PMID- 3185099
OWN - NLM
STAT- MEDLINE
DCOM- 19881201
LR  - 20190701
IS  - 0024-3205 (Print)
IS  - 0024-3205 (Linking)
VI  - 43
IP  - 17
DP  - 1988
TI  - The antinociceptive effect and pharmacokinetics of olvanil following oral and 
      subcutaneous dosing in the mouse.
PG  - 1385-91
AB  - Mice were tested for response latency on a 55 degrees C hot plate after 
      subcutaneous (S.C.) or oral administration of olvanil (dose level 200 and 300 
      mg/kg, respectively). Only the S.C. injection of olvanil produced 
      antinociception. A pharmacokinetics experiment with radiolabeled olvanil (200 
      mg/kg) was conducted to determine whether this antinociception difference was 
      related to a difference in plasma concentration of olvanil following the two 
      routes of administration. The results indicate that concentrations of 
      radioactivity (olvanil plus metabolites) in plasma reach a peak higher and faster 
      after oral dosing than after S.C. injection. However, the area under the 
      concentration-time curve (AUC) for recovery of radioactivity was slightly higher 
      after the S.C. injection than after the oral dose of olvanil. In contrast, intact 
      olvanil is barely measurable (10 to 30 ng/g) in plasma following an oral dose but 
      is present in high concentration (100 to 2000 ng/g) following S.C. injection. The 
      AUC for olvanil was also higher following a S.C. dose. These data indicate that 
      olvanil fails to produce antinociception after oral dosing in mice not due to 
      lack of absorption, but because it undergoes first pass metabolism.
FAU - Sietsema, W K
AU  - Sietsema WK
AD  - Procter and Gamble Company, Cincinnati, Ohio 45239-8707.
FAU - Berman, E F
AU  - Berman EF
FAU - Farmer, R W
AU  - Farmer RW
FAU - Maddin, C S
AU  - Maddin CS
LA  - eng
PT  - Journal Article
PL  - Netherlands
TA  - Life Sci
JT  - Life sciences
JID - 0375521
RN  - 0 (Anti-Inflammatory Agents, Non-Steroidal)
RN  - 4P7KIU7003 (olvanil)
RN  - S07O44R1ZM (Capsaicin)
SB  - IM
MH  - Administration, Oral
MH  - Animals
MH  - Anti-Inflammatory Agents, Non-Steroidal/administration & dosage/pharmacokinetics
MH  - Biological Availability
MH  - Capsaicin/administration & dosage/*analogs & 
      derivatives/pharmacokinetics/pharmacology
MH  - Chromatography, High Pressure Liquid
MH  - Injections, Subcutaneous
MH  - Male
MH  - Mice
EDAT- 1988/01/01 00:00
MHDA- 1988/01/01 00:01
CRDT- 1988/01/01 00:00
PHST- 1988/01/01 00:00 [pubmed]
PHST- 1988/01/01 00:01 [medline]
PHST- 1988/01/01 00:00 [entrez]
AID - 0024-3205(88)90305-0 [pii]
AID - 10.1016/0024-3205(88)90305-0 [doi]
PST - ppublish
SO  - Life Sci. 1988;43(17):1385-91. doi: 10.1016/0024-3205(88)90305-0.