Thursday, March 27, 2014

Suboxone

Suboxone is a combination of opioid, Buprenophine and opioid antagonist, naloxone. It is used as an alternative to Methadone Maintenance Therapy for a person addicted to narcotics or opiates such as street heroin or prescription oxycontins. 
Suboxone is taken sub lingually because the Buprenophines is absorbed this way while the Naloxone is not. However if a person were to try to take the Suboxone and inject it recreationally the naloxone would be absorbed immediately and counteract the narcotic effect. This makes suboxone a medication that is least likely to be diverted for illegal purposes.
To start suboxone one should be in early stages of withdrawal from whatever other opioid drug being consumed. This takes usually 1 - 3 days depending on the drug and dose that was being taken. The reason for this is that Buprenorphine is a partial mu opioid receptor agonist and a kappa receptor antagonist. The mu opioid receptor accounts for analgesia, euphoria, sedation and respiratory depression. Because it is a partial receptor it has less sedation.  The kappa antagonism may be the cause of the antidepressant effect noted with buprenorphine.  Because of the strong binding effect of buprenorphine on receptors the buprenorphine will displace other weaker binding opioids potentially causing withdrawal effects if a person isn't already weaning off the opioid drug they are switching from.
With changing a person from methadone, the person is first reduced to only 30 mg a day of methadone.  A person would then likely miss a day of methadone then start suboxone the next day.
The difficulty here is with those people who are on high dose methadone, which can be as high as 250 mg.  First reducing them to where switching is possible is it's own challenge.
With heroin the 'dosage' a person is taking on the street is always uncertain because of the quality and amount of 'cutting' of the heroin.  Patient's may take as little as a 1 pt or $10 a day to as high as the normal heroin dependent person uses in the range of grams, at $200 to $400 or more a day habit (356 days a year).
To start buprenorphine a person having waited at least 4 hours after last short acting opioid or 24 hours after last long acting opioid, takes 4 mg witnessed under the tongue.  This is given by the pharmacist or at the clinic and a person waits this first day to be reassessed.  and waits to ensure they're not going into withdrawal. Buprenorphine peaks at 1 to 4 hours. It is eliminated over 2 to 3 days making a once a day dosage work fine.
The normal starting dosage of Suboxone is 4 mg.  The eyes are observed because dilated pupils are associated with withdrawal while constricted pupils are associated with opioid use.  If after 5 hours a patient has withdrawal signs including dilated pupils another 4 mg of Suboxone can be safely added. The concern is that a person will overdose as suboxone can cause respiratory failure.  One doesn't want to give too much suboxone the first day.
The normal maintenance dose is 8 mg to 24 mg and the medication can be increased over the next week or two to the maximum dosage needed. This is an advantage over methadone where a person may start 30 to 40 mg but increased dosage is only by 10 mg.  The more rapid induction with buprenorphine is an appreciated quality.
This medication is available as an alternative to methadone maintenance therapy.

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