What is the difference between heroin and methadone (Dolophine)?

From the Guidelines

Heroin and methadone (Dolophine) are two distinct opioids with different properties and uses.

Key Differences

• Origin and Composition: Heroin, also known as diacetylmorphine, is a synthetic opioid derived from morphine, a natural opioid extracted from the opium poppy 1. Methadone, on the other hand, is a synthetic opioid with a long half-life, used to treat opioid addiction and manage pain 2, 3.
• Pharmacological Effects: Both heroin and methadone activate opioid receptors in the central nervous system (CNS), producing analgesia, sedation, euphoria, and other effects 1. However, methadone has a longer duration of action and is used to ameliorate the cycle of intense euphoria followed by intense withdrawal associated with opioid use 2.
• Addiction Treatment: Methadone is used as a medication-assisted treatment for opioid addiction, whereas heroin is a highly addictive substance that can lead to opioid use disorder 2, 4.
• Prescription and Regulation: Methadone is a Schedule II controlled substance, strictly regulated for outpatient prescription and use in opioid treatment programs 3. Heroin, being a highly addictive and illegal substance, is not prescribed for medical use in most countries.
• Dosage and Administration: Methadone has a complex pharmacokinetic profile, with pronounced interindividual differences in its plasma half-life, relative analgesic potency, and duration of action 5. Heroin, due to its illegal status, does not have established medical dosing guidelines.

Clinical Considerations

When considering the use of methadone for opioid addiction treatment or pain management, it is essential to weigh the benefits against the risks, including the potential for physical dependence, addiction, and overdose 4, 3. Heroin, being a highly addictive and illegal substance, poses significant risks to individuals and public health, and its use is strongly discouraged 4.

From the FDA Drug Label

Methadone hydrochloride is a µ agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine, the most prominent of which involve the central nervous system and organs composed of smooth muscle. The main difference between heroin and methadone (Dolophine) is that methadone is a synthetic opioid analgesic, whereas heroin is a naturally occurring opioid. Methadone has a longer duration of action and is used for detoxification and maintenance of opiate dependence, whereas heroin is a short-acting opioid with a high potential for abuse and addiction 6.

• Key differences: + Synthetic vs natural origin + Duration of action + Medical use for detoxification and maintenance Note that heroin is not mentioned in the provided drug labels, and the information provided is based on the properties and uses of methadone [7] [8].

From the Research

Differences between Heroin and Methadone

• Heroin is a short-acting opioid, while methadone is a long-acting opioid agonist used in the treatment of heroin addiction 9, 10.
• Methadone maintenance treatment has been shown to be effective in reducing heroin use and retaining patients in treatment, but it may not be suitable for all patients due to differences in pharmacokinetics and side effects 9, 11.
• Methadone treatment can contribute to the control of addictive behavior, reduce craving, and restore the balance of disrupted endocrine function, but it may also have risks such as an increased risk of death during induction into treatment and risks of diversion of drugs to the black market 10, 12.
• Heroin addiction is strongly associated with deviant behavior and crime, and the objectives of treating heroin addiction include humane support, rehabilitation, public health intervention, and crime control 9.
• Methadone treatment has been found to induce differential desensitization of mu-opioid receptors across brain regions compared to heroin, which could provide insights to improve the pharmacotherapy of heroin addiction 13.

Pharmacological Effects

• Methadone has a higher relative intrinsic efficacy than the active metabolites of heroin at mu-opioid receptors, and the extent of mu-opioid receptor desensitization is dependent upon agonist efficacy 13.
• Methadone treatment can decrease the activation of G-proteins by the high efficacy agonist DAMGO and the partial agonist endomorphin in various brain regions, which could contribute to its therapeutic effects 13.
• Buprenorphine, a partial agonist, is a less reinforcing medication with different side effects and less risk of overdose, and it can be used in a different paradigm of treatment, office-based opioid treatment, with less structure and offering greater patient autonomy 9.

Treatment Outcomes

• Methadone maintenance treatment has been found to be more effective than non-pharmacological approaches in retaining patients in treatment and suppressing heroin use, but it may not have a statistically significant superior effect on criminal activity 11.
• The quality of treatment can reduce risks and increase benefits, and the availability of new pharmacotherapies may provide useful options for patients who experience adverse effects of methadone 12.