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Opiate Agonist and Antagonist Drugs

What Are Opiate Agonists?

An opiate agonist is a drug that mimics the effects of naturally occurring endorphins in the body and produces an opiate effect by interacting with specific receptor sites. For example, full opiate agonists include heroin, oxycodone, methadone, hydrocodone, morphine, opium, and several other drugs. An agonist is a chemical that binds and activates the receptor to produce a specific biological response. In contrast, an antagonist blocks the action of the agonist and has an inverse agonist effect. Additionally, opiate antagonists include naloxone and naltrexone.

Opiate Agonist

Methadone is the most widely known opiate agonist used to treat opioid dependence. It can help patients ween off opiates of abuse because it decreases drug cravings. Patients must go to licensed methadone clinics to receive their doses. Because it is a narcotic, methadone has the potential to cause dependence.

Methadone is a synthetic opiate drug and pain reliever. Additionally, it acts on the same receptors as heroin, morphine, and other opiates. While the drug does not produce the same high heroin, it is also highly addictive and has an increased risk of overdose. German scientists first developed it in 1937 by searching for a surgical painkiller named “Dolophine.” Later, exported to the U.S. and renamed methadone, the drug became the treatment for heroin addiction. Unfortunately, it proved to be even more addictive than heroin.

Heroin was first manufactured in 1898 by Bayer Pharmaceuticals in Germany to treat tuberculosis and as a remedy for morphine addiction. Its appearance can be powdery white, rose gray, brown, or black. The different colors come from additives, including sugar, caffeine, or sometimes lethal substances. Besides, people can cut heroin with strychnine or other harmful substances. Various additives can lead to the infection or destruction of vital organs. The buyer never knows the strength or the additives to the heroin. Therefore, there is a constant and high risk of overdose with every use. It can be injected, smoked, or sniffed. Heroin is a highly addictive drug, and the withdrawal can be excruciating.

Oxycodone is a schedule II medication (a category of drugs that have a high potential for addiction but has a legitimate medical use) often used to treat moderate to severe pain. As helpful as it is to control pain, it carries a significant risk of addiction and dependence. Oxycodone in high doses, or when combined with other drugs or alcohol, can cause respiratory distress and even death. It is a semi-synthetic opioid synthesized from thebaine, an alkaloid found in the Persian poppy.

Oxycodone brand names are OxyContin, Roxicodone, Xtampza ER, and OxyIR. It is marketed either alone or with nonnarcotic analgesics such as aspirin (Percodan®) or acetaminophen (Percocet®).

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Partial Opiate Agonist

BuprenorphineSuboxone, and Subutex are partial opiate agonist drugs. These partial antagonist drugs bind to the opioid receptors but do not have a “full agonist” effect like heroin. These drugs are typical for the treatment of heroin addiction. Again, they can help prevent withdrawal and cravings. However, the downside of substituting treatment utilizing opiate agonists is that patients usually develop a dependence and tolerance to the medication.

Opioid Antagonists

The two most common opioid antagonists are naloxone and naltrexone. Naloxone is FDA-approved for use in opioid overdose and is sold in intravenous, intramuscular, and intranasal formulations.

Naltrexone, on the other hand, is available in both oral and monthly injectable formulations (Vivitrol) and is a blocker that significantly reduces the physical cravings for opioid drugs.

Naloxone binds to opioid receptors, which rapidly reverse and block the effects of other opioids. In case of an overdose, that drug can quickly restore breathing, making it a life-saving medication. The drug is available in the prefilled auto-injectable device as Evizio® or a nasal spray Narcan®.

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Medical Treatment for Opioid Use Disorder

Pharmaceutical treatments for opioid dependence can be helpful in the battle against addiction. However, many pose a risk of dependency and keep patients from being truly free of opiates. Ultimately, total abstinence is possible in days because of the Waismann Method’s rapid opiate detox. We offer opioid detoxification from OAT drugs, such as methadone and buprenorphine, in an accredited hospital under our quadruple board-certified medical director and other specialists’ guidance.

Waismann Treatment™ for Opioid Use Disorder Exclusive Features:

  • Quadruple board-certified physician and a leader in medical opioid detoxification and rapid detox. Our medical director, Michael H. Lowenstein, M.D., has himself successfully medically detoxed thousands of patients.
  • Patients receive a private room at a full-service accredited JCAHO hospital. In an accredited hospital, vast medical specialists and resources are immediately available for patients.
  • Admission on the day before anesthesia assisted rapid detox treatment for comprehensive medical evaluation and proper stabilization
  • Every rapid detox procedure is performed in a private ICU room. The medical team treats patients individually and privately.
  • Additional opioid detox protocol options are available with and without anesthesia based on patient needs and preferences.
  • Hospital discharge is based on the doctors’ evaluation and not on a pre-established time or facility limits.
  • Inclusive recovery retreat for a few days with multiple services to ensure comfort and well-being throughout the regulation and adaptation period
  • Nearly 100% opioid detox success rate

Our exceptional medical professionals’ outstanding team provides patients with superior physical and emotional support in a caring and supportive environment.
Call us today at 1-800-423-2482 to discuss how the Waismann Method® can free you from your opiate dependency and get you safely and comfortably where you want to be.

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