Medicinal reference book geotar. Ephedrine - instructions for use, analogs, reviews and release forms (injections in ampoules for injection hydrochloride, tablets) of the drug for the treatment of arterial hypotension, bronchial asthma and rhinitis in adults, children and patients with

People use many medications for other purposes, without even knowing the negative consequences this causes. One such remedy is Ephedrine, which many athletes use as a stimulant, similar to adrenaline in its effect on the body. This drug is highly addictive and is under special government control. Find out how it works and why it is dangerous without a prescription.

What is Ephedrine

This is a sympathomimetic drug. The active substance is a psychoactive poisonous alkaloid contained in the ephedra plant species. IN present time this medicine is under strict control. Storage, sale and use of Ephedrine with a concentration above 10% is limited. The drug is outdated, unsafe (addictive) and ineffective.

Ephedra alkaloid and isomers (pseudoephedrine) are obtained by extraction or synthetically from natural raw materials and purified from impurities. The authenticity of a substance is determined:

  • reaction with a solution of silver nitrate and nitric acid;
  • reaction with a solution of copper sulfate and alkali;
  • reaction with potassium ferricyanide in an alkaline medium.

Composition and release form

The drug is sold in tablets and injection form. The main active ingredient in it is the substance “ephedrine hydrochloride”. The table below shows how much it is contained in different versions of the drug:

Effect on the body

The active component of the drug, ephedrine hydrochloride, stimulates alpha and beta adrenergic receptors. Under the influence of varicose thickenings, norepinephrine is released into the lumen of the synaptic cleft. Ephedrine has a mild stimulating effect and affects efferent and adrenergic fibers. The drug causes vasoconstrictor, bronchodilator and psychostimulant effects. The medicine improves atrioventricular conduction, increases the strength and frequency of heart contractions, increases arterial pressure, skeletal muscle tone.

When using the medicine, dilation of the pupils is observed, although it does not affect intraocular pressure and accommodation. The psychostimulating effect is approximately the same as that of phenamine. Ephedrine can reduce swelling in urticaria by stimulating alpha-adrenergic receptors in the blood vessels skin, their narrowing and reduction of increased permeability.

Indications for use

The drug is prescribed to treat many diseases. Experts recommend taking it for:

  • hay fever;
  • arterial hypotension due to trauma, spinal anesthesia, blood loss, surgery, bacteremia, shock, overdose of a number of drugs, collapse;
  • catarrhal rhinitis;
  • sinusitis;
  • vasomotor rhinitis;
  • depression;
  • allergic rhinitis;
  • diagnostics in ophthalmological practice;
  • narcolepsy;
  • drug poisoning;
  • bronchial asthma;
  • bleeding from the gums and dental pulp;
  • poisoning with sleeping pills;
  • diseases of the cardiovascular system;
  • hives;
  • serum sickness.

Instructions for use of Ephedrine

The method of using the medicine depends on the diagnosis, age and weight of the patient, and other parameters. The medicine is allowed to be used only under the supervision of a doctor, strictly in accordance with the recommendations. It is important to remember that the drug is highly addictive, so the prescription must be justified. The choice of drug release form is influenced by the disease being treated.

Ephedrine tablets

For bronchial asthma or allergic diseases The medication is prescribed for 10-15 days. Take 25-50 mg (1-2 tablets) twice or thrice a day. It is possible to use it in cycles of three days with the same break. Long-term use of the medicine is strictly prohibited. The therapeutic effect reaches its maximum after 15-60 minutes. Lasts up to 5 hours.

Solution

The method of using Ephedrine in this release form depends on the disease. Peculiarities:

  1. 20-50 mg of the drug is administered intramuscularly or subcutaneously before spinal anesthesia, in case of bacteremia. Injections are repeated 2-3 times a day.
  2. Children may be prescribed subcutaneous or intravenous injections medications as a bronchodilator (treatment of asthma) and a central nervous system stimulant, 3 mg per 1 kg of weight.
  3. For arterial hypotension, slow intravenous or subcutaneous administration of 20-50 mg of the drug with saline is indicated.
  4. In ophthalmological practice, a 1-5% solution is prescribed, for vasomotor rhinitis - 2-3%.
  5. The maximum permissible single dose of the drug is 50 mg, daily dose is 150 mg.
  6. The effect becomes noticeable after 10-20 minutes. Lasts about one hour.

special instructions

The drug is potent. By not following the rules of use, the patient can cause serious harm to his body. What you need to remember when treating with Ephedrine:

  1. For infusions, it is necessary to use a special device with a measuring scale to regulate the rate of administration. It is better to inject into large veins, preferably into the central one.
  2. The entire period of drug therapy must be monitored ECG changes, blood and other types of pressure, urine volume.
  3. To avoid sleep disturbances, the product is used in the evening. It's better to do this just before going to bed.
  4. Care must be taken to ensure that the product does not penetrate the perivascular tissue. This causes their necrosis.
  5. A large amount of the drug during myocardial infarction can provoke increased and progression of ischemia.
  6. Before starting therapy, hypovolemia must be corrected.
  7. Long-term treatment with the drug is unacceptable.
  8. When administering spinal anesthesia to a pregnant woman, the medicine can cause increased heart rate in the fetus. Interacting with drugs to enhance labor causes persistent arterial hypertension.
  9. It is forbidden to inject an opaque solution. Residues after injection should be destroyed.

Ephedrine for weight loss

With constant and regular use, the drug helps reduce body weight. It speeds up the burning subcutaneous fat, reduces appetite, stimulates metabolism. Nowadays, ephedrine fat burners are rarely used for weight loss, although it is currently illegal. They used to be very popular. Manufacturers of dietary supplements are strictly prohibited from adding ephedra extract to their products in a concentration of more than 15%.

Application in bodybuilding

The product is used in conjunction with aspirin and caffeine. The ECA complex helps during the drying period, increases performance and endurance. However, the combination of ephedrine with caffeine and aspirin can cause harm to the body. In most countries, fat burners containing ephedra are prohibited from being produced or taken. The substance causes many side effects(especially with caffeine), most of them have a long-term effect.

Ephedrine drug

The medicine has a stimulating effect on the nervous system, similar to amphetamine. It is sometimes used by people suffering from drug addiction. For this reason, the sale of the drug is strictly prohibited in some countries. The consequences of uncontrolled use of the drug are unpredictable. This action can cause serious, irreparable damage to your health. The narcotic substance is used as a raw material for the illegal production of ephedrone and methamphetamine.

Drug interactions

Ephedrine in combination with other drugs may cause different effects, which must be taken into account when taking them together. How does Ephedrine work together with a number of medications:

  1. The drug weakens the effect of sleeping pills and narcotic analgesics.
  2. Medicines that alkalinize the urine prolong the elimination period of ephedrine. This increases the risk of intoxication.
  3. Combined use with dopamine, cardiac glycosides, quinidine, drugs for inhalation anesthesia, tricyclic antidepressants can lead to severe ventricular arrhythmia.
  4. When taken with antihypertensive drugs, diuretics, antispasmodics, rauwolfia alkaloids, the hypotensive effect is reduced.
  5. When used together with bronchodilator adrenergic medications, increased side effects are observed.
  6. Combination with reserpine, monoamine oxidase inhibitors, furazolidone, procarbazine, selegiline causes a strong increase in blood pressure, hypertensive crises, arrhythmia, vomiting, headache.
  7. Side effects, especially from the nervous system, increase with joint use with methylphenidate, ritodrine, mazindol.
  8. When used simultaneously with ergotamine, methylergometrine, oxytocin, ergometrine, there is a high risk of intracranial hemorrhage, ischemia, and gangrene.

Side effects

Even if all the rules for taking the medicine are followed, it can have a serious effect on the body. During use of the product, the following conditions may occur:

  • motor restlessness;
  • dyspnea;
  • nervousness;
  • chills;
  • weakness;
  • hyperthermia;
  • sleep disorders;
  • dilated pupils;
  • headache;
  • allergic reactions;
  • tremor of the limbs;
  • blurred visual perception;
  • muscle spasms;
  • labored breathing;
  • convulsions;
  • increased sweating;
  • dizziness;
  • pale skin;
  • changes in mood and psyche;
  • vasoconstriction;
  • hallucinations;
  • pain and burning at the injection site;
  • drowsiness;
  • difficult and painful urination;
  • numbness of legs and arms;
  • nausea;
  • pain and discomfort behind the sternum;
  • vomit;
  • ventricular arrhythmias;
  • dryness and irritation of the mouth and pharynx;
  • decreased blood pressure;
  • appetite disorders;
  • tachycardia or bradycardia;
  • heartburn;
  • angina pectoris;
  • hyperemia of the skin.

Overdose

If you use or inject an excessive amount of the drug, a rash may appear on the skin. Additional symptoms there will be increased sweating, decreased appetite, vomiting, urinary retention, severe increase in blood pressure, severe weakness and insomnia or overexcitement. In case of overdose, it is recommended to administer short-acting alpha-blockers.

Contraindications

There are a number of conditions and diagnoses for which the use of the drug is prohibited. Contraindications for treatment with Ephedrine are:

  • insomnia;
  • ventricular fibridation;
  • intolerance to the main component;
  • arterial hypertension with uncontrolled course;
  • pheochromocytoma;
  • tachycardia;
  • GOKMP.

For certain diseases, the medicine can be used, but only with caution, under the supervision of a doctor. This list includes:

  • hypoxia;
  • coronary insufficiency;
  • hypercapnia;
  • arterial hypertension;
  • metabolic acidosis;
  • angina pectoris;
  • hypovolemia;
  • tachyarrhythmia;
  • pulmonary hypertension;
  • ventricular arrhythmia;
  • closed-angle form of glaucoma;
  • benign prostatic hyperplasia;
  • atrial fibrillation;
  • diabetes;
  • Bruger's disease;
  • thyrotoxicosis;
  • atherosclerosis;
  • frostbite;
  • arterial embolism;
  • diabetic endarteritis;
  • history of occlusive lesions of peripheral vessels;
  • Raynaud's disease;
  • Myrcardial infarction.

Terms of sale and storage

You can buy Ephedrine in the form of tablets or solution only with a doctor's prescription. The drug is included in the list of potent substances No. 1. The medicine is stored for up to 5 years at an air temperature of no more than 25 degrees in a dark place inaccessible to children.

Analogs

There are a number of drugs with the same active ingredient and a similar effect. Most of them contain many other additional components, the dose of sympathomimetic is minimal. Analogues of the drug are:

  • Teofedrine-N;
  • Bronholitin;
  • Cefedrine;
  • Natural dietrin;
  • Ephedrine hydrochloride;
  • Bronchoton;
  • Neo Theophedrine;
  • Bronchocin;
  • Bronchitusen Vramed.

Ephedrine price

The cost of the medicine depends on the form of release, volume, and manufacturer. You can find approximate prices in the table below:

Video

240. Ephedrinihydrochloridum

Ephedrine hydrochloride

Ephedrinumhydrochloricum

l-1-Phenyl-2-methylaminopropanol-1 hydrochloride

C 10 H 15 NO * HCl M.c. 201.70

Description. Colorless needle-shaped crystals or white crystalline powder, odorless, bitter taste.

Solubility. Easily soluble in water, soluble in 95% alcohol, practically insoluble in ether.

Authenticity. 0.01 G the drug is dissolved in 1 ml water, add 0.1 ml copper sulfate solution and 1 ml caustic soda solution; a blue color appears. When shaking this solution with I ml ether, the ethereal layer is colored violet-red, the aqueous layer retains a blue color.

0,05 G the drug is dissolved in 1 ml water, add a crystal of potassium ferricyanide and heat to a boil; the smell of benzaldehyde appears.

0,01 G the drug gives a characteristic reaction to chlorides (p. 747).

Melting point 216-220°.

Specific rotation from -33° to -36° (5% aqueous solution).

Acidity. 0.2 G the drug is dissolved in 5 ml freshly boiled and cooled water, add 1 drop of methyl red solution; the red color that appears should turn yellow with an addition of no more than 0.05 ml 0.05 n. caustic soda solution.

Ammonium salts. 0.3 G the drug is placed in a test tube, 2 are added ml water and 1 ml caustic soda solution. IN top part test tubes are placed in a thin layer without a large number of cotton wool. Red litmus paper moistened with water is placed on top of the test tube. The test tube is placed for five minutes in a water bath with a temperature of about 65°. There should be no release of ammonia, which is determined by the smell and blueness of red litmus paper.

Sulfates. A solution of 0.2 g of the drug in 10 ml water must pass the test for sulfates (no more than 0.05% in the preparation).

Organic impurities. Solution 0.15 G drug at 5 ml concentrated sulfuric acid should be colorless.

Weight loss during drying. About 0.5 G The drug (accurately weighed) is dried at 100-105° to constant weight. Weight loss should not exceed 0.5%.

Sulfated ash from 0.5 G of the drug should not exceed 0.1% -

Quantitation. About 0.1 G drug (exactly weighed) - dissolve when heated at 10 ml ice acetic acid, after cooling add 5 ml a previously neutralized solution of mercuric oxide acetate and titrated with 0.1 N. solution of perchloric acid until blue coloring (indicator - crystalline violet).

1 ml 0.1 n. perchloric acid solution corresponds to 0.02017 G C 10 H 15 NO * HCI, which must be at least 99.0% in the preparation.

Storage. List B. In a well-closed container, protected from light.

The highest single dose orally and subcutaneously is 0.05 G.

Higher daily dose inside and under the skin 0.15 G.

Sympathomimetic (vasoconstrictor, bronchodilator) agent.

Pharmacological group: alkaloids
Pharmacological action: sympathomimetic, stimulates alpha and beta adrenergic receptors. Acting on varicose thickenings of efferent adrenergic fibers, it promotes the release of norepinephrine into the synaptic cleft. In addition, it has a weak stimulating effect directly on adrenergic receptors. Causes vasoconstrictor, bronchodilator and psychostimulating effects. Increases total peripheral vascular resistance (TPVR) and systemic blood pressure, increases minute volume of blood circulation, heart rate and strength of heart contractions, improves AV conduction; increases skeletal muscle tone and blood glucose concentration. Inhibits intestinal motility, dilates the pupil (without affecting accommodation and intraocular pressure). Stimulates the central nervous system; its psychostimulating effect is similar to that of phenamine. Inhibits the activity of MAO and catecholamine-O-methyltransferase. Has a stimulating effect on alpha-adrenergic receptors blood vessels in the skin, causing a narrowing of dilated vessels, thus reducing their increased permeability, leading to a decrease in swelling in urticaria.
Effect on receptors: alpha and beta adrenergic receptors (stimulant).

Ephedrine is one of the four active components of the ephedra plant. Ephedrine can stimulate weight loss by producing more fat available for fuel, as well as by increasing the heat used by the body. Ephedrine is purported to speed up metabolism in humans by 5%.

Description

Ephedrine is a stimulant drug that belongs to a group of drugs known as sympathomimetics. In particular, it is an alpha- and beta-adrenergic receptor agonist (selective beta-2-adrenergic receptor agonist). In addition, ephedrine enhances the release of norepinephrine. The action of this compound is similar to the main adrenergic hormone in the human body - epinephrine (adrenaline), which also acts on alpha and beta receptors. When administered, ephedrine significantly increases the activity of the central nervous system and also stimulates other target cells.
Ephedrine can be used in sports.
When the amount of free fatty acids increases due to the breakdown of triglycerides in adipose tissue, body temperature increases slightly (resulting in stimulation of metabolism), fat levels decrease and blood supply increases. Ephedrine is also believed to increase the anabolic effectiveness of steroids to some extent. The stimulating effect of this drug is also expressed in an increase in the force of contraction of skeletal muscles.

general information

Ephedrine is one of the four active components of the ephedra plant. Ephedrine can stimulate weight loss by producing more fat available for fuel, as well as by increasing the heat used by the body. Ephedrine is purported to speed up metabolism in humans by 5%. By increasing the heat used by the body, ephedrine also affects muscle cells and fat cells. Ephedrine also helps prevent muscle tissue breakdown in some cases. Ephedrine can enhance the properties of , and is usually included in the so-called “ECA” drugs (weight loss mixtures that include ephedrine, caffeine and aspirin). Ephedrine has virtually no side effects, except that it can cause an increase in blood pressure and also increase the level of glucose in the blood, but these effects disappear when you stop using the drug. Ephedrine in overdose is a hyperstimulant. Ephedrine is a well-studied and fairly safe compound, although not always effective. To increase effectiveness and reduce the risk of side effects, the drug should be taken taking into account physical activity and diets. Also known as Ephedra Vulgaris, Ephedraceae, ma huang.

Not to be confused with Ephedrone, Epinephrine

It is important to note! Ephedrine is a stimulant, and the ephedra plant is an even greater stimulant.

Pharmacological action: fat burner. Combines well with: methylxanthines such as caffeine and theopillin (found in green tea). Particularly effective when

    Fighting excess weight

    Need to suppress appetite

Ephedrine can also increase dopamine levels in the brain and should be combined with yohimbine with caution. If you have heart disease, ephedrine should only be taken under the supervision of your doctor.

Ephedrine: instructions for use

All recommendations for use below apply to the drug Ephedrine HCl. In ECA-type drugs, the daily dosage of ephedrine is 20-24 mg three times a day. Ephedrine in pure form gave positive results on the rate of fat metabolism in human studies, the dosage was 20-50 mg three times a day. An increased dose (150 mg) may cause headaches and mild hand tremors in some users. Ephedrine is commonly consumed along with xanthine compounds - and sometimes. Caffeine significantly enhances the effect of ephedrine.

Story

Ephedrine is a long-established drug that has been used in the United States for many years, including as a stimulant, appetite suppressant, and to treat anesthesia-associated hypotension. IN last years In the United States, control over the ephedrine market has increased due to the fact that the drug can be used as a precursor to the production of methamphetamine. Given the high availability of ephedrine as an over-the-counter drug, clandestine factories have every opportunity to use it for their own purposes. A trend has developed towards large quantities of ephedrine being purchased at retail, and many states have been faced with the need to create legislation to control the sale of ephedrine and similar substances used to create narcotic drugs. In 2006 it was adopted the federal law, restricting the consumption and sales channels of ephedrine in the United States. With methamphetamine addiction (and related crimes) on the rise, some believe ephedrine may soon be added to the government's list of controlled substances. Despite strict measures, the substance is still available for sale without a prescription.

How supplied

Ephedrine (either ephedrine hydrochloride or ephedrine sulfate) is most often supplied in tablets of 25 or 50 mg each.

Origin and structure of ephedrine

Composition (ephedra)

Ephedrine is found in the Ephedra Sinica plant, also known as Ma Huang or Chinese ephedra. This is especially important because there is an entire species of Ephedrea in the Ephedraceae family, and the fat-burning ephedrine alkaloids are found only in Ephedra Sinica. The ephedra species includes 50 plants that grow everywhere in the world, many of them are adapted to semi-arid and desert conditions, some to the humid and temperate climates of the Mediterranean and North America. Ma Huang (Ephedra Sinica), marketed as a fat burner, contains:

Ephedra plants from Northern and South America make up about half of all existing species and do not contain a sufficiently large amount of ephedrine alkaloids, however, according to anecdotal evidence, they may contain pseudoephedrine. According to some studies, ephedra plants from North America do not contain either ephedrine or pseudoephedrine.

Ephedrine: composition (ephedrine alkaloids)

Ephedrine as a molecule has two chiral centers, and due to this it has four variations (or four stereomers):

    1R,2S (-)- ephedrine

    1S,2S (+)- pseudoephedrine

    1S,2R (+)- ephedrine

    1R,2R (-)- pseudoephedrine

In addition, ephedrine and pseudoephedrine tend to lose a methyl group and become norephedrines, or methylate and create N-methylephedrine. Norephedrine and norpseudoephedrine are also known as phenylpropinolamine, or PPA.

Ephedrine: properties

Ephedrine can remain in the urine in a stable state for up to 9 months at temperatures from -20°C to 37°C, or for 15 hours at 60 degrees, which is equivalent to the temperature in the trunk or glove compartment of a car in hot weather. Ephedrine also appeared to be stable under 6 cycles of alternating freezing and thawing.

Structural characteristics

Ephedrine is a sympathomimetic amine, similar in structure to amphetamine or methamphetamine. It has the chemical name (1 R,2S)-2-(methylamino)-1phenylpropane1-0l.

Side effects

Ephedrine can cause a variety of unwanted side effects. The stimulating effect can cause hand tremors, tremors, sweating, rapid heartbeat, dizziness and a feeling of inner restlessness. When addiction occurs or the dose is reduced, these effects appear to a lesser extent. Simply put, if a person does not like the effects of , he is unlikely to like ephedrine, which has a stronger effect on the body. The mental and physical changes that occur as a result of taking this drug are very similar to the changes observed when taking. When using the drug, there is a noticeable decrease in appetite, which is usually perceived as positive effect. Ephedrine is very often found in appetite suppressants. With regular use of ephedrine, headaches and increased blood pressure may occur. For users with medical conditions thyroid gland People with high blood pressure or heart problems should avoid taking this drug. Ephedrine is a CNS stimulant with the potential for fatal overdose. Symptoms of overdose may include rapid breathing, abnormal blood pressure, palpitations, loss of consciousness, trembling, panic, extreme restlessness, severe nausea, vomiting, and diarrhea.

Ephedrine use

Ephedrine is used (off-label) among bodybuilders and athletes as a fat burner. The drug is usually used several times a day during drying at a dose of 25 to 50 mg at a time.

Pharmacology

Digestion and absorption

A dose of 50 mg of ephedrine causes a decrease in the time it takes for a person to empty the stomach and reduces the time it takes for food to be absorbed. Systemic absorption Ephedrine directly interacts with muscle cells and induces thermogenesis in myocytes. Ephedrine is also able to reduce nitrogen excretion in the urine, which indicates that ephedrine has a muscle-sparing effect. Ephedrine may also increase thermogenesis due to its vasoconstrictor properties (vascular thermogenesis). Ephedrine supplementation increases plasma, glucose, and C-peptide levels, depending on the ephedrine content of the preparation. Methylxanthine drugs (such as caffeine and theophylline) are likely to enhance the effects of ephedrine. The dosage of ephedrine//theophylline at 22mg/30mg/50mg, respectively, turned out to be twice as effective as ephedrine alone, but the greatest effectiveness was shown by the mixture of ephedrine/caffeine 20mg/200mg, respectively, which led to the creation of the drug ECA, which contains ephedrine/caffeine/aspirin dosed 20mg/200mg/91mg respectively.

Impact on the body

Neurology

Ephedrine is the most effective stimulant during calorie restriction. The effect of stimulating brain activity is most powerful when ephedrine is combined with.

Fat mass and obesity

Ephedrine: action

Ephedrine is capable of simultaneously negatively influencing all three subtypes of beta-adrenergic receptors in brown adipose tissue, resulting in increased thermogenesis without significant activation of the alpha-adrenergic receptor class, and may also be able to counteract the activation of agonists of these receptors.

Metabolic rate and oxygen consumption

Human studies have shown that oxygen consumption following an initial dose of ephedrine (20 mg) increases 30 to 60 minutes after ingestion in all cases (with additional activity in individuals without stimulant tolerance), although chronic ephedrine dosing slows the expected decline oxygen consumption 1-3 hours after administration. This suggests that ephedrine provides greater fat-burning benefits when used over a longer period (4-12 weeks) rather than intermittently, and it is possible that the mechanism behind this is increased beta-adrenergic sensitization. Ephedrine may increase metabolic rate independent of exercise; this is different from, which acts as a fat burner only in the presence of physical activity. By the way, this may be the reason that the combination of ephedrine acts in synergy with physical activity, leading to an increase in oxygen consumption. The combination of ephedrine is equally as effective (or even more effective) than 15 mg dexfenfluramine when taken over 12 weeks. It has been noted that caffeine can, however, increase the effect of ephedrine, regardless of exercise, and that this effect is also observed with green tea. This suggests that methylxanthine compounds (through an increase in adrenaline levels) cause an increase in the effects of ephedrine. Previous animal studies have shown a 10% increase in oxygen consumption with ephedrine supplementation, however human studies are more variable (3.6%, 10.7% (with) and 7.1%). In studies using indirect calorimetry, varying increases were observed, for example, 30.1 ± 5.4 kcal/3 hours with 20 mg ephedrine + 200 mg and 22.7 ± 7.7 kcal/3 hours with half-dose ephedrine. Metabolic rate, thermogenesis, and oxygen consumption are increased when taking ephedrine supplements. This increase is enhanced by the intake of other xanthine compounds. The effect is greater in obese people, and most of all during periods of caloric restriction. The increase in metabolic rate is estimated to be around 5-12%.

Ephedrine: fat burner

Some studies have confirmed that ephedrine (together with ) may have long-term beneficial effects in the fight against diencephalic obesity. Studies of overweight women have shown that three doses of ephedrine at a dose of 20 mg promote weight loss of 2.5 kg in 4 weeks and 5.5 kg in 12 weeks, regardless of changes in diet and exercise. It follows from this that the effect of taking ephedrine decreases over time (regardless of oxygen consumption). Studies have been conducted on drugs such as ECA, which showed that without deliberately restricting the number of calories consumed, obese people lost 2.2 kg of weight in 8 weeks, while the placebo resulted in a weight loss of 0.7 kg. After revealing the drug to the subjects, the result of 2.2 kg increased to 3.2 kg. When restricting caloric intake, over 16 weeks, EC reduced the weight of obese people by 3.4 kg more effectively than placebo, and 30-60 mg of ephedrine (together with 300-600 mg) over 20 weeks reduced weight in adolescents by 5.9 kg more. Moreover, the result of long-term use of ephedrine (5 months) is a constant reduction in weight (5.2 kg), compared with the control group (-0.03 kg). In some studies in which the difference in weight loss among subjects is not statistically significant, important factor are positive trends in the composition of body tissues.

Exercise and skeletal muscle

Skeletal muscle hypertrophy

Ephedrine, as a beta-adrenergic agonist, may preserve muscle mass by reducing nitrogen excretion from the body (and titrating nitrogen balance in positive side). Studies show a decrease in urinary nitrogen after ephedrine use, and in at least one case there was no weight loss due to fat loss, while an increase muscle mass, where over the past eight weeks the subject has lost 4.5kg of fat and 2.8kg of muscle mass. These rates may increase when observing women who are initially obese. Skeletal Muscle enhances ephedrine's fat burning potential by 50% as it primarily targets brown fat stores and skeletal muscle itself.

Ephedrine in bodybuilding

In the study, nine healthy, trained men took 300mg and 60mg of Ephedra sinensis (unaware of the ephedrine content) 60 and 150 minutes before exercise tests - one set each of bench press and vertical row, however, in addition to increasing effort and concentration during exercise, the effect of taking the drugs was no different from the effect of taking 300 mg of sugar (placebo). Then another study was conducted to evaluate the energy return of weight-bearing exercise, this time increasing the dosage of ephedrine (0.8 mg/kg 90 minutes before leg exercise: multiple sets of bench press), and subjects who received ephedrine were able to do 3 more sets than those who received placebo (16 to 13), and in combination with the result increased by another 6 approaches (19 to 16), however, with a smaller increase in approaches (1 to 2, respectively); The researchers believe that fatigue may have played a role in the multiple sets, and that only the results obtained in the first phase of the study are significant (while the subsequent two phases, which included a two-minute break, are statistically insignificant). A single dose of 24 mg ephedrine administered to healthy, trained men did not produce any increase in energy. Dynamometer studies showed no increase in energy from consuming 60mg of Ephedra sinensis (along with 300mg), whereas ephedrine showed an increase in energy during the 30-second Wingate test (only at 5 and 10 seconds) for 90 minutes after administration of 1mg/kg. ; although this study has been criticized for its results being too small (less than 1% improvement over a 30-second period) and therefore not worth the risk of using high doses of ephedrine. Energy gains with lower doses of ephedrine were not significant, while higher doses (0.8-1 mg/kg) produced greater results when administered 90 minutes before exercise. However, due to unnecessary risks and side effects, the advisability of using high dosages is questioned by some researchers.

Physical endurance

In a speed cycling test (in which the placebo response resulted in 12.6 minutes), 1mg/kg ephedrine reduced fatigue by 19%, which is statistically insignificant, however, together with 5mg/kg, the effect increased to 39%, which is already more significant result. A similar result was achieved by other researchers using similar dosages, and an increase in heart rate and a decrease in the feeling of fatigue during physical activity was also noted. Another study was conducted - a 10-kilometer race with equipment (11kg) after taking 0.8 mg/kg ephedrine, which showed that running speed increased by 2.8% in subjects taking ephedrine compared to those taking placebo (same as taking and ephedrine), as a result, the running pace increased in the last 5 km, but the VO2max test did not show any significant changes; this is explained by an increase in serum free fatty acids and modulation of catecholamines (less adrenaline and more dopamine). Ephedrine has been reported to increase endurance during exercise, which may simply be due to an increase in serum free fatty acid levels and possibly a reduction in fatigue during exercise.

Interaction with hormones

Estrogen

Daily administration of 0.5 mg/kg ephedrine has an anti-estrogenic effect in mice and in this regard is more effective than Chinese ephedra and Synephrine.

The cardiovascular system

Blood pressure

Many human studies report small increases in systolic blood pressure ranging from 5 to 23 mmHg, with no effect on diastolic pressure. This effect was short-lived and was caused by exposure to ephedrine. Over a long period of time (8-12 weeks), ephedrine lowers blood pressure, although this is due to weight loss. Sometimes, however, blood pressure does not change. For people with high blood pressure who do not get it lower, taking ephedrine may be problematic, but it is believed that over time the blood pressure may decrease along with weight loss. Apparently, taking ephedrine in controlled dosages has no effect on heart rate. Its change is usually associated with either anxiety or an excessive amount of adrenaline, which is observed when taking ephedrine and.

Heartbeat and heart health

The study found a decrease in serum potassium levels with ephedrine (20 mg x 3). On average, this decrease ranged from 4.1 mmol to 3.7 mmol, although this figure decreased with continuous use of the drug. Other studies have shown a less significant increase in adrenaline levels, although this increase was not observed in urine, but a decrease in nitrogen levels was observed, indicating an improvement in nitrogen balance, and therefore an increase in the ability of muscles to store ephedrine (50 mg three times a day).

Cardiotoxicity and overdose

At high dosages (50 mg/kg body weight) of ma huang (ephedra) or 25 mg/kg ephedrine, clinical and biological signs of toxicity are observed. A dosage of 12.5 mg of Ma Huang per kilogram of body weight (equivalent to 6.25 mg/kg ephedrine) is associated with minimal signs of toxicity. A one-time forced dose of 25 mg of the drug per kilogram of weight (14 times more than the permissible norm for humans) is lethal for rats. According to tests in rats, cardiotoxicity is more pronounced in older individuals. )]

Lipoproteins and triglycerides

Ephedrine (in collaborative studies with ) lowers HDL-C levels during a low-calorie diet without significantly affecting total body cholesterol levels.

Nutrient interactions

Ephedrine, caffeine, aspirin (ECA)

ECA-type drugs were first proposed in 1989 and tested in 1990 as dietary supplements that interact with each other. By that time, it was already known that xanthine compounds (including caffeine), together with 22 mg of ephedrine, accelerate metabolism by approximately two times, and cause a decrease in appetite in animals. Caffeine can speed up metabolism on its own, however, when combined with ephedrine, they enhance each other's effects. The combination of the two drugs is associated with a more effective acceleration of metabolism than taking both drugs separately. This is thought to be due to adenosine antagonism, while the other theory (phosphodiesterase inhibition) is likely to fail in vivo due to the low cellular concentration being insufficient for significant inhibition. Caffeine acts synergistically with ephedrine in vivo and is widely used in weight loss studies in parallel with diet or physical exercise, and some researchers believe that this combination is necessary to ensure that the fat-burning effect of ephedrine differs from the effect of placebo. This may be of minor importance to those for whom ephedrine has no effect without joint reception xanthine compounds. Simply put, those who do not respond to ephedrine respond to the combination of ephedrine and xanthines. It has been estimated that the combination of ephedrine and xanthines is 64% more effective than the effects on the body of each individual. This effect is achieved by pharmacodynamic enhancement, and the combination of drugs does not alter their pharmacokinetic profile in any way. According to the study, the combination of ephedrine does not affect diastolic blood pressure, whereas each drug alone has such an effect. This suggests that the drug combination does not affect systolic blood pressure more than either drug alone. Aspirin has an indirect effect through ephedrine, since aspirin by itself is not as effective in influencing weight change. Ephedrine reduces the weight of animals by 18%, while ephedrine in combination with analgin - by 27%. This combination works through prostaglandin inhibition, resulting in the release of epinephrine when taking ephedrine. Aspirin (together with ephedrine) is not able to significantly increase the thermic effect of food. The combination of ephedrine (25-50 mg), (200 mg) and (300 mg) (“ECA”) is widely known to be an extremely powerful fat burner and has more wide application than ephedrine alone. In this combination, ephedrine acts as a powerful thermogenic stimulant. Helps inhibit lipogenesis by blocking the incorporation of acetate into fatty acids. The athlete can monitor body temperature as a marker for the proper operation of this combination. As a rule, when taking ECA, the temperature increases by 1 degree, which does not cause any noticeable discomfort. The combination is taken 2-3 times a day for several weeks. When body temperature returns to normal, ECA is discontinued because its effectiveness decreases. In order for the drugs to start working at an optimal level again, it is necessary to take a break of at least 4-6 weeks.
Ephedrine is also used by some professional athletes(including in powerlifting) as a stimulant before training or competitions. Small increases in strength and energy can improve anaerobic performance and the final performance of major lifts. It is also believed that the drug enhances brain activity, resulting in increased energy and improved ability to focus on necessary tasks. To produce these effects when needed, ephedrine is usually used in doses of 25-50 mg. It is important to note that this compound is not used continuously, as its effects diminish with habituation. In most cases, the drug is taken only 2 or 3 times a week, usually on days of special importance.
After several weeks of using the drug, it is better to take a break (at least for 1-2 months) to maintain its effectiveness at an optimal level.

Nicotine

Ephedrine and caffeine have been used in studies for weight loss in smokers, smoking cessation has been tried together to reduce weight gain, and although there has been some progress, ephedrine has not been particularly effective in promoting weight loss.

Safety and toxicity

With proper supervision, the combination of ephedrine and is safe for adolescents (14-17 years of age). Some observations suggest that the effects of the drugs are no different from the placebo effect, although a meta-analysis showed a range of 2 to 3.5 units and found that the benefits of such therapy exceed the costs of it. When consuming 20mg/200mg ephedrine/three times daily for 24 weeks, no clinically significant withdrawal symptoms were observed.

Clinical observations

It should be noted that, according to multiple measures obtained during the study of subjects tolerant to ephedrine and patients who did not develop tolerance, no significant differences in the functioning of the cardiovascular system were observed. Moreover, a meta-analysis of 50 studies and 284 case reports submitted to the Office of Quality Assurance food products And medicines, showed that there was an association between ephedrine/ephedra use and increased heart rate, but case reports are not sufficient to draw general conclusions. More serious side effects were identified in a review of the Drug Administration's side-effect data, but the information could cause public panic. This analysis identified only 284 eligible cases out of 18,000 (assuming ephedrine was taken 24 hours before examination). It follows that 98.5% of non-medical cases are caused by hypochondria, although this does not exclude the possibility of actual harm. In people with a history of drug use, ephedrine can cause stroke. There was at least one case of heart damage in a 44-year-old man, but the numbers were skewed by multiple doses of various drugs. Another case report mentioned the use of ephedra, xenadrine and hydroxycut for 2 years, which caused an aneurysm coronary artery, although this was due to xenadrine rather than ephedrine. One case report linked ephedrine to the formation of kidney stones. Ephedrine alkaloids accounted for 95% of the weight of kidney stones in a man with one kidney who was taking 4 medications and had a history of renal failure. However, there have been “more than 200” other cases of kidney stones containing ephedra alkaloids. On at least one occasion, ephedrine has been used to commit suicide. Exact dosage unknown, but it significantly exceeded the dose recommended for therapeutic purposes.

Filterable list

Instructions for medical use

Ephedrine
Instructions for medical use- RU No. LP-000377

Last modified date: 29.03.2017

Dosage form

Injection

Compound

1 ml of solution contains:

Active substance:

Ephedrine hydrochloride – 50 mg.

Excipient :

Water for injection – up to 1 ml

Description of the dosage form

Transparent colorless liquid.

Pharmacological group

Sympathomimetic agent.

Pharmacodynamics

Sympathomimetic, stimulates alpha and beta adrenergic receptors. Acting on varicose thickenings of efferent adrenergic fibers, it promotes the release of norepinephrine into the synaptic cleft. In addition, it has a weak stimulating effect directly on adrenergic receptors. Causes vasoconstrictor, bronchodilator and psychostimulating effects. Increases total peripheral vascular resistance and systemic blood pressure, increases minute blood volume, number of heart contractions and strength of heart contractions, improves atrioventricular conduction; increases skeletal muscle tone and blood glucose concentration; inhibits intestinal motility, dilates the pupil (without affecting accommodation and intraocular pressure). Stimulates the central nervous system; its psychostimulating effect is similar to phenamine. Inhibits the activity of monoamine oxidase and catecholamine-O-methyltransferase. It has a stimulating effect on alpha-adrenergic receptors of blood vessels in the skin, causing constriction of dilated vessels, thus reducing their increased permeability, leading to a decrease in swelling in urticaria.

The onset of therapeutic effect at intramuscular injection 25-50 mg - after 10-20 minutes, duration of action - 0.5-1 hour. With repeated administration at a short interval (10-30 minutes), the pressor effect of ephedrine quickly decreases (tachyphylaxis occurs, associated with a progressive decrease in norepinephrine reserves in varicose thickenings).

Pharmacokinetics

Absorption after intramuscular or subcutaneous administration is rapid.

Metabolized in small quantities in the liver. The half-life at urine pH 5 is 3 hours, at urine pH 6.3 -6 hours.

It is excreted by the kidneys, mainly unchanged. The amount of drug excreted depends on the pH of the urine and increases when the pH of the urine shifts to the acidic side.

Indications

Arterial hypotension (collapse, shock, surgical interventions, spinal anesthesia, trauma, blood loss, bacteremia, overdose of ganglion blockers, adrenergic blockers and other antihypertensive drugs); uncontrolled sympathetic block with various types of central segmental blocks.

Contraindications

Hypersensitivity, insomnia, hypertrophic obstructive cardiomyopathy, pheochromocytoma, ventricular fibrillation, uncontrolled hypertension and tachycardia.

Carefully:

Metabolic acidosis, hypercapnia, hypoxia, atrial fibrillation, angle-closure glaucoma, pulmonary hypertension, hypovolemia, myocardial infarction, occlusive vascular diseases (including a history): arterial embolism, atherosclerosis, Buerger's disease, frostbite, diabetic endarteritis, Raynaud's disease; diseases of the cardiovascular system (including angina pectoris, tachyarrhythmia, ventricular arrhythmia, coronary insufficiency, arterial hypertension), diabetes mellitus, thyrotoxicosis, benign prostatic hyperplasia, simultaneous use of inhalation anesthesia.

If you have one of the listed diseases, be sure to consult your doctor before taking the drug.

Directions for use and doses

Subcutaneously, intravenously and intramuscularly. The route of administration depends on the indications. In case of acute decrease in blood pressure, slow intravenous administration; at infectious diseases, before spinal anesthesia - subcutaneous or intramuscular injection.

Ephedrine is used intravenously as a stream or drip. For a one-step injection, 0.02-0.05 g (0.4-1 ml of a solution with a concentration of 50 mg/ml) is administered slowly in a stream.

When administered by drip, ephedrine is used in an isotonic solution of sodium chloride in a total dose of 0.06-0.08 g; the amount of isotonic solution is from 100 to 800 ml.

For subcutaneous administration, use 0.02-0.05 g (0.4-1 ml) of a solution with a concentration of 50 mg/ml 1-2 times a day.

To prevent a decrease in blood pressure during spinal anesthesia, 1 ml of a solution with a concentration of 50 mg/ml is injected under the skin 10-30 minutes before the start of anesthesia.

Higher doses of ephedrine for adults with subcutaneous administration: single - 0.05 g, daily - 0.1 g.

Side effects

From the nervous system and sensory organs: more often- headache, sleep disturbance; less often- weakness, nervousness, restlessness, dizziness; frequency unknown- convulsions, muscle spasms, tremors, numbness of the arms or legs, drowsiness; when used in high doses- hallucinations, changes in mood or psyche.

From the cardiovascular system: less often- angina pectoris, bradycardia or tachycardia, palpitations, increased or decreased blood pressure, at high doses - ventricular arrhythmias; rarely- feeling of discomfort or pain in chest; frequency unknown- unusual hemorrhages, flushing of the facial skin.

From the digestive system: more often- nausea, vomiting; less often- dryness or irritation of the mouth or throat, loss of appetite; frequency unknown - heartburn.

From the urinary system: less often- difficult and painful urination.

Local reactions: pain or burning at the site of intramuscular injection.

Other: less often- increased sweating, pale skin; narrowing of peripheral blood vessels, allergic reactions, shortness of breath or difficulty breathing, chills, hyperthermia, dilated pupils, blurred vision.

If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor about it .

Overdose

Symptoms: severe weakness, agitation, insomnia, urinary retention, excessive increase in blood pressure, decreased appetite, vomiting, increased sweating, rash.

Treatment: if the hypertensive effect is excessive, reduce the rate of administration or temporarily stop the administration; if ineffective, use short-acting alpha-blockers.

Interaction

Weakens the effects of narcotic analgesics and sleeping pills.

Medicines that alkalinize urine (including antacids containing Ca 2+ and Mg 2+, carbonic anhydrase inhibitors, citrates, sodium bicarbonate) increase the half-life of ephedrine and the risk of intoxication.

When used simultaneously with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, inhalation anesthesia agents (chloroform, enflurane, halothane, isoflurane, methoxyflurane, trichlorethylene), the risk of developing severe ventricular arrhythmias increases; with other sympathomimetic drugs - increased severity of side effects from the cardiovascular system; with antihypertensive drugs (including sympatholytics, diuretics, rauwolfia alkaloids) - a decrease in the hypotensive effect.

Concomitant use with adrenergic bronchodilators can lead to additional excessive stimulation of the central nervous system, which can cause increased excitability, irritability, insomnia, convulsions, and arrhythmias.

Cocaine enhances the stimulant effect on the central nervous system and cardiovascular system.

Co-administration with reserpine and monoamine oxidase inhibitors (including furazolidone, procarbazine, selegiline) can cause headache, cardiac arrhythmias, vomiting, a sudden and pronounced increase in blood pressure, hyperpyretic crisis; with non-selective beta-blockers and nitrates - weakening of the therapeutic effect (blockade of beta-adrenergic receptors can lead to the predominance of alpha-adrenergic activity with the risk of developing arterial hypertension and pronounced bradycardia with the possible development of heart block; blockade of run-adrenergic receptors also interferes with the beta 2 -adrenergic bronchodilator effect); with phenoxybenzamine - increased hypotensive effect and tachycardia; with phenytoin - a sudden decrease in blood pressure and bradycardia (depending on the dose and rate of administration); with thyroid hormone preparations - mutual enhancement of action.

Increases the metabolic clearance of glucocorticosteroids, adrenocorticotron hormones with long-term use (adjustment of their doses may be required); neurological effects of diatrizoates, iothalamic and ioxaglic acids.

Ergometrine, ergotamine, methylergometrine, oxytocin increase the vasoconstrictor effect and the risk of ischemia and gangrene, as well as severe arterial hypertension, including intracranial hemorrhage.

Doxapram, sympatholytics (guanadrel, guanethidine), mazindol, mecamylamine, methyldopa, trimethaphan, methylphenidate enhance the pressor effect.

Levodopa increases the risk of arrhythmias (requires a reduction in the dose of the sympathomimetic).

Strengthens the stimulating effect (mutually) on the central nervous system of mazindol, methylphenidate.

Ritodrine enhances (mutually) the effects (including side effects).

Strengthens the stimulating effect on the central nervous system and the risk of toxic effects of xanthines (including aminophylline, caffeine, diphylline, oxtriphylline, theophylline).

special instructions

During infusion, a device with a measuring device should be used to regulate the rate of infusion. Infusions should be carried out into a large (preferably central) vein. During the treatment period, it is recommended to measure blood pressure, urine volume, minute blood volume, electrocardiogram, central venous pressure, pressure in pulmonary artery and pulmonary capillary wedge pressure.

To avoid the development of sleep disturbances at night, ephedrine and medications containing it should not be prescribed at the end of the day or before bedtime.

It is recommended to be careful to avoid the drug entering the perivascular tissue, which can cause necrosis (in the event of extravasation formation, infiltration of 10-15 ml of 0.9% NaCl containing 5-10 ml of phentolamine should be immediately infiltrated). Excessive doses during myocardial infarction may increase ischemia by increasing myocardial oxygen demand.

Before starting treatment, hypovolemia should be corrected if possible. Treatment with ephedrine does not replace transfusions of blood, plasma, blood substitutes and/or saline solutions.

Ephedrine is not advisable for long-term use (narrowing of peripheral blood vessels, leading to the possible development of necrosis or gangrene).

When prescribed for the correction of arterial hypotension or adding a local anesthetic drug to the solution during labor/delivery, as well as joint administration with certain medicines, stimulating labor (for example, vasopressin, ergotamine, ergonovine, methylergonovine), can cause persistent arterial hypertension (up to rupture of cerebral vessels); during spinal anesthesia, it may increase the fetal heart rate.

If the mother's blood pressure exceeds 130/80 mmHg, ephedrine is not recommended.

Due to its stimulating effect on the central nervous system, it can be abused by drug addicts.

When discontinuing treatment, doses should be reduced gradually, as sudden discontinuation of therapy can lead to severe hypotension. If the solution is opaque, it cannot be administered. The unused portion should be destroyed.

Monoamine oxidase inhibitors, increasing the pressor effect of sympathomimetics, can cause headaches, arrhythmia, vomiting, hypertensive crisis, therefore, when patients take monoamine oxidase inhibitors in the previous 2-3 weeks, the dose of sympathomimetics should be reduced (to 1/10 of the usual dose).

Release form

Solution for injection 50 mg/ml in ampoules of 1 ml.

5 ampoules in a blister pack made of polyvinyl chloride film and printed aluminum foil, varnished or without foil.

1 or 2 blister packs (with or without foil) together with instructions for use of the drug, a knife or an ampoule scarifier are placed in a cardboard pack.

20, 50 or 100 contour blister packs with foil along with 20, 50 or 100 instructions for use of the drug, respectively, knives or ampoule scarifiers are placed in a cardboard box or in a corrugated cardboard box (for a hospital).

When packaging ampoules with rings or break points, scarifiers or ampoule knives are not used.

Storage conditions

In a place protected from light at a temperature not exceeding 25 o C.

Keep out of the reach of children.

Best before date

5 years. Do not use after the expiration date indicated on the packaging.

Conditions for dispensing from pharmacies

Dispensed by prescription.

Ephedrine - instructions for medical use - RU No.

Ephedrine has psychostimulating, vasoconstrictor, bronchodilator, hypertensive, hyperglycemic effects.

Has a large list of indications. Despite the fact that this drug is prohibited in some countries, in Russia the drug is actively used to treat adult patients.

Medicines are dispensed from pharmacies with a prescription.

Before use, you should consult your doctor.

pharmachologic effect

It is a sympathomimetic, stimulates beta and alpha adrenergic receptors. It has a weak stimulating effect on adrenergic receptors. It has a psychostimulating, bronchodilating, vasoconstrictor effect.

Increases the strength of heart contractions, improves AV conduction, heart rate and IOC, increases systemic blood pressure and peripheral vascular resistance; increases blood glucose concentration and skeletal muscle tone; dilates the pupil (without affecting intraocular pressure and accommodation), inhibits intestinal motility.

Stimulates the central nervous system, close to phenamine in psychostimulating effect. Inhibits the activity of catecholamine-O-methyltransferase and MAO. It has a stimulating effect on alpha-adrenergic receptors of blood vessels, causes a narrowing of dilated blood vessels, reduces increased vascular permeability and reduces swelling in urticaria.

15-60 minutes after using Ephedrine, the onset of the therapeutic effect is noted, and the duration of action is three to five hours. With intramuscular administration of 25-50 mg of the drug, the effect is observed within 10-20 minutes and 30-60 minutes. respectively.

If the drug is administered repeatedly at short intervals (from 10 to 30 minutes), the pressor effect of the active component is sharply reduced (tachyphylaxis appears due to a progressive decrease in norepinephrine reserves in varicose thickenings).

Indications for use

The medicine is prescribed for rhinitis (including vasomotor, catarrhal), hay fever, sinusitis, arterial hypotension (shock, collapse, spinal anesthesia, surgery, trauma, bacteremia, blood loss, overdose of ganglion-blocking blockers and other antihypertensive drugs); urticaria, bronchial asthma, serum sickness (as part of combination treatment); depression, narcolepsy, bleeding from the pulp of teeth and gums, poisoning with drugs and sleeping pills; diagnostic activities in ophthalmology (to dilate the pupil).

Mode of application

Ephedrine is used orally, intramuscularly, locally, intravenously, subcutaneously.

For bronchial asthma and other allergic diseases take 25-50 mg of the drug orally twice or thrice a day for 10-25 days or in cycles of 3-4 days with three-day breaks.
Before spinal anesthesia and during bacteremia IM and SC, adults – 20-50 mg twice or thrice a day.
For arterial hypotension subcutaneously, intravenously in a stream (slow), 0.4-1 ml of a five percent solution (20-50 mg), or 750 mcg/kg, or 25 mg/sq.m., or intravenously drip, in 100-500 ml 0.9 - percent NaCl solution or five percent dextrose solution in a total dose of up to 80 mg. The dose can be repeated subject to blood pressure control.
For children as a central nervous system stimulant or bronchodilator orally, subcutaneously or intravenously – 100 mg/sq.m./day or 3 mg/kg in four to six divided doses.
For children as a vasoconstrictor drug subcutaneously or intravenously, 750 mcg/kg or 25 per 1 square meter of body surface four times a day, according to the patient’s response.
In ophthalmological practice Ephedrine solutions 1-5%, for vasomotor rhinitis - 2-3% solution.

Maximum doses of the drug for oral administration and subcutaneous administration: daily – 150 mg, single – 50 mg.

Release form, composition

The drug is available in the form of nasal drops, tablets, and solution for injection.

The active component of the drug is ephedrine hydrochloride.

Interaction with other drugs

Drugs that alkalinize urine (including antacids containing Mg2+ Ca2+, sodium bicarbonate, citrates, carbonic anhydrase inhibitors) increase the risk of intoxication, as well as the half-life of ephedrine.

The use of the drug weakens the effects of hypnotics and narcotic analgesics.

Concurrent use of quinidine, cardiac glycosides, dopamine, tricyclic antidepressants, inhalation anesthesia (enflurane, isoflurane, trichlorethylene, chloroform, halothane, methoxyflurane) is fraught with the development of severe ventricular arrhythmias; antihypertensive drugs (including sympatholytics, rauwolfia alkaloids, diuretics) – decreased hypotensive effect; other sympathomimetic drugs – increased severity of adverse reactions from the cardiovascular system.

Cocaine enhances the stimulating effect on the cardiovascular system and central nervous system.

The simultaneous use of adrenergic bronchodilators can cause excessive stimulation of the central nervous system, increased excitability, insomnia, irritability, arrhythmia, and convulsions.

Mutually enhances the stimulating effect on the central nervous system of methylphenidate, mazindol.

Co-administration with MAO inhibitors (including selegiline, procarbazine, furazolidone) and reserpine can cause cardiac arrhythmias, headaches, hyperpyretic crisis, severe sudden increase in blood pressure, vomiting; with nitrates, non-selective beta-blockers - weakening of the therapeutic effect; with phenoxybenzamine – tachycardia, increased hypotensive effect; with phenytoin - bradycardia and sudden decrease in blood pressure (depending on the rate of administration and dose); with thyroid hormone preparations – mutual enhancement of action.

Ergotamine, oxytocin, ergometrine, methylergometrine increase the vasoconstrictor effect of the drug, the risk of gangrene and ischemia, as well as severe arterial hypertension, including intracranial hemorrhage.

Helps increase the metabolic clearance of GCS, ACTH with long-term use (it may be necessary to adjust their doses); neurological effects of ioxaglic and iothalamic acids, diatrizoates.

Levodopa increases the risk of arrhythmias (reducing the dose of the sympathomimetic is necessary).

Doxapram, mazindol, methyldopa, methylphenidate, sympatholytics (guanethidine, guanadrel), mecamylamine, trimetaphan enhance the pressor effect.

The drug increases the likelihood of developing toxic effects of xanthines (including caffeine, oxtriphylline, aminophylline, diphylline, theophylline), ritodrine mutually enhances the effects (including side effects)

Side effects

Nervous system frequency unknown - muscle spasms, numbness of extremities, drowsiness, tremor, convulsions; when prescribed in high doses – changes in mentality/mood, hallucinations; more often – sleep disturbance, headaches; less often – dizziness, nervousness, weakness, restlessness.
Digestive system frequency unknown – heartburn; more often – vomiting, nausea; less often - irritation or dryness of the pharynx or oral cavity (for parenteral use), loss of appetite.
Local reactions burning or pain at the site of intramuscular injection.
SSS less often – tachycardia, bradycardia, angina pectoris, palpitations, decreased or increased blood pressure; when prescribed in high doses – ventricular arrhythmias; frequency unknown - facial skin flushing, unusual hemorrhages; rarely – pain or discomfort in the chest.
Urinary system less often – painful and difficult urination.
Others less often – pallor of the skin, increased sweating; allergic reactions, constriction of peripheral vessels, difficulty breathing or shortness of breath, blurred visual perception, dilated pupils, hyperthermia, chills.

Overdose

Accompanied by agitation, severe weakness, urinary retention, insomnia, decreased appetite, severe increase in blood pressure, heavy sweating, vomiting, rash.

Therapy: if the hypertensive effect is pronounced, temporarily stop administration or reduce the rate of administration. If these measures are ineffective, short-acting alpha-blockers are used.

Contraindications

The medicine is not prescribed to patients with insomnia, hypersensitivity to Ephedrine, pheochromocytoma, HOCM, uncontrolled arterial hypertension and tachycardia, ventricular fibrillation.

The drug is prescribed with caution for hypercapnia, metabolic acidosis, atrial fibrillation, hypoxia, pulmonary hypertension, angle-closure glaucoma, myocardial infarction, hypovolemia; diseases of occlusive vessels (including previously suffered): atherosclerosis, arterial embolism, frostbite, Buerger's disease, Raynaud's disease, diabetic endarteritis; diseases of the cardiovascular system (including tachyarrhythmia, angina pectoris, ventricular arrhythmia, arterial hypertension, coronary insufficiency); thyrotoxicosis, diabetes mellitus, benign prostatic hyperplasia, concurrent use of drugs for inhalation anesthesia.

During pregnancy

Prescribing Ephedrine to nursing and pregnant patients is possible provided that the expected benefit to the mother or expectant mother is higher than the existing risk to the child/fetus.

Prescribing drugs to correct arterial hypotension or adding local anesthetic drugs to the solution during childbirth, as well as simultaneous administration with certain drugs that stimulate labor, is fraught with the development of persistent arterial hypertension; during spinal anesthesia, the drug may increase the fetal heart rate.

If the mother's blood pressure rises above 130/80, it is better not to use the drug.

Terms, storage conditions

The drug can be stored for no more than five years in its original packaging. The storage place should be dark, and the temperature there should not exceed 25 degrees.

Price

Approximate cost of the drug in the Russian Federation is 1000 rubles.

In Ukrainian pharmacies the drug is not presented.

Analogs

Ephedrine analogues include drugs containing the same active ingredient: Broncholitin, Teofedrine-N, Ephedrine Hydrochloride.

These drugs can be purchased only with a prescription, because they are considered potent.