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. 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.
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%.
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 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.
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, as well as increase the glucose level in the blood, however, 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 improve efficiency 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
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.
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.
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 recent 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 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.
Ephedrine (either ephedrine hydrochloride or ephedrine sulfate) is most often supplied in tablets of 25 or 50 mg each.
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 don't contain enough large number ephedrine alkaloids, however, anecdotally, may contain pseudoephedrine. According to some studies, ephedra plants from North America do not contain either ephedrine or pseudoephedrine.
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 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.
Ephedrine is a sympathomimetic amine, similar in structure to amphetamine or methamphetamine. It has the chemical name (1 R,2S)-2-(methylamino)-1phenylpropane1-0l.
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. Mental and physical changes The changes that occur as a result of taking this drug are very similar to the changes observed with 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 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.
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 supplements increase 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.
Ephedrine is the most effective stimulant during calorie restriction. Stimulation effect brain activity is most powerful when combined with ephedrine.
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.
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 for longer. long period(4-12 weeks) rather than intermittently, and it is possible that the underlying mechanism for 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 more pronounced in obese people, and most of all during periods of caloric restriction. The increase in metabolic rate is estimated to be around 5-12%.
Some studies have confirmed that ephedrine (along with ) may have long-term benefits. positive impact 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.
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 acts on storage brown fat and the skeletal muscles themselves.
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). One single dose 24 mg of 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), making the risk of using high doses of ephedrine unjustified. 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.
In a cycling speed test (in which the placebo response was 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.
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.
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 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.
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).
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. )]
Ephedrine (in joint research c) lowers HDL-C levels during a low-calorie diet without significantly affecting general level cholesterol in the body.
ECA-type drugs were first proposed in 1989 and tested in 1990 as biological active additives, which 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 two drugs is associated with more efficient acceleration 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 in those who are not affected by ephedrine without co-administration of 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 extremely powerful tool for burning fat, and having 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 track body temperature as a marker proper operation 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 powerlifting) as a stimulant before training or competition. Small increases in strength and energy can improve anaerobic performance and the final performance of major lifts. The drug is also believed to enhance brain activity, resulting in increased energy and an 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.
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.
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.
It should be noted that, according to multiple measures obtained during the study of ephedrine-tolerant and non-tolerant subjects, no significant differences in performance were observed. cardiovascular system. Moreover, a meta-analysis of 50 studies and 284 case reports submitted to the Office of Quality Assurance food products and medications, showed that there was an association between ephedrine/ephedra use and increased heart rate, but medical records 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 who have taken in the past narcotic substances, 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 the use of many different 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 kidney stones in a person with one kidney who was taking 4 types of medications and had a history of kidney 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. The exact dosage is unknown, but it was significantly higher than the dose recommended for therapeutic purposes.
Name:
Name: Ephedrine hydrochloride (Ephedrini hydrochloridum)
Indications for use:
Ephedrine is used to constrict blood vessels and reduce inflammation in rhinitis (inflammation of the nasal mucosa), as a means to increase blood pressure at surgical interventions(especially when spinal anesthesia), for injuries, blood loss, infectious diseases, hypotension (low blood pressure), etc. It is also used (usually in combination with other drugs) for bronchial asthma, and sometimes for hay fever, urticaria, serum sickness and others allergic diseases. It is also used for myasthenia gravis (muscle weakness), narcolepsy (disease of the central nervous system), poisoning with sleeping pills and drugs, and enuresis (bedwetting). The effect of enuresis is associated with a stimulating effect on the central nervous system, due to which sleep becomes less deep and it is easier to wake up when the urge to urinate appears.
A solution of ephedrine is used locally as a vasoconstrictor and to dilate the pupil (with diagnostic purpose V ophthalmological practice).
The drug is also used in cardiology to treat disorders heart rate.
Pharmacological action:
Stimulates alpha and beta adrenoreceptors.
In terms of its peripheral sympathomimetic effect, ephedrine is close to adrenaline. Causes vasoconstriction, increased blood pressure, dilation of the bronchi, inhibition of intestinal peristalsis (wave-like movements), dilated pupils, and increased blood glucose levels.
Compared to adrenaline, ephedrine has a less dramatic, but much longer-lasting effect. Due to its greater stability, ephedrine is effective when administered orally and is convenient for use in course treatment(for example, for allergic diseases).
Unlike adrenaline, ephedrine has a specific stimulating effect on the central nervous system. In this respect, it is close to phenamine, but subsequently it acts much more strongly.
Ephedrine hydrochloride: route of administration and dosage:
Ephedrine is used orally (before meals), under the skin, into muscles and into a vein, also topically.
In case of acute decrease in blood pressure, slow intravenous administration; for infectious diseases, before spinal anesthesia, etc. - subcutaneous or intramuscular administration; for bronchial asthma and other allergic diseases it is usually prescribed orally.
Adults are prescribed 0.025-0.05 g orally 2-3 times every day.
The course of treatment usually lasts 10-15 days. You can also prescribe in cycles of 3-4 days with 3-day breaks.
For enuresis, it is prescribed before bedtime.
For bronchial asthma, ephedrine is used in combination with theophylline, diphenhydramine, calcium gluconate and other drugs.
Children are prescribed ephedrine orally in the following doses: from 1 year of age - 0.002-0.003 g; 2-5 years - 0.003-0.01 g; from 6 to 12 years - 0.01-0.02 g per dose.
For adults, 0.02-0.05 g is administered subcutaneously and intramuscularly 2-3 times every day; administered intravenously to adults in a stream (slowly) of 0.02-0.05 g (0.4-1 ml of a 5% solution) or by drip in 100-500 ml isotonic solution sodium chloride or 5% glucose solution in a total dose of up to 0.08 g (80 mg).
Higher doses of ephedrine for adults orally and under the skin: single - 0.05 g, daily - 0.15 g.
In ophthalmic practice, 1-5% solutions are used ( eye drops). At vasomotor rhinitis(inflammation of the nasal mucosa) - 2-3% solutions.
Ephedrine is used only as prescribed by a doctor.
Ephedrine should not be used for a long time.
To avoid disruption of nighttime sleep, ephedrine and products containing it should not be administered at the end of the day or before bedtime.
Ephedrine hydrochloride contraindications:
Insomnia, hypertension (high blood pressure), atherosclerosis, organic heart disease, hyperthyroidism (thyroid disease).
Ephedrine hydrochloride side effects:
The drug is usually well tolerated. Sometimes, 15-30 minutes after ingestion, slight trembling and palpitations are observed. These phenomena pass quickly. An overdose of the product can cause a number of toxic phenomena: nervous agitation, insomnia, circulatory disorders, tremors of the limbs, urinary retention, loss of appetite, vomiting, increased sweating, rash.
Release form:
Powder; tablets 0.002; 0.003 and 0.001 g (for pediatric practice); 5% solution (for injection) in ampoules of 1 ml; 2% and 3% solutions in 10 ml bottles (for otorhinolaryngological practice).
Synonyms:
Ephedrine hydrochloride, Efalon, Ephedrozan, Neofedrin, Sanedrin, Efetonin, etc.
Storage conditions:
List B. Powder - in a well-closed container, protected from light; tablets, ampoules and solutions in bottles - in a place protected from light.
Additionally:
An alkaloid contained in various types of ephedra (Ephedra L.), fam. ephedraaceae (Ephedraceae), including Ephedra equisetina Bge. (ephedra horsetail), growing in the mountainous regions of Central Asia and Western Siberia, Ephedra monosperma S.A.M., growing in Transbaikalia, etc.
Ephedrine is also included in the combination products aitastman, astapect, astapectcodeine, astfillin, broncholitin, gambaran, dixafen, ear drops with prednisolone, Coldex Teva, sunoref ointment, passuma, solutan, spasmoveralgin, theophedrine, theophedrine N, franol, efatin.
Attention!
Before using the medication, you should consult your doctor.
The instructions are provided for informational purposes only.
Instructions for use medicine for specialists
Ephedrine hydrochloride
Trade name
Ephedrine hydrochloride
International nonproprietary name
Dosage form
Solution for injection, 5% 1 ml
1 ml of solution contains
active substance - ephedrine hydrochloride 50.0 mg,
excipients - water for injection up to 1.0 ml.
Description
Transparent, colorless or slightly yellowish liquid
Pharmacotherapeutic group
Drugs for the treatment of obstructive airway diseases. Alpha and beta adrenergic agonists.
ATC code R03CA02
Pharmacological properties
Pharmacokinetics
Metabolized in small quantities in the liver. The half-life is 3-6 hours. It is excreted by the kidneys, mainly unchanged.
Pharmacodynamics
Ephedrine hydrochloride stimulates the activity of the heart (increases the frequency and strength of contractions), facilitates atrioventricular conduction, increases blood pressure, causes a bronchodilator effect, suppresses intestinal motility, dilates the pupil (without affecting accommodation and intraocular pressure), increases the tone of skeletal muscles, causes hyperglycemia. Unlike adrenaline ephedrine has a specific stimulating effect on the central nervous system. Ephedrine is used to constrict blood vessels and reduce inflammation in rhinitis, to increase blood pressure during surgery, in case of injuries, blood loss, arterial hypotension. Sometimes used for bronchial asthma.
Indications for use
Arterial hypotension (collapse, shock, surgical interventions,
especially spinal anesthesia, trauma, blood loss,
infectious diseases)
Bronchial asthma, hay fever, urticaria, serum sickness
(as part of combination therapy)
Myasthenia gravis, narcolepsy
Poisoning sleeping pills and drugs
Directions for use and doses
Adults are administered 20-50 mg (0.4-1 ml of 5% solution) 2-3 times a day under the skin and intramuscularly. In case of acute decrease in blood pressure, adults are administered intravenously in a stream (slowly!) at 20-50 mg (0.4-1 ml of a 5% solution) or by drip in 100-500 ml of isotonic sodium chloride solution or 5% glucose solution in a total dose of up to 80 mg ( up to 1.6 ml). Higher doses of ephedrine for adults under the skin: single 50 mg (1 ml of 5% solution), daily 150 mg (3 ml of 5% solution).
Ephedrine hydrochloride is not intended for long-term use.
Ephedrine is used only as prescribed by a doctor!
Side effects
Loss of appetite, vomiting
Increased sweating, palpitations
Heart rhythm disturbances
Significant increase in blood pressure
Excitation
Insomnia
Tremor of limbs
Urinary retention
Skin rash
Contraindications
atherosclerosis
arterial hypertension
organic heart disease
hyperthyroidism
insomnia
glaucoma
Drug interactions
Ephedrine weakens the effect of opioid analgesics and other central nervous system depressants. With simultaneous use of sreserpine and monoamine oxidase inhibitors (MAOIs), a sharp increase in blood pressure is possible, with non-selective beta-blockers - a decrease in bronchodilator effect. When used simultaneously with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, drugs for inhalation anesthesia(chloroform, enflurane, halothane, isoflurane, methoxyflurane, trichlorethylene) the risk of developing severe ventricular arrhythmias increases; with other sympathomimetic drugs - increased severity of side effects from cardiovascular system.Use with antihypertensive drugs (including sympatholytics, diuretics, rauwolfia alkaloids) leads to a decrease 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. Ergometrine, ergotamine, methylergometrine, oxytocin increase the vasoconstrictor effect and the risk of ischemia and gangrene, as well as severe arterial hypertension, up to intracranial hemorrhage.
Special instructions
To avoid disruption of nighttime sleep, ephedrine hydrochloride should not be administered late in the day or before bedtime. If the solution is opaque, it cannot be administered; the unused part should be destroyed.
Pregnancy and lactation
The use of ephedrine during pregnancy and lactation is only possible if the potential benefit to the mother outweighs possible risk for fetus or infant
Features of the effect of the drug on the ability to drive vehicle or potentially dangerous mechanisms
Considering the side effects of the drug, caution should be exercised when driving vehicles and moving machinery.
Overdose
Symptoms: nervous excitement, insomnia, urinary retention, increased blood pressure, trembling limbs, loss of appetite, vomiting, increased sweating, rash.
Treatment is symptomatic.
Release form and packaging
1 ml in ampoules of neutral glass No. 5 or No. 10 in a blister pack or 1 ml in ampoules No. 10 in a cardboard box along with instructions for use.
Storage conditions
Store in a dry place, protected from light, at a temperature from +2°C to +30°C.
Keep out of the reach of children!
Shelf life
Do not use after expiration date.
Conditions for dispensing from pharmacies
By prescription
Manufacturer
JSC "Khimpharm", Shymkent,
REPUBLIC OF KAZAKHSTAN, st. Rashidova, b/n,
t/f (725-2) 560722, (725-2) 560533.
The main substance is ephedrine hydrochloride. What is it and how does it work? Active ingredient stimulates beta and alpha adrenergic receptors. Under the influence of the drug, release occurs norepinephrine into the lumen of the synaptic cleft. The medication acts on varicose thickenings in adrenergic, efferent fibers. Ephedrine can have a mild stimulating effect on adrenergic receptors.
The drug causes psychostimulant, bronchodilator and vasoconstrictor effects on the body. The drug improves atrioventricular conduction , increases heart rate, IOC, strength of heart contractions, increases the level of systemic and peripheral vascular resistance, inhibits intestinal motility, increases blood sugar levels, and increases the tone of skeletal muscles.
The active substance dilates the pupil without affecting And accommodation . In terms of psychostimulating effects, the medication is close to . Medicine is able to inhibit the activity of catecholamine-0-methyltransferase, monoamine oxidase. The medication stimulates alpha adrenergic receptors in blood vessels skin, narrowing dilated vessels, which leads to a decrease in their increased permeability. This mechanism explains the decrease in the severity of edema with.
When taking ephedrine orally therapeutic effect develops in 15-60 minutes, lasts about 5 hours. At intramuscular injection the effect is registered after 10-20 minutes and lasts about an hour.
Pressor effect medicine for reintroduction after 10-30 minutes it quickly decreases, tachyphylaxis develops, caused by a decrease in norepinephrine reserves in varicose thickenings.
Cardiovascular system: discomfort and pain in the chest, ventricular , drop in blood pressure, palpitations, tachycardia or bradycardia, angina pectoris, skin hyperemia, unusual hemorrhages.
Excessive amounts of the drug during myocardial infarction can cause intensification and progression ischemia due to increased oxygen demand of myocardial tissue.
Before therapy, hypovolemia is corrected.
The administration of ephedrine is not a replacement for saline solutions, blood substitute fluids, plasma, or blood.
Unacceptable long-term treatment ephedrine.
During spinal anesthesia, the drug may cause increased heart rate in the fetus.
The medication can cause persistent arterial hypertension when combined with drugs that increase labor, when adding local anesthetics during delivery.
It is unacceptable to use an opaque solution.
The remaining solution after infusion is destroyed.
Previously, ephedrine was taken orally for the treatment of myasthenia gravis and enuresis.
When taking monoamine oxidase inhibitors together, there is an increase in the pressor effect of sympathomimetics, which causes vomiting, headaches, arrhythmia, and increases the risk hypertensive crisis .
There are many ways to synthesize this alkaloid.
The medicine is described in Wikipedia. There is also a corresponding pharmacopoeial monograph.
The combination of ephedrine + caffeine + is used in bodybuilding and fitness for “drying”. However, we do not recommend using it as it may be dangerous to your health.
Level 4 ATX code matches:
Analogues include drugs containing the same active substance: , , Ephedrine Hydrochloride. These medications can only be purchased with a prescription, as they are potent. They should also be used under the supervision of a doctor.
Included in the preparations
ATX:R.03.C.A.02 Ephedrine
Pharmacodynamics:Sympathomimetic (indirect-acting adrenergic agonist), an alkaloid derived from various types ephedra (Ephedra L.) of the ephedra family (Ephedraceae). , found in plants, is a levorotatory isomer. Synthetically obtained racemate, inferior in activity levorotatory isomer.
After the administration of ephedrine, α- and β-adrenergic receptors are excited: acting on varicose thickenings of efferent adrenergic fibers, it promotes the release of the mediator norepinephrine into the synaptic cleft. In addition, it has a weak stimulating effect directly on adrenergic receptors.
Stimulates the activity of the heart (increases the frequency and strength of contractions), facilitates atrioventricular conduction, increases blood pressure, causes a bronchodilator effect, suppresses intestinal motility, dilates the pupil (without affecting accommodation and intraocular pressure), increases the tone of skeletal muscles, causes hyperglycemia.
Unlike epinephrine, the effect of ephedrine develops slowly but lasts longer. With repeated administration of ephedrine at a short interval (10-30 minutes), its pressor effect quickly decreases - tachyphylaxis (rapid addiction) occurs, associated with a progressive decrease in norepinephrine reserves in varicose thickenings.
Ephedrine stimulates the central nervous system and is similar in psychostimulating effect to phenamine.
Inhibits the activity of MAO and catechol-O-methyltransferase.
Pharmacokinetics:Absorption is good. Biotransformation in the liver (insignificant). The half-life is 3-6 hours (shortened by acidification of urine). Elimination by the kidneys, mainly unchanged (increased by acidification of urine).
Indications:Arterial hypotension with surgical operations(especially during spinal anesthesia), trauma, blood loss, infectious diseases.
Bronchial asthma and other obstructive diseases respiratory tract, vasomotor and allergic rhinitis, sinusitis (for narrowing of blood vessels in the nasal mucosa), serum sickness, urticaria and other allergic conditions.
Narcolepsy, enuresis (as a result of the stimulating effect on the central nervous system, sleep becomes less deep, waking up becomes easier when the urge to urinate appears), myasthenia gravis.
In ophthalmological practice: to dilate the pupil for diagnostic purposes.
V.F90-F98.F98.0 Enuresis of inorganic nature
VI.G70-G73.G70.2 Congenital or acquired myasthenia gravis
IX.I95-I99.I95 Hypotension
X.J30-J39.J30.3 Other allergic rhinitis
X.J30-J39.J30.1 Allergic rhinitis caused by plant pollen
X.J30-J39.J30.0 Vasomotor rhinitis
X.J30-J39.J32 Chronic sinusitis
X.J00-J06.J01 Acute sinusitis
X.J40-J47.J44 Other chronic obstructive pulmonary disease
X.J40-J47.J45 Asthma
XII.L50-L54.L50 Urticaria
XXI.Z00-Z13.Z01.0 Eye and vision examination
XIX.T80-T88.T80.6 Other serum reactions
Contraindications:Uncontrolled arterial hypertension and tachycardia, hypertrophic obstructive cardiomyopathy, insomnia, pheochromocytoma, ventricular fibrillation.
With caution:Use with caution in 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 hyperplasia prostate gland, simultaneous use of inhalation anesthesia.
Pregnancy and lactation:The use of ephedrine during pregnancy and lactation ( breastfeeding) is possible only if the potential benefit to the mother outweighs the possible risk to the fetus or infant.
Directions for use and dosage:Adults are administered 20-50 mg subcutaneously, intramuscularly or intravenously; orally - 25-50 mg 2-3 times a day.
For local use, the dosage regimen is individual.
Maximum doses: for adults, when taken orally and subcutaneously, a single dose is 50 mg, daily dose- 150 mg.
Side effects:From the outside CNS and peripheral nervous system: headache, sleep disturbance, weakness, nervousness, restlessness, dizziness, convulsions, muscle spasms, tremor, numbness of the arms or legs, drowsiness, dilated pupils, blurred vision; when used in high doses - hallucinations, changes in mood or psyche.
From the outside cardiovascular system: angina, bradycardia or tachycardia, palpitations, increased or decreased blood pressure, ventricular arrhythmias, discomfort or pain in chest, hemorrhages, flushing of the facial skin, narrowing of peripheral vessels.
From the outside digestive system: nausea, vomiting, dryness or irritation of the mouth or pharynx (with parenteral use), loss of appetite, heartburn.
From the outside urinary system: difficult and painful urination.
Others: increased sweating, pale skin, allergic reactions, shortness of breath or difficulty breathing, chills, hyperthermia; local reactions- pain or burning at the site of intramuscular injection.
Overdose:Hypertension, arrhythmias, transient bradycardia with transition to tachycardia, myocardial infarction, pulmonary edema, renal failure, metabolic acidosis, dyspnea, headache, vomiting, unusual pallor, cold skin.
Treatment is symptomatic.
Interaction:Ephedrine weakens the effect of opioid analgesics and other CNS depressants.
When used simultaneously with non-selective beta-blockers and nitrates - weakening therapeutic action(blockade of β-adrenergic receptors can lead to the predominance of alpha-adrenergic activity with the risk of developing arterial hypertension and pronounced bradycardia with possible development heart block; blockade of beta-adrenergic receptors also interferes with the beta 2 -adrenergic bronchodilator effect).
Drugs that alkalinize urine (including antacids containing calcium and magnesium ions, carbonic anhydrase inhibitors, citrates) increase the half-life of ephedrine and the risk of intoxication.
When used simultaneously with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, inhalation anesthesia (chloroform, enflurane, methoxyflurane, trichlorethylene), the risk of developing severe ventricular arrhythmias increases; with other sympathomimetics - increased severity of side effects from the cardiovascular system; with antihypertensive drugs (including sympatholytics, diuretics, rauwolfia alkaloids) - a decrease in the hypotensive effect.
Simultaneous use with bronchodilators and beta-agonists may result in additional excessive stimulation of the central nervous system, which can cause increased excitability, irritability, insomnia, convulsions, and arrhythmias.
When used simultaneously with reserpine and MAO inhibitors (including,), headache, heart rhythm disturbances, vomiting, sudden and pronounced increase in blood pressure, hyperpyretic crisis are possible; 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 metabolic clearance of glucocorticosteroids, ACTH with long-term use(dosage adjustment may be required). , ergotamine, increase the vasoconstrictor effect and the risk of ischemia and gangrene.
Levodopa increases the risk of arrhythmias (reducing the dose of the sympathomimetic is required).
Increases the stimulating effect on the central nervous system and the risk of toxic effects of xanthines (including aminophylline, theophylline, caffeine).
Cocaine enhances the stimulating effect on the central nervous system and cardiovascular system.
Special instructions:To avoid disruption of night sleep, medications containing it should not be used at the end of the day or before bedtime.
It is not advisable to use for a long time. Due to its stimulating effect on the central nervous system, it can be abused.
Instructions
