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Opioid Pharmacology
1.
Comparative Opioid
Pharmacology
2.
3.
4.
5.
6.
7.
Morphine The prototypical
opioid
8.
9.
Simulation of Morphine
Time Course Dahan et al. Anesthesiology. 2004 Nov;101(5):1201-9.
10.
Fentanyl The ever
morphing molecule
11.
12.
How we think
of fentanyl: (small part of the market)
13.
Fentanyl morph 1:
Duragesic
14.
Fentanyl morph 2:
Actiq
15.
Fentanyl morph 3:
E-trans fentanyl Viscusi et al, JAMA 2004 291:1333
16.
Fentanyl morph 4:
Inhaled liposomal fentanyl Hung et al, Anesthesiology 1995 83:277-84
17.
Fentanyl morph 5:
Inhaled fentanyl aerosol Mather et al, Br J Clin Pharmacol 1998 46:37
18.
Fentanyl morph 6:
Effervescent Fentanyl (OraVescent) Pather et al, http://www.drugdeliverytech.com/cgi-bin/articles.cgi?idArticle=5
19.
Sufentanil Newly morphing
molecule
20.
21.
Sufentanil morph 1:
Implantable sufentanil delivery http://www.drugdeliverytech.com/cgi-bin/articles.cgi?idArticle=115
22.
23.
Hydromorphone A better
morphine
24.
25.
26.
27.
Methadone The Under-Utilized
Opioid
28.
29.
Fundamental PK/PD Parameters
30.
Comparative Opioid PK
31.
Comparative Opioid PK
32.
Comparative Onset of
Opioid Drug Effect
33.
Context Sensitive Half
Time
34.
50% Effect Site
Decrement Time
35.
20% Effect Site
Decrement Time
36.
Rise to Steady
State
37.
Relative Potency
38.
50
g fentanyl at 10 minutes
39.
50
g/hour fentanyl at 2 hours
40.
Opioid
Receptor
41.
42.
43.
44.
MOR-1 gene splice
variants (gene=OPRM) Gavril Pasternak, http://www.mskcc.org/mskcc/html/11384.cfm
45.
Antisense lowers
morphine analgesia (no effect on m6g) Gavril Pasternak, Life Sciences 2001:68, 2213
46.
Antisense lowers
m6g analgesia (no effect on morphine) Gavril Pasternak, Life Sciences 2001:68, 2213
47.
48.
49.
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