Norepinephrine hydrotartrat (Noradrenalini hydrotartras)

Pharmacodynamics and pharmacokinetics

This drug has a significant effect on alpha-adrenergic receptors, exhibiting a noticeable vasoconstrictor and pressor effect compared to adrenaline . At the same time, there is less stimulation of heart contractions, a weak bronchodilator effect and an effect on metabolism, and a pronounced hyperglycemic effect does not appear.

Norepinephrine is characterized by a cardiotropic effect, stimulating cardiac beta-adrenergic receptors, which can be masked by reflex bradycardia , high tone of the vagus nerve, provoked by high blood pressure .

When norepinephrine is administered, cardiac output increases and perfusion pressure in the coronary arteries increases, along with peripheral vascular resistance and central venous pressure.

This drug is widely used when it is necessary to increase blood pressure and increase heart contractions. But this is done primarily to increase peripheral vascular resistance and heart rate. In addition, blood flow in the vessels of the kidneys and gastrointestinal tract decreases. Ventricular arrhythmias . For this reason, norepinephrine is not used in complex cases of cardiogenic shock.

This can cause a vasoconstrictor reaction in peripheral vessels, which means their resistance can lead to an undesirable effect. The myocardial oxygen demand also increases significantly , which negatively affects the condition of the whole organism.

Norepinephrine hydrotartrate

Name: Norepinephrine hydrotartrat (Noradrenalini hydrotartras) Pharmacological action: The action of norepinephrine is associated with a predominant effect on alpha-adrenergic receptors (namely, alpha-adrenergic receptors). It differs from adrenaline in having a stronger vasoconstrictor and pressor (increasing blood pressure) effect, a lesser stimulating effect on heart contractions, a weak bronchodilator (expanding the lumen of the bronchi) effect, a weak effect on metabolism (no pronounced hyperglycemic / increasing blood glucose / effect). The cardiotropic effect (effect on the heart) of norepinephrine is associated with its stimulating effect on beta-adrenergic receptors of the heart, however, the beta-adrenergic stimulating effect is masked by reflex bradycardia (rare pulse) and increased tone of the vagus nerve in response to increased blood pressure. Administration of norepinephrine causes an increase in cardiac output; due to increased blood pressure, perfusion pressure in the coronary (heart) arteries increases. At the same time, peripheral vascular resistance (resistance of blood vessels to blood flow) and central venous pressure increase significantly. Norepinephrine is very effective in raising blood pressure and increasing heart rate. However, the increase in blood pressure is mainly due to an increase in peripheral vascular resistance and heart rate. Under the influence of norepinephrine, blood flow in the renal and mesenteric vessels (intestinal vessels) also decreases. Ventricular arrhythmias (heart rhythm disturbances) may occur. Therefore, in case of cardiogenic shock, especially in severe cases, the use of norepinephrine is considered inappropriate. Typically, severe cases of cardiogenic (and hemorrhagic) shock are accompanied by a vasoconstrictor reaction (sharp narrowing of the lumen) of peripheral vessels. In these cases, the administration of norepinephrine and other substances that increase peripheral vascular resistance may have a negative effect. It should be taken into account that under the influence of norepinephrine, the need of the myocardium (heart muscle) for oxygen increases.

Indications for use: Used to increase blood pressure during acute decrease due to surgical interventions, injuries, poisoning, accompanied by inhibition of vasomotor centers, etc., as well as to stabilize blood pressure during surgical interventions on the sympathetic nervous system after removal of pheochromocytoma (adrenal tumors) ) and etc.

Directions for use: Administered intravenously (drip). An ampoule solution of norepinephrine is diluted in a 5% glucose solution or isotonic sodium chloride solution so that 1 liter of solution contains 2-4 ml of a 0.2% solution (4-8 mg) of norepinephrine hydrogen tartrate. The initial rate of administration is 10-15 drops per minute. To achieve a therapeutic effect (maintaining systolic pressure at 100-115 mm Hg), the rate of administration is usually increased to 20-60 drops per minute. You should be careful about injecting norepinephrine solution under the skin and into muscles due to the risk of developing necrosis (tissue death).

Side effects: With rapid administration, nausea, headache, chills, tachycardia (increased heart rate), necrosis if it gets under the skin (therefore, constant monitoring of the position of the needle in the vein is necessary). If norepinephrine gets under the skin, inject 5-10 ml of phentolamine in 10 ml of saline.

Contraindications: The administration of norepinephrine is contraindicated during fluorotane and cyclopropane anesthesia. Norepinephrine should also not be used in cases of complete atrioventricular block (impaired conduction of excitation through the conduction system of the heart), in case of cardiac weakness, or severe atherosclerosis.

Release form: 0.2% solution in ampoules of 1 ml.

Storage conditions: List B. Protected from light.

Synonyms: Levarterenol bitartrate, Arterenol, Levarterenol, Levofed, Norarthrinal, Norepinephrine, Norexadrin, etc.

Attention! The description of the drug “ Norepinephrine hydrotartrate ” on this page is a simplified and expanded version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and read the instructions approved by the manufacturer. Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Interaction

The simultaneous use of norepinephrine and inhalational anesthetics can lead to complicated ventricular arrhythmia.

Combination with adrenergic and serotonergic antidepressants, imipramine or amitriptyline leads to the development of paroxysmal hypertension , cardiac arrhythmia caused by an adrenergic blocking effect on the functioning of the nervous system.

The use of selective and non-selective MAO inhibitors, Linezolid , etc., together with Norepinephrine can enhance its pressor effect, so constant medical monitoring is required.

Analogs

Level 4 ATX code matches:
Mezaton

Dobutamine

Dopamine

Dopamine

Adrenalin

Main analogues: Arterenol, Levarterenol, Levofed, Norarthrinal, Norepinephrine and Norexadrin .

Differences between Noranrenaline and Adrenaline

Adrenaline is produced by the adrenal medulla. This component is involved in various processes in the body: stimulating the breakdown of glycogen in liver hepatocytes, which leads to an increase in glucose in the blood , activates the lipase enzyme and the breakdown of triglycerides in adipose tissue, as well as glycogenolysis in muscle cells.

The contraction of the heart muscles also increases and blood pressure increases, the muscle and heart vessels dilate, but the vessels of the abdominal organs, skin and mucous membranes narrow. A significant influence of adrenaline on the body's response to stressful situations has been noted.

Norepinephrine has a pronounced vasoconstrictor effect, has less effect on heart contractions, has a weak bronchodilator effect and influence on metabolic processes.

The normal content of adrenaline in the blood is 88 mcg/l, and norepinephrine is in the range of 104-548 mcg/l.

The need to determine the concentration of these components arises when it is necessary to identify pheochromocytomas and carry out a differential diagnosis of hypertension.

Norepinephrine Agetan conc for preparation of IV solution 2 mg/ml amp 4 ml N 10

Active substance : norepinephrine

Release form, packaging and composition of the drug Noradrenaline Agetan

Concentrate for preparing a solution for intravenous administration 1 ml 1 amp.

norepinephrine tartrate (as monohydrate) 2 mg 8 mg

Clinical and pharmacological group: Alpha-, beta-adrenergic agonist

Pharmacotherapeutic group: Alpha adrenergic agonist

pharmachologic effect

Adrenomimetic. It has a pronounced direct effect on α-adrenergic receptors, as well as a weak effect on β1-adrenergic receptors and has a slight effect on β2-adrenergic receptors. The predominance of α-adrenomimetic action leads to vasoconstriction, an increase in peripheral vascular resistance and systemic blood pressure, and central venous pressure also increases. Since the stimulating effect on the heart (on β1-adrenergic receptors of the myocardium) is very weakly expressed, compensatory mechanisms associated with vagal excitation in response to increased blood pressure prevail, which ultimately leads to a decrease in heart rate and the development of bradycardia. However, despite the decrease in heart rate, the positive inotropic effect on the heart remains, so the IOC decreases slightly.

Under the influence of norepinephrine, blood flow in the renal and mesenteric vessels also decreases.

It has a slight effect on myocardial oxygen consumption, and therefore has a less pronounced arrhythmogenic effect than epinephrine.

Unlike epinephrine, it has a stronger (1.5 times) vasoconstrictor and pressor effect, a less pronounced stimulating effect on heart contractions, a weak bronchodilator effect and a very weak (more than 20 times) hyperglycemic effect.

Pharmacokinetics

Plasma protein binding is 50%.

Intensively metabolized in adrenergic neurons and in the liver with the participation of MAO by oxidative deamination. It is a metabolic substrate for COMT, which methylates the cyclic part of the molecule in the ortho position. Inactive metabolites partially form paired compounds with glucuronic or sulfuric acid and are excreted in this form by the kidneys.

After the administration of norepinephrine, the following most important compounds are found in the urine: norepinephrine-4 - 24%, normetanephrine (o-methyl-norepinephrine) - 21-25%, o-methyl glycol derivative - 20-23%, vanillylmandelic acid - 32- 35%. Normally, 5 mg/day of vanillylmandelic acid is excreted in the urine (at higher levels, the presence of pheochromocytoma should be excluded).

Norepinephrine does not penetrate the BBB and penetrates the placental barrier.

Indications of the active substances of the drug Norepinephrine Agetan

Acute arterial hypotension in injuries, surgical interventions, poisoning, accompanied by inhibition of vasomotor centers, overdose of ganglion blockers and other antihypertensive drugs.

To stabilize blood pressure during operations on the sympathetic nervous system after removal of pheochromocytoma.

Side effect

With rapid intravenous administration: nausea, headache, chills, palpitations are possible.

From the cardiovascular system: possible bradycardia (eliminates by administering atropine subcutaneously), cerebral hemorrhage (due to a sharp increase in blood pressure).

Local reactions: necrosis upon contact with the skin.

Contraindications for use

Complete AV block, chronic heart failure, atherosclerosis, anesthesia with fluorotane, chloroform or cyclopropane (risk of ventricular fibrillation), increased sensitivity to norepinephrine.

Use during pregnancy and breastfeeding

Norepinephrine should not be used during pregnancy due to the risk of fetal hypoxia. It is believed that use is possible only for health reasons (including collapse, myocardial infarction).

Use in elderly patients

When administering norepinephrine, careful monitoring of blood pressure in elderly patients is necessary.

special instructions

Use is not recommended for cardiogenic and hemorrhagic shock with severe arterial hypotension, because the spasm of arterioles caused by norepinephrine further impairs the blood supply to the tissues.

It is not recommended to use norepinephrine for conduction anesthesia of fingers and toes to avoid tissue necrosis.

In case of severe atherosclerosis, arterial hypertension, thyrotoxicosis, use is possible only for health reasons (including collapse, myocardial infarction).

Use with caution in patients with coronary artery disease, arrhythmia, tachycardia, diabetes mellitus, and angle-closure glaucoma.

When norepinephrine is administered, careful monitoring of blood pressure is necessary in patients with atherosclerosis, arterial hypertension, and the elderly.

It should be borne in mind that the use of norepinephrine does not replace blood transfusions or the introduction of blood substitutes if shock is due to large loss of plasma, because norepinephrine only causes an increase in vascular tone.

In case of extravasation, skin necrosis may develop.

Drug interactions

When used simultaneously with MAO inhibitors, a slight increase in the pressor effects of norepinephrine is possible.

When used simultaneously with inhalation anesthesia, there is a high risk of developing heart rhythm disturbances.

When used simultaneously with tricyclic antidepressants (including amitriptyline, desipramine, imipramine), it is possible to enhance the effect of norepinephrine on the cardiovascular system and increase the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension.

When used simultaneously with guanethidine and bretylium, the pressor effects of norepinephrine are enhanced.

When used simultaneously with lithium carbonate, the effectiveness of norepinephrine may be reduced.

When used simultaneously with reserpine, the effects of norepinephrine are enhanced.

Reviews about Norepinephrine

It should be noted that this drug is often used in critical cases when there is a fight for a person’s life. Therefore, it is impossible to find reviews about Norepinephrine left by patients. In such situations, people are unlikely to be able to assess the effect of a particular drug, and most likely do not even know that they received such treatment.

As a rule, medical specialists discuss this drug online. This is usually related to the question of how to increase Norepinephrine when critical situations arise. The fact is that this needs to be done quickly, but the speed of introduction of the solution is an important aspect of its use. Therefore, you have to use all your experience and knowledge, which helps a person not to die and conduct full-fledged intensive therapy.

The features of this drug are described in detail by Wikipedia, where it is reported that there is no need to administer it independently. As for medical professionals, it is important that they have sufficient experience and professionalism to use Norepinephrine in practice.

Adrenaline, norepinephrine, dopamine, serotonin are biogenic amines that are hormones and neurotransmitters. Their content increases significantly in biological fluids in some neuroendocrine neoplasms. * The study determines the quantity of each indicator separately.

Synonyms Russian

Free catecholamines in the blood.

English synonyms

Catecholamines - adrenaline, norepinephrine, dopamine + serotonin.

Research method

High performance liquid chromatography.

Units

Pg/ml (picograms per milliliter), ng/ml (nanograms per milliliter).

What biomaterial can be used for research?

Venous blood.

How to properly prepare for research?

• Children under 1 year of age should not eat for 30-40 minutes before the test.
• Children aged 1 to 5 years should not eat for 2-3 hours before the test.
• Eliminate avocados, bananas, eggplants, pineapples, plums, tomatoes, and walnuts from your diet for 72 hours before the test.
• Do not eat for 12 hours before the test; you can drink clean still water.
• Discontinue (in consultation with your doctor) sympathomimetics 14 days before the study.
• Completely avoid (in consultation with your doctor) taking medications for 24 hours before the test.
• Avoid physical and emotional stress for 24 hours before the test.
• Do not smoke for 2 hours before the test.

General information about the study

Catecholamines are a group of similar hormones produced by the adrenal medulla. The main catecholamines are dopamine, adrenaline (epinephrine) and norepinephrine. They are released into the blood in response to physical or emotional stress and are involved in the transmission of nerve impulses to the brain, promote the release of glucose and fatty acids as energy sources, and dilate bronchioles and pupils. Norepinephrine constricts blood vessels, increasing blood pressure, while adrenaline increases heart rate and stimulates metabolism. After completing their action, these hormones are broken down into physiologically inactive substances (homovanillic acid, normetanephrine, etc.).

Normally, catecholamines and their breakdown products are present in the body in small quantities. Their content increases significantly for a short time only under stress. However, chromaffin and other neuroendocrine tumors can produce large amounts of catecholamines, leading to significant increases in the levels of these hormones and their breakdown products in the blood and urine. This threatens long-term or short-term increases in blood pressure and, accordingly, severe headaches. Other symptoms of elevated catecholamines include shaking, sweating, nausea, restlessness, and tingling in the extremities. In addition to catecholamines, pheochromocytomas can synthesize serotonin, adrenocorticotropic hormone, vasoactive intestinal peptide, somatostatin and other hormones. There is no correspondence between the size of the tumor, the level of catecholamines in the blood and the clinical picture.

Serotonin is not a catecholamine, but also belongs to the group of biogenic amines with hormonal and neurotransmitter activity. It is synthesized from the amino acid tryptophan and is stored in enterochromaffin cells of the gastrointestinal tract (80-95% of the total), various structures of the brain, mast cells of the skin, platelets and some other endocrine organs. Serotonin lowers the threshold of pain sensitivity, regulates the function of the pituitary gland, affects vascular tone, blood clotting, motility and secretory activity of the gastrointestinal tract.

Approximately 90% of chromaffin tumors are located in the adrenal glands. Most are benign and do not spread beyond the adrenal glands, although they may continue to grow. Without further treatment, as the tumor grows over time, symptoms of the disease sometimes become more severe. High blood pressure caused by a chromaffin tumor can cause kidney and heart damage and even hemorrhage or a heart attack.

In most cases, these tumors are removed surgically, after which the catecholamine levels are significantly reduced, and tumor-related symptoms and complications are alleviated or disappear altogether.

A blood test reveals the amount of the hormone at the time of taking the test, while a urine test reveals the amount of the hormone over the previous 24 hours.

What is the research used for?

• For the diagnosis of chromaffin tumors in symptomatic patients.
• To monitor the effectiveness of treatment of a chromaffin tumor, in particular after its removal, to ensure that there are no relapses.

When is the study scheduled?

• If a chromaffin tumor is suspected.
• If the patient has chronic hypertension, accompanied by headache, sweating, and rapid pulse.
• When hypertension is not treatable (since hypertensive patients with chromaffin tumors are often resistant to traditional therapy).
• If an adrenal tumor or neuroendocrine tumor was detected during a scan, or if the patient has a hereditary predisposition to their formation.
• When monitoring the condition of patients who have already been treated for chromaffin tumor.

What do the results mean?

Reference values

• Adrenalin

• Norepinephrine

• Dopamine: 5.6 - 44 pg/ml.
• Serotonin: 50 - 220 ng/ml.

Since the results of this test can be influenced by many factors, and chromaffin tumors are quite rare, the results are often false positive. To make a confident diagnosis, a general examination of the patient is necessary: ​​an assessment of his physical and emotional state, the medications he takes and the food he eats. Once interfering factors have been identified and corrected, the test is often repeated to determine whether catecholamine levels will still be high. In addition, a test for metanephrine in the blood and/or urine and a magnetic resonance imaging scan of the tumor may be ordered to confirm the results.

Elevated catecholamine levels in a patient who has previously been treated for a chromaffin tumor indicate recurrence of the tumor or that therapy was not entirely effective.

If the concentration of catecholamines is normal, then the presence of a chromaffin tumor is unlikely. However, these tumors do not always produce catecholamines at a constant rate. If there have been no recent exacerbations of hypertension, then the concentration of catecholamines may be close to normal even with existing pheochromocytoma.

Possible causes of increased serotonin levels: carcinoid tumors; medullary thyroid cancer; testicular tumors; celiac disease; endocarditis; dumping syndrome; acute intestinal obstruction; cystic fibrosis; acute myocardial infarction; taking medications (paracetamol, diazepam, naproxen, pindolol). Reasons for decreased serotonin levels: mastocytosis; phenylketonuria; Down syndrome; carcinoid tumors of the rectum; Hartnup's disease; taking medications (ethanol, imipramine, isoniazid, sulfasalazine).

What can influence the result?

• Medicines you are taking (acetaminophen, aminophylline, amphetamines, appetite suppressants, caffeine-containing medications, chloral hydrate, clonidine, dexamethasone, diuretics, epinephrine, ethanol, insulin, imipramine, lithium, methyldopa, nicotine, nitroglycerin, nasal drops, tricyclic antidepressants, and vasodilators ).
• Food consumed (tea, coffee, alcohol).
• Stress.

Norepinephrine price, where to buy

The price of Noradrenaline for a package of 10 ampoules is from 1,550 rubles.

You can buy Noradrenaline in Kyiv at a cost of 1300 UAH.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine

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