OPIOID ADDICTION THERAPY
OPIOID ADDICTION THERAPY
Opioid addiction should be treated pharmacologically. The most effective options are Buprenorphine and Methadone.
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VOCABULARY
Opiate - naturally derived from poppies (opium, morphine, heroin, codeine)
Opioid - a synthetic opiate (fentanyl, hydromorphone, methadone). These two terms are often used interchangeably.
OPIOID BLOCKERS
Naloxone (Narcan) immediately reverses Opioids. It outcompetes them. It saves someone who has overdosed on opioids. Injected (or sprayed nasally) by EMS into anyone found unresponsive. It instantly wakes up those who’ve overdosed on heroin, fentanyl or morphine. This is very dramatic! Akin to waking up the dead! The patient wakes up feeling miserable, because that Naloxone just instantly put them into withdrawal.
Naltrexone slowly blocks Opioids. It’s an opioid antagonist. It reduces cravings after you’ve detoxed. Given as a monthly injection. It blocks the effects of Opioids if they are used (it also lowers alcohol cravings). Like Buprenorphine, it can precipitate withdrawal (see below). Mnemonics: NalTRExone TREads slowly; TREes grow slowly)
OPIOID AGONISTS
Methadone is a very slow opioid. That's because it pools inside your fat cells. From there, it slowly leaks out of your fat, providing a slow continuous supply of opioids. It has a huge VD and a long half life. Methadone is almost exclusively used in the setting of addiction. It gives the body a smooth and steady supply of opioids to prevent craving sensations. Since the methadone molecule binds to opioid receptors very strongly, if you shoot up heroin after taking methadone, you won't get as high. Since methadone has a high potential for abuse (i.e., injecting it gets you high), patients must swallow the medication under the direct supervision of a healthcare professional. Methadone is traditionally distributed at "Methadone clinics."
Buprenorphine is a rather special opioid. It has two unique properties that enable it to fight addiction.
First, buprenorphine only partially binds onto opioid receptors. Neurons aren't fully activated by this partial bind. This gives a muted analgesic and euphoric effect. No high!
Second, it's grip is extremely strong (it's receptor affinity is about 1000 times stronger than morphine). It's stronger than every other opioid. If you take heroin on top of buprenorphine, the heroin will have a much weaker effect. In fact Buprenorphine is so strong, that it can kick out opioids already bound to the receptor -- the downside here is that it can precipitate withdrawal. Patients should ideally be opioid-free when they begin taking buprenorphine.
Here's why giving Buprenorphine to someone already on Opioids can precipitate withdrawal
MIXED AGONISTS & ANTAGONISTS
Suboxone is a new oral formulation of Buprenorphine that’s mixed with Naloxone. It's incredibly popular. Why are they mixed together? The short answer is to prevent abuse. Here's the long answer. Naloxone doesn’t work if taken orally (due to a large first pass metabolism). If a patient eats their Suboxone as directed, the Naloxone is swiftly destroyed by the liver. But if a sneaky patient broke the rules and injected the Suboxone (injecting Buprenorphine or Methadone gets you pretty high), the Naloxone would kick in, block the Buprenorphine and prevent the patient’s high.
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