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Buprenorphine in the treatment of opioid dependence
1. Buprenorphine in theBuprenorphine in the
treatment of Opioidtreatment of Opioid
DependenceDependence
““Addiction doesn’t come heralded by a brass band, itAddiction doesn’t come heralded by a brass band, it
sneaks up on you, and sometimes with extraordinarysneaks up on you, and sometimes with extraordinary
speed”speed”
C. Everett Koop (former US Surgeon General), 2003
Dr Jacqueline BOUTROUILLEDr Jacqueline BOUTROUILLE
2. What is the cost to
society?
• $20 billion per year total cost of heroin
abuse
(Harwood et al, 1998)
• The economic cost of drug use and
dependence estimated to be $98 billion
(Harwood et al, 1998)
• Figures do not take into account social
impact of drug addiction
– Crime / legal costs
– Absenteeism from work /
unemployment
3. Choosing to use?
• A non-dependent user controls his/her use
• A dependent person is controlled by his/her addiction
– People suffering from addiction often seek treatment
because they “want their life back”
“Addiction doesn’t come heralded by a band, it sneaks up
on you, and sometimes with extraordinary speed”
Koop, 2003
4. Are opioid-dependent
individuals bad or sick?
• Opioid dependence has several features in
common with diabetes and hypertension
– Chronic, relapsing nature
– Genetic vulnerability
– Physiologic brain changes
– Responds to chronic disease management
strategies, not short-term symptomatic relief
5. Diagnosing addiction?
• More than 3 of the following during last 12 months:
– Tolerance
– Withdrawal syndrome
– Use of the drug to avoid/reverse withdrawal symptoms
– Compulsion to use drug, especially when trying to stop
– Narrowed repertoire of behaviors associated with
drug use
– Drug-related behaviors more important than other
previously more important activities/behaviors
– Early relapse after withdrawal
World Health Organization
6. What are the usual signs
and symptoms?
• Sweating
• Yawning
• Anxiety
• Increased BP and respiratory rate
• Cravings
• Lacrimation
• Piloerection
• Rhinitis
• Gastrointestinal symptoms
– Abdominal cramps
– Diarrhea
7. Once addicted, why isn’t it
easy to stop?
• Withdrawal from opioids is associated with an extremely
unpleasant syndrome:
– Physical pain (muscle aches, cramps)
– Nausea and vomiting
– Diarrhea
– Dysphoria
– Depression
– Irritability and anxiety
– Dysregulation of brain reward systems
• Pharmacologic intervention proven to help relieve
symptoms of withdrawal
8. OPIOID RECEPTORS:OPIOID RECEPTORS:
Activity determined by -Activity determined by -
• AffinityAffinity - how tight does the drug bind to the- how tight does the drug bind to the
receptorreceptor
• Intrinsic ActivityIntrinsic Activity - how much does the drug- how much does the drug
stimulate the receptorstimulate the receptor
• DissociationDissociation - how fast does the drug leave- how fast does the drug leave
thethe receptorreceptor
9. OPIOID RECEPTOR PHARMACOLOGYOPIOID RECEPTOR PHARMACOLOGY
Agonists, antagonists, and partialAgonists, antagonists, and partial
agonistsagonists
Agonists:Agonists: substances that bind to the receptor andsubstances that bind to the receptor and
produces a full biological responseproduces a full biological response
Antagonists:Antagonists: substances that bind to the receptorsubstances that bind to the receptor
and do not produce a biological responseand do not produce a biological response
Partial agonists:Partial agonists: substances that bind to thesubstances that bind to the
receptor and produce a limited response – less thanreceptor and produce a limited response – less than
the full response produced an agonistthe full response produced an agonist
11. ProvisionsProvisions
An Amendment to the Controlled SubstancesAn Amendment to the Controlled Substances
Act that allows certified physicians toAct that allows certified physicians to
prescribe and dispense Schedule III, IV, andprescribe and dispense Schedule III, IV, and
V narcotic drugs that have been approved byV narcotic drugs that have been approved by
the Food and Drug Administration for use inthe Food and Drug Administration for use in
addiction treatment (i.e., maintenance oraddiction treatment (i.e., maintenance or
medical withdrawal (detoxification))medical withdrawal (detoxification))
What is DATA (Drug & AlcoholWhat is DATA (Drug & Alcohol
Treatment Act) 2000?Treatment Act) 2000?
12. LimitationsLimitations
• The total number of patients for aThe total number of patients for a
practitioner or group practice to 30practitioner or group practice to 30
• Secretary of HHS may change this numberSecretary of HHS may change this number
by regulation (group practice number isby regulation (group practice number is
currently under review)currently under review)
13. Enter buprenorphine
• Effective treatment option for opioid
dependence (Ling et al 1998)
• Reduces morbidity and mortality (Auriacombe et al
1998)
• Improves quality of life (Giacomuzzi, et al 2003, Anisse,
2001)
14. BuprenorphineBuprenorphine
• A synthetic opioidA synthetic opioid
• Partial agonist at thePartial agonist at the µµ receptorreceptor
-- Low intrinsic activity only partiallyLow intrinsic activity only partially
activating opiate receptorsactivating opiate receptors
- Exhibits ‘ceiling’ effects on respiratory- Exhibits ‘ceiling’ effects on respiratory
depressiondepression
• High affinity for theHigh affinity for the µµ receptorreceptor
- Binds more tightly to opiate receptors than- Binds more tightly to opiate receptors than
other opiates or opiate antagonistsother opiates or opiate antagonists
• Slow dissociation from the receptorSlow dissociation from the receptor
–milder withdrawalmilder withdrawal
15. Duration of effectsDuration of effects
• Rapid onset of action: 30 – 60 minutesRapid onset of action: 30 – 60 minutes
(after S/L administration)(after S/L administration)
• Peak effects: 1 – 4 hoursPeak effects: 1 – 4 hours
• Duration of action is dose relatedDuration of action is dose related
• low dose : 4 – 12 hrslow dose : 4 – 12 hrs
• med dose : ~ 24 hrsmed dose : ~ 24 hrs
• high dose : 2 – 3 dayshigh dose : 2 – 3 days
• Elimination half-life ~24 to 36 hoursElimination half-life ~24 to 36 hours
16. Pharmacological & ClinicalPharmacological & Clinical
PropertiesProperties
•Similar to other opiates, but lessSimilar to other opiates, but less
sedating and safer in overdosesedating and safer in overdose
•Side effectsSide effects
•Daily or alternate day dosingDaily or alternate day dosing•Long duration of actionLong duration of action
•Reduces opioid useReduces opioid use•‘‘Blocks’ effects of opiatesBlocks’ effects of opiates
•Reduces cravingsReduces cravings
•Increases treatment retentionIncreases treatment retention
•Opiate-like effectsOpiate-like effects
•Prevents withdrawalPrevents withdrawal
•Can be used for maintenance /Can be used for maintenance /
withdrawalwithdrawal
•Substitutes for heroinSubstitutes for heroin
Clinical implicationClinical implicationPharmacologicalPharmacological
propertyproperty
18. Interactions with other opioids?
• Opioid antagonists:
– Incomplete reversal by naloxone
• Opioid agonists:
– Blockade effect, limiting the effects of
additional opioid use
– Potential for precipitated withdrawal when
taken too soon after a full agonist
19. Side-effectsSide-effects
• All opioids have a qualitatively similar profile ofAll opioids have a qualitatively similar profile of
side-effectsside-effects
• Side-effects generally transientSide-effects generally transient
• Experience of side-effects variableExperience of side-effects variable
-A client may experience side-effect to oneA client may experience side-effect to one
opioid but not to anotheropioid but not to another
• Not all symptoms are necessarily side-effects:Not all symptoms are necessarily side-effects:
consider other causesconsider other causes
Hinweis der Redaktion
1. According to the National Household Survey on Drug Abuse, in 1998, 2,371,000 persons reported ever using heroin, and in 1999, 149,000 reported initiating use. Among the latter, 42,000 were between the ages of 12-17 years, and 73,000 between the ages of 18-25 years.
2. It is also estimated, based on the National Household Survey on Drug Abuse and the Drug Use Forecasting program, that there were 980,000 people who use heroin at least once per week, and 253,000 people who use heroin less than once per week in the United States in 1998.
3. The Office of National Drug Control Policy reports that there are 810,000 chronic opioid users in the United States, and that this is the highest number since the late 1970s.
[References:
National Drug Control Strategy: 2000 Annual Report. Office of National Drug Control Policy, page 116.
National Household Survey on Drug Abuse, Population Estimates 1998. Substance Abuse and Mental Health Services Administration, Office of Applied Studies, Rockville, Maryland, 1999.
Office of National Drug Control Policy. What America's Users Spend on Illegal Drugs: 1988-1995. Washington, DC: Office of National Drug Control Policy 1997.
Summary of Findings from the 1999 National Household Survey on Drug Abuse. Substance Abuse and Mental Health Services Administration, Office of Applied Studies, Rockville, Maryland, 2000.
Web sites: Substance Abuse and Mental Health Services Administration (www.samhsa.gov); National Institute on Drug Abuse (www.nida.nih.gov)]
Note physical features of dependence vs psychological features
