L-form is used for protein synthesis and muscle growth. The D-shape can also be used by humans, but it performs slightly different functions.

The aspartic amino acid also exists in 2 configurations. L-aspartic acid is more common and is involved in many biochemical processes. The biological role of the D-form is not as diverse as its mirror isomer. The body, as a result of enzymatic activity, is able to produce both forms of the substance, which then form the so-called racemic mixture of DL-aspartic acid.

The highest concentration of the substance is found in brain cells. By influencing the central nervous system, it increases concentration and learning abilities. At the same time, researchers say that an increased concentration of the amino acid is found in the brains of people suffering from epilepsy, but in people with depression, on the contrary, it is much less.

Aspartic acid, reacting with another amino acid, forms aspartame. This artificial sweetener is actively used in the food industry, and acts as an irritant on the cells of the nervous system. For this reason, doctors do not recommend frequent use of aspartic acid supplements, especially for children whose nervous systems are more sensitive. They may develop autism against the background of aspartates. The amino acid can also affect women’s health and regulate the chemical composition of follicular fluid, which affects reproductive potential. And frequent consumption of aspartates by pregnant women can negatively affect the health of the fetus.

Role in the body:

  1. Aspartic acid is important in the formation of other amino acids such as asparagine, and.
  2. Relieves chronic fatigue.
  3. Important for the transport of minerals necessary for the formation and functioning of DNA and RNA.
  4. Strengthens the immune system by promoting the production of antibodies and immunoglobulins.
  5. It has a positive effect on the functioning of the central nervous system, maintains concentration, and sharpens brain function.
  6. Helps remove toxins from the body, including ammonia, which has an extremely negative effect on the functioning of the brain, nervous system and liver.
  7. Under stress, the body needs additional doses of amino acids.
  8. It is an effective remedy against depression.
  9. Helps convert carbohydrates into energy.

Differences between forms

On dietary supplement labels, amino acids L and D forms are often referred to by a common name - aspartic acid. But still, structurally, both substances differ from each other, and each of them plays its own role in the body.

The L-form is present in our body more abundantly, helps synthesize proteins and cleanse the body of excess ammonia. The D form of aspartic acid is found in small quantities in the body of adults and is responsible for hormone production and brain function.

Even though both variants of the amino acid are created from identical components, the atoms within the molecule are connected in such a way that the L and D forms are mirror images of each other. Both have a central nucleus and a group of atoms attached to the side. The L-form has a group of atoms attached to the left, while its mirror image has a group of atoms attached to the right. It is these differences that are responsible for the polarity of the molecule and determine the functions of amino acid isomers. True, the L-form, when entering the body, is often transformed into the D-isomer. Meanwhile, as experiments have shown, the “transformed” amino acid does not affect testosterone levels.

Role of the L-isomer

Almost all amino acids have two isomers - L and D. L-amino acids are primarily used for the production of proteins. The same function is performed by the L-isomer of aspartic acid. In addition, this substance promotes the process of urine formation and helps remove ammonia and toxins from the body. In addition, like other amino acids, this substance is important for glucose synthesis and energy production. L-form aspartic acid is also known to be involved in the creation of molecules for DNA.

Benefits of D-isomer

The D-form of aspartic acid is primarily important for the functioning of the nervous and reproductive systems. Concentrated mainly in the brain and genitals. Responsible for the production of growth hormone and also regulates testosterone synthesis. And against the background of increased testosterone, endurance increases (this property of acid is actively used by bodybuilders), and libido also increases. Meanwhile, this form of aspartic acid in no way affects the structure and volume of muscles.

Studies have shown that testosterone levels increase significantly in people taking the D-isomer of the amino acid for 12 days. Scientists argue whether the D-form of this substance is needed as a dietary supplement for people under 21 years of age, but there is no consensus yet.

In addition, studies have shown that the level of D-aspartic acid in brain tissue increases steadily until the age of 35, then the reverse process begins - a decrease in the concentration of the substance.

Although D-aspartic acid is rarely associated with protein structures, it has been found that this substance is found in cartilage and enamel, can accumulate in brain tissue, and is also present in the membranes of red blood cells. Moreover, in the embryonic brain the amount of this amino acid is 10 times greater than in the adult brain. Scientists also compared the composition of the brain of a healthy person and those with Alzheimer's disease. It turned out that in patients the concentration of aspartic acid was higher, but deviations from the norm were recorded only in the white matter of the brain. It is also interesting that in older people the concentration of the D-isomer in the hippocampus (dentate gyrus of the brain) is significantly lower than in young people.

Daily norms

Scientists continue to study the effect of aspartic acid on humans.

The safe norm is currently 312 mg of the substance per day, divided into 2-3 doses.

It is recommended to use an amino acid-based dietary supplement for approximately 4-12 weeks.

The D-form is used to increase testosterone levels. A study found that men who consumed 3 grams of D-aspartic acid for 12 days increased their testosterone levels by almost 40 percent. But after just 3 days without the supplement, the levels dropped by about 10 percent.

Who needs higher doses?

Undoubtedly, this substance is extremely necessary for people of all age groups, but in some cases the need for aspartic acid increases sharply. First of all, this applies to people with depression, poor memory, brain diseases, and mental disorders. It is important to take regularly for people with reduced performance, cardiac diseases and vision problems.

In addition, it is important to know that high blood pressure, increased testosterone levels, and the presence of atherosclerotic plaques in the vessels of the brain are the reasons for reducing the intensity of taking the substance.

Amino acid deficiency

Individuals whose diet does not contain enough protein foods are at risk of developing a deficiency not only of aspartic acid, but also of other beneficial substances. Lack of amino acids is manifested by severe fatigue, depression, and frequent infectious diseases.

Food sources

The issue of consuming aspartic acid in the form of food is not so acute, since a healthy body can independently provide itself with the necessary portions of the substance (in two forms). But, nevertheless, you can also get the amino acid from food, mainly high-protein.

Sources of animal origin: all meat products, including smoked meats, dairy foods, fish, eggs.

Plant Sources: Asparagus, sprouted seeds, alfalfa, rolled oats, avocados, asparagus, molasses, beans, lentils, soybeans, brown rice, nuts, brewer's yeast, tropical fruit juices, apple juices (Semerenko), potatoes .

Aspartic acid is an important component for maintaining health. Meanwhile, when taking, it is important to remember the recommendations of doctors so as not to harm your body.

Gross formula

C10H21N5O6

Pharmacological group of the substance Arginine aspartate

Nosological classification (ICD-10)

CAS Code

7675-83-4

Characteristics of the substance Arginine aspartate

Amino acid, dietary supplement. White crystalline, water-soluble powder, odorless.

Pharmacology

pharmachologic effect- antiasthenic, replenishing amino acid deficiency.

Increases endurance. Activates cellular metabolism, urea metabolism, promotes the neutralization and removal of ammonia, stimulates the release of growth hormone from the pituitary gland. Regulates blood sugar levels and reduces lactic acidosis caused by muscle load, transfers metabolism to the aerobic pathway. Shows nootropic and anti-amnesic activity, prevents stress changes in the metabolism of mediator amino acids, increases phosphorylation of a number of proteins in the central nervous system. The aspartate component normalizes nervous regulation processes.

Arginine and aspartate are quickly absorbed from the gastrointestinal tract, pass histohematic barriers and are distributed to all organs and tissues. Partially utilized in metabolic processes, the remaining part is excreted by the kidneys (mainly).

Application of the substance Arginine aspartate

Overwork, general physical and mental fatigue associated with protein deficiency, asthenic conditions during the recovery process, incl. after infectious diseases and operations, metabolic alkalosis, hyperammonemia types I and II, citrullinemia, argininosuccinic aciduria and N-acetylglutamate synthetase deficiency.

Contraindications

Hypersensitivity, severe liver or kidney dysfunction, children under 3 years of age (for solution), up to 12 years of age (for tablets).

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