Buprenorphine - Revision history

Spacer: Added: * Dizziness and Vertigo + few spelling errors.

2017-06-10T01:55:06Z

Added: * Dizziness and Vertigo + few spelling errors.

← Older revision		Revision as of 20:55, 9 June 2017
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	== Uses ==		== Uses ==

	Buprenorphine is usually sold in the form of sublingual tablets (Suboxone), or ~~transdermal~~ patches (Butrans). Patches can be attached to skin for long release as treatment for opioid withdrawal, or cut and chewed for recreational use. Usual (30 minutes) sub-lingual use of patches is not 100% effective, so patches can be re-used. Buprenorphine is water-soluble, and can be extracted with a [[Cold Water Extraction]] (takes more time, usually 24 hours, or around 4 hours with few drops of strong alcohol). Since buprenorphine is a long acting opioid antagonist, other opioids won't work for at least 36 hours after dosing buprenorphine (though some negative effects will be garnered).		Buprenorphine is usually sold in the form of sublingual tablets (Suboxone), or trans dermal patches (Butrans). Patches can be attached to skin for long release as treatment for opioid withdrawal, or cut and chewed for recreational use. Usual (30 minutes) sub-lingual use of patches is not 100% effective, so patches can be re-used. Buprenorphine is water-soluble, and can be extracted with a [[Cold Water Extraction]] (takes more time, usually 24 hours, or around 4 hours with few drops of strong alcohol). Since buprenorphine is a long acting opioid antagonist, other opioids won't work for at least 36 hours after dosing buprenorphine (though some negative effects will be garnered).

	Buprenorphine will cause withdrawal if you have an opioid tolerance and don't wait long enough (typically 48~ hours) before taking it.		Buprenorphine will cause withdrawal if you have an opioid tolerance and don't wait long enough (typically 48~ hours) before taking it.

	Respiratory depression from buprenorphine (or buprenorphine/naloxone) overdose is less likely than from other opioids. There is no evidence of organ damage with chronic use of buprenorphine, although increases in liver enzymes are sometimes seen. Likewise, there is no evidence of significant disruption of cognitive or ~~psychomotor~~ performance with buprenorphine maintenance dosing.		Respiratory depression from buprenorphine (or buprenorphine/naloxone) overdose is less likely than from other opioids. There is no evidence of organ damage with chronic use of buprenorphine, although increases in liver enzymes are sometimes seen. Likewise, there is no evidence of significant disruption of cognitive or psycho motor performance with buprenorphine maintenance dosing.

	== Dosage ==		== Dosage ==

Spacer: /* Negative */

2017-06-07T18:26:49Z

Negative

← Older revision		Revision as of 13:26, 7 June 2017
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	* Distress/irritability		* Distress/irritability

			* Dizziness and Vertigo

	== Harm Reduction ==		== Harm Reduction ==

GrimReaper: /* Dosage */

2015-04-13T15:30:32Z

Dosage

← Older revision		Revision as of 10:30, 13 April 2015
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	{\| class="wikitable"		{\| class="wikitable"
	\|+ ~~Siblingual~~		\|+ Sublingual
	\|-		\|-
	\| Light \|\| 1-2mg		\| Light \|\| 1-2mg

GrimReaper at 10:08, 10 March 2015

2015-03-10T10:08:24Z

← Older revision		Revision as of 05:08, 10 March 2015
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	[[File:Suboxone.jpg\|350px\|right]]		[[File:Suboxone.jpg\|350px\|right]]

	Buprenorphine is a semi-synthetic opioid derived from thebaine which is typically used for treatment of opioid addiction. It is an analgesic, and has gained notoriety for its ability to successfully interrupt severe opiate addictions. Buprenorphine has a higher affinity for μ-opioid receptors compared to full opioid agonists. Because of this, buprenorphine can block the effects of other opioid agonists in a dose-dependent fashion. By its dual effects of reducing craving and attenuating the response to administered heroin, buprenorphine reduces the self-administration of heroin. Methadone, a full opioid agonist, also reduces the impact of additional heroin, but the effect of methadone is primarily due to the induction of cross-tolerance which is dose dependent. In contrast buprenorphine achieves its effect primarily by prolonged occupancy of a high proportion of opioid receptors, blocking the action of heroin and other opioid receptor agonists.		'''Buprenorphine''' is a semi-synthetic opioid derived from thebaine which is typically used for treatment of opioid addiction. It is an analgesic, and has gained notoriety for its ability to successfully interrupt severe opiate addictions. Buprenorphine has a higher affinity for μ-opioid receptors compared to full opioid agonists. Because of this, buprenorphine can block the effects of other opioid agonists in a dose-dependent fashion. By its dual effects of reducing craving and attenuating the response to administered heroin, buprenorphine reduces the self-administration of heroin. Methadone, a full opioid agonist, also reduces the impact of additional heroin, but the effect of methadone is primarily due to the induction of cross-tolerance which is dose dependent. In contrast buprenorphine achieves its effect primarily by prolonged occupancy of a high proportion of opioid receptors, blocking the action of heroin and other opioid receptor agonists.

	== History ==		== History ==
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	The difficulties of coordinating public and private interests, local and global effects, changes in domestic regulatory mechanisms, and perceptions of addiction and its treatment charted buprenorphine’s tortuous, 30-year path to FDA approval and market. Buprenorphine arose as a maintenance therapy at a time when addicts - like other citizens - were expected to take personal responsibility for health and healthcare, and where such decisions were seen as individual matters of choice and political entitlement.		The difficulties of coordinating public and private interests, local and global effects, changes in domestic regulatory mechanisms, and perceptions of addiction and its treatment charted buprenorphine’s tortuous, 30-year path to FDA approval and market. Buprenorphine arose as a maintenance therapy at a time when addicts - like other citizens - were expected to take personal responsibility for health and healthcare, and where such decisions were seen as individual matters of choice and political entitlement.

	= Uses =		== Uses ==

	Buprenorphine is usually sold in the form of sublingual tablets (Suboxone), or transdermal patches (Butrans). Patches can be attached to skin for long release as treatment for opioid withdrawal, or cut and chewed for recreational use. Usual (30 minutes) sub-lingual use of patches is not 100% effective, so patches can be re-used. Buprenorphine is water-soluble, and can be extracted with a [[Cold Water Extraction]] (takes more time, usually 24 hours, or around 4 hours with few drops of strong alcohol). Since buprenorphine is a long acting opioid antagonist, other opioids won't work for at least 36 hours after dosing buprenorphine (though some negative effects will be garnered).		Buprenorphine is usually sold in the form of sublingual tablets (Suboxone), or transdermal patches (Butrans). Patches can be attached to skin for long release as treatment for opioid withdrawal, or cut and chewed for recreational use. Usual (30 minutes) sub-lingual use of patches is not 100% effective, so patches can be re-used. Buprenorphine is water-soluble, and can be extracted with a [[Cold Water Extraction]] (takes more time, usually 24 hours, or around 4 hours with few drops of strong alcohol). Since buprenorphine is a long acting opioid antagonist, other opioids won't work for at least 36 hours after dosing buprenorphine (though some negative effects will be garnered).
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	Respiratory depression from buprenorphine (or buprenorphine/naloxone) overdose is less likely than from other opioids. There is no evidence of organ damage with chronic use of buprenorphine, although increases in liver enzymes are sometimes seen. Likewise, there is no evidence of significant disruption of cognitive or psychomotor performance with buprenorphine maintenance dosing.		Respiratory depression from buprenorphine (or buprenorphine/naloxone) overdose is less likely than from other opioids. There is no evidence of organ damage with chronic use of buprenorphine, although increases in liver enzymes are sometimes seen. Likewise, there is no evidence of significant disruption of cognitive or psychomotor performance with buprenorphine maintenance dosing.

	= Dosage =		== Dosage ==

	Dosage is usually 2-3mg (assuming 100% effectiveness), and most users don't feel the need to take more. Ceiling effect is 16-32mg, and redosing is not effective.		Dosage is usually 2-3mg (assuming 100% effectiveness), and most users don't feel the need to take more. Ceiling effect is 16-32mg, and redosing is not effective.
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	\|}		\|}

	= Duration =		== Duration ==

	{\| class="wikitable"		{\| class="wikitable"
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	\|}		\|}

	= Effects =		== Effects ==

	Because of its ceiling effect and poor bio-availability, buprenorphine is safer in high doses compared to full opioid agonists. The maximal effects of buprenorphine appear to occur in the 16–32 mg dose range for sublingual tablets. Higher doses are unlikely to produce greater effects.		Because of its ceiling effect and poor bio-availability, buprenorphine is safer in high doses compared to full opioid agonists. The maximal effects of buprenorphine appear to occur in the 16–32 mg dose range for sublingual tablets. Higher doses are unlikely to produce greater effects.

	== Positive ==		=== Positive ===

	* Euphoria		* Euphoria
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	* Overall feeling of contentedness		* Overall feeling of contentedness

	== Neutral ==		=== Neutral ===

	* Pupillary dilation		* Pupillary dilation

	== Negative ==		=== Negative ===

	* Dysphoric mood		* Dysphoric mood
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	* Distress/irritability		* Distress/irritability

	= Harm Reduction =		== Harm Reduction ==

	Unlike methadone, the effect of buprenorphine on respiratory depression reaches a ceiling, therefore higher doses do not increase risk of respiratory depression to a significant degree.		Unlike methadone, the effect of buprenorphine on respiratory depression reaches a ceiling, therefore higher doses do not increase risk of respiratory depression to a significant degree.
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	However, if buprenorphine is used in combination with other central nervous system depressants, such as benzodiazepines and other CNS [[Depressants]], the combined effect on respiration can be life threatening.		However, if buprenorphine is used in combination with other central nervous system depressants, such as benzodiazepines and other CNS [[Depressants]], the combined effect on respiration can be life threatening.

	== Interactions ==		=== Interactions ===

	[[Drug Combinations]]		[[Drug Combinations]]
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	Combination of buprenorphine and SSRIs [http://www.ncbi.nlm.nih.gov/pubmed/18774063 can cause] Serotonin Syndrome.		Combination of buprenorphine and SSRIs [http://www.ncbi.nlm.nih.gov/pubmed/18774063 can cause] Serotonin Syndrome.

	= Chemistry and Pharmacology =		== Chemistry and Pharmacology ==

	Buprenorphine is a derivative of the opioid alkaloid thebaine that is a more potent (25 – 40 times) and longer lasting analgesic than morphine. It appears to act as a partial agonist at the μ- and κ-opioid receptors and as an antagonist at δ-opioid-receptors. The lack of δ-opioid agonism has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.		Buprenorphine is a derivative of the opioid alkaloid thebaine that is a more potent (25 – 40 times) and longer lasting analgesic than morphine. It appears to act as a partial agonist at the μ- and κ-opioid receptors and as an antagonist at δ-opioid-receptors. The lack of δ-opioid agonism has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.
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	Buprenorphine is metabolised by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation).		Buprenorphine is metabolised by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation).

	= Links =		== Links ==

	[https://en.wikipedia.org/wiki/Buprenorphine Wikipedia]		[https://en.wikipedia.org/wiki/Buprenorphine Wikipedia]

Roi at 06:22, 21 July 2014

2014-07-21T06:22:25Z

← Older revision		Revision as of 01:22, 21 July 2014
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	[[File:Suboxone.jpg\|350px\|right]]		[[File:Suboxone.jpg\|350px\|right]]

	Buprenorphine is a semi-synthetic opioid derived from thebaine which is typically used for treatment of opioid addiction. It is an analgesic, and has gained notoriety for its ability to successfully interrupt severe opiate addictions. Buprenorphine has a higher affinity for μ-opioid receptors compared to full opioid agonists. Because of this, buprenorphine can block the effects of other opioid agonists in a dose-dependent fashion. By its dual effects of reducing craving and attenuating the response to administered heroin, buprenorphine reduces the self-administration of heroin. Methadone, a full opioid agonist, also reduces the impact of additional heroin, but the effect of methadone is primarily due to the induction of cross-tolerance which is dose dependent. In contrast buprenorphine achieves its effect primarily by prolonged occupancy of a high proportion of opioid receptors, blocking the action of heroin.		Buprenorphine is a semi-synthetic opioid derived from thebaine which is typically used for treatment of opioid addiction. It is an analgesic, and has gained notoriety for its ability to successfully interrupt severe opiate addictions. Buprenorphine has a higher affinity for μ-opioid receptors compared to full opioid agonists. Because of this, buprenorphine can block the effects of other opioid agonists in a dose-dependent fashion. By its dual effects of reducing craving and attenuating the response to administered heroin, buprenorphine reduces the self-administration of heroin. Methadone, a full opioid agonist, also reduces the impact of additional heroin, but the effect of methadone is primarily due to the induction of cross-tolerance which is dose dependent. In contrast buprenorphine achieves its effect primarily by prolonged occupancy of a high proportion of opioid receptors, blocking the action of heroin and other opioid receptor agonists.

	== History ==		== History ==

GrimReaper: /* Negative */

2014-07-16T15:22:41Z

Negative

← Older revision		Revision as of 10:22, 16 July 2014
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	* Nausea or vomiting		* Nausea or vomiting

	* ~~Diarrhoea~~		* Diarrhea

	* Muscle aches/cramps		* Muscle aches/cramps

GrimReaper: /* Duration */

2014-07-16T15:22:27Z

Duration

← Older revision		Revision as of 10:22, 16 July 2014
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	{\| class="wikitable"		{\| class="wikitable"
	\|+ ~~Siblingual~~		\|+ Sublingual
	\|-		\|-
	\| Onset \|\| 30-60 minutes		\| Onset \|\| 30-60 minutes

Reality at 14:04, 16 July 2014

2014-07-16T14:04:22Z

← Older revision		Revision as of 09:04, 16 July 2014
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	[[File:Suboxone.jpg\|350px\|right]]		[[File:Suboxone.jpg\|350px\|right]]

	~~= General Information =~~

	Buprenorphine is a semi-synthetic opioid derived from thebaine which is typically used for treatment of opioid addiction. It is an analgesic, and has gained notoriety for its ability to successfully interrupt severe opiate addictions. Buprenorphine has a higher affinity for μ-opioid receptors compared to full opioid agonists. Because of this, buprenorphine can block the effects of other opioid agonists in a dose-dependent fashion. By its dual effects of reducing craving and attenuating the response to administered heroin, buprenorphine reduces the self-administration of heroin. Methadone, a full opioid agonist, also reduces the impact of additional heroin, but the effect of methadone is primarily due to the induction of cross-tolerance which is dose dependent. In contrast buprenorphine achieves its effect primarily by prolonged occupancy of a high proportion of opioid receptors, blocking the action of heroin.		Buprenorphine is a semi-synthetic opioid derived from thebaine which is typically used for treatment of opioid addiction. It is an analgesic, and has gained notoriety for its ability to successfully interrupt severe opiate addictions. Buprenorphine has a higher affinity for μ-opioid receptors compared to full opioid agonists. Because of this, buprenorphine can block the effects of other opioid agonists in a dose-dependent fashion. By its dual effects of reducing craving and attenuating the response to administered heroin, buprenorphine reduces the self-administration of heroin. Methadone, a full opioid agonist, also reduces the impact of additional heroin, but the effect of methadone is primarily due to the induction of cross-tolerance which is dose dependent. In contrast buprenorphine achieves its effect primarily by prolonged occupancy of a high proportion of opioid receptors, blocking the action of heroin.
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	600µg is considered equivalent to 10 mg morphine for pain relief.		600µg is considered equivalent to 10 mg morphine for pain relief.

	=~~= Sublingual ==~~		{\| class="wikitable"
			\|+ Siblingual
	Light: 1-~~2 mg~~		\|-
			\| Light \|\| 1-2mg
	Common: 3-~~6 mg~~		\|-
			\| Common \|\| 3-6mg
	Strong: 6-~~8 mg~~		\|-
			\| Strong \|\| 6-8mg
	Heavy~~: 8 mg~~+ (16-~~32 mg ceiling effect)~~		\|-
			\| Heavy \|\| 8mg+
			\|-
			\| Ceiling \|\| 16-32mg
			\|}

	= Duration =		= Duration =

	=~~= Sublingual ==~~		{\| class="wikitable"
			\|+ Siblingual
	Onset~~: 30–60~~ minutes		\|-
			\| Onset \|\| 30-60 minutes
	Peak~~: 1–4~~ hours		\|-
			\| Peak \|\| 1-4 hours
	Total ~~Duration: 8–12 hours at~~ low ~~doses (e.g. 2 mg~~)~~, 24–72~~ hours at high ~~doses (e.g. >16 mg~~)		\|-
			\| Total (low dose) \|\| 8-12 hours
			\|-
			\| Total (high dose) \|\| 24-72 hours
			\|}

	= Effects =		= Effects =

Roi: /* Links */

2014-07-14T19:47:23Z

Links

← Older revision		Revision as of 14:47, 14 July 2014
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	= Links =		= Links =

	https://en.wikipedia.org/wiki/Buprenorphine		[https://en.wikipedia.org/wiki/Buprenorphine Wikipedia]

	https://erowid.org/pharms/buprenorphine/buprenorphine.shtml		[https://erowid.org/pharms/buprenorphine/buprenorphine.shtml Erowid]

	http://buprenorphine.samhsa.gov/about.html		http://buprenorphine.samhsa.gov/about.html

	http://www.ncbi.nlm.nih.gov/pubmed/22256949		[http://www.ncbi.nlm.nih.gov/pubmed/22256949 The history of the development of buprenorphine as an addiction therapeutic.]

	http://www.nationaldrugstrategy.gov.au/internet/drugstrategy/publishing.nsf/content/9011C92D2F6E1FC5CA2575B4001353B6/$File/bupren1.pdf		http://www.nationaldrugstrategy.gov.au/internet/drugstrategy/publishing.nsf/content/9011C92D2F6E1FC5CA2575B4001353B6/$File/bupren1.pdf

GrimReaper at 11:13, 10 July 2014

2014-07-10T11:13:40Z

← Older revision		Revision as of 06:13, 10 July 2014
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	Buprenorphine is metabolised by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation).		Buprenorphine is metabolised by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation).

	~~= Legal status=~~

	= Links =		= Links =