Ken Saffier, MD, Natasha Pinto, MD
And Patients
CCRMC/HC Noon Conference
February 18, 2010
Drs. Pinto and Saffier have no financial interest
or other relationship with the manufacturer of
any commercial product discussed in this
presentation.
At the end of this presentation, participants will be
able to:
 List at least 2 patient criteria needed for
buprenorphine treatment.
 Explain why an opioid dependent patient must
be in opioid withdrawal prior to taking their first
dose of buprenorphine.
 Understand and experience aspects of what a
buprenorphine treatment group is like.
.
Oxycodone and hydrocodone both registered
substantial increases in emergency department
mentions in the last 5 years
Number of mentions
30,000
Hydrocodone
Oxycodone
20,000
10,000
0
1995
2/2004
1996
1997
1998
Source: SAMHSA, Drug Abuse Warning Network.
1999
2000
2001
2002
Over 2 million are estimated to be dependent on or
abusing prescription drugs in the past year.
Past Year Dependent/Abusers, Ages 12 or Older (in Thousands)
4,294
Marijuana
2,018
Prescription Drugs
1,488
Cocaine
426
Hallucinogens
Heroin
214
Inhalants
180
0
1,000
2,000
3,000
Source: SAMHSA, 2002 National Survey on Drug Use and Health.
1/2004
4,000
5,000
Issues of Concern
Percent of 12th Graders Reporting
Nonmedical Use of OxyContin and Vicodin
in the Past Year Remained High
12.0
10.5
9.6
Percent
10.0
9.3
8.0
6.0
4.0
5.0
4.5
4.0
2.0
0.0
OxyContin
2002
Vicodin
2003
2004
No year-to-year differences are statistically significant.

Agonist


Antagonist


Naloxone, naltrexone
Mixed agonist/antagonist


Heroin, hydrocodone, oxycodone, fentanyl
Pentozacine, butorphanol (Stadol)
Partial agonist

Buprenorphine
Intrinsic mu Activity: Full Agonist (Methadone), Partial
Agonist (Buprenorphine), Antagonist (Naloxone)
100
90
Full Agonist
(Methadone)
80
70
Intrinsic Activity 60
Partial Agonist
(Buprenorphine)
50
40
30
20
10
Antagonist (Naloxone)
0
-10
-9
-8
-7
Log Dose of Opioid
-6
-5
-4

High affinity for the mu opioid receptor



Slow dissociation from the mu receptor


Competes with other opioids and blocks their effects
Can precipitate withdrawal in highly opioid
dependent individuals
Prolonged therapeutic effect for opioid dependence
treatment
“Ceiling effect” for stimulation of a given
receptor
Human Opioid Receptors , ,
and 



H2N
extracellular fluid
S
S
AA identical in
3 receptors
AA identical in
2 receptors
AA different in
3 receptors
cell membrane
cell interior
HOOC
LaForge, Yuferov and Kreek, 2000
Zubieta et al., 2000






Poor oral bioavailability
Fair sublingual bioavailability
Takes about 10 minutes to dissolve
Schedule III drug
With naloxone (4:1) (Suboxone) or without
(Subutex)
Analgesic dose for mild to moderate pain is 0.3
– 0.6 mg. (0.4 mg = ~10 mg morphine)







Opioid dependent
Wants to stop using
Psychiatrically stable
Interested in office-based care
Reliable – can keep appointments
Agrees to urine tox screens
Has social support





Went to the ED in withdrawal.
Longstanding use of OxyContin.
$100/day “habit”.
Snorts q day for months, then stops.
Moves back to the Bay Area and within days,
he’s back to using.






I’m snorting 5 oxies per day – it’s an insane
amount to be putting into my body.
My palms are sweaty in the morning.
Then I have intense pain in my thighs.
I feel fidgety to an extreme.
So much physical and mental anguish.
I don’t want to waste money on this. It’s
destroying my life.







Dysphoric mood
Craving
Irritability
Tearing, rhinorrhea
Fever, chills
Sweating
Gooseflesh (cold
turkey)

Dilated pupils








Muscle aches
Back pain
Tremor
Yawning
Restless sleep, then
Insomnia
Anorexia
N/V, diarrhea,
cramps

Buprenorphine maintenance





Short acting opioids
Long acting opioids
Buprenorphine detox
Buprenorphine taper
(As an analgesic (buprenex))
Remaining in treatment (nr)
20
15
4 Subjects in Control Group Died
10
Detoxification
5
Maintenance
0
0
50
100
150
200
250
Treatment duration (days)
300
350

Our patients, especially Ryan.

Drs. Michael Saxon and Mary Jeanne Kreek

Chris Verdugo, CCTV

Gary Larson
Substance Abuse and Mental Health Administration
Center for Substance Abuse Treatment
Treatment Improvement Protocol (TIP) Series
Clinical Guidelines for the Use of
Buprenorphine in the Treatment of Opioid
Addiction # 40
National Clearinghouse for Alcohol and Drug Information
(800) 729 – 6686 or (301) 468 – 2600
www.buppractice.com
(discounted for residents)



Buprenorphine at CCRMC & HC’s:
 925 370 5868 (leave message)
or
 925 370 5859 (leave message)
 Call Ken Saffier, MD, pager 334
http://buprenorphine.samhsa.gov/about.h
tml#top
www.csam-asam.org