What Is Medetomidine?
Medetomidine hydrochloride (often referred to as simply medetomidine) is a veterinary drug, meaning it is prescribed to animals (typically dogs) and is not intended for human use. However, it is rapidly emerging as a drug adulterant in the illicit drug supply. This means it is being added to street drugs. The unpredictable effects of this and other substances that people are unknowingly ingesting are a cause for concern. Read on to learn more about the background of this substance, its introduction into the illicit drug supply, and its dangers.
Legal Distribution of Medetomidine
Medetomidine is a relatively new drug with a limited history. It was developed by Orion Pharmaceuticals in 2007. Today, it is approved for use in dogs in the United States and in Canada. There are different distributors in each of these countries, although the same brand name is used in both areas.
Novartis Animal Health Canada
Novartis Animal Health Canada sells medetomidine under the brand name Domitor in Canada for use in dogs. There is no information on their website about this product, which may be because it is for use in dogs. Doses must be purchased by approved veterinarians and reported to authorities who monitor its administration in dogs. Low doses are typical.
Pfizer Animal Health
In the United States, medetomidine is sold for use in dogs under the same brand name, Domitor. Pfizer also markets Dexdomitor, a very similar chemical that reportedly has a lower metabolic load and less potential for negative interactions with other drugs. The chemical name for Dexdomitor is dexmedtomidine. This chemical is approved for human use, unlike medetomidine. The human form is sold under the name Precedex as a non-opioid analgesic and sedative.
The Intended Uses of Medetomidine In Veterinary Medicine
In veterinary medicine, medetomidine hydrochloride is mainly used for its potent sedative effects. It is also used as a pain reliever for dogs. It is also used in carefully controlled clinical settings on humans, but this use is very rare. There have not been enough clinical studies for its widespread use in humans to be approved. Here are some common reasons for the administration of doses of medetomidine hydrochloride, specifically in dogs.
Sedation
Medetomidine helps achieve sedation in otherwise healthy animals during medical exams or minor procedures, making them easier to handle and reducing stress. This is important during the administration of surgeries or diagnostic procedures that require dogs to be still.
Reversible Sedation
An advantage of medetomidine is that its sedative effects can be reversed in a short time. After a procedure, the sedative effects can be reversed with the administration of a drug called atipamezole, allowing dogs to recover quickly.
Anesthesia Support
Medetomidine is often used in combination with other anesthetics for surgeries or more invasive procedures on dogs, either to deepen the level of anesthesia or as a pre-anesthetic to relax dogs before full anesthesia. It is not typically a primary general anesthesia. Rather, it is used in combination with general anesthesia administration, like halothane anesthesia, to keep dogs under sedation for the desired duration.
Pain Relief (Analgesia)
Medetomidine is also used for its analgesic properties. Administration of medetomidine provides pain relief during or after surgical or diagnostic procedures. This analgesic effect is another reason it is used as an adulterant for opiates.
Muscle Relaxation
Medetomidine administration relaxes the animal’s muscles, which is useful during surgeries or procedures that require stillness. Healthy animals like dogs recover quickly from the effects of muscle relaxation after atipamezole is administered.
Medetomidine In The Illicit Drug Supply
Beginning in 2022, medetomidine has been observed in samples of drugs purchased on the street in the United States. Drug researchers and prevention groups often collect samples and analyze their contents to detect new substances and be aware of trends.
Medetomidine has been detected to some degree in California, Colorado, Illinois, Pennsylvania, Missouri, and Maryland. These are all states with high rates of opiate abuse and overdose.
Drug Adulterants Explained
Medetomidine is an example of a drug adulterant. It is not sold to users under its brand name, nor are they typically informed that it is in the drug. Almost all drugs that reach users in the United States are adulterated to one degree or another.
A drug adulterant is any substance added to a drug, intentionally or unintentionally, that changes its makeup. These substances are often used to increase the amount of the drug or alter its effects. They typically reduce the purity of the substance in question and can make the end product more hazardous.
In illegal drugs, adulterants are commonly mixed in to cut costs, increase volume, or mimic the drug’s desired effects. However, they pose serious health risks, as users often don’t know what has been added or how potent it is. Medetomidine is just one kind of adulterant.
Types of Adulterants
Drug adulterants are added to other substances by producers of illicit drugs for multiple reasons. Sometimes, they are added to increase the volume of the substance in question. For example, relatively harmless substances like baby laxatives may be added to cocaine. This increases the weight of the product, enabling the dealer or distributor to sell it for more money. While it makes the drug less potent, this type of adulterant has few adverse effects. In fact, the combination will be less strong than the normal, pure form of the drug.
Other substances used as adulterants may be intended to make the drug more potent or to mimic the effects of the substance it is being marketed and sold as. The adulterant may “potentiate” the primary drug, meaning that the resulting effect is stronger than the sum of the two substances if they are administered on separate occasions. The combination may prolong the duration of the primary drug’s effect, leading to a longer half-life.
Fentanyl’s Origins As An Adulterant
A significant portion of the increase in drug overdoses in recent years is due to fentanyl and its analogs. Fentanyl is a synthetic opioid that is 50 to 100 times more potent than morphine, making even small amounts deadly.
In the U.S., fentanyl has been the primary driver of the rise in opioid overdose deaths. The CDC reported that in 2022, over 70% of opioid-related overdose deaths involved synthetic opioids like fentanyl. Between 2013 and 2020, fentanyl-related overdose deaths increased by more than 540%.
Fentanyl was initially introduced to the illicit drug supply as an adulterant. This is because it is cheaper to produce than poppy-based opiates like heroin and easier to obtain than prescription painkillers. Its potency, combined with the fact that it is often mixed into other drugs (like heroin, cocaine, or counterfeit pills) without users’ knowledge, makes it particularly dangerous.
Now, many users seek out fentanyl. Many addicts know that the counterfeit pills they are buying (often known as blues) are not the prescription drug that they resemble, and some buy fentanyl in powder form for IV use.
However, even users who know what they are consuming are still at high risk. Even a low dose of fentanyl can cause respiratory depression and a lowered heart rate. These effects are compounded when fentanyl (or fentanyl-adulterated heroin) is further adulterated with sedatives like medetomidine. These sedative adulterants have been reported as the cause of a spike in overdose deaths.
Sedative Adulterants
Medetomidine is one of a group of sedatives that have become popular as drug adulterants in the illicit drug supply. Others include xylazine, which is added to fentanyl or fentanyl analogues to create so-called “tranq” dope. Xylazine is another veterinary drug that has attracted attention for the sedation it causes and the higher risk of overdose it poses, even at low doses.
Ketamine, which is both a prescription drug and a popular recreational drug under its own name, may also be added to opiates in the illicit drug supply. Ketamine has unique sedative effects that differentiate it from other sedatives. Its use as an adulterant puts drug users who are unaware that they are consuming ketamine at risk, as the combination of drugs can lead to confusion and a decrease in awareness that is atypical of opiates.
Why Medetomidine?
The analgesic properties of medetomidine are one reason it is used as an adulterant in opiates, which are used in part for their analgesic effect. It reduces sensitivity to pain through its effects on the central nervous system, mimicking the pain relief effects of heroin, fentanyl, or prescription opioids. This makes the overall drug more potent, which may attract more users who have a high tolerance to opioids.
The sedation that medetomidine causes is another reason for its use as an adulterant for other drugs. As a powerful sedative, it may be added to enhance the calming, sedating, or “downer” effects of opioids or other depressant drugs.
Aside from opiates, medetomidine may also be used to mimic the effects of prescription sedatives like benzodiazepines, especially in counterfeit pills. Users seek out these drugs because they decrease anxiety and lower the heart rate, so medetomidine can substitute for more expensive chemicals.
Xylazine Restrictions
Restrictions on xylazine are another reason that medetomidine is showing up more in combination with other street drugs. Xylazine-laced drugs attracted headlines for their potent sedative effects, visible in the high number of people experiencing adverse effects and “nodding out” in cities like Philadelphia. This led to the FDA restricting unlawful imports of xylazine and the chemicals used to produce it in February of 2023. As is common with illicit drugs, the decrease in availability of xylazine created the demand for an alternative, and medetomidine emerged to fill the gap.
Of course, the underlying reason that medetomidine is being introduced into the illicit drug supply is cost. By substituting this relatively cheap substance for more expensive opioids or benzodiazepines, or for xylazine, drug producers and suppliers can decrease their overhead costs while still supplying a potent dose. They are not concerned about the overdose deaths that this combination of substances is causing.
Where Is Medetomidine Coming From?
While the Drug Enforcement Administration has yet to issue a clear statement on where the medetomidine in the illicit drug supply is coming from, there are a few possible explanations.
Theft From Veterinary Practices
Medetomidine could be stolen from veterinary practices or animal hospitals where it is supposed to be kept under secure conditions. Although these businesses are regulated, there is less oversight than in hospitals and clinics for humans. One possible solution is increased regulation of these practices to prevent illicit drugs from leaving the premises.
Illicit Online Purchases
Some individuals may try to purchase medetomidine through unauthorized or illegal online sources, often from suppliers that do not adhere to legal regulations. These sources can be particularly dangerous, as there is no legal oversight to ensure that the dose (or doses) are in the amount they are labeled as.
The Food and Drug Administration has noted the acute threat of substances bought on the so-called dark web, a parallel Internet that is only accessible through special encrypted browsers. It is possible that this is one source of the medetomidine that is entering the illicit drug supply.
Diversion from Legal Sources
Medetomidine might be diverted from legitimate sources, such as veterinary suppliers or pharmacies, through fraudulent activities or by insiders. High doses that are intended for the treatment of dogs might be smuggled out by workers in the veterinary service or pharmacy who are looking to make money by selling them. In theory, their absence will be noted by the people in charge, but sometimes theft is detected too late to prevent the substance from entering the illicit drug supply.
In addition to being used for its sedative effects in dogs, medetomidine is sold in its free base form as an ingredient in paint for marine vehicles. Medetomidine is used in marine paint as an anti-fouling agent, which helps prevent the growth of marine organisms, such as barnacles, algae, and mussels, on the hulls of ships and other submerged surfaces.
Medetomidine interferes with the settlement behavior of marine organisms by disrupting the central nervous system signals that help them attach to surfaces. This keeps the hulls of ships cleaner and reduces drag in the water. It is possible that people with access to this paint ingredient could be diverting or stealing it.
Medetomidine’s Effects On The Body
Medetomidine is an Alpha-2 adrenergic agonist. To understand how medetomidine works in the bodies of dogs (and the bodies of humans) it’s important to understand what each of these words means.
“Alpha-2 Receptors” Explained
Alpha-2 receptors are special proteins found mostly in the brain and nervous system. They help control the body’s stress response, blood pressure, and pain levels.
Alpha-2 receptors can be thought of as a brake pedal for stress. When they are pressed, they reduce stress, calming the body and reducing the perceived level of pain (what is known as analgesia). They lead to lower blood pressure, known as hypotension.
Other substances target other receptors. This is why some drugs (like medetomidine and the drugs it is usually added to) make people feel calm, while others have the opposite effect, making people feel more alert or energetic. Still, others target other receptors and have more complicated effects entirely.
“Adrenergic” Explained
The word “adrenergic” refers to anything involving the chemicals adrenaline and noradrenaline, which are involved in the body’s stress response. In this context, it means that medetomidine and other Alpha-2 adrenergic agonists affect the levels of adrenaline and noradrenaline.
Adrenaline and noradrenaline are chemicals that help prepare the body for stress or danger, like making the heart beat faster or opening up the airways. Medetomidine causes inhibition of the release of adrenaline and noradrenaline, lowering stress, decreasing heart rate, and causing low blood pressure. This also leads to respiratory depression, slowed breathing, and lowered body temperature.
“Agonists” Explained
Agonists are substances (like drugs) that activate certain receptors in the body to produce a specific effect. Think of receptors as “locks” and agonists as “keys” that fit into those locks and turn them on.
When an agonist binds to a receptor, it triggers a response in the body. For example, if an agonist activates a receptor that controls pain, it can reduce the feeling of pain. If it activates a receptor that controls sleep, it might make someone feel sleepy.
In the case of medetomidine, the receptors control things like stress, pain, and alertness. When an alpha-2 adrenergic agonist drug is given, it presses these buttons, telling the body to slow down its activity. As a result, the person or animal becomes more relaxed, feels less pain, and may get sleepy or calm.
Agonists vs. Antagonists
In contrast to agonists, antagonists are substances that block or stop the action of receptors in the body. If receptors are like “locks,” antagonists act like “keys” that fit into the locks– but don’t turn them on. Instead, they prevent other substances (like agonists) from activating the receptors.
In simple terms, antagonists stop certain effects in the body. For example, if a drug normally causes pain relief by activating a receptor, an antagonist could block that receptor and prevent the pain relief from happening.
Atipamezole is the drug that is used to reverse the effects of medetomidine following veterinary surgery. It is an alpha-2 adrenergic antagonist, which means it blocks the alpha-2 receptors that medetomidine activates in patients.
Understanding antagonists can help explain why patients suffering from overdoses of medetomidine are more difficult to treat than those overdosing on opioids alone. Narcan is an opioid antagonist, meaning it blocks the effects of opioids like fentanyl. It has no effect on the receptors that are targeted by medetomidine. This puts users of medetomidine at increased risk of death by overdose because in an emergency situation, Narcan is often the only option to inhibit the effects of the drugs causing the overdose.
Medetomidine In The Central Nervous System
As noted above, medetomidine acts on alpha-2 adrenergic receptors. When these receptors are activated, they also reduce the release of norepinephrine, a neurotransmitter that plays a key role in the central nervous system.
Norepinephrine is partially responsible for maintaining alertness and the body’s “fight or flight” response. The reductions in adrenaline, noradrenaline, and norepinephrine caused by medetomidine lead to analgesia, muscle relaxation, sedation, drowsiness, and reduced anxiety. It quiets the arousal centers in the brain. This is the effect sought by producers and users.
Medetomidine’s central nervous system effects can also result in significant depression of bodily functions regulated by the brain. As it slows down nerve signaling, it can lead to bradycardia (slowed heart rate), hypotension (low blood pressure), lowered body temperature, and depressed respiratory function (slowed breathing).
These effects are particularly dangerous if the drug is used outside of controlled medical settings or combined with doses of other central nervous system depressants like opioids or alcohol. This combination can lead to acute and life-threatening conditions like severe hypotension, respiratory failure or coma, and eventually to death.
Medetomidine’s Impact On The Liver
Medetomidine can have an impact on the liver, primarily through its effect on liver function and metabolism. The drug is metabolized in the liver, and in people with compromised liver function, its sedative effects can be prolonged or intensified due to slower clearance from the body. This means that individuals with pre-existing liver conditions may be more susceptible to the drug’s sedative and depressant effects, as their liver may not process and eliminate the drug as efficiently.
Additionally, medetomidine may reduce body temperature and blood flow to the liver, which can impair its functioning over time, especially with prolonged or repeated use. In veterinary patients, this is closely observed, as reduced blood flow to the liver can affect the ability of dogs to metabolize not only medetomidine but also other medications administered concurrently.
This monitoring is obviously not possible for street users, who don’t stick to the small doses used in clinical settings. Addicts who already have liver disease or who are taking multiple medications that rely on liver metabolism are at increased risk if they use drugs laced with this substance.
Other Impacts On The Body
As noted above, medetomidine can lower the body temperature and blood pressure. The sedation it produces also affects mucous membranes. Mucous membranes require the production of secretions to stay lubricated, and the parasympathetic nervous system does not produce these secretions on high doses of sedatives. This leads to dryness in the eyes and respiratory passages.
Metedomidine can also lead to an increased risk of cardiovascular disease. The slowed heart rate (bradycardia) caused by its sedative effects can strain the heart. This is particularly true if the substance is combined with other drugs that further depress cardiovascular function, leading to long-term heart issues.
The low blood pressure (hypotension) that medetomidine causes by relaxing blood vessels also contributes to cardiovascular disease. If blood pressure drops too low for extended periods, it can reduce blood flow to vital organs, including the heart, weakening cardiovascular function over time. When users are withdrawing from the sedation, their blood pressure is likely to “rebound” and spike to unhealthy levels, further increasing strain on the cardiovascular system.
Medetomidine can also lead to serious skin issues at the injection site. Improper injection can lead to bacterial infection. Observers of street drug use have reported that many users of so-called “tranq” develop skin lesions and abscesses. The potent analgesic properties of medetomidine can lead users to underestimate the severity or degree of pain they are experiencing, making them slow to seek treatment for these issues. Each dose of the substance leads to further analgesia and less awareness of pain at the injection site.
Medetomidine also has potential negative effects during pregnancy. Reduced uteroplacental blood flow due to hypotension and bradycardia (slow heart rate) could potentially lead to fetal hypoxia, where the fetus does not receive enough oxygen, increasing the risk of fetal distress, developmental issues, or miscarriage.
Since medetomidine crosses the placental barrier, it could have a direct effect on the developing fetus. The drug’s sedative and depressant effects on the central nervous system could interfere with fetal brain development or cause sedation in the fetus, potentially leading to complications in birth or development.
If medetomidine is used close to the time of delivery, it may depress respiratory function in the newborn, which can lead to difficulty breathing and require immediate medical treatment. This is particularly concerning if other depressant drugs, such as opioids, are also involved.
Philadelphia: A Case Study
Now that we understand the strong sedation and analgesia that medetomidine produces in the body, we can see why it is so dangerous when combined with opioids. There have been reported “mass overdose events” in multiple cities.
In Philadelphia alone, 160 people were reported to suffer from overdose in one three-day period. Doctors administering treatment for these overdoses first noticed the remarkable decrease in heart rate caused by medetomidine, finding that many of them had heart rates below 20 beats per minute. They were not responding to a dose of naloxone (Narcan), the opioid reversal medication. This puts users at a greatly increased risk of death. Medetomidine was first detected in April by doctors rushing to discover the cause of this problem. Its limited history as an adulterant made this a difficult task.
Philadelphia has been grappling with a severe opioid crisis, marked by a significant increase in overdose deaths and a profound impact on public health and safety. The city has witnessed a dramatic rise in the misuse of prescription opioids, heroin, and synthetic opioids like fentanyl, leading to a crisis that has overwhelmed local healthcare systems and emergency services.
The proliferation of fentanyl, in particular, has exacerbated the problem, as it is often mixed with other drugs like xylazine and medetomidine, making overdoses more frequent and more fatal. The epidemic has also contributed to a surge in related issues, including homelessness, crime, and strained social services. In response, Philadelphia has implemented various harm reduction strategies, such as supervised injection sites and increased access to naloxone.
Overdose Prevention
Public health agencies are employing a multi-faceted approach to prevent overdoses on opiates and sedatives like medetomidine, focusing on harm reduction, education, and policy changes.
One key strategy is the widespread distribution of naloxone (a.k.a Narcan), the previously mentioned opioid overdose reversal medication, available as a nasal spray or injection. Agencies are making naloxone more accessible to first responders, healthcare providers, and the public, ensuring that it is available in emergency situations to counteract the effects of an opioid overdose.
Education and awareness campaigns are another crucial component. Public health initiatives aim to inform the community about the risks of opioid use, the signs of overdose, and the importance of seeking help. These campaigns often target both the general public and specific populations to promote safe medication practices and encourage the use of treatment services. Spreading the word about the additional dangers posed by medetomidine is one step that may reduce its impact.
Additionally, policies are being implemented to regulate the prescribing of opioids, which often lead people to use street drugs. Guidelines for healthcare providers emphasize prescribing the lowest effective dose for the shortest duration and exploring non-opioid pain management alternatives. Public health agencies are also enhancing drug monitoring programs to track prescriptions and identify patterns of misuse or overprescription.
By combining these strategies, public health agencies are working to reduce the incidence of opioid and sedative overdoses, mitigate their impact, and ultimately save lives.
Treatment for Dependence on Medetomidine and Opioids
Users who consistently dose opioids that are mixed with medetomidine may develop a dependence on the sedation provided by the adulterant. This means that they are now addicted to both substances, and a “normal” shot of fentanyl will be unsatisfying for them. This makes their problem even worse, as they are now at increased risk of overdose and death every time they use it.
Whether a person has a long history of use or is new to abusing opioids, they are likely to need treatment for their addiction. Opioids (particularly fentanyl, which is the most common other substance that medetomidine is combined with) are among the most immediately addictive substances and have some of the worst impacts on users’ health. Users often require a medical detox to separate them from their drug (or drugs), and a long-term regimen to keep them clean.
Turning Point of Tampa
Turning Point of Tampa offers a comprehensive program for treating the mental, physical, and spiritual symptoms of addiction. Their licensed professionals are experts in the prevention of relapse on sedatives like medetomidine.
Turning Point focuses on the 12 Steps, a program of action to create total abstinence from drugs and alcohol. The 12 Steps are highly effective in treating opiate and sedative addiction. They provide a structured framework that addresses both the psychological and social aspects of addiction, which is often accompanied by depression and low self-esteem. The 12-step approach, originally developed by Alcoholics Anonymous (AA), has been adapted to address a wide range of substance use disorders, including opiate addiction. This method emphasizes personal accountability, support from peers, and a spiritual component, which together create a comprehensive experience.
The core of the 12-step program involves a series of recommendations designed to help individuals recognize their addiction, take responsibility for their actions, and make amends for past behaviors. The first step involves admitting powerlessness over the addiction and recognizing that life has become unmanageable, which is a crucial realization for individuals beginning their recovery journey.
Subsequent steps guide individuals through making amends, seeking forgiveness, and maintaining a spiritual connection, all of which contribute to building a solid foundation for long-term sobriety. This structured progression helps individuals break free from the cycle of addiction by fostering self-awareness, personal growth, and a commitment to change.
Turning Point of Tampa emphasizes the importance of peer support and community. Patients attend regular meetings where they share experiences, receive support, and build connections with others who understand the struggles of addiction. This sense of community helps reduce feelings of isolation and provides a network of support that is critical for maintaining motivation and accountability, especially when leaving treatment.
In addition to the 12-step framework, Turning Point of Tampa integrates other therapeutic modalities to address the multifaceted nature of opiate addiction. This includes cognitive-behavioral therapy (CBT) to help individuals change harmful thought patterns and behaviors, as well as medication-assisted treatment (MAT) to manage withdrawal symptoms and cravings. The combination of 12-step principles with these additional therapies provides a holistic approach to recovery, addressing both the mental and physical aspects of addiction. By offering a structured, supportive environment and a range of therapeutic options, Turning Point of Tampa can effectively guide you (or a loved one) through the complex process of overcoming opiate addiction and achieving lasting recovery. Reach out today.
Sources for More Info:
https://homelabvet.com/product/domior-for-dogs-and-cats-10ml-0-33-oz
https://drugfree.org/drugs/medetomidine/
https://www.npr.org/2024/05/31/nx-s1-4974959/medetomidine-overdose-fentanyl-sedative
