What is oxilofrine used for? Understanding its medical and illicit applications

October 6, 2025 •

4 min read

Developed as a cardiac stimulant in the 1930s, oxilofrine is a pharmaceutical stimulant prescribed in some countries for conditions like low blood pressure and as a cough suppressant. This raises the question: What is oxilofrine used for medically, in contrast to its illicit use in dietary supplements?

Quick Summary

Oxilofrine is a sympathomimetic drug with limited medical use for low blood pressure and cough in certain regions. As a banned substance, it is not approved for dietary supplements, where it has been illicitly found and marketed for weight loss and performance enhancement.

Key Points

Medical Uses: In some countries, oxilofrine is a prescription drug for treating orthostatic hypotension (low blood pressure) and as a cough suppressant.
Illicit Supplement Ingredient: Oxilofrine is not approved for use in dietary supplements and is unlawfully added to products marketed for weight loss and pre-workout energy.
Health Risks: Unregulated consumption can lead to serious adverse events, including increased heart rate, elevated blood pressure, cardiac dysrhythmia, and cardiac arrest.
Banned in Sports: As a performance-enhancing stimulant, oxilofrine is on the World Anti-Doping Agency (WADA) list of prohibited substances for athletes.
Deceptive Labeling: Illicit supplements often mislabel oxilofrine as 'methylsynephrine' to avoid detection and mislead consumers.
No US Approval: Oxilofrine has never been approved by the FDA for use as a prescription drug or dietary supplement in the United States.

Medical and Pharmacological Use of Oxilofrine

Oxilofrine, also known by alternative names such as methylsynephrine, is a sympathomimetic drug first developed in the 1930s. It is structurally related to ephedrine and acts as a norepinephrine releasing agent, which stimulates both alpha- and beta-adrenergic receptors in the body. By mimicking the body's 'fight or flight' response, oxilofrine causes vasoconstriction and increases heart rate and contractility. These physiological effects are the basis for its approved medical applications in certain countries.

Approved Clinical Applications

For decades, oxilofrine has been used primarily as an antihypotensive agent to treat low blood pressure, particularly orthostatic hypotension. This condition causes a sudden drop in blood pressure upon standing, leading to dizziness or fainting. By stimulating the heart and increasing blood pressure, oxilofrine helps alleviate these symptoms.

In combination with other medications, such as normethadone, oxilofrine has also been marketed as a cough suppressant. As an alpha-1 adrenergic receptor agonist, it can cause vasoconstriction, which helps reduce mucus secretion in the airways and lessen the urge to cough. These legitimate medical applications, however, are limited to specific regions and are not universally recognized. For instance, oxilofrine has never been approved as a prescription drug or dietary supplement in the United States.

The Illicit and Dangerous Side of Oxilofrine

Despite its narrow medical use, oxilofrine has gained notoriety for its illicit inclusion in dietary and sports supplements. Manufacturers, particularly in the US, have unlawfully included this unapproved pharmaceutical in products marketed for weight loss, fat burning, and as pre-workout stimulants.

To circumvent regulatory scrutiny, supplement companies have frequently disguised oxilofrine on product labels under other names, most commonly "methylsynephrine". This deceptive practice often misleads consumers and regulators alike, with consumers potentially confusing the name with synephrine, a legal ingredient derived from bitter orange.

Serious Health Risks

The consequences of consuming oxilofrine from unregulated supplements can be severe. Studies have revealed that some of these products contain pharmaceutical or even higher dosages of the drug, far exceeding recommended medical levels. This unregulated exposure carries significant cardiac risks, including:

Increased Heart Rate: Tachycardia and cardiac dysrhythmia are major concerns.
Elevated Blood Pressure: Dangerous increases in blood pressure, potentially leading to hemorrhagic stroke, especially in individuals with normal blood pressure.
Cardiac Arrest: In extreme cases, consumption has been linked to cardiac arrest.
Agitation and Vomiting: Adverse events reported have also included agitation and vomiting.

The Anti-Doping Prohibitions

As a potent stimulant, oxilofrine is on the World Anti-Doping Agency (WADA) list of prohibited substances. Its stimulant properties, which increase alertness, focus, and endurance, are considered performance-enhancing. The strict liability rule in competitive sports holds athletes responsible for any substances found in their bodies, regardless of intent.

This has led to numerous high-profile doping cases involving athletes who unknowingly consumed oxilofrine through contaminated supplements. These cases underscore the danger of relying on unregulated dietary supplements and the importance of checking for banned substances. Prominent examples include Olympic sprinters and other professional athletes who faced suspensions after testing positive for the drug.

Comparison of Oxilofrine Use


Aspect	Legitimate Medical Use	Illicit Supplement Use
Purpose	Treating orthostatic hypotension or cough.	Weight loss, fat burning, and performance enhancement.
Regulation	Prescription drug, regulated by health authorities in some countries.	Unregulated and illegal in many regions, including the US.
Dosage	Clinically determined pharmaceutical dosages.	Unregulated and often excessively high, with potential for accidental overdose.
Labeling	Clearly labeled as a prescription drug.	Deceptively labeled as 'methylsynephrine' or other names.
Oversight	Subject to pharmaceutical safety regulations.	Lacks oversight, leading to contamination risks and health hazards.
Risks	Monitored by a healthcare provider.	Significant cardiac risks, including cardiac arrest, from high, unregulated doses.

Understanding the Mechanism

Oxilofrine's stimulant effects are achieved by its action as a sympathomimetic agent, which means it mimics the effects of the sympathetic nervous system. It does this by increasing the release of norepinephrine, a neurotransmitter that plays a key role in the 'fight or flight' response. The activation of adrenergic receptors by norepinephrine causes a cascade of effects, including increased heart rate and vasoconstriction. This is what provides the performance-enhancing effects sought by some athletes but also poses significant health risks when abused.

Conclusion

In conclusion, what is oxilofrine used for has evolved from a controlled medical application to a dangerous, illicit use. As a pharmaceutical stimulant, its original and limited purpose was to address low blood pressure and specific types of cough in a regulated medical context. However, its potent stimulant properties have led to its unauthorized inclusion in dietary supplements, marketed for weight loss and athletic performance. This unregulated use is associated with serious cardiac risks and has earned oxilofrine a place on the World Anti-Doping Agency's prohibited list. The contrast between its cautious medical application and its dangerous, deceptive use in supplements serves as a critical warning to consumers. For more information on the dangers of unregulated supplements, consumers can visit the FDA website.

Frequently Asked Questions

No, oxilofrine is not approved as a prescription drug or dietary supplement in the United States. Its inclusion in dietary supplements is unlawful, and the FDA has issued warnings to manufacturers.

Oxilofrine is a potent stimulant that can enhance performance by increasing heart rate, focus, and endurance. For this reason, the World Anti-Doping Agency (WADA) classifies it as a prohibited substance for competitive athletes.

Side effects can be severe, especially from the high doses found in illicit supplements. They include increased heart rate (tachycardia), palpitations, elevated blood pressure, agitation, vomiting, and in serious cases, cardiac arrest.

To evade regulation, manufacturers frequently list oxilofrine under alternative names, most commonly 'methylsynephrine', on product labels. This can confuse consumers who might mistake it for synephrine, a legal ingredient.

Yes, oxilofrine is a substituted amphetamine and a sympathomimetic agent, which means it acts similarly to amphetamines by affecting the sympathetic nervous system.

Yes, standard anti-doping tests can detect oxilofrine. Athletes who have consumed it unknowingly through contaminated supplements have tested positive and faced suspension.

If a supplement lists 'methylsynephrine' or you suspect it contains oxilofrine, stop using the product immediately. It is crucial to consult a healthcare provider and report the product to the appropriate regulatory body, such as the FDA.