Methadone is a potent synthetic opioid receptor agonist that acts on the central nervous system (CNS) to alter how the brain and nervous system respond to pain. Methadone is a narcotic analgesic used to treat moderate to severe chronic pain in patients who aren’t clinically responding to other types of pain medication.
Methadone is also commonly used in opioid addiction treatment programs when combined with other medications, counseling and behavioral therapy. When correctly administered at appropriate doses, methadone lessens opioid withdrawal symptoms and cravings and distorts or blocks the effects of opioids.
Methadone is FDA-approved medication-assisted treatment for Opioid Use Disorder (OUD). It is also used to treat other forms of drug abuse including heroin addiction. Patients who have developed opioid tolerance may not respond to conventional analgesic regimens. So, methadone is used to improve their response to analgesic interventions. When used, methadone dosages are altered or combined with other opioids as adjuvant therapies.
Methadone is an antagonist of the N-methyl-d-aspartate (NMDA) receptor and a full agonist of the opioid receptor (MOR). It also has a comparatively longer duration of action and half-life than short-acting and extended-release morphine formulations. This longer duration of action makes methadone a good option for treating addiction since fewer doses are required to maintain analgesia and prevent opioid withdrawal symptoms.
Methadone blocks opioid effects by acting on opioid receptors in the brain, the same receptors that other opioids (e.g., codeine, heroin, hydrocodone, morphine, and oxycodone) stimulate. However, while methadone occupies and activates these opioid receptors, it does not cause a euphoric high at the dosages recommended for drug abuse treatment.
Its pharmacodynamic and pharmacokinetic characteristics reduce withdrawal symptoms and cravings. Thereby allowing patients to function normally and participate in other treatment or recovery support services.
Withdrawal symptoms are developed when opioid use is reduced or stopped. As a full opioid agonist, methadone fully activates and competitively blocks the opioid receptors in the body. These opiate-blocking qualities lessen the effects of other opioids while reducing cravings.
Therefore, in treatment programs, methadone is typically prescribed if a patient meets the following criteria:
Methadone dosing is dependent on the therapeutic need.
For pain management, the recommended dose is 2.5 mg orally every eight hours with slight dose increments if needed weekly. This applies to people who haven’t developed any form of opioid tolerance. In individuals with opioid tolerance, 10mg of methadone is given orally.
For opioid disorders, the recommended dose is 30 to 40 mg/day. It is titrated upwards by 10 to 20 mg/week to an optimal of 80 to 150 mg/day. Long-term treatment is optimal if it lasts for at least 14 months.
For opioid withdrawal, dosing is between 10 to 20 mg. This dose is increased by 10mg till withdrawal symptoms subside. After 2 to 3 days, this dose is reduced daily by 10% to 20% as withdrawal symptoms reduce.
Methadone hydrochloride is chemically identified as 3-Heptanone, 6-(dimethylamino)-4,4-diphenyl-, hydrochloride.
Methadone is a white, odorless, bitter-tasting powder with a crystal structure. It dissolves readily in water, isopropranolol, and chloroform but is almost completely insoluble in ether and glycerine. Methadone Hydrochloride Oral Concentrate contains a racemic mixture of two enantiomers, (S)-methadone and (R) methadone.
The properties of methadone hydrochloride include the following;
Pure methadone is a white powder that can dissolve into a solution. As a lipophilic hydrochloride salt, methadone is available in oral, intramuscular, intravenous, subcutaneous, epidural, and intrathecal formulations. Depending on the intended use, different dosages and formulations are necessary. Still, oral formulation tablets or concentrated syrup are the most popular.
Methadone is an opiate drug. Opioids are a highly addictive drug class that can cause physical dependence in as little as 4 to 8 weeks. As such, like other opioids, methadone can become extremely habit-forming. Methadone has different effects from other opioids; still, drug dependence can develop. This results in withdrawal symptoms if methadone use is abruptly stopped.
Like other opiates, methadone has a high potential for addiction because it stimulates the brain’s potent reward centers. For instance, methadone stimulates the release of endorphins, feel-good neurotransmitters in the brain. These neurotransmitters increase pleasure-related feelings while reducing pain perception. In addition, like morphine, methadone mimics the effects of endogenous peptides at central nervous system (CNS) opioid receptors, primarily on the mu-receptor.
As a result, methadone in high doses can equally induce euphoria, drowsiness, pulmonary edema, hypotonia, cardiogenic shock, and physical dependence.
When the euphoric feelings eventually fade, it triggers more concentrated use. Also, when used to relieve pain, methadone addiction can develop due to heightened tolerance. This leads to higher doses of methadone being taken to achieve a baseline effect.
Methadone has been available in the US legally since 1947. However, it is classified as a schedule II drug amongst other substances with a high potential for abuse, such as methamphetamine and cocaine. Common street names for methadone include fizzies, Amidone, wafer, street methadone and chocolate chip cookies (when combined with MDMA).
As of 2017, methadone was reported to be involved in over 3,000 overdose deaths in the United States. The Substance Abuse and Mental Health Services Administration (SAMHSA) estimates that 3.2 million Americans age 12 and older regularly misuse methadone and other prescription opioids. Also, The National Institute on Drug Abuse (NIDA) reports that between 21% and 29% of patients who receive opioids like methadone for chronic pain abuse them.
Clinicians should dispense methadone prescriptions with care. The FDA released a public health warning in 2016 highlighting the risks of methadone prescriptions. Although methadone helps prevent opioid use-related mortality and morbidity, improper use may lead to severe health implications. According to the CDC, in 2014, methadone accounted for about 23% of all prescription opioid deaths. This occurred with methadone accounting for about 1% of all opioid prescriptions.
The effects of methadone use vary from person to person. This effect variation is due to factors such as;
It can be challenging to detect methadone use, particularly if taken appropriately. Still, symptoms and side effects of methadone use can appear, especially during the initial phase of methadone treatment.
Clinicians may prescribe methadone to manage opioid addiction, and consistent use may lead to drug dependence. Withdrawal symptoms develop when an individual abruptly stops methadone use after dependence sets in. These withdrawal symptoms are highly intense and may also be observed during methadone abuse. Typically, the first signs of methadone withdrawal appear 24 to 36 hours after the last dose.
Methadone withdrawal symptoms include:
Methadone addiction is described as persistent methadone use and compulsive drug-seeking behavior in the presence of negative consequences.
Signs of methadone addiction include:
Irrespective of how methadone abuse began, either as a recreational activity or through dependency during an opioid addiction treatment program. Effective methadone addiction treatment requires a multifaceted approach. This approach combines medication management with psychotherapy and social support.
Treatment options for methadone addiction include:
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