WHAT IS NALTREXONE?
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Naltrexone is an opioid antagonist that completely blocks the effects of opioids on the brain
What does “antagonist” mean?
This means that it acts as a blocker, a protector, and a ‘guard,’ with a strong affinity for opioid receptors. As an antagonist, it closely resembles opioids molecules and binds to the receptors. Thanks to that it prevents other substances from attaching.
What does “pure opioid antagonist” mean?
It means that it doesn’t have any agonist characteristics nor stimulates opioid receptors in any way and doesn’t make any “buzz” effect.
What does “a total opioid antagonist” mean?
Total’ means that it affects all four groups of opioid receptors, with a particular focus on the Mu and Kappa receptors. These receptors are responsible for the ‘high’ as well as the physical and psychological effects of opioids. They play a key role in the development of dependency. In this way, naltrexone protects all opioid receptor groups from drugs, preventing any specific drug-related sensations.
How was Naltrexone discovered?
Naltrexone was first developed in 1963 by the American company DuPont Pharmaceuticals. After extensive research, they created this pharmacological substance based on compounds derived from the poppy plant.
Since then, it has been widely used to treat alcohol and opioid dependence. Later, after extensive medical research and clinical trials, it was also found to be effective in treating crack-cocaine dependence
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Naltrexone blocks the effects opioids have on the brain and prevents the feeling of getting high.
It will trigger withdrawal symptoms if you are currently physically dependent on opiate drugs. It’s important to refrain from taking opioids for a minimum of 7-20 (depending on the type of opioid you use) days before taking Naltrexone to reduce the risk of a withdrawal "cold turkey".
Recovering from an addiction to opioids takes time and patience, as it’s rather slow process. But with the help of medications like Naltrexone, you will have support every step of the way.
Uses of Naltrexone
Naltrexone works differently than other types of medication used in opioid dependency treatment. Naltrexone often eliminates any desire to take opioids. By blocking these opioid receptors, Naltrexone users do not experience the euphoric and sedative effects of taking opioids.
Naltrexone does not cause any withdrawals or cravings when you stop taking it.
Oftentimes, opioids will give you a “high” or “rush” feeling – a feeling of contentment and pain relief. When taking naltrexone, these feelings will be blocked. Over time, you will regain a drug-free state of mind, allowing you to focus on developing a healthier lifestyle.
Although it is commonly used to treat an opioid addiction, it may not stop drug cravings. For this reason, Naltrexone is usually best suited for those who have completed the opiate detox and are motivated to continue on in the recovery process.
You may be more sensitive to lower doses of opioids after taking the tablet or having the implant, so you should abstain from taking any drugs at the conclusion of your medication-assisted treatment. Falling back on heroin or any other opioids could cause serious complications, including an overdose.
How is it Administered?
Naltrexone is available in three forms: tablet, injectable and implant forms. Common brand names for the tablet are ReVia and Depade. The injectable extended-release form of the drug is often sold under the name Vivitrol or Naltrexone in oil.
Naltrexone is most commonly administered in a tablet form; however, the injectable and implant options are gaining momentum.
Tablet-form doses of this medication will vary by person, strength of the medicine and the amount of medicine required each day. Follow your doctor’s instructions for consumption information. If you’re taking the tablet form at home, it may be helpful to have a family member or caregiver administer the doses as scheduled.
Another form of Naltrexone is a type of implant used for treatment. Implants are shaped like small pellets and are inserted into the lower abdominal wall. Insertion is completed with a local anesthetic. Once implanted, the device releases a consistent amount of naltrexone in the body for approximately 3-12 months.
The medication can also be administered through an extended-release injectable. Each month, Naltrexone in oil is injected into a muscle. It can only be administered by a doctor or nurse in a clinic setting, so it’s important to receive doses regularly in order to achieve the greatest benefit. Shortly after receiving the medication, you may notice pain, redness, bruising or swelling near the injection site. While this is common, be sure to notify your doctor if it does not go away or gets worse within two weeks.