Ephedrine is a medication once widely used to increase blood pressure and relieve asthma symptoms. Some have also used it to promote weight loss and lower cholesterol levels. However, the health authorities banned it due to a high risk of abuse and adverse health effects. Read more to learn the uses, side effects, and dangers of ephedrine.
Disclaimer: By writing this post, we are not recommending this drug. Some of our readers who were already taking the drug requested that we commission a post on it, and we are simply providing information that is available in the clinical and scientific literature. Please discuss your medications with your doctor.
As a matter of fact, we strongly advise against the use of banned and unapproved drugs or substances.
What is Ephedrine?
Ephedrine (commonly known as Akovaz) is a medication and stimulant commonly used to increase blood pressure and promote airflow to the lungs [1, 2].
Ephedrine is derived from the plant Ephedra, which has long been used by the Chinese for medicinal purposes. After its initial discovery in 1885, ephedrine became a popular and effective treatment for asthma [3].
It is now used as a recreational drug or nutritional supplement. Ephedrine is banned in many countries including the United States, as it can be misused to make methamphetamine (crystal meth) [3, 4].
Additionally, the FDA prohibited the sale of all dietary supplements containing Ephedra alkaloids, including ephedrine, due to potential adverse effects on heart health [5].
While it is most known to increase blood pressure and treat asthma, people also use ephedrine for weight loss, fatigue, and narcolepsy [6, 7, 8].
Components
Ephedrine exists in 4 different molecular arrangements or isomers. The 4 isomers are classified as true ephedrine or pseudoephedrine, depending on the way their chemical structures are rotated around their centers [9].
Pseudoephedrine is a diastereomer of ephedrine. This means that while they are made of the same elements, the 2 molecules differ in the arrangement at 2 molecular centers [10].
The 2 types of ephedrine are called (+)-ephedrine or L-ephedrine, and (-)-ephedrine or D-ephedrine, depending on if the molecule is rotated clockwise or counterclockwise around their centers, respectively [1].
Mechanism of Action
Ephedrine mainly functions by increasing the release and activity of adrenaline on its receptors. This action increases heart rate, narrows the blood vessels, opens the airways to the lungs, and stimulates the brain [11].
Ephedrine stimulates 3 main types of adrenaline receptors: alpha, beta-1, and beta-2. It specifically targets the beta-type adrenaline receptors and increases the production of the messenger molecule, cyclic AMP (cAMP). Ephedrine acts on alpha receptors by decreasing the production of cAMP. Decreasing cAMP decreases glycogen, sugar, and fat production [3, 4, 12].
It can also increase or decrease blood pressure based on the type of beta receptors it targets. By stimulating the beta-1 receptors in the heart, ephedrine can cause high blood pressure. On the other hand, ephedrine can lower blood pressure by activating beta-2 receptors, leading to fainting and flushing [4].
Ephedrine also acts as a mild brain stimulant. Because of its unique structure, it can easily dissolve through fats and act directly on the brain. This increases the activity of sections of the brain that control emotion (limbic system) [3].
It may also act by:
- Blocking adrenaline transporters, which increases the activity of adrenaline by allowing it to remain active longer in the brain. This increases heart rate and blood pressure [4, 13].
- Partially inhibiting monoamine oxidase (MAO), an enzyme that breaks down adrenaline. This causes adrenaline to stay active longer, resulting in irregular heartbeat and headaches [4].
- Increasing the release and blocking the uptake of dopamine, which enhances physical activity [14, 15].
- Increasing the release of acetylcholine at adrenaline nerves [16].
- Increasing serotonin release, which promotes weight loss by suppressing appetite [17].
Uses
Possibly Effective:
1) Low Blood Pressure
In a study of 204 pregnant female patients under spinal anesthesia, ephedrine was more effective in treating low blood pressure than phenylephrine [18].
However, in a review of 7 such studies (292 pregnant women), there was no difference in blood pressure increase between ephedrine and phenylephrine. In fact, phenylephrine was more likely to increase heart rate than ephedrine [19].
In a randomized study of 51 vein-surgery patients under long-term treatment for high blood pressure, ephedrine effectively increased blood pressure when it went below normal levels [20].
Ephedrine administered through the veins increased the rate at which the heart contracted in dogs, which can cause a rise in blood pressure [21].
In male rats, the (-)-ephedrine isomer contracted blood vessels more than a racemic mixture of ephedrine, which can result in higher blood pressure [1].
Ephedrine has a greater capacity to constrict veins than arteries, which increases blood pressure [22].
In one study of 32 adolescents, ephedrine did not significantly increase blood pressure and heart rate [23].
2) Asthma Symptoms
Ephedrine may relieve shortness of breath and airway spasms. In a study of 25 asthma patients, ⅔ of the group experienced relief from their symptoms [24].
In 12 patients with inflamed and spasming airways, gaseous ephedrine was 50% effective in reducing the symptoms. Oral ephedrine was not effective at all [25].
In a 2-week study of 8 asthma patients, ephedrine prevented lung function decline. However, after being treated with ephedrine 3 times per day in this 2-week period, a single dose of ephedrine had no additional effect in opening up the patients’ airways, which may indicate treatment tolerance [2].
In a trial of 20 asthma patients comparing the immediate effects of terbutaline (a bronchodilator) and ephedrine on the heart and bronchial tubes, ephedrine significantly widened the airways, but not as much as terbutaline [26].
While ephedrine is generally effective in treating asthma, there are some instances where it does not work. This may be because the dosage was too small to have any effect on the airway spasms [27].
3) Weight Loss
Many supplements are promoted to stimulate weight loss, but none of them has yet been supported by strong clinical evidence and approved by the health authorities. A healthy, calorie-controlled diet and increased physical activity remain the only proven strategies for weight control [28].
Particular caution is warranted when it comes to banned substances like ephedrine with a high potential of abuse and adverse health effects.
A randomized trial conducted on 43 obese patients (41 women) found that the patients lost an average of 12.6 kg after taking a combination of ephedrine and caffeine 3 times a day for 8 weeks, coupled with a low-calorie diet [29].
In another 16-week study of 57 patients, a combination of ephedrine and caffeine reduced body fat by 6%, and triglycerides by 15.2 mg/dL. When combined with a drug used to treat type 2 diabetes, ephedrine reduced triglyceride levels by 41 mg/mL [30].
In a 6-month study of 167 patients, herbal ephedra and caffeine decreased body weight and body fat two times more efficiently than placebo [31].
In a study of 67 subjects, an herbal mixture of Ma Huang (ephedrine plant) and Guarana (caffeine plant) promoted short-term weight and fat loss [32].
In a study with a 1-year follow-up period of 225 heavy smokers, weight gain was significantly reduced when ephedrine and caffeine were taken during the first 12 weeks of the study [33].
In naturally obese mice, ephedrine reduced weight and suppressed appetite [34].
4) Cholesterol Levels
According to a clinical review, ephedrine helps breaks down a type of LDL cholesterol that blocks arteries. When combined with caffeine, it increases HDL cholesterol. This protects against artery blockage and may prevent cholesterol-related heart disease [35].
In a 6-month trial of 167 subjects, herbal ephedra and caffeine significantly decreased LDL cholesterol and increased HDL cholesterol levels [31].
A combination of 20 mg ephedrine and 200 mg caffeine reduced triglycerides and prevented a drop in HDL cholesterol levels in 32 obese women on a strict dietary regiment [36].
In a 16-week trial of 57 patients, a combination of ephedrine, caffeine, and a diabetes drug increased HDL cholesterol by 7.8 mg/dL [30].
Ephedrine reduced cholesterol levels in the blood of obese mice in one study [34].
Insufficient Evidence:
No valid clinical evidence supports the use of ephedrine for any of the conditions in this section. Below is a summary of up-to-date animal studies, cell-based research, or low-quality clinical trials which should spark further investigation. However, you shouldn’t interpret them as supportive of any health benefit.
5) Brain Protection
Ephedrine acts on and activates beta adrenaline receptors, which are involved in increasing memory [37, 38].
In a 2-week trial, ephedrine had mild effect in improving attention [39].
In rats, Ephedra plant extract treated blood-brain barrier breakage and an abnormal buildup of fluid in the brain after spinal cord and brain injury. This may be a protective factor against early brain injury caused by bleeding [40].
6) Narcolepsy Symptoms
In a trial conducted on 46 narcolepsy patients, 20 were completely relieved of their symptoms, and all but 2 had some form of improvement [41].
Some doctors reported preliminary success with ephedrine for narcolepsy in children. A 13-year-old male and two 9-year-old females were all cured of daytime sleepiness with ephedrine [8].
In 5 narcolepsy cases, the mid-sleep seizures stopped within 24 hours of taking ephedrine [42].
However, we can’t draw any conclusions from one small trial and individual case reports.
7) Athletic Performance
Ephedrine has been used by athletes and bodybuilders for its supposed ergogenic properties that stem from the effects on mood, energy, fat metabolism, and heart rate [43].
A comprehensive clinical review found moderate benefits of ephedrine only on short-term performance. The authors also emphasized low-quality clinical evidence as a major limitation. In one study, ephedrine was effective only in combination with caffeine [44].
Another review concluded that ergogenic (performance-enhancing) properties are being overplayed and that the risks outweigh the potential benefits [45].
8) Myasthenia Gravis
Ephedrine has been used to treat Myasthenia gravis, a disease that causes rapid weakness and fatigue of the muscles.
Four patients in a series of placebo-controlled studies took ephedrine as an add-on to their main treatment. This resulted in a small but consistent reduction of their symptoms and weakness [46].
In a separate follow-up study, 10/12 patients experienced greater strength and mobility after 6-8 months of ephedrine treatment, but this study lacked a control group [47].
9) Bladder Control
In a study of 37 patients with a loss of bladder control (urinary incontinence), ephedrine improved control in those with mild wetting problems, regardless of the cause [48].
Ephedrine Side Effects and Precautions
This list does not cover all possible side effects. Contact your doctor or pharmacist if you notice any other side effects. In the US, you may report side effects to the FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch. In Canada, you may report side effects to Health Canada at 1-866-234-2345.
If you have been exposed to ephedrine and experience poisoning, urgently contact a poison control center near you (call 1-800-222-1222).
Ephedrine is known to have a variety of side effects, including:
- Nausea and vomiting [49]
- Anxiety [50]
- Mood change [50]
- Increased heart rate [50]
- Painful urination [3]
- Increased blood pressure [45]
- Insomnia [51]
- A headache [52]
- Irregular heartbeat [52]
- Dry mouth [31]
- Loss of vision [53]
The more serious possible side effects, usually from abuse of higher doses, include:
- Heart attacks [50, 54, 55, 56]
- Seizures [50]
- Stroke [54]
- Schizophrenia (only after prolonged exposure) [57]
- Mania and psychosis [58, 59]
- Coma [60]
- Death [50, 61, 62, 63]
There is a high risk of abuse of ephedrine.
While ephedrine has been given to young children in the US trials in the past, French medical societies strongly advise against giving ephedrine to children under the age of 15. The age limit for the safe use of ephedrine remains unclear [64].
Drug Interactions
Drug interactions can be dangerous and, in rare cases, even life-threatening. Always consult your doctor before supplementing and let them know about all drugs and supplements you are using or considering.
Combining ephedrine with other drugs can be beneficial, but also cause problematic side effects.
Taking ephedrine with aspirin is not advised. When combined with potassium permanganate (a chemical used to clean wounds) and aspirin, ephedrine caused nerve and movement disorders in teenagers [65].
Ephedrine should not be taken with drugs that prevent the reabsorption of adrenaline, such as antidepressants monoamine oxidase inhibitors (MAOIs). This combination can cause severely high blood pressure, irregular heartbeats, and headaches [66, 67, 52].
Taking ephedrine with painkillers like acetaminophen (Tylenol) is not advised, as this combination caused a heart attack in a healthy 46-year-old male [68].
When combined with theophylline, ephedrine caused insomnia, nervousness, and stomach issues during a trial conducted on 23 children with chronic asthma [69].
Ephedrine can cancel the effects of some drugs that lower blood pressure. In rats, ephedrine not only reversed the suppressive effects of guanethidine on the nervous system but also reduced its uptake by adrenaline receptors. This caused an increase in blood pressure [70].
Overdose
Ephedrine can be hazardous if taken in excess amounts and outside of medical supervision. Ephedrine poisoning and death have occurred in some cases of excessive consumption [63, 71, 62].
Make sure not to take ephedrine before talking with your doctor.
Ephedrine Sources and Drug Forms
Natural Sources
In 2004, the FDA prohibited the sale of all dietary supplements containing Ephedra alkaloids due to potential adverse effects on heart health. We strongly advise against using banned products and substances [5].
Ephedrine is derived naturally from the plant type Ephedra. Different species of this plant can be found in many regions around the world, but the first known extraction was an ephedrine alkaloid (an organic, nitrogen-containing compound) obtained from the Chinese herb, Ma Huang [72].
Ephedrine is also naturally found in Indian species of the ephedra plant [73].
There are many other species of this plant that ephedrine can be extracted from, such as ephedra sinica. Extracts from ephedra sinica are used in weight loss supplements [74].
Some other plants that ephedrine can be derived from are Ephedra major, Ephedra fragilis, Ephedra vulgaris, and Ephedra foliata [75, 73].
Forms and Dosage
There is no safe dosage for ephedrine, since it is an unapproved drug that poses a significant safety risk. Below is a summary of the dosages used in scientific research, outlined for informational purposes. We highly advise against the use of ephedrine.
Ephedrine can be taken by mouth, nose or by injection, and normally lasts in the body for up to 6 hours [76].
In clinical trials, this drug is commonly taken in 32-65 mg doses [77].
Children normally receive small amounts of ephedrine, about 0.1 to 0.2 mg per dose [78].
User Experiences
The opinions expressed in this section are solely from the users who may or may not have a medical background. SelfDecode does not endorse any specific product, service, or treatment. Do not consider user experiences as medical advice. Never delay or disregard seeking professional medical advice because of something you have read on SelfDecode.
Some users report that ephedrine increased their energy levels and suppressed appetite.
Other users experienced negative effects when combining caffeine and ephedrine. They felt more tired, could not think, and experienced compulsive urges such as nose-blowing or cleaning their nose with their nails, to the point where they drew blood. After stopping the drug combination, their compulsions ceased.
One user experienced prostate complications and bleeding from his genitals after prolonged consumption of a caffeine and ephedrine combination.
Many other users suggest drinking water when taking ephedrine, as it can cause bad breath and upset stomach.
A few users experienced increased acne, mild abnormal heartbeats, chest tingling, numbness, dizziness, and sweating (in the heat) after taking ephedrine.
